Ligand source activities (1 row/activity)





Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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DOI

2274 3173 58 None -10 36 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
4917 3173 58 None -10 36 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
7279 3173 58 None -10 36 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
CHEMBL728 3173 58 None -10 36 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
DB00433 3173 58 None -10 36 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
2470 3653 50 None -38018 23 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
3300 3653 50 None -38018 23 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
5265 3653 50 None -38018 23 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
99 3653 50 None -38018 23 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL267930 3653 50 None -38018 23 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
3081361 93934 123 None 1 14 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 474 5 1 5 4.4 COc1cc2/c(=N/c3ccc(Br)cc3F)nc[nH]c2cc1OCC1CCN(C)CC1 10.1038/s41467-023-40064-9
CHEMBL24828 93934 123 None 1 14 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 474 5 1 5 4.4 COc1cc2/c(=N/c3ccc(Br)cc3F)nc[nH]c2cc1OCC1CCN(C)CC1 10.1038/s41467-023-40064-9
214 3860 58 None -31 28 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
2740 3860 58 None -31 28 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
5566 3860 58 None -31 28 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
66064 3860 58 None -31 28 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL422 3860 58 None -31 28 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
DB00831 3860 58 None -31 28 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
242 470 124 None -97 33 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
34 470 124 None -97 33 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
60795 470 124 None -97 33 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
CHEMBL1112 470 124 None -97 33 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
DB01238 470 124 None -97 33 Human 5.7 pAC50 = 5.7 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
2393 3334 82 None -2041 9 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1038/s41467-023-40064-9
5078 3334 82 None -2041 9 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1038/s41467-023-40064-9
51 3334 82 None -2041 9 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1038/s41467-023-40064-9
CHEMBL905 3334 82 None -2041 9 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1038/s41467-023-40064-9
DB00953 3334 82 None -2041 9 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1038/s41467-023-40064-9
3547 141373 71 None -3 8 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 291 2 1 4 1.2 O=S(=O)(c1cccc2cnccc12)N1CCCNCC1 10.1038/s41467-023-40064-9
CHEMBL38380 141373 71 None -3 8 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 291 2 1 4 1.2 O=S(=O)(c1cccc2cnccc12)N1CCCNCC1 10.1038/s41467-023-40064-9
CHEMBL541388 141373 71 None -3 8 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 291 2 1 4 1.2 O=S(=O)(c1cccc2cnccc12)N1CCCNCC1 10.1038/s41467-023-40064-9
71398 106439 44 None -3235 14 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 302 5 4 4 3.6 C[C@@H](Cc1ccc(O)c(O)c1)[C@H](C)Cc1ccc(O)c(O)c1 10.1038/s41467-023-40064-9
CHEMBL313972 106439 44 None -3235 14 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 302 5 4 4 3.6 C[C@@H](Cc1ccc(O)c(O)c1)[C@H](C)Cc1ccc(O)c(O)c1 10.1038/s41467-023-40064-9
68617 205527 62 None -66 30 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1709 205527 62 None -66 30 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL809 205527 62 None -66 30 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
367 3824 12 None -1548 8 Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
5487427 3824 12 None -1548 8 Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
8592 3824 12 None -1548 8 Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
CHEMBL1900528 3824 12 None -1548 8 Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
CHEMBL3305968 3824 12 None -1548 8 Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
CHEMBL4650755 3824 12 None -1548 8 Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
DB01409 3824 12 None -1548 8 Human 6.6 pAC50 = 6.6 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
168871 89130 14 None -1949 13 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 563 4 3 6 2.1 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C[C@@H]4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 10.1038/s41467-023-40064-9
CHEMBL2365712 89130 14 None -1949 13 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 563 4 3 6 2.1 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C[C@@H]4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 10.1038/s41467-023-40064-9
2771 195017 74 None -25 16 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
CHEMBL1200781 195017 74 None -25 16 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
CHEMBL549 195017 74 None -25 16 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
191 403 98 None -21 36 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
201 403 98 None -21 36 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
2170 403 98 None -21 36 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
CHEMBL1113 403 98 None -21 36 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
DB00543 403 98 None -21 36 Human 6.5 pAC50 = 6.5 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
1400 1957 70 None 1 16 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
3658 1957 70 None 1 16 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
7199 1957 70 None 1 16 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
91513 1957 70 None 1 16 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL896 1957 70 None 1 16 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
DB00557 1957 70 None 1 16 Human 6.4 pAC50 = 6.4 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
146570 43454 67 None 1 7 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 324 5 0 3 3.8 CN(C)CCC[C@@]1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
CHEMBL1508 43454 67 None 1 7 Human 5.3 pAC50 = 5.3 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 324 5 0 3 3.8 CN(C)CCC[C@@]1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
1210 918 51 None -2 22 Human 7.3 pAC50 = 7.3 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
1213 918 51 None -2 22 Human 7.3 pAC50 = 7.3 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
2725 918 51 None -2 22 Human 7.3 pAC50 = 7.3 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
33036 918 51 None -2 22 Human 7.3 pAC50 = 7.3 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
4411 918 51 None -2 22 Human 7.3 pAC50 = 7.3 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
616 918 51 None -2 22 Human 7.3 pAC50 = 7.3 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
6976 918 51 None -2 22 Human 7.3 pAC50 = 7.3 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
716121 918 51 None -2 22 Human 7.3 pAC50 = 7.3 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
CHEMBL1201353 918 51 None -2 22 Human 7.3 pAC50 = 7.3 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
CHEMBL1554789 918 51 None -2 22 Human 7.3 pAC50 = 7.3 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
CHEMBL505 918 51 None -2 22 Human 7.3 pAC50 = 7.3 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
DB01114 918 51 None -2 22 Human 7.3 pAC50 = 7.3 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
DB13679 918 51 None -2 22 Human 7.3 pAC50 = 7.3 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
100 3805 58 None -33 38 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
2637 3805 58 None -33 38 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
5452 3805 58 None -33 38 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
CHEMBL479 3805 58 None -33 38 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
DB00679 3805 58 None -33 38 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
16351 102730 47 None -18 17 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
CHEMBL304902 102730 47 None -18 17 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
213 3853 55 None -79 22 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
2717 3853 55 None -79 22 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
5533 3853 55 None -79 22 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
CHEMBL621 3853 55 None -79 22 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
DB00656 3853 55 None -79 22 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
4640 78266 30 None -9 11 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 379 6 1 4 3.9 COc1cc2[nH]c(C)c(CCN3CCN(c4ccccc4)CC3)c2cc1OC 10.1038/s41467-023-40064-9
CHEMBL2107011 78266 30 None -9 11 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 379 6 1 4 3.9 COc1cc2[nH]c(C)c(CCN3CCN(c4ccccc4)CC3)c2cc1OC 10.1038/s41467-023-40064-9
19861 207523 50 None 3 10 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 290 0 0 2 3.7 CN1CCC(=C2c3ccccc3CCc3cccnc32)CC1 10.1038/s41467-023-40064-9
CHEMBL946 207523 50 None 3 10 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 290 0 0 2 3.7 CN1CCC(=C2c3ccccc3CCc3cccnc32)CC1 10.1038/s41467-023-40064-9
2220 3134 82 None -6 17 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
27400 3134 82 None -6 17 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
93 3134 82 None -6 17 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
CHEMBL294951 3134 82 None -6 17 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
DB06153 3134 82 None -6 17 Human 7.2 pAC50 = 7.2 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
1385580 29276 76 None -18 19 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
4615 29276 76 None -18 19 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL13828 29276 76 None -18 19 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
2470 3653 50 None -38018 23 Human 5.2 pAC50 = 5.2 Functional
Agonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
3300 3653 50 None -38018 23 Human 5.2 pAC50 = 5.2 Functional
Agonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
5265 3653 50 None -38018 23 Human 5.2 pAC50 = 5.2 Functional
Agonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
99 3653 50 None -38018 23 Human 5.2 pAC50 = 5.2 Functional
Agonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL267930 3653 50 None -38018 23 Human 5.2 pAC50 = 5.2 Functional
Agonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
2601 3780 33 None -1288 17 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
443951 3780 33 None -1288 17 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
56 3780 33 None -1288 17 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
CHEMBL73151 3780 33 None -1288 17 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
DB13399 3780 33 None -1288 17 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
2218 15283 23 None -3 12 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 322 8 0 2 4.4 CCN(CC)CCCN(c1ccccc1)C1Cc2ccccc2C1 10.1038/s41467-023-40064-9
CHEMBL1213033 15283 23 None -3 12 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 322 8 0 2 4.4 CCN(CC)CCCN(c1ccccc1)C1Cc2ccccc2C1 10.1038/s41467-023-40064-9
21722 17992 31 None -1 21 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 10.1038/s41467-023-40064-9
CHEMBL126224 17992 31 None -1 21 Human 6.1 pAC50 = 6.1 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 10.1038/s41467-023-40064-9
2247 505 81 None -4 42 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
249 505 81 None -4 42 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
2603 505 81 None -4 42 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
CHEMBL296419 505 81 None -4 42 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
DB00637 505 81 None -4 42 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
2333 142335 97 None -7 14 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 422 3 1 3 5.5 CCc1oc2ccccc2c1C(=O)c1cc(Br)c(O)c(Br)c1 10.1038/s41467-023-40064-9
CHEMBL388590 142335 97 None -7 14 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 422 3 1 3 5.5 CCc1oc2ccccc2c1C(=O)c1cc(Br)c(O)c(Br)c1 10.1038/s41467-023-40064-9
10042467 1426 1 None -1 2 Guinea pig 6.9 pEC50 = 6.9 Functional
Effective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segmentEffective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segment
ChEMBL 333 8 1 2 4.3 CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C 10.1021/jm991056a
1203 1426 1 None -1 2 Guinea pig 6.9 pEC50 = 6.9 Functional
Effective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segmentEffective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segment
ChEMBL 333 8 1 2 4.3 CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C 10.1021/jm991056a
CHEMBL11553 1426 1 None -1 2 Guinea pig 6.9 pEC50 = 6.9 Functional
Effective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segmentEffective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segment
ChEMBL 333 8 1 2 4.3 CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C 10.1021/jm991056a
10689833 12766 0 None -4 2 Rat 5.9 pEC50 = 5.9 Functional
Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619
ChEMBL 359 8 1 2 4.8 c1ccc(C(CCc2nc(CCN3CCCC3)c[nH]2)c2ccccc2)cc1 10.1021/jm991056a
CHEMBL11879 12766 0 None -4 2 Rat 5.9 pEC50 = 5.9 Functional
Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619
ChEMBL 359 8 1 2 4.8 c1ccc(C(CCc2nc(CCN3CCCC3)c[nH]2)c2ccccc2)cc1 10.1021/jm991056a
11791817 98303 0 None -1 2 Guinea pig 6.8 pEC50 = 6.8 Functional
Effective concentration for agonist activity in guinea pig ileum whole segmentEffective concentration for agonist activity in guinea pig ileum whole segment
ChEMBL 345 9 2 2 4.5 c1ccc(C(CCc2nc(CCNC3CC3)c[nH]2)c2ccccc2)cc1 10.1021/jm991056a
CHEMBL274831 98303 0 None -1 2 Guinea pig 6.8 pEC50 = 6.8 Functional
Effective concentration for agonist activity in guinea pig ileum whole segmentEffective concentration for agonist activity in guinea pig ileum whole segment
ChEMBL 345 9 2 2 4.5 c1ccc(C(CCc2nc(CCNC3CC3)c[nH]2)c2ccccc2)cc1 10.1021/jm991056a
10403687 2511 3 None -1 2 Rat 6.8 pEC50 = 6.8 Functional
Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
1205 2511 3 None -1 2 Rat 6.8 pEC50 = 6.8 Functional
Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
CHEMBL275035 2511 3 None -1 2 Rat 6.8 pEC50 = 6.8 Functional
Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
1269 121 41 None -354 6 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assayAgonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assay
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1021/jm900526h
37463 121 41 None -354 6 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assayAgonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assay
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1021/jm900526h
CHEMBL275443 121 41 None -354 6 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assayAgonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assay
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1021/jm900526h
126688 404 33 None -57 2 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay
ChEMBL 157 2 2 4 0.5 NCCc1sc(nc1C)N 10.1016/j.bmcl.2010.10.041
4025 404 33 None -57 2 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay
ChEMBL 157 2 2 4 0.5 NCCc1sc(nc1C)N 10.1016/j.bmcl.2010.10.041
CHEMBL293762 404 33 None -57 2 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay
ChEMBL 157 2 2 4 0.5 NCCc1sc(nc1C)N 10.1016/j.bmcl.2010.10.041
11617365 74275 0 None - 1 Guinea pig 5.8 pEC50 = 5.8 Functional
Agonist activity at histamine H1 receptor in guinea pig ileumAgonist activity at histamine H1 receptor in guinea pig ileum
ChEMBL 319 7 2 3 3.3 NCCc1c[nH]c(C(=O)CC(c2ccccc2)c2ccccc2)n1 10.1016/j.bmcl.2005.10.030
CHEMBL202371 74275 0 None - 1 Guinea pig 5.8 pEC50 = 5.8 Functional
Agonist activity at histamine H1 receptor in guinea pig ileumAgonist activity at histamine H1 receptor in guinea pig ileum
ChEMBL 319 7 2 3 3.3 NCCc1c[nH]c(C(=O)CC(c2ccccc2)c2ccccc2)n1 10.1016/j.bmcl.2005.10.030
10042467 1426 1 None 1 2 Rat 6.8 pEC50 = 6.8 Functional
Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619
ChEMBL 333 8 1 2 4.3 CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C 10.1021/jm991056a
1203 1426 1 None 1 2 Rat 6.8 pEC50 = 6.8 Functional
Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619
ChEMBL 333 8 1 2 4.3 CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C 10.1021/jm991056a
CHEMBL11553 1426 1 None 1 2 Rat 6.8 pEC50 = 6.8 Functional
Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619
ChEMBL 333 8 1 2 4.3 CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C 10.1021/jm991056a
10447834 1933 4 None 2 3 Guinea pig 6.7 pEC50 = 6.7 Functional
Effective concentration for agonist activity in guinea pig ileum whole segmentEffective concentration for agonist activity in guinea pig ileum whole segment
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
4026 1933 4 None 2 3 Guinea pig 6.7 pEC50 = 6.7 Functional
Effective concentration for agonist activity in guinea pig ileum whole segmentEffective concentration for agonist activity in guinea pig ileum whole segment
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
CHEMBL275507 1933 4 None 2 3 Guinea pig 6.7 pEC50 = 6.7 Functional
Effective concentration for agonist activity in guinea pig ileum whole segmentEffective concentration for agonist activity in guinea pig ileum whole segment
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
1204 1932 119 None -4 10 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assayAgonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
1247 1932 119 None -4 10 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assayAgonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
1375 1932 119 None -4 10 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assayAgonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
774 1932 119 None -4 10 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assayAgonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
CHEMBL90 1932 119 None -4 10 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assayAgonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
DB05381 1932 119 None -4 10 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assayAgonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
10447834 1933 4 None 2 3 Guinea pig 5.7 pEC50 = 5.7 Functional
Effective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segmentEffective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segment
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
4026 1933 4 None 2 3 Guinea pig 5.7 pEC50 = 5.7 Functional
Effective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segmentEffective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segment
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
CHEMBL275507 1933 4 None 2 3 Guinea pig 5.7 pEC50 = 5.7 Functional
Effective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segmentEffective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segment
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
1204 1932 119 None -3 10 Guinea pig 6.7 pEC50 = 6.7 Functional
Agonist activity at histamine H1 receptor in guinea pig ileumAgonist activity at histamine H1 receptor in guinea pig ileum
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2005.10.030
1247 1932 119 None -3 10 Guinea pig 6.7 pEC50 = 6.7 Functional
Agonist activity at histamine H1 receptor in guinea pig ileumAgonist activity at histamine H1 receptor in guinea pig ileum
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2005.10.030
1375 1932 119 None -3 10 Guinea pig 6.7 pEC50 = 6.7 Functional
Agonist activity at histamine H1 receptor in guinea pig ileumAgonist activity at histamine H1 receptor in guinea pig ileum
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2005.10.030
774 1932 119 None -3 10 Guinea pig 6.7 pEC50 = 6.7 Functional
Agonist activity at histamine H1 receptor in guinea pig ileumAgonist activity at histamine H1 receptor in guinea pig ileum
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2005.10.030
CHEMBL90 1932 119 None -3 10 Guinea pig 6.7 pEC50 = 6.7 Functional
Agonist activity at histamine H1 receptor in guinea pig ileumAgonist activity at histamine H1 receptor in guinea pig ileum
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2005.10.030
DB05381 1932 119 None -3 10 Guinea pig 6.7 pEC50 = 6.7 Functional
Agonist activity at histamine H1 receptor in guinea pig ileumAgonist activity at histamine H1 receptor in guinea pig ileum
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2005.10.030
1194 45 3 None 50 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay
ChEMBL 265 3 2 2 2.3 NCCc1cnc([nH]1)c1cccc(c1)Br 10.1016/j.bmcl.2010.10.041
23786499 45 3 None 50 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay
ChEMBL 265 3 2 2 2.3 NCCc1cnc([nH]1)c1cccc(c1)Br 10.1016/j.bmcl.2010.10.041
CHEMBL26116 45 3 None 50 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay
ChEMBL 265 3 2 2 2.3 NCCc1cnc([nH]1)c1cccc(c1)Br 10.1016/j.bmcl.2010.10.041
1204 1932 119 None -4 10 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1247 1932 119 None -4 10 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1375 1932 119 None -4 10 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
774 1932 119 None -4 10 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL90 1932 119 None -4 10 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
DB05381 1932 119 None -4 10 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
11791817 98303 0 None -1 2 Guinea pig 5.6 pEC50 = 5.6 Functional
Effective concentration for agonism activity in endothelium-denuded guinea pig aortic segmentEffective concentration for agonism activity in endothelium-denuded guinea pig aortic segment
ChEMBL 345 9 2 2 4.5 c1ccc(C(CCc2nc(CCNC3CC3)c[nH]2)c2ccccc2)cc1 10.1021/jm991056a
CHEMBL274831 98303 0 None -1 2 Guinea pig 5.6 pEC50 = 5.6 Functional
Effective concentration for agonism activity in endothelium-denuded guinea pig aortic segmentEffective concentration for agonism activity in endothelium-denuded guinea pig aortic segment
ChEMBL 345 9 2 2 4.5 c1ccc(C(CCc2nc(CCNC3CC3)c[nH]2)c2ccccc2)cc1 10.1021/jm991056a
5310982 93612 4 None 3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay
ChEMBL 255 3 2 2 2.6 NCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1 10.1016/j.bmcl.2010.10.041
CHEMBL24665 93612 4 None 3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay
ChEMBL 255 3 2 2 2.6 NCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1 10.1016/j.bmcl.2010.10.041
44267376 10221 1 None - 1 Guinea pig 5.6 pEC50 = 5.6 Functional
Effective concentration for agonist activity in guinea pig ileum whole segmentEffective concentration for agonist activity in guinea pig ileum whole segment
ChEMBL 277 5 2 2 3.1 NCCc1c[nH]c(C(c2ccccc2)c2ccccc2)n1 10.1021/jm991056a
CHEMBL11603 10221 1 None - 1 Guinea pig 5.6 pEC50 = 5.6 Functional
Effective concentration for agonist activity in guinea pig ileum whole segmentEffective concentration for agonist activity in guinea pig ileum whole segment
ChEMBL 277 5 2 2 3.1 NCCc1c[nH]c(C(c2ccccc2)c2ccccc2)n1 10.1021/jm991056a
10689833 12766 0 None 4 2 Guinea pig 6.5 pEC50 = 6.5 Functional
Effective concentration for agonist activity in guinea pig ileum whole segmentEffective concentration for agonist activity in guinea pig ileum whole segment
ChEMBL 359 8 1 2 4.8 c1ccc(C(CCc2nc(CCN3CCCC3)c[nH]2)c2ccccc2)cc1 10.1021/jm991056a
CHEMBL11879 12766 0 None 4 2 Guinea pig 6.5 pEC50 = 6.5 Functional
Effective concentration for agonist activity in guinea pig ileum whole segmentEffective concentration for agonist activity in guinea pig ileum whole segment
ChEMBL 359 8 1 2 4.8 c1ccc(C(CCc2nc(CCN3CCCC3)c[nH]2)c2ccccc2)cc1 10.1021/jm991056a
10688111 10040 1 None 2 2 Guinea pig 6.5 pEC50 = 6.5 Functional
Effective concentration for agonist activity in guinea pig ileum whole segmentEffective concentration for agonist activity in guinea pig ileum whole segment
ChEMBL 333 9 2 2 4.3 CCNCCc1c[nH]c(CCC(c2ccccc2)c2ccccc2)n1 10.1021/jm991056a
CHEMBL11515 10040 1 None 2 2 Guinea pig 6.5 pEC50 = 6.5 Functional
Effective concentration for agonist activity in guinea pig ileum whole segmentEffective concentration for agonist activity in guinea pig ileum whole segment
ChEMBL 333 9 2 2 4.3 CCNCCc1c[nH]c(CCC(c2ccccc2)c2ccccc2)n1 10.1021/jm991056a
10447834 1933 4 None 2 3 Guinea pig 6.5 pEC50 = 6.5 Functional
Effective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segmentEffective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segment
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
4026 1933 4 None 2 3 Guinea pig 6.5 pEC50 = 6.5 Functional
Effective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segmentEffective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segment
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
CHEMBL275507 1933 4 None 2 3 Guinea pig 6.5 pEC50 = 6.5 Functional
Effective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segmentEffective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segment
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
11791817 98303 0 None 1 2 Rat 6.5 pEC50 = 6.5 Functional
Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619
ChEMBL 345 9 2 2 4.5 c1ccc(C(CCc2nc(CCNC3CC3)c[nH]2)c2ccccc2)cc1 10.1021/jm991056a
CHEMBL274831 98303 0 None 1 2 Rat 6.5 pEC50 = 6.5 Functional
Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619
ChEMBL 345 9 2 2 4.5 c1ccc(C(CCc2nc(CCNC3CC3)c[nH]2)c2ccccc2)cc1 10.1021/jm991056a
10685002 10160 0 None - 1 Guinea pig 4.4 pEC50 = 4.4 Functional
Effective concentration for agonist activity in guinea pig ileum whole segmentEffective concentration for agonist activity in guinea pig ileum whole segment
ChEMBL 291 6 2 2 3.3 NCCc1c[nH]c(CC(c2ccccc2)c2ccccc2)n1 10.1021/jm991056a
CHEMBL11584 10160 0 None - 1 Guinea pig 4.4 pEC50 = 4.4 Functional
Effective concentration for agonist activity in guinea pig ileum whole segmentEffective concentration for agonist activity in guinea pig ileum whole segment
ChEMBL 291 6 2 2 3.3 NCCc1c[nH]c(CC(c2ccccc2)c2ccccc2)n1 10.1021/jm991056a
1204 1932 119 None -4 10 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human H1 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H1 receptor expressed in 293-EBNA cells by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0603318
1247 1932 119 None -4 10 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human H1 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H1 receptor expressed in 293-EBNA cells by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0603318
1375 1932 119 None -4 10 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human H1 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H1 receptor expressed in 293-EBNA cells by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0603318
774 1932 119 None -4 10 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human H1 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H1 receptor expressed in 293-EBNA cells by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0603318
CHEMBL90 1932 119 None -4 10 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human H1 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H1 receptor expressed in 293-EBNA cells by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0603318
DB05381 1932 119 None -4 10 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human H1 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H1 receptor expressed in 293-EBNA cells by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0603318
10403687 2511 3 None 1 2 Guinea pig 6.3 pEC50 = 6.3 Functional
Effective concentration for agonism activity in endothelium-denuded guinea pig aortic segmentEffective concentration for agonism activity in endothelium-denuded guinea pig aortic segment
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
1205 2511 3 None 1 2 Guinea pig 6.3 pEC50 = 6.3 Functional
Effective concentration for agonism activity in endothelium-denuded guinea pig aortic segmentEffective concentration for agonism activity in endothelium-denuded guinea pig aortic segment
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
CHEMBL275035 2511 3 None 1 2 Guinea pig 6.3 pEC50 = 6.3 Functional
Effective concentration for agonism activity in endothelium-denuded guinea pig aortic segmentEffective concentration for agonism activity in endothelium-denuded guinea pig aortic segment
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
10403687 2511 3 None 1 2 Guinea pig 7.2 pEC50 = 7.2 Functional
Effective concentration for agonist activity in guinea pig ileum whole segmentEffective concentration for agonist activity in guinea pig ileum whole segment
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
1205 2511 3 None 1 2 Guinea pig 7.2 pEC50 = 7.2 Functional
Effective concentration for agonist activity in guinea pig ileum whole segmentEffective concentration for agonist activity in guinea pig ileum whole segment
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
CHEMBL275035 2511 3 None 1 2 Guinea pig 7.2 pEC50 = 7.2 Functional
Effective concentration for agonist activity in guinea pig ileum whole segmentEffective concentration for agonist activity in guinea pig ileum whole segment
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
11846300 80266 3 None 2 2 Human 8.2 pEC50 = 8.2 Functional
Activity at human histamine H1 receptor transfected in COS7 cells by NF-kappaB luciferase reporter assayActivity at human histamine H1 receptor transfected in COS7 cells by NF-kappaB luciferase reporter assay
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm051008s
CHEMBL213912 80266 3 None 2 2 Human 8.2 pEC50 = 8.2 Functional
Activity at human histamine H1 receptor transfected in COS7 cells by NF-kappaB luciferase reporter assayActivity at human histamine H1 receptor transfected in COS7 cells by NF-kappaB luciferase reporter assay
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm051008s
10688111 10040 1 None -2 2 Rat 6.2 pEC50 = 6.2 Functional
Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619
ChEMBL 333 9 2 2 4.3 CCNCCc1c[nH]c(CCC(c2ccccc2)c2ccccc2)n1 10.1021/jm991056a
CHEMBL11515 10040 1 None -2 2 Rat 6.2 pEC50 = 6.2 Functional
Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619
ChEMBL 333 9 2 2 4.3 CCNCCc1c[nH]c(CCC(c2ccccc2)c2ccccc2)n1 10.1021/jm991056a
10403687 2511 3 None 1 2 Guinea pig 7.1 pEC50 = 7.1 Functional
Effective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segmentEffective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segment
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
1205 2511 3 None 1 2 Guinea pig 7.1 pEC50 = 7.1 Functional
Effective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segmentEffective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segment
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
CHEMBL275035 2511 3 None 1 2 Guinea pig 7.1 pEC50 = 7.1 Functional
Effective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segmentEffective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segment
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
91613 17987 34 None 5 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay
ChEMBL 125 2 2 2 0.2 Cc1ncc(CCN)[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL12620 17987 34 None 5 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay
ChEMBL 125 2 2 2 0.2 Cc1ncc(CCN)[nH]1 10.1016/j.bmcl.2010.10.041
10042467 1426 1 None -1 2 Guinea pig 7.1 pEC50 = 7.1 Functional
Effective concentration for agonist activity in guinea pig ileum whole segmentEffective concentration for agonist activity in guinea pig ileum whole segment
ChEMBL 333 8 1 2 4.3 CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C 10.1021/jm991056a
1203 1426 1 None -1 2 Guinea pig 7.1 pEC50 = 7.1 Functional
Effective concentration for agonist activity in guinea pig ileum whole segmentEffective concentration for agonist activity in guinea pig ileum whole segment
ChEMBL 333 8 1 2 4.3 CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C 10.1021/jm991056a
CHEMBL11553 1426 1 None -1 2 Guinea pig 7.1 pEC50 = 7.1 Functional
Effective concentration for agonist activity in guinea pig ileum whole segmentEffective concentration for agonist activity in guinea pig ileum whole segment
ChEMBL 333 8 1 2 4.3 CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C 10.1021/jm991056a
10042467 1426 1 None -1 2 Guinea pig 6.1 pEC50 = 6.1 Functional
Effective concentration for agonism activity in endothelium-denuded guinea pig aortic segmentEffective concentration for agonism activity in endothelium-denuded guinea pig aortic segment
ChEMBL 333 8 1 2 4.3 CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C 10.1021/jm991056a
1203 1426 1 None -1 2 Guinea pig 6.1 pEC50 = 6.1 Functional
Effective concentration for agonism activity in endothelium-denuded guinea pig aortic segmentEffective concentration for agonism activity in endothelium-denuded guinea pig aortic segment
ChEMBL 333 8 1 2 4.3 CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C 10.1021/jm991056a
CHEMBL11553 1426 1 None -1 2 Guinea pig 6.1 pEC50 = 6.1 Functional
Effective concentration for agonism activity in endothelium-denuded guinea pig aortic segmentEffective concentration for agonism activity in endothelium-denuded guinea pig aortic segment
ChEMBL 333 8 1 2 4.3 CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C 10.1021/jm991056a
10447834 1933 4 None -2 3 Rat 6.1 pEC50 = 6.1 Functional
Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
4026 1933 4 None -2 3 Rat 6.1 pEC50 = 6.1 Functional
Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
CHEMBL275507 1933 4 None -2 3 Rat 6.1 pEC50 = 6.1 Functional
Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
11976 920 59 None -9 16 Human 9.0 pIC50 = 9 Functional
Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1021/jm300671m
667467 920 59 None -9 16 Human 9.0 pIC50 = 9 Functional
Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1021/jm300671m
CHEMBL908 920 59 None -9 16 Human 9.0 pIC50 = 9 Functional
Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1021/jm300671m
DB01239 920 59 None -9 16 Human 9.0 pIC50 = 9 Functional
Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1021/jm300671m
13623342 64347 0 None - 1 Guinea pig 8.0 pIC50 = 8 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 286 5 0 5 1.9 C=COCCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
CHEMBL18123 64347 0 None - 1 Guinea pig 8.0 pIC50 = 8 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 286 5 0 5 1.9 C=COCCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
3071006 65015 1 None - 1 Guinea pig 8.0 pIC50 = 8 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 314 6 0 5 2.4 C=CCOCCn1c(N2CCCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
CHEMBL18233 65015 1 None - 1 Guinea pig 8.0 pIC50 = 8 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 314 6 0 5 2.4 C=CCOCCn1c(N2CCCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
13623366 66714 0 None - 1 Guinea pig 8.0 pIC50 = 8 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 330 7 0 5 3.0 CCCCOCCn1c(N2CCCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
CHEMBL18561 66714 0 None - 1 Guinea pig 8.0 pIC50 = 8 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 330 7 0 5 3.0 CCCCOCCn1c(N2CCCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
3071004 167760 5 None - 1 Guinea pig 8.0 pIC50 = 8 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 288 5 0 5 1.8 CCOCCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
CHEMBL430338 167760 5 None - 1 Guinea pig 8.0 pIC50 = 8 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 288 5 0 5 1.8 CCOCCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
1227 2489 43 None 2 14 Human 8.0 pIC50 = 8 Functional
Inverse agonist activity at human wild-type histamine H1 receptor assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assayInverse agonist activity at human wild-type histamine H1 receptor assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assay
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1038/nchembio714
2331 2489 43 None 2 14 Human 8.0 pIC50 = 8 Functional
Inverse agonist activity at human wild-type histamine H1 receptor assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assayInverse agonist activity at human wild-type histamine H1 receptor assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assay
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1038/nchembio714
3957 2489 43 None 2 14 Human 8.0 pIC50 = 8 Functional
Inverse agonist activity at human wild-type histamine H1 receptor assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assayInverse agonist activity at human wild-type histamine H1 receptor assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assay
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1038/nchembio714
4992 2489 43 None 2 14 Human 8.0 pIC50 = 8 Functional
Inverse agonist activity at human wild-type histamine H1 receptor assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assayInverse agonist activity at human wild-type histamine H1 receptor assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assay
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1038/nchembio714
CHEMBL511 2489 43 None 2 14 Human 8.0 pIC50 = 8 Functional
Inverse agonist activity at human wild-type histamine H1 receptor assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assayInverse agonist activity at human wild-type histamine H1 receptor assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assay
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1038/nchembio714
DB06691 2489 43 None 2 14 Human 8.0 pIC50 = 8 Functional
Inverse agonist activity at human wild-type histamine H1 receptor assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assayInverse agonist activity at human wild-type histamine H1 receptor assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assay
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1038/nchembio714
44458944 99060 0 None - 1 Guinea pig 8.0 pIC50 = 8.0 Functional
In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum
ChEMBL 337 3 0 1 5.5 c1ccc(CN2CCC3C(=C(c4ccccc4)c4ccccc43)C2)cc1 10.1016/s0960-894x(00)00199-2
CHEMBL280432 99060 0 None - 1 Guinea pig 8.0 pIC50 = 8.0 Functional
In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum
ChEMBL 337 3 0 1 5.5 c1ccc(CN2CCC3C(=C(c4ccccc4)c4ccccc43)C2)cc1 10.1016/s0960-894x(00)00199-2
44224259 62723 5 None 30 2 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 291 3 0 3 3.3 CN1CCc2c(c3ccccc3n2CCc2cccnc2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783959 62723 5 None 30 2 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 291 3 0 3 3.3 CN1CCc2c(c3ccccc3n2CCc2cccnc2)C1 10.1016/j.bmcl.2009.04.128
3529324 208354 1 None - 1 Guinea pig 6.0 pIC50 = 6 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 306 6 0 3 3.3 CC(C)c1ccc(C2SCC(=O)N2CCCN(C)C)cc1 10.1021/jm00093a025
CHEMBL1202934 208354 1 None - 1 Guinea pig 6.0 pIC50 = 6 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 306 6 0 3 3.3 CC(C)c1ccc(C2SCC(=O)N2CCCN(C)C)cc1 10.1021/jm00093a025
CHEMBL99417 208354 1 None - 1 Guinea pig 6.0 pIC50 = 6 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 306 6 0 3 3.3 CC(C)c1ccc(C2SCC(=O)N2CCCN(C)C)cc1 10.1021/jm00093a025
44126329 62718 6 None -2 2 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay
ChEMBL 305 3 0 3 3.6 Cc1ccc2c(c1)c1c(n2CCc2ccccn2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783954 62718 6 None -2 2 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay
ChEMBL 305 3 0 3 3.6 Cc1ccc2c(c1)c1c(n2CCc2ccccn2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
153996 112668 2 None -57 6 Human 5.0 pIC50 = 5 Functional
Compound was evaluated for the antagonistic activity against H1 receptorCompound was evaluated for the antagonistic activity against H1 receptor
ChEMBL 639 10 1 6 5.7 COc1cc(C(=O)N2CC[C@](CCN3CCC(C(N)=O)(c4ccccc4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10097-X
CHEMBL330366 112668 2 None -57 6 Human 5.0 pIC50 = 5 Functional
Compound was evaluated for the antagonistic activity against H1 receptorCompound was evaluated for the antagonistic activity against H1 receptor
ChEMBL 639 10 1 6 5.7 COc1cc(C(=O)N2CC[C@](CCN3CCC(C(N)=O)(c4ccccc4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10097-X
CHEMBL539021 112668 2 None -57 6 Human 5.0 pIC50 = 5 Functional
Compound was evaluated for the antagonistic activity against H1 receptorCompound was evaluated for the antagonistic activity against H1 receptor
ChEMBL 639 10 1 6 5.7 COc1cc(C(=O)N2CC[C@](CCN3CCC(C(N)=O)(c4ccccc4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10097-X
44126270 199151 6 None 10 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge
ChEMBL 320 4 0 3 3.9 COc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL589389 199151 6 None 10 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge
ChEMBL 320 4 0 3 3.9 COc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
3071008 98749 2 None - 1 Guinea pig 8.0 pIC50 = 8.0 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 274 5 1 5 1.5 CCOCCn1c(N2CCNCC2)nc2ccccc21 10.1021/jm00157a010
CHEMBL278053 98749 2 None - 1 Guinea pig 8.0 pIC50 = 8.0 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 274 5 1 5 1.5 CCOCCn1c(N2CCNCC2)nc2ccccc21 10.1021/jm00157a010
54585846 62727 5 None 38 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 323 3 0 3 3.7 Cc1ccc(CCn2c3c(c4cc(F)ccc42)CN(C)CC3)cn1 10.1016/j.bmcl.2009.04.128
CHEMBL1783963 62727 5 None 38 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 323 3 0 3 3.7 Cc1ccc(CCn2c3c(c4cc(F)ccc42)CN(C)CC3)cn1 10.1016/j.bmcl.2009.04.128
44126269 201484 5 None 2 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge
ChEMBL 318 3 0 2 4.5 Cc1ccc(CCn2c3c(c4cc(C)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
CHEMBL605081 201484 5 None 2 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge
ChEMBL 318 3 0 2 4.5 Cc1ccc(CCn2c3c(c4cc(C)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
1210 918 51 None 2 22 Guinea pig 7.9 pIC50 = 7.9 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm00157a010
1213 918 51 None 2 22 Guinea pig 7.9 pIC50 = 7.9 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm00157a010
2725 918 51 None 2 22 Guinea pig 7.9 pIC50 = 7.9 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm00157a010
33036 918 51 None 2 22 Guinea pig 7.9 pIC50 = 7.9 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm00157a010
4411 918 51 None 2 22 Guinea pig 7.9 pIC50 = 7.9 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm00157a010
616 918 51 None 2 22 Guinea pig 7.9 pIC50 = 7.9 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm00157a010
6976 918 51 None 2 22 Guinea pig 7.9 pIC50 = 7.9 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm00157a010
716121 918 51 None 2 22 Guinea pig 7.9 pIC50 = 7.9 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm00157a010
CHEMBL1201353 918 51 None 2 22 Guinea pig 7.9 pIC50 = 7.9 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm00157a010
CHEMBL1554789 918 51 None 2 22 Guinea pig 7.9 pIC50 = 7.9 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm00157a010
CHEMBL505 918 51 None 2 22 Guinea pig 7.9 pIC50 = 7.9 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm00157a010
DB01114 918 51 None 2 22 Guinea pig 7.9 pIC50 = 7.9 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm00157a010
DB13679 918 51 None 2 22 Guinea pig 7.9 pIC50 = 7.9 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm00157a010
3071000 98656 1 None - 1 Guinea pig 7.9 pIC50 = 7.9 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 298 5 0 5 1.4 C#CCOCCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
CHEMBL277311 98656 1 None - 1 Guinea pig 7.9 pIC50 = 7.9 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 298 5 0 5 1.4 C#CCOCCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
54582939 62721 6 None 8 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 369 3 0 3 4.0 CN1CCc2c(c3cc(Br)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783957 62721 6 None 8 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 369 3 0 3 4.0 CN1CCc2c(c3cc(Br)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
54579957 62728 5 None 36 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 291 3 0 3 3.3 CN1CCc2c(c3ccccc3n2CCc2ccncc2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783964 62728 5 None 36 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 291 3 0 3 3.3 CN1CCc2c(c3ccccc3n2CCc2ccncc2)C1 10.1016/j.bmcl.2009.04.128
54580942 62731 9 None 13 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 309 3 0 3 3.4 CN1CCc2c(c3cc(F)ccc3n2CCc2ccncc2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783967 62731 9 None 13 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 309 3 0 3 3.4 CN1CCc2c(c3cc(F)ccc3n2CCc2ccncc2)C1 10.1016/j.bmcl.2009.04.128
4440380 4255 3 None - 1 Guinea pig 5.9 pIC50 = 5.9 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 278 5 0 3 2.5 Cc1ccc(C2SCC(=O)N2CCCN(C)C)cc1 10.1021/jm00093a025
CHEMBL100487 4255 3 None - 1 Guinea pig 5.9 pIC50 = 5.9 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 278 5 0 3 2.5 Cc1ccc(C2SCC(=O)N2CCCN(C)C)cc1 10.1021/jm00093a025
CHEMBL1202938 4255 3 None - 1 Guinea pig 5.9 pIC50 = 5.9 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 278 5 0 3 2.5 Cc1ccc(C2SCC(=O)N2CCCN(C)C)cc1 10.1021/jm00093a025
10234086 111634 0 None -6 2 Human 5.9 pIC50 = 5.9 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 744 13 0 10 6.7 COC(=O)c1ccc(Cn2c(C(=O)C3CCN(CCC4(c5ccccc5)CCN(C(=O)c5cc(OC)c(OC)c(OC)c5)C4)CC3)nc3ccccc32)cc1 10.1016/S0960-894X(97)10097-X
CHEMBL328511 111634 0 None -6 2 Human 5.9 pIC50 = 5.9 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 744 13 0 10 6.7 COC(=O)c1ccc(Cn2c(C(=O)C3CCN(CCC4(c5ccccc5)CCN(C(=O)c5cc(OC)c(OC)c(OC)c5)C4)CC3)nc3ccccc32)cc1 10.1016/S0960-894X(97)10097-X
10190770 208015 0 None -1 2 Human 6.9 pIC50 = 6.9 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 772 12 0 8 8.3 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10097-X
CHEMBL330430 208015 0 None -1 2 Human 6.9 pIC50 = 6.9 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 772 12 0 8 8.3 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10097-X
CHEMBL97357 208015 0 None -1 2 Human 6.9 pIC50 = 6.9 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 772 12 0 8 8.3 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10097-X
54585848 62734 6 None 5 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 316 3 0 4 3.1 CN1CCc2c(c3cc(C#N)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783971 62734 6 None 5 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 316 3 0 4 3.1 CN1CCc2c(c3cc(C#N)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
13623354 98980 0 None - 1 Guinea pig 7.9 pIC50 = 7.9 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 274 4 0 5 1.4 COCCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
CHEMBL279872 98980 0 None - 1 Guinea pig 7.9 pIC50 = 7.9 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 274 4 0 5 1.4 COCCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
46225000 199115 5 None 9 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challenge
ChEMBL 308 3 0 2 4.0 CN1CCc2c(c3cc(F)ccc3n2CCc2ccccc2)C1 10.1016/j.bmcl.2009.11.037
CHEMBL589148 199115 5 None 9 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challenge
ChEMBL 308 3 0 2 4.0 CN1CCc2c(c3cc(F)ccc3n2CCc2ccccc2)C1 10.1016/j.bmcl.2009.11.037
13623347 61054 0 None - 1 Guinea pig 5.9 pIC50 = 5.9 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 286 4 0 4 3.1 CCCC(C)n1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
CHEMBL17635 61054 0 None - 1 Guinea pig 5.9 pIC50 = 5.9 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 286 4 0 4 3.1 CCCC(C)n1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
13623346 98945 0 None - 1 Guinea pig 5.9 pIC50 = 5.9 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 286 4 0 4 2.8 CC(C)CCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
CHEMBL279621 98945 0 None - 1 Guinea pig 5.9 pIC50 = 5.9 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 286 4 0 4 2.8 CC(C)CCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
42631003 199618 13 None 2 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challenge
ChEMBL 304 3 0 2 4.2 Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL592752 199618 13 None 2 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challenge
ChEMBL 304 3 0 2 4.2 Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
13623371 65205 0 None - 1 Guinea pig 7.8 pIC50 = 7.8 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 378 7 0 5 3.8 CCOCCn1c(N2CCCN(Cc3ccccc3)CC2)nc2ccccc21 10.1021/jm00157a010
CHEMBL18255 65205 0 None - 1 Guinea pig 7.8 pIC50 = 7.8 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 378 7 0 5 3.8 CCOCCn1c(N2CCCN(Cc3ccccc3)CC2)nc2ccccc21 10.1021/jm00157a010
13623360 98808 0 None - 1 Guinea pig 7.8 pIC50 = 7.8 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 330 8 0 5 3.0 CCCCN1CCN(c2nc3ccccc3n2CCOCC)CC1 10.1021/jm00157a010
CHEMBL278504 98808 0 None - 1 Guinea pig 7.8 pIC50 = 7.8 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 330 8 0 5 3.0 CCCCN1CCN(c2nc3ccccc3n2CCOCC)CC1 10.1021/jm00157a010
13623338 63348 0 None - 1 Guinea pig 6.8 pIC50 = 6.8 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 314 7 0 4 3.8 CCCCCCCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
CHEMBL17946 63348 0 None - 1 Guinea pig 6.8 pIC50 = 6.8 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 314 7 0 4 3.8 CCCCCCCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
46224879 201547 3 None -1 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challenge
ChEMBL 302 2 0 2 4.6 Cc1ccc2c(c1)c1c(n2/C=C\c2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL605405 201547 3 None -1 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challenge
ChEMBL 302 2 0 2 4.6 Cc1ccc2c(c1)c1c(n2/C=C\c2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
9832306 112724 0 None 2 2 Human 6.8 pIC50 = 6.8 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 806 17 0 10 8.2 CCOc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(OC)c(OC)c3)C2)cc(OCC)c1OCC 10.1016/S0960-894X(97)10097-X
CHEMBL330367 112724 0 None 2 2 Human 6.8 pIC50 = 6.8 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 806 17 0 10 8.2 CCOc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(OC)c(OC)c3)C2)cc(OCC)c1OCC 10.1016/S0960-894X(97)10097-X
CHEMBL330462 112724 0 None 2 2 Human 6.8 pIC50 = 6.8 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 806 17 0 10 8.2 CCOc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(OC)c(OC)c3)C2)cc(OCC)c1OCC 10.1016/S0960-894X(97)10097-X
197033 199152 64 None 1 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL589390 199152 64 None 1 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
1227 2489 43 None 2 14 Human 6.8 pIC50 = 6.8 Functional
Inverse agonist activity at human wild-type histamine H1 receptor N7.45L mutant assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assayInverse agonist activity at human wild-type histamine H1 receptor N7.45L mutant assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assay
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1038/nchembio714
2331 2489 43 None 2 14 Human 6.8 pIC50 = 6.8 Functional
Inverse agonist activity at human wild-type histamine H1 receptor N7.45L mutant assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assayInverse agonist activity at human wild-type histamine H1 receptor N7.45L mutant assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assay
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1038/nchembio714
3957 2489 43 None 2 14 Human 6.8 pIC50 = 6.8 Functional
Inverse agonist activity at human wild-type histamine H1 receptor N7.45L mutant assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assayInverse agonist activity at human wild-type histamine H1 receptor N7.45L mutant assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assay
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1038/nchembio714
4992 2489 43 None 2 14 Human 6.8 pIC50 = 6.8 Functional
Inverse agonist activity at human wild-type histamine H1 receptor N7.45L mutant assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assayInverse agonist activity at human wild-type histamine H1 receptor N7.45L mutant assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assay
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1038/nchembio714
CHEMBL511 2489 43 None 2 14 Human 6.8 pIC50 = 6.8 Functional
Inverse agonist activity at human wild-type histamine H1 receptor N7.45L mutant assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assayInverse agonist activity at human wild-type histamine H1 receptor N7.45L mutant assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assay
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1038/nchembio714
DB06691 2489 43 None 2 14 Human 6.8 pIC50 = 6.8 Functional
Inverse agonist activity at human wild-type histamine H1 receptor N7.45L mutant assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assayInverse agonist activity at human wild-type histamine H1 receptor N7.45L mutant assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assay
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1038/nchembio714
197033 199152 64 None 1 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challenge
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL589390 199152 64 None 1 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challenge
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
197033 199152 64 None 1 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
CHEMBL589390 199152 64 None 1 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
54582940 62722 5 None 1 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay
ChEMBL 359 3 0 3 4.3 CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783958 62722 5 None 1 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay
ChEMBL 359 3 0 3 4.3 CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
13623367 60379 0 None - 1 Guinea pig 7.8 pIC50 = 7.8 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 316 6 0 5 2.6 CCOCCn1c(N2CCCN(CC)CC2)nc2ccccc21 10.1021/jm00157a010
CHEMBL17474 60379 0 None - 1 Guinea pig 7.8 pIC50 = 7.8 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 316 6 0 5 2.6 CCOCCn1c(N2CCCN(CC)CC2)nc2ccccc21 10.1021/jm00157a010
13623359 64562 1 None - 1 Guinea pig 7.8 pIC50 = 7.8 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 316 7 0 5 2.6 CCCN1CCN(c2nc3ccccc3n2CCOCC)CC1 10.1021/jm00157a010
CHEMBL18151 64562 1 None - 1 Guinea pig 7.8 pIC50 = 7.8 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 316 7 0 5 2.6 CCCN1CCN(c2nc3ccccc3n2CCOCC)CC1 10.1021/jm00157a010
3071032 65039 1 None - 1 Guinea pig 7.8 pIC50 = 7.8 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 316 6 0 5 2.6 CCCOCCn1c(N2CCCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
CHEMBL18234 65039 1 None - 1 Guinea pig 7.8 pIC50 = 7.8 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 316 6 0 5 2.6 CCCOCCn1c(N2CCCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
621659 62729 10 None -2 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 305 3 0 3 3.6 Cc1ccc2c(c1)c1c(n2CCc2ccncc2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783965 62729 10 None -2 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 305 3 0 3 3.6 Cc1ccc2c(c1)c1c(n2CCc2ccncc2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
197033 199152 64 None 1 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
CHEMBL589390 199152 64 None 1 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
44458903 90646 0 None - 1 Guinea pig 7.8 pIC50 = 7.8 Functional
In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum
ChEMBL 275 2 0 1 4.3 CCN1CCC2=C(C1)C(c1ccccc1)c1ccccc12 10.1016/s0960-894x(00)00199-2
CHEMBL23897 90646 0 None - 1 Guinea pig 7.8 pIC50 = 7.8 Functional
In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum
ChEMBL 275 2 0 1 4.3 CCN1CCC2=C(C1)C(c1ccccc1)c1ccccc12 10.1016/s0960-894x(00)00199-2
2773189 59739 3 None - 1 Guinea pig 7.8 pIC50 = 7.8 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 306 3 0 4 2.8 CN1CCN(c2nc3ccccc3n2Cc2ccccc2)CC1 10.1021/jm00157a010
CHEMBL17246 59739 3 None - 1 Guinea pig 7.8 pIC50 = 7.8 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 306 3 0 4 2.8 CN1CCN(c2nc3ccccc3n2Cc2ccccc2)CC1 10.1021/jm00157a010
3071002 63017 1 None - 1 Guinea pig 7.8 pIC50 = 7.8 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 300 6 0 5 2.0 C=CCOCCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
CHEMBL17876 63017 1 None - 1 Guinea pig 7.8 pIC50 = 7.8 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 300 6 0 5 2.0 C=CCOCCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
145990794 166800 0 None -28 6 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 437 6 0 5 3.8 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4284346 166800 0 None -28 6 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 437 6 0 5 3.8 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
4919 206234 23 None -263 5 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay
ChEMBL 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 10.1021/jm300671m
CHEMBL86715 206234 23 None -263 5 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay
ChEMBL 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 10.1021/jm300671m
13623352 60006 0 None - 1 Guinea pig 7.8 pIC50 = 7.8 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 288 5 0 5 2.2 CCCOCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
CHEMBL17349 60006 0 None - 1 Guinea pig 7.8 pIC50 = 7.8 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 288 5 0 5 2.2 CCCOCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
3071010 63919 1 None - 1 Guinea pig 7.8 pIC50 = 7.8 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 302 6 0 5 2.2 CCOCCn1c(N2CCN(CC)CC2)nc2ccccc21 10.1021/jm00157a010
CHEMBL18060 63919 1 None - 1 Guinea pig 7.8 pIC50 = 7.8 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 302 6 0 5 2.2 CCOCCn1c(N2CCN(CC)CC2)nc2ccccc21 10.1021/jm00157a010
46224877 200701 5 None 74 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challenge
ChEMBL 288 2 0 2 4.3 CN1CCc2c(c3ccccc3n2/C=C\c2ccccc2)C1 10.1016/j.bmcl.2009.11.037
CHEMBL599913 200701 5 None 74 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challenge
ChEMBL 288 2 0 2 4.3 CN1CCc2c(c3ccccc3n2/C=C\c2ccccc2)C1 10.1016/j.bmcl.2009.11.037
54586812 62717 5 None 12 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 291 3 0 3 3.3 CN1CCc2c(c3ccccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783953 62717 5 None 12 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 291 3 0 3 3.3 CN1CCc2c(c3ccccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
13623336 60496 0 None - 1 Guinea pig 7.7 pIC50 = 7.7 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 286 5 0 4 3.0 CCCCCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
CHEMBL17555 60496 0 None - 1 Guinea pig 7.7 pIC50 = 7.7 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 286 5 0 4 3.0 CCCCCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
13623350 63112 0 None - 1 Guinea pig 7.7 pIC50 = 7.7 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 304 5 0 5 2.5 CCSCCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
CHEMBL17893 63112 0 None - 1 Guinea pig 7.7 pIC50 = 7.7 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 304 5 0 5 2.5 CCSCCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
145983928 166412 0 None -53 6 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 435 6 0 5 3.6 O=C1[C@H]2[C@@H]3C=C[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4277101 166412 0 None -53 6 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 435 6 0 5 3.6 O=C1[C@H]2[C@@H]3C=C[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
3071014 98085 1 None - 1 Guinea pig 7.7 pIC50 = 7.7 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 302 6 0 5 2.2 CCCOCCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
CHEMBL273320 98085 1 None - 1 Guinea pig 7.7 pIC50 = 7.7 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 302 6 0 5 2.2 CCCOCCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
126624 208290 10 None - 1 Guinea pig 4.7 pIC50 = 4.7 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 264 5 0 3 2.2 CN(C)CCCN1C(=O)CSC1c1ccccc1 10.1021/jm00093a025
CHEMBL1202936 208290 10 None - 1 Guinea pig 4.7 pIC50 = 4.7 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 264 5 0 3 2.2 CN(C)CCCN1C(=O)CSC1c1ccccc1 10.1021/jm00093a025
CHEMBL98989 208290 10 None - 1 Guinea pig 4.7 pIC50 = 4.7 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 264 5 0 3 2.2 CN(C)CCCN1C(=O)CSC1c1ccccc1 10.1021/jm00093a025
10123138 108526 0 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 748 12 0 10 6.7 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc4c(c3)OCO4)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10097-X
CHEMBL317524 108526 0 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 748 12 0 10 6.7 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc4c(c3)OCO4)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10097-X
CHEMBL320002 108526 0 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 748 12 0 10 6.7 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc4c(c3)OCO4)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10097-X
2861271 4254 9 None - 1 Guinea pig 4.7 pIC50 = 4.7 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 298 5 0 3 2.9 CN(C)CCCN1C(=O)CSC1c1ccc(Cl)cc1 10.1021/jm00093a025
CHEMBL100486 4254 9 None - 1 Guinea pig 4.7 pIC50 = 4.7 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 298 5 0 3 2.9 CN(C)CCCN1C(=O)CSC1c1ccc(Cl)cc1 10.1021/jm00093a025
46224878 199469 0 None 2 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challenge
ChEMBL 290 2 0 2 4.0 CN1CCC2C(C1)c1ccccc1N2/C=C/c1ccccc1 10.1016/j.bmcl.2009.11.037
CHEMBL591568 199469 0 None 2 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challenge
ChEMBL 290 2 0 2 4.0 CN1CCC2C(C1)c1ccccc1N2/C=C/c1ccccc1 10.1016/j.bmcl.2009.11.037
54585847 62732 6 None 29 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 359 3 0 3 4.3 CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2ccncc2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783968 62732 6 None 29 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 359 3 0 3 4.3 CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2ccncc2)C1 10.1016/j.bmcl.2009.04.128
198539 99231 3 None - 1 Guinea pig 6.7 pIC50 = 6.7 Functional
In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum
ChEMBL 259 1 0 1 3.8 CN1CC=C2C(=C(c3ccccc3)c3ccccc32)C1 10.1016/s0960-894x(00)00199-2
CHEMBL281638 99231 3 None - 1 Guinea pig 6.7 pIC50 = 6.7 Functional
In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum
ChEMBL 259 1 0 1 3.8 CN1CC=C2C(=C(c3ccccc3)c3ccccc32)C1 10.1016/s0960-894x(00)00199-2
2860026 108376 7 None - 1 Guinea pig 5.7 pIC50 = 5.7 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 298 5 0 3 2.9 CN(C)CCCN1C(=O)CSC1c1cccc(Cl)c1 10.1021/jm00093a025
CHEMBL319829 108376 7 None - 1 Guinea pig 5.7 pIC50 = 5.7 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 298 5 0 3 2.9 CN(C)CCCN1C(=O)CSC1c1cccc(Cl)c1 10.1021/jm00093a025
7430452 99478 2 None - 1 Guinea pig 7.6 pIC50 = 7.6 Functional
In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum
ChEMBL 309 4 1 3 3.1 CCN1CC[C@@](O)(c2ccccc2)[C@H](C(=O)c2ccccc2)C1 10.1016/s0960-894x(00)00199-2
CHEMBL283169 99478 2 None - 1 Guinea pig 7.6 pIC50 = 7.6 Functional
In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum
ChEMBL 309 4 1 3 3.1 CCN1CC[C@@](O)(c2ccccc2)[C@H](C(=O)c2ccccc2)C1 10.1016/s0960-894x(00)00199-2
2861590 107260 7 None - 1 Guinea pig 5.6 pIC50 = 5.6 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 342 5 0 3 3.0 CN(C)CCCN1C(=O)CSC1c1ccc(Br)cc1 10.1021/jm00093a025
CHEMBL1202937 107260 7 None - 1 Guinea pig 5.6 pIC50 = 5.6 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 342 5 0 3 3.0 CN(C)CCCN1C(=O)CSC1c1ccc(Br)cc1 10.1021/jm00093a025
CHEMBL316951 107260 7 None - 1 Guinea pig 5.6 pIC50 = 5.6 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 342 5 0 3 3.0 CN(C)CCCN1C(=O)CSC1c1ccc(Br)cc1 10.1021/jm00093a025
10212223 208140 0 None -2 2 Human 6.6 pIC50 = 6.6 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 704 12 0 8 7.0 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10097-X
CHEMBL431458 208140 0 None -2 2 Human 6.6 pIC50 = 6.6 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 704 12 0 8 7.0 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10097-X
CHEMBL98079 208140 0 None -2 2 Human 6.6 pIC50 = 6.6 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 704 12 0 8 7.0 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10097-X
10190056 111438 0 None 1 2 Human 6.6 pIC50 = 6.6 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 674 11 0 7 7.0 COc1ccc(C2(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)CCN(C(=O)c3ccccc3)C2)cc1OC 10.1016/S0960-894X(97)10097-X
CHEMBL327497 111438 0 None 1 2 Human 6.6 pIC50 = 6.6 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 674 11 0 7 7.0 COc1ccc(C2(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)CCN(C(=O)c3ccccc3)C2)cc1OC 10.1016/S0960-894X(97)10097-X
13623341 62120 0 None - 1 Guinea pig 6.6 pIC50 = 6.6 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 320 4 0 4 3.0 CN1CCN(c2nc3ccccc3n2CCc2ccccc2)CC1 10.1021/jm00157a010
CHEMBL17763 62120 0 None - 1 Guinea pig 6.6 pIC50 = 6.6 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 320 4 0 4 3.0 CN1CCN(c2nc3ccccc3n2CCc2ccccc2)CC1 10.1021/jm00157a010
2872050 208226 3 None - 1 Guinea pig 4.6 pIC50 = 4.6 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 282 5 0 3 2.4 CN(C)CCCN1C(=O)CSC1c1ccc(F)cc1 10.1021/jm00093a025
CHEMBL1202939 208226 3 None - 1 Guinea pig 4.6 pIC50 = 4.6 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 282 5 0 3 2.4 CN(C)CCCN1C(=O)CSC1c1ccc(F)cc1 10.1021/jm00093a025
CHEMBL98605 208226 3 None - 1 Guinea pig 4.6 pIC50 = 4.6 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 282 5 0 3 2.4 CN(C)CCCN1C(=O)CSC1c1ccc(F)cc1 10.1021/jm00093a025
2284 3182 33 None -3 34 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1021/jm300671m
4926 3182 33 None -3 34 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1021/jm300671m
7281 3182 33 None -3 34 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1021/jm300671m
CHEMBL564 3182 33 None -3 34 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1021/jm300671m
DB00420 3182 33 None -3 34 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1021/jm300671m
9984168 98289 9 None - 1 Guinea pig 7.6 pIC50 = 7.6 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 288 5 1 5 1.9 CCOCCn1c(N2CCCNCC2)nc2ccccc21 10.1021/jm00157a010
CHEMBL274747 98289 9 None - 1 Guinea pig 7.6 pIC50 = 7.6 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 288 5 1 5 1.9 CCOCCn1c(N2CCCNCC2)nc2ccccc21 10.1021/jm00157a010
14984033 208178 1 None - 1 Guinea pig 4.6 pIC50 = 4.6 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 294 6 0 4 2.2 COc1cccc(C2SCC(=O)N2CCCN(C)C)c1 10.1021/jm00093a025
CHEMBL1202941 208178 1 None - 1 Guinea pig 4.6 pIC50 = 4.6 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 294 6 0 4 2.2 COc1cccc(C2SCC(=O)N2CCCN(C)C)c1 10.1021/jm00093a025
CHEMBL98334 208178 1 None - 1 Guinea pig 4.6 pIC50 = 4.6 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 294 6 0 4 2.2 COc1cccc(C2SCC(=O)N2CCCN(C)C)c1 10.1021/jm00093a025
145993117 166921 0 None -204 6 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 427 7 0 5 4.4 CCC1(C)CC(=O)N(CCCCN2CCN(c3cccc4sccc34)CC2)C(=O)C1 10.1016/j.ejmech.2017.12.099
CHEMBL4286717 166921 0 None -204 6 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 427 7 0 5 4.4 CCC1(C)CC(=O)N(CCCCN2CCN(c3cccc4sccc34)CC2)C(=O)C1 10.1016/j.ejmech.2017.12.099
708981 88792 2 None - 1 Guinea pig 7.6 pIC50 = 7.6 Functional
In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum
ChEMBL 295 3 1 3 2.7 CN1CC[C@@](O)(c2ccccc2)[C@H](C(=O)c2ccccc2)C1 10.1016/s0960-894x(00)00199-2
CHEMBL23638 88792 2 None - 1 Guinea pig 7.6 pIC50 = 7.6 Functional
In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum
ChEMBL 295 3 1 3 2.7 CN1CC[C@@](O)(c2ccccc2)[C@H](C(=O)c2ccccc2)C1 10.1016/s0960-894x(00)00199-2
13623337 98802 0 None - 1 Guinea pig 7.6 pIC50 = 7.6 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 300 6 0 4 3.4 CCCCCCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
CHEMBL278457 98802 0 None - 1 Guinea pig 7.6 pIC50 = 7.6 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 300 6 0 4 3.4 CCCCCCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
15585276 61966 0 None - 1 Guinea pig 7.6 pIC50 = 7.6 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 364 7 0 5 3.4 CCOCCn1c(N2CCN(Cc3ccccc3)CC2)nc2ccccc21 10.1021/jm00157a010
CHEMBL17742 61966 0 None - 1 Guinea pig 7.6 pIC50 = 7.6 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 364 7 0 5 3.4 CCOCCn1c(N2CCN(Cc3ccccc3)CC2)nc2ccccc21 10.1021/jm00157a010
54582000 62736 5 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 388 4 0 4 4.0 Cc1ccc2c(c1)c1c(n2CCc2cccnc2)CCN(C2CCN(C)CC2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783974 62736 5 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 388 4 0 4 4.0 Cc1ccc2c(c1)c1c(n2CCc2cccnc2)CCN(C2CCN(C)CC2)C1 10.1016/j.bmcl.2009.04.128
162910 84621 6 None - 1 Guinea pig 7.6 pIC50 = 7.6 Functional
In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum
ChEMBL 261 1 0 1 3.9 CN1CCC2C(=C(c3ccccc3)c3ccccc32)C1 10.1016/s0960-894x(00)00199-2
CHEMBL22215 84621 6 None - 1 Guinea pig 7.6 pIC50 = 7.6 Functional
In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum
ChEMBL 261 1 0 1 3.9 CN1CCC2C(=C(c3ccccc3)c3ccccc32)C1 10.1016/s0960-894x(00)00199-2
15542879 112824 0 None -2 2 Human 6.5 pIC50 = 6.5 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 687 12 0 9 6.3 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccncc4)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10097-X
CHEMBL330719 112824 0 None -2 2 Human 6.5 pIC50 = 6.5 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 687 12 0 9 6.3 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccncc4)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10097-X
13623357 63379 0 None - 1 Guinea pig 6.5 pIC50 = 6.5 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 287 5 1 5 1.4 CCNCCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
CHEMBL17959 63379 0 None - 1 Guinea pig 6.5 pIC50 = 6.5 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 287 5 1 5 1.4 CCNCCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
10168749 207621 0 None -3 2 Human 6.5 pIC50 = 6.5 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 676 12 0 9 6.5 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccco4)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10097-X
CHEMBL95127 207621 0 None -3 2 Human 6.5 pIC50 = 6.5 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 676 12 0 9 6.5 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccco4)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10097-X
1227 2489 43 None 2 14 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human recombinant H1 receptor assessed as inhibition of histamine-induced intracellular Ca2+ releaseAntagonist activity at human recombinant H1 receptor assessed as inhibition of histamine-induced intracellular Ca2+ release
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm401895u
2331 2489 43 None 2 14 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human recombinant H1 receptor assessed as inhibition of histamine-induced intracellular Ca2+ releaseAntagonist activity at human recombinant H1 receptor assessed as inhibition of histamine-induced intracellular Ca2+ release
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm401895u
3957 2489 43 None 2 14 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human recombinant H1 receptor assessed as inhibition of histamine-induced intracellular Ca2+ releaseAntagonist activity at human recombinant H1 receptor assessed as inhibition of histamine-induced intracellular Ca2+ release
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm401895u
4992 2489 43 None 2 14 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human recombinant H1 receptor assessed as inhibition of histamine-induced intracellular Ca2+ releaseAntagonist activity at human recombinant H1 receptor assessed as inhibition of histamine-induced intracellular Ca2+ release
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm401895u
CHEMBL511 2489 43 None 2 14 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human recombinant H1 receptor assessed as inhibition of histamine-induced intracellular Ca2+ releaseAntagonist activity at human recombinant H1 receptor assessed as inhibition of histamine-induced intracellular Ca2+ release
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm401895u
DB06691 2489 43 None 2 14 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human recombinant H1 receptor assessed as inhibition of histamine-induced intracellular Ca2+ releaseAntagonist activity at human recombinant H1 receptor assessed as inhibition of histamine-induced intracellular Ca2+ release
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm401895u
44126326 199619 7 None 32 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge
ChEMBL 322 3 0 2 4.3 Cc1ccc2c(c1)c1c(n2CCc2ccc(F)cc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL592753 199619 7 None 32 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge
ChEMBL 322 3 0 2 4.3 Cc1ccc2c(c1)c1c(n2CCc2ccc(F)cc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
13623361 64645 0 None - 1 Guinea pig 7.5 pIC50 = 7.5 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 344 9 0 5 3.4 CCCCCN1CCN(c2nc3ccccc3n2CCOCC)CC1 10.1021/jm00157a010
CHEMBL18181 64645 0 None - 1 Guinea pig 7.5 pIC50 = 7.5 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 344 9 0 5 3.4 CCCCCN1CCN(c2nc3ccccc3n2CCOCC)CC1 10.1021/jm00157a010
145993493 167357 0 None -38 6 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 439 6 0 5 4.5 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4294617 167357 0 None -38 6 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 439 6 0 5 4.5 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
9918576 207337 0 None -2 3 Human 6.5 pIC50 = 6.5 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 764 14 0 10 7.0 COc1ccc(C2(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C2)cc1OC 10.1016/S0960-894X(97)10097-X
CHEMBL93556 207337 0 None -2 3 Human 6.5 pIC50 = 6.5 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 764 14 0 10 7.0 COc1ccc(C2(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C2)cc1OC 10.1016/S0960-894X(97)10097-X
44126328 201105 5 None 74 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge
ChEMBL 322 3 0 2 4.3 Cc1ccc(CCn2c3c(c4cc(F)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
CHEMBL603049 201105 5 None 74 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge
ChEMBL 322 3 0 2 4.3 Cc1ccc(CCn2c3c(c4cc(F)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
13623363 99036 0 None - 1 Guinea pig 7.5 pIC50 = 7.5 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 378 8 0 5 3.4 CCOCCn1c(N2CCN(CCc3ccccc3)CC2)nc2ccccc21 10.1021/jm00157a010
CHEMBL280255 99036 0 None - 1 Guinea pig 7.5 pIC50 = 7.5 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 378 8 0 5 3.4 CCOCCn1c(N2CCN(CCc3ccccc3)CC2)nc2ccccc21 10.1021/jm00157a010
14984031 208373 1 None - 1 Guinea pig 5.5 pIC50 = 5.5 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 282 5 0 3 2.4 CN(C)CCCN1C(=O)CSC1c1cccc(F)c1 10.1021/jm00093a025
CHEMBL1202933 208373 1 None - 1 Guinea pig 5.5 pIC50 = 5.5 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 282 5 0 3 2.4 CN(C)CCCN1C(=O)CSC1c1cccc(F)c1 10.1021/jm00093a025
CHEMBL99529 208373 1 None - 1 Guinea pig 5.5 pIC50 = 5.5 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 282 5 0 3 2.4 CN(C)CCCN1C(=O)CSC1c1cccc(F)c1 10.1021/jm00093a025
44126330 62724 5 None -2 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay
ChEMBL 305 3 0 3 3.6 Cc1ccc2c(c1)c1c(n2CCc2cccnc2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783960 62724 5 None -2 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay
ChEMBL 305 3 0 3 3.6 Cc1ccc2c(c1)c1c(n2CCc2cccnc2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
46225027 199117 5 None 74 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge
ChEMBL 338 4 0 3 4.0 COc1ccc(CCn2c3c(c4cc(F)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
CHEMBL589150 199117 5 None 74 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge
ChEMBL 338 4 0 3 4.0 COc1ccc(CCn2c3c(c4cc(F)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
54583938 62733 0 None 1 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 306 3 0 4 3.0 Cc1ccc2c(c1)c1c(n2CCc2cnccn2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783970 62733 0 None 1 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 306 3 0 4 3.0 Cc1ccc2c(c1)c1c(n2CCc2cnccn2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
2773179 98717 5 None - 1 Guinea pig 6.5 pIC50 = 6.5 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 230 1 0 4 1.3 CN1CCN(c2nc3ccccc3n2C)CC1 10.1021/jm00157a010
CHEMBL277749 98717 5 None - 1 Guinea pig 6.5 pIC50 = 6.5 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 230 1 0 4 1.3 CN1CCN(c2nc3ccccc3n2C)CC1 10.1021/jm00157a010
46224877 200701 5 None 74 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge
ChEMBL 288 2 0 2 4.3 CN1CCc2c(c3ccccc3n2/C=C\c2ccccc2)C1 10.1016/j.bmcl.2009.11.037
CHEMBL599913 200701 5 None 74 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge
ChEMBL 288 2 0 2 4.3 CN1CCc2c(c3ccccc3n2/C=C\c2ccccc2)C1 10.1016/j.bmcl.2009.11.037
1227 2489 43 None -2 14 Guinea pig 7.5 pIC50 = 7.5 Functional
In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/s0960-894x(00)00199-2
2331 2489 43 None -2 14 Guinea pig 7.5 pIC50 = 7.5 Functional
In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/s0960-894x(00)00199-2
3957 2489 43 None -2 14 Guinea pig 7.5 pIC50 = 7.5 Functional
In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/s0960-894x(00)00199-2
4992 2489 43 None -2 14 Guinea pig 7.5 pIC50 = 7.5 Functional
In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/s0960-894x(00)00199-2
CHEMBL511 2489 43 None -2 14 Guinea pig 7.5 pIC50 = 7.5 Functional
In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/s0960-894x(00)00199-2
DB06691 2489 43 None -2 14 Guinea pig 7.5 pIC50 = 7.5 Functional
In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/s0960-894x(00)00199-2
10123040 161095 0 None -7 2 Human 5.5 pIC50 = 5.5 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 730 13 1 9 6.6 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(C(=O)O)cc4)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10097-X
CHEMBL411691 161095 0 None -7 2 Human 5.5 pIC50 = 5.5 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 730 13 1 9 6.6 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(C(=O)O)cc4)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10097-X
CHEMBL537027 161095 0 None -7 2 Human 5.5 pIC50 = 5.5 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 730 13 1 9 6.6 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(C(=O)O)cc4)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10097-X
46224878 199469 0 None 2 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge
ChEMBL 290 2 0 2 4.0 CN1CCC2C(C1)c1ccccc1N2/C=C/c1ccccc1 10.1016/j.bmcl.2009.11.037
CHEMBL591568 199469 0 None 2 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge
ChEMBL 290 2 0 2 4.0 CN1CCC2C(C1)c1ccccc1N2/C=C/c1ccccc1 10.1016/j.bmcl.2009.11.037
46225002 199494 5 None 602 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge
ChEMBL 376 3 0 2 5.0 CN1CCc2c(c3cc(F)ccc3n2CCc2ccc(C(F)(F)F)cc2)C1 10.1016/j.bmcl.2009.11.037
CHEMBL591803 199494 5 None 602 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge
ChEMBL 376 3 0 2 5.0 CN1CCc2c(c3cc(F)ccc3n2CCc2ccc(C(F)(F)F)cc2)C1 10.1016/j.bmcl.2009.11.037
11291 98796 25 None 223 3 Guinea pig 7.4 pIC50 = 7.4 Functional
In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum
ChEMBL 261 1 0 1 3.9 CN1CCC2=C(C1)C(c1ccccc1)c1ccccc12 10.1016/s0960-894x(00)00199-2
CHEMBL278398 98796 25 None 223 3 Guinea pig 7.4 pIC50 = 7.4 Functional
In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum
ChEMBL 261 1 0 1 3.9 CN1CCC2=C(C1)C(c1ccccc1)c1ccccc12 10.1016/s0960-894x(00)00199-2
10233656 207851 0 None -3 2 Human 6.4 pIC50 = 6.4 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 687 12 0 9 6.3 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccccn4)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10097-X
CHEMBL96442 207851 0 None -3 2 Human 6.4 pIC50 = 6.4 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 687 12 0 9 6.3 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccccn4)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10097-X
13623343 98501 0 None - 1 Guinea pig 7.4 pIC50 = 7.4 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 316 7 0 5 2.6 CCCCOCCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
CHEMBL276070 98501 0 None - 1 Guinea pig 7.4 pIC50 = 7.4 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 316 7 0 5 2.6 CCCCOCCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
13623334 63923 0 None - 1 Guinea pig 6.4 pIC50 = 6.4 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 258 3 0 4 2.2 CCCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
CHEMBL18062 63923 0 None - 1 Guinea pig 6.4 pIC50 = 6.4 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 258 3 0 4 2.2 CCCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
10122529 109556 0 None -3 2 Human 6.4 pIC50 = 6.4 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 668 14 0 9 5.9 CCOCCn1c(C(=O)C2CCN(CCC3(c4ccccc4)CCN(C(=O)c4cc(OC)c(OC)c(OC)c4)C3)CC2)nc2ccccc21 10.1016/S0960-894X(97)10097-X
CHEMBL322194 109556 0 None -3 2 Human 6.4 pIC50 = 6.4 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 668 14 0 9 5.9 CCOCCn1c(C(=O)C2CCN(CCC3(c4ccccc4)CCN(C(=O)c4cc(OC)c(OC)c(OC)c4)C3)CC2)nc2ccccc21 10.1016/S0960-894X(97)10097-X
54581997 62730 6 None 11 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 321 4 0 4 3.3 COc1ccc2c(c1)c1c(n2CCc2ccncc2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783966 62730 6 None 11 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 321 4 0 4 3.3 COc1ccc2c(c1)c1c(n2CCc2ccncc2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
621659 62729 10 None -2 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay
ChEMBL 305 3 0 3 3.6 Cc1ccc2c(c1)c1c(n2CCc2ccncc2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783965 62729 10 None -2 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay
ChEMBL 305 3 0 3 3.6 Cc1ccc2c(c1)c1c(n2CCc2ccncc2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
10123040 161095 0 None -7 2 Human 8.4 pIC50 = 8.4 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 730 13 1 9 6.6 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(C(=O)O)cc4)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
CHEMBL411691 161095 0 None -7 2 Human 8.4 pIC50 = 8.4 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 730 13 1 9 6.6 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(C(=O)O)cc4)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
CHEMBL537027 161095 0 None -7 2 Human 8.4 pIC50 = 8.4 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 730 13 1 9 6.6 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(C(=O)O)cc4)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
10212725 98169 0 None 1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 790 15 1 11 6.6 COc1ccc(C2(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(C(=O)O)cc4)CC3)CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C2)cc1OC 10.1016/S0960-894X(97)10098-1
CHEMBL273915 98169 0 None 1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 790 15 1 11 6.6 COc1ccc(C2(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(C(=O)O)cc4)CC3)CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C2)cc1OC 10.1016/S0960-894X(97)10098-1
46225000 199115 5 None 9 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge
ChEMBL 308 3 0 2 4.0 CN1CCc2c(c3cc(F)ccc3n2CCc2ccccc2)C1 10.1016/j.bmcl.2009.11.037
CHEMBL589148 199115 5 None 9 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge
ChEMBL 308 3 0 2 4.0 CN1CCc2c(c3cc(F)ccc3n2CCc2ccccc2)C1 10.1016/j.bmcl.2009.11.037
42631003 199618 13 None 2 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge
ChEMBL 304 3 0 2 4.2 Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL592752 199618 13 None 2 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge
ChEMBL 304 3 0 2 4.2 Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
14984030 107330 1 None - 1 Guinea pig 4.4 pIC50 = 4.4 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 279 5 1 4 1.8 CN(C)CCCN1C(=O)CSC1c1ccc(N)cc1 10.1021/jm00093a025
CHEMBL1202935 107330 1 None - 1 Guinea pig 4.4 pIC50 = 4.4 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 279 5 1 4 1.8 CN(C)CCCN1C(=O)CSC1c1ccc(N)cc1 10.1021/jm00093a025
CHEMBL317518 107330 1 None - 1 Guinea pig 4.4 pIC50 = 4.4 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 279 5 1 4 1.8 CN(C)CCCN1C(=O)CSC1c1ccc(N)cc1 10.1021/jm00093a025
44224259 62723 5 None 30 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay
ChEMBL 291 3 0 3 3.3 CN1CCc2c(c3ccccc3n2CCc2cccnc2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783959 62723 5 None 30 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay
ChEMBL 291 3 0 3 3.3 CN1CCc2c(c3ccccc3n2CCc2cccnc2)C1 10.1016/j.bmcl.2009.04.128
13623358 98738 1 None - 1 Guinea pig 6.4 pIC50 = 6.4 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 260 3 1 5 0.8 CN1CCN(c2nc3ccccc3n2CCO)CC1 10.1021/jm00157a010
CHEMBL277956 98738 1 None - 1 Guinea pig 6.4 pIC50 = 6.4 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 260 3 1 5 0.8 CN1CCN(c2nc3ccccc3n2CCO)CC1 10.1021/jm00157a010
15542881 112591 0 None -3 2 Human 6.4 pIC50 = 6.4 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 687 12 0 9 6.3 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4cccnc4)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10097-X
CHEMBL330172 112591 0 None -3 2 Human 6.4 pIC50 = 6.4 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 687 12 0 9 6.3 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4cccnc4)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10097-X
145966333 164060 0 None -346 6 Human 6.4 pIC50 = 6.4 Functional
Antagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 424 8 1 6 3.6 CNC(=O)c1cc(OCCCCN2CCN(c3cccc4sccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
CHEMBL4209188 164060 0 None -346 6 Human 6.4 pIC50 = 6.4 Functional
Antagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 424 8 1 6 3.6 CNC(=O)c1cc(OCCCCN2CCN(c3cccc4sccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
13623355 64344 0 None - 1 Guinea pig 7.4 pIC50 = 7.4 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 304 6 1 6 0.8 CN1CCN(c2nc3ccccc3n2CCOCCO)CC1 10.1021/jm00157a010
CHEMBL18122 64344 0 None - 1 Guinea pig 7.4 pIC50 = 7.4 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 304 6 1 6 0.8 CN1CCN(c2nc3ccccc3n2CCOCCO)CC1 10.1021/jm00157a010
242 470 124 None -97 33 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2017.12.099
34 470 124 None -97 33 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2017.12.099
60795 470 124 None -97 33 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2017.12.099
CHEMBL1112 470 124 None -97 33 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2017.12.099
DB01238 470 124 None -97 33 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2017.12.099
242 470 124 None -97 33 Human 6.4 pIC50 = 6.4 Functional
Antagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2018.01.038
34 470 124 None -97 33 Human 6.4 pIC50 = 6.4 Functional
Antagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2018.01.038
60795 470 124 None -97 33 Human 6.4 pIC50 = 6.4 Functional
Antagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2018.01.038
CHEMBL1112 470 124 None -97 33 Human 6.4 pIC50 = 6.4 Functional
Antagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2018.01.038
DB01238 470 124 None -97 33 Human 6.4 pIC50 = 6.4 Functional
Antagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2018.01.038
13623339 63295 0 None - 1 Guinea pig 5.4 pIC50 = 5.4 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 356 10 0 4 4.9 CCCCCCCCCCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
CHEMBL17931 63295 0 None - 1 Guinea pig 5.4 pIC50 = 5.4 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 356 10 0 4 4.9 CCCCCCCCCCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
13623356 62492 0 None - 1 Guinea pig 6.4 pIC50 = 6.4 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 350 6 0 5 3.0 CN1CCN(c2nc3ccccc3n2CCOCc2ccccc2)CC1 10.1021/jm00157a010
CHEMBL17808 62492 0 None - 1 Guinea pig 6.4 pIC50 = 6.4 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 350 6 0 5 3.0 CN1CCN(c2nc3ccccc3n2CCOCc2ccccc2)CC1 10.1021/jm00157a010
10283825 96693 0 None -1 2 Human 6.4 pIC50 = 6.4 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 740 12 0 8 7.3 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(F)cc3F)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10097-X
CHEMBL264007 96693 0 None -1 2 Human 6.4 pIC50 = 6.4 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 740 12 0 8 7.3 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(F)cc3F)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10097-X
10147107 207620 0 None -3 2 Human 6.4 pIC50 = 6.4 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 755 12 0 9 7.6 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccccn4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10097-X
CHEMBL431850 207620 0 None -3 2 Human 6.4 pIC50 = 6.4 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 755 12 0 9 7.6 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccccn4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10097-X
CHEMBL95125 207620 0 None -3 2 Human 6.4 pIC50 = 6.4 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 755 12 0 9 7.6 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccccn4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10097-X
145964299 164132 0 None -489 6 Human 5.4 pIC50 = 5.4 Functional
Antagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 426 8 1 6 3.8 CNC(=O)c1cc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
CHEMBL4210030 164132 0 None -489 6 Human 5.4 pIC50 = 5.4 Functional
Antagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 426 8 1 6 3.8 CNC(=O)c1cc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
44327909 112358 0 None -37 2 Human 6.4 pIC50 = 6.4 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 706 14 0 10 6.5 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4CCOc4ccco4)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10097-X
CHEMBL329450 112358 0 None -37 2 Human 6.4 pIC50 = 6.4 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 706 14 0 10 6.5 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4CCOc4ccco4)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10097-X
736282 78142 12 None -3 2 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay
ChEMBL 337 6 1 3 4.2 CN1[C@H](CC(=O)c2ccccc2)CCC[C@@H]1C[C@H](O)c1ccccc1 10.1021/jm300671m
CHEMBL2103769 78142 12 None -3 2 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay
ChEMBL 337 6 1 3 4.2 CN1[C@H](CC(=O)c2ccccc2)CCC[C@@H]1C[C@H](O)c1ccccc1 10.1021/jm300671m
2389 3331 118 None -234 29 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2017.12.099
5073 3331 118 None -234 29 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2017.12.099
96 3331 118 None -234 29 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2017.12.099
CHEMBL85 3331 118 None -234 29 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2017.12.099
DB00734 3331 118 None -234 29 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2017.12.099
2389 3331 118 None -234 29 Human 6.3 pIC50 = 6.3 Functional
Antagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2018.01.038
5073 3331 118 None -234 29 Human 6.3 pIC50 = 6.3 Functional
Antagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2018.01.038
96 3331 118 None -234 29 Human 6.3 pIC50 = 6.3 Functional
Antagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2018.01.038
CHEMBL85 3331 118 None -234 29 Human 6.3 pIC50 = 6.3 Functional
Antagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2018.01.038
DB00734 3331 118 None -234 29 Human 6.3 pIC50 = 6.3 Functional
Antagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2018.01.038
1227 2489 43 None 2 14 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm300671m
2331 2489 43 None 2 14 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm300671m
3957 2489 43 None 2 14 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm300671m
4992 2489 43 None 2 14 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm300671m
CHEMBL511 2489 43 None 2 14 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm300671m
DB06691 2489 43 None 2 14 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm300671m
75201901 166425 19 None -208 4 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b01622
CHEMBL4277264 166425 19 None -208 4 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b01622
54582938 62719 6 None 1 2 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 321 4 0 4 3.3 COc1ccc2c(c1)c1c(n2CCc2ccccn2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783955 62719 6 None 1 2 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 321 4 0 4 3.3 COc1ccc2c(c1)c1c(n2CCc2ccccn2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
54580942 62731 9 None 13 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay
ChEMBL 309 3 0 3 3.4 CN1CCc2c(c3cc(F)ccc3n2CCc2ccncc2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783967 62731 9 None 13 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay
ChEMBL 309 3 0 3 3.4 CN1CCc2c(c3cc(F)ccc3n2CCc2ccncc2)C1 10.1016/j.bmcl.2009.04.128
10315027 98929 0 None - 1 Guinea pig 6.3 pIC50 = 6.3 Functional
In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum
ChEMBL 337 3 0 1 5.5 c1ccc(CN2CCC3=C(C2)C(c2ccccc2)c2ccccc23)cc1 10.1016/s0960-894x(00)00199-2
CHEMBL279454 98929 0 None - 1 Guinea pig 6.3 pIC50 = 6.3 Functional
In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum
ChEMBL 337 3 0 1 5.5 c1ccc(CN2CCC3=C(C2)C(c2ccccc2)c2ccccc23)cc1 10.1016/s0960-894x(00)00199-2
15542673 207564 0 None -1 2 Human 6.3 pIC50 = 6.3 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 772 12 0 8 8.0 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(C(F)(F)F)cc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10097-X
CHEMBL94834 207564 0 None -1 2 Human 6.3 pIC50 = 6.3 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 772 12 0 8 8.0 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(C(F)(F)F)cc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10097-X
10305888 207555 0 None 1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 750 14 1 9 7.0 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4CCCC(=O)O)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
CHEMBL94788 207555 0 None 1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 750 14 1 9 7.0 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4CCCC(=O)O)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
44328321 167788 0 None 1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 788 17 1 10 7.4 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4CCCCOc4ccccc4C(=O)O)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
CHEMBL430471 167788 0 None 1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 788 17 1 10 7.4 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4CCCCOc4ccccc4C(=O)O)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
10305069 207850 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 656 12 1 9 5.4 COc1ccc(C2(CCN3CCC(C(=O)c4nc5ccccc5[nH]4)CC3)CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C2)cc1OC 10.1016/S0960-894X(97)10098-1
CHEMBL96441 207850 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 656 12 1 9 5.4 COc1ccc(C2(CCN3CCC(C(=O)c4nc5ccccc5[nH]4)CC3)CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C2)cc1OC 10.1016/S0960-894X(97)10098-1
10234086 111634 0 None -6 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 744 13 0 10 6.7 COC(=O)c1ccc(Cn2c(C(=O)C3CCN(CCC4(c5ccccc5)CCN(C(=O)c5cc(OC)c(OC)c(OC)c5)C4)CC3)nc3ccccc32)cc1 10.1016/S0960-894X(97)10098-1
CHEMBL328511 111634 0 None -6 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 744 13 0 10 6.7 COC(=O)c1ccc(Cn2c(C(=O)C3CCN(CCC4(c5ccccc5)CCN(C(=O)c5cc(OC)c(OC)c(OC)c5)C4)CC3)nc3ccccc32)cc1 10.1016/S0960-894X(97)10098-1
13623335 98801 0 None - 1 Guinea pig 7.3 pIC50 = 7.3 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 272 4 0 4 2.6 CCCCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
CHEMBL278456 98801 0 None - 1 Guinea pig 7.3 pIC50 = 7.3 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 272 4 0 4 2.6 CCCCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
10121390 112739 0 None -3 2 Human 6.3 pIC50 = 6.3 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 596 10 1 7 5.4 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5[nH]4)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10097-X
CHEMBL330499 112739 0 None -3 2 Human 6.3 pIC50 = 6.3 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 596 10 1 7 5.4 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5[nH]4)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10097-X
10190413 207329 0 None -3 2 Human 6.3 pIC50 = 6.3 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 717 13 0 10 6.3 COc1ccc(C2(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccccn4)CC3)CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C2)cc1 10.1016/S0960-894X(97)10097-X
CHEMBL410270 207329 0 None -3 2 Human 6.3 pIC50 = 6.3 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 717 13 0 10 6.3 COc1ccc(C2(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccccn4)CC3)CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C2)cc1 10.1016/S0960-894X(97)10097-X
CHEMBL93519 207329 0 None -3 2 Human 6.3 pIC50 = 6.3 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 717 13 0 10 6.3 COc1ccc(C2(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccccn4)CC3)CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C2)cc1 10.1016/S0960-894X(97)10097-X
54579957 62728 5 None 36 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay
ChEMBL 291 3 0 3 3.3 CN1CCc2c(c3ccccc3n2CCc2ccncc2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783964 62728 5 None 36 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay
ChEMBL 291 3 0 3 3.3 CN1CCc2c(c3ccccc3n2CCc2ccncc2)C1 10.1016/j.bmcl.2009.04.128
44126329 62718 6 None -2 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 305 3 0 3 3.6 Cc1ccc2c(c1)c1c(n2CCc2ccccn2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783954 62718 6 None -2 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 305 3 0 3 3.6 Cc1ccc2c(c1)c1c(n2CCc2ccccn2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
44126330 62724 5 None -2 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 305 3 0 3 3.6 Cc1ccc2c(c1)c1c(n2CCc2cccnc2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783960 62724 5 None -2 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 305 3 0 3 3.6 Cc1ccc2c(c1)c1c(n2CCc2cccnc2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
13623348 59042 0 None - 1 Guinea pig 6.3 pIC50 = 6.3 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 300 5 0 4 3.2 CCCC(C)Cn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
CHEMBL16939 59042 0 None - 1 Guinea pig 6.3 pIC50 = 6.3 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 300 5 0 4 3.2 CCCC(C)Cn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
10423703 107295 0 None - 1 Guinea pig 5.3 pIC50 = 5.3 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 278 5 0 3 2.5 Cc1cccc(C2SCC(=O)N2CCCN(C)C)c1 10.1021/jm00093a025
CHEMBL1202942 107295 0 None - 1 Guinea pig 5.3 pIC50 = 5.3 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 278 5 0 3 2.5 Cc1cccc(C2SCC(=O)N2CCCN(C)C)c1 10.1021/jm00093a025
CHEMBL317171 107295 0 None - 1 Guinea pig 5.3 pIC50 = 5.3 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 278 5 0 3 2.5 Cc1cccc(C2SCC(=O)N2CCCN(C)C)c1 10.1021/jm00093a025
10300214 84199 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 492 9 2 5 5.0 O=C(Nc1ccccc1OCC(O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)C1CCC1 10.1016/j.bmcl.2012.09.113
CHEMBL2208416 84199 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 492 9 2 5 5.0 O=C(Nc1ccccc1OCC(O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)C1CCC1 10.1016/j.bmcl.2012.09.113
15830914 98906 0 None - 1 Guinea pig 7.3 pIC50 = 7.3 Functional
In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum
ChEMBL 245 1 1 1 3.5 C1=C2C(=C(c3ccccc3)c3ccccc32)CNC1 10.1016/s0960-894x(00)00199-2
CHEMBL279297 98906 0 None - 1 Guinea pig 7.3 pIC50 = 7.3 Functional
In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum
ChEMBL 245 1 1 1 3.5 C1=C2C(=C(c3ccccc3)c3ccccc32)CNC1 10.1016/s0960-894x(00)00199-2
13623351 61156 0 None - 1 Guinea pig 6.3 pIC50 = 6.3 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 318 6 0 5 2.9 CCSCCCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
CHEMBL17655 61156 0 None - 1 Guinea pig 6.3 pIC50 = 6.3 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 318 6 0 5 2.9 CCSCCCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
54582940 62722 5 None 1 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 359 3 0 3 4.3 CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783958 62722 5 None 1 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 359 3 0 3 4.3 CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
2600 3779 74 None 4 32 Human 6.3 pIC50 = 6.3 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1016/S0960-894X(97)10097-X
2608 3779 74 None 4 32 Human 6.3 pIC50 = 6.3 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1016/S0960-894X(97)10097-X
5405 3779 74 None 4 32 Human 6.3 pIC50 = 6.3 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1016/S0960-894X(97)10097-X
CHEMBL17157 3779 74 None 4 32 Human 6.3 pIC50 = 6.3 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1016/S0960-894X(97)10097-X
DB00342 3779 74 None 4 32 Human 6.3 pIC50 = 6.3 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1016/S0960-894X(97)10097-X
10917690 207605 1 None -3 4 Human 7.2 pIC50 = 7.2 Functional
Compound was evaluated for the antagonistic activity against H1 receptorCompound was evaluated for the antagonistic activity against H1 receptor
ChEMBL 471 8 0 5 5.4 COc1ccc(CCN2CCC(C(=O)c3nc4ccccc4n3Cc3ccc(F)cc3)CC2)cc1 10.1016/S0960-894X(97)10097-X
CHEMBL95051 207605 1 None -3 4 Human 7.2 pIC50 = 7.2 Functional
Compound was evaluated for the antagonistic activity against H1 receptorCompound was evaluated for the antagonistic activity against H1 receptor
ChEMBL 471 8 0 5 5.4 COc1ccc(CCN2CCC(C(=O)c3nc4ccccc4n3Cc3ccc(F)cc3)CC2)cc1 10.1016/S0960-894X(97)10097-X
44328320 207601 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 802 17 0 11 7.5 COC(=O)c1ccccc1OCCCCn1c(C(=O)C2CCN(CCC3(c4ccccc4)CCN(C(=O)c4cc(OC)c(OC)c(OC)c4)C3)CC2)nc2ccccc21 10.1016/S0960-894X(97)10098-1
CHEMBL95029 207601 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 802 17 0 11 7.5 COC(=O)c1ccccc1OCCCCn1c(C(=O)C2CCN(CCC3(c4ccccc4)CCN(C(=O)c4cc(OC)c(OC)c(OC)c4)C3)CC2)nc2ccccc21 10.1016/S0960-894X(97)10098-1
10147218 107466 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 778 15 0 10 7.5 CCOC(=O)CCCn1c(C(=O)C2CCN(CCC3(c4ccc(Cl)c(Cl)c4)CCN(C(=O)c4cc(OC)c(OC)c(OC)c4)C3)CC2)nc2ccccc21 10.1016/S0960-894X(97)10098-1
CHEMBL318369 107466 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 778 15 0 10 7.5 CCOC(=O)CCCn1c(C(=O)C2CCN(CCC3(c4ccc(Cl)c(Cl)c4)CCN(C(=O)c4cc(OC)c(OC)c(OC)c4)C3)CC2)nc2ccccc21 10.1016/S0960-894X(97)10098-1
10169609 207645 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 804 15 0 12 6.7 COC(=O)c1ccc(Cn2c(C(=O)C3CCN(CCC4(c5ccc(OC)c(OC)c5)CCN(C(=O)c5cc(OC)c(OC)c(OC)c5)C4)CC3)nc3ccccc32)cc1 10.1016/S0960-894X(97)10098-1
CHEMBL95243 207645 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 804 15 0 12 6.7 COC(=O)c1ccc(Cn2c(C(=O)C3CCN(CCC4(c5ccc(OC)c(OC)c5)CCN(C(=O)c5cc(OC)c(OC)c(OC)c5)C4)CC3)nc3ccccc32)cc1 10.1016/S0960-894X(97)10098-1
3219 199795 60 None - 1 Guinea pig 8.2 pIC50 = 8.2 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 302 5 0 5 2.2 CCOCCn1c(N2CCCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
CHEMBL594 199795 60 None - 1 Guinea pig 8.2 pIC50 = 8.2 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 302 5 0 5 2.2 CCOCCn1c(N2CCCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
44328188 111526 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 728 16 0 11 5.9 CCOCCn1c(C(=O)C2CCN(CCC3(c4ccc(OC)c(OC)c4)CCN(C(=O)c4cc(OC)c(OC)c(OC)c4)C3)CC2)nc2ccccc21 10.1016/S0960-894X(97)10098-1
CHEMBL327888 111526 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 728 16 0 11 5.9 CCOCCn1c(C(=O)C2CCN(CCC3(c4ccc(OC)c(OC)c4)CCN(C(=O)c4cc(OC)c(OC)c(OC)c4)C3)CC2)nc2ccccc21 10.1016/S0960-894X(97)10098-1
15542880 207506 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 705 12 0 9 6.4 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccccn4)CC3)(c3ccc(F)cc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
CHEMBL94480 207506 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 705 12 0 9 6.4 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccccn4)CC3)(c3ccc(F)cc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
10284042 207986 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 777 13 0 10 6.5 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4CCN4CCOCC4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
CHEMBL97240 207986 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 777 13 0 10 6.5 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4CCN4CCOCC4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
10121390 112739 0 None -3 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 596 10 1 7 5.4 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5[nH]4)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
CHEMBL330499 112739 0 None -3 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 596 10 1 7 5.4 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5[nH]4)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
10190413 207329 0 None -3 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 717 13 0 10 6.3 COc1ccc(C2(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccccn4)CC3)CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C2)cc1 10.1016/S0960-894X(97)10098-1
CHEMBL410270 207329 0 None -3 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 717 13 0 10 6.3 COc1ccc(C2(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccccn4)CC3)CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C2)cc1 10.1016/S0960-894X(97)10098-1
CHEMBL93519 207329 0 None -3 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 717 13 0 10 6.3 COc1ccc(C2(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccccn4)CC3)CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C2)cc1 10.1016/S0960-894X(97)10098-1
15542673 207564 0 None -1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 772 12 0 8 8.0 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(C(F)(F)F)cc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
CHEMBL94834 207564 0 None -1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 772 12 0 8 8.0 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(C(F)(F)F)cc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
15542869 207609 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 720 15 0 10 6.6 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4CCOCc4ccco4)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
CHEMBL95076 207609 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 720 15 0 10 6.6 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4CCOCc4ccco4)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
10283825 96693 0 None -1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 740 12 0 8 7.3 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(F)cc3F)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
CHEMBL264007 96693 0 None -1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 740 12 0 8 7.3 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(F)cc3F)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
10147107 207620 0 None -3 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 755 12 0 9 7.6 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccccn4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
CHEMBL431850 207620 0 None -3 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 755 12 0 9 7.6 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccccn4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
CHEMBL95125 207620 0 None -3 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 755 12 0 9 7.6 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccccn4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
15542881 112591 0 None -3 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 687 12 0 9 6.3 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4cccnc4)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
CHEMBL330172 112591 0 None -3 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 687 12 0 9 6.3 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4cccnc4)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
15542679 108527 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 664 10 1 7 6.7 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5[nH]4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
CHEMBL320003 108527 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 664 10 1 7 6.7 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5[nH]4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
10122529 109556 0 None -3 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 668 14 0 9 5.9 CCOCCn1c(C(=O)C2CCN(CCC3(c4ccccc4)CCN(C(=O)c4cc(OC)c(OC)c(OC)c4)C3)CC2)nc2ccccc21 10.1016/S0960-894X(97)10098-1
CHEMBL322194 109556 0 None -3 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 668 14 0 9 5.9 CCOCCn1c(C(=O)C2CCN(CCC3(c4ccccc4)CCN(C(=O)c4cc(OC)c(OC)c(OC)c4)C3)CC2)nc2ccccc21 10.1016/S0960-894X(97)10098-1
10233656 207851 0 None -3 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 687 12 0 9 6.3 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccccn4)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
CHEMBL96442 207851 0 None -3 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 687 12 0 9 6.3 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccccn4)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
18333241 207793 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 736 14 0 9 7.2 CCOCCn1c(C(=O)C2CCN(CCC3(c4ccc(Cl)c(Cl)c4)CCN(C(=O)c4cc(OC)c(OC)c(OC)c4)C3)CC2)nc2ccccc21 10.1016/S0960-894X(97)10098-1
CHEMBL96141 207793 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 736 14 0 9 7.2 CCOCCn1c(C(=O)C2CCN(CCC3(c4ccc(Cl)c(Cl)c4)CCN(C(=O)c4cc(OC)c(OC)c(OC)c4)C3)CC2)nc2ccccc21 10.1016/S0960-894X(97)10098-1
9918576 207337 0 None -2 3 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 764 14 0 10 7.0 COc1ccc(C2(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C2)cc1OC 10.1016/S0960-894X(97)10098-1
CHEMBL93556 207337 0 None -2 3 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 764 14 0 10 7.0 COc1ccc(C2(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C2)cc1OC 10.1016/S0960-894X(97)10098-1
10168749 207621 0 None -3 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 676 12 0 9 6.5 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccco4)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
CHEMBL95127 207621 0 None -3 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 676 12 0 9 6.5 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccco4)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
15542879 112824 0 None -2 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 687 12 0 9 6.3 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccncc4)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
CHEMBL330719 112824 0 None -2 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 687 12 0 9 6.3 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccncc4)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
10190770 208015 0 None -1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 772 12 0 8 8.3 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
CHEMBL330430 208015 0 None -1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 772 12 0 8 8.3 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
CHEMBL97357 208015 0 None -1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 772 12 0 8 8.3 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
10190638 207542 0 None -1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 748 12 0 10 6.7 COc1ccc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc4c(c3)OCO4)C2)c(OC)c1OC 10.1016/S0960-894X(97)10098-1
CHEMBL94726 207542 0 None -1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 748 12 0 10 6.7 COc1ccc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc4c(c3)OCO4)C2)c(OC)c1OC 10.1016/S0960-894X(97)10098-1
10283765 108087 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 730 12 0 8 7.4 CC(C)Oc1cccc(CC(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc4c(c3)OCO4)C2)c1 10.1016/S0960-894X(97)10098-1
CHEMBL319535 108087 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 730 12 0 8 7.4 CC(C)Oc1cccc(CC(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc4c(c3)OCO4)C2)c1 10.1016/S0960-894X(97)10098-1
18333379 207575 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 686 15 0 9 5.9 CCOCCn1c(C(=O)C2CCN(CCC3(c4ccc(F)cc4)CCN(Cc4cc(OC)c(OC)c(OC)c4)C3=O)CC2)nc2ccccc21 10.1016/S0960-894X(97)10098-1
CHEMBL94906 207575 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 686 15 0 9 5.9 CCOCCn1c(C(=O)C2CCN(CCC3(c4ccc(F)cc4)CCN(Cc4cc(OC)c(OC)c(OC)c4)C3=O)CC2)nc2ccccc21 10.1016/S0960-894X(97)10098-1
10190056 111438 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 674 11 0 7 7.0 COc1ccc(C2(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)CCN(C(=O)c3ccccc3)C2)cc1OC 10.1016/S0960-894X(97)10098-1
CHEMBL327497 111438 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 674 11 0 7 7.0 COc1ccc(C2(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)CCN(C(=O)c3ccccc3)C2)cc1OC 10.1016/S0960-894X(97)10098-1
10212223 208140 0 None -2 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 704 12 0 8 7.0 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
CHEMBL431458 208140 0 None -2 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 704 12 0 8 7.0 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
CHEMBL98079 208140 0 None -2 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 704 12 0 8 7.0 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
15542874 112169 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 786 12 0 8 8.7 COc1cc(C(=O)N2CCCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
CHEMBL329055 112169 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 786 12 0 8 8.7 COc1cc(C(=O)N2CCCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
10123138 108526 0 None -1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 748 12 0 10 6.7 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc4c(c3)OCO4)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
CHEMBL317524 108526 0 None -1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 748 12 0 10 6.7 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc4c(c3)OCO4)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
CHEMBL320002 108526 0 None -1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 748 12 0 10 6.7 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc4c(c3)OCO4)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10098-1
9832306 112724 0 None 2 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 806 17 0 10 8.2 CCOc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(OC)c(OC)c3)C2)cc(OCC)c1OCC 10.1016/S0960-894X(97)10098-1
CHEMBL330367 112724 0 None 2 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 806 17 0 10 8.2 CCOc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(OC)c(OC)c3)C2)cc(OCC)c1OCC 10.1016/S0960-894X(97)10098-1
CHEMBL330462 112724 0 None 2 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 806 17 0 10 8.2 CCOc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(OC)c(OC)c3)C2)cc(OCC)c1OCC 10.1016/S0960-894X(97)10098-1
15542871 207855 0 None -1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 726 9 0 7 8.0 O=C(c1nc2ccccc2n1Cc1ccc(F)cc1)C1CCN(CCC2(c3ccc4c(c3)OCO4)CCN(C(=O)c3ccc(Cl)cc3Cl)C2)CC1 10.1016/S0960-894X(97)10098-1
CHEMBL96466 207855 0 None -1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 726 9 0 7 8.0 O=C(c1nc2ccccc2n1Cc1ccc(F)cc1)C1CCN(CCC2(c3ccc4c(c3)OCO4)CCN(C(=O)c3ccc(Cl)cc3Cl)C2)CC1 10.1016/S0960-894X(97)10098-1
3071016 98578 1 None - 1 Guinea pig 8.2 pIC50 = 8.2 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 336 5 0 5 2.9 CN1CCN(c2nc3ccccc3n2CCOc2ccccc2)CC1 10.1021/jm00157a010
CHEMBL276735 98578 1 None - 1 Guinea pig 8.2 pIC50 = 8.2 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 336 5 0 5 2.9 CN1CCN(c2nc3ccccc3n2CCOc2ccccc2)CC1 10.1021/jm00157a010
14984032 208341 1 None - 1 Guinea pig 4.2 pIC50 = 4.2 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 342 5 0 3 3.0 CN(C)CCCN1C(=O)CSC1c1cccc(Br)c1 10.1021/jm00093a025
CHEMBL1202932 208341 1 None - 1 Guinea pig 4.2 pIC50 = 4.2 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 342 5 0 3 3.0 CN(C)CCCN1C(=O)CSC1c1cccc(Br)c1 10.1021/jm00093a025
CHEMBL99350 208341 1 None - 1 Guinea pig 4.2 pIC50 = 4.2 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 342 5 0 3 3.0 CN(C)CCCN1C(=O)CSC1c1cccc(Br)c1 10.1021/jm00093a025
54579956 62720 5 None 3 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay
ChEMBL 309 3 0 3 3.4 CN1CCc2c(c3cc(F)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783956 62720 5 None 3 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay
ChEMBL 309 3 0 3 3.4 CN1CCc2c(c3cc(F)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
54586813 62725 5 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 309 3 0 3 3.4 CN1CCc2c(c3cc(F)ccc3n2CCc2cccnc2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783961 62725 5 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 309 3 0 3 3.4 CN1CCc2c(c3cc(F)ccc3n2CCc2cccnc2)C1 10.1016/j.bmcl.2009.04.128
44126325 199114 5 None 10 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge
ChEMBL 334 4 0 3 4.2 COc1ccc(CCn2c3c(c4cc(C)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
CHEMBL589147 199114 5 None 10 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge
ChEMBL 334 4 0 3 4.2 COc1ccc(CCn2c3c(c4cc(C)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
44126272 199150 5 None 14 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge
ChEMBL 358 3 0 2 4.9 CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2ccccc2)C1 10.1016/j.bmcl.2009.11.037
CHEMBL589388 199150 5 None 14 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge
ChEMBL 358 3 0 2 4.9 CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2ccccc2)C1 10.1016/j.bmcl.2009.11.037
13623349 98583 0 None - 1 Guinea pig 7.2 pIC50 = 7.2 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 304 5 0 5 2.9 CCCSCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
CHEMBL276774 98583 0 None - 1 Guinea pig 7.2 pIC50 = 7.2 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 304 5 0 5 2.9 CCCSCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
16082828 80260 0 None -398 3 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human H1 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assayAntagonist activity at human H1 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay
ChEMBL 275 6 2 2 3.3 Clc1ccc(CNCC[C@@H]2C[C@H]2c2c[nH]cn2)cc1 10.1021/jm0603318
CHEMBL213886 80260 0 None -398 3 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human H1 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assayAntagonist activity at human H1 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay
ChEMBL 275 6 2 2 3.3 Clc1ccc(CNCC[C@@H]2C[C@H]2c2c[nH]cn2)cc1 10.1021/jm0603318
10917690 207605 1 None -3 4 Human 8.1 pIC50 = 8.1 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 471 8 0 5 5.4 COc1ccc(CCN2CCC(C(=O)c3nc4ccccc4n3Cc3ccc(F)cc3)CC2)cc1 10.1016/S0960-894X(97)10098-1
CHEMBL95051 207605 1 None -3 4 Human 8.1 pIC50 = 8.1 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 471 8 0 5 5.4 COc1ccc(CCN2CCC(C(=O)c3nc4ccccc4n3Cc3ccc(F)cc3)CC2)cc1 10.1016/S0960-894X(97)10098-1
44328187 208139 0 None -1 2 Human 8.1 pIC50 = 8.1 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 456 7 0 5 5.6 COc1ccc(CCN2CCC(=Nc3nc4ccccc4n3Cc3ccc(F)cc3)CC2)cc1 10.1016/S0960-894X(97)10098-1
CHEMBL98076 208139 0 None -1 2 Human 8.1 pIC50 = 8.1 Functional
Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor
ChEMBL 456 7 0 5 5.6 COc1ccc(CCN2CCC(=Nc3nc4ccccc4n3Cc3ccc(F)cc3)CC2)cc1 10.1016/S0960-894X(97)10098-1
13623370 98391 0 None - 1 Guinea pig 8.1 pIC50 = 8.1 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 358 9 0 5 3.8 CCCCCN1CCCN(c2nc3ccccc3n2CCOCC)CC1 10.1021/jm00157a010
CHEMBL275383 98391 0 None - 1 Guinea pig 8.1 pIC50 = 8.1 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 358 9 0 5 3.8 CCCCCN1CCCN(c2nc3ccccc3n2CCOCC)CC1 10.1021/jm00157a010
46224879 201547 3 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge
ChEMBL 302 2 0 2 4.6 Cc1ccc2c(c1)c1c(n2/C=C\c2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL605405 201547 3 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge
ChEMBL 302 2 0 2 4.6 Cc1ccc2c(c1)c1c(n2/C=C\c2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
54581998 62735 3 None 5 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 368 4 0 4 4.3 CN1CCc2c(c3cc(-c4cccnc4)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783972 62735 3 None 5 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 368 4 0 4 4.3 CN1CCc2c(c3cc(-c4cccnc4)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
54585846 62727 5 None 38 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay
ChEMBL 323 3 0 3 3.7 Cc1ccc(CCn2c3c(c4cc(F)ccc42)CN(C)CC3)cn1 10.1016/j.bmcl.2009.04.128
CHEMBL1783963 62727 5 None 38 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay
ChEMBL 323 3 0 3 3.7 Cc1ccc(CCn2c3c(c4cc(F)ccc42)CN(C)CC3)cn1 10.1016/j.bmcl.2009.04.128
54583939 62737 5 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 388 4 0 4 4.0 Cc1ccc2c(c1)c1c(n2CCc2ccncc2)CCN(C2CCN(C)CC2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783975 62737 5 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 388 4 0 4 4.0 Cc1ccc2c(c1)c1c(n2CCc2ccncc2)CCN(C2CCN(C)CC2)C1 10.1016/j.bmcl.2009.04.128
13623340 59041 0 None - 1 Guinea pig 6.1 pIC50 = 6.1 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 292 2 0 4 2.8 CN1CCN(c2nc3ccccc3n2-c2ccccc2)CC1 10.1021/jm00157a010
CHEMBL16938 59041 0 None - 1 Guinea pig 6.1 pIC50 = 6.1 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 292 2 0 4 2.8 CN1CCN(c2nc3ccccc3n2-c2ccccc2)CC1 10.1021/jm00157a010
54583938 62733 0 None 1 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay
ChEMBL 306 3 0 4 3.0 Cc1ccc2c(c1)c1c(n2CCc2cnccn2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783970 62733 0 None 1 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay
ChEMBL 306 3 0 4 3.0 Cc1ccc2c(c1)c1c(n2CCc2cnccn2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
13623369 62393 0 None - 1 Guinea pig 8.1 pIC50 = 8.1 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 344 8 0 5 3.4 CCCCN1CCCN(c2nc3ccccc3n2CCOCC)CC1 10.1021/jm00157a010
CHEMBL17795 62393 0 None - 1 Guinea pig 8.1 pIC50 = 8.1 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 344 8 0 5 3.4 CCCCN1CCCN(c2nc3ccccc3n2CCOCC)CC1 10.1021/jm00157a010
13623368 162246 0 None - 1 Guinea pig 8.1 pIC50 = 8.1 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 330 7 0 5 3.0 CCCN1CCCN(c2nc3ccccc3n2CCOCC)CC1 10.1021/jm00157a010
CHEMBL416357 162246 0 None - 1 Guinea pig 8.1 pIC50 = 8.1 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 330 7 0 5 3.0 CCCN1CCCN(c2nc3ccccc3n2CCOCC)CC1 10.1021/jm00157a010
13623362 98083 0 None - 1 Guinea pig 8.1 pIC50 = 8.1 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 358 10 0 5 3.8 CCCCCCN1CCN(c2nc3ccccc3n2CCOCC)CC1 10.1021/jm00157a010
CHEMBL273315 98083 0 None - 1 Guinea pig 8.1 pIC50 = 8.1 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 358 10 0 5 3.8 CCCCCCN1CCN(c2nc3ccccc3n2CCOCC)CC1 10.1021/jm00157a010
16082831 80346 0 None -1000 3 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human H1 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assayAntagonist activity at human H1 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay
ChEMBL 275 6 2 2 3.3 Clc1ccc(CNCC[C@H]2C[C@@H]2c2c[nH]cn2)cc1 10.1021/jm0603318
CHEMBL214311 80346 0 None -1000 3 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human H1 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assayAntagonist activity at human H1 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay
ChEMBL 275 6 2 2 3.3 Clc1ccc(CNCC[C@H]2C[C@@H]2c2c[nH]cn2)cc1 10.1021/jm0603318
13623353 60498 0 None - 1 Guinea pig 6.1 pIC50 = 6.1 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 288 5 0 5 1.8 COCCCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
CHEMBL17556 60498 0 None - 1 Guinea pig 6.1 pIC50 = 6.1 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 288 5 0 5 1.8 COCCCn1c(N2CCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
11976 920 59 None -9 16 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1021/jm300671m
667467 920 59 None -9 16 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1021/jm300671m
CHEMBL908 920 59 None -9 16 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1021/jm300671m
DB01239 920 59 None -9 16 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1021/jm300671m
3071012 163290 1 None - 1 Guinea pig 8.0 pIC50 = 8.0 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 350 5 0 5 3.3 CN1CCCN(c2nc3ccccc3n2CCOc2ccccc2)CC1 10.1021/jm00157a010
CHEMBL418731 163290 1 None - 1 Guinea pig 8.0 pIC50 = 8.0 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 350 5 0 5 3.3 CN1CCCN(c2nc3ccccc3n2CCOc2ccccc2)CC1 10.1021/jm00157a010
3070998 98981 1 None - 1 Guinea pig 8.0 pIC50 = 8 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 312 5 0 5 1.8 C#CCOCCn1c(N2CCCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
CHEMBL279875 98981 1 None - 1 Guinea pig 8.0 pIC50 = 8 Functional
In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum
ChEMBL 312 5 0 5 1.8 C#CCOCCn1c(N2CCCN(C)CC2)nc2ccccc21 10.1021/jm00157a010
145963961 164403 0 None -416 6 Human 6.0 pIC50 = 6.0 Functional
Antagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 425 8 1 7 3.0 CNC(=O)c1cc(OCCCCN2CCN(c3nsc4ccccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
CHEMBL4213342 164403 0 None -416 6 Human 6.0 pIC50 = 6.0 Functional
Antagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 425 8 1 7 3.0 CNC(=O)c1cc(OCCCCN2CCN(c3nsc4ccccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
54586812 62717 5 None 12 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay
ChEMBL 291 3 0 3 3.3 CN1CCc2c(c3ccccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783953 62717 5 None 12 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay
ChEMBL 291 3 0 3 3.3 CN1CCc2c(c3ccccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
54586813 62725 5 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay
ChEMBL 309 3 0 3 3.4 CN1CCc2c(c3cc(F)ccc3n2CCc2cccnc2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783961 62725 5 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay
ChEMBL 309 3 0 3 3.4 CN1CCc2c(c3cc(F)ccc3n2CCc2cccnc2)C1 10.1016/j.bmcl.2009.04.128
54579956 62720 5 None 3 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 309 3 0 3 3.4 CN1CCc2c(c3cc(F)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783956 62720 5 None 3 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay
ChEMBL 309 3 0 3 3.4 CN1CCc2c(c3cc(F)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
10212645 13289 0 None -346 2 Human 5.0 pIC50 = 5.0 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 774 16 1 10 7.0 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4CCCOc4ccccc4C(=O)O)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10097-X
CHEMBL1191766 13289 0 None -346 2 Human 5.0 pIC50 = 5.0 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 774 16 1 10 7.0 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4CCCOc4ccccc4C(=O)O)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10097-X
CHEMBL542908 13289 0 None -346 2 Human 5.0 pIC50 = 5.0 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 774 16 1 10 7.0 COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4CCCOc4ccccc4C(=O)O)CC3)(c3ccccc3)C2)cc(OC)c1OC 10.1016/S0960-894X(97)10097-X
4601 206747 35 None -549 19 Human 4.0 pIC50 = 4.0 Functional
Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 10.1021/jm300671m
CHEMBL1201023 206747 35 None -549 19 Human 4.0 pIC50 = 4.0 Functional
Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 10.1021/jm300671m
CHEMBL900 206747 35 None -549 19 Human 4.0 pIC50 = 4.0 Functional
Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 10.1021/jm300671m
44126327 201653 5 None 41 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge
ChEMBL 372 3 0 2 5.2 Cc1ccc2c(c1)c1c(n2CCc2ccc(C(F)(F)F)cc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL606036 201653 5 None 41 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge
ChEMBL 372 3 0 2 5.2 Cc1ccc2c(c1)c1c(n2CCc2ccc(C(F)(F)F)cc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
10190842 107224 0 None -63 2 Human 6.0 pIC50 = 6 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 788 16 0 11 7.1 COC(=O)c1ccccc1OCCCn1c(C(=O)C2CCN(CCC3(c4ccccc4)CCN(C(=O)c4cc(OC)c(OC)c(OC)c4)C3)CC2)nc2ccccc21 10.1016/S0960-894X(97)10097-X
CHEMBL316705 107224 0 None -63 2 Human 6.0 pIC50 = 6 Functional
Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor
ChEMBL 788 16 0 11 7.1 COC(=O)c1ccccc1OCCCn1c(C(=O)C2CCN(CCC3(c4ccccc4)CCN(C(=O)c4cc(OC)c(OC)c(OC)c4)C3)CC2)nc2ccccc21 10.1016/S0960-894X(97)10097-X
71461781 80469 0 None - 0 Human 10.4 pKd = 10.4 Functional
Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay
ChEMBL 409 7 0 4 4.9 CCCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1016/j.bmc.2012.08.032
CHEMBL2146802 80469 0 None - 0 Human 10.4 pKd = 10.4 Functional
Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay
ChEMBL 409 7 0 4 4.9 CCCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1016/j.bmc.2012.08.032
15254720 61301 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay
ChEMBL 367 4 0 4 3.7 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1016/j.bmc.2012.08.032
CHEMBL1767136 61301 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay
ChEMBL 367 4 0 4 3.7 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1016/j.bmc.2012.08.032
71461782 80473 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay
ChEMBL 410 7 0 5 4.3 CCCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cnccc2c1=O 10.1016/j.bmc.2012.08.032
CHEMBL2146806 80473 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay
ChEMBL 410 7 0 5 4.3 CCCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cnccc2c1=O 10.1016/j.bmc.2012.08.032
2267 559 71 None 32 14 Human 9.7 pKd = 9.7 Functional
Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmc.2012.08.032
271 559 71 None 32 14 Human 9.7 pKd = 9.7 Functional
Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmc.2012.08.032
7121 559 71 None 32 14 Human 9.7 pKd = 9.7 Functional
Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmc.2012.08.032
CHEMBL639 559 71 None 32 14 Human 9.7 pKd = 9.7 Functional
Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmc.2012.08.032
DB00972 559 71 None 32 14 Human 9.7 pKd = 9.7 Functional
Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmc.2012.08.032
2267 559 71 None 32 14 Human 9.7 pKd = 9.7 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmcl.2016.11.022
271 559 71 None 32 14 Human 9.7 pKd = 9.7 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmcl.2016.11.022
7121 559 71 None 32 14 Human 9.7 pKd = 9.7 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmcl.2016.11.022
CHEMBL639 559 71 None 32 14 Human 9.7 pKd = 9.7 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmcl.2016.11.022
DB00972 559 71 None 32 14 Human 9.7 pKd = 9.7 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmcl.2016.11.022
2267 559 71 None 32 14 Human 9.7 pKd = 9.7 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmcl.2017.09.020
271 559 71 None 32 14 Human 9.7 pKd = 9.7 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmcl.2017.09.020
7121 559 71 None 32 14 Human 9.7 pKd = 9.7 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmcl.2017.09.020
CHEMBL639 559 71 None 32 14 Human 9.7 pKd = 9.7 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmcl.2017.09.020
DB00972 559 71 None 32 14 Human 9.7 pKd = 9.7 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmcl.2017.09.020
24824726 161109 1 None - 0 Human 9.7 pKd = 9.7 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 496 11 1 6 3.6 COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1016/j.bmcl.2017.09.020
CHEMBL4060529 161109 1 None - 0 Human 9.7 pKd = 9.7 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 496 11 1 6 3.6 COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1016/j.bmcl.2017.09.020
CHEMBL4117079 161109 1 None - 0 Human 9.7 pKd = 9.7 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 496 11 1 6 3.6 COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1016/j.bmcl.2017.09.020
CHEMBL5282336 161109 1 None - 0 Human 9.7 pKd = 9.7 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 496 11 1 6 3.6 COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1016/j.bmcl.2017.09.020
CHEMBL5286389 161109 1 None - 0 Human 9.7 pKd = 9.7 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 496 11 1 6 3.6 COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1016/j.bmcl.2017.09.020
25189511 161118 0 None - 0 Human 9.7 pKd = 9.7 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 461 13 1 5 4.5 CCCCc1cc(OC2CCN(CCCCNS(=O)(=O)CCC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4059750 161118 0 None - 0 Human 9.7 pKd = 9.7 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 461 13 1 5 4.5 CCCCc1cc(OC2CCN(CCCCNS(=O)(=O)CCC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4117137 161118 0 None - 0 Human 9.7 pKd = 9.7 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 461 13 1 5 4.5 CCCCc1cc(OC2CCN(CCCCNS(=O)(=O)CCC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
2267 559 71 None 32 14 Human 9.7 pKd = 9.7 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1021/jm1013874
271 559 71 None 32 14 Human 9.7 pKd = 9.7 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1021/jm1013874
7121 559 71 None 32 14 Human 9.7 pKd = 9.7 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1021/jm1013874
CHEMBL639 559 71 None 32 14 Human 9.7 pKd = 9.7 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1021/jm1013874
DB00972 559 71 None 32 14 Human 9.7 pKd = 9.7 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1021/jm1013874
71452871 80468 0 None - 0 Human 9.6 pKd = 9.6 Functional
Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay
ChEMBL 412 7 0 6 3.1 COCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cnccc2c1=O 10.1016/j.bmc.2012.08.032
CHEMBL2146801 80468 0 None - 0 Human 9.6 pKd = 9.6 Functional
Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay
ChEMBL 412 7 0 6 3.1 COCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cnccc2c1=O 10.1016/j.bmc.2012.08.032
25190195 157912 0 None - 0 Human 9.6 pKd = 9.6 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 446 9 0 5 5.0 CCCCc1cc(OC2CCN(CCCS(=O)(=O)C(C)(C)C)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4084325 157912 0 None - 0 Human 9.6 pKd = 9.6 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 446 9 0 5 5.0 CCCCc1cc(OC2CCN(CCCS(=O)(=O)C(C)(C)C)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
71458203 80472 0 None - 0 Human 9.5 pKd = 9.5 Functional
Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay
ChEMBL 368 4 0 5 3.1 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cnccc2c1=O 10.1016/j.bmc.2012.08.032
CHEMBL2146805 80472 0 None - 0 Human 9.5 pKd = 9.5 Functional
Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay
ChEMBL 368 4 0 5 3.1 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cnccc2c1=O 10.1016/j.bmc.2012.08.032
71451044 80474 0 None - 0 Human 9.5 pKd = 9.5 Functional
Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay
ChEMBL 410 7 0 5 4.3 CCCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cccnc2c1=O 10.1016/j.bmc.2012.08.032
CHEMBL2146807 80474 0 None - 0 Human 9.5 pKd = 9.5 Functional
Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay
ChEMBL 410 7 0 5 4.3 CCCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cccnc2c1=O 10.1016/j.bmc.2012.08.032
71458204 80476 0 None - 0 Human 9.5 pKd = 9.5 Functional
Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay
ChEMBL 368 4 0 5 3.1 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ncccc2c1=O 10.1016/j.bmc.2012.08.032
CHEMBL2146809 80476 0 None - 0 Human 9.5 pKd = 9.5 Functional
Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay
ChEMBL 368 4 0 5 3.1 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ncccc2c1=O 10.1016/j.bmc.2012.08.032
1530 2182 50 None - 25 Guinea pig 9.5 pKd = 9.5 Functional
H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1021/jm00161a022
3827 2182 50 None - 25 Guinea pig 9.5 pKd = 9.5 Functional
H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1021/jm00161a022
7206 2182 50 None - 25 Guinea pig 9.5 pKd = 9.5 Functional
H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1021/jm00161a022
CHEMBL534 2182 50 None - 25 Guinea pig 9.5 pKd = 9.5 Functional
H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1021/jm00161a022
DB00920 2182 50 None - 25 Guinea pig 9.5 pKd = 9.5 Functional
H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1021/jm00161a022
1530 2182 50 None - 25 Guinea pig 9.5 pKd = 9.5 Functional
H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1021/jm00377a013
3827 2182 50 None - 25 Guinea pig 9.5 pKd = 9.5 Functional
H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1021/jm00377a013
7206 2182 50 None - 25 Guinea pig 9.5 pKd = 9.5 Functional
H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1021/jm00377a013
CHEMBL534 2182 50 None - 25 Guinea pig 9.5 pKd = 9.5 Functional
H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1021/jm00377a013
DB00920 2182 50 None - 25 Guinea pig 9.5 pKd = 9.5 Functional
H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1021/jm00377a013
25190192 160995 0 None - 0 Human 9.5 pKd = 9.5 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 418 10 0 5 4.2 CCCCc1cc(OC2CCN(CCCS(=O)(=O)CC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4098917 160995 0 None - 0 Human 9.5 pKd = 9.5 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 418 10 0 5 4.2 CCCCc1cc(OC2CCN(CCCS(=O)(=O)CC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4116155 160995 0 None - 0 Human 9.5 pKd = 9.5 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 418 10 0 5 4.2 CCCCc1cc(OC2CCN(CCCS(=O)(=O)CC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
1227 2489 43 None -2 14 Guinea pig 9.4 pKd = 9.4 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/s0960-894x(03)00113-6
2331 2489 43 None -2 14 Guinea pig 9.4 pKd = 9.4 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/s0960-894x(03)00113-6
3957 2489 43 None -2 14 Guinea pig 9.4 pKd = 9.4 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/s0960-894x(03)00113-6
4992 2489 43 None -2 14 Guinea pig 9.4 pKd = 9.4 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/s0960-894x(03)00113-6
CHEMBL511 2489 43 None -2 14 Guinea pig 9.4 pKd = 9.4 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/s0960-894x(03)00113-6
DB06691 2489 43 None -2 14 Guinea pig 9.4 pKd = 9.4 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/s0960-894x(03)00113-6
25190372 160975 0 None - 0 Human 9.4 pKd = 9.4 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 433 11 1 5 3.8 CCCCc1cc(OC2CCN(CCCCNS(C)(=O)=O)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4098192 160975 0 None - 0 Human 9.4 pKd = 9.4 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 433 11 1 5 3.8 CCCCc1cc(OC2CCN(CCCCNS(C)(=O)=O)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4115992 160975 0 None - 0 Human 9.4 pKd = 9.4 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 433 11 1 5 3.8 CCCCc1cc(OC2CCN(CCCCNS(C)(=O)=O)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
25190194 161162 0 None - 0 Human 9.4 pKd = 9.4 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 432 10 0 5 4.6 CCCCc1cc(OC2CCN(CCCS(=O)(=O)C(C)C)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4102287 161162 0 None - 0 Human 9.4 pKd = 9.4 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 432 10 0 5 4.6 CCCCc1cc(OC2CCN(CCCS(=O)(=O)C(C)C)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4117432 161162 0 None - 0 Human 9.4 pKd = 9.4 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 432 10 0 5 4.6 CCCCc1cc(OC2CCN(CCCS(=O)(=O)C(C)C)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
71452872 80434 0 None - 0 Human 9.3 pKd = 9.3 Functional
Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay
ChEMBL 368 4 0 5 3.1 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cccnc2c1=O 10.1016/j.bmc.2012.08.032
CHEMBL2146484 80434 0 None - 0 Human 9.3 pKd = 9.3 Functional
Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay
ChEMBL 368 4 0 5 3.1 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cccnc2c1=O 10.1016/j.bmc.2012.08.032
25164129 161160 0 None - 1 Human 9.3 pKd = 9.3 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 447 12 1 5 4.1 CCCCc1cc(OC2CCN(CCCCNS(=O)(=O)CC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4088036 161160 0 None - 1 Human 9.3 pKd = 9.3 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 447 12 1 5 4.1 CCCCc1cc(OC2CCN(CCCCNS(=O)(=O)CC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4117406 161160 0 None - 1 Human 9.3 pKd = 9.3 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 447 12 1 5 4.1 CCCCc1cc(OC2CCN(CCCCNS(=O)(=O)CC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
25189509 161072 0 None - 0 Human 9.2 pKd = 9.2 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 461 10 1 5 4.5 CCCCc1cc(OC2CCN(CCCS(=O)(=O)NC(C)(C)C)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4069073 161072 0 None - 0 Human 9.2 pKd = 9.2 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 461 10 1 5 4.5 CCCCc1cc(OC2CCN(CCCS(=O)(=O)NC(C)(C)C)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4116734 161072 0 None - 0 Human 9.2 pKd = 9.2 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 461 10 1 5 4.5 CCCCc1cc(OC2CCN(CCCS(=O)(=O)NC(C)(C)C)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
44320707 106030 0 None - 0 Guinea pig 9.2 pKd = 9.2 Functional
Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum
ChEMBL 293 4 1 2 2.9 CN(C)CCc1c[nH]c(-c2cccc(Br)c2)n1 10.1016/s0960-894x(98)00461-2
CHEMBL313301 106030 0 None - 0 Guinea pig 9.2 pKd = 9.2 Functional
Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum
ChEMBL 293 4 1 2 2.9 CN(C)CCc1c[nH]c(-c2cccc(Br)c2)n1 10.1016/s0960-894x(98)00461-2
10403687 2511 3 None 1 2 Guinea pig 9.1 pKd = 9.1 Functional
Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
1205 2511 3 None 1 2 Guinea pig 9.1 pKd = 9.1 Functional
Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
CHEMBL275035 2511 3 None 1 2 Guinea pig 9.1 pKd = 9.1 Functional
Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
25190193 161199 0 None - 0 Human 9.1 pKd = 9.1 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 432 11 0 5 4.6 CCCCc1cc(OC2CCN(CCCS(=O)(=O)CCC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4080880 161199 0 None - 0 Human 9.1 pKd = 9.1 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 432 11 0 5 4.6 CCCCc1cc(OC2CCN(CCCS(=O)(=O)CCC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4117740 161199 0 None - 0 Human 9.1 pKd = 9.1 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 432 11 0 5 4.6 CCCCc1cc(OC2CCN(CCCS(=O)(=O)CCC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
1194 45 3 None - 2 Guinea pig 9.1 pKd = 9.1 Functional
Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum
ChEMBL 265 3 2 2 2.3 NCCc1cnc([nH]1)c1cccc(c1)Br 10.1016/s0960-894x(98)00461-2
23786499 45 3 None - 2 Guinea pig 9.1 pKd = 9.1 Functional
Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum
ChEMBL 265 3 2 2 2.3 NCCc1cnc([nH]1)c1cccc(c1)Br 10.1016/s0960-894x(98)00461-2
CHEMBL26116 45 3 None - 2 Guinea pig 9.1 pKd = 9.1 Functional
Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum
ChEMBL 265 3 2 2 2.3 NCCc1cnc([nH]1)c1cccc(c1)Br 10.1016/s0960-894x(98)00461-2
44320708 206377 0 None - 0 Guinea pig 9.1 pKd = 9.1 Functional
Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum
ChEMBL 295 5 2 2 3.4 FC(F)(F)c1cccc(-c2nc(CCNC3CC3)c[nH]2)c1 10.1016/s0960-894x(98)00461-2
CHEMBL87583 206377 0 None - 0 Guinea pig 9.1 pKd = 9.1 Functional
Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum
ChEMBL 295 5 2 2 3.4 FC(F)(F)c1cccc(-c2nc(CCNC3CC3)c[nH]2)c1 10.1016/s0960-894x(98)00461-2
44320686 206453 1 None - 0 Guinea pig 9.1 pKd = 9.1 Functional
Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum
ChEMBL 279 4 2 2 2.6 CNCCc1c[nH]c(-c2cccc(Br)c2)n1 10.1016/s0960-894x(98)00461-2
CHEMBL88075 206453 1 None - 0 Guinea pig 9.1 pKd = 9.1 Functional
Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum
ChEMBL 279 4 2 2 2.6 CNCCc1c[nH]c(-c2cccc(Br)c2)n1 10.1016/s0960-894x(98)00461-2
10042467 1426 1 None -1 2 Guinea pig 9.1 pKd = 9.1 Functional
Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine
ChEMBL 333 8 1 2 4.3 CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C 10.1021/jm991056a
1203 1426 1 None -1 2 Guinea pig 9.1 pKd = 9.1 Functional
Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine
ChEMBL 333 8 1 2 4.3 CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C 10.1021/jm991056a
CHEMBL11553 1426 1 None -1 2 Guinea pig 9.1 pKd = 9.1 Functional
Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine
ChEMBL 333 8 1 2 4.3 CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C 10.1021/jm991056a
10447834 1933 4 None 2 3 Guinea pig 9.1 pKd = 9.1 Functional
Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
4026 1933 4 None 2 3 Guinea pig 9.1 pKd = 9.1 Functional
Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
CHEMBL275507 1933 4 None 2 3 Guinea pig 9.1 pKd = 9.1 Functional
Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
1204 1932 119 None -3 10 Guinea pig 9.1 pKd = 9.1 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nM
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm991056a
1247 1932 119 None -3 10 Guinea pig 9.1 pKd = 9.1 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nM
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm991056a
1375 1932 119 None -3 10 Guinea pig 9.1 pKd = 9.1 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nM
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm991056a
774 1932 119 None -3 10 Guinea pig 9.1 pKd = 9.1 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nM
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm991056a
CHEMBL90 1932 119 None -3 10 Guinea pig 9.1 pKd = 9.1 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nM
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm991056a
DB05381 1932 119 None -3 10 Guinea pig 9.1 pKd = 9.1 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nM
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm991056a
1204 1932 119 None -3 10 Guinea pig 9.1 pKd = 9.1 Functional
Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/s0960-894x(98)00461-2
1247 1932 119 None -3 10 Guinea pig 9.1 pKd = 9.1 Functional
Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/s0960-894x(98)00461-2
1375 1932 119 None -3 10 Guinea pig 9.1 pKd = 9.1 Functional
Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/s0960-894x(98)00461-2
774 1932 119 None -3 10 Guinea pig 9.1 pKd = 9.1 Functional
Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/s0960-894x(98)00461-2
CHEMBL90 1932 119 None -3 10 Guinea pig 9.1 pKd = 9.1 Functional
Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/s0960-894x(98)00461-2
DB05381 1932 119 None -3 10 Guinea pig 9.1 pKd = 9.1 Functional
Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/s0960-894x(98)00461-2
17747460 61329 12 None - 2 Human 9.1 pKd = 9.1 Functional
Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay
ChEMBL 640 14 0 6 7.8 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1016/j.bmc.2012.08.032
CHEMBL1767164 61329 12 None - 2 Human 9.1 pKd = 9.1 Functional
Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay
ChEMBL 640 14 0 6 7.8 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1016/j.bmc.2012.08.032
71456360 80475 0 None - 0 Human 9.1 pKd = 9.1 Functional
Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay
ChEMBL 412 7 0 6 3.1 COCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cccnc2c1=O 10.1016/j.bmc.2012.08.032
CHEMBL2146808 80475 0 None - 0 Human 9.1 pKd = 9.1 Functional
Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay
ChEMBL 412 7 0 6 3.1 COCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cccnc2c1=O 10.1016/j.bmc.2012.08.032
17747460 61329 12 None - 2 Human 9.1 pKd = 9.1 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 640 14 0 6 7.8 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1016/j.bmcl.2016.11.022
CHEMBL1767164 61329 12 None - 2 Human 9.1 pKd = 9.1 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 640 14 0 6 7.8 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1016/j.bmcl.2016.11.022
17747460 61329 12 None - 2 Human 9.1 pKd = 9.1 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assay
ChEMBL 640 14 0 6 7.8 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1021/jm1013874
CHEMBL1767164 61329 12 None - 2 Human 9.1 pKd = 9.1 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assay
ChEMBL 640 14 0 6 7.8 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1021/jm1013874
1227 2489 43 None -2 14 Guinea pig 9.1 pKd = 9.1 Functional
H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm00161a022
2331 2489 43 None -2 14 Guinea pig 9.1 pKd = 9.1 Functional
H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm00161a022
3957 2489 43 None -2 14 Guinea pig 9.1 pKd = 9.1 Functional
H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm00161a022
4992 2489 43 None -2 14 Guinea pig 9.1 pKd = 9.1 Functional
H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm00161a022
CHEMBL511 2489 43 None -2 14 Guinea pig 9.1 pKd = 9.1 Functional
H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm00161a022
DB06691 2489 43 None -2 14 Guinea pig 9.1 pKd = 9.1 Functional
H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm00161a022
13676700 204784 0 None - 0 Guinea pig 9.1 pKd = 9.1 Functional
H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum
ChEMBL 453 7 1 8 3.7 Oc1c2nnnc-2oc2cc(OCCCN3CCN(Cc4ccc(Cl)cc4)CC3)ccc12 10.1021/jm00161a022
CHEMBL74870 204784 0 None - 0 Guinea pig 9.1 pKd = 9.1 Functional
H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum
ChEMBL 453 7 1 8 3.7 Oc1c2nnnc-2oc2cc(OCCCN3CCN(Cc4ccc(Cl)cc4)CC3)ccc12 10.1021/jm00161a022
1227 2489 43 None -2 14 Guinea pig 9.1 pKd = 9.1 Functional
H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm00377a013
2331 2489 43 None -2 14 Guinea pig 9.1 pKd = 9.1 Functional
H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm00377a013
3957 2489 43 None -2 14 Guinea pig 9.1 pKd = 9.1 Functional
H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm00377a013
4992 2489 43 None -2 14 Guinea pig 9.1 pKd = 9.1 Functional
H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm00377a013
CHEMBL511 2489 43 None -2 14 Guinea pig 9.1 pKd = 9.1 Functional
H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm00377a013
DB06691 2489 43 None -2 14 Guinea pig 9.1 pKd = 9.1 Functional
H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm00377a013
25190374 161178 0 None - 0 Human 9.1 pKd = 9.1 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 475 13 1 5 4.8 CCCCc1cc(OC2CCN(CCCCNS(=O)(=O)CC(C)C)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4082646 161178 0 None - 0 Human 9.1 pKd = 9.1 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 475 13 1 5 4.8 CCCCc1cc(OC2CCN(CCCCNS(=O)(=O)CC(C)C)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4117608 161178 0 None - 0 Human 9.1 pKd = 9.1 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 475 13 1 5 4.8 CCCCc1cc(OC2CCN(CCCCNS(=O)(=O)CC(C)C)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
9993212 206207 1 None - 0 Guinea pig 9.1 pKd = 9.1 Functional
Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.
ChEMBL 269 4 2 2 2.9 CNCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1 10.1016/s0960-894x(98)00461-2
CHEMBL86522 206207 1 None - 0 Guinea pig 9.1 pKd = 9.1 Functional
Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.
ChEMBL 269 4 2 2 2.9 CNCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1 10.1016/s0960-894x(98)00461-2
1227 2489 43 None -2 14 Guinea pig 9.1 pKd = 9.1 Functional
Antagonism against H1 histamine receptor of guinea pig ileumAntagonism against H1 histamine receptor of guinea pig ileum
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/0960-894X(95)00092-8
2331 2489 43 None -2 14 Guinea pig 9.1 pKd = 9.1 Functional
Antagonism against H1 histamine receptor of guinea pig ileumAntagonism against H1 histamine receptor of guinea pig ileum
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/0960-894X(95)00092-8
3957 2489 43 None -2 14 Guinea pig 9.1 pKd = 9.1 Functional
Antagonism against H1 histamine receptor of guinea pig ileumAntagonism against H1 histamine receptor of guinea pig ileum
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/0960-894X(95)00092-8
4992 2489 43 None -2 14 Guinea pig 9.1 pKd = 9.1 Functional
Antagonism against H1 histamine receptor of guinea pig ileumAntagonism against H1 histamine receptor of guinea pig ileum
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/0960-894X(95)00092-8
CHEMBL511 2489 43 None -2 14 Guinea pig 9.1 pKd = 9.1 Functional
Antagonism against H1 histamine receptor of guinea pig ileumAntagonism against H1 histamine receptor of guinea pig ileum
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/0960-894X(95)00092-8
DB06691 2489 43 None -2 14 Guinea pig 9.1 pKd = 9.1 Functional
Antagonism against H1 histamine receptor of guinea pig ileumAntagonism against H1 histamine receptor of guinea pig ileum
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/0960-894X(95)00092-8
1227 2489 43 None -2 14 Guinea pig 9.1 pKd = 9.1 Functional
Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmcl.2011.09.001
2331 2489 43 None -2 14 Guinea pig 9.1 pKd = 9.1 Functional
Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmcl.2011.09.001
3957 2489 43 None -2 14 Guinea pig 9.1 pKd = 9.1 Functional
Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmcl.2011.09.001
4992 2489 43 None -2 14 Guinea pig 9.1 pKd = 9.1 Functional
Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmcl.2011.09.001
CHEMBL511 2489 43 None -2 14 Guinea pig 9.1 pKd = 9.1 Functional
Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmcl.2011.09.001
DB06691 2489 43 None -2 14 Guinea pig 9.1 pKd = 9.1 Functional
Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmcl.2011.09.001
1204 1932 119 None -3 10 Guinea pig 9.1 pKd = 9.1 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nM
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm991056a
1247 1932 119 None -3 10 Guinea pig 9.1 pKd = 9.1 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nM
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm991056a
1375 1932 119 None -3 10 Guinea pig 9.1 pKd = 9.1 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nM
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm991056a
774 1932 119 None -3 10 Guinea pig 9.1 pKd = 9.1 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nM
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm991056a
CHEMBL90 1932 119 None -3 10 Guinea pig 9.1 pKd = 9.1 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nM
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm991056a
DB05381 1932 119 None -3 10 Guinea pig 9.1 pKd = 9.1 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nM
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm991056a
1204 1932 119 None -3 10 Guinea pig 9.1 pKd = 9.1 Functional
Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/s0960-894x(98)00461-2
1247 1932 119 None -3 10 Guinea pig 9.1 pKd = 9.1 Functional
Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/s0960-894x(98)00461-2
1375 1932 119 None -3 10 Guinea pig 9.1 pKd = 9.1 Functional
Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/s0960-894x(98)00461-2
774 1932 119 None -3 10 Guinea pig 9.1 pKd = 9.1 Functional
Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/s0960-894x(98)00461-2
CHEMBL90 1932 119 None -3 10 Guinea pig 9.1 pKd = 9.1 Functional
Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/s0960-894x(98)00461-2
DB05381 1932 119 None -3 10 Guinea pig 9.1 pKd = 9.1 Functional
Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/s0960-894x(98)00461-2
5310982 93612 4 None - 2 Guinea pig 9.1 pKd = 9.1 Functional
Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum
ChEMBL 255 3 2 2 2.6 NCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1 10.1016/s0960-894x(98)00461-2
CHEMBL24665 93612 4 None - 2 Guinea pig 9.1 pKd = 9.1 Functional
Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum
ChEMBL 255 3 2 2 2.6 NCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1 10.1016/s0960-894x(98)00461-2
9993212 206207 1 None - 0 Guinea pig 9.0 pKd = 9.0 Functional
Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum
ChEMBL 269 4 2 2 2.9 CNCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1 10.1016/s0960-894x(98)00461-2
CHEMBL86522 206207 1 None - 0 Guinea pig 9.0 pKd = 9.0 Functional
Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum
ChEMBL 269 4 2 2 2.9 CNCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1 10.1016/s0960-894x(98)00461-2
10689833 12766 0 None 4 2 Guinea pig 9.0 pKd = 9.0 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nM; value ranges from 9.02 to 9.42Compound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nM; value ranges from 9.02 to 9.42
ChEMBL 359 8 1 2 4.8 c1ccc(C(CCc2nc(CCN3CCCC3)c[nH]2)c2ccccc2)cc1 10.1021/jm991056a
CHEMBL11879 12766 0 None 4 2 Guinea pig 9.0 pKd = 9.0 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nM; value ranges from 9.02 to 9.42Compound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nM; value ranges from 9.02 to 9.42
ChEMBL 359 8 1 2 4.8 c1ccc(C(CCc2nc(CCN3CCCC3)c[nH]2)c2ccccc2)cc1 10.1021/jm991056a
10447834 1933 4 None 2 3 Guinea pig 9.0 pKd = 9.0 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
4026 1933 4 None 2 3 Guinea pig 9.0 pKd = 9.0 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
CHEMBL275507 1933 4 None 2 3 Guinea pig 9.0 pKd = 9.0 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
5310982 93612 4 None - 2 Guinea pig 9.0 pKd = 9.0 Functional
Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.
ChEMBL 255 3 2 2 2.6 NCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1 10.1016/s0960-894x(98)00461-2
CHEMBL24665 93612 4 None - 2 Guinea pig 9.0 pKd = 9.0 Functional
Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.
ChEMBL 255 3 2 2 2.6 NCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1 10.1016/s0960-894x(98)00461-2
44320686 206453 1 None - 0 Guinea pig 9.0 pKd = 9.0 Functional
Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.
ChEMBL 279 4 2 2 2.6 CNCCc1c[nH]c(-c2cccc(Br)c2)n1 10.1016/s0960-894x(98)00461-2
CHEMBL88075 206453 1 None - 0 Guinea pig 9.0 pKd = 9.0 Functional
Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.
ChEMBL 279 4 2 2 2.6 CNCCc1c[nH]c(-c2cccc(Br)c2)n1 10.1016/s0960-894x(98)00461-2
24804150 80480 0 None - 0 Human 9.0 pKd = 9 Functional
Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay
ChEMBL 641 14 0 7 7.2 O=c1c2ccncc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1016/j.bmc.2012.08.032
CHEMBL2146813 80480 0 None - 0 Human 9.0 pKd = 9 Functional
Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay
ChEMBL 641 14 0 7 7.2 O=c1c2ccncc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1016/j.bmc.2012.08.032
25189510 156109 0 None - 0 Human 9.0 pKd = 9 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 461 13 1 5 4.5 CCCCc1cc(OC2CCN(CCCCS(=O)(=O)NCCC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4063163 156109 0 None - 0 Human 9.0 pKd = 9 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 461 13 1 5 4.5 CCCCc1cc(OC2CCN(CCCCS(=O)(=O)NCCC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
25190375 161084 0 None - 0 Human 9.0 pKd = 9 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 501 12 1 5 5.5 CCCCc1cc(OC2CCN(CCCCNS(=O)(=O)C3CCCCC3)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4088039 161084 0 None - 0 Human 9.0 pKd = 9 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 501 12 1 5 5.5 CCCCc1cc(OC2CCN(CCCCNS(=O)(=O)C3CCCCC3)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4116791 161084 0 None - 0 Human 9.0 pKd = 9 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 501 12 1 5 5.5 CCCCc1cc(OC2CCN(CCCCNS(=O)(=O)C3CCCCC3)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
25190431 161213 0 None - 0 Human 9.0 pKd = 9 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 461 12 0 5 4.5 CCCCc1cc(OC2CCN(CCCCN(C)S(=O)(=O)CC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4065123 161213 0 None - 0 Human 9.0 pKd = 9 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 461 12 0 5 4.5 CCCCc1cc(OC2CCN(CCCCN(C)S(=O)(=O)CC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4117871 161213 0 None - 0 Human 9.0 pKd = 9 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 461 12 0 5 4.5 CCCCc1cc(OC2CCN(CCCCN(C)S(=O)(=O)CC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
1204 1932 119 None -3 10 Guinea pig 9.0 pKd = 9 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm991056a
1247 1932 119 None -3 10 Guinea pig 9.0 pKd = 9 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm991056a
1375 1932 119 None -3 10 Guinea pig 9.0 pKd = 9 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm991056a
774 1932 119 None -3 10 Guinea pig 9.0 pKd = 9 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm991056a
CHEMBL90 1932 119 None -3 10 Guinea pig 9.0 pKd = 9 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm991056a
DB05381 1932 119 None -3 10 Guinea pig 9.0 pKd = 9 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm991056a
54710796 120423 0 None - 0 Guinea pig 9.0 pKd = 9 Functional
H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum
ChEMBL 473 8 1 8 3.6 O=c1oc2cc(OCCCN3CCN(Cc4ccc(Cl)cc4)CC3)ccc2c(O)c1[N+](=O)[O-] 10.1021/jm00377a013
CHEMBL35376 120423 0 None - 0 Guinea pig 9.0 pKd = 9 Functional
H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum
ChEMBL 473 8 1 8 3.6 O=c1oc2cc(OCCCN3CCN(Cc4ccc(Cl)cc4)CC3)ccc2c(O)c1[N+](=O)[O-] 10.1021/jm00377a013
1227 2489 43 None -2 14 Guinea pig 9.0 pKd = 9 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm00093a025
2331 2489 43 None -2 14 Guinea pig 9.0 pKd = 9 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm00093a025
3957 2489 43 None -2 14 Guinea pig 9.0 pKd = 9 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm00093a025
4992 2489 43 None -2 14 Guinea pig 9.0 pKd = 9 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm00093a025
CHEMBL511 2489 43 None -2 14 Guinea pig 9.0 pKd = 9 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm00093a025
DB06691 2489 43 None -2 14 Guinea pig 9.0 pKd = 9 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm00093a025
1204 1932 119 None -3 10 Guinea pig 9.0 pKd = 9 Functional
Relative potency against Histamine H1 receptor in endothelium-Denuded rings of guinea pig AortaRelative potency against Histamine H1 receptor in endothelium-Denuded rings of guinea pig Aorta
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0309147
1247 1932 119 None -3 10 Guinea pig 9.0 pKd = 9 Functional
Relative potency against Histamine H1 receptor in endothelium-Denuded rings of guinea pig AortaRelative potency against Histamine H1 receptor in endothelium-Denuded rings of guinea pig Aorta
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0309147
1375 1932 119 None -3 10 Guinea pig 9.0 pKd = 9 Functional
Relative potency against Histamine H1 receptor in endothelium-Denuded rings of guinea pig AortaRelative potency against Histamine H1 receptor in endothelium-Denuded rings of guinea pig Aorta
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0309147
774 1932 119 None -3 10 Guinea pig 9.0 pKd = 9 Functional
Relative potency against Histamine H1 receptor in endothelium-Denuded rings of guinea pig AortaRelative potency against Histamine H1 receptor in endothelium-Denuded rings of guinea pig Aorta
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0309147
CHEMBL90 1932 119 None -3 10 Guinea pig 9.0 pKd = 9 Functional
Relative potency against Histamine H1 receptor in endothelium-Denuded rings of guinea pig AortaRelative potency against Histamine H1 receptor in endothelium-Denuded rings of guinea pig Aorta
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0309147
DB05381 1932 119 None -3 10 Guinea pig 9.0 pKd = 9 Functional
Relative potency against Histamine H1 receptor in endothelium-Denuded rings of guinea pig AortaRelative potency against Histamine H1 receptor in endothelium-Denuded rings of guinea pig Aorta
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0309147
44320685 206452 0 None - 0 Guinea pig 9.0 pKd = 9.0 Functional
Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum
ChEMBL 283 5 2 2 3.2 CCNCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1 10.1016/s0960-894x(98)00461-2
CHEMBL88074 206452 0 None - 0 Guinea pig 9.0 pKd = 9.0 Functional
Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum
ChEMBL 283 5 2 2 3.2 CCNCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1 10.1016/s0960-894x(98)00461-2
1227 2489 43 None -2 14 Guinea pig 9.0 pKd = 9.0 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as histamine-induced contractions
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.ejmech.2008.09.019
2331 2489 43 None -2 14 Guinea pig 9.0 pKd = 9.0 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as histamine-induced contractions
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.ejmech.2008.09.019
3957 2489 43 None -2 14 Guinea pig 9.0 pKd = 9.0 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as histamine-induced contractions
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.ejmech.2008.09.019
4992 2489 43 None -2 14 Guinea pig 9.0 pKd = 9.0 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as histamine-induced contractions
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.ejmech.2008.09.019
CHEMBL511 2489 43 None -2 14 Guinea pig 9.0 pKd = 9.0 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as histamine-induced contractions
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.ejmech.2008.09.019
DB06691 2489 43 None -2 14 Guinea pig 9.0 pKd = 9.0 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as histamine-induced contractions
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.ejmech.2008.09.019
44320707 106030 0 None - 0 Guinea pig 8.9 pKd = 8.9 Functional
Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.
ChEMBL 293 4 1 2 2.9 CN(C)CCc1c[nH]c(-c2cccc(Br)c2)n1 10.1016/s0960-894x(98)00461-2
CHEMBL313301 106030 0 None - 0 Guinea pig 8.9 pKd = 8.9 Functional
Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.
ChEMBL 293 4 1 2 2.9 CN(C)CCc1c[nH]c(-c2cccc(Br)c2)n1 10.1016/s0960-894x(98)00461-2
10407870 106761 0 None - 0 Guinea pig 8.9 pKd = 8.9 Functional
Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum
ChEMBL 283 4 1 2 3.2 CN(C)CCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1 10.1016/s0960-894x(98)00461-2
CHEMBL314438 106761 0 None - 0 Guinea pig 8.9 pKd = 8.9 Functional
Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum
ChEMBL 283 4 1 2 3.2 CN(C)CCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1 10.1016/s0960-894x(98)00461-2
25190317 161058 0 None - 0 Human 8.9 pKd = 8.9 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 433 11 1 5 3.8 CCCCc1cc(OC2CCN(CCCNS(=O)(=O)CC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4080166 161058 0 None - 0 Human 8.9 pKd = 8.9 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 433 11 1 5 3.8 CCCCc1cc(OC2CCN(CCCNS(=O)(=O)CC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4116610 161058 0 None - 0 Human 8.9 pKd = 8.9 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 433 11 1 5 3.8 CCCCc1cc(OC2CCN(CCCNS(=O)(=O)CC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
24803638 61330 0 None - 0 Human 8.9 pKd = 8.9 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assay
ChEMBL 636 15 0 7 7.1 COc1ccc(Cc2nn(C[C@H]3CCCN3CCCCc3ccc(OCCCN4CCCCCC4)cc3)c(=O)c3ccccc23)cc1 10.1021/jm1013874
CHEMBL1767165 61330 0 None - 0 Human 8.9 pKd = 8.9 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assay
ChEMBL 636 15 0 7 7.1 COc1ccc(Cc2nn(C[C@H]3CCCN3CCCCc3ccc(OCCCN4CCCCCC4)cc3)c(=O)c3ccccc23)cc1 10.1021/jm1013874
24803483 61332 0 None - 0 Human 8.9 pKd = 8.9 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assay
ChEMBL 654 15 0 6 8.2 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1021/jm1013874
CHEMBL1767167 61332 0 None - 0 Human 8.9 pKd = 8.9 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assay
ChEMBL 654 15 0 6 8.2 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1021/jm1013874
1194 45 3 None - 2 Guinea pig 8.9 pKd = 8.9 Functional
Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.
ChEMBL 265 3 2 2 2.3 NCCc1cnc([nH]1)c1cccc(c1)Br 10.1016/s0960-894x(98)00461-2
23786499 45 3 None - 2 Guinea pig 8.9 pKd = 8.9 Functional
Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.
ChEMBL 265 3 2 2 2.3 NCCc1cnc([nH]1)c1cccc(c1)Br 10.1016/s0960-894x(98)00461-2
CHEMBL26116 45 3 None - 2 Guinea pig 8.9 pKd = 8.9 Functional
Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.
ChEMBL 265 3 2 2 2.3 NCCc1cnc([nH]1)c1cccc(c1)Br 10.1016/s0960-894x(98)00461-2
10403687 2511 3 None 1 2 Guinea pig 8.9 pKd = 8.9 Functional
Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
1205 2511 3 None 1 2 Guinea pig 8.9 pKd = 8.9 Functional
Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
CHEMBL275035 2511 3 None 1 2 Guinea pig 8.9 pKd = 8.9 Functional
Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
10042467 1426 1 None -1 2 Guinea pig 8.9 pKd = 8.9 Functional
Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine
ChEMBL 333 8 1 2 4.3 CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C 10.1021/jm991056a
1203 1426 1 None -1 2 Guinea pig 8.9 pKd = 8.9 Functional
Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine
ChEMBL 333 8 1 2 4.3 CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C 10.1021/jm991056a
CHEMBL11553 1426 1 None -1 2 Guinea pig 8.9 pKd = 8.9 Functional
Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine
ChEMBL 333 8 1 2 4.3 CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C 10.1021/jm991056a
1524 2181 96 None - 18 Guinea pig 8.9 pKd = 8.9 Functional
Antagonism against H1 histamine receptor of guinea pig ileumAntagonism against H1 histamine receptor of guinea pig ileum
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/0960-894X(95)00092-8
197 2181 96 None - 18 Guinea pig 8.9 pKd = 8.9 Functional
Antagonism against H1 histamine receptor of guinea pig ileumAntagonism against H1 histamine receptor of guinea pig ileum
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/0960-894X(95)00092-8
3822 2181 96 None - 18 Guinea pig 8.9 pKd = 8.9 Functional
Antagonism against H1 histamine receptor of guinea pig ileumAntagonism against H1 histamine receptor of guinea pig ileum
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/0960-894X(95)00092-8
88 2181 96 None - 18 Guinea pig 8.9 pKd = 8.9 Functional
Antagonism against H1 histamine receptor of guinea pig ileumAntagonism against H1 histamine receptor of guinea pig ileum
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/0960-894X(95)00092-8
CHEMBL51 2181 96 None - 18 Guinea pig 8.9 pKd = 8.9 Functional
Antagonism against H1 histamine receptor of guinea pig ileumAntagonism against H1 histamine receptor of guinea pig ileum
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/0960-894X(95)00092-8
DB12465 2181 96 None - 18 Guinea pig 8.9 pKd = 8.9 Functional
Antagonism against H1 histamine receptor of guinea pig ileumAntagonism against H1 histamine receptor of guinea pig ileum
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1016/0960-894X(95)00092-8
11791817 98303 0 None -1 2 Guinea pig 8.9 pKd = 8.9 Functional
Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine
ChEMBL 345 9 2 2 4.5 c1ccc(C(CCc2nc(CCNC3CC3)c[nH]2)c2ccccc2)cc1 10.1021/jm991056a
CHEMBL274831 98303 0 None -1 2 Guinea pig 8.9 pKd = 8.9 Functional
Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine
ChEMBL 345 9 2 2 4.5 c1ccc(C(CCc2nc(CCNC3CC3)c[nH]2)c2ccccc2)cc1 10.1021/jm991056a
25190253 161117 0 None - 0 Human 8.9 pKd = 8.9 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 460 10 0 5 5.4 CCCCc1cc(OC2CCN(CCCCS(=O)(=O)C(C)(C)C)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4095759 161117 0 None - 0 Human 8.9 pKd = 8.9 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 460 10 0 5 5.4 CCCCc1cc(OC2CCN(CCCCS(=O)(=O)C(C)(C)C)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4117136 161117 0 None - 0 Human 8.9 pKd = 8.9 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 460 10 0 5 5.4 CCCCc1cc(OC2CCN(CCCCS(=O)(=O)C(C)(C)C)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
10407870 106761 0 None - 0 Guinea pig 8.9 pKd = 8.9 Functional
Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.
ChEMBL 283 4 1 2 3.2 CN(C)CCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1 10.1016/s0960-894x(98)00461-2
CHEMBL314438 106761 0 None - 0 Guinea pig 8.9 pKd = 8.9 Functional
Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.
ChEMBL 283 4 1 2 3.2 CN(C)CCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1 10.1016/s0960-894x(98)00461-2
10688111 10040 1 None 2 2 Guinea pig 8.8 pKd = 8.8 Functional
Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine
ChEMBL 333 9 2 2 4.3 CCNCCc1c[nH]c(CCC(c2ccccc2)c2ccccc2)n1 10.1021/jm991056a
CHEMBL11515 10040 1 None 2 2 Guinea pig 8.8 pKd = 8.8 Functional
Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine
ChEMBL 333 9 2 2 4.3 CCNCCc1c[nH]c(CCC(c2ccccc2)c2ccccc2)n1 10.1021/jm991056a
57780020 143450 0 None - 0 Human 8.8 pKd = 8.8 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 600 15 1 6 6.6 CCCCc1cc(N2CCN(CCc3ccc(OCCCN4CCCCCC4)cc3)CC2)c2nc(CCC(=O)O)ccc2c1 10.1016/j.bmcl.2016.11.022
CHEMBL3898341 143450 0 None - 0 Human 8.8 pKd = 8.8 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 600 15 1 6 6.6 CCCCc1cc(N2CCN(CCc3ccc(OCCCN4CCCCCC4)cc3)CC2)c2nc(CCC(=O)O)ccc2c1 10.1016/j.bmcl.2016.11.022
10447834 1933 4 None 2 3 Guinea pig 8.8 pKd = 8.8 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
4026 1933 4 None 2 3 Guinea pig 8.8 pKd = 8.8 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
CHEMBL275507 1933 4 None 2 3 Guinea pig 8.8 pKd = 8.8 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
13676694 103712 0 None - 0 Guinea pig 8.8 pKd = 8.8 Functional
H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum
ChEMBL 467 7 1 8 4.0 Cc1c(OCCCN2CCN(Cc3ccc(Cl)cc3)CC2)ccc2c(O)c3nnnc-3oc12 10.1021/jm00161a022
CHEMBL308791 103712 0 None - 0 Guinea pig 8.8 pKd = 8.8 Functional
H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum
ChEMBL 467 7 1 8 4.0 Cc1c(OCCCN2CCN(Cc3ccc(Cl)cc3)CC2)ccc2c(O)c3nnnc-3oc12 10.1021/jm00161a022
10410901 119747 0 None 23 2 Guinea pig 8.8 pKd = 8.8 Functional
Apparent pA2 value of compound at 10 nM concentration of mepyramine in guinea pig ileumApparent pA2 value of compound at 10 nM concentration of mepyramine in guinea pig ileum
ChEMBL 438 13 2 3 5.7 c1ccc(C(CCc2nc(CCNCCCCc3ccccn3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
CHEMBL347796 119747 0 None 23 2 Guinea pig 8.8 pKd = 8.8 Functional
Apparent pA2 value of compound at 10 nM concentration of mepyramine in guinea pig ileumApparent pA2 value of compound at 10 nM concentration of mepyramine in guinea pig ileum
ChEMBL 438 13 2 3 5.7 c1ccc(C(CCc2nc(CCNCCCCc3ccccn3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
10403687 2511 3 None 1 2 Guinea pig 8.8 pKd = 8.8 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
1205 2511 3 None 1 2 Guinea pig 8.8 pKd = 8.8 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
CHEMBL275035 2511 3 None 1 2 Guinea pig 8.8 pKd = 8.8 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
10484346 98726 0 None - 0 Guinea pig 8.7 pKd = 8.7 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 646 22 2 11 5.8 COc1ccc(CN(CCN(C)CCCCCCNC(=O)CCCCCNc2ccc([N+](=O)[O-])c3nonc23)c2ccccn2)cc1 10.1016/s0960-894x(03)00113-6
CHEMBL277848 98726 0 None - 0 Guinea pig 8.7 pKd = 8.7 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 646 22 2 11 5.8 COc1ccc(CN(CCN(C)CCCCCCNC(=O)CCCCCNc2ccc([N+](=O)[O-])c3nonc23)c2ccccn2)cc1 10.1016/s0960-894x(03)00113-6
25190435 158404 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 447 9 1 5 4.1 CCCCc1cc(OC2CCN(CCS(=O)(=O)NC(C)(C)C)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4090136 158404 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 447 9 1 5 4.1 CCCCc1cc(OC2CCN(CCS(=O)(=O)NC(C)(C)C)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
25190373 161088 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 461 12 1 5 4.5 CCCCc1cc(OC2CCN(CCCCNS(=O)(=O)C(C)C)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4060765 161088 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 461 12 1 5 4.5 CCCCc1cc(OC2CCN(CCCCNS(=O)(=O)C(C)C)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4116847 161088 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 461 12 1 5 4.5 CCCCc1cc(OC2CCN(CCCCNS(=O)(=O)C(C)C)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
25190254 161103 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 432 10 0 5 4.6 CCCCc1cc(OC2CCN(CCC(C)S(=O)(=O)CC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4068414 161103 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 432 10 0 5 4.6 CCCCc1cc(OC2CCN(CCC(C)S(=O)(=O)CC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4117012 161103 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 432 10 0 5 4.6 CCCCc1cc(OC2CCN(CCC(C)S(=O)(=O)CC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
3529324 208354 1 None - 1 Guinea pig 8.7 pKd = 8.7 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 306 6 0 3 3.3 CC(C)c1ccc(C2SCC(=O)N2CCCN(C)C)cc1 10.1021/jm00093a025
CHEMBL1202934 208354 1 None - 1 Guinea pig 8.7 pKd = 8.7 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 306 6 0 3 3.3 CC(C)c1ccc(C2SCC(=O)N2CCCN(C)C)cc1 10.1021/jm00093a025
CHEMBL99417 208354 1 None - 1 Guinea pig 8.7 pKd = 8.7 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 306 6 0 3 3.3 CC(C)c1ccc(C2SCC(=O)N2CCCN(C)C)cc1 10.1021/jm00093a025
57780008 149726 0 None - 0 Human 8.0 pKd = 8 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 472 9 0 5 5.2 c1cnc2c(N3CCN(CCc4ccc(OCCCN5CCCCCC5)cc4)CC3)cccc2c1 10.1016/j.bmcl.2016.11.022
CHEMBL3947980 149726 0 None - 0 Human 8.0 pKd = 8 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 472 9 0 5 5.2 c1cnc2c(N3CCN(CCc4ccc(OCCCN5CCCCCC5)cc4)CC3)cccc2c1 10.1016/j.bmcl.2016.11.022
1204 1932 119 None -3 10 Guinea pig 8.0 pKd = 8 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nM
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm991056a
1247 1932 119 None -3 10 Guinea pig 8.0 pKd = 8 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nM
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm991056a
1375 1932 119 None -3 10 Guinea pig 8.0 pKd = 8 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nM
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm991056a
774 1932 119 None -3 10 Guinea pig 8.0 pKd = 8 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nM
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm991056a
CHEMBL90 1932 119 None -3 10 Guinea pig 8.0 pKd = 8 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nM
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm991056a
DB05381 1932 119 None -3 10 Guinea pig 8.0 pKd = 8 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nM
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm991056a
1204 1932 119 None -9 10 Rat 8.0 pKd = 8 Functional
Relative potency against Histamine H1 receptor in rat aortaRelative potency against Histamine H1 receptor in rat aorta
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0309147
1247 1932 119 None -9 10 Rat 8.0 pKd = 8 Functional
Relative potency against Histamine H1 receptor in rat aortaRelative potency against Histamine H1 receptor in rat aorta
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0309147
1375 1932 119 None -9 10 Rat 8.0 pKd = 8 Functional
Relative potency against Histamine H1 receptor in rat aortaRelative potency against Histamine H1 receptor in rat aorta
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0309147
774 1932 119 None -9 10 Rat 8.0 pKd = 8 Functional
Relative potency against Histamine H1 receptor in rat aortaRelative potency against Histamine H1 receptor in rat aorta
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0309147
CHEMBL90 1932 119 None -9 10 Rat 8.0 pKd = 8 Functional
Relative potency against Histamine H1 receptor in rat aortaRelative potency against Histamine H1 receptor in rat aorta
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0309147
DB05381 1932 119 None -9 10 Rat 8.0 pKd = 8 Functional
Relative potency against Histamine H1 receptor in rat aortaRelative potency against Histamine H1 receptor in rat aorta
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0309147
10364258 45769 0 None -12 2 Rat 8.0 pKd = 8.0 Functional
Apparent pA2 value of compound at 50 nM concentration of mepyramine in rat aortaApparent pA2 value of compound at 50 nM concentration of mepyramine in rat aorta
ChEMBL 410 11 2 3 4.9 c1ccc(C(CCc2nc(CCNCCc3ccccn3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
CHEMBL153067 45769 0 None -12 2 Rat 8.0 pKd = 8.0 Functional
Apparent pA2 value of compound at 50 nM concentration of mepyramine in rat aortaApparent pA2 value of compound at 50 nM concentration of mepyramine in rat aorta
ChEMBL 410 11 2 3 4.9 c1ccc(C(CCc2nc(CCNCCc3ccccn3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
10042467 1426 1 None -1 2 Guinea pig 8.0 pKd = 8.0 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nM
ChEMBL 333 8 1 2 4.3 CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C 10.1021/jm991056a
1203 1426 1 None -1 2 Guinea pig 8.0 pKd = 8.0 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nM
ChEMBL 333 8 1 2 4.3 CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C 10.1021/jm991056a
CHEMBL11553 1426 1 None -1 2 Guinea pig 8.0 pKd = 8.0 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nM
ChEMBL 333 8 1 2 4.3 CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C 10.1021/jm991056a
57402471 67876 0 None - 0 Guinea pig 8.0 pKd = 8.0 Functional
Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins
ChEMBL 469 8 1 5 4.0 COc1ccc(CN(CCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
CHEMBL1910378 67876 0 None - 0 Guinea pig 8.0 pKd = 8.0 Functional
Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins
ChEMBL 469 8 1 5 4.0 COc1ccc(CN(CCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
14113352 170208 0 None - 0 Guinea pig 7.0 pKd = 7 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 394 10 4 4 3.4 N=C(NCCCc1c[nH]cn1)NCCSC(c1ccccc1)c1ccccn1 10.1021/jm00128a045
CHEMBL444531 170208 0 None - 0 Guinea pig 7.0 pKd = 7 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 394 10 4 4 3.4 N=C(NCCCc1c[nH]cn1)NCCSC(c1ccccc1)c1ccccn1 10.1021/jm00128a045
14984030 107330 1 None - 1 Guinea pig 6.0 pKd = 6 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 279 5 1 4 1.8 CN(C)CCCN1C(=O)CSC1c1ccc(N)cc1 10.1021/jm00093a025
CHEMBL1202935 107330 1 None - 1 Guinea pig 6.0 pKd = 6 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 279 5 1 4 1.8 CN(C)CCCN1C(=O)CSC1c1ccc(N)cc1 10.1021/jm00093a025
CHEMBL317518 107330 1 None - 1 Guinea pig 6.0 pKd = 6 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 279 5 1 4 1.8 CN(C)CCCN1C(=O)CSC1c1ccc(N)cc1 10.1021/jm00093a025
10246247 98293 0 None - 0 Guinea pig 6.0 pKd = 6 Functional
Relative potency was recorded in endothelium-denuded guinea pig; value ranges from 5.75 to 6.25Relative potency was recorded in endothelium-denuded guinea pig; value ranges from 5.75 to 6.25
ChEMBL 333 9 2 2 4.5 NCCc1c[nH]c(CCCCC(c2ccccc2)c2ccccc2)n1 10.1021/jm991056a
CHEMBL274767 98293 0 None - 0 Guinea pig 6.0 pKd = 6 Functional
Relative potency was recorded in endothelium-denuded guinea pig; value ranges from 5.75 to 6.25Relative potency was recorded in endothelium-denuded guinea pig; value ranges from 5.75 to 6.25
ChEMBL 333 9 2 2 4.5 NCCc1c[nH]c(CCCCC(c2ccccc2)c2ccccc2)n1 10.1021/jm991056a
10684712 11392 0 None - 0 Guinea pig 5.0 pKd = 5 Functional
Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum
ChEMBL 287 8 2 4 3.4 CCC/C(=N\O)c1ccc(OCCCc2c[nH]cn2)cc1 10.1021/jm000971p
CHEMBL112301 11392 0 None - 0 Guinea pig 5.0 pKd = 5 Functional
Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum
ChEMBL 287 8 2 4 3.4 CCC/C(=N\O)c1ccc(OCCCc2c[nH]cn2)cc1 10.1021/jm000971p
CHEMBL1180048 11392 0 None - 0 Guinea pig 5.0 pKd = 5 Functional
Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum
ChEMBL 287 8 2 4 3.4 CCC/C(=N\O)c1ccc(OCCCc2c[nH]cn2)cc1 10.1021/jm000971p
6422121 205449 1 None - 0 Guinea pig 5.0 pKd = 5 Functional
Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum
ChEMBL 285 7 2 4 3.0 O/N=C(/c1ccc(OCCCc2c[nH]cn2)cc1)C1CC1 10.1021/jm000971p
CHEMBL116270 205449 1 None - 0 Guinea pig 5.0 pKd = 5 Functional
Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum
ChEMBL 285 7 2 4 3.0 O/N=C(/c1ccc(OCCCc2c[nH]cn2)cc1)C1CC1 10.1021/jm000971p
CHEMBL80348 205449 1 None - 0 Guinea pig 5.0 pKd = 5 Functional
Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum
ChEMBL 285 7 2 4 3.0 O/N=C(/c1ccc(OCCCc2c[nH]cn2)cc1)C1CC1 10.1021/jm000971p
2860933 208172 3 None - 0 Guinea pig 5.0 pKd = 5 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 294 6 0 4 2.2 COc1ccc(C2SCC(=O)N2CCCN(C)C)cc1 10.1021/jm00093a025
CHEMBL1202929 208172 3 None - 0 Guinea pig 5.0 pKd = 5 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 294 6 0 4 2.2 COc1ccc(C2SCC(=O)N2CCCN(C)C)cc1 10.1021/jm00093a025
CHEMBL98319 208172 3 None - 0 Guinea pig 5.0 pKd = 5 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 294 6 0 4 2.2 COc1ccc(C2SCC(=O)N2CCCN(C)C)cc1 10.1021/jm00093a025
54726349 112370 0 None - 0 Guinea pig 4.0 pKd = 4 Functional
H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum
ChEMBL 363 6 1 8 1.4 CN1CCN(CCCOc2ccc3c(O)c([N+](=O)[O-])c(=O)oc3c2)CC1 10.1021/jm00377a013
CHEMBL32953 112370 0 None - 0 Guinea pig 4.0 pKd = 4 Functional
H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum
ChEMBL 363 6 1 8 1.4 CN1CCN(CCCOc2ccc3c(O)c([N+](=O)[O-])c(=O)oc3c2)CC1 10.1021/jm00377a013
10246247 98293 0 None - 0 Rat 6.0 pKd = 6.0 Functional
Relative potency was recorded in in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619 valueRelative potency was recorded in in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619 value
ChEMBL 333 9 2 2 4.5 NCCc1c[nH]c(CCCCC(c2ccccc2)c2ccccc2)n1 10.1021/jm991056a
CHEMBL274767 98293 0 None - 0 Rat 6.0 pKd = 6.0 Functional
Relative potency was recorded in in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619 valueRelative potency was recorded in in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619 value
ChEMBL 333 9 2 2 4.5 NCCc1c[nH]c(CCCCC(c2ccccc2)c2ccccc2)n1 10.1021/jm991056a
11779175 63166 0 None - 1 Guinea pig 5.0 pKd = 5.0 Functional
Antagonist activity at histamine H1 receptor in guinea-pig ileumAntagonist activity at histamine H1 receptor in guinea-pig ileum
ChEMBL 293 8 2 3 3.4 O=C(NCCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1774600 63166 0 None - 1 Guinea pig 5.0 pKd = 5.0 Functional
Antagonist activity at histamine H1 receptor in guinea-pig ileumAntagonist activity at histamine H1 receptor in guinea-pig ileum
ChEMBL 293 8 2 3 3.4 O=C(NCCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1789801 63166 0 None - 1 Guinea pig 5.0 pKd = 5.0 Functional
Antagonist activity at histamine H1 receptor in guinea-pig ileumAntagonist activity at histamine H1 receptor in guinea-pig ileum
ChEMBL 293 8 2 3 3.4 O=C(NCCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
14660374 100690 0 None - 0 Guinea pig 6.0 pKd = 6.0 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 394 9 3 3 3.6 CN(CCC(c1ccc(F)cc1)c1ccccn1)C(=N)NCCCc1c[nH]cn1 10.1021/jm00128a045
CHEMBL292395 100690 0 None - 0 Guinea pig 6.0 pKd = 6.0 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 394 9 3 3 3.6 CN(CCC(c1ccc(F)cc1)c1ccccn1)C(=N)NCCCc1c[nH]cn1 10.1021/jm00128a045
1224 1432 83 None 85 22 Guinea pig 7.9 pKd = 7.9 Functional
Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1016/j.bmcl.2011.09.001
3100 1432 83 None 85 22 Guinea pig 7.9 pKd = 7.9 Functional
Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1016/j.bmcl.2011.09.001
8980 1432 83 None 85 22 Guinea pig 7.9 pKd = 7.9 Functional
Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1016/j.bmcl.2011.09.001
916 1432 83 None 85 22 Guinea pig 7.9 pKd = 7.9 Functional
Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1016/j.bmcl.2011.09.001
CHEMBL657 1432 83 None 85 22 Guinea pig 7.9 pKd = 7.9 Functional
Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1016/j.bmcl.2011.09.001
DB01075 1432 83 None 85 22 Guinea pig 7.9 pKd = 7.9 Functional
Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1016/j.bmcl.2011.09.001
25149611 179175 0 None - 0 Guinea pig 5.0 pKd = 5.0 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 376 8 4 4 2.6 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccn1 10.1021/jm800841w
CHEMBL472272 179175 0 None - 0 Guinea pig 5.0 pKd = 5.0 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 376 8 4 4 2.6 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccn1 10.1021/jm800841w
14660410 199054 0 None - 0 Guinea pig 6.9 pKd = 6.9 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 396 9 4 4 2.1 N/C(=N\CCC(O)(c1ccc(F)cc1)c1ccccn1)NCCCc1c[nH]cn1 10.1021/jm00128a045
CHEMBL58621 199054 0 None - 0 Guinea pig 6.9 pKd = 6.9 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 396 9 4 4 2.1 N/C(=N\CCC(O)(c1ccc(F)cc1)c1ccccn1)NCCCc1c[nH]cn1 10.1021/jm00128a045
57398985 67883 0 None - 0 Guinea pig 7.9 pKd = 7.9 Functional
Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins
ChEMBL 569 12 2 7 4.4 COc1ccc(CN(CCN(C)CC(C)Nc2ccc3[nH]c(C(=O)N4CCN(C)CC4)cc3c2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
CHEMBL1910385 67883 0 None - 0 Guinea pig 7.9 pKd = 7.9 Functional
Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins
ChEMBL 569 12 2 7 4.4 COc1ccc(CN(CCN(C)CC(C)Nc2ccc3[nH]c(C(=O)N4CCN(C)CC4)cc3c2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
54710799 96781 0 None - 0 Guinea pig 7.9 pKd = 7.9 Functional
H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum
ChEMBL 439 8 1 8 3.0 O=c1oc2cc(OCCCN3CCN(Cc4ccccc4)CC3)ccc2c(O)c1[N+](=O)[O-] 10.1021/jm00377a013
CHEMBL264756 96781 0 None - 0 Guinea pig 7.9 pKd = 7.9 Functional
H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum
ChEMBL 439 8 1 8 3.0 O=c1oc2cc(OCCCN3CCN(Cc4ccccc4)CC3)ccc2c(O)c1[N+](=O)[O-] 10.1021/jm00377a013
19762600 79999 0 None - 0 Guinea pig 7.9 pKd = 7.9 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 370 13 1 5 3.5 COc1ccc(CN(CCN(C)CCCCCCN)c2ccccn2)cc1 10.1016/s0960-894x(03)00113-6
CHEMBL21278 79999 0 None - 0 Guinea pig 7.9 pKd = 7.9 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 370 13 1 5 3.5 COc1ccc(CN(CCN(C)CCCCCCN)c2ccccn2)cc1 10.1016/s0960-894x(03)00113-6
10003410 200642 0 None - 0 Guinea pig 6.9 pKd = 6.9 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 440 9 4 3 3.8 N=C(NCCCc1c[nH]cn1)NCCC(c1ccc(Br)cc1)c1ccccn1 10.1021/jm00128a045
CHEMBL59951 200642 0 None - 0 Guinea pig 6.9 pKd = 6.9 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 440 9 4 3 3.8 N=C(NCCCc1c[nH]cn1)NCCC(c1ccc(Br)cc1)c1ccccn1 10.1021/jm00128a045
10852834 11393 0 None - 0 Guinea pig 4.9 pKd = 4.9 Functional
Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum
ChEMBL 315 10 2 4 4.2 CCCCC/C(=N\O)c1ccc(OCCCc2c[nH]cn2)cc1 10.1021/jm000971p
CHEMBL112629 11393 0 None - 0 Guinea pig 4.9 pKd = 4.9 Functional
Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum
ChEMBL 315 10 2 4 4.2 CCCCC/C(=N\O)c1ccc(OCCCc2c[nH]cn2)cc1 10.1021/jm000971p
CHEMBL1180064 11393 0 None - 0 Guinea pig 4.9 pKd = 4.9 Functional
Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum
ChEMBL 315 10 2 4 4.2 CCCCC/C(=N\O)c1ccc(OCCCc2c[nH]cn2)cc1 10.1021/jm000971p
10659856 11397 0 None - 0 Guinea pig 4.9 pKd = 4.9 Functional
Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum
ChEMBL 273 7 1 4 2.8 CO/N=C(\C)c1ccc(OCCCc2c[nH]cn2)cc1 10.1021/jm000971p
CHEMBL112753 11397 0 None - 0 Guinea pig 4.9 pKd = 4.9 Functional
Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum
ChEMBL 273 7 1 4 2.8 CO/N=C(\C)c1ccc(OCCCc2c[nH]cn2)cc1 10.1021/jm000971p
CHEMBL1180075 11397 0 None - 0 Guinea pig 4.9 pKd = 4.9 Functional
Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum
ChEMBL 273 7 1 4 2.8 CO/N=C(\C)c1ccc(OCCCc2c[nH]cn2)cc1 10.1021/jm000971p
10828008 11410 0 None - 0 Guinea pig 4.9 pKd = 4.9 Functional
Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum
ChEMBL 299 6 1 3 2.7 O=C(c1ccc(OCCCc2c[nH]cn2)cc1)N1CCCC1 10.1021/jm000971p
CHEMBL115169 11410 0 None - 0 Guinea pig 4.9 pKd = 4.9 Functional
Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum
ChEMBL 299 6 1 3 2.7 O=C(c1ccc(OCCCc2c[nH]cn2)cc1)N1CCCC1 10.1021/jm000971p
CHEMBL1180148 11410 0 None - 0 Guinea pig 4.9 pKd = 4.9 Functional
Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum
ChEMBL 299 6 1 3 2.7 O=C(c1ccc(OCCCc2c[nH]cn2)cc1)N1CCCC1 10.1021/jm000971p
19762590 162263 1 None - 0 Guinea pig 7.9 pKd = 7.9 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 314 9 1 5 2.0 COc1ccc(CN(CCN(C)CCN)c2ccccn2)cc1 10.1016/s0960-894x(03)00113-6
CHEMBL416378 162263 1 None - 0 Guinea pig 7.9 pKd = 7.9 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 314 9 1 5 2.0 COc1ccc(CN(CCN(C)CCN)c2ccccn2)cc1 10.1016/s0960-894x(03)00113-6
25149335 184225 0 None - 3 Guinea pig 5.9 pKd = 5.9 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/jm9000693
CHEMBL483406 184225 0 None - 3 Guinea pig 5.9 pKd = 5.9 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/jm9000693
25149335 184225 0 None - 3 Guinea pig 5.9 pKd = 5.9 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/jm800841w
CHEMBL483406 184225 0 None - 3 Guinea pig 5.9 pKd = 5.9 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/jm800841w
52949049 10555 0 None - 0 Guinea pig 7.8 pKd = 7.8 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 673 17 1 7 7.2 COc1ccc(CN(CCN(C)CCCCCCNC(=O)CCC2=C3C(C)=CC(C)N3[B-](F)(F)n3c(C)cc(C)c32)c2ccccn2)cc1 10.1016/s0960-894x(03)00113-6
CHEMBL1169587 10555 0 None - 0 Guinea pig 7.8 pKd = 7.8 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 673 17 1 7 7.2 COc1ccc(CN(CCN(C)CCCCCCNC(=O)CCC2=C3C(C)=CC(C)N3[B-](F)(F)n3c(C)cc(C)c32)c2ccccn2)cc1 10.1016/s0960-894x(03)00113-6
14660389 202293 0 None - 0 Guinea pig 6.9 pKd = 6.9 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 393 10 4 2 4.0 N=C(NCCCc1c[nH]cn1)NCCC(Cc1ccccc1)c1ccc(F)cc1 10.1021/jm00128a045
CHEMBL61022 202293 0 None - 0 Guinea pig 6.9 pKd = 6.9 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 393 10 4 2 4.0 N=C(NCCCc1c[nH]cn1)NCCC(Cc1ccccc1)c1ccc(F)cc1 10.1021/jm00128a045
44457703 99546 0 None - 0 Guinea pig 6.8 pKd = 6.8 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 672 13 3 9 5.7 COc1ccc(CN(CCN(C)CCNC(=O)c2ccc(C(=O)O)c(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c2)c2ccccn2)cc1 10.1016/s0960-894x(03)00113-6
CHEMBL283527 99546 0 None - 0 Guinea pig 6.8 pKd = 6.8 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 672 13 3 9 5.7 COc1ccc(CN(CCN(C)CCNC(=O)c2ccc(C(=O)O)c(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c2)c2ccccn2)cc1 10.1016/s0960-894x(03)00113-6
14660348 199654 0 None - 0 Guinea pig 6.8 pKd = 6.8 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 376 9 3 3 3.2 Cc1ccc(C(CC/N=C(\N)NCCCc2c[nH]cn2)c2ccccn2)cc1 10.1021/jm00128a045
CHEMBL59294 199654 0 None - 0 Guinea pig 6.8 pKd = 6.8 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 376 9 3 3 3.2 Cc1ccc(C(CC/N=C(\N)NCCCc2c[nH]cn2)c2ccccn2)cc1 10.1021/jm00128a045
13676692 105484 0 None - 0 Guinea pig 7.8 pKd = 7.8 Functional
Compound was tested for H1-antihistamine activity in guinea pig ileum.Compound was tested for H1-antihistamine activity in guinea pig ileum.
ChEMBL 447 7 1 8 3.6 Cc1ccc(CN2CCN(CCCOc3ccc4c(O)c5nnnc-5oc4c3C)CC2)cc1 10.1021/jm00161a022
CHEMBL312083 105484 0 None - 0 Guinea pig 7.8 pKd = 7.8 Functional
Compound was tested for H1-antihistamine activity in guinea pig ileum.Compound was tested for H1-antihistamine activity in guinea pig ileum.
ChEMBL 447 7 1 8 3.6 Cc1ccc(CN2CCN(CCCOc3ccc4c(O)c5nnnc-5oc4c3C)CC2)cc1 10.1021/jm00161a022
13676699 163768 0 None - 0 Guinea pig 7.8 pKd = 7.8 Functional
H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum
ChEMBL 434 7 1 9 2.7 Cc1c(OCCCN2CCN(Cc3ccccn3)CC2)ccc2c(O)c3nnnc-3oc12 10.1021/jm00161a022
CHEMBL420567 163768 0 None - 0 Guinea pig 7.8 pKd = 7.8 Functional
H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum
ChEMBL 434 7 1 9 2.7 Cc1c(OCCCN2CCN(Cc3ccccn3)CC2)ccc2c(O)c3nnnc-3oc12 10.1021/jm00161a022
14660357 202702 0 None - 0 Guinea pig 6.8 pKd = 6.8 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 380 9 4 3 3.2 N=C(NCCCc1c[nH]cn1)NCCC(c1cccc(F)c1)c1ccccn1 10.1021/jm00128a045
CHEMBL61675 202702 0 None - 0 Guinea pig 6.8 pKd = 6.8 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 380 9 4 3 3.2 N=C(NCCCc1c[nH]cn1)NCCC(c1cccc(F)c1)c1ccccn1 10.1021/jm00128a045
54710801 99907 0 None - 0 Guinea pig 6.8 pKd = 6.8 Functional
H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum
ChEMBL 459 7 1 8 3.3 O=c1oc2cc(OCCN3CCN(Cc4ccc(Cl)cc4)CC3)ccc2c(O)c1[N+](=O)[O-] 10.1021/jm00377a013
CHEMBL286094 99907 0 None - 0 Guinea pig 6.8 pKd = 6.8 Functional
H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum
ChEMBL 459 7 1 8 3.3 O=c1oc2cc(OCCN3CCN(Cc4ccc(Cl)cc4)CC3)ccc2c(O)c1[N+](=O)[O-] 10.1021/jm00377a013
10825231 9630 1 None - 0 Guinea pig 6.8 pKd = 6.8 Functional
Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum
ChEMBL 260 6 1 4 2.2 COC(=O)c1ccc(OCCCc2c[nH]cn2)cc1 10.1021/jm000971p
CHEMBL112670 9630 1 None - 0 Guinea pig 6.8 pKd = 6.8 Functional
Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum
ChEMBL 260 6 1 4 2.2 COC(=O)c1ccc(OCCCc2c[nH]cn2)cc1 10.1021/jm000971p
1278 2150 84 None - 4 Guinea pig 5.8 pKd = 5.8 Functional
Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.09.001
1279 2150 84 None - 4 Guinea pig 5.8 pKd = 5.8 Functional
Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.09.001
4908365 2150 84 None - 4 Guinea pig 5.8 pKd = 5.8 Functional
Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.09.001
CHEMBL129198 2150 84 None - 4 Guinea pig 5.8 pKd = 5.8 Functional
Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.09.001
15179507 204179 0 None - 0 Guinea pig 5.8 pKd = 5.8 Functional
Histamine H1 receptor antagonistic activity on the isolated guinea pig ileum determined by Schild plot.Histamine H1 receptor antagonistic activity on the isolated guinea pig ileum determined by Schild plot.
ChEMBL 729 11 4 6 3.7 N#CN/C(=N\CCNC(=O)c1cc(I)c(N)c(I)c1)NCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm00090a013
CHEMBL70746 204179 0 None - 0 Guinea pig 5.8 pKd = 5.8 Functional
Histamine H1 receptor antagonistic activity on the isolated guinea pig ileum determined by Schild plot.Histamine H1 receptor antagonistic activity on the isolated guinea pig ileum determined by Schild plot.
ChEMBL 729 11 4 6 3.7 N#CN/C(=N\CCNC(=O)c1cc(I)c(N)c(I)c1)NCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm00090a013
11459067 11348 0 None - 0 Guinea pig 4.8 pKd = 4.8 Functional
Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum
ChEMBL 238 11 1 2 3.7 CCCCCCCCOCCCc1c[nH]cn1 10.1021/jm031065q
CHEMBL1179647 11348 0 None - 0 Guinea pig 4.8 pKd = 4.8 Functional
Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum
ChEMBL 238 11 1 2 3.7 CCCCCCCCOCCCc1c[nH]cn1 10.1021/jm031065q
CHEMBL91523 11348 0 None - 0 Guinea pig 4.8 pKd = 4.8 Functional
Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum
ChEMBL 238 11 1 2 3.7 CCCCCCCCOCCCc1c[nH]cn1 10.1021/jm031065q
10730975 12105 0 None - 0 Guinea pig 4.8 pKd = 4.8 Functional
Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum
ChEMBL 273 6 2 4 2.9 C/C(=N\O)c1ccc(OCCCc2c[nH]cn2)c(C)c1 10.1021/jm000971p
CHEMBL1183977 12105 0 None - 0 Guinea pig 4.8 pKd = 4.8 Functional
Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum
ChEMBL 273 6 2 4 2.9 C/C(=N\O)c1ccc(OCCCc2c[nH]cn2)c(C)c1 10.1021/jm000971p
CHEMBL326624 12105 0 None - 0 Guinea pig 4.8 pKd = 4.8 Functional
Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum
ChEMBL 273 6 2 4 2.9 C/C(=N\O)c1ccc(OCCCc2c[nH]cn2)c(C)c1 10.1021/jm000971p
14660414 199072 0 None - 0 Guinea pig 5.8 pKd = 5.8 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 407 10 3 5 2.8 N/C(=N\CCC(c1cccc([N+](=O)[O-])c1)c1ccccn1)NCCCc1c[nH]cn1 10.1021/jm00128a045
CHEMBL58750 199072 0 None - 0 Guinea pig 5.8 pKd = 5.8 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 407 10 3 5 2.8 N/C(=N\CCC(c1cccc([N+](=O)[O-])c1)c1ccccn1)NCCCc1c[nH]cn1 10.1021/jm00128a045
44457690 85526 0 None - 0 Guinea pig 7.8 pKd = 7.8 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 603 17 1 7 5.8 COc1ccc(CN(CCN(C)CCCCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)c2ccccn2)cc1 10.1016/s0960-894x(03)00113-6
CHEMBL22749 85526 0 None - 0 Guinea pig 7.8 pKd = 7.8 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 603 17 1 7 5.8 COc1ccc(CN(CCN(C)CCCCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)c2ccccn2)cc1 10.1016/s0960-894x(03)00113-6
25149427 185961 0 None - 0 Guinea pig 5.7 pKd = 5.7 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 313 8 4 3 2.0 N=C(NCCCc1c[nH]cn1)NC(=O)CCCc1ccccc1 10.1021/jm800841w
CHEMBL486962 185961 0 None - 0 Guinea pig 5.7 pKd = 5.7 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 313 8 4 3 2.0 N=C(NCCCc1c[nH]cn1)NC(=O)CCCc1ccccc1 10.1021/jm800841w
10423703 107295 0 None - 1 Guinea pig 7.7 pKd = 7.7 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 278 5 0 3 2.5 Cc1cccc(C2SCC(=O)N2CCCN(C)C)c1 10.1021/jm00093a025
CHEMBL1202942 107295 0 None - 1 Guinea pig 7.7 pKd = 7.7 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 278 5 0 3 2.5 Cc1cccc(C2SCC(=O)N2CCCN(C)C)c1 10.1021/jm00093a025
CHEMBL317171 107295 0 None - 1 Guinea pig 7.7 pKd = 7.7 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 278 5 0 3 2.5 Cc1cccc(C2SCC(=O)N2CCCN(C)C)c1 10.1021/jm00093a025
14660380 198707 0 None - 0 Guinea pig 6.7 pKd = 6.7 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 380 9 4 3 3.2 N=C(NCCCc1c[nH]cn1)NCCC(c1ccc(F)cc1)c1cccnc1 10.1021/jm00128a045
CHEMBL58170 198707 0 None - 0 Guinea pig 6.7 pKd = 6.7 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 380 9 4 3 3.2 N=C(NCCCc1c[nH]cn1)NCCC(c1ccc(F)cc1)c1cccnc1 10.1021/jm00128a045
10342634 200019 0 None - 0 Guinea pig 6.7 pKd = 6.7 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 429 9 4 2 5.0 N=C(NCCCc1c[nH]cn1)NCCC(c1ccccc1)c1ccc(Cl)c(Cl)c1 10.1021/jm00128a045
CHEMBL59544 200019 0 None - 0 Guinea pig 6.7 pKd = 6.7 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 429 9 4 2 5.0 N=C(NCCCc1c[nH]cn1)NCCC(c1ccccc1)c1ccc(Cl)c(Cl)c1 10.1021/jm00128a045
11436304 11337 0 None - 0 Guinea pig 4.7 pKd = 4.7 Functional
Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum
ChEMBL 236 8 1 2 3.3 c1nc(CCCOCCCC2CCCC2)c[nH]1 10.1021/jm031065q
CHEMBL1179594 11337 0 None - 0 Guinea pig 4.7 pKd = 4.7 Functional
Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum
ChEMBL 236 8 1 2 3.3 c1nc(CCCOCCCC2CCCC2)c[nH]1 10.1021/jm031065q
CHEMBL88306 11337 0 None - 0 Guinea pig 4.7 pKd = 4.7 Functional
Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum
ChEMBL 236 8 1 2 3.3 c1nc(CCCOCCCC2CCCC2)c[nH]1 10.1021/jm031065q
10375442 11340 0 None - 1 Guinea pig 4.7 pKd = 4.7 Functional
Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum
ChEMBL 196 8 1 2 2.5 CCCCCOCCCc1c[nH]cn1 10.1021/jm031065q
CHEMBL1179604 11340 0 None - 1 Guinea pig 4.7 pKd = 4.7 Functional
Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum
ChEMBL 196 8 1 2 2.5 CCCCCOCCCc1c[nH]cn1 10.1021/jm031065q
CHEMBL88746 11340 0 None - 1 Guinea pig 4.7 pKd = 4.7 Functional
Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum
ChEMBL 196 8 1 2 2.5 CCCCCOCCCc1c[nH]cn1 10.1021/jm031065q
25190258 161152 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 419 10 1 5 3.4 CCCCc1cc(OC2CCN(CCNS(=O)(=O)CC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4079248 161152 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 419 10 1 5 3.4 CCCCc1cc(OC2CCN(CCNS(=O)(=O)CC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4117327 161152 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 419 10 1 5 3.4 CCCCc1cc(OC2CCN(CCNS(=O)(=O)CC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
11791817 98303 0 None -1 2 Guinea pig 8.7 pKd = 8.7 Functional
Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine
ChEMBL 345 9 2 2 4.5 c1ccc(C(CCc2nc(CCNC3CC3)c[nH]2)c2ccccc2)cc1 10.1021/jm991056a
CHEMBL274831 98303 0 None -1 2 Guinea pig 8.7 pKd = 8.7 Functional
Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine
ChEMBL 345 9 2 2 4.5 c1ccc(C(CCc2nc(CCNC3CC3)c[nH]2)c2ccccc2)cc1 10.1021/jm991056a
71449250 80471 0 None - 0 Human 8.6 pKd = 8.6 Functional
Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay
ChEMBL 368 4 0 5 3.1 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccncc2c1=O 10.1016/j.bmc.2012.08.032
CHEMBL2146804 80471 0 None - 0 Human 8.6 pKd = 8.6 Functional
Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay
ChEMBL 368 4 0 5 3.1 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccncc2c1=O 10.1016/j.bmc.2012.08.032
57780007 146991 0 None - 0 Human 8.6 pKd = 8.6 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 572 13 1 6 5.8 CCc1cc(N2CCN(CCc3ccc(OCCCN4CCCCCC4)cc3)CC2)c2nc(CCC(=O)O)ccc2c1 10.1016/j.bmcl.2016.11.022
CHEMBL3926412 146991 0 None - 0 Human 8.6 pKd = 8.6 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 572 13 1 6 5.8 CCc1cc(N2CCN(CCc3ccc(OCCCN4CCCCCC4)cc3)CC2)c2nc(CCC(=O)O)ccc2c1 10.1016/j.bmcl.2016.11.022
25190254 161103 0 None - 0 Human 8.6 pKd = 8.6 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 432 10 0 5 4.6 CCCCc1cc(OC2CCN(CCC(C)S(=O)(=O)CC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4068414 161103 0 None - 0 Human 8.6 pKd = 8.6 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 432 10 0 5 4.6 CCCCc1cc(OC2CCN(CCC(C)S(=O)(=O)CC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4117012 161103 0 None - 0 Human 8.6 pKd = 8.6 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 432 10 0 5 4.6 CCCCc1cc(OC2CCN(CCC(C)S(=O)(=O)CC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
10042467 1426 1 None -1 2 Guinea pig 8.6 pKd = 8.6 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM
ChEMBL 333 8 1 2 4.3 CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C 10.1021/jm991056a
1203 1426 1 None -1 2 Guinea pig 8.6 pKd = 8.6 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM
ChEMBL 333 8 1 2 4.3 CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C 10.1021/jm991056a
CHEMBL11553 1426 1 None -1 2 Guinea pig 8.6 pKd = 8.6 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM
ChEMBL 333 8 1 2 4.3 CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C 10.1021/jm991056a
57390224 67877 0 None - 0 Guinea pig 7.7 pKd = 7.7 Functional
Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins
ChEMBL 503 8 1 5 4.7 COc1ccc(CN(CCN2CCN(C(=O)c3cc4cc(Cl)ccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
CHEMBL1910379 67877 0 None - 0 Guinea pig 7.7 pKd = 7.7 Functional
Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins
ChEMBL 503 8 1 5 4.7 COc1ccc(CN(CCN2CCN(C(=O)c3cc4cc(Cl)ccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
44457702 83169 0 None - 0 Guinea pig 7.7 pKd = 7.7 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 728 17 3 9 7.3 COc1ccc(CN(CCN(C)CCCCCCNC(=O)c2ccc(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c(C(=O)O)c2)c2ccccn2)cc1 10.1016/s0960-894x(03)00113-6
CHEMBL21833 83169 0 None - 0 Guinea pig 7.7 pKd = 7.7 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 728 17 3 9 7.3 COc1ccc(CN(CCN(C)CCCCCCNC(=O)c2ccc(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c(C(=O)O)c2)c2ccccn2)cc1 10.1016/s0960-894x(03)00113-6
25149712 178986 0 None - 3 Guinea pig 5.7 pKd = 5.7 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 299 7 4 3 1.6 N=C(NCCCc1c[nH]cn1)NC(=O)CCc1ccccc1 10.1021/jm800841w
CHEMBL470790 178986 0 None - 3 Guinea pig 5.7 pKd = 5.7 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 299 7 4 3 1.6 N=C(NCCCc1c[nH]cn1)NC(=O)CCc1ccccc1 10.1021/jm800841w
11956130 185965 0 None - 0 Guinea pig 5.7 pKd = 5.7 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 319 7 4 3 2.6 CC(CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1 10.1021/jm800841w
CHEMBL486965 185965 0 None - 0 Guinea pig 5.7 pKd = 5.7 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 319 7 4 3 2.6 CC(CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1 10.1021/jm800841w
1221 475 9 None - 0 Guinea pig 7.7 pKd = 7.7 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 380 9 3 3 3.0 NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)F 10.1021/jm00128a045
65895 475 9 None - 0 Guinea pig 7.7 pKd = 7.7 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 380 9 3 3 3.0 NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)F 10.1021/jm00128a045
CHEMBL293802 475 9 None - 0 Guinea pig 7.7 pKd = 7.7 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 380 9 3 3 3.0 NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)F 10.1021/jm00128a045
1221 475 9 None - 0 Guinea pig 7.7 pKd = 7.7 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 380 9 3 3 3.0 NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)F 10.1021/jm800841w
65895 475 9 None - 0 Guinea pig 7.7 pKd = 7.7 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 380 9 3 3 3.0 NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)F 10.1021/jm800841w
CHEMBL293802 475 9 None - 0 Guinea pig 7.7 pKd = 7.7 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 380 9 3 3 3.0 NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)F 10.1021/jm800841w
19762580 80793 0 None - 0 Guinea pig 7.7 pKd = 7.7 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 342 11 1 5 2.8 COc1ccc(CN(CCN(C)CCCCN)c2ccccn2)cc1 10.1016/s0960-894x(03)00113-6
CHEMBL21520 80793 0 None - 0 Guinea pig 7.7 pKd = 7.7 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 342 11 1 5 2.8 COc1ccc(CN(CCN(C)CCCCN)c2ccccn2)cc1 10.1016/s0960-894x(03)00113-6
15179508 204695 0 None - 0 Guinea pig 5.7 pKd = 5.7 Functional
Histamine H1 receptor antagonistic activity on the isolated guinea pig ileum determined by Schild plot.Histamine H1 receptor antagonistic activity on the isolated guinea pig ileum determined by Schild plot.
ChEMBL 588 11 3 5 3.5 N#CN/C(=N\CCNC(=O)c1cccc(I)c1)NCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm00090a013
CHEMBL73994 204695 0 None - 0 Guinea pig 5.7 pKd = 5.7 Functional
Histamine H1 receptor antagonistic activity on the isolated guinea pig ileum determined by Schild plot.Histamine H1 receptor antagonistic activity on the isolated guinea pig ileum determined by Schild plot.
ChEMBL 588 11 3 5 3.5 N#CN/C(=N\CCNC(=O)c1cccc(I)c1)NCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm00090a013
14660391 199053 0 None - 0 Guinea pig 6.6 pKd = 6.6 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 272 5 3 2 2.2 N=C(N)NCCC(c1ccc(F)cc1)c1ccccn1 10.1021/jm00128a045
CHEMBL58620 199053 0 None - 0 Guinea pig 6.6 pKd = 6.6 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 272 5 3 2 2.2 N=C(N)NCCC(c1ccc(F)cc1)c1ccccn1 10.1021/jm00128a045
25149429 185964 0 None - 0 Guinea pig 5.6 pKd = 5.6 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 305 6 4 3 2.2 CC(C(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1 10.1021/jm800841w
CHEMBL486964 185964 0 None - 0 Guinea pig 5.6 pKd = 5.6 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 305 6 4 3 2.2 CC(C(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1 10.1021/jm800841w
25149814 185324 0 None - 0 Guinea pig 5.6 pKd = 5.6 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 291 6 4 3 2.0 N=C(NCCCc1c[nH]cn1)NC(=O)CC1CCCCC1 10.1021/jm800841w
CHEMBL485958 185324 0 None - 0 Guinea pig 5.6 pKd = 5.6 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 291 6 4 3 2.0 N=C(NCCCc1c[nH]cn1)NC(=O)CC1CCCCC1 10.1021/jm800841w
10022429 162789 0 None - 0 Guinea pig 6.6 pKd = 6.6 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 376 10 4 3 3.5 N=C(NCCCc1c[nH]cn1)NCCCC(c1ccccc1)c1ccccn1 10.1021/jm00128a045
CHEMBL417221 162789 0 None - 0 Guinea pig 6.6 pKd = 6.6 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 376 10 4 3 3.5 N=C(NCCCc1c[nH]cn1)NCCCC(c1ccccc1)c1ccccn1 10.1021/jm00128a045
11276413 12071 0 None - 0 Guinea pig 5.6 pKd = 5.6 Functional
Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum
ChEMBL 236 7 1 2 3.3 c1nc(CCCOCCC2CCCCC2)c[nH]1 10.1021/jm031065q
CHEMBL1183700 12071 0 None - 0 Guinea pig 5.6 pKd = 5.6 Functional
Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum
ChEMBL 236 7 1 2 3.3 c1nc(CCCOCCC2CCCCC2)c[nH]1 10.1021/jm031065q
CHEMBL313803 12071 0 None - 0 Guinea pig 5.6 pKd = 5.6 Functional
Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum
ChEMBL 236 7 1 2 3.3 c1nc(CCCOCCC2CCCCC2)c[nH]1 10.1021/jm031065q
54710792 126417 0 None - 0 Guinea pig 5.6 pKd = 5.6 Functional
H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum
ChEMBL 429 5 1 7 3.4 O=c1oc2cc(CN3CCN(Cc4ccc(Cl)cc4)CC3)ccc2c(O)c1[N+](=O)[O-] 10.1021/jm00377a013
CHEMBL36517 126417 0 None - 0 Guinea pig 5.6 pKd = 5.6 Functional
H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum
ChEMBL 429 5 1 7 3.4 O=c1oc2cc(CN3CCN(Cc4ccc(Cl)cc4)CC3)ccc2c(O)c1[N+](=O)[O-] 10.1021/jm00377a013
2861271 4254 9 None - 1 Guinea pig 5.6 pKd = 5.6 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 298 5 0 3 2.9 CN(C)CCCN1C(=O)CSC1c1ccc(Cl)cc1 10.1021/jm00093a025
CHEMBL100486 4254 9 None - 1 Guinea pig 5.6 pKd = 5.6 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 298 5 0 3 2.9 CN(C)CCCN1C(=O)CSC1c1ccc(Cl)cc1 10.1021/jm00093a025
10729993 11408 1 None - 0 Guinea pig 4.6 pKd = 4.6 Functional
Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum
ChEMBL 259 6 2 4 2.6 C/C(=N\O)c1ccc(OCCCc2c[nH]cn2)cc1 10.1021/jm000971p
CHEMBL114085 11408 1 None - 0 Guinea pig 4.6 pKd = 4.6 Functional
Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum
ChEMBL 259 6 2 4 2.6 C/C(=N\O)c1ccc(OCCCc2c[nH]cn2)cc1 10.1021/jm000971p
CHEMBL1180120 11408 1 None - 0 Guinea pig 4.6 pKd = 4.6 Functional
Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum
ChEMBL 259 6 2 4 2.6 C/C(=N\O)c1ccc(OCCCc2c[nH]cn2)cc1 10.1021/jm000971p
10492497 12374 0 None - 0 Guinea pig 4.6 pKd = 4.6 Functional
Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum
ChEMBL 273 7 2 4 3.0 CC/C(=N\O)c1ccc(OCCCc2c[nH]cn2)cc1 10.1021/jm000971p
CHEMBL1185539 12374 0 None - 0 Guinea pig 4.6 pKd = 4.6 Functional
Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum
ChEMBL 273 7 2 4 3.0 CC/C(=N\O)c1ccc(OCCCc2c[nH]cn2)cc1 10.1021/jm000971p
CHEMBL420124 12374 0 None - 0 Guinea pig 4.6 pKd = 4.6 Functional
Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum
ChEMBL 273 7 2 4 3.0 CC/C(=N\O)c1ccc(OCCCc2c[nH]cn2)cc1 10.1021/jm000971p
44274554 83293 0 None - 0 Guinea pig 7.6 pKd = 7.6 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 726 17 4 9 7.3 COc1ccc(CN(CCN(C)CCCCCCNC(=O)c2ccc(-c3c4ccc(=N)cc-4oc4cc(N)ccc34)c(C(=O)O)c2)c2ccccn2)cc1 10.1016/s0960-894x(03)00113-6
CHEMBL21898 83293 0 None - 0 Guinea pig 7.6 pKd = 7.6 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 726 17 4 9 7.3 COc1ccc(CN(CCN(C)CCCCCCNC(=O)c2ccc(-c3c4ccc(=N)cc-4oc4cc(N)ccc34)c(C(=O)O)c2)c2ccccn2)cc1 10.1016/s0960-894x(03)00113-6
44457689 94149 0 None - 0 Guinea pig 7.6 pKd = 7.6 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 728 17 3 9 7.3 COc1ccc(CN(CCN(C)CCCCCCNC(=O)c2ccc(C(=O)O)c(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c2)c2ccccn2)cc1 10.1016/s0960-894x(03)00113-6
CHEMBL24940 94149 0 None - 0 Guinea pig 7.6 pKd = 7.6 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 728 17 3 9 7.3 COc1ccc(CN(CCN(C)CCCCCCNC(=O)c2ccc(C(=O)O)c(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c2)c2ccccn2)cc1 10.1016/s0960-894x(03)00113-6
14660350 199443 0 None - 0 Guinea pig 6.6 pKd = 6.6 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 392 10 3 4 2.9 COc1ccc(C(CC/N=C(\N)NCCCc2c[nH]cn2)c2ccccn2)cc1 10.1021/jm00128a045
CHEMBL59138 199443 0 None - 0 Guinea pig 6.6 pKd = 6.6 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 392 10 3 4 2.9 COc1ccc(C(CC/N=C(\N)NCCCc2c[nH]cn2)c2ccccn2)cc1 10.1021/jm00128a045
164435 204542 32 None - 0 Guinea pig 4.6 pKd = 4.6 Functional
Histamine H1 receptor antagonistic activity on the isolated guinea pig ileum determined by Schild plot.Histamine H1 receptor antagonistic activity on the isolated guinea pig ileum determined by Schild plot.
ChEMBL 477 11 4 6 2.5 N#CN/C(=N\CCNC(=O)c1ccc(N)cc1)NCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm00090a013
CHEMBL72844 204542 32 None - 0 Guinea pig 4.6 pKd = 4.6 Functional
Histamine H1 receptor antagonistic activity on the isolated guinea pig ileum determined by Schild plot.Histamine H1 receptor antagonistic activity on the isolated guinea pig ileum determined by Schild plot.
ChEMBL 477 11 4 6 2.5 N#CN/C(=N\CCNC(=O)c1ccc(N)cc1)NCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm00090a013
3081064 200435 12 None - 0 Guinea pig 6.6 pKd = 6.6 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 398 9 4 3 3.4 N=C(NCCCc1c[nH]cn1)NCCC(c1cc(F)cc(F)c1)c1ccccn1 10.1021/jm00128a045
CHEMBL59832 200435 12 None - 0 Guinea pig 6.6 pKd = 6.6 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 398 9 4 3 3.4 N=C(NCCCc1c[nH]cn1)NCCC(c1cc(F)cc(F)c1)c1ccccn1 10.1021/jm00128a045
14660355 100545 0 None - 0 Guinea pig 6.6 pKd = 6.6 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 430 9 4 3 4.1 N=C(NCCCc1c[nH]cn1)NCCC(c1ccc(C(F)(F)F)cc1)c1ccccn1 10.1021/jm00128a045
CHEMBL291396 100545 0 None - 0 Guinea pig 6.6 pKd = 6.6 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 430 9 4 3 4.1 N=C(NCCCc1c[nH]cn1)NCCC(c1ccc(C(F)(F)F)cc1)c1ccccn1 10.1021/jm00128a045
14660372 199231 0 None - 0 Guinea pig 6.5 pKd = 6.5 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 430 9 4 3 4.4 N=C(NCCCc1c[nH]cn1)NCCC(c1ccccn1)c1ccc(Cl)cc1Cl 10.1021/jm00128a045
CHEMBL58999 199231 0 None - 0 Guinea pig 6.5 pKd = 6.5 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 430 9 4 3 4.4 N=C(NCCCc1c[nH]cn1)NCCC(c1ccccn1)c1ccc(Cl)cc1Cl 10.1021/jm00128a045
11741669 96753 0 None 39 2 Guinea pig 8.5 pKd = 8.5 Functional
Apparent pA2 value of compound at 10 nM concentration of mepyramine in guinea pig ileumApparent pA2 value of compound at 10 nM concentration of mepyramine in guinea pig ileum
ChEMBL 399 11 3 3 4.3 c1ccc(C(CCc2nc(CCNCCc3cnc[nH]3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
CHEMBL264491 96753 0 None 39 2 Guinea pig 8.5 pKd = 8.5 Functional
Apparent pA2 value of compound at 10 nM concentration of mepyramine in guinea pig ileumApparent pA2 value of compound at 10 nM concentration of mepyramine in guinea pig ileum
ChEMBL 399 11 3 3 4.3 c1ccc(C(CCc2nc(CCNCCc3cnc[nH]3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
11269875 121004 0 None - 1 Guinea pig 8.5 pKd = 8.5 Functional
Apparent pA2 value of compound at 10 nM concentration of mepyramine in guinea pig ileumApparent pA2 value of compound at 10 nM concentration of mepyramine in guinea pig ileum
ChEMBL 410 11 2 3 4.9 c1ccc(C(CCc2nc(CCNCCc3cccnc3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
CHEMBL356449 121004 0 None - 1 Guinea pig 8.5 pKd = 8.5 Functional
Apparent pA2 value of compound at 10 nM concentration of mepyramine in guinea pig ileumApparent pA2 value of compound at 10 nM concentration of mepyramine in guinea pig ileum
ChEMBL 410 11 2 3 4.9 c1ccc(C(CCc2nc(CCNCCc3cccnc3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
44274585 82302 0 None - 0 Guinea pig 8.5 pKd = 8.5 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 756 19 3 9 8.1 COc1ccc(CN(CCN(C)CCCCCCCCNC(=O)c2ccc(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c(C(=O)O)c2)c2ccccn2)cc1 10.1016/s0960-894x(03)00113-6
CHEMBL21721 82302 0 None - 0 Guinea pig 8.5 pKd = 8.5 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 756 19 3 9 8.1 COc1ccc(CN(CCN(C)CCCCCCCCNC(=O)c2ccc(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c(C(=O)O)c2)c2ccccn2)cc1 10.1016/s0960-894x(03)00113-6
25190134 161144 0 None - 0 Human 8.4 pKd = 8.4 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 404 9 0 5 3.9 CCCCc1cc(OC2CCN(CCS(=O)(=O)CC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4085417 161144 0 None - 0 Human 8.4 pKd = 8.4 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 404 9 0 5 3.9 CCCCc1cc(OC2CCN(CCS(=O)(=O)CC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
CHEMBL4117296 161144 0 None - 0 Human 8.4 pKd = 8.4 Functional
Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method
ChEMBL 404 9 0 5 3.9 CCCCc1cc(OC2CCN(CCS(=O)(=O)CC)CC2)c2ncccc2c1 10.1016/j.bmcl.2017.09.020
2247 505 81 None - 42 Guinea pig 8.4 pKd = 8.4 Functional
Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1016/j.bmcl.2011.09.001
249 505 81 None - 42 Guinea pig 8.4 pKd = 8.4 Functional
Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1016/j.bmcl.2011.09.001
2603 505 81 None - 42 Guinea pig 8.4 pKd = 8.4 Functional
Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1016/j.bmcl.2011.09.001
CHEMBL296419 505 81 None - 42 Guinea pig 8.4 pKd = 8.4 Functional
Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1016/j.bmcl.2011.09.001
DB00637 505 81 None - 42 Guinea pig 8.4 pKd = 8.4 Functional
Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1016/j.bmcl.2011.09.001
57393730 67884 0 None - 0 Guinea pig 8.4 pKd = 8.4 Functional
Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins
ChEMBL 579 8 2 6 5.0 O=C(c1cc2ccccc2[nH]1)N1CCN(CCN2CCC(Nc3nc4ccccc4n3Cc3ccc(F)cc3)CC2)CC1 10.1016/j.bmcl.2011.09.001
CHEMBL1910386 67884 0 None - 0 Guinea pig 8.4 pKd = 8.4 Functional
Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins
ChEMBL 579 8 2 6 5.0 O=C(c1cc2ccccc2[nH]1)N1CCN(CCN2CCC(Nc3nc4ccccc4n3Cc3ccc(F)cc3)CC2)CC1 10.1016/j.bmcl.2011.09.001
71456361 80479 0 None - 0 Human 8.4 pKd = 8.4 Functional
Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay
ChEMBL 369 4 0 6 2.5 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2nccnc2c1=O 10.1016/j.bmc.2012.08.032
CHEMBL2146812 80479 0 None - 0 Human 8.4 pKd = 8.4 Functional
Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay
ChEMBL 369 4 0 6 2.5 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2nccnc2c1=O 10.1016/j.bmc.2012.08.032
24803639 61331 0 None - 0 Human 8.4 pKd = 8.4 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assay
ChEMBL 622 14 1 7 6.8 O=c1c2ccccc2c(Cc2ccc(O)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1021/jm1013874
CHEMBL1767166 61331 0 None - 0 Human 8.4 pKd = 8.4 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assay
ChEMBL 622 14 1 7 6.8 O=c1c2ccccc2c(Cc2ccc(O)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1021/jm1013874
13676696 164073 0 None - 0 Guinea pig 8.4 pKd = 8.4 Functional
H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum
ChEMBL 467 7 1 8 4.0 Cc1c(OCCCN2CCN(Cc3cccc(Cl)c3)CC2)ccc2c(O)c3nnnc-3oc12 10.1021/jm00161a022
CHEMBL420934 164073 0 None - 0 Guinea pig 8.4 pKd = 8.4 Functional
H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum
ChEMBL 467 7 1 8 4.0 Cc1c(OCCCN2CCN(Cc3cccc(Cl)c3)CC2)ccc2c(O)c3nnnc-3oc12 10.1021/jm00161a022
13676697 204794 0 None - 0 Guinea pig 8.4 pKd = 8.4 Functional
H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum
ChEMBL 467 7 1 8 4.0 Cc1c(OCCCN2CCN(Cc3ccccc3Cl)CC2)ccc2c(O)c3nnnc-3oc12 10.1021/jm00161a022
CHEMBL74989 204794 0 None - 0 Guinea pig 8.4 pKd = 8.4 Functional
H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum
ChEMBL 467 7 1 8 4.0 Cc1c(OCCCN2CCN(Cc3ccccc3Cl)CC2)ccc2c(O)c3nnnc-3oc12 10.1021/jm00161a022
54710795 99897 0 None - 0 Guinea pig 8.4 pKd = 8.4 Functional
H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum
ChEMBL 531 10 2 9 3.6 CCCc1c(OCC(O)CN2CCN(Cc3ccc(Cl)cc3)CC2)ccc2c(O)c([N+](=O)[O-])c(=O)oc12 10.1021/jm00377a013
CHEMBL286017 99897 0 None - 0 Guinea pig 8.4 pKd = 8.4 Functional
H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum
ChEMBL 531 10 2 9 3.6 CCCc1c(OCC(O)CN2CCN(Cc3ccc(Cl)cc3)CC2)ccc2c(O)c([N+](=O)[O-])c(=O)oc12 10.1021/jm00377a013
42625223 179925 0 None - 3 Guinea pig 5.5 pKd = 5.5 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions
ChEMBL 395 8 4 3 1.4 CN(CCC(=O)/N=C(\N)NCCCc1c[nH]cn1)C(=O)c1cc2ccccc2[nH]1 10.1021/jm9000693
CHEMBL474617 179925 0 None - 3 Guinea pig 5.5 pKd = 5.5 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions
ChEMBL 395 8 4 3 1.4 CN(CCC(=O)/N=C(\N)NCCCc1c[nH]cn1)C(=O)c1cc2ccccc2[nH]1 10.1021/jm9000693
44274584 80684 0 None - 0 Guinea pig 7.5 pKd = 7.5 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 700 15 3 9 6.5 COc1ccc(CN(CCN(C)CCCCNC(=O)c2ccc(C(=O)O)c(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c2)c2ccccn2)cc1 10.1016/s0960-894x(03)00113-6
CHEMBL21514 80684 0 None - 0 Guinea pig 7.5 pKd = 7.5 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 700 15 3 9 6.5 COc1ccc(CN(CCN(C)CCCCNC(=O)c2ccc(C(=O)O)c(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c2)c2ccccn2)cc1 10.1016/s0960-894x(03)00113-6
44274555 77008 0 None - 0 Guinea pig 7.5 pKd = 7.5 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 782 18 1 9 6.0 COc1ccc(CN(CCN(C)CCCCCCNC(=O)c2ccc(-c3c4ccc(=[N+](C)C)cc-4oc4cc(N(C)C)ccc34)c(C(=O)[O-])c2)c2ccccn2)cc1 10.1016/s0960-894x(03)00113-6
CHEMBL20713 77008 0 None - 0 Guinea pig 7.5 pKd = 7.5 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 782 18 1 9 6.0 COc1ccc(CN(CCN(C)CCCCCCNC(=O)c2ccc(-c3c4ccc(=[N+](C)C)cc-4oc4cc(N(C)C)ccc34)c(C(=O)[O-])c2)c2ccccn2)cc1 10.1016/s0960-894x(03)00113-6
14660378 100647 0 None - 0 Guinea pig 5.5 pKd = 5.5 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 348 8 4 3 2.7 N=C(NCCCc1c[nH]cn1)NCC(c1ccccc1)c1ccccn1 10.1021/jm00128a045
CHEMBL292170 100647 0 None - 0 Guinea pig 5.5 pKd = 5.5 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 348 8 4 3 2.7 N=C(NCCCc1c[nH]cn1)NCC(c1ccccc1)c1ccccn1 10.1021/jm00128a045
1226 2019 20 None - 1 Guinea pig 5.5 pKd = 5.5 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 10.1021/jm800841w
41376 2019 20 None - 1 Guinea pig 5.5 pKd = 5.5 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 10.1021/jm800841w
CHEMBL12608 2019 20 None - 1 Guinea pig 5.5 pKd = 5.5 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 10.1021/jm800841w
14660384 202733 0 None - 0 Guinea pig 7.5 pKd = 7.5 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 379 9 4 2 3.8 N=C(NCCCc1c[nH]cn1)NCCC(c1ccccc1)c1ccc(F)cc1 10.1021/jm00128a045
CHEMBL61852 202733 0 None - 0 Guinea pig 7.5 pKd = 7.5 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 379 9 4 2 3.8 N=C(NCCCc1c[nH]cn1)NCCC(c1ccccc1)c1ccc(F)cc1 10.1021/jm00128a045
14660395 202781 0 None - 0 Guinea pig 6.5 pKd = 6.5 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 378 8 4 3 3.1 N=C(NC/C=C(\c1ccc(F)cc1)c1ccccn1)NCCCc1c[nH]cn1 10.1021/jm00128a045
CHEMBL62147 202781 0 None - 0 Guinea pig 6.5 pKd = 6.5 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 378 8 4 3 3.1 N=C(NC/C=C(\c1ccc(F)cc1)c1ccccn1)NCCCc1c[nH]cn1 10.1021/jm00128a045
42625386 178353 0 None - 4 Guinea pig 5.5 pKd = 5.5 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions
ChEMBL 237 6 3 2 0.6 CCCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL465170 178353 0 None - 4 Guinea pig 5.5 pKd = 5.5 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions
ChEMBL 237 6 3 2 0.6 CCCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
44274553 82399 0 None - 0 Guinea pig 7.4 pKd = 7.4 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 828 17 3 9 9.7 COc1ccc(CN(CCN(C)CCCCCCNC(=O)c2ccc(-c3c4ccc5cc(O)ccc5c4oc4c3ccc3cc(=O)ccc34)c(C(=O)O)c2)c2ccccn2)cc1 10.1016/s0960-894x(03)00113-6
CHEMBL21727 82399 0 None - 0 Guinea pig 7.4 pKd = 7.4 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 828 17 3 9 9.7 COc1ccc(CN(CCN(C)CCCCCCNC(=O)c2ccc(-c3c4ccc5cc(O)ccc5c4oc4c3ccc3cc(=O)ccc34)c(C(=O)O)c2)c2ccccn2)cc1 10.1016/s0960-894x(03)00113-6
14660382 198660 0 None - 0 Guinea pig 7.4 pKd = 7.4 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 380 9 4 3 3.2 N=C(NCCCc1c[nH]cn1)NCCC(c1ccncc1)c1ccc(F)cc1 10.1021/jm00128a045
CHEMBL57933 198660 0 None - 0 Guinea pig 7.4 pKd = 7.4 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 380 9 4 3 3.2 N=C(NCCCc1c[nH]cn1)NCCC(c1ccncc1)c1ccc(F)cc1 10.1021/jm00128a045
1199 2976 0 None - 0 Guinea pig 5.4 pKd = 5.4 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 394 8 3 4 2.5 NC(=NCCCc1[nH]cnc1)NC(=O)CC(c1ccccn1)c1ccc(cc1)F 10.1021/jm800841w
25149244 2976 0 None - 0 Guinea pig 5.4 pKd = 5.4 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 394 8 3 4 2.5 NC(=NCCCc1[nH]cnc1)NC(=O)CC(c1ccccn1)c1ccc(cc1)F 10.1021/jm800841w
CHEMBL472273 2976 0 None - 0 Guinea pig 5.4 pKd = 5.4 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 394 8 3 4 2.5 NC(=NCCCc1[nH]cnc1)NC(=O)CC(c1ccccn1)c1ccc(cc1)F 10.1021/jm800841w
42626109 179768 0 None - 2 Guinea pig 7.4 pKd = 7.4 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions
ChEMBL 324 6 4 2 1.5 N/C(=N\C(=O)Cc1c[nH]c2ccccc12)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL474447 179768 0 None - 2 Guinea pig 7.4 pKd = 7.4 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions
ChEMBL 324 6 4 2 1.5 N/C(=N\C(=O)Cc1c[nH]c2ccccc12)NCCCc1c[nH]cn1 10.1021/jm9000693
14660376 202568 0 None - 0 Guinea pig 6.4 pKd = 6.4 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 363 9 4 4 2.5 N=C(NCCCc1c[nH]cn1)NCCC(c1ccccn1)c1ccccn1 10.1021/jm00128a045
CHEMBL61185 202568 0 None - 0 Guinea pig 6.4 pKd = 6.4 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 363 9 4 4 2.5 N=C(NCCCc1c[nH]cn1)NCCC(c1ccccn1)c1ccccn1 10.1021/jm00128a045
2861590 107260 7 None - 1 Guinea pig 7.4 pKd = 7.4 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 342 5 0 3 3.0 CN(C)CCCN1C(=O)CSC1c1ccc(Br)cc1 10.1021/jm00093a025
CHEMBL1202937 107260 7 None - 1 Guinea pig 7.4 pKd = 7.4 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 342 5 0 3 3.0 CN(C)CCCN1C(=O)CSC1c1ccc(Br)cc1 10.1021/jm00093a025
CHEMBL316951 107260 7 None - 1 Guinea pig 7.4 pKd = 7.4 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 342 5 0 3 3.0 CN(C)CCCN1C(=O)CSC1c1ccc(Br)cc1 10.1021/jm00093a025
126624 208290 10 None - 1 Guinea pig 7.4 pKd = 7.4 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 264 5 0 3 2.2 CN(C)CCCN1C(=O)CSC1c1ccccc1 10.1021/jm00093a025
CHEMBL1202936 208290 10 None - 1 Guinea pig 7.4 pKd = 7.4 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 264 5 0 3 2.2 CN(C)CCCN1C(=O)CSC1c1ccccc1 10.1021/jm00093a025
CHEMBL98989 208290 10 None - 1 Guinea pig 7.4 pKd = 7.4 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 264 5 0 3 2.2 CN(C)CCCN1C(=O)CSC1c1ccccc1 10.1021/jm00093a025
42625221 189588 0 None - 2 Guinea pig 6.4 pKd = 6.4 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions
ChEMBL 338 7 4 2 1.9 N/C(=N\C(=O)CCc1c[nH]c2ccccc12)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL514641 189588 0 None - 2 Guinea pig 6.4 pKd = 6.4 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions
ChEMBL 338 7 4 2 1.9 N/C(=N\C(=O)CCc1c[nH]c2ccccc12)NCCCc1c[nH]cn1 10.1021/jm9000693
14984033 208178 1 None - 1 Guinea pig 6.4 pKd = 6.4 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 294 6 0 4 2.2 COc1cccc(C2SCC(=O)N2CCCN(C)C)c1 10.1021/jm00093a025
CHEMBL1202941 208178 1 None - 1 Guinea pig 6.4 pKd = 6.4 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 294 6 0 4 2.2 COc1cccc(C2SCC(=O)N2CCCN(C)C)c1 10.1021/jm00093a025
CHEMBL98334 208178 1 None - 1 Guinea pig 6.4 pKd = 6.4 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 294 6 0 4 2.2 COc1cccc(C2SCC(=O)N2CCCN(C)C)c1 10.1021/jm00093a025
14984032 208341 1 None - 1 Guinea pig 6.4 pKd = 6.4 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 342 5 0 3 3.0 CN(C)CCCN1C(=O)CSC1c1cccc(Br)c1 10.1021/jm00093a025
CHEMBL1202932 208341 1 None - 1 Guinea pig 6.4 pKd = 6.4 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 342 5 0 3 3.0 CN(C)CCCN1C(=O)CSC1c1cccc(Br)c1 10.1021/jm00093a025
CHEMBL99350 208341 1 None - 1 Guinea pig 6.4 pKd = 6.4 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 342 5 0 3 3.0 CN(C)CCCN1C(=O)CSC1c1cccc(Br)c1 10.1021/jm00093a025
14984031 208373 1 None - 1 Guinea pig 6.4 pKd = 6.4 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 282 5 0 3 2.4 CN(C)CCCN1C(=O)CSC1c1cccc(F)c1 10.1021/jm00093a025
CHEMBL1202933 208373 1 None - 1 Guinea pig 6.4 pKd = 6.4 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 282 5 0 3 2.4 CN(C)CCCN1C(=O)CSC1c1cccc(F)c1 10.1021/jm00093a025
CHEMBL99529 208373 1 None - 1 Guinea pig 6.4 pKd = 6.4 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 282 5 0 3 2.4 CN(C)CCCN1C(=O)CSC1c1cccc(F)c1 10.1021/jm00093a025
2861786 208177 8 None - 0 Guinea pig 5.4 pKd = 5.4 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 309 6 0 5 2.1 CN(C)CCCN1C(=O)CSC1c1cccc([N+](=O)[O-])c1 10.1021/jm00093a025
CHEMBL1202940 208177 8 None - 0 Guinea pig 5.4 pKd = 5.4 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 309 6 0 5 2.1 CN(C)CCCN1C(=O)CSC1c1cccc([N+](=O)[O-])c1 10.1021/jm00093a025
CHEMBL98333 208177 8 None - 0 Guinea pig 5.4 pKd = 5.4 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 309 6 0 5 2.1 CN(C)CCCN1C(=O)CSC1c1cccc([N+](=O)[O-])c1 10.1021/jm00093a025
10364258 45769 0 None 12 2 Guinea pig 8.4 pKd = 8.4 Functional
Apparent pA2 value of compound at 10 nM concentration of mepyramine in guinea pig ileumApparent pA2 value of compound at 10 nM concentration of mepyramine in guinea pig ileum
ChEMBL 410 11 2 3 4.9 c1ccc(C(CCc2nc(CCNCCc3ccccn3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
CHEMBL153067 45769 0 None 12 2 Guinea pig 8.4 pKd = 8.4 Functional
Apparent pA2 value of compound at 10 nM concentration of mepyramine in guinea pig ileumApparent pA2 value of compound at 10 nM concentration of mepyramine in guinea pig ileum
ChEMBL 410 11 2 3 4.9 c1ccc(C(CCc2nc(CCNCCc3ccccn3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
44274569 80841 0 None - 0 Guinea pig 8.4 pKd = 8.4 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 700 15 3 9 6.5 COc1ccc(CN(CCN(C)CCCCNC(=O)c2ccc(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c(C(=O)O)c2)c2ccccn2)cc1 10.1016/s0960-894x(03)00113-6
CHEMBL21525 80841 0 None - 0 Guinea pig 8.4 pKd = 8.4 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 700 15 3 9 6.5 COc1ccc(CN(CCN(C)CCCCNC(=O)c2ccc(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c(C(=O)O)c2)c2ccccn2)cc1 10.1016/s0960-894x(03)00113-6
44274548 99186 0 None - 0 Guinea pig 8.3 pKd = 8.3 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 477 12 1 10 3.6 COc1ccc(CN(CCN(C)CCNc2ccc([N+](=O)[O-])c3nonc23)c2ccccn2)cc1 10.1016/s0960-894x(03)00113-6
CHEMBL281365 99186 0 None - 0 Guinea pig 8.3 pKd = 8.3 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 477 12 1 10 3.6 COc1ccc(CN(CCN(C)CCNc2ccc([N+](=O)[O-])c3nonc23)c2ccccn2)cc1 10.1016/s0960-894x(03)00113-6
57402472 67879 0 None - 0 Guinea pig 8.3 pKd = 8.3 Functional
Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins
ChEMBL 526 11 1 6 4.0 COc1ccc(CN(CCN(C)CCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
CHEMBL1910381 67879 0 None - 0 Guinea pig 8.3 pKd = 8.3 Functional
Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins
ChEMBL 526 11 1 6 4.0 COc1ccc(CN(CCN(C)CCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
1200 3963 2 None - 0 Guinea pig 5.4 pKd = 5.4 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 335 8 4 5 0.7 O=C(NC(=NCCCc1cnc[nH]1)N)CSCc1nc[nH]c1C 10.1021/jm800841w
25149519 3963 2 None - 0 Guinea pig 5.4 pKd = 5.4 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 335 8 4 5 0.7 O=C(NC(=NCCCc1cnc[nH]1)N)CSCc1nc[nH]c1C 10.1021/jm800841w
CHEMBL513056 3963 2 None - 0 Guinea pig 5.4 pKd = 5.4 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 335 8 4 5 0.7 O=C(NC(=NCCCc1cnc[nH]1)N)CSCc1nc[nH]c1C 10.1021/jm800841w
14660370 163245 0 None - 0 Guinea pig 7.4 pKd = 7.4 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 430 9 4 3 4.4 N=C(NCCCc1c[nH]cn1)NCCC(c1cc(Cl)cc(Cl)c1)c1ccccn1 10.1021/jm00128a045
CHEMBL418508 163245 0 None - 0 Guinea pig 7.4 pKd = 7.4 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 430 9 4 3 4.4 N=C(NCCCc1c[nH]cn1)NCCC(c1cc(Cl)cc(Cl)c1)c1ccccn1 10.1021/jm00128a045
14660363 202678 0 None - 0 Guinea pig 6.4 pKd = 6.4 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 380 9 4 3 3.2 N=C(NCCCc1c[nH]cn1)NCCC(c1ccccn1)c1ccccc1F 10.1021/jm00128a045
CHEMBL61523 202678 0 None - 0 Guinea pig 6.4 pKd = 6.4 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 380 9 4 3 3.2 N=C(NCCCc1c[nH]cn1)NCCC(c1ccccn1)c1ccccc1F 10.1021/jm00128a045
14660411 199714 0 None - 0 Guinea pig 7.3 pKd = 7.3 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 368 9 4 4 3.1 N=C(NCCCc1c[nH]cn1)NCCC(c1ccccn1)c1cccs1 10.1021/jm00128a045
CHEMBL59339 199714 0 None - 0 Guinea pig 7.3 pKd = 7.3 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 368 9 4 4 3.1 N=C(NCCCc1c[nH]cn1)NCCC(c1ccccn1)c1cccs1 10.1021/jm00128a045
14660345 199093 0 None - 0 Guinea pig 7.3 pKd = 7.3 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 394 10 4 3 3.6 N=C(NCCCc1c[nH]cn1)NCCCC(c1ccc(F)cc1)c1ccccn1 10.1021/jm00128a045
CHEMBL58869 199093 0 None - 0 Guinea pig 7.3 pKd = 7.3 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 394 10 4 3 3.6 N=C(NCCCc1c[nH]cn1)NCCCC(c1ccc(F)cc1)c1ccccn1 10.1021/jm00128a045
25149613 179200 0 None - 2 Guinea pig 5.3 pKd = 5.3 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 382 8 4 5 2.7 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1nccs1 10.1021/jm800841w
CHEMBL472441 179200 0 None - 2 Guinea pig 5.3 pKd = 5.3 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 382 8 4 5 2.7 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1nccs1 10.1021/jm800841w
25149246 189476 0 None - 0 Guinea pig 5.3 pKd = 5.3 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 418 8 4 5 2.9 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccc(F)c(F)c1)c1nccs1 10.1021/jm800841w
CHEMBL513755 189476 0 None - 0 Guinea pig 5.3 pKd = 5.3 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 418 8 4 5 2.9 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccc(F)c(F)c1)c1nccs1 10.1021/jm800841w
54587323 63116 0 None - 1 Guinea pig 4.3 pKd = 4.3 Functional
Antagonist activity at histamine H1 receptor in guinea-pig ileumAntagonist activity at histamine H1 receptor in guinea-pig ileum
ChEMBL 277 7 2 3 3.0 O=C(NCCC1=CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1774596 63116 0 None - 1 Guinea pig 4.3 pKd = 4.3 Functional
Antagonist activity at histamine H1 receptor in guinea-pig ileumAntagonist activity at histamine H1 receptor in guinea-pig ileum
ChEMBL 277 7 2 3 3.0 O=C(NCCC1=CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1789341 63116 0 None - 1 Guinea pig 4.3 pKd = 4.3 Functional
Antagonist activity at histamine H1 receptor in guinea-pig ileumAntagonist activity at histamine H1 receptor in guinea-pig ileum
ChEMBL 277 7 2 3 3.0 O=C(NCCC1=CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
134136763 142848 0 None - 0 Human 8.3 pKd = 8.3 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 500 11 0 5 6.0 c1cnc2c(N3CCN(CCCCc4ccc(OCCCN5CCCCCC5)cc4)CC3)cccc2c1 10.1016/j.bmcl.2016.11.022
CHEMBL3893197 142848 0 None - 0 Human 8.3 pKd = 8.3 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 500 11 0 5 6.0 c1cnc2c(N3CCN(CCCCc4ccc(OCCCN5CCCCCC5)cc4)CC3)cccc2c1 10.1016/j.bmcl.2016.11.022
54710793 108821 0 None - 0 Guinea pig 8.3 pKd = 8.3 Functional
H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum
ChEMBL 489 8 2 9 2.6 O=c1oc2cc(OCC(O)CN3CCN(Cc4ccc(Cl)cc4)CC3)ccc2c(O)c1[N+](=O)[O-] 10.1021/jm00377a013
CHEMBL32097 108821 0 None - 0 Guinea pig 8.3 pKd = 8.3 Functional
H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum
ChEMBL 489 8 2 9 2.6 O=c1oc2cc(OCC(O)CN3CCN(Cc4ccc(Cl)cc4)CC3)ccc2c(O)c1[N+](=O)[O-] 10.1021/jm00377a013
44274583 98727 0 None - 0 Guinea pig 8.3 pKd = 8.3 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 756 19 3 9 8.1 COc1ccc(CN(CCN(C)CCCCCCCCNC(=O)c2ccc(C(=O)O)c(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c2)c2ccccn2)cc1 10.1016/s0960-894x(03)00113-6
CHEMBL277850 98727 0 None - 0 Guinea pig 8.3 pKd = 8.3 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 756 19 3 9 8.1 COc1ccc(CN(CCN(C)CCCCCCCCNC(=O)c2ccc(C(=O)O)c(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c2)c2ccccn2)cc1 10.1016/s0960-894x(03)00113-6
4440380 4255 3 None - 1 Guinea pig 8.3 pKd = 8.3 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 278 5 0 3 2.5 Cc1ccc(C2SCC(=O)N2CCCN(C)C)cc1 10.1021/jm00093a025
CHEMBL100487 4255 3 None - 1 Guinea pig 8.3 pKd = 8.3 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 278 5 0 3 2.5 Cc1ccc(C2SCC(=O)N2CCCN(C)C)cc1 10.1021/jm00093a025
CHEMBL1202938 4255 3 None - 1 Guinea pig 8.3 pKd = 8.3 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 278 5 0 3 2.5 Cc1ccc(C2SCC(=O)N2CCCN(C)C)cc1 10.1021/jm00093a025
11791817 98303 0 None -1 2 Guinea pig 8.2 pKd = 8.2 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nM
ChEMBL 345 9 2 2 4.5 c1ccc(C(CCc2nc(CCNC3CC3)c[nH]2)c2ccccc2)cc1 10.1021/jm991056a
CHEMBL274831 98303 0 None -1 2 Guinea pig 8.2 pKd = 8.2 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nM
ChEMBL 345 9 2 2 4.5 c1ccc(C(CCc2nc(CCNC3CC3)c[nH]2)c2ccccc2)cc1 10.1021/jm991056a
10083274 11394 0 None - 0 Guinea pig 4.3 pKd = 4.3 Functional
Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum
ChEMBL 246 6 2 3 2.5 CC(O)c1ccc(OCCCc2c[nH]cn2)cc1 10.1021/jm000971p
CHEMBL112676 11394 0 None - 0 Guinea pig 4.3 pKd = 4.3 Functional
Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum
ChEMBL 246 6 2 3 2.5 CC(O)c1ccc(OCCCc2c[nH]cn2)cc1 10.1021/jm000971p
CHEMBL1180069 11394 0 None - 0 Guinea pig 4.3 pKd = 4.3 Functional
Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum
ChEMBL 246 6 2 3 2.5 CC(O)c1ccc(OCCCc2c[nH]cn2)cc1 10.1021/jm000971p
14660365 199987 0 None - 0 Guinea pig 6.3 pKd = 6.3 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 396 9 4 3 3.7 N=C(NCCCc1c[nH]cn1)NCCC(c1ccccn1)c1ccccc1Cl 10.1021/jm00128a045
CHEMBL59521 199987 0 None - 0 Guinea pig 6.3 pKd = 6.3 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 396 9 4 3 3.7 N=C(NCCCc1c[nH]cn1)NCCC(c1ccccn1)c1ccccc1Cl 10.1021/jm00128a045
42625303 180766 0 None - 6 Guinea pig 5.3 pKd = 5.3 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions
ChEMBL 223 5 3 2 0.2 CCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL475621 180766 0 None - 6 Guinea pig 5.3 pKd = 5.3 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions
ChEMBL 223 5 3 2 0.2 CCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
25149431 185437 0 None - 0 Guinea pig 5.3 pKd = 5.3 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 277 5 4 3 1.6 N=C(NCCCc1c[nH]cn1)NC(=O)C1CCCCC1 10.1021/jm800841w
CHEMBL486153 185437 0 None - 0 Guinea pig 5.3 pKd = 5.3 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 277 5 4 3 1.6 N=C(NCCCc1c[nH]cn1)NC(=O)C1CCCCC1 10.1021/jm800841w
14660361 201502 0 None - 0 Guinea pig 6.3 pKd = 6.3 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 430 9 4 3 4.1 N=C(NCCCc1c[nH]cn1)NCCC(c1cccc(C(F)(F)F)c1)c1ccccn1 10.1021/jm00128a045
CHEMBL60515 201502 0 None - 0 Guinea pig 6.3 pKd = 6.3 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 430 9 4 3 4.1 N=C(NCCCc1c[nH]cn1)NCCC(c1cccc(C(F)(F)F)c1)c1ccccn1 10.1021/jm00128a045
25149811 185962 0 None - 0 Guinea pig 6.3 pKd = 6.3 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 327 9 4 3 2.4 N=C(NCCCc1c[nH]cn1)NC(=O)CCCCc1ccccc1 10.1021/jm800841w
CHEMBL486963 185962 0 None - 0 Guinea pig 6.3 pKd = 6.3 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 327 9 4 3 2.4 N=C(NCCCc1c[nH]cn1)NC(=O)CCCCc1ccccc1 10.1021/jm800841w
25149425 188206 0 None - 0 Guinea pig 6.2 pKd = 6.2 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 285 6 4 3 1.2 N=C(NCCCc1c[nH]cn1)NC(=O)Cc1ccccc1 10.1021/jm800841w
CHEMBL499092 188206 0 None - 0 Guinea pig 6.2 pKd = 6.2 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 285 6 4 3 1.2 N=C(NCCCc1c[nH]cn1)NC(=O)Cc1ccccc1 10.1021/jm800841w
10410901 119747 0 None -23 2 Rat 8.2 pKd = 8.2 Functional
Apparent pA2 value of compound at 50 nM concentration of mepyramine in rat aortaApparent pA2 value of compound at 50 nM concentration of mepyramine in rat aorta
ChEMBL 438 13 2 3 5.7 c1ccc(C(CCc2nc(CCNCCCCc3ccccn3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
CHEMBL347796 119747 0 None -23 2 Rat 8.2 pKd = 8.2 Functional
Apparent pA2 value of compound at 50 nM concentration of mepyramine in rat aortaApparent pA2 value of compound at 50 nM concentration of mepyramine in rat aorta
ChEMBL 438 13 2 3 5.7 c1ccc(C(CCc2nc(CCNCCCCc3ccccn3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
23582308 145864 0 None - 0 Human 8.2 pKd = 8.2 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 634 14 1 6 6.9 O=C(O)CCc1ccc2cc(Cc3ccccc3)cc(N3CCN(CCc4ccc(OCCCN5CCCCCC5)cc4)CC3)c2n1 10.1016/j.bmcl.2016.11.022
CHEMBL3917428 145864 0 None - 0 Human 8.2 pKd = 8.2 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 634 14 1 6 6.9 O=C(O)CCc1ccc2cc(Cc3ccccc3)cc(N3CCN(CCc4ccc(OCCCN5CCCCCC5)cc4)CC3)c2n1 10.1016/j.bmcl.2016.11.022
153224 202827 27 None - 0 Guinea pig 8.2 pKd = 8.2 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 271 7 1 4 2.3 CNCCN(Cc1ccc(OC)cc1)c1ccccn1 10.1016/s0960-894x(03)00113-6
CHEMBL624 202827 27 None - 0 Guinea pig 8.2 pKd = 8.2 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 271 7 1 4 2.3 CNCCN(Cc1ccc(OC)cc1)c1ccccn1 10.1016/s0960-894x(03)00113-6
25149433 185976 3 None - 0 Guinea pig 5.2 pKd = 5.2 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 305 7 4 3 2.3 N=C(NCCCc1c[nH]cn1)NC(=O)CCC1CCCCC1 10.1021/jm800841w
CHEMBL486974 185976 3 None - 0 Guinea pig 5.2 pKd = 5.2 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 305 7 4 3 2.3 N=C(NCCCc1c[nH]cn1)NC(=O)CCC1CCCCC1 10.1021/jm800841w
13676693 103001 0 None - 0 Guinea pig 7.2 pKd = 7.2 Functional
Compound was tested for H1-antihistamine activity in guinea pig ileum.Compound was tested for H1-antihistamine activity in guinea pig ileum.
ChEMBL 463 8 1 9 3.3 COc1ccc(CN2CCN(CCCOc3ccc4c(O)c5nnnc-5oc4c3C)CC2)cc1 10.1021/jm00161a022
CHEMBL306807 103001 0 None - 0 Guinea pig 7.2 pKd = 7.2 Functional
Compound was tested for H1-antihistamine activity in guinea pig ileum.Compound was tested for H1-antihistamine activity in guinea pig ileum.
ChEMBL 463 8 1 9 3.3 COc1ccc(CN2CCN(CCCOc3ccc4c(O)c5nnnc-5oc4c3C)CC2)cc1 10.1021/jm00161a022
2860026 108376 7 None - 1 Guinea pig 6.2 pKd = 6.2 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 298 5 0 3 2.9 CN(C)CCCN1C(=O)CSC1c1cccc(Cl)c1 10.1021/jm00093a025
CHEMBL319829 108376 7 None - 1 Guinea pig 6.2 pKd = 6.2 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 298 5 0 3 2.9 CN(C)CCCN1C(=O)CSC1c1cccc(Cl)c1 10.1021/jm00093a025
2861042 111583 8 None - 0 Guinea pig 5.2 pKd = 5.2 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 309 6 0 5 2.1 CN(C)CCCN1C(=O)CSC1c1ccc([N+](=O)[O-])cc1 10.1021/jm00093a025
CHEMBL1202943 111583 8 None - 0 Guinea pig 5.2 pKd = 5.2 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 309 6 0 5 2.1 CN(C)CCCN1C(=O)CSC1c1ccc([N+](=O)[O-])cc1 10.1021/jm00093a025
CHEMBL328201 111583 8 None - 0 Guinea pig 5.2 pKd = 5.2 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 309 6 0 5 2.1 CN(C)CCCN1C(=O)CSC1c1ccc([N+](=O)[O-])cc1 10.1021/jm00093a025
11356502 11338 0 None - 0 Guinea pig 4.2 pKd = 4.2 Functional
Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum
ChEMBL 222 6 1 2 3.3 c1nc(COCCCC2CCCCC2)c[nH]1 10.1021/jm031065q
CHEMBL1179596 11338 0 None - 0 Guinea pig 4.2 pKd = 4.2 Functional
Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum
ChEMBL 222 6 1 2 3.3 c1nc(COCCCC2CCCCC2)c[nH]1 10.1021/jm031065q
CHEMBL88362 11338 0 None - 0 Guinea pig 4.2 pKd = 4.2 Functional
Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum
ChEMBL 222 6 1 2 3.3 c1nc(COCCCC2CCCCC2)c[nH]1 10.1021/jm031065q
14660412 202206 0 None - 0 Guinea pig 6.2 pKd = 6.2 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pigAntagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig
ChEMBL 378 9 4 4 2.6 N/C(=N\CCC(c1ccc(O)cc1)c1ccccn1)NCCCc1c[nH]cn1 10.1021/jm00128a045
CHEMBL60972 202206 0 None - 0 Guinea pig 6.2 pKd = 6.2 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pigAntagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig
ChEMBL 378 9 4 4 2.6 N/C(=N\CCC(c1ccc(O)cc1)c1ccccn1)NCCCc1c[nH]cn1 10.1021/jm00128a045
44457674 84311 0 None - 0 Guinea pig 7.2 pKd = 7.2 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 672 13 3 9 5.7 COc1ccc(CN(CCN(C)CCNC(=O)c2ccc(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c(C(=O)O)c2)c2ccccn2)cc1 10.1016/s0960-894x(03)00113-6
CHEMBL22152 84311 0 None - 0 Guinea pig 7.2 pKd = 7.2 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 672 13 3 9 5.7 COc1ccc(CN(CCN(C)CCNC(=O)c2ccc(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c(C(=O)O)c2)c2ccccn2)cc1 10.1016/s0960-894x(03)00113-6
57391869 63120 0 None - 1 Guinea pig 4.2 pKd = 4.2 Functional
Antagonist activity at histamine H1 receptor in guinea-pig ileumAntagonist activity at histamine H1 receptor in guinea-pig ileum
ChEMBL 223 6 2 3 1.6 CC=CCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1774589 63120 0 None - 1 Guinea pig 4.2 pKd = 4.2 Functional
Antagonist activity at histamine H1 receptor in guinea-pig ileumAntagonist activity at histamine H1 receptor in guinea-pig ileum
ChEMBL 223 6 2 3 1.6 CC=CCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1789349 63120 0 None - 1 Guinea pig 4.2 pKd = 4.2 Functional
Antagonist activity at histamine H1 receptor in guinea-pig ileumAntagonist activity at histamine H1 receptor in guinea-pig ileum
ChEMBL 223 6 2 3 1.6 CC=CCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
57400700 67878 0 None - 0 Guinea pig 8.1 pKd = 8.1 Functional
Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins
ChEMBL 470 8 1 6 3.4 COc1ccc(CN(CCN2CCN(C(=O)c3nc4ccccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
CHEMBL1910380 67878 0 None - 0 Guinea pig 8.1 pKd = 8.1 Functional
Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins
ChEMBL 470 8 1 6 3.4 COc1ccc(CN(CCN2CCN(C(=O)c3nc4ccccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
57397301 67880 0 None - 0 Guinea pig 8.1 pKd = 8.1 Functional
Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins
ChEMBL 560 11 1 6 4.6 COc1ccc(CN(CCN(C)CCN2CCN(C(=O)c3cc4cc(Cl)ccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
CHEMBL1910382 67880 0 None - 0 Guinea pig 8.1 pKd = 8.1 Functional
Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins
ChEMBL 560 11 1 6 4.6 COc1ccc(CN(CCN(C)CCN2CCN(C(=O)c3cc4cc(Cl)ccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
145961372 161607 0 None - 1 Guinea pig 6.2 pKd = 6.2 Functional
Antagonist potency at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions at 0.3 to 3 uM after 15 minsAntagonist potency at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions at 0.3 to 3 uM after 15 mins
ChEMBL 311 7 0 2 5.3 c1ccc2c(OCCCCCN3CCCCCC3)cccc2c1 10.1016/j.bmc.2018.04.023
CHEMBL4129589 161607 0 None - 1 Guinea pig 6.2 pKd = 6.2 Functional
Antagonist potency at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions at 0.3 to 3 uM after 15 minsAntagonist potency at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions at 0.3 to 3 uM after 15 mins
ChEMBL 311 7 0 2 5.3 c1ccc2c(OCCCCCN3CCCCCC3)cccc2c1 10.1016/j.bmc.2018.04.023
2200 20203 61 None - 12 Guinea pig 7.1 pKd = 7.1 Functional
Antagonist potency at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions after 15 minsAntagonist potency at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions after 15 mins
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1016/j.bmc.2018.04.023
CHEMBL1256819 20203 61 None - 12 Guinea pig 7.1 pKd = 7.1 Functional
Antagonist potency at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions after 15 minsAntagonist potency at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions after 15 mins
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1016/j.bmc.2018.04.023
CHEMBL1305 20203 61 None - 12 Guinea pig 7.1 pKd = 7.1 Functional
Antagonist potency at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions after 15 minsAntagonist potency at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions after 15 mins
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1016/j.bmc.2018.04.023
42625224 180764 0 None - 1 Guinea pig 6.1 pKd = 6.1 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions
ChEMBL 395 9 5 3 1.5 N/C(=N\C(=O)CCCNC(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL475620 180764 0 None - 1 Guinea pig 6.1 pKd = 6.1 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions
ChEMBL 395 9 5 3 1.5 N/C(=N\C(=O)CCCNC(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1 10.1021/jm9000693
25149521 179052 0 None - 2 Guinea pig 6.1 pKd = 6.1 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 375 8 4 3 3.2 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccc1 10.1021/jm800841w
CHEMBL471413 179052 0 None - 2 Guinea pig 6.1 pKd = 6.1 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 375 8 4 3 3.2 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccc1 10.1021/jm800841w
25149515 185830 0 None - 0 Guinea pig 6.1 pKd = 6.1 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 319 8 4 3 2.7 N=C(NCCCc1c[nH]cn1)NC(=O)CCCC1CCCCC1 10.1021/jm800841w
CHEMBL486746 185830 0 None - 0 Guinea pig 6.1 pKd = 6.1 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 319 8 4 3 2.7 N=C(NCCCc1c[nH]cn1)NC(=O)CCCC1CCCCC1 10.1021/jm800841w
1219 737 0 None - 0 Guinea pig 7.1 pKd = 7.1 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 396 9 3 3 3.5 NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)Cl 10.1021/jm00128a045
14660352 737 0 None - 0 Guinea pig 7.1 pKd = 7.1 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 396 9 3 3 3.5 NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)Cl 10.1021/jm00128a045
CHEMBL304239 737 0 None - 0 Guinea pig 7.1 pKd = 7.1 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 396 9 3 3 3.5 NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)Cl 10.1021/jm00128a045
42625304 179100 0 None - 4 Guinea pig 5.1 pKd = 5.1 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions
ChEMBL 237 5 3 2 0.4 CC(C)C(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL471724 179100 0 None - 4 Guinea pig 5.1 pKd = 5.1 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions
ChEMBL 237 5 3 2 0.4 CC(C)C(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
10094258 199070 0 None - 0 Guinea pig 7.1 pKd = 7.1 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 430 9 4 3 4.4 N=C(NCCCc1c[nH]cn1)NCCC(c1ccc(Cl)c(Cl)c1)c1ccccn1 10.1021/jm00128a045
CHEMBL58740 199070 0 None - 0 Guinea pig 7.1 pKd = 7.1 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 430 9 4 3 4.4 N=C(NCCCc1c[nH]cn1)NCCC(c1ccc(Cl)c(Cl)c1)c1ccccn1 10.1021/jm00128a045
13676703 204605 0 None - 0 Guinea pig 7.1 pKd = 7.1 Functional
Compound was tested for H1-antihistamine activity in guinea pig ileum.Compound was tested for H1-antihistamine activity in guinea pig ileum.
ChEMBL 469 10 1 8 4.2 Cc1c(OCCCN(C)CCN(C)Cc2ccc(Cl)cc2)ccc2c(O)c3nnnc-3oc12 10.1021/jm00161a022
CHEMBL73265 204605 0 None - 0 Guinea pig 7.1 pKd = 7.1 Functional
Compound was tested for H1-antihistamine activity in guinea pig ileum.Compound was tested for H1-antihistamine activity in guinea pig ileum.
ChEMBL 469 10 1 8 4.2 Cc1c(OCCCN(C)CCN(C)Cc2ccc(Cl)cc2)ccc2c(O)c3nnnc-3oc12 10.1021/jm00161a022
2872050 208226 3 None - 1 Guinea pig 7.1 pKd = 7.1 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 282 5 0 3 2.4 CN(C)CCCN1C(=O)CSC1c1ccc(F)cc1 10.1021/jm00093a025
CHEMBL1202939 208226 3 None - 1 Guinea pig 7.1 pKd = 7.1 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 282 5 0 3 2.4 CN(C)CCCN1C(=O)CSC1c1ccc(F)cc1 10.1021/jm00093a025
CHEMBL98605 208226 3 None - 1 Guinea pig 7.1 pKd = 7.1 Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
ChEMBL 282 5 0 3 2.4 CN(C)CCCN1C(=O)CSC1c1ccc(F)cc1 10.1021/jm00093a025
11345716 11344 0 None - 0 Guinea pig 5.1 pKd = 5.1 Functional
Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum
ChEMBL 250 8 1 2 3.7 c1nc(CCCOCCCC2CCCCC2)c[nH]1 10.1021/jm031065q
CHEMBL1179627 11344 0 None - 0 Guinea pig 5.1 pKd = 5.1 Functional
Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum
ChEMBL 250 8 1 2 3.7 c1nc(CCCOCCCC2CCCCC2)c[nH]1 10.1021/jm031065q
CHEMBL89999 11344 0 None - 0 Guinea pig 5.1 pKd = 5.1 Functional
Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum
ChEMBL 250 8 1 2 3.7 c1nc(CCCOCCCC2CCCCC2)c[nH]1 10.1021/jm031065q
11413171 12110 0 None - 1 Guinea pig 5.1 pKd = 5.1 Functional
Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum
ChEMBL 210 9 1 2 2.9 CCCCCCOCCCc1c[nH]cn1 10.1021/jm031065q
CHEMBL1184057 12110 0 None - 1 Guinea pig 5.1 pKd = 5.1 Functional
Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum
ChEMBL 210 9 1 2 2.9 CCCCCCOCCCc1c[nH]cn1 10.1021/jm031065q
CHEMBL330688 12110 0 None - 1 Guinea pig 5.1 pKd = 5.1 Functional
Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum
ChEMBL 210 9 1 2 2.9 CCCCCCOCCCc1c[nH]cn1 10.1021/jm031065q
54584376 63168 0 None - 1 Guinea pig 4.1 pKd = 4.1 Functional
Antagonist activity at histamine H1 receptor in guinea-pig ileumAntagonist activity at histamine H1 receptor in guinea-pig ileum
ChEMBL 237 7 2 3 2.0 CC/C=C\CNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1774592 63168 0 None - 1 Guinea pig 4.1 pKd = 4.1 Functional
Antagonist activity at histamine H1 receptor in guinea-pig ileumAntagonist activity at histamine H1 receptor in guinea-pig ileum
ChEMBL 237 7 2 3 2.0 CC/C=C\CNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1789809 63168 0 None - 1 Guinea pig 4.1 pKd = 4.1 Functional
Antagonist activity at histamine H1 receptor in guinea-pig ileumAntagonist activity at histamine H1 receptor in guinea-pig ileum
ChEMBL 237 7 2 3 2.0 CC/C=C\CNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
10635074 11404 0 None - 0 Guinea pig 4.1 pKd = 4.1 Functional
Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum
ChEMBL 260 6 3 4 1.0 NNC(=O)c1ccc(OCCCc2c[nH]cn2)cc1 10.1021/jm000971p
CHEMBL113404 11404 0 None - 0 Guinea pig 4.1 pKd = 4.1 Functional
Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum
ChEMBL 260 6 3 4 1.0 NNC(=O)c1ccc(OCCCc2c[nH]cn2)cc1 10.1021/jm000971p
CHEMBL1180094 11404 0 None - 0 Guinea pig 4.1 pKd = 4.1 Functional
Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum
ChEMBL 260 6 3 4 1.0 NNC(=O)c1ccc(OCCCc2c[nH]cn2)cc1 10.1021/jm000971p
57390225 67882 0 None - 0 Guinea pig 8.1 pKd = 8.1 Functional
Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins
ChEMBL 469 9 2 5 4.1 COc1ccc(CN(CCN[C@H]2CCN(C(=O)c3cc4ccccc4[nH]3)C2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
CHEMBL1910384 67882 0 None - 0 Guinea pig 8.1 pKd = 8.1 Functional
Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins
ChEMBL 469 9 2 5 4.1 COc1ccc(CN(CCN[C@H]2CCN(C(=O)c3cc4ccccc4[nH]3)C2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
10246247 98293 0 None - 0 Guinea pig 6.1 pKd = 6.1 Functional
Relative potency was recorded in endothelium-denuded guinea pig(pre contracted with PGF-2 alpha); value ranges from 5.76 to 6.40Relative potency was recorded in endothelium-denuded guinea pig(pre contracted with PGF-2 alpha); value ranges from 5.76 to 6.40
ChEMBL 333 9 2 2 4.5 NCCc1c[nH]c(CCCCC(c2ccccc2)c2ccccc2)n1 10.1021/jm991056a
CHEMBL274767 98293 0 None - 0 Guinea pig 6.1 pKd = 6.1 Functional
Relative potency was recorded in endothelium-denuded guinea pig(pre contracted with PGF-2 alpha); value ranges from 5.76 to 6.40Relative potency was recorded in endothelium-denuded guinea pig(pre contracted with PGF-2 alpha); value ranges from 5.76 to 6.40
ChEMBL 333 9 2 2 4.5 NCCc1c[nH]c(CCCCC(c2ccccc2)c2ccccc2)n1 10.1021/jm991056a
3081063 201509 22 None - 0 Guinea pig 7.1 pKd = 7.1 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 398 9 4 3 3.4 N=C(NCCCc1c[nH]cn1)NCCC(c1ccc(F)c(F)c1)c1ccccn1 10.1021/jm00128a045
CHEMBL60519 201509 22 None - 0 Guinea pig 7.1 pKd = 7.1 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 398 9 4 3 3.4 N=C(NCCCc1c[nH]cn1)NCCC(c1ccc(F)c(F)c1)c1ccccn1 10.1021/jm00128a045
14660416 200729 1 None - 0 Guinea pig 6.1 pKd = 6.1 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 377 9 4 4 2.4 N/C(=N\CCC(c1cccc(N)c1)c1ccccn1)NCCCc1c[nH]cn1 10.1021/jm00128a045
CHEMBL60006 200729 1 None - 0 Guinea pig 6.1 pKd = 6.1 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 377 9 4 4 2.4 N/C(=N\CCC(c1cccc(N)c1)c1ccccn1)NCCCc1c[nH]cn1 10.1021/jm00128a045
42625384 169773 0 None - 4 Guinea pig 5.1 pKd = 5.1 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions
ChEMBL 209 4 3 2 -0.2 CC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL443896 169773 0 None - 4 Guinea pig 5.1 pKd = 5.1 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions
ChEMBL 209 4 3 2 -0.2 CC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
14660359 199129 0 None - 0 Guinea pig 7.1 pKd = 7.1 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 396 9 4 3 3.7 N=C(NCCCc1c[nH]cn1)NCCC(c1cccc(Cl)c1)c1ccccn1 10.1021/jm00128a045
CHEMBL58922 199129 0 None - 0 Guinea pig 7.1 pKd = 7.1 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 396 9 4 3 3.7 N=C(NCCCc1c[nH]cn1)NCCC(c1cccc(Cl)c1)c1ccccn1 10.1021/jm00128a045
10447834 1933 4 None -2 3 Rat 8.0 pKd = 8.0 Functional
Compound was evaluated for mepyramine antagonism effects in rat aorta (relaxation) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in rat aorta (relaxation) at a mepyramine concentration of 100 nM
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
4026 1933 4 None -2 3 Rat 8.0 pKd = 8.0 Functional
Compound was evaluated for mepyramine antagonism effects in rat aorta (relaxation) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in rat aorta (relaxation) at a mepyramine concentration of 100 nM
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
CHEMBL275507 1933 4 None -2 3 Rat 8.0 pKd = 8.0 Functional
Compound was evaluated for mepyramine antagonism effects in rat aorta (relaxation) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in rat aorta (relaxation) at a mepyramine concentration of 100 nM
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
10447834 1933 4 None -2 3 Rat 8.0 pKd = 8.0 Functional
Maximum response (E max) against Histamine H1 receptor in rat aortaMaximum response (E max) against Histamine H1 receptor in rat aorta
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm0309147
4026 1933 4 None -2 3 Rat 8.0 pKd = 8.0 Functional
Maximum response (E max) against Histamine H1 receptor in rat aortaMaximum response (E max) against Histamine H1 receptor in rat aorta
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm0309147
CHEMBL275507 1933 4 None -2 3 Rat 8.0 pKd = 8.0 Functional
Maximum response (E max) against Histamine H1 receptor in rat aortaMaximum response (E max) against Histamine H1 receptor in rat aorta
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm0309147
11741669 96753 0 None -39 2 Rat 8.0 pKd = 8.0 Functional
Apparent pA2 value of compound at 50 nM concentration of mepyramine in rat aortaApparent pA2 value of compound at 50 nM concentration of mepyramine in rat aorta
ChEMBL 399 11 3 3 4.3 c1ccc(C(CCc2nc(CCNCCc3cnc[nH]3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
CHEMBL264491 96753 0 None -39 2 Rat 8.0 pKd = 8.0 Functional
Apparent pA2 value of compound at 50 nM concentration of mepyramine in rat aortaApparent pA2 value of compound at 50 nM concentration of mepyramine in rat aorta
ChEMBL 399 11 3 3 4.3 c1ccc(C(CCc2nc(CCNCCc3cnc[nH]3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
10403687 2511 3 None -1 2 Rat 8.0 pKd = 8.0 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nM
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
1205 2511 3 None -1 2 Rat 8.0 pKd = 8.0 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nM
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
CHEMBL275035 2511 3 None -1 2 Rat 8.0 pKd = 8.0 Functional
Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nM
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
10403687 2511 3 None -1 2 Rat 8.0 pKd = 8.0 Functional
Maximum response (E max) against Histamine H1 receptor in guinea pig ileumMaximum response (E max) against Histamine H1 receptor in guinea pig ileum
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm0309147
1205 2511 3 None -1 2 Rat 8.0 pKd = 8.0 Functional
Maximum response (E max) against Histamine H1 receptor in guinea pig ileumMaximum response (E max) against Histamine H1 receptor in guinea pig ileum
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm0309147
CHEMBL275035 2511 3 None -1 2 Rat 8.0 pKd = 8.0 Functional
Maximum response (E max) against Histamine H1 receptor in guinea pig ileumMaximum response (E max) against Histamine H1 receptor in guinea pig ileum
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm0309147
44274460 82411 0 None - 0 Guinea pig 8.0 pKd = 8.0 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 398 15 1 5 4.3 COc1ccc(CN(CCN(C)CCCCCCCCN)c2ccccn2)cc1 10.1016/s0960-894x(03)00113-6
CHEMBL21735 82411 0 None - 0 Guinea pig 8.0 pKd = 8.0 Functional
Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand
ChEMBL 398 15 1 5 4.3 COc1ccc(CN(CCN(C)CCCCCCCCN)c2ccccn2)cc1 10.1016/s0960-894x(03)00113-6
11726167 199657 0 None - 0 Guinea pig 7.0 pKd = 7.0 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 362 9 4 3 3.1 N=C(NCCCc1c[nH]cn1)NCCC(c1ccccc1)c1ccccn1 10.1021/jm00128a045
CHEMBL59295 199657 0 None - 0 Guinea pig 7.0 pKd = 7.0 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 362 9 4 3 3.1 N=C(NCCCc1c[nH]cn1)NCCC(c1ccccc1)c1ccccn1 10.1021/jm00128a045
14660386 202780 0 None - 0 Guinea pig 7.0 pKd = 7.0 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 395 9 4 2 4.3 N=C(NCCCc1c[nH]cn1)NCCC(c1ccccc1)c1ccc(Cl)cc1 10.1021/jm00128a045
CHEMBL62142 202780 0 None - 0 Guinea pig 7.0 pKd = 7.0 Functional
Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.
ChEMBL 395 9 4 2 4.3 N=C(NCCCc1c[nH]cn1)NCCC(c1ccccc1)c1ccc(Cl)cc1 10.1021/jm00128a045
1201 3964 1 None - 0 Guinea pig 5.0 pKd = 5.0 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 361 7 3 3 2.6 O=C(CC(c1ccccc1)c1ccccc1)NC(=NCCc1cnc[nH]1)N 10.1021/jm800841w
25150700 3964 1 None - 0 Guinea pig 5.0 pKd = 5.0 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 361 7 3 3 2.6 O=C(CC(c1ccccc1)c1ccccc1)NC(=NCCc1cnc[nH]1)N 10.1021/jm800841w
CHEMBL499301 3964 1 None - 0 Guinea pig 5.0 pKd = 5.0 Functional
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 361 7 3 3 2.6 O=C(CC(c1ccccc1)c1ccccc1)NC(=NCCc1cnc[nH]1)N 10.1021/jm800841w
52937526 61302 0 None - 0 Human 10.0 pKi = 10 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 363 5 0 5 3.1 COc1ccc(Cc2nn(C[C@H]3CCCN3C)c(=O)c3ccccc23)cc1 10.1021/jm1013874
CHEMBL1767137 61302 0 None - 0 Human 10.0 pKi = 10 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 363 5 0 5 3.1 COc1ccc(Cc2nn(C[C@H]3CCCN3C)c(=O)c3ccccc23)cc1 10.1021/jm1013874
1530 2182 50 None 3 25 Human 9.8 pKi = 9.8 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1021/jm100856p
3827 2182 50 None 3 25 Human 9.8 pKi = 9.8 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1021/jm100856p
7206 2182 50 None 3 25 Human 9.8 pKi = 9.8 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1021/jm100856p
CHEMBL534 2182 50 None 3 25 Human 9.8 pKi = 9.8 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1021/jm100856p
DB00920 2182 50 None 3 25 Human 9.8 pKi = 9.8 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1021/jm100856p
15254720 61301 0 None - 0 Human 9.8 pKi = 9.8 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 367 4 0 4 3.7 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/jm1013874
CHEMBL1767136 61301 0 None - 0 Human 9.8 pKi = 9.8 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 367 4 0 4 3.7 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/jm1013874
52937527 61303 0 None - 0 Human 9.8 pKi = 9.8 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 349 4 1 5 2.8 CN1CCC[C@@H]1Cn1nc(Cc2ccc(O)cc2)c2ccccc2c1=O 10.1021/jm1013874
CHEMBL1767138 61303 0 None - 0 Human 9.8 pKi = 9.8 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 349 4 1 5 2.8 CN1CCC[C@@H]1Cn1nc(Cc2ccc(O)cc2)c2ccccc2c1=O 10.1021/jm1013874
15254720 61301 0 None - 0 Human 9.8 pKi = 9.8 Functional
Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 367 4 0 4 3.7 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1016/j.bmc.2012.08.032
CHEMBL1767136 61301 0 None - 0 Human 9.8 pKi = 9.8 Functional
Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 367 4 0 4 3.7 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1016/j.bmc.2012.08.032
52937631 61307 0 None - 0 Human 9.7 pKi = 9.7 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 347 4 0 4 3.4 Cc1ccc(Cc2nn(C[C@H]3CCCN3C)c(=O)c3ccccc23)cc1 10.1021/jm1013874
CHEMBL1767141 61307 0 None - 0 Human 9.7 pKi = 9.7 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 347 4 0 4 3.4 Cc1ccc(Cc2nn(C[C@H]3CCCN3C)c(=O)c3ccccc23)cc1 10.1021/jm1013874
71452871 80468 0 None - 0 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 412 7 0 6 3.1 COCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cnccc2c1=O 10.1016/j.bmc.2012.08.032
CHEMBL2146801 80468 0 None - 0 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 412 7 0 6 3.1 COCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cnccc2c1=O 10.1016/j.bmc.2012.08.032
203096 61299 3 None - 0 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 341 5 0 4 3.2 CN(C)CCn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/jm1013874
CHEMBL1767134 61299 3 None - 0 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 341 5 0 4 3.2 CN(C)CCn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/jm1013874
52937732 61314 0 None - 0 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 369 4 0 4 3.4 CN1CCC[C@@H]1Cn1nc(Cc2ccc(F)c(F)c2)c2ccccc2c1=O 10.1021/jm1013874
CHEMBL1767149 61314 0 None - 0 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 369 4 0 4 3.4 CN1CCC[C@@H]1Cn1nc(Cc2ccc(F)c(F)c2)c2ccccc2c1=O 10.1021/jm1013874
71458204 80476 0 None - 0 Human 9.5 pKi = 9.5 Functional
Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 368 4 0 5 3.1 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ncccc2c1=O 10.1016/j.bmc.2012.08.032
CHEMBL2146809 80476 0 None - 0 Human 9.5 pKi = 9.5 Functional
Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 368 4 0 5 3.1 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ncccc2c1=O 10.1016/j.bmc.2012.08.032
52937630 61306 0 None - 0 Human 9.5 pKi = 9.5 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 351 4 0 4 3.2 CN1CCC[C@@H]1Cn1nc(Cc2ccc(F)cc2)c2ccccc2c1=O 10.1021/jm1013874
CHEMBL1767140 61306 0 None - 0 Human 9.5 pKi = 9.5 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 351 4 0 4 3.2 CN1CCC[C@@H]1Cn1nc(Cc2ccc(F)cc2)c2ccccc2c1=O 10.1021/jm1013874
52937830 61319 0 None - 0 Human 9.5 pKi = 9.5 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 367 4 0 4 3.7 CN1CCC[C@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/jm1013874
CHEMBL1767154 61319 0 None - 0 Human 9.5 pKi = 9.5 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 367 4 0 4 3.7 CN1CCC[C@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/jm1013874
71458203 80472 0 None - 0 Human 9.5 pKi = 9.5 Functional
Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 368 4 0 5 3.1 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cnccc2c1=O 10.1016/j.bmc.2012.08.032
CHEMBL2146805 80472 0 None - 0 Human 9.5 pKi = 9.5 Functional
Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 368 4 0 5 3.1 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cnccc2c1=O 10.1016/j.bmc.2012.08.032
71452872 80434 0 None - 0 Human 9.5 pKi = 9.5 Functional
Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 368 4 0 5 3.1 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cccnc2c1=O 10.1016/j.bmc.2012.08.032
CHEMBL2146484 80434 0 None - 0 Human 9.5 pKi = 9.5 Functional
Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 368 4 0 5 3.1 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cccnc2c1=O 10.1016/j.bmc.2012.08.032
71461782 80473 0 None - 0 Human 9.4 pKi = 9.4 Functional
Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 410 7 0 5 4.3 CCCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cnccc2c1=O 10.1016/j.bmc.2012.08.032
CHEMBL2146806 80473 0 None - 0 Human 9.4 pKi = 9.4 Functional
Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 410 7 0 5 4.3 CCCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cnccc2c1=O 10.1016/j.bmc.2012.08.032
46861860 7491 1 None - 0 Human 9.3 pKi = 9.3 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 323 3 0 3 4.0 CN1CCCC(c2nc3ccccc3n2Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2011.10.115
CHEMBL1087089 7491 1 None - 0 Human 9.3 pKi = 9.3 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 323 3 0 3 4.0 CN1CCCC(c2nc3ccccc3n2Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2011.10.115
52937728 61310 0 None - 0 Human 9.3 pKi = 9.3 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 351 4 0 4 3.2 CN1CCC[C@@H]1Cn1nc(Cc2cccc(F)c2)c2ccccc2c1=O 10.1021/jm1013874
CHEMBL1767145 61310 0 None - 0 Human 9.3 pKi = 9.3 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 351 4 0 4 3.2 CN1CCC[C@@H]1Cn1nc(Cc2cccc(F)c2)c2ccccc2c1=O 10.1021/jm1013874
71456359 80470 0 None - 0 Human 9.3 pKi = 9.3 Functional
Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 411 7 0 5 3.8 COCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1016/j.bmc.2012.08.032
CHEMBL2146803 80470 0 None - 0 Human 9.3 pKi = 9.3 Functional
Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 411 7 0 5 3.8 COCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1016/j.bmc.2012.08.032
71458205 80478 0 None - 0 Human 9.3 pKi = 9.3 Functional
Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 412 7 0 6 3.1 COCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ncccc2c1=O 10.1016/j.bmc.2012.08.032
CHEMBL2146811 80478 0 None - 0 Human 9.3 pKi = 9.3 Functional
Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 412 7 0 6 3.1 COCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ncccc2c1=O 10.1016/j.bmc.2012.08.032
71451044 80474 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 410 7 0 5 4.3 CCCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cccnc2c1=O 10.1016/j.bmc.2012.08.032
CHEMBL2146807 80474 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 410 7 0 5 4.3 CCCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cccnc2c1=O 10.1016/j.bmc.2012.08.032
71454639 80477 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 410 7 0 5 4.3 CCCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ncccc2c1=O 10.1016/j.bmc.2012.08.032
CHEMBL2146810 80477 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 410 7 0 5 4.3 CCCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ncccc2c1=O 10.1016/j.bmc.2012.08.032
49864841 15731 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay
ChEMBL 266 1 1 4 1.6 C1=C(N2CCNCC2)c2nccn2Cc2ccccc21 10.1016/j.bmcl.2010.07.029
CHEMBL1222552 15731 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay
ChEMBL 266 1 1 4 1.6 C1=C(N2CCNCC2)c2nccn2Cc2ccccc21 10.1016/j.bmcl.2010.07.029
71449250 80471 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 368 4 0 5 3.1 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccncc2c1=O 10.1016/j.bmc.2012.08.032
CHEMBL2146804 80471 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 368 4 0 5 3.1 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccncc2c1=O 10.1016/j.bmc.2012.08.032
52937731 61313 0 None - 0 Human 9.1 pKi = 9.1 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 347 4 0 4 3.4 Cc1cccc(Cc2nn(C[C@H]3CCCN3C)c(=O)c3ccccc23)c1 10.1021/jm1013874
CHEMBL1767148 61313 0 None - 0 Human 9.1 pKi = 9.1 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 347 4 0 4 3.4 Cc1cccc(Cc2nn(C[C@H]3CCCN3C)c(=O)c3ccccc23)c1 10.1021/jm1013874
46861858 8562 0 None - 0 Human 9.1 pKi = 9.1 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 335 5 0 4 3.9 CN1CCCC(c2nc3ccccc3n2CCOc2ccccc2)C1 10.1016/j.bmcl.2011.10.115
CHEMBL1094510 8562 0 None - 0 Human 9.1 pKi = 9.1 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 335 5 0 4 3.9 CN1CCCC(c2nc3ccccc3n2CCOc2ccccc2)C1 10.1016/j.bmcl.2011.10.115
57402315 69712 0 None - 0 Human 9.1 pKi = 9.1 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 311 3 1 4 2.9 Fc1ccc(Cn2c([C@H]3CNCCO3)nc3ccccc32)cc1 10.1016/j.bmcl.2011.10.115
CHEMBL1935442 69712 0 None - 0 Human 9.1 pKi = 9.1 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 311 3 1 4 2.9 Fc1ccc(Cn2c([C@H]3CNCCO3)nc3ccccc32)cc1 10.1016/j.bmcl.2011.10.115
46888857 8712 0 None - 0 Human 9.1 pKi = 9.1 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 323 3 0 3 4.0 CN1CCC[C@@H](c2nc3ccccc3n2Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2011.10.115
CHEMBL1095819 8712 0 None - 0 Human 9.1 pKi = 9.1 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 323 3 0 3 4.0 CN1CCC[C@@H](c2nc3ccccc3n2Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2011.10.115
71461781 80469 0 None - 0 Human 9.0 pKi = 9.0 Functional
Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 409 7 0 4 4.9 CCCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1016/j.bmc.2012.08.032
CHEMBL2146802 80469 0 None - 0 Human 9.0 pKi = 9.0 Functional
Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 409 7 0 4 4.9 CCCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1016/j.bmc.2012.08.032
57398830 69706 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 353 5 1 4 3.4 OCCN1CCCC(c2nc3ccccc3n2Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2011.10.115
CHEMBL1935436 69706 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 353 5 1 4 3.4 OCCN1CCCC(c2nc3ccccc3n2Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2011.10.115
57400501 69708 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 321 5 1 4 3.6 c1ccc(OCCn2c(C3CCCNC3)nc3ccccc32)cc1 10.1016/j.bmcl.2011.10.115
CHEMBL1935438 69708 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 321 5 1 4 3.6 c1ccc(OCCn2c(C3CCCNC3)nc3ccccc32)cc1 10.1016/j.bmcl.2011.10.115
57395287 69711 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 307 3 1 4 3.1 Cc1ccc(Cn2c([C@H]3CNCCO3)nc3ccccc32)cc1 10.1016/j.bmcl.2011.10.115
CHEMBL1935441 69711 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 307 3 1 4 3.1 Cc1ccc(Cn2c([C@H]3CNCCO3)nc3ccccc32)cc1 10.1016/j.bmcl.2011.10.115
71456360 80475 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 412 7 0 6 3.1 COCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cccnc2c1=O 10.1016/j.bmc.2012.08.032
CHEMBL2146808 80475 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 412 7 0 6 3.1 COCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cccnc2c1=O 10.1016/j.bmc.2012.08.032
52937222 61321 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 367 3 0 4 3.9 CN1CCC(n2nc(Cc3ccc(Cl)cc3)c3ccccc3c2=O)CC1 10.1021/jm1013874
CHEMBL1767156 61321 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 367 3 0 4 3.9 CN1CCC(n2nc(Cc3ccc(Cl)cc3)c3ccccc3c2=O)CC1 10.1021/jm1013874
57404030 69707 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 309 3 1 3 3.7 Fc1ccc(Cn2c([C@@H]3CCCNC3)nc3ccccc32)cc1 10.1016/j.bmcl.2011.10.115
CHEMBL1935437 69707 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 309 3 1 3 3.7 Fc1ccc(Cn2c([C@@H]3CCCNC3)nc3ccccc32)cc1 10.1016/j.bmcl.2011.10.115
2267 559 71 None 32 14 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmc.2012.08.032
271 559 71 None 32 14 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmc.2012.08.032
7121 559 71 None 32 14 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmc.2012.08.032
CHEMBL639 559 71 None 32 14 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmc.2012.08.032
DB00972 559 71 None 32 14 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmc.2012.08.032
2267 559 71 None 32 14 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmcl.2016.11.022
271 559 71 None 32 14 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmcl.2016.11.022
7121 559 71 None 32 14 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmcl.2016.11.022
CHEMBL639 559 71 None 32 14 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmcl.2016.11.022
DB00972 559 71 None 32 14 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1016/j.bmcl.2016.11.022
2267 559 71 None 32 14 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1021/jm1013874
271 559 71 None 32 14 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1021/jm1013874
7121 559 71 None 32 14 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1021/jm1013874
CHEMBL639 559 71 None 32 14 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1021/jm1013874
DB00972 559 71 None 32 14 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1021/jm1013874
71456361 80479 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 369 4 0 6 2.5 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2nccnc2c1=O 10.1016/j.bmc.2012.08.032
CHEMBL2146812 80479 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 369 4 0 6 2.5 CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2nccnc2c1=O 10.1016/j.bmc.2012.08.032
57400503 69714 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 323 3 1 4 3.8 Cc1ccc(Cn2c(C3CNCCS3)nc3ccccc32)cc1 10.1016/j.bmcl.2011.10.115
CHEMBL1935444 69714 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 323 3 1 4 3.8 Cc1ccc(Cn2c(C3CNCCS3)nc3ccccc32)cc1 10.1016/j.bmcl.2011.10.115
57397056 69716 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 327 3 1 4 3.6 Fc1ccc(Cn2c([C@H]3CNCCS3)nc3ccccc32)cc1 10.1016/j.bmcl.2011.10.115
CHEMBL1935446 69716 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 327 3 1 4 3.6 Fc1ccc(Cn2c([C@H]3CNCCS3)nc3ccccc32)cc1 10.1016/j.bmcl.2011.10.115
57400505 69717 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 339 4 1 5 3.5 COc1ccc(Cn2c([C@H]3CNCCS3)nc3ccccc32)cc1 10.1016/j.bmcl.2011.10.115
CHEMBL1935447 69717 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 339 4 1 5 3.5 COc1ccc(Cn2c([C@H]3CNCCS3)nc3ccccc32)cc1 10.1016/j.bmcl.2011.10.115
57400503 69714 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 323 3 1 4 3.8 Cc1ccc(Cn2c(C3CNCCS3)nc3ccccc32)cc1 10.1016/j.bmcl.2011.10.115
CHEMBL1935444 69714 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 323 3 1 4 3.8 Cc1ccc(Cn2c(C3CNCCS3)nc3ccccc32)cc1 10.1016/j.bmcl.2011.10.115
52937729 61311 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 367 4 0 4 3.7 CN1CCC[C@@H]1Cn1nc(Cc2cccc(Cl)c2)c2ccccc2c1=O 10.1021/jm1013874
CHEMBL1767146 61311 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 367 4 0 4 3.7 CN1CCC[C@@H]1Cn1nc(Cc2cccc(Cl)c2)c2ccccc2c1=O 10.1021/jm1013874
52937829 61318 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 313 6 0 4 3.2 CCCCCc1nn(C[C@H]2CCCN2C)c(=O)c2ccccc12 10.1021/jm1013874
CHEMBL1767153 61318 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 313 6 0 4 3.2 CCCCCc1nn(C[C@H]2CCCN2C)c(=O)c2ccccc12 10.1021/jm1013874
57400502 69713 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 321 3 1 4 3.4 Cc1ccc(Cn2c(C3CNCCO3)nc3ccccc32)cc1C 10.1016/j.bmcl.2011.10.115
CHEMBL1935443 69713 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 321 3 1 4 3.4 Cc1ccc(Cn2c(C3CNCCO3)nc3ccccc32)cc1C 10.1016/j.bmcl.2011.10.115
52937730 61312 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 363 5 0 5 3.1 COc1cccc(Cc2nn(C[C@H]3CCCN3C)c(=O)c3ccccc23)c1 10.1021/jm1013874
CHEMBL1767147 61312 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 363 5 0 5 3.1 COc1cccc(Cc2nn(C[C@H]3CCCN3C)c(=O)c3ccccc23)c1 10.1021/jm1013874
52945978 18796 0 None - 0 Human 8.0 pKi = 8 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 335 4 2 2 3.7 O=C(O)CCNC1CC[C@]2(Cc3ccccc3Cc3ccccc32)C1 10.1021/jm100856p
CHEMBL1278114 18796 0 None - 0 Human 8.0 pKi = 8 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 335 4 2 2 3.7 O=C(O)CCNC1CC[C@]2(Cc3ccccc3Cc3ccccc32)C1 10.1021/jm100856p
17747460 61329 12 None - 2 Human 8.0 pKi = 8 Functional
Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 640 14 0 6 7.8 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1016/j.bmc.2012.08.032
CHEMBL1767164 61329 12 None - 2 Human 8.0 pKi = 8 Functional
Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 640 14 0 6 7.8 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1016/j.bmc.2012.08.032
17747460 61329 12 None - 2 Human 8.0 pKi = 8 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 640 14 0 6 7.8 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1016/j.bmcl.2016.11.022
CHEMBL1767164 61329 12 None - 2 Human 8.0 pKi = 8 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 640 14 0 6 7.8 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1016/j.bmcl.2016.11.022
52937018 61300 0 None - 0 Human 8.0 pKi = 8 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 355 6 0 4 3.6 CN(C)CCCn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/jm1013874
CHEMBL1767135 61300 0 None - 0 Human 8.0 pKi = 8 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 355 6 0 4 3.6 CN(C)CCCn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/jm1013874
17747460 61329 12 None - 2 Human 8.0 pKi = 8 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 640 14 0 6 7.8 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1021/jm1013874
CHEMBL1767164 61329 12 None - 2 Human 8.0 pKi = 8 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 640 14 0 6 7.8 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1021/jm1013874
49836636 18677 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 375 2 1 3 4.5 O=C(O)C1=CCCN(C2CCC3(Cc4ccccc4Oc4ccccc43)C2)C1 10.1021/jm100856p
CHEMBL1277125 18677 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 375 2 1 3 4.5 O=C(O)C1=CCCN(C2CCC3(Cc4ccccc4Oc4ccccc43)C2)C1 10.1021/jm100856p
49836522 18795 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 376 2 2 3 3.0 O=C(O)C1CN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)CCN1 10.1021/jm100856p
CHEMBL1278113 18795 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 376 2 2 3 3.0 O=C(O)C1CN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)CCN1 10.1021/jm100856p
11648990 95646 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 498 6 0 8 5.4 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6onc(C)c6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL257946 95646 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 498 6 0 8 5.4 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6onc(C)c6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
185 4006 60 None - 1 Human 6.0 pKi = 6 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O 10.1021/jm100856p
5311271 4006 60 None - 1 Human 6.0 pKi = 6 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O 10.1021/jm100856p
CHEMBL74355 4006 60 None - 1 Human 6.0 pKi = 6 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O 10.1021/jm100856p
DB16351 4006 60 None - 1 Human 6.0 pKi = 6 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O 10.1021/jm100856p
49836740 18704 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 425 2 1 4 4.9 O=C(O)C1CCN(C2CCC3(C2)C(=O)c2cc(Cl)ccc2Oc2ccccc23)CC1 10.1021/jm100856p
CHEMBL1277401 18704 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 425 2 1 4 4.9 O=C(O)C1CCN(C2CCC3(C2)C(=O)c2cc(Cl)ccc2Oc2ccccc23)CC1 10.1021/jm100856p
44454458 95125 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 618 6 0 8 7.1 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C(C)(C)C)oc6c(Br)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL255566 95125 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 618 6 0 8 7.1 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C(C)(C)C)oc6c(Br)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
44454382 95582 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 517 6 0 8 5.2 Cc1ccc2c(-c3nnc(SCCCN4CCc5nc6ccc(Cl)cn6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
CHEMBL257716 95582 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 517 6 0 8 5.2 Cc1ccc2c(-c3nnc(SCCCN4CCc5nc6ccc(Cl)cn6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
11642163 97505 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 522 6 0 9 5.3 Cc1nc(C)c(-c2nnc(SCCCN3CCc4ccc5oc(C(F)(F)F)nc5c4CC3)n2C)s1 10.1016/j.bmcl.2007.12.042
CHEMBL270376 97505 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 522 6 0 9 5.3 Cc1nc(C)c(-c2nnc(SCCCN3CCc4ccc5oc(C(F)(F)F)nc5c4CC3)n2C)s1 10.1016/j.bmcl.2007.12.042
11663526 97752 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 514 6 0 8 5.8 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C)sc6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL271632 97752 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 514 6 0 8 5.8 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C)sc6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
44454223 97974 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 542 6 0 8 4.7 CC(=O)N1CCOc2cc3c(cc21)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.066
CHEMBL272702 97974 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 542 6 0 8 4.7 CC(=O)N1CCOc2cc3c(cc21)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.066
11527195 98058 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 590 6 0 8 6.5 Cc1ccc2c(-c3nnc(SCCC(C)N4CCc5cc6nc(C)oc6c(Br)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL273165 98058 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 590 6 0 8 6.5 Cc1ccc2c(-c3nnc(SCCC(C)N4CCc5cc6nc(C)oc6c(Br)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
11721190 155274 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 578 7 0 10 5.8 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6oc(-c7cc(C)nn7C)nc6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
CHEMBL402853 155274 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 578 7 0 10 5.8 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6oc(-c7cc(C)nn7C)nc6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
134143913 150330 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 497 9 0 6 5.1 N#Cc1ccc(N2CCN(CCc3ccc(OCCCN4CCCCCC4)cc3)CC2)c2ncccc12 10.1016/j.bmcl.2016.11.022
CHEMBL3953018 150330 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 497 9 0 6 5.1 N#Cc1ccc(N2CCN(CCc3ccc(OCCCN4CCCCCC4)cc3)CC2)c2ncccc12 10.1016/j.bmcl.2016.11.022
57393573 69709 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 406 7 0 5 3.4 CN(C)C(=O)CN1CCCC(c2nc3ccccc3n2CCOc2ccccc2)C1 10.1016/j.bmcl.2011.10.115
CHEMBL1935439 69709 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 406 7 0 5 3.4 CN(C)C(=O)CN1CCCC(c2nc3ccccc3n2CCOc2ccccc2)C1 10.1016/j.bmcl.2011.10.115
49836525 18807 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 375 2 1 2 4.4 CC1(C(=O)O)CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
CHEMBL1278202 18807 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 375 2 1 2 4.4 CC1(C(=O)O)CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
57780020 143450 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 600 15 1 6 6.6 CCCCc1cc(N2CCN(CCc3ccc(OCCCN4CCCCCC4)cc3)CC2)c2nc(CCC(=O)O)ccc2c1 10.1016/j.bmcl.2016.11.022
CHEMBL3898341 143450 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 600 15 1 6 6.6 CCCCc1cc(N2CCN(CCc3ccc(OCCCN4CCCCCC4)cc3)CC2)c2nc(CCC(=O)O)ccc2c1 10.1016/j.bmcl.2016.11.022
57780017 148118 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 544 12 1 6 5.3 O=C(O)CCc1ccc2cccc(N3CCN(CCc4ccc(OCCCN5CCCCCC5)cc4)CC3)c2n1 10.1016/j.bmcl.2016.11.022
CHEMBL3935303 148118 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 544 12 1 6 5.3 O=C(O)CCc1ccc2cccc(N3CCN(CCc4ccc(OCCCN5CCCCCC5)cc4)CC3)c2n1 10.1016/j.bmcl.2016.11.022
49834051 15747 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay
ChEMBL 364 3 1 5 2.2 O=C(O)C1CC(N2CCN(C3=Cc4ccccc4Cn4ccnc43)CC2)C1 10.1016/j.bmcl.2010.07.029
CHEMBL1222626 15747 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay
ChEMBL 364 3 1 5 2.2 O=C(O)C1CC(N2CCN(C3=Cc4ccccc4Cn4ccnc43)CC2)C1 10.1016/j.bmcl.2010.07.029
24803639 61331 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 622 14 1 7 6.8 O=c1c2ccccc2c(Cc2ccc(O)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1021/jm1013874
CHEMBL1767166 61331 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 622 14 1 7 6.8 O=c1c2ccccc2c(Cc2ccc(O)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1021/jm1013874
24803483 61332 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 654 15 0 6 8.2 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1021/jm1013874
CHEMBL1767167 61332 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 654 15 0 6 8.2 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1021/jm1013874
49836738 18694 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 377 2 1 3 4.6 O=C(O)[C@@H]1CCCN(C2CCC3(Cc4ccccc4Oc4ccccc43)C2)C1 10.1021/jm100856p
CHEMBL1277311 18694 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 377 2 1 3 4.6 O=C(O)[C@@H]1CCCN(C2CCC3(Cc4ccccc4Oc4ccccc43)C2)C1 10.1021/jm100856p
11591601 155333 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 512 7 0 8 5.6 CCc1noc2cc3c(cc12)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.066
CHEMBL403181 155333 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 512 7 0 8 5.6 CCc1noc2cc3c(cc12)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.066
49833882 15760 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay
ChEMBL 392 3 1 5 3.0 O=C(O)C1CCC(N2CCN(C3=Cc4ccccc4Cn4ccnc43)CC2)CC1 10.1016/j.bmcl.2010.07.029
CHEMBL1222692 15760 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay
ChEMBL 392 3 1 5 3.0 O=C(O)C1CCC(N2CCN(C3=Cc4ccccc4Cn4ccnc43)CC2)CC1 10.1016/j.bmcl.2010.07.029
49833886 15778 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay
ChEMBL 396 5 1 6 2.5 COc1cnc2n1Cc1ccccc1C=C2N1CCN(CC(C)(C)C(=O)O)CC1 10.1016/j.bmcl.2010.07.029
CHEMBL1222764 15778 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay
ChEMBL 396 5 1 6 2.5 COc1cnc2n1Cc1ccccc1C=C2N1CCN(CC(C)(C)C(=O)O)CC1 10.1016/j.bmcl.2010.07.029
11657494 95509 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 644 7 0 8 7.2 Cc1ccc2c(-c3nnc(SCCCCN4CCc5cc6nc(C(F)(F)F)oc6c(Br)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL257369 95509 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 644 7 0 8 7.2 Cc1ccc2c(-c3nnc(SCCCCN4CCc5cc6nc(C(F)(F)F)oc6c(Br)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
11641641 97507 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 487 6 0 7 5.2 Cn1c(SCCCN2CCc3ccc4oc(C(F)(F)F)nc4c3CC2)nnc1-c1ccccc1 10.1016/j.bmcl.2007.12.042
CHEMBL270387 97507 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 487 6 0 7 5.2 Cn1c(SCCCN2CCc3ccc4oc(C(F)(F)F)nc4c3CC2)nnc1-c1ccccc1 10.1016/j.bmcl.2007.12.042
24749507 14008 4 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization
ChEMBL 421 7 0 4 3.4 O=C(c1ccccc1)N1CCN(c2ccc(OCCCN3CCCCC3)cc2)C(=O)C1 10.1021/jm0708228
CHEMBL1197067 14008 4 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization
ChEMBL 421 7 0 4 3.4 O=C(c1ccccc1)N1CCN(c2ccc(OCCCN3CCCCC3)cc2)C(=O)C1 10.1021/jm0708228
CHEMBL559206 14008 4 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization
ChEMBL 421 7 0 4 3.4 O=C(c1ccccc1)N1CCN(c2ccc(OCCCN3CCCCC3)cc2)C(=O)C1 10.1021/jm0708228
57397055 69705 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 390 5 0 5 4.6 Fc1ccc(Cn2c(C3CCCN(Cc4ncco4)C3)nc3ccccc32)cc1 10.1016/j.bmcl.2011.10.115
CHEMBL1935435 69705 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 390 5 0 5 4.6 Fc1ccc(Cn2c(C3CCCN(Cc4ncco4)C3)nc3ccccc32)cc1 10.1016/j.bmcl.2011.10.115
49836294 18779 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 387 2 0 3 4.4 COC(=O)C1=CCCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
CHEMBL1278020 18779 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 387 2 0 3 4.4 COC(=O)C1=CCCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
49836524 18806 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 361 2 1 2 4.0 O=C(O)C1CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
CHEMBL1278201 18806 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 361 2 1 2 4.0 O=C(O)C1CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
134136763 142848 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 500 11 0 5 6.0 c1cnc2c(N3CCN(CCCCc4ccc(OCCCN5CCCCCC5)cc4)CC3)cccc2c1 10.1016/j.bmcl.2016.11.022
CHEMBL3893197 142848 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 500 11 0 5 6.0 c1cnc2c(N3CCN(CCCCc4ccc(OCCCN5CCCCCC5)cc4)CC3)cccc2c1 10.1016/j.bmcl.2016.11.022
57780007 146991 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 572 13 1 6 5.8 CCc1cc(N2CCN(CCc3ccc(OCCCN4CCCCCC4)cc3)CC2)c2nc(CCC(=O)O)ccc2c1 10.1016/j.bmcl.2016.11.022
CHEMBL3926412 146991 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 572 13 1 6 5.8 CCc1cc(N2CCN(CCc3ccc(OCCCN4CCCCCC4)cc3)CC2)c2nc(CCC(=O)O)ccc2c1 10.1016/j.bmcl.2016.11.022
24803797 61080 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 626 11 0 6 7.6 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C1CCCN(CCc2ccc(OCCCN3CCCCCC3)cc2)CC1 10.1021/jm1013874
CHEMBL1765111 61080 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 626 11 0 6 7.6 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C1CCCN(CCc2ccc(OCCCN3CCCCCC3)cc2)CC1 10.1021/jm1013874
24803798 61325 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 640 12 0 6 7.9 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C1CCCN(CCCc2ccc(OCCCN3CCCCCC3)cc2)CC1 10.1021/jm1013874
CHEMBL1767160 61325 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 640 12 0 6 7.9 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C1CCCN(CCCc2ccc(OCCCN3CCCCCC3)cc2)CC1 10.1021/jm1013874
49836737 18685 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 395 2 1 3 4.7 O=C(O)C1(F)CCN(C2CCC3(Cc4ccccc4Oc4ccccc43)C2)CC1 10.1021/jm100856p
CHEMBL1277217 18685 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 395 2 1 3 4.7 O=C(O)C1(F)CCN(C2CCC3(Cc4ccccc4Oc4ccccc43)C2)CC1 10.1021/jm100856p
49836189 18780 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 373 2 1 2 4.3 O=C(O)C1=CCCN(C2CC[C@@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
CHEMBL1278021 18780 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 373 2 1 2 4.3 O=C(O)C1=CCCN(C2CC[C@@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
44454309 97639 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 514 6 1 8 4.3 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6c(cc5CC4)OCC(=O)N6)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL271066 97639 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 514 6 1 8 4.3 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6c(cc5CC4)OCC(=O)N6)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
11568714 95307 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 454 6 0 9 4.3 Cc1nc2cc3c(cc2s1)CCN(CCCSc1nnc(-c2ocnc2C)n1C)CC3 10.1016/j.bmcl.2007.12.066
CHEMBL256471 95307 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 454 6 0 9 4.3 Cc1nc2cc3c(cc2s1)CCN(CCCSc1nnc(-c2ocnc2C)n1C)CC3 10.1016/j.bmcl.2007.12.066
11606378 95315 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 548 7 0 8 6.2 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6nc(C(C)(F)F)oc6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
CHEMBL256488 95315 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 548 7 0 8 6.2 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6nc(C(C)(F)F)oc6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
11533473 97551 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 503 6 0 9 4.3 Cc1cnc(-c2nnc(SCCCN3CCc4ccc5oc(C(F)(F)F)nc5c4CC3)n2C)cn1 10.1016/j.bmcl.2007.12.042
CHEMBL270602 97551 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 503 6 0 9 4.3 Cc1cnc(-c2nnc(SCCCN3CCc4ccc5oc(C(F)(F)F)nc5c4CC3)n2C)cn1 10.1016/j.bmcl.2007.12.042
44454401 155140 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 554 6 0 8 6.7 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C(C)(C)C)oc6c(C)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL402087 155140 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 554 6 0 8 6.7 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C(C)(C)C)oc6c(C)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
11504077 168829 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 488 7 0 9 4.6 Cc1ncoc1-c1nnc(SCCCN2CCc3ccc4oc(C(C)(F)F)nc4c3CC2)n1C 10.1016/j.bmcl.2007.12.042
CHEMBL437792 168829 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 488 7 0 9 4.6 Cc1ncoc1-c1nnc(SCCCN2CCc3ccc4oc(C(C)(F)F)nc4c3CC2)n1C 10.1016/j.bmcl.2007.12.042
52937733 61315 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 393 6 0 6 3.1 COc1ccc(Cc2nn(C[C@H]3CCCN3C)c(=O)c3ccccc23)cc1OC 10.1021/jm1013874
CHEMBL1767150 61315 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 393 6 0 6 3.1 COc1ccc(Cc2nn(C[C@H]3CCCN3C)c(=O)c3ccccc23)cc1OC 10.1021/jm1013874
57391843 69704 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 436 5 0 5 3.3 O=C(CN1CCCC(c2nc3ccccc3n2Cc2ccc(F)cc2)C1)N1CCOCC1 10.1016/j.bmcl.2011.10.115
CHEMBL1935434 69704 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 436 5 0 5 3.3 O=C(CN1CCCC(c2nc3ccccc3n2Cc2ccc(F)cc2)C1)N1CCOCC1 10.1016/j.bmcl.2011.10.115
24804150 80480 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 641 14 0 7 7.2 O=c1c2ccncc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1016/j.bmc.2012.08.032
CHEMBL2146813 80480 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 641 14 0 7 7.2 O=c1c2ccncc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1016/j.bmc.2012.08.032
49836412 18724 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 375 2 1 2 4.4 O=C(O)[C@@H]1CCCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
CHEMBL1277584 18724 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 375 2 1 2 4.4 O=C(O)[C@@H]1CCCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
49836295 18766 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 373 2 1 2 4.3 O=C(O)C1=CCCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
CHEMBL1277935 18766 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 373 2 1 2 4.3 O=C(O)C1=CCCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
57780008 149726 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 472 9 0 5 5.2 c1cnc2c(N3CCN(CCc4ccc(OCCCN5CCCCCC5)cc4)CC3)cccc2c1 10.1016/j.bmcl.2016.11.022
CHEMBL3947980 149726 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 472 9 0 5 5.2 c1cnc2c(N3CCN(CCc4ccc(OCCCN5CCCCCC5)cc4)CC3)cccc2c1 10.1016/j.bmcl.2016.11.022
49864886 15745 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay
ChEMBL 366 4 1 5 2.6 CC1CN(C2=Cc3ccccc3Cn3ccnc32)CC(C)N1CCC(=O)O 10.1016/j.bmcl.2010.07.029
CHEMBL1222624 15745 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay
ChEMBL 366 4 1 5 2.6 CC1CN(C2=Cc3ccccc3Cn3ccnc32)CC(C)N1CCC(=O)O 10.1016/j.bmcl.2010.07.029
24803799 61326 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 654 13 0 6 8.3 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C1CCCN(CCCCc2ccc(OCCCN3CCCCCC3)cc2)CC1 10.1021/jm1013874
CHEMBL1767161 61326 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 654 13 0 6 8.3 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C1CCCN(CCCCc2ccc(OCCCN3CCCCCC3)cc2)CC1 10.1021/jm1013874
49836635 18667 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 359 2 1 2 4.0 O=C(O)C=C1CN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
CHEMBL1277035 18667 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 359 2 1 2 4.0 O=C(O)C=C1CN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
49836741 18713 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 425 2 1 4 4.8 O=C(O)C1CCN(C2CCC3(C2)C(=O)c2cc(F)ccc2Sc2ccccc23)CC1 10.1021/jm100856p
CHEMBL1277491 18713 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 425 2 1 4 4.8 O=C(O)C1CCN(C2CCC3(C2)C(=O)c2cc(F)ccc2Sc2ccccc23)CC1 10.1021/jm100856p
49836842 18714 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 425 2 1 4 4.9 O=C(O)[C@@H]1CCCN(C2CCC3(C2)C(=O)c2cc(Cl)ccc2Oc2ccccc23)C1 10.1021/jm100856p
CHEMBL1277492 18714 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 425 2 1 4 4.9 O=C(O)[C@@H]1CCCN(C2CCC3(C2)C(=O)c2cc(Cl)ccc2Oc2ccccc23)C1 10.1021/jm100856p
57780016 150297 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 542 11 1 6 5.3 O=C(O)/C=C/c1ccc2cccc(N3CCN(CCc4ccc(OCCCN5CCCCCC5)cc4)CC3)c2n1 10.1016/j.bmcl.2016.11.022
CHEMBL3952802 150297 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 542 11 1 6 5.3 O=C(O)/C=C/c1ccc2cccc(N3CCN(CCc4ccc(OCCCN5CCCCCC5)cc4)CC3)c2n1 10.1016/j.bmcl.2016.11.022
11585248 95314 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 604 8 0 8 6.8 CCc1nc2cc3c(c(Br)c2o1)CCN(CCCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.066
CHEMBL256482 95314 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 604 8 0 8 6.8 CCc1nc2cc3c(c(Br)c2o1)CCN(CCCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.066
11669953 95540 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 468 6 0 9 2.7 Cc1ncoc1-c1nnc(SCCCN2CCc3cc4c(cc3CC2)N(C)C(=O)CO4)n1C 10.1016/j.bmcl.2007.12.066
CHEMBL257534 95540 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 468 6 0 9 2.7 Cc1ncoc1-c1nnc(SCCCN2CCc3cc4c(cc3CC2)N(C)C(=O)CO4)n1C 10.1016/j.bmcl.2007.12.066
44454278 95541 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 454 6 1 9 2.7 Cc1ncoc1-c1nnc(SCCCN2CCc3cc4c(cc3CC2)OCC(=O)N4)n1C 10.1016/j.bmcl.2007.12.066
CHEMBL257536 95541 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 454 6 1 9 2.7 Cc1ncoc1-c1nnc(SCCCN2CCc3cc4c(cc3CC2)OCC(=O)N4)n1C 10.1016/j.bmcl.2007.12.066
11621352 97633 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 602 7 0 8 6.7 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6oc(C(F)(F)C(F)(F)F)nc6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
CHEMBL271034 97633 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 602 7 0 8 6.7 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6oc(C(F)(F)C(F)(F)F)nc6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
11677768 155574 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 502 6 0 8 4.9 Cc1ccc(-c2nnc(SCCCN3CCc4ccc5oc(C(F)(F)F)nc5c4CC3)n2C)cn1 10.1016/j.bmcl.2007.12.042
CHEMBL404404 155574 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 502 6 0 8 4.9 Cc1ccc(-c2nnc(SCCCN3CCc4ccc5oc(C(F)(F)F)nc5c4CC3)n2C)cn1 10.1016/j.bmcl.2007.12.042
44454353 156421 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 483 6 0 8 4.6 Cc1ccc2c(-c3nnc(SCCCN4CCc5nc6ccccn6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
CHEMBL406678 156421 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 483 6 0 8 4.6 Cc1ccc2c(-c3nnc(SCCCN4CCc5nc6ccccn6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
15986135 12329 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization
ChEMBL 457 7 0 4 3.7 O=C(c1ccc(F)cc1F)N1CCN(c2ccc(OCCCN3CCCCC3)cc2)C(=O)C1 10.1021/jm0708228
CHEMBL1185220 12329 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization
ChEMBL 457 7 0 4 3.7 O=C(c1ccc(F)cc1F)N1CCN(c2ccc(OCCCN3CCCCC3)cc2)C(=O)C1 10.1021/jm0708228
CHEMBL398812 12329 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization
ChEMBL 457 7 0 4 3.7 O=C(c1ccc(F)cc1F)N1CCN(c2ccc(OCCCN3CCCCC3)cc2)C(=O)C1 10.1021/jm0708228
15986915 12774 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization
ChEMBL 455 7 0 4 4.1 O=C(c1ccc(Cl)cc1)N1CCN(c2ccc(OCCCN3CCCCC3)cc2)C(=O)C1 10.1021/jm0708228
CHEMBL1187963 12774 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization
ChEMBL 455 7 0 4 4.1 O=C(c1ccc(Cl)cc1)N1CCN(c2ccc(OCCCN3CCCCC3)cc2)C(=O)C1 10.1021/jm0708228
CHEMBL534512 12774 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization
ChEMBL 455 7 0 4 4.1 O=C(c1ccc(Cl)cc1)N1CCN(c2ccc(OCCCN3CCCCC3)cc2)C(=O)C1 10.1021/jm0708228
24749508 12789 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization
ChEMBL 446 7 0 5 3.3 N#Cc1ccc(C(=O)N2CCN(c3ccc(OCCCN4CCCCC4)cc3)C(=O)C2)cc1 10.1021/jm0708228
CHEMBL1188060 12789 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization
ChEMBL 446 7 0 5 3.3 N#Cc1ccc(C(=O)N2CCN(c3ccc(OCCCN4CCCCC4)cc3)C(=O)C2)cc1 10.1021/jm0708228
CHEMBL534958 12789 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization
ChEMBL 446 7 0 5 3.3 N#Cc1ccc(C(=O)N2CCN(c3ccc(OCCCN4CCCCC4)cc3)C(=O)C2)cc1 10.1021/jm0708228
15986914 12858 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization
ChEMBL 435 7 0 4 3.7 Cc1ccc(C(=O)N2CCN(c3ccc(OCCCN4CCCCC4)cc3)C(=O)C2)cc1 10.1021/jm0708228
CHEMBL1188657 12858 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization
ChEMBL 435 7 0 4 3.7 Cc1ccc(C(=O)N2CCN(c3ccc(OCCCN4CCCCC4)cc3)C(=O)C2)cc1 10.1021/jm0708228
CHEMBL536991 12858 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization
ChEMBL 435 7 0 4 3.7 Cc1ccc(C(=O)N2CCN(c3ccc(OCCCN4CCCCC4)cc3)C(=O)C2)cc1 10.1021/jm0708228
15987452 91433 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization
ChEMBL 443 7 0 4 3.3 O=C(c1ccc(F)cc1F)N1CCN(c2ccc(OCCCN3CCCC3)cc2)C(=O)C1 10.1021/jm0708228
CHEMBL240352 91433 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization
ChEMBL 443 7 0 4 3.3 O=C(c1ccc(F)cc1F)N1CCN(c2ccc(OCCCN3CCCC3)cc2)C(=O)C1 10.1021/jm0708228
1524 2181 96 None -47 18 Human 8.7 pKi = 8.7 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm300338m
197 2181 96 None -47 18 Human 8.7 pKi = 8.7 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm300338m
3822 2181 96 None -47 18 Human 8.7 pKi = 8.7 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm300338m
88 2181 96 None -47 18 Human 8.7 pKi = 8.7 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm300338m
CHEMBL51 2181 96 None -47 18 Human 8.7 pKi = 8.7 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm300338m
DB12465 2181 96 None -47 18 Human 8.7 pKi = 8.7 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm300338m
45358442 61323 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 381 3 0 4 4.3 CN1CCCCC(n2nc(Cc3ccc(Cl)cc3)c3ccccc3c2=O)C1 10.1021/jm1013874
CHEMBL1767158 61323 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 381 3 0 4 4.3 CN1CCCCC(n2nc(Cc3ccc(Cl)cc3)c3ccccc3c2=O)C1 10.1021/jm1013874
53359025 62353 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 339 5 1 3 2.5 O=C(CCCN1C2C3C4CC5C6C4C2C6C1(O)C53)c1ccc(F)cc1 10.1016/j.bmcl.2011.04.098
CHEMBL1779058 62353 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 339 5 1 3 2.5 O=C(CCCN1C2C3C4CC5C6C4C2C6C1(O)C53)c1ccc(F)cc1 10.1016/j.bmcl.2011.04.098
57404031 69710 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 402 7 0 6 4.5 c1ccc(OCCn2c(C3CCCN(Cc4ncco4)C3)nc3ccccc32)cc1 10.1016/j.bmcl.2011.10.115
CHEMBL1935440 69710 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 402 7 0 6 4.5 c1ccc(OCCn2c(C3CCCN(Cc4ncco4)C3)nc3ccccc32)cc1 10.1016/j.bmcl.2011.10.115
49836411 18725 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 389 3 1 2 4.8 O=C(O)CC1CCN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)CC1 10.1021/jm100856p
CHEMBL1277585 18725 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 389 3 1 2 4.8 O=C(O)CC1CCN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)CC1 10.1021/jm100856p
49836295 18766 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 373 2 1 2 4.3 O=C(O)C1=CCCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
CHEMBL1277935 18766 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 373 2 1 2 4.3 O=C(O)C1=CCCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
49836187 18797 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 335 4 2 2 3.7 O=C(O)CCNC1CC[C@@]2(Cc3ccccc3Cc3ccccc32)C1 10.1021/jm100856p
CHEMBL1278115 18797 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 335 4 2 2 3.7 O=C(O)CCNC1CC[C@@]2(Cc3ccccc3Cc3ccccc32)C1 10.1021/jm100856p
23582308 145864 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 634 14 1 6 6.9 O=C(O)CCc1ccc2cc(Cc3ccccc3)cc(N3CCN(CCc4ccc(OCCCN5CCCCCC5)cc4)CC3)c2n1 10.1016/j.bmcl.2016.11.022
CHEMBL3917428 145864 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 634 14 1 6 6.9 O=C(O)CCc1ccc2cc(Cc3ccccc3)cc(N3CCN(CCc4ccc(OCCCN5CCCCCC5)cc4)CC3)c2n1 10.1016/j.bmcl.2016.11.022
46933089 15733 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay
ChEMBL 366 4 1 5 2.5 CC(C)(CN1CCN(C2=Cc3ccccc3Cn3ccnc32)CC1)C(=O)O 10.1016/j.bmcl.2010.07.029
CHEMBL1222554 15733 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay
ChEMBL 366 4 1 5 2.5 CC(C)(CN1CCN(C2=Cc3ccccc3Cn3ccnc32)CC1)C(=O)O 10.1016/j.bmcl.2010.07.029
49834051 15747 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay
ChEMBL 364 3 1 5 2.2 O=C(O)C1CC(N2CCN(C3=Cc4ccccc4Cn4ccnc43)CC2)C1 10.1016/j.bmcl.2010.07.029
CHEMBL1222626 15747 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay
ChEMBL 364 3 1 5 2.2 O=C(O)C1CC(N2CCN(C3=Cc4ccccc4Cn4ccnc43)CC2)C1 10.1016/j.bmcl.2010.07.029
24803482 61333 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 640 14 0 6 7.8 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1021/jm1013874
CHEMBL1767168 61333 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 640 14 0 6 7.8 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1021/jm1013874
11627879 95347 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 528 6 0 8 4.3 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6c(cc5CC4)N(C)C(=O)CO6)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL256652 95347 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 528 6 0 8 4.3 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6c(cc5CC4)N(C)C(=O)CO6)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
11577158 97807 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 514 6 0 8 5.8 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6nc(C)sc6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
CHEMBL271909 97807 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 514 6 0 8 5.8 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6nc(C)sc6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
134143679 145902 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 516 10 1 6 4.9 O=C(O)c1ccc2cccc(N3CCN(CCc4ccc(OCCCN5CCCCCC5)cc4)CC3)c2n1 10.1016/j.bmcl.2016.11.022
CHEMBL3917794 145902 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 516 10 1 6 4.9 O=C(O)c1ccc2cccc(N3CCN(CCc4ccc(OCCCN5CCCCCC5)cc4)CC3)c2n1 10.1016/j.bmcl.2016.11.022
44454120 95172 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 438 6 0 9 3.8 Cc1nc2cc3c(cc2o1)CCN(CCCSc1nnc(-c2ocnc2C)n1C)CC3 10.1016/j.bmcl.2007.12.066
CHEMBL255827 95172 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 438 6 0 9 3.8 Cc1nc2cc3c(cc2o1)CCN(CCCSc1nnc(-c2ocnc2C)n1C)CC3 10.1016/j.bmcl.2007.12.066
11548755 97655 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 580 7 0 8 6.8 Cc1ccc2c(-c3nnc(SCCCCN4CCc5cc6nc(C(F)(F)F)oc6c(C)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL271097 97655 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 580 7 0 8 6.8 Cc1ccc2c(-c3nnc(SCCCCN4CCc5cc6nc(C(F)(F)F)oc6c(C)c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
44454443 97763 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 449 6 0 9 3.6 Cc1cnc(-c2nnc(SCCCN3CCc4ccc5c(C)noc5c4CC3)n2C)cn1 10.1016/j.bmcl.2007.12.042
CHEMBL271702 97763 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 449 6 0 9 3.6 Cc1cnc(-c2nnc(SCCCN3CCc4ccc5c(C)noc5c4CC3)n2C)cn1 10.1016/j.bmcl.2007.12.042
11641596 97798 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 484 6 0 8 5.1 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6ncoc6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL271844 97798 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 484 6 0 8 5.1 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6ncoc6cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
15986645 12870 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization
ChEMBL 451 5 0 4 3.7 O=C(c1ccc(F)cc1)N1CCN(c2ccc(OC3CCN(C4CCC4)CC3)cc2)C(=O)C1 10.1021/jm0708228
CHEMBL1188742 12870 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization
ChEMBL 451 5 0 4 3.7 O=C(c1ccc(F)cc1)N1CCN(c2ccc(OC3CCN(C4CCC4)CC3)cc2)C(=O)C1 10.1021/jm0708228
CHEMBL537219 12870 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization
ChEMBL 451 5 0 4 3.7 O=C(c1ccc(F)cc1)N1CCN(c2ccc(OC3CCN(C4CCC4)CC3)cc2)C(=O)C1 10.1021/jm0708228
44250284 195222 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 436 6 0 5 4.6 CN(CC1CCOCC1)C1CCN(c2nc3ccccc3n2Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2011.10.115
CHEMBL550818 195222 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 436 6 0 5 4.6 CN(CC1CCOCC1)C1CCN(c2nc3ccccc3n2Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2011.10.115
52944115 18798 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 291 1 0 1 4.2 CN(C)C1CC[C@]2(Cc3ccccc3Cc3ccccc32)C1 10.1021/jm100856p
CHEMBL1278116 18798 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 291 1 0 1 4.2 CN(C)C1CC[C@]2(Cc3ccccc3Cc3ccccc32)C1 10.1021/jm100856p
49836526 18648 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 375 3 1 2 4.4 O=C(O)CC1CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
CHEMBL1276859 18648 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 375 3 1 2 4.4 O=C(O)CC1CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
49836528 18658 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 373 2 1 2 4.0 O=C(O)[C@]12C[C@H]1CN(C1CC[C@]3(Cc4ccccc4Cc4ccccc43)C1)C2 10.1021/jm100856p
CHEMBL1276947 18658 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 373 2 1 2 4.0 O=C(O)[C@]12C[C@H]1CN(C1CC[C@]3(Cc4ccccc4Cc4ccccc43)C1)C2 10.1021/jm100856p
49834052 15746 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay
ChEMBL 350 4 1 5 2.0 C=C(CN1CCN(C2=Cc3ccccc3Cn3ccnc32)CC1)C(=O)O 10.1016/j.bmcl.2010.07.029
CHEMBL1222625 15746 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay
ChEMBL 350 4 1 5 2.0 C=C(CN1CCN(C2=Cc3ccccc3Cn3ccnc32)CC1)C(=O)O 10.1016/j.bmcl.2010.07.029
52937828 61317 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 347 5 0 4 3.3 CN1CCC[C@@H]1Cn1nc(CCc2ccccc2)c2ccccc2c1=O 10.1021/jm1013874
CHEMBL1767152 61317 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 347 5 0 4 3.3 CN1CCC[C@@H]1Cn1nc(CCc2ccccc2)c2ccccc2c1=O 10.1021/jm1013874
49836634 18666 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 361 3 1 2 4.0 O=C(O)CC1CN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
CHEMBL1277034 18666 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 361 3 1 2 4.0 O=C(O)CC1CN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
44454434 97907 0 None - 0 Human 5.5 pKi = 5.5 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 512 6 0 7 4.5 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6c(cc5CC4)C(=O)N(C)C6)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
CHEMBL272480 97907 0 None - 0 Human 5.5 pKi = 5.5 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 512 6 0 7 4.5 Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6c(cc5CC4)C(=O)N(C)C6)n3C)cccc2n1 10.1016/j.bmcl.2007.12.066
57400502 69713 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 321 3 1 4 3.4 Cc1ccc(Cn2c(C3CNCCO3)nc3ccccc32)cc1C 10.1016/j.bmcl.2011.10.115
CHEMBL1935443 69713 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 321 3 1 4 3.4 Cc1ccc(Cn2c(C3CNCCO3)nc3ccccc32)cc1C 10.1016/j.bmcl.2011.10.115
49836527 18649 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 373 2 1 2 3.9 O=C(O)[C@@H]1[C@H]2CN(C3CCC4(Cc5ccccc5Cc5ccccc54)C3)C[C@H]21 10.1021/jm100856p
CHEMBL1276860 18649 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 373 2 1 2 3.9 O=C(O)[C@@H]1[C@H]2CN(C3CCC4(Cc5ccccc5Cc5ccccc54)C3)C[C@H]21 10.1021/jm100856p
49836410 18735 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 393 2 1 2 4.5 O=C(O)C1(F)CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)CC1 10.1021/jm100856p
CHEMBL1277678 18735 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 393 2 1 2 4.5 O=C(O)C1(F)CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)CC1 10.1021/jm100856p
49836298 18753 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 373 2 1 2 4.3 O=C(O)C1=CCN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)CC1 10.1021/jm100856p
CHEMBL1277854 18753 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 373 2 1 2 4.3 O=C(O)C1=CCN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)CC1 10.1021/jm100856p
49836296 18754 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 391 2 1 2 4.5 O=C(O)C1=CCCN(C2CCC3(Cc4cc(F)ccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
CHEMBL1277855 18754 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 391 2 1 2 4.5 O=C(O)C1=CCCN(C2CCC3(Cc4cc(F)ccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
57780018 144553 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 544 12 1 6 5.3 O=C(O)CCc1cnc2c(N3CCN(CCc4ccc(OCCCN5CCCCCC5)cc4)CC3)cccc2c1 10.1016/j.bmcl.2016.11.022
CHEMBL3907368 144553 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 544 12 1 6 5.3 O=C(O)CCc1cnc2c(N3CCN(CCc4ccc(OCCCN5CCCCCC5)cc4)CC3)cccc2c1 10.1016/j.bmcl.2016.11.022
49833883 15761 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay
ChEMBL 394 4 1 5 3.1 Cc1nc2n(c1C)Cc1ccccc1C=C2N1CCN(CC(C)(C)C(=O)O)CC1 10.1016/j.bmcl.2010.07.029
CHEMBL1222693 15761 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay
ChEMBL 394 4 1 5 3.1 Cc1nc2n(c1C)Cc1ccccc1C=C2N1CCN(CC(C)(C)C(=O)O)CC1 10.1016/j.bmcl.2010.07.029
46933090 15776 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay
ChEMBL 400 4 1 5 3.1 CC(C)(CN1CCN(C2=Cc3ccccc3Cn3c(Cl)cnc32)CC1)C(=O)O 10.1016/j.bmcl.2010.07.029
CHEMBL1222762 15776 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay
ChEMBL 400 4 1 5 3.1 CC(C)(CN1CCN(C2=Cc3ccccc3Cn3c(Cl)cnc32)CC1)C(=O)O 10.1016/j.bmcl.2010.07.029
49834053 15777 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay
ChEMBL 384 4 1 5 2.6 CC(C)(CN1CCN(C2=Cc3ccccc3Cn3cc(F)nc32)CC1)C(=O)O 10.1016/j.bmcl.2010.07.029
CHEMBL1222763 15777 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay
ChEMBL 384 4 1 5 2.6 CC(C)(CN1CCN(C2=Cc3ccccc3Cn3cc(F)nc32)CC1)C(=O)O 10.1016/j.bmcl.2010.07.029
24803316 61327 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 600 15 1 6 6.9 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1CCNCCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1021/jm1013874
CHEMBL1767162 61327 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 600 15 1 6 6.9 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1CCNCCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1021/jm1013874
24803480 61328 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 614 15 0 6 7.2 CN(CCCCc1ccc(OCCCN2CCCCCC2)cc1)CCn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/jm1013874
CHEMBL1767163 61328 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 614 15 0 6 7.2 CN(CCCCc1ccc(OCCCN2CCCCCC2)cc1)CCn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/jm1013874
11548239 95299 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 528 7 0 8 6.1 CCc1nc2ccc3c(c2s1)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.042
CHEMBL256442 95299 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 528 7 0 8 6.1 CCc1nc2ccc3c(c2s1)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.042
134150412 152102 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 516 10 1 6 4.9 O=C(O)c1cnc2c(N3CCN(CCc4ccc(OCCCN5CCCCCC5)cc4)CC3)cccc2c1 10.1016/j.bmcl.2016.11.022
CHEMBL3967709 152102 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 516 10 1 6 4.9 O=C(O)c1cnc2c(N3CCN(CCc4ccc(OCCCN5CCCCCC5)cc4)CC3)cccc2c1 10.1016/j.bmcl.2016.11.022
52937632 61308 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 389 4 0 4 4.4 CN1CCC[C@@H]1Cn1nc(Cc2ccc(C(C)(C)C)cc2)c2ccccc2c1=O 10.1021/jm1013874
CHEMBL1767142 61308 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 389 4 0 4 4.4 CN1CCC[C@@H]1Cn1nc(Cc2ccc(C(C)(C)C)cc2)c2ccccc2c1=O 10.1021/jm1013874
11497679 155564 0 None - 0 Human 5.4 pKi = 5.4 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 552 6 0 8 6.1 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6nc(C(F)(F)F)oc6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
CHEMBL404363 155564 0 None - 0 Human 5.4 pKi = 5.4 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 552 6 0 8 6.1 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6nc(C(F)(F)F)oc6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
57400504 69715 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 327 3 1 4 3.6 Fc1ccc(Cn2c(C3CNCCS3)nc3ccccc32)cc1 10.1016/j.bmcl.2011.10.115
CHEMBL1935445 69715 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 327 3 1 4 3.6 Fc1ccc(Cn2c(C3CNCCS3)nc3ccccc32)cc1 10.1016/j.bmcl.2011.10.115
57402314 69703 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 434 5 0 4 4.4 O=C(CN1CCCC(c2nc3ccccc3n2Cc2ccc(F)cc2)C1)N1CCCCC1 10.1016/j.bmcl.2011.10.115
CHEMBL1935433 69703 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 434 5 0 4 4.4 O=C(CN1CCCC(c2nc3ccccc3n2Cc2ccc(F)cc2)C1)N1CCCCC1 10.1016/j.bmcl.2011.10.115
57393573 69709 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 406 7 0 5 3.4 CN(C)C(=O)CN1CCCC(c2nc3ccccc3n2CCOc2ccccc2)C1 10.1016/j.bmcl.2011.10.115
CHEMBL1935439 69709 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 406 7 0 5 3.4 CN(C)C(=O)CN1CCCC(c2nc3ccccc3n2CCOc2ccccc2)C1 10.1016/j.bmcl.2011.10.115
16681693 82572 1 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at histamine H1 receptor expressed in human PC3 cells inhibition of histamine-induced calcium influx by cell based assayAntagonist activity at histamine H1 receptor expressed in human PC3 cells inhibition of histamine-induced calcium influx by cell based assay
ChEMBL 487 5 1 5 3.6 Cc1ccc(C(=O)N2CCC(=CC(=O)N[C@@H]3CCN(Cc4ccc5cc(F)ccc5c4)C3)CC2)nn1 10.1021/jm300682j
CHEMBL2178580 82572 1 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at histamine H1 receptor expressed in human PC3 cells inhibition of histamine-induced calcium influx by cell based assayAntagonist activity at histamine H1 receptor expressed in human PC3 cells inhibition of histamine-induced calcium influx by cell based assay
ChEMBL 487 5 1 5 3.6 Cc1ccc(C(=O)N2CCC(=CC(=O)N[C@@H]3CCN(Cc4ccc5cc(F)ccc5c4)C3)CC2)nn1 10.1021/jm300682j
52937629 61304 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 377 6 0 5 3.5 CCOc1ccc(Cc2nn(C[C@H]3CCCN3C)c(=O)c3ccccc23)cc1 10.1021/jm1013874
CHEMBL1767139 61304 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 377 6 0 5 3.5 CCOc1ccc(Cc2nn(C[C@H]3CCCN3C)c(=O)c3ccccc23)cc1 10.1021/jm1013874
57395286 69701 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 394 5 0 4 3.5 CN(C)C(=O)CN1CCCC(c2nc3ccccc3n2Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2011.10.115
CHEMBL1935431 69701 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 394 5 0 4 3.5 CN(C)C(=O)CN1CCCC(c2nc3ccccc3n2Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2011.10.115
49836637 18678 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 375 2 1 3 4.5 O=C(O)C1=CCN(C2CCC3(Cc4ccccc4Oc4ccccc43)C2)CC1 10.1021/jm100856p
CHEMBL1277126 18678 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 375 2 1 3 4.5 O=C(O)C1=CCN(C2CCC3(Cc4ccccc4Oc4ccccc43)C2)CC1 10.1021/jm100856p
25184832 18695 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 349 2 1 3 3.8 O=C(O)C1CN(C2CCC3(Cc4ccccc4Oc4ccccc43)C2)C1 10.1021/jm100856p
CHEMBL1277312 18695 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 349 2 1 3 3.8 O=C(O)C1CN(C2CCC3(Cc4ccccc4Oc4ccccc43)C2)C1 10.1021/jm100856p
49836409 18736 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 391 2 2 3 3.5 O=C(O)C1(O)CCN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)CC1 10.1021/jm100856p
CHEMBL1277679 18736 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 391 2 2 3 3.5 O=C(O)C1(O)CCN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)CC1 10.1021/jm100856p
49836300 18743 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 389 2 1 2 4.8 CC1(C(=O)O)CCN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)CC1 10.1021/jm100856p
CHEMBL1277769 18743 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 389 2 1 2 4.8 CC1(C(=O)O)CCN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)CC1 10.1021/jm100856p
49836299 18744 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 375 2 1 2 4.4 O=C(O)C1CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)CC1 10.1021/jm100856p
CHEMBL1277770 18744 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 375 2 1 2 4.4 O=C(O)C1CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)CC1 10.1021/jm100856p
49834050 15732 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay
ChEMBL 338 4 1 5 1.8 O=C(O)CCN1CCN(C2=Cc3ccccc3Cn3ccnc32)CC1 10.1016/j.bmcl.2010.07.029
CHEMBL1222553 15732 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay
ChEMBL 338 4 1 5 1.8 O=C(O)CCN1CCN(C2=Cc3ccccc3Cn3ccnc32)CC1 10.1016/j.bmcl.2010.07.029
49864885 15744 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay
ChEMBL 380 4 1 5 2.9 CC(C)(CN1CCCN(C2=Cc3ccccc3Cn3ccnc32)CC1)C(=O)O 10.1016/j.bmcl.2010.07.029
CHEMBL1222623 15744 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay
ChEMBL 380 4 1 5 2.9 CC(C)(CN1CCCN(C2=Cc3ccccc3Cn3ccnc32)CC1)C(=O)O 10.1016/j.bmcl.2010.07.029
49833884 15762 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay
ChEMBL 380 4 1 5 2.8 Cc1cn2c(n1)C(N1CCN(CC(C)(C)C(=O)O)CC1)=Cc1ccccc1C2 10.1016/j.bmcl.2010.07.029
CHEMBL1222694 15762 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay
ChEMBL 380 4 1 5 2.8 Cc1cn2c(n1)C(N1CCN(CC(C)(C)C(=O)O)CC1)=Cc1ccccc1C2 10.1016/j.bmcl.2010.07.029
24803641 61324 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 612 10 0 6 7.5 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C1CCCN(Cc2ccc(OCCCN3CCCCCC3)cc2)CC1 10.1021/jm1013874
CHEMBL1767159 61324 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 612 10 0 6 7.5 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C1CCCN(Cc2ccc(OCCCN3CCCCCC3)cc2)CC1 10.1021/jm1013874
11497680 97852 7 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 552 6 0 8 6.1 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6oc(C(F)(F)F)nc6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
CHEMBL272150 97852 7 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 552 6 0 8 6.1 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6oc(C(F)(F)F)nc6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
11519133 169423 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 512 7 0 8 5.6 CCc1nc2c3c(ccc2o1)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.042
CHEMBL442456 169423 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 512 7 0 8 5.6 CCc1nc2c3c(ccc2o1)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.042
57398829 69702 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 422 7 0 4 4.3 CCN(CC)C(=O)CN1CCCC(c2nc3ccccc3n2Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2011.10.115
CHEMBL1935432 69702 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 422 7 0 4 4.3 CCN(CC)C(=O)CN1CCCC(c2nc3ccccc3n2Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2011.10.115
49836633 18659 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 347 2 1 2 3.6 O=C(O)C1CN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
CHEMBL1276948 18659 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 347 2 1 2 3.6 O=C(O)C1CN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
52937119 61320 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 367 4 0 4 3.6 CN1CCC(Cn2nc(Cc3ccc(Cl)cc3)c3ccccc3c2=O)C1 10.1021/jm1013874
CHEMBL1767155 61320 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 367 4 0 4 3.6 CN1CCC(Cn2nc(Cc3ccc(Cl)cc3)c3ccccc3c2=O)C1 10.1021/jm1013874
45272895 195657 18 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 389 4 0 5 4.6 Cc1cnn(C2CCN(c3nc4ccccc4n3Cc3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2011.10.115
CHEMBL556450 195657 18 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 389 4 0 5 4.6 Cc1cnn(C2CCN(c3nc4ccccc4n3Cc3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2011.10.115
57400503 69714 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 323 3 1 4 3.8 Cc1ccc(Cn2c(C3CNCCS3)nc3ccccc32)cc1 10.1016/j.bmcl.2011.10.115
CHEMBL1935444 69714 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 323 3 1 4 3.8 Cc1ccc(Cn2c(C3CNCCS3)nc3ccccc32)cc1 10.1016/j.bmcl.2011.10.115
49836414 18794 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 377 2 1 3 3.4 O=C(O)C1CN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)CCO1 10.1021/jm100856p
CHEMBL1278112 18794 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 377 2 1 3 3.4 O=C(O)C1CN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)CCO1 10.1021/jm100856p
49833882 15760 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay
ChEMBL 392 3 1 5 3.0 O=C(O)C1CCC(N2CCN(C3=Cc4ccccc4Cn4ccnc43)CC2)CC1 10.1016/j.bmcl.2010.07.029
CHEMBL1222692 15760 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay
ChEMBL 392 3 1 5 3.0 O=C(O)C1CCC(N2CCN(C3=Cc4ccccc4Cn4ccnc43)CC2)CC1 10.1016/j.bmcl.2010.07.029
52937223 61322 23 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 381 5 0 4 4.1 CN1CCCC1CCn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/jm1013874
CHEMBL1767157 61322 23 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 381 5 0 4 4.1 CN1CCCC1CCn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/jm1013874
143 3515 51 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 438 5 1 4 4.8 N#Cc1ccc2c(c1)CCN(C2)CC[C@@H]1CC[C@H](CC1)NC(=O)c1ccnc2c1cccc2 10.1016/j.bmcl.2007.12.042
143 3515 51 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 438 5 1 4 4.8 N#Cc1ccc2c(c1)CCN(C2)CC[C@@H]1CC[C@H](CC1)NC(=O)c1ccnc2c1cccc2 10.1016/j.bmcl.2007.12.066
5311096 3515 51 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 438 5 1 4 4.8 N#Cc1ccc2c(c1)CCN(C2)CC[C@@H]1CC[C@H](CC1)NC(=O)c1ccnc2c1cccc2 10.1016/j.bmcl.2007.12.042
5311096 3515 51 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 438 5 1 4 4.8 N#Cc1ccc2c(c1)CCN(C2)CC[C@@H]1CC[C@H](CC1)NC(=O)c1ccnc2c1cccc2 10.1016/j.bmcl.2007.12.066
CHEMBL85606 3515 51 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 438 5 1 4 4.8 N#Cc1ccc2c(c1)CCN(C2)CC[C@@H]1CC[C@H](CC1)NC(=O)c1ccnc2c1cccc2 10.1016/j.bmcl.2007.12.042
CHEMBL85606 3515 51 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 438 5 1 4 4.8 N#Cc1ccc2c(c1)CCN(C2)CC[C@@H]1CC[C@H](CC1)NC(=O)c1ccnc2c1cccc2 10.1016/j.bmcl.2007.12.066
11569996 95312 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 525 7 0 8 5.4 CCc1nn(C)c2cc3c(cc12)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.066
CHEMBL256477 95312 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 525 7 0 8 5.4 CCc1nn(C)c2cc3c(cc12)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3 10.1016/j.bmcl.2007.12.066
11518972 155032 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 501 6 0 7 5.5 Cc1noc2cc3c(cc12)CCN(CCCSc1nnc(-c2ccc(C(F)(F)F)cc2)n1C)CC3 10.1016/j.bmcl.2007.12.066
CHEMBL401576 155032 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 501 6 0 7 5.5 Cc1noc2cc3c(cc12)CCN(CCCSc1nnc(-c2ccc(C(F)(F)F)cc2)n1C)CC3 10.1016/j.bmcl.2007.12.066
52937633 61309 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 391 5 0 6 2.9 COC(=O)c1ccc(Cc2nn(C[C@H]3CCCN3C)c(=O)c3ccccc23)cc1 10.1021/jm1013874
CHEMBL1767143 61309 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 391 5 0 6 2.9 COC(=O)c1ccc(Cc2nn(C[C@H]3CCCN3C)c(=O)c3ccccc23)cc1 10.1021/jm1013874
24803638 61330 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 636 15 0 7 7.1 COc1ccc(Cc2nn(C[C@H]3CCCN3CCCCc3ccc(OCCCN4CCCCCC4)cc3)c(=O)c3ccccc23)cc1 10.1021/jm1013874
CHEMBL1767165 61330 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 636 15 0 7 7.1 COc1ccc(Cc2nn(C[C@H]3CCCN3CCCCc3ccc(OCCCN4CCCCCC4)cc3)c(=O)c3ccccc23)cc1 10.1021/jm1013874
49836639 18684 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 377 2 1 3 4.6 O=C(O)C1CCN(C2CCC3(Cc4ccccc4Oc4ccccc43)C2)CC1 10.1021/jm100856p
CHEMBL1277216 18684 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 377 2 1 3 4.6 O=C(O)C1CCN(C2CCC3(Cc4ccccc4Oc4ccccc43)C2)CC1 10.1021/jm100856p
49836739 18703 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 387 2 1 3 4.0 O=C(O)C1=CCCN(C2CCC3(C2)C(=O)c2ccccc2Cc2ccccc23)C1 10.1021/jm100856p
CHEMBL1277400 18703 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 387 2 1 3 4.0 O=C(O)C1=CCCN(C2CCC3(C2)C(=O)c2ccccc2Cc2ccccc23)C1 10.1021/jm100856p
134139893 146413 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 486 10 0 5 5.6 c1cnc2c(N3CCN(CCCc4ccc(OCCCN5CCCCCC5)cc4)CC3)cccc2c1 10.1016/j.bmcl.2016.11.022
CHEMBL3921827 146413 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay
ChEMBL 486 10 0 5 5.6 c1cnc2c(N3CCN(CCCc4ccc(OCCCN5CCCCCC5)cc4)CC3)cccc2c1 10.1016/j.bmcl.2016.11.022
46933091 15763 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay
ChEMBL 400 4 1 5 3.1 CC(C)(CN1CCN(C2=Cc3ccccc3Cn3cc(Cl)nc32)CC1)C(=O)O 10.1016/j.bmcl.2010.07.029
CHEMBL1222695 15763 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay
ChEMBL 400 4 1 5 3.1 CC(C)(CN1CCN(C2=Cc3ccccc3Cn3cc(Cl)nc32)CC1)C(=O)O 10.1016/j.bmcl.2010.07.029
52937734 61316 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 339 4 0 4 3.6 CN1CCC[C@@H]1Cn1nc(CC2CCCCC2)c2ccccc2c1=O 10.1021/jm1013874
CHEMBL1767151 61316 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay
ChEMBL 339 4 0 4 3.6 CN1CCC[C@@H]1Cn1nc(CC2CCCCC2)c2ccccc2c1=O 10.1021/jm1013874
49836413 18777 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 393 2 1 2 4.5 O=C(O)C1(F)CCCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
CHEMBL1278019 18777 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 393 2 1 2 4.5 O=C(O)C1(F)CCCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
11584660 93268 8 None - 5 Human 6.1 pKi = 6.1 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 537 7 0 8 5.6 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc(-c6cc(C)nn6C)cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
CHEMBL244946 93268 8 None - 5 Human 6.1 pKi = 6.1 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 537 7 0 8 5.6 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc(-c6cc(C)nn6C)cc5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
44454190 98065 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 537 7 0 8 5.6 Cc1cc2c(-c3nnc(SCCCN4CCc5ccc(-c6cc(C)nn6C)cc5CC4)n3C)cccc2cn1 10.1016/j.bmcl.2007.12.066
CHEMBL273199 98065 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 537 7 0 8 5.6 Cc1cc2c(-c3nnc(SCCCN4CCc5ccc(-c6cc(C)nn6C)cc5CC4)n3C)cccc2cn1 10.1016/j.bmcl.2007.12.066
44454351 160607 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 551 6 0 8 5.6 Cc1ccc2c(-c3nnc(SCCCN4CCc5nc6cc(C(F)(F)F)ccn6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
CHEMBL411293 160607 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay
ChEMBL 551 6 0 8 5.6 Cc1ccc2c(-c3nnc(SCCCN4CCc5nc6cc(C(F)(F)F)ccn6c5CC4)n3C)cccc2n1 10.1016/j.bmcl.2007.12.042
57397055 69705 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 390 5 0 5 4.6 Fc1ccc(Cn2c(C3CCCN(Cc4ncco4)C3)nc3ccccc32)cc1 10.1016/j.bmcl.2011.10.115
CHEMBL1935435 69705 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 390 5 0 5 4.6 Fc1ccc(Cn2c(C3CCCN(Cc4ncco4)C3)nc3ccccc32)cc1 10.1016/j.bmcl.2011.10.115
57395286 69701 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 394 5 0 4 3.5 CN(C)C(=O)CN1CCCC(c2nc3ccccc3n2Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2011.10.115
CHEMBL1935431 69701 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 394 5 0 4 3.5 CN(C)C(=O)CN1CCCC(c2nc3ccccc3n2Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2011.10.115
57402230 69718 0 None - 0 Human 7.0 pKi = 7.0 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 339 4 1 5 3.5 COc1ccc(Cn2c(C3CNCCS3)nc3ccccc32)cc1 10.1016/j.bmcl.2011.10.115
CHEMBL1935448 69718 0 None - 0 Human 7.0 pKi = 7.0 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 339 4 1 5 3.5 COc1ccc(Cn2c(C3CNCCS3)nc3ccccc32)cc1 10.1016/j.bmcl.2011.10.115
57400504 69715 0 None - 0 Human 7.0 pKi = 7.0 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 327 3 1 4 3.6 Fc1ccc(Cn2c(C3CNCCS3)nc3ccccc32)cc1 10.1016/j.bmcl.2011.10.115
CHEMBL1935445 69715 0 None - 0 Human 7.0 pKi = 7.0 Functional
Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor
ChEMBL 327 3 1 4 3.6 Fc1ccc(Cn2c(C3CNCCS3)nc3ccccc32)cc1 10.1016/j.bmcl.2011.10.115
2247 505 81 None -4 42 Human 8.1 pA2 = 8.1 Functional
NoneNone
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
249 505 81 None -4 42 Human 8.1 pA2 = 8.1 Functional
NoneNone
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
2603 505 81 None -4 42 Human 8.1 pA2 = 8.1 Functional
NoneNone
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
CHEMBL296419 505 81 None -4 42 Human 8.1 pA2 = 8.1 Functional
NoneNone
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
DB00637 505 81 None -4 42 Human 8.1 pA2 = 8.1 Functional
NoneNone
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
1204 1932 119 None -9 10 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1932 119 None -9 10 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1932 119 None -9 10 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1932 119 None -9 10 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1932 119 None -9 10 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1932 119 None -9 10 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1204 1932 119 None -3 10 Guinea pig 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1932 119 None -3 10 Guinea pig 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1932 119 None -3 10 Guinea pig 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1932 119 None -3 10 Guinea pig 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1932 119 None -3 10 Guinea pig 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1932 119 None -3 10 Guinea pig 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1427 2013 54 None 5 30 Rat 8.0 pIC50 = 8.0 Functional
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
357 2013 54 None 5 30 Rat 8.0 pIC50 = 8.0 Functional
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
3696 2013 54 None 5 30 Rat 8.0 pIC50 = 8.0 Functional
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
CHEMBL11 2013 54 None 5 30 Rat 8.0 pIC50 = 8.0 Functional
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
DB00458 2013 54 None 5 30 Rat 8.0 pIC50 = 8.0 Functional
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
1971 2866 38 None 6 32 Rat 8.0 pIC50 = 8.0 Functional
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
2404 2866 38 None 6 32 Rat 8.0 pIC50 = 8.0 Functional
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
4543 2866 38 None 6 32 Rat 8.0 pIC50 = 8.0 Functional
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
CHEMBL445 2866 38 None 6 32 Rat 8.0 pIC50 = 8.0 Functional
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
DB00540 2866 38 None 6 32 Rat 8.0 pIC50 = 8.0 Functional
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
180 401 56 None 3 38 Rat 8.0 pIC50 = 8.0 Functional
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 401 56 None 3 38 Rat 8.0 pIC50 = 8.0 Functional
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 401 56 None 3 38 Rat 8.0 pIC50 = 8.0 Functional
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 401 56 None 3 38 Rat 8.0 pIC50 = 8.0 Functional
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 401 56 None 3 38 Rat 8.0 pIC50 = 8.0 Functional
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
40466858 16155 67 None -5 4 Guinea pig 8.3 pIC50 = 8.3 Functional
Inhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challengeInhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challenge
Drug Central 348 6 1 3 4.0 Cc1ccc(/C(=C\CN2CCCC2)c2cccc(/C=C/C(=O)O)n2)cc1 None
5284514 16155 67 None -5 4 Guinea pig 8.3 pIC50 = 8.3 Functional
Inhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challengeInhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challenge
Drug Central 348 6 1 3 4.0 Cc1ccc(/C(=C\CN2CCCC2)c2cccc(/C=C/C(=O)O)n2)cc1 None
CHEMBL1224 16155 67 None -5 4 Guinea pig 8.3 pIC50 = 8.3 Functional
Inhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challengeInhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challenge
Drug Central 348 6 1 3 4.0 Cc1ccc(/C(=C\CN2CCCC2)c2cccc(/C=C/C(=O)O)n2)cc1 None
1599 2341 50 None -3 21 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
3955 2341 50 None -3 21 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
7215 2341 50 None -3 21 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
CHEMBL841 2341 50 None -3 21 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
DB00836 2341 50 None -3 21 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
4223 3992 94 None -199 16 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
6918314 3992 94 None -199 16 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
7427 3992 94 None -199 16 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
CHEMBL439849 3992 94 None -199 16 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
DB06684 3992 94 None -199 16 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
40466858 16155 67 None 5 4 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 348 6 1 3 4.0 Cc1ccc(/C(=C\CN2CCCC2)c2cccc(/C=C/C(=O)O)n2)cc1 None
5284514 16155 67 None 5 4 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 348 6 1 3 4.0 Cc1ccc(/C(=C\CN2CCCC2)c2cccc(/C=C/C(=O)O)n2)cc1 None
CHEMBL1224 16155 67 None 5 4 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 348 6 1 3 4.0 Cc1ccc(/C(=C\CN2CCCC2)c2cccc(/C=C/C(=O)O)n2)cc1 None
2762 3863 31 None 100 9 Human 8.1 pIC50 = 8.1 Functional
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
Drug Central 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C None
5587 3863 31 None 100 9 Human 8.1 pIC50 = 8.1 Functional
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
Drug Central 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C None
7318 3863 31 None 100 9 Human 8.1 pIC50 = 8.1 Functional
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
Drug Central 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C None
CHEMBL1241 3863 31 None 100 9 Human 8.1 pIC50 = 8.1 Functional
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
Drug Central 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C None
DB00792 3863 31 None 100 9 Human 8.1 pIC50 = 8.1 Functional
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
Drug Central 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C None
1427 2013 54 None -19 30 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
357 2013 54 None -19 30 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
3696 2013 54 None -19 30 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
CHEMBL11 2013 54 None -19 30 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
DB00458 2013 54 None -19 30 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
2337 3256 77 None -1 29 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 77 None -1 29 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 77 None -1 29 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 77 None -1 29 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 77 None -1 29 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
10103 3416 72 None 28 2 Human 8.1 pIC50 = 8.1 Functional
Inhibitory concentration against histamine H1 receptorInhibitory concentration against histamine H1 receptor
Drug Central 415 2 0 3 5.6 Cc1cncc(c1)CN1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 None
133017 3416 72 None 28 2 Human 8.1 pIC50 = 8.1 Functional
Inhibitory concentration against histamine H1 receptorInhibitory concentration against histamine H1 receptor
Drug Central 415 2 0 3 5.6 Cc1cncc(c1)CN1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 None
2413 3416 72 None 28 2 Human 8.1 pIC50 = 8.1 Functional
Inhibitory concentration against histamine H1 receptorInhibitory concentration against histamine H1 receptor
Drug Central 415 2 0 3 5.6 Cc1cncc(c1)CN1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 None
CHEMBL91397 3416 72 None 28 2 Human 8.1 pIC50 = 8.1 Functional
Inhibitory concentration against histamine H1 receptorInhibitory concentration against histamine H1 receptor
Drug Central 415 2 0 3 5.6 Cc1cncc(c1)CN1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 None
DB11614 3416 72 None 28 2 Human 8.1 pIC50 = 8.1 Functional
Inhibitory concentration against histamine H1 receptorInhibitory concentration against histamine H1 receptor
Drug Central 415 2 0 3 5.6 Cc1cncc(c1)CN1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 None
1027 1576 73 None 6 7 Guinea pig 8.1 pIC50 = 8.1 Functional
Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum
Drug Central 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 None
3241 1576 73 None 6 7 Guinea pig 8.1 pIC50 = 8.1 Functional
Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum
Drug Central 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 None
7176 1576 73 None 6 7 Guinea pig 8.1 pIC50 = 8.1 Functional
Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum
Drug Central 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 None
CHEMBL1106 1576 73 None 6 7 Guinea pig 8.1 pIC50 = 8.1 Functional
Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum
Drug Central 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 None
DB00751 1576 73 None 6 7 Guinea pig 8.1 pIC50 = 8.1 Functional
Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum
Drug Central 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 None
1224 1432 83 None 85 22 Guinea pig 8.1 pIC50 = 8.1 Functional
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
3100 1432 83 None 85 22 Guinea pig 8.1 pIC50 = 8.1 Functional
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
8980 1432 83 None 85 22 Guinea pig 8.1 pIC50 = 8.1 Functional
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
916 1432 83 None 85 22 Guinea pig 8.1 pIC50 = 8.1 Functional
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
CHEMBL657 1432 83 None 85 22 Guinea pig 8.1 pIC50 = 8.1 Functional
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
DB01075 1432 83 None 85 22 Guinea pig 8.1 pIC50 = 8.1 Functional
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
2995 204405 53 None 2 18 Rat 8.0 pIC50 = 8.0 Functional
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 204405 53 None 2 18 Rat 8.0 pIC50 = 8.0 Functional
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 204405 53 None 2 18 Rat 8.0 pIC50 = 8.0 Functional
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
2398 954 62 None 2 36 Rat 8.0 pIC50 = 8.0 Functional
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
2801 954 62 None 2 36 Rat 8.0 pIC50 = 8.0 Functional
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
701 954 62 None 2 36 Rat 8.0 pIC50 = 8.0 Functional
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
CHEMBL415 954 62 None 2 36 Rat 8.0 pIC50 = 8.0 Functional
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
DB01242 954 62 None 2 36 Rat 8.0 pIC50 = 8.0 Functional
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
4223 3992 94 None -199 16 Human 6.5 pIC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 15341484
6918314 3992 94 None -199 16 Human 6.5 pIC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 15341484
7427 3992 94 None -199 16 Human 6.5 pIC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 15341484
CHEMBL439849 3992 94 None -199 16 Human 6.5 pIC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 15341484
DB06684 3992 94 None -199 16 Human 6.5 pIC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 15341484
2762 3863 31 None 100 9 Human 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 14667234
5587 3863 31 None 100 9 Human 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 14667234
7318 3863 31 None 100 9 Human 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 14667234
CHEMBL1241 3863 31 None 100 9 Human 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 14667234
DB00792 3863 31 None 100 9 Human 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 14667234
10103 3416 72 None 28 2 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 415 2 0 3 5.6 Cc1cncc(c1)CN1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 16220969
133017 3416 72 None 28 2 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 415 2 0 3 5.6 Cc1cncc(c1)CN1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 16220969
2413 3416 72 None 28 2 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 415 2 0 3 5.6 Cc1cncc(c1)CN1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 16220969
CHEMBL91397 3416 72 None 28 2 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 415 2 0 3 5.6 Cc1cncc(c1)CN1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 16220969
DB11614 3416 72 None 28 2 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 415 2 0 3 5.6 Cc1cncc(c1)CN1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 16220969




Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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DOI

3158 56267 27 None 40 20 Human 9.0 pAC50 = 9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1628227 56267 27 None 40 20 Human 9.0 pAC50 = 9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
135 2532 43 None -1 58 Human 8.7 pAC50 = 8.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
1796 2532 43 None -1 58 Human 8.7 pAC50 = 8.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
4184 2532 43 None -1 58 Human 8.7 pAC50 = 8.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
CHEMBL6437 2532 43 None -1 58 Human 8.7 pAC50 = 8.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
DB06148 2532 43 None -1 58 Human 8.7 pAC50 = 8.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
3121 7885 104 None - 0 Human 7.0 pAC50 = 7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 144 5 1 1 2.3 CCCC(CCC)C(=O)O 10.1038/s41467-023-40064-9
CHEMBL109 7885 104 None - 0 Human 7.0 pAC50 = 7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 144 5 1 1 2.3 CCCC(CCC)C(=O)O 10.1038/s41467-023-40064-9
CHEMBL433 7885 104 None - 0 Human 7.0 pAC50 = 7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 144 5 1 1 2.3 CCCC(CCC)C(=O)O 10.1038/s41467-023-40064-9
213 3853 55 None -8 44 Human 6.0 pAC50 = 6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
2717 3853 55 None -8 44 Human 6.0 pAC50 = 6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
5533 3853 55 None -8 44 Human 6.0 pAC50 = 6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
CHEMBL621 3853 55 None -8 44 Human 6.0 pAC50 = 6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
DB00656 3853 55 None -8 44 Human 6.0 pAC50 = 6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
3689 102771 55 None - 0 Human 6.0 pAC50 = 6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 325 5 2 3 3.8 CC(C(O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL1372983 102771 55 None - 0 Human 6.0 pAC50 = 6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 325 5 2 3 3.8 CC(C(O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL305187 102771 55 None - 0 Human 6.0 pAC50 = 6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 325 5 2 3 3.8 CC(C(O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1038/s41467-023-40064-9
42890 9425 59 None - 0 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 497 3 5 10 1.0 CC(=O)[C@]1(O)Cc2c(O)c3c(c(O)c2[C@@H](O[C@H]2C[C@H](N)[C@H](O)[C@H](C)O2)C1)C(=O)c1ccccc1C3=O 10.1038/s41467-023-40064-9
CHEMBL1117 9425 59 None - 0 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 497 3 5 10 1.0 CC(=O)[C@]1(O)Cc2c(O)c3c(c(O)c2[C@@H](O[C@H]2C[C@H](N)[C@H](O)[C@H](C)O2)C1)C(=O)c1ccccc1C3=O 10.1038/s41467-023-40064-9
44139752 104284 45 None - 0 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 227 1 0 3 2.4 N#Cc1ccc([C@H]2CCc3cncn32)c(F)c1 10.1038/s41467-023-40064-9
CHEMBL3099695 104284 45 None - 0 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 227 1 0 3 2.4 N#Cc1ccc([C@H]2CCc3cncn32)c(F)c1 10.1038/s41467-023-40064-9
2477 745 59 None - 29 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1038/s41467-023-40064-9
36 745 59 None - 29 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1038/s41467-023-40064-9
437 745 59 None - 29 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1038/s41467-023-40064-9
CHEMBL49 745 59 None - 29 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1038/s41467-023-40064-9
DB00490 745 59 None - 29 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1038/s41467-023-40064-9
11693 1827 16 None - 5 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
3494 1827 16 None - 5 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
4302 1827 16 None - 5 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
7459 1827 16 None - 5 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
CHEMBL1201335 1827 16 None - 5 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
DB00986 1827 16 None - 5 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
5048 3133 64 None -109 7 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1038/s41467-023-40064-9
8924 3133 64 None -109 7 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1038/s41467-023-40064-9
9948102 3133 64 None -109 7 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL462605 3133 64 None -109 7 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1038/s41467-023-40064-9
DB11642 3133 64 None -109 7 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1038/s41467-023-40064-9
4846 27987 53 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 308 1 2 6 2.2 O=C(O)c1cc(O)c2c3nc4ccccc4oc-3cc(=O)c2n1 10.1038/s41467-023-40064-9
CHEMBL1372341 27987 53 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 308 1 2 6 2.2 O=C(O)c1cc(O)c2c3nc4ccccc4oc-3cc(=O)c2n1 10.1038/s41467-023-40064-9
5284632 67402 13 None - 5 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 392 4 1 3 3.8 O=C(O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]21CCCC1)C(O)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1888176 67402 13 None - 5 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 392 4 1 3 3.8 O=C(O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]21CCCC1)C(O)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL3084748 67402 13 None - 5 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 392 4 1 3 3.8 O=C(O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]21CCCC1)C(O)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
1549120 196486 85 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 319 4 1 4 2.9 CC(/C=C1\SC(=S)N(CC(=O)O)C1=O)=C\c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL56337 196486 85 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 319 4 1 4 2.9 CC(/C=C1\SC(=S)N(CC(=O)O)C1=O)=C\c1ccccc1 10.1038/s41467-023-40064-9
2600 3779 74 None 1 13 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
2608 3779 74 None 1 13 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
5405 3779 74 None 1 13 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
CHEMBL17157 3779 74 None 1 13 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
DB00342 3779 74 None 1 13 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
2564 206184 51 None -2 3 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 290 6 0 3 3.4 CN(C)CCOC(c1ccc(Cl)cc1)c1ccccn1 10.1038/s41467-023-40064-9
CHEMBL864 206184 51 None -2 3 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 290 6 0 3 3.4 CN(C)CCOC(c1ccc(Cl)cc1)c1ccccn1 10.1038/s41467-023-40064-9
6337614 12996 54 None - 0 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 296 1 0 2 2.7 O=C1c2cccc3c2[C@H](CCC3)CN1[C@@H]1CN2CCC1CC2 10.1038/s41467-023-40064-9
CHEMBL1189679 12996 54 None - 0 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 296 1 0 2 2.7 O=C1c2cccc3c2[C@H](CCC3)CN1[C@@H]1CN2CCC1CC2 10.1038/s41467-023-40064-9
4260 52558 31 None - 0 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 279 6 0 4 3.0 CC(=O)Oc1cc(C(C)C)c(OCCN(C)C)cc1C 10.1038/s41467-023-40064-9
CHEMBL159226 52558 31 None - 0 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 279 6 0 4 3.0 CC(=O)Oc1cc(C(C)C)c(OCCN(C)C)cc1C 10.1038/s41467-023-40064-9
4034 55822 55 None - 1 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 390 5 0 2 5.6 Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1 10.1038/s41467-023-40064-9
CHEMBL1623 55822 55 None - 1 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 390 5 0 2 5.6 Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1 10.1038/s41467-023-40064-9
5656 203066 87 None -79 40 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 10.1038/s41467-023-40064-9
CHEMBL637 203066 87 None -79 40 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 10.1038/s41467-023-40064-9
214 3860 58 None -43 30 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
2740 3860 58 None -43 30 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
5566 3860 58 None -43 30 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
66064 3860 58 None -43 30 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL422 3860 58 None -43 30 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
DB00831 3860 58 None -43 30 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
367 3824 12 None - 8 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
5487427 3824 12 None - 8 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
8592 3824 12 None - 8 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
CHEMBL1900528 3824 12 None - 8 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
CHEMBL3305968 3824 12 None - 8 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
CHEMBL4650755 3824 12 None - 8 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
DB01409 3824 12 None - 8 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
2218 15283 23 None - 0 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 322 8 0 2 4.4 CCN(CC)CCCN(c1ccccc1)C1Cc2ccccc2C1 10.1038/s41467-023-40064-9
CHEMBL1213033 15283 23 None - 0 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 322 8 0 2 4.4 CCN(CC)CCCN(c1ccccc1)C1Cc2ccccc2C1 10.1038/s41467-023-40064-9
1613 2348 53 None -3 44 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
205 2348 53 None -3 44 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
3964 2348 53 None -3 44 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
CHEMBL831 2348 53 None -3 44 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
DB00408 2348 53 None -3 44 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
1170 1633 75 None - 1 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1038/s41467-023-40064-9
3348 1633 75 None - 1 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1038/s41467-023-40064-9
4819 1633 75 None - 1 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1038/s41467-023-40064-9
74685737 1633 75 None - 1 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1038/s41467-023-40064-9
CHEMBL914 1633 75 None - 1 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1038/s41467-023-40064-9
DB00950 1633 75 None - 1 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1038/s41467-023-40064-9
260 3869 54 None - 5 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1038/s41467-023-40064-9
2775 3869 54 None - 5 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1038/s41467-023-40064-9
656665 3869 54 None - 5 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL56564 3869 54 None - 5 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB11699 3869 54 None - 5 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1038/s41467-023-40064-9
3149 12614 15 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 334 15 0 1 6.1 CCCCCCCCCCCC[N+](C)(C)CCOc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1187011 12614 15 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 334 15 0 1 6.1 CCCCCCCCCCCC[N+](C)(C)CCOc1ccccc1 10.1038/s41467-023-40064-9
7029 13669 19 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 205 5 0 2 2.6 CCN(CC)C(C)C(=O)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1194666 13669 19 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 205 5 0 2 2.6 CCN(CC)C(C)C(=O)c1ccccc1 10.1038/s41467-023-40064-9
11980903 14492 19 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
22526 14492 19 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
5281035 14492 19 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1201303 14492 19 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
54841 203127 52 None -2 27 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 255 6 1 2 3.7 CNCC[C@@H](Oc1ccccc1C)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL641 203127 52 None -2 27 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 255 6 1 2 3.7 CNCC[C@@H](Oc1ccccc1C)c1ccccc1 10.1038/s41467-023-40064-9
10531 1420 21 None - 23 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
121 1420 21 None - 23 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
888 1420 21 None - 23 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
CHEMBL1732 1420 21 None - 23 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
DB00320 1420 21 None - 23 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
135398747 33453 24 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 137 1 1 2 0.3 C[n+]1ccccc1C=NO 10.1038/s41467-023-40064-9
135484646 33453 24 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 137 1 1 2 0.3 C[n+]1ccccc1C=NO 10.1038/s41467-023-40064-9
4884 33453 24 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 137 1 1 2 0.3 C[n+]1ccccc1C=NO 10.1038/s41467-023-40064-9
CHEMBL1420 33453 24 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 137 1 1 2 0.3 C[n+]1ccccc1C=NO 10.1038/s41467-023-40064-9
180 401 56 None -1 40 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
200 401 56 None -1 40 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
2160 401 56 None -1 40 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL629 401 56 None -1 40 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00321 401 56 None -1 40 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
124087 1389 114 None 3 15 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
7157 1389 114 None 3 15 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
814 1389 114 None 3 15 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
CHEMBL1172 1389 114 None 3 15 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
DB00967 1389 114 None 3 15 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
1201549 597 24 None -1 20 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
333 597 24 None -1 20 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
7601 597 24 None -1 20 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1201203 597 24 None -1 20 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL438151 597 24 None -1 20 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
DB00245 597 24 None -1 20 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
2318 154856 29 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 351 7 1 3 4.1 CC(Cc1cccc(C(F)(F)F)c1)NCCOC(=O)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL400599 154856 29 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 351 7 1 3 4.1 CC(Cc1cccc(C(F)(F)F)c1)NCCOC(=O)c1ccccc1 10.1038/s41467-023-40064-9
2402 3370 62 None - 24 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1038/s41467-023-40064-9
5095 3370 62 None - 24 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1038/s41467-023-40064-9
7295 3370 62 None - 24 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1038/s41467-023-40064-9
CHEMBL589 3370 62 None - 24 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1038/s41467-023-40064-9
DB00268 3370 62 None - 24 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1038/s41467-023-40064-9
2274 3173 58 None -3 31 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
4917 3173 58 None -3 31 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
7279 3173 58 None -3 31 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
CHEMBL728 3173 58 None -3 31 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
DB00433 3173 58 None -3 31 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
2995 204405 53 None -14 23 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1696 204405 53 None -14 23 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL72 204405 53 None -14 23 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
16362 3125 71 None -489 30 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
2172 3125 71 None -489 30 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
90 3125 71 None -489 30 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL1423 3125 71 None -489 30 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB01100 3125 71 None -489 30 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
2470 3653 50 None -4570 59 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
3300 3653 50 None -4570 59 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
5265 3653 50 None -4570 59 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
99 3653 50 None -4570 59 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL267930 3653 50 None -4570 59 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
10007 14484 38 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 183 2 1 1 2.6 CC(C)(N)Cc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL1201269 14484 38 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 183 2 1 1 2.6 CC(C)(N)Cc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
20628 96548 28 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 324 6 1 5 3.7 CN(C)CCCNc1c2ccccc2nc2cccc([N+](=O)[O-])c12 10.1038/s41467-023-40064-9
CHEMBL26291 96548 28 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 324 6 1 5 3.7 CN(C)CCCNc1c2ccccc2nc2cccc([N+](=O)[O-])c12 10.1038/s41467-023-40064-9
5365247 138429 33 None - 1 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 316 4 0 2 3.8 CN(C)C/C=C(/c1ccc(Br)cc1)c1cccnc1 10.1038/s41467-023-40064-9
CHEMBL37744 138429 33 None - 1 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 316 4 0 2 3.8 CN(C)C/C=C(/c1ccc(Br)cc1)c1cccnc1 10.1038/s41467-023-40064-9
21772 78399 31 None - 0 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 293 4 0 1 4.5 CC(CC1c2ccccc2CCc2ccccc21)CN(C)C 10.1038/s41467-023-40064-9
CHEMBL2110816 78399 31 None - 0 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 293 4 0 1 4.5 CC(CC1c2ccccc2CCc2ccccc21)CN(C)C 10.1038/s41467-023-40064-9
228 445 28 None - 24 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
33 445 28 None - 24 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
6005 445 28 None - 24 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
CHEMBL53 445 28 None - 24 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
DB00714 445 28 None - 24 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
2264 53190 38 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 349 2 1 4 1.5 CN1C(=O)COc2c(C(=O)NC3CN4CCC3CC4)cc(Cl)cc21 10.1038/s41467-023-40064-9
CHEMBL1598608 53190 38 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 349 2 1 4 1.5 CN1C(=O)COc2c(C(=O)NC3CN4CCC3CC4)cc(Cl)cc21 10.1038/s41467-023-40064-9
CHEMBL5292015 194537 0 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 398 6 1 3 3.6 C[N@+]1(CCF)[C@@H]2CC[C@H]1C[C@@H](OC(=O)C(O)(c1ccccc1)c1ccccc1)C2 10.1038/s41467-023-40064-9
55483 205097 40 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 356 13 4 4 3.6 Oc1ccc(CCNCCCCCCNCCc2ccccc2)cc1O 10.1038/s41467-023-40064-9
CHEMBL77622 205097 40 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 356 13 4 4 3.6 Oc1ccc(CCNCCCCCCNCCc2ccccc2)cc1O 10.1038/s41467-023-40064-9
4066 204626 78 None -1 7 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 10.1038/s41467-023-40064-9
CHEMBL73451 204626 78 None -1 7 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 10.1038/s41467-023-40064-9
156419 938 74 None - 1 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
3308 938 74 None - 1 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
647 938 74 None - 1 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL1201284 938 74 None - 1 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
DB01012 938 74 None - 1 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
3042 1414 35 None - 14 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
355 1414 35 None - 14 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
868 1414 35 None - 14 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
CHEMBL1123 1414 35 None - 14 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
DB00804 1414 35 None - 14 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
2169 44847 35 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 380 9 3 6 1.4 COc1ccccc1OCCNCC(O)c1ccc(C)c(S(N)(=O)=O)c1 10.1038/s41467-023-40064-9
CHEMBL152231 44847 35 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 380 9 3 6 1.4 COc1ccccc1OCCNCC(O)c1ccc(C)c(S(N)(=O)=O)c1 10.1038/s41467-023-40064-9
1427 2013 54 None -5 27 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
357 2013 54 None -5 27 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
3696 2013 54 None -5 27 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL11 2013 54 None -5 27 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00458 2013 54 None -5 27 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
40466858 16155 67 None - 0 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 348 6 1 3 4.0 Cc1ccc(/C(=C\CN2CCCC2)c2cccc(/C=C/C(=O)O)n2)cc1 10.1038/s41467-023-40064-9
5284514 16155 67 None - 0 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 348 6 1 3 4.0 Cc1ccc(/C(=C\CN2CCCC2)c2cccc(/C=C/C(=O)O)n2)cc1 10.1038/s41467-023-40064-9
CHEMBL1224 16155 67 None - 0 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 348 6 1 3 4.0 Cc1ccc(/C(=C\CN2CCCC2)c2cccc(/C=C/C(=O)O)n2)cc1 10.1038/s41467-023-40064-9
5440 28724 37 None -1 9 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL1378 28724 37 None -1 9 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
2142 3096 58 None -263 36 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
4920903 3096 58 None -263 36 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
502 3096 58 None -263 36 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
5775 3096 58 None -263 36 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
CHEMBL597 3096 58 None -263 36 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
DB00692 3096 58 None -263 36 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
4632 56058 115 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 228 3 1 3 2.6 COc1ccc(C(=O)c2ccccc2)c(O)c1 10.1038/s41467-023-40064-9
CHEMBL1625 56058 115 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 228 3 1 3 2.6 COc1ccc(C(=O)c2ccccc2)c(O)c1 10.1038/s41467-023-40064-9
3704 78189 41 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 231 3 1 3 1.6 C1=Cc2cccc(OCC3CNCCO3)c2C1 10.1038/s41467-023-40064-9
CHEMBL2105022 78189 41 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 231 3 1 3 1.6 C1=Cc2cccc(OCC3CNCCO3)c2C1 10.1038/s41467-023-40064-9
4942 5718 50 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 367 7 0 4 4.0 CCCOC(C(=O)OC1CCN(C)CC1)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1078261 5718 50 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 367 7 0 4 4.0 CCCOC(C(=O)OC1CCN(C)CC1)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
1971 2866 38 None -1 30 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
2404 2866 38 None -1 30 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
4543 2866 38 None -1 30 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL445 2866 38 None -1 30 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
DB00540 2866 38 None -1 30 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
1228 3866 34 None -5 4 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 10.1038/s41467-023-40064-9
2763 3866 34 None -5 4 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 10.1038/s41467-023-40064-9
5282443 3866 34 None -5 4 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 10.1038/s41467-023-40064-9
CHEMBL855 3866 34 None -5 4 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 10.1038/s41467-023-40064-9
DB00427 3866 34 None -5 4 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 10.1038/s41467-023-40064-9
1605 2342 117 None -2 4 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1038/s41467-023-40064-9
3957 2342 117 None -2 4 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1038/s41467-023-40064-9
7216 2342 117 None -2 4 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1038/s41467-023-40064-9
CHEMBL998 2342 117 None -2 4 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1038/s41467-023-40064-9
DB00455 2342 117 None -2 4 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1038/s41467-023-40064-9
30323 62485 57 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 527 4 5 11 1.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(C)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
CHEMBL1563 62485 57 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 527 4 5 11 1.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(C)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
CHEMBL178 62485 57 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 527 4 5 11 1.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(C)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
2812 4779 101 None -28 34 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 10.1038/s41467-023-40064-9
CHEMBL104 4779 101 None -28 34 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 10.1038/s41467-023-40064-9
72093 35061 9 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
CHEMBL1433361 35061 9 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
CHEMBL2103773 35061 9 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
5284550 41721 15 None -1 9 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1492500 41721 15 None -1 9 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 10.1038/s41467-023-40064-9
4640 78266 30 None - 0 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 379 6 1 4 3.9 COc1cc2[nH]c(C)c(CCN3CCN(c4ccccc4)CC3)c2cc1OC 10.1038/s41467-023-40064-9
CHEMBL2107011 78266 30 None - 0 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 379 6 1 4 3.9 COc1cc2[nH]c(C)c(CCN3CCN(c4ccccc4)CC3)c2cc1OC 10.1038/s41467-023-40064-9
2771 195017 74 None -2 27 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
CHEMBL1200781 195017 74 None -2 27 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
CHEMBL549 195017 74 None -2 27 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
46780481 107531 20 None -13 53 Human 8.7 pAC50 = 8.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
9903970 107531 20 None -13 53 Human 8.7 pAC50 = 8.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
CHEMBL3187365 107531 20 None -13 53 Human 8.7 pAC50 = 8.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
CHEMBL3544974 107531 20 None -13 53 Human 8.7 pAC50 = 8.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
1210 918 51 None -20 21 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
1213 918 51 None -20 21 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
2725 918 51 None -20 21 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
33036 918 51 None -20 21 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
4411 918 51 None -20 21 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
616 918 51 None -20 21 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
6976 918 51 None -20 21 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
716121 918 51 None -20 21 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
CHEMBL1201353 918 51 None -20 21 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
CHEMBL1554789 918 51 None -20 21 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
CHEMBL505 918 51 None -20 21 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
DB01114 918 51 None -20 21 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
DB13679 918 51 None -20 21 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
16351 102730 47 None - 6 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
CHEMBL304902 102730 47 None - 6 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
225609 14452 56 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 422 3 2 6 2.4 CC(=O)OCC(=O)[C@@]1(O)CC[C@H]2[C@@H]3CCC4=CC(=O)CC[C@]4(C)[C@@]3(F)[C@@H](O)C[C@@]21C 10.1038/s41467-023-40064-9
CHEMBL1201010 14452 56 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 422 3 2 6 2.4 CC(=O)OCC(=O)[C@@]1(O)CC[C@H]2[C@@H]3CCC4=CC(=O)CC[C@]4(C)[C@@]3(F)[C@@H](O)C[C@@]21C 10.1038/s41467-023-40064-9
216416 111581 48 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 413 6 1 3 5.7 Oc1ccc2c(c1)CC[C@H](c1ccccc1)[C@@H]2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
CHEMBL328190 111581 48 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 413 6 1 3 5.7 Oc1ccc2c(c1)CC[C@H](c1ccccc1)[C@@H]2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
2895 203592 41 None -1 8 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 275 3 0 1 4.6 CN(C)CCC=C1c2ccccc2C=Cc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL669 203592 41 None -1 8 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 275 3 0 1 4.6 CN(C)CCC=C1c2ccccc2C=Cc2ccccc21 10.1038/s41467-023-40064-9
1524 2181 96 None -2 52 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
197 2181 96 None -2 52 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
3822 2181 96 None -2 52 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
88 2181 96 None -2 52 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
CHEMBL51 2181 96 None -2 52 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
DB12465 2181 96 None -2 52 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
2601 3780 33 None - 21 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
443951 3780 33 None - 21 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
56 3780 33 None - 21 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
CHEMBL73151 3780 33 None - 21 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
DB13399 3780 33 None - 21 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
6729 14485 41 None - 0 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 432 5 0 2 6.5 CC(C)(C)c1ccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)cc1 10.1038/s41467-023-40064-9
CHEMBL1201271 14485 41 None - 0 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 432 5 0 2 6.5 CC(C)(C)c1ccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)cc1 10.1038/s41467-023-40064-9
24826799 10798 104 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 532 4 1 6 4.5 Cc1ccc(C(=O)Nc2ccc(CN3CCN(C)CC3)c(C(F)(F)F)c2)cc1C#Cc1cnc2cccnn12 10.1038/s41467-023-40064-9
CHEMBL1171837 10798 104 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 532 4 1 6 4.5 Cc1ccc(C(=O)Nc2ccc(CN3CCN(C)CC3)c(C(F)(F)F)c2)cc1C#Cc1cnc2cccnn12 10.1038/s41467-023-40064-9
107771 120248 49 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 517 7 2 7 6.1 COc1ccc2nc3cc(Cl)ccc3c(Nc3cc(CN4CCCC4)c(O)c(CN4CCCC4)c3)c2n1 10.1038/s41467-023-40064-9
CHEMBL35228 120248 49 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 517 7 2 7 6.1 COc1ccc2nc3cc(Cl)ccc3c(Nc3cc(CN4CCCC4)c(O)c(CN4CCCC4)c3)c2n1 10.1038/s41467-023-40064-9
240 944 43 None - 24 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1038/s41467-023-40064-9
2769 944 43 None - 24 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1038/s41467-023-40064-9
44279790 944 43 None - 24 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1038/s41467-023-40064-9
660 944 43 None - 24 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1038/s41467-023-40064-9
CHEMBL1729 944 43 None - 24 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1038/s41467-023-40064-9
CHEMBL560739 944 43 None - 24 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1038/s41467-023-40064-9
DB00604 944 43 None - 24 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1038/s41467-023-40064-9
104850 3330 96 None - 5 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
4150 3330 96 None - 5 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
743 3330 96 None - 5 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL111 3330 96 None - 5 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
DB06155 3330 96 None - 5 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
444 206666 53 None -2089 18 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 239 3 1 2 3.3 CC(NC(C)(C)C)C(=O)c1cccc(Cl)c1 10.1038/s41467-023-40064-9
CHEMBL894 206666 53 None -2089 18 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 239 3 1 2 3.3 CC(NC(C)(C)C)C(=O)c1cccc(Cl)c1 10.1038/s41467-023-40064-9
2726 919 68 None -2 72 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
621 919 68 None -2 72 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
83 919 68 None -2 72 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL71 919 68 None -2 72 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB00477 919 68 None -2 72 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
21722 17992 31 None 1 6 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 10.1038/s41467-023-40064-9
CHEMBL126224 17992 31 None 1 6 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 10.1038/s41467-023-40064-9
2200 20203 61 None - 2 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL1256819 20203 61 None - 2 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL1305 20203 61 None - 2 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
1164 1630 26 None - 12 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1038/s41467-023-40064-9
1626 1630 26 None - 12 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1038/s41467-023-40064-9
3345 1630 26 None - 12 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL596 1630 26 None - 12 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1038/s41467-023-40064-9
DB00813 1630 26 None - 12 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1038/s41467-023-40064-9
46220502 112583 84 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 506 7 1 8 4.9 CCN1CCN(Cc2ccc(Nc3ncc(F)c(-c4cc(F)c5nc(C)n(C(C)C)c5c4)n3)nc2)CC1 10.1038/s41467-023-40064-9
CHEMBL3301610 112583 84 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 506 7 1 8 4.9 CCN1CCN(Cc2ccc(Nc3ncc(F)c(-c4cc(F)c5nc(C)n(C(C)C)c5c4)n3)nc2)CC1 10.1038/s41467-023-40064-9
68617 205527 62 None -1023 26 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1709 205527 62 None -1023 26 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL809 205527 62 None -1023 26 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
176 398 66 None - 31 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
2157 398 66 None - 31 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
2566 398 66 None - 31 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
CHEMBL633 398 66 None - 31 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
DB01118 398 66 None - 31 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
2381 663 48 None - 8 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1038/s41467-023-40064-9
374 663 48 None - 8 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1038/s41467-023-40064-9
7128 663 48 None - 8 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL1101 663 48 None - 8 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1038/s41467-023-40064-9
DB00810 663 48 None - 8 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1038/s41467-023-40064-9
2267 559 71 None 10 7 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
271 559 71 None 10 7 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
7121 559 71 None 10 7 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
CHEMBL639 559 71 None 10 7 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
DB00972 559 71 None 10 7 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
2865 4143 73 None -58 53 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
59 4143 73 None -58 53 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
60854 4143 73 None -58 53 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL708 4143 73 None -58 53 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
DB00246 4143 73 None -58 53 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
65709 59881 39 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 365 8 0 5 3.3 CCN(CC)CCn1c(=O)c(Cc2ccc(OC)cc2)nc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1729803 59881 39 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 365 8 0 5 3.3 CCN(CC)CCn1c(=O)c(Cc2ccc(OC)cc2)nc2ccccc21 10.1038/s41467-023-40064-9
71481097 120510 48 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 443 5 2 7 3.4 O=C(/C=C\n1cnc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)n1)NNc1cnccn1 10.1038/s41467-023-40064-9
CHEMBL3545185 120510 48 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 443 5 2 7 3.4 O=C(/C=C\n1cnc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)n1)NNc1cnccn1 10.1038/s41467-023-40064-9
2337 3256 77 None 1 62 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
50 3256 77 None 1 62 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
5002 3256 77 None 1 62 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL716 3256 77 None 1 62 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
DB01224 3256 77 None 1 62 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
150 2509 21 None - 16 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1038/s41467-023-40064-9
1764 2509 21 None - 16 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1038/s41467-023-40064-9
8226 2509 21 None - 16 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1038/s41467-023-40064-9
CHEMBL1201356 2509 21 None - 16 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1038/s41467-023-40064-9
DB00353 2509 21 None - 16 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1038/s41467-023-40064-9
2389 3331 118 None -46 67 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
5073 3331 118 None -46 67 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
96 3331 118 None -46 67 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
CHEMBL85 3331 118 None -46 67 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
DB00734 3331 118 None -46 67 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
4832 55420 17 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 354 5 1 3 3.1 CC[N+]1(C)CCCC(OC(=O)C(O)(c2ccccc2)c2ccccc2)C1 10.1038/s41467-023-40064-9
CHEMBL1619528 55420 17 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 354 5 1 3 3.1 CC[N+]1(C)CCCC(OC(=O)C(O)(c2ccccc2)c2ccccc2)C1 10.1038/s41467-023-40064-9
68867 78173 38 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 402 7 2 6 3.1 CCOc1cc(N)c([N+](=O)[O-])cc1C(=O)NC1CCN(CC2CC=CCC2)CC1 10.1038/s41467-023-40064-9
CHEMBL2104523 78173 38 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 402 7 2 6 3.1 CCOc1cc(N)c([N+](=O)[O-])cc1C(=O)NC1CCN(CC2CC=CCC2)CC1 10.1038/s41467-023-40064-9
60065 84369 6 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 505 7 1 8 4.2 COC(=O)C1=C(C)NC(C)=C(C(=O)O[C@@H]2CCCN(Cc3ccccc3)C2)C1c1cccc([N+](=O)[O-])c1 10.1038/s41467-023-40064-9
CHEMBL2218858 84369 6 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 505 7 1 8 4.2 COC(=O)C1=C(C)NC(C)=C(C(=O)O[C@@H]2CCCN(Cc3ccccc3)C2)C1c1cccc([N+](=O)[O-])c1 10.1038/s41467-023-40064-9
146570 43454 67 None -1 4 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 324 5 0 3 3.8 CN(C)CCC[C@@]1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
CHEMBL1508 43454 67 None -1 4 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 324 5 0 3 3.8 CN(C)CCC[C@@]1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
1212 1662 50 None -41 65 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
204 1662 50 None -41 65 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
3372 1662 50 None -41 65 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL726 1662 50 None -41 65 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
DB00623 1662 50 None -41 65 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
5311507 194815 41 None - 1 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 400 5 1 4 4.2 OCCN1CCN(CC/C=C2/c3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
CHEMBL53904 194815 41 None - 1 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 400 5 1 4 4.2 OCCN1CCN(CC/C=C2/c3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
55645 84370 8 None - 0 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 395 7 2 4 2.1 CCCN1CC(NS(=O)(=O)N(CC)CC)CC2Cc3c(O)cccc3CC21 10.1038/s41467-023-40064-9
CHEMBL2218861 84370 8 None - 0 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 395 7 2 4 2.1 CCCN1CC(NS(=O)(=O)N(CC)CC)CC2Cc3c(O)cccc3CC21 10.1038/s41467-023-40064-9
11658860 2344 51 None - 3 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1038/s41467-023-40064-9
2941 2344 51 None - 3 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1038/s41467-023-40064-9
4374 2344 51 None - 3 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1038/s41467-023-40064-9
CHEMBL360328 2344 51 None - 3 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1038/s41467-023-40064-9
DB04871 2344 51 None - 3 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1038/s41467-023-40064-9
4046 2483 33 None - 2 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
4252 2483 33 None - 2 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
CHEMBL416956 2483 33 None - 2 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
DB00358 2483 33 None - 2 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
104870 98880 47 None - 21 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 10.1038/s41467-023-40064-9
5374 98880 47 None - 21 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 10.1038/s41467-023-40064-9
CHEMBL279085 98880 47 None - 21 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 10.1038/s41467-023-40064-9
3081361 93934 123 None - 0 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 474 5 1 5 4.4 COc1cc2/c(=N/c3ccc(Br)cc3F)nc[nH]c2cc1OCC1CCN(C)CC1 10.1038/s41467-023-40064-9
CHEMBL24828 93934 123 None - 0 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 474 5 1 5 4.4 COc1cc2/c(=N/c3ccc(Br)cc3F)nc[nH]c2cc1OCC1CCN(C)CC1 10.1038/s41467-023-40064-9
2540 4401 111 None - 4 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 610 10 1 11 6.3 CCOc1nc2cccc(C(=O)OC(C)OC(=O)OC3CCCCC3)c2n1Cc1ccc(-c2ccccc2-c2nn[nH]n2)cc1 10.1038/s41467-023-40064-9
CHEMBL1014 4401 111 None - 4 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 610 10 1 11 6.3 CCOc1nc2cccc(C(=O)OC(C)OC(=O)OC3CCCCC3)c2n1Cc1ccc(-c2ccccc2-c2nn[nH]n2)cc1 10.1038/s41467-023-40064-9
6127 14499 8 None - 0 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 278 2 0 0 4.4 C[N+]1(C)CCC(=C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL1201340 14499 8 None - 0 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 278 2 0 0 4.4 C[N+]1(C)CCC(=C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
179 400 115 None -4365 49 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC 10.1038/s41467-023-40064-9
2159 400 115 None -4365 49 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC 10.1038/s41467-023-40064-9
963 400 115 None -4365 49 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC 10.1038/s41467-023-40064-9
CHEMBL243712 400 115 None -4365 49 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC 10.1038/s41467-023-40064-9
DB06288 400 115 None -4365 49 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC 10.1038/s41467-023-40064-9
131411 15392 70 None - 0 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 476 7 1 6 5.2 CCOC(=O)c1c(CSc2ccccc2)n(C)c2cc(Br)c(O)c(CN(C)C)c12 10.1038/s41467-023-40064-9
28446253 15392 70 None - 0 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 476 7 1 6 5.2 CCOC(=O)c1c(CSc2ccccc2)n(C)c2cc(Br)c(O)c(CN(C)C)c12 10.1038/s41467-023-40064-9
CHEMBL1214598 15392 70 None - 0 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 476 7 1 6 5.2 CCOC(=O)c1c(CSc2ccccc2)n(C)c2cc(Br)c(O)c(CN(C)C)c12 10.1038/s41467-023-40064-9
CHEMBL2103737 78140 0 None - 0 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL None None None None 10.1038/s41467-023-40064-9
4528 98126 80 None -1 10 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 238 1 1 2 2.8 CN1Cc2c(N)cccc2C(c2ccccc2)C1 10.1038/s41467-023-40064-9
CHEMBL273575 98126 80 None -1 10 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 238 1 1 2 2.8 CN1Cc2c(N)cccc2C(c2ccccc2)C1 10.1038/s41467-023-40064-9
2284 3182 33 None 1 29 Human 8.5 pAC50 = 8.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
4926 3182 33 None 1 29 Human 8.5 pAC50 = 8.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
7281 3182 33 None 1 29 Human 8.5 pAC50 = 8.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL564 3182 33 None 1 29 Human 8.5 pAC50 = 8.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00420 3182 33 None 1 29 Human 8.5 pAC50 = 8.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
26987 949 33 None 16 21 Human 8.5 pAC50 = 8.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
6063 949 33 None 16 21 Human 8.5 pAC50 = 8.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
671 949 33 None 16 21 Human 8.5 pAC50 = 8.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
CHEMBL1626 949 33 None 16 21 Human 8.5 pAC50 = 8.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
DB00283 949 33 None 16 21 Human 8.5 pAC50 = 8.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
2782 32000 67 None - 1 Human 8.5 pAC50 = 8.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 325 4 0 3 4.3 Clc1ccc(Cn2c(CN3CCCC3)nc3ccccc32)cc1 10.1038/s41467-023-40064-9
CHEMBL1407943 32000 67 None - 1 Human 8.5 pAC50 = 8.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 325 4 0 3 4.3 Clc1ccc(Cn2c(CN3CCCC3)nc3ccccc32)cc1 10.1038/s41467-023-40064-9
CHEMBL3216363 32000 67 None - 1 Human 8.5 pAC50 = 8.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 325 4 0 3 4.3 Clc1ccc(Cn2c(CN3CCCC3)nc3ccccc32)cc1 10.1038/s41467-023-40064-9
2136 3095 30 None - 6 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
4768 3095 30 None - 6 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
7268 3095 30 None - 6 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL753 3095 30 None - 6 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
DB00925 3095 30 None - 6 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
4614 5391 103 None - 0 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 293 5 1 3 4.0 O=C(O)CCc1nc(-c2ccccc2)c(-c2ccccc2)o1 10.1038/s41467-023-40064-9
CHEMBL1071 5391 103 None - 0 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 293 5 1 3 4.0 O=C(O)CCc1nc(-c2ccccc2)c(-c2ccccc2)o1 10.1038/s41467-023-40064-9
1224 1432 83 None -2 13 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
3100 1432 83 None -2 13 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
8980 1432 83 None -2 13 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
916 1432 83 None -2 13 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
CHEMBL657 1432 83 None -2 13 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
DB01075 1432 83 None -2 13 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
1210 918 51 None -20 21 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
1213 918 51 None -20 21 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
2725 918 51 None -20 21 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
33036 918 51 None -20 21 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
4411 918 51 None -20 21 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
616 918 51 None -20 21 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
6976 918 51 None -20 21 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
716121 918 51 None -20 21 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
CHEMBL1201353 918 51 None -20 21 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
CHEMBL1554789 918 51 None -20 21 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
CHEMBL505 918 51 None -20 21 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
DB01114 918 51 None -20 21 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
DB13679 918 51 None -20 21 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
1547484 940 74 None -1 20 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
654 940 74 None -1 20 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
9072 940 74 None -1 20 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL43064 940 74 None -1 20 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
DB00568 940 74 None -1 20 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
9429 202133 58 None - 5 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 446 6 0 6 3.2 CN1CCN(CCCN2c3ccccc3Sc3ccc(S(=O)(=O)N(C)C)cc32)CC1 10.1038/s41467-023-40064-9
CHEMBL609109 202133 58 None - 5 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 446 6 0 6 3.2 CN1CCN(CCCN2c3ccccc3Sc3ccc(S(=O)(=O)N(C)C)cc32)CC1 10.1038/s41467-023-40064-9
5329102 194726 86 None - 0 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
CHEMBL535 194726 86 None - 0 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
154417 23181 60 None - 5 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 289 4 1 4 1.9 CN1[C@@H]2CC[C@H]1C[C@@H](OC(=O)[C@H](CO)c1ccccc1)C2 10.1038/s41467-023-40064-9
CHEMBL1331216 23181 60 None - 5 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 289 4 1 4 1.9 CN1[C@@H]2CC[C@H]1C[C@@H](OC(=O)[C@H](CO)c1ccccc1)C2 10.1038/s41467-023-40064-9
4940 14470 35 None - 0 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 340 5 0 4 4.8 CCC(=O)c1ccc2c(c1)N(CC(C)N(C)C)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL1201210 14470 35 None - 0 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 340 5 0 4 4.8 CCC(=O)c1ccc2c(c1)N(CC(C)N(C)C)c1ccccc1S2 10.1038/s41467-023-40064-9
1385580 29276 76 None -1 5 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
4615 29276 76 None -1 5 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL13828 29276 76 None -1 5 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
19675 51670 43 None - 0 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 410 7 1 5 5.0 CC(=O)c1ccc2c(c1)N(CCCN1CCC(CCO)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL1584 51670 43 None - 0 Human 7.5 pAC50 = 7.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 410 7 1 5 5.0 CC(=O)c1ccc2c(c1)N(CCCN1CCC(CCO)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
65700 78260 28 None - 0 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 238 1 1 2 3.3 CNC1Cc2ccccc2N(C)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL2106919 78260 28 None - 0 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 238 1 1 2 3.3 CNC1Cc2ccccc2N(C)c2ccccc21 10.1038/s41467-023-40064-9
212 3806 47 None -5 25 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
2639 3806 47 None -5 25 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
941651 3806 47 None -5 25 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
CHEMBL1201 3806 47 None -5 25 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
DB01623 3806 47 None -5 25 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
25382 9157 37 None - 0 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 291 3 0 1 4.7 CN(C)CCC=C1c2ccccc2C(C)(C)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL110094 9157 37 None - 0 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 291 3 0 1 4.7 CN(C)CCC=C1c2ccccc2C(C)(C)c2ccccc21 10.1038/s41467-023-40064-9
4008 7226 92 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 610 10 1 9 5.0 COC(=O)C1=C(C)NC(C)=C(C(=O)OCCN2CCN(C(c3ccccc3)c3ccccc3)CC2)C1c1cccc([N+](=O)[O-])c1 10.1038/s41467-023-40064-9
CHEMBL1085699 7226 92 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 610 10 1 9 5.0 COC(=O)C1=C(C)NC(C)=C(C(=O)OCCN2CCN(C(c3ccccc3)c3ccccc3)CC2)C1c1cccc([N+](=O)[O-])c1 10.1038/s41467-023-40064-9
1400 1957 70 None 2 3 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
3658 1957 70 None 2 3 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
7199 1957 70 None 2 3 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
91513 1957 70 None 2 3 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL896 1957 70 None 2 3 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
DB00557 1957 70 None 2 3 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
3151 1462 97 None -41 27 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
945 1462 97 None -41 27 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
965 1462 97 None -41 27 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL219916 1462 97 None -41 27 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB01184 1462 97 None -41 27 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL4743867 214033 14 None - 0 Human 8.3 pAC50 = 8.3 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL None None None OCCN1CCN(CCC=C2c3ccccc3Sc3ccc(C(F)(F)F)cc32)CC1 10.1038/s41467-023-40064-9
135398737 958 93 None 2 89 Human 8.3 pAC50 = 8.3 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
38 958 93 None 2 89 Human 8.3 pAC50 = 8.3 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
722 958 93 None 2 89 Human 8.3 pAC50 = 8.3 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL42 958 93 None 2 89 Human 8.3 pAC50 = 8.3 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
DB00363 958 93 None 2 89 Human 8.3 pAC50 = 8.3 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
2220 3134 82 None - 14 Human 8.3 pAC50 = 8.3 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
27400 3134 82 None - 14 Human 8.3 pAC50 = 8.3 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
93 3134 82 None - 14 Human 8.3 pAC50 = 8.3 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
CHEMBL294951 3134 82 None - 14 Human 8.3 pAC50 = 8.3 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
DB06153 3134 82 None - 14 Human 8.3 pAC50 = 8.3 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
2705 3842 64 None - 10 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1038/s41467-023-40064-9
360 3842 64 None - 10 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1038/s41467-023-40064-9
443879 3842 64 None - 10 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1038/s41467-023-40064-9
CHEMBL1382 3842 64 None - 10 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1038/s41467-023-40064-9
DB01036 3842 64 None - 10 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1038/s41467-023-40064-9
1890 2759 49 None -44 16 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
4449 2759 49 None -44 16 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
7247 2759 49 None -44 16 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
CHEMBL623 2759 49 None -44 16 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
DB01149 2759 49 None -44 16 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
209 3057 97 None -11 23 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
2113 3057 97 None -11 23 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
4748 3057 97 None -11 23 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
CHEMBL567 3057 97 None -11 23 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
DB00850 3057 97 None -11 23 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
1209 1658 75 None -144 32 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
203 1658 75 None -144 32 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
3386 1658 75 None -144 32 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL41 1658 75 None -144 32 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
DB00472 1658 75 None -144 32 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
242 470 124 None -22 51 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
34 470 124 None -22 51 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
60795 470 124 None -22 51 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
CHEMBL1112 470 124 None -22 51 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
DB01238 470 124 None -22 51 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
4452 2762 19 None - 19 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1038/s41467-023-40064-9
983 2762 19 None - 19 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1038/s41467-023-40064-9
CHEMBL20734 2762 19 None - 19 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1038/s41467-023-40064-9
2407 3372 76 None - 7 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
59227 3372 76 None - 7 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
941 3372 76 None - 7 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
CHEMBL1303 3372 76 None - 7 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
DB05271 3372 76 None - 7 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
5639 98895 75 None - 5 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 387 7 1 8 0.7 COc1ccccc1N1CCN(CCCNc2cc(=O)n(C)c(=O)n2C)CC1 10.1038/s41467-023-40064-9
CHEMBL279229 98895 75 None - 5 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 387 7 1 8 0.7 COc1ccccc1N1CCN(CCCNc2cc(=O)n(C)c(=O)n2C)CC1 10.1038/s41467-023-40064-9
3294 2006 111 None -14 45 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
71360 2006 111 None -14 45 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
87 2006 111 None -14 45 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
CHEMBL14376 2006 111 None -14 45 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
DB04946 2006 111 None -14 45 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
134 2514 24 None -933 67 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1038/s41467-023-40064-9
1775 2514 24 None -933 67 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1038/s41467-023-40064-9
9681 2514 24 None -933 67 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1038/s41467-023-40064-9
CHEMBL1065 2514 24 None -933 67 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1038/s41467-023-40064-9
DB00247 2514 24 None -933 67 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1038/s41467-023-40064-9
11434515 261 6 None - 5 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1038/s41467-023-40064-9
11519741 261 6 None - 5 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1038/s41467-023-40064-9
4484 261 6 None - 5 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1038/s41467-023-40064-9
7449 261 6 None - 5 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1038/s41467-023-40064-9
CHEMBL1194325 261 6 None - 5 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1038/s41467-023-40064-9
DB08897 261 6 None - 5 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1038/s41467-023-40064-9
4756 16649 50 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 213 2 2 5 2.7 Nc1ccc(/N=N/c2ccccc2)c(N)n1 10.1038/s41467-023-40064-9
CHEMBL1201022 16649 50 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 213 2 2 5 2.7 Nc1ccc(/N=N/c2ccccc2)c(N)n1 10.1038/s41467-023-40064-9
CHEMBL1242 16649 50 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 213 2 2 5 2.7 Nc1ccc(/N=N/c2ccccc2)c(N)n1 10.1038/s41467-023-40064-9
3949 100614 50 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 468 8 0 5 4.9 COc1ccc(CN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c(OC)c1OC 10.1038/s41467-023-40064-9
CHEMBL29188 100614 50 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 468 8 0 5 4.9 COc1ccc(CN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c(OC)c1OC 10.1038/s41467-023-40064-9
29566 78204 82 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 284 2 2 6 -2.7 O=S1(=O)CCN(CN2CCS(=O)(=O)NC2)CN1 10.1038/s41467-023-40064-9
CHEMBL2105420 78204 82 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 284 2 2 6 -2.7 O=S1(=O)CCN(CN2CCS(=O)(=O)NC2)CN1 10.1038/s41467-023-40064-9
17676 7072 29 None - 3 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 411 7 1 6 3.5 CC(=O)c1ccc2c(c1)N(CCCN1CCN(CCO)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
5281082 7072 29 None - 3 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 411 7 1 6 3.5 CC(=O)c1ccc2c(c1)N(CCCN1CCN(CCO)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL1085 7072 29 None - 3 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 411 7 1 6 3.5 CC(=O)c1ccc2c(c1)N(CCCN1CCN(CCO)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
19910 37408 106 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 190 1 1 4 1.8 O=[N+]([O-])c1ccc(O)c2ncccc12 10.1038/s41467-023-40064-9
CHEMBL1454910 37408 106 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 190 1 1 4 1.8 O=[N+]([O-])c1ccc(O)c2ncccc12 10.1038/s41467-023-40064-9
4976 203579 29 None -1 12 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 263 4 1 1 4.3 CNCCCC1c2ccccc2C=Cc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL668 203579 29 None -1 12 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 263 4 1 1 4.3 CNCCCC1c2ccccc2C=Cc2ccccc21 10.1038/s41467-023-40064-9
2105 3054 37 None - 33 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
47811 3054 37 None - 33 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
48 3054 37 None - 33 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
CHEMBL531 3054 37 None - 33 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
DB01186 3054 37 None - 33 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
6834 205552 45 None -1 2 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 318 5 0 2 3.9 CN(C)CCC(c1ccc(Br)cc1)c1ccccn1 10.1038/s41467-023-40064-9
CHEMBL811 205552 45 None -1 2 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 318 5 0 2 3.9 CN(C)CCC(c1ccc(Br)cc1)c1ccccn1 10.1038/s41467-023-40064-9
7045767 59108 27 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 203 5 0 4 -1.2 CC(=O)O[C@H](CC(=O)[O-])C[N+](C)(C)C 10.1038/s41467-023-40064-9
CHEMBL1697733 59108 27 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 203 5 0 4 -1.2 CC(=O)O[C@H](CC(=O)[O-])C[N+](C)(C)C 10.1038/s41467-023-40064-9
11949652 80512 60 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 426 4 1 7 1.6 Cc1cc(N2CCN([C@@H]3CN[C@H](C(=O)N4CCSC4)C3)CC2)n(-c2ccccc2)n1 10.1038/s41467-023-40064-9
CHEMBL2147777 80512 60 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 426 4 1 7 1.6 Cc1cc(N2CCN([C@@H]3CN[C@H](C(=O)N4CCSC4)C3)CC2)n(-c2ccccc2)n1 10.1038/s41467-023-40064-9
44093 48931 94 None - 0 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 217 3 2 3 0.6 C[C@H](CS)C(=O)N1CCC[C@H]1C(=O)O 10.1038/s41467-023-40064-9
CHEMBL1560 48931 94 None - 0 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 217 3 2 3 0.6 C[C@H](CS)C(=O)N1CCC[C@H]1C(=O)O 10.1038/s41467-023-40064-9
2393 3334 82 None - 5 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1038/s41467-023-40064-9
5078 3334 82 None - 5 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1038/s41467-023-40064-9
51 3334 82 None - 5 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1038/s41467-023-40064-9
CHEMBL905 3334 82 None - 5 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1038/s41467-023-40064-9
DB00953 3334 82 None - 5 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1038/s41467-023-40064-9
16960 14487 23 None - 0 Human 8.2 pAC50 = 8.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 318 5 0 2 3.9 CN(C)CC[C@@H](c1ccc(Br)cc1)c1ccccn1 10.1038/s41467-023-40064-9
CHEMBL1201287 14487 23 None - 0 Human 8.2 pAC50 = 8.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 318 5 0 2 3.9 CN(C)CC[C@@H](c1ccc(Br)cc1)c1ccccn1 10.1038/s41467-023-40064-9
1816 2540 102 None -3 18 Human 8.2 pAC50 = 8.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1038/s41467-023-40064-9
4205 2540 102 None -3 18 Human 8.2 pAC50 = 8.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1038/s41467-023-40064-9
7241 2540 102 None -3 18 Human 8.2 pAC50 = 8.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1038/s41467-023-40064-9
CHEMBL654 2540 102 None -3 18 Human 8.2 pAC50 = 8.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1038/s41467-023-40064-9
DB00370 2540 102 None -3 18 Human 8.2 pAC50 = 8.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1038/s41467-023-40064-9
19861 207523 50 None - 1 Human 8.2 pAC50 = 8.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 290 0 0 2 3.7 CN1CCC(=C2c3ccccc3CCc3cccnc32)CC1 10.1038/s41467-023-40064-9
CHEMBL946 207523 50 None - 1 Human 8.2 pAC50 = 8.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 290 0 0 2 3.7 CN1CCC(=C2c3ccccc3CCc3cccnc32)CC1 10.1038/s41467-023-40064-9
3926 207241 40 None - 0 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 491 9 1 3 5.8 Cc1cccc(C)c1NC(=O)CN1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1038/s41467-023-40064-9
CHEMBL92870 207241 40 None - 0 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 491 9 1 3 5.8 Cc1cccc(C)c1NC(=O)CN1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1038/s41467-023-40064-9
146015336 53348 111 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 252 2 2 2 2.0 O=C1N=C(O)NC1(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
1775 53348 111 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 252 2 2 2 2.0 O=C1N=C(O)NC1(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL16 53348 111 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 252 2 2 2 2.0 O=C1N=C(O)NC1(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1611 53348 111 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 252 2 2 2 2.0 O=C1N=C(O)NC1(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
1353 1911 93 None -489 83 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
3559 1911 93 None -489 83 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
86 1911 93 None -489 83 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
CHEMBL54 1911 93 None -489 83 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
DB00502 1911 93 None -489 83 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
5453 203619 102 None - 0 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 189 3 0 1 0.2 S=P(N1CC1)(N1CC1)N1CC1 10.1038/s41467-023-40064-9
CHEMBL671 203619 102 None - 0 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 189 3 0 1 0.2 S=P(N1CC1)(N1CC1)N1CC1 10.1038/s41467-023-40064-9
2435 3590 83 None -95 48 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
60149 3590 83 None -95 48 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
98 3590 83 None -95 48 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
CHEMBL12713 3590 83 None -95 48 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
DB06144 3590 83 None -95 48 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
65866 94264 73 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 611 12 1 8 6.5 COC(=O)C1=C(C)NC(C)=C(C(=O)OC(C)(C)CN(C)CCC(c2ccccc2)c2ccccc2)C1c1cccc([N+](=O)[O-])c1 10.1038/s41467-023-40064-9
CHEMBL250270 94264 73 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 611 12 1 8 6.5 COC(=O)C1=C(C)NC(C)=C(C(=O)OC(C)(C)CN(C)CCC(c2ccccc2)c2ccccc2)C1c1cccc([N+](=O)[O-])c1 10.1038/s41467-023-40064-9
4450 178228 69 None - 3 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 253 1 0 2 3.2 CN1CCOC(c2ccccc2)c2ccccc2C1 10.1038/s41467-023-40064-9
CHEMBL465026 178228 69 None - 3 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 253 1 0 2 3.2 CN1CCOC(c2ccccc2)c2ccccc2C1 10.1038/s41467-023-40064-9
3947 206395 53 None -7 16 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL87708 206395 53 None -7 16 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 10.1038/s41467-023-40064-9
2398 954 62 None -1 29 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2801 954 62 None -1 29 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
701 954 62 None -1 29 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL415 954 62 None -1 29 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB01242 954 62 None -1 29 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
191 403 98 None -56 29 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
201 403 98 None -56 29 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
2170 403 98 None -56 29 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
CHEMBL1113 403 98 None -56 29 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
DB00543 403 98 None -56 29 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
37 778 60 None - 17 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
460 778 60 None - 17 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
54746 778 60 None - 17 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
CHEMBL1201087 778 60 None - 17 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
DB00248 778 60 None - 17 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
5904 100392 40 None - 1 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 334 4 2 4 0.9 CC1(C)S[C@@H]2[C@H](NC(=O)Cc3ccccc3)C(=O)N2[C@H]1C(=O)O 10.1038/s41467-023-40064-9
CHEMBL1223 100392 40 None - 1 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 334 4 2 4 0.9 CC1(C)S[C@@H]2[C@H](NC(=O)Cc3ccccc3)C(=O)N2[C@H]1C(=O)O 10.1038/s41467-023-40064-9
CHEMBL29 100392 40 None - 1 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 334 4 2 4 0.9 CC1(C)S[C@@H]2[C@H](NC(=O)Cc3ccccc3)C(=O)N2[C@H]1C(=O)O 10.1038/s41467-023-40064-9
2286 3183 51 None -2 30 Human 8.2 pAC50 = 8.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
4927 3183 51 None -2 30 Human 8.2 pAC50 = 8.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
7282 3183 51 None -2 30 Human 8.2 pAC50 = 8.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
CHEMBL643 3183 51 None -2 30 Human 8.2 pAC50 = 8.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
DB01069 3183 51 None -2 30 Human 8.2 pAC50 = 8.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
103 4153 61 None -1 53 Human 8.2 pAC50 = 8.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2875 4153 61 None -1 53 Human 8.2 pAC50 = 8.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
5736 4153 61 None -1 53 Human 8.2 pAC50 = 8.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL285802 4153 61 None -1 53 Human 8.2 pAC50 = 8.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB09225 4153 61 None -1 53 Human 8.2 pAC50 = 8.2 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
4011 82408 49 None 6 24 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 10.1038/s41467-023-40064-9
CHEMBL21731 82408 49 None 6 24 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 10.1038/s41467-023-40064-9
16363 596 53 None - 7 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
312 596 53 None - 7 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
9215 596 53 None - 7 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL297302 596 53 None - 7 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB12867 596 53 None - 7 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
4418 34222 85 None - 6 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1038/s41467-023-40064-9
CHEMBL142635 34222 85 None - 6 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1038/s41467-023-40064-9
4020 205150 39 None - 1 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 284 1 1 3 2.6 OC1(c2ccc(Cl)cc2)c2ccccc2C2=NCCN21 10.1038/s41467-023-40064-9
CHEMBL781 205150 39 None - 1 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 284 1 1 3 2.6 OC1(c2ccc(Cl)cc2)c2ccccc2C2=NCCN21 10.1038/s41467-023-40064-9
23480 124090 23 None - 0 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 281 5 1 1 5.0 CC(CC(c1ccccc1)c1ccccc1)NC(C)(C)C 10.1038/s41467-023-40064-9
CHEMBL363295 124090 23 None - 0 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 281 5 1 1 5.0 CC(CC(c1ccccc1)c1ccccc1)NC(C)(C)C 10.1038/s41467-023-40064-9
1222 881 0 None -1 2 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
2678 881 0 None -1 2 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
581 881 0 None -1 2 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1000 881 0 None -1 2 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
DB00341 881 0 None -1 2 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
9801 91585 35 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 329 8 1 1 5.4 CC(Cc1ccccc1)NCCC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL24072 91585 35 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 329 8 1 1 5.4 CC(Cc1ccccc1)NCCC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
5411 204033 89 None - 2 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 264 8 1 4 2.6 CCCCNc1ccc(C(=O)OCCN(C)C)cc1 10.1038/s41467-023-40064-9
CHEMBL698 204033 89 None - 2 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 264 8 1 4 2.6 CCCCNc1ccc(C(=O)OCCN(C)C)cc1 10.1038/s41467-023-40064-9
135398745 2914 112 None 1 65 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
47 2914 112 None 1 65 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
CHEMBL715 2914 112 None 1 65 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
DB00334 2914 112 None 1 65 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
2762 3863 31 None -9 2 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 10.1038/s41467-023-40064-9
5587 3863 31 None -9 2 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 10.1038/s41467-023-40064-9
7318 3863 31 None -9 2 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 10.1038/s41467-023-40064-9
CHEMBL1241 3863 31 None -9 2 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 10.1038/s41467-023-40064-9
DB00792 3863 31 None -9 2 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 10.1038/s41467-023-40064-9
2247 505 81 None -4 42 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
249 505 81 None -4 42 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
2603 505 81 None -4 42 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
CHEMBL296419 505 81 None -4 42 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
DB00637 505 81 None -4 42 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
9417 133512 54 None - 0 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 363 6 1 4 3.3 OCCN1CCN(CCCN2c3ccccc3C=Cc3ccccc32)CC1 10.1038/s41467-023-40064-9
CHEMBL1524185 133512 54 None - 0 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 363 6 1 4 3.3 OCCN1CCN(CCCN2c3ccccc3C=Cc3ccccc32)CC1 10.1038/s41467-023-40064-9
CHEMBL370753 133512 54 None - 0 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 363 6 1 4 3.3 OCCN1CCN(CCCN2c3ccccc3C=Cc3ccccc32)CC1 10.1038/s41467-023-40064-9
11291 98796 25 None - 2 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 261 1 0 1 3.9 CN1CCC2=C(C1)C(c1ccccc1)c1ccccc12 10.1038/s41467-023-40064-9
CHEMBL278398 98796 25 None - 2 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 261 1 0 1 3.9 CN1CCC2=C(C1)C(c1ccccc1)c1ccccc12 10.1038/s41467-023-40064-9
2712 916 34 None -5 4 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl 10.1038/s41467-023-40064-9
3370 916 34 None -5 4 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl 10.1038/s41467-023-40064-9
594 916 34 None -5 4 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl 10.1038/s41467-023-40064-9
CHEMBL451 916 34 None -5 4 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl 10.1038/s41467-023-40064-9
DB00475 916 34 None -5 4 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl 10.1038/s41467-023-40064-9
1193 1656 108 None - 0 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 281 3 2 2 4.1 OC(=O)c1ccccc1Nc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
2447 1656 108 None - 0 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 281 3 2 2 4.1 OC(=O)c1ccccc1Nc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
3371 1656 108 None - 0 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 281 3 2 2 4.1 OC(=O)c1ccccc1Nc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL23588 1656 108 None - 0 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 281 3 2 2 4.1 OC(=O)c1ccccc1Nc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
DB02266 1656 108 None - 0 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 281 3 2 2 4.1 OC(=O)c1ccccc1Nc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
135564886 14493 5 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
135673376 14493 5 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
137157436 14493 5 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
145948239 14493 5 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
71587099 14493 5 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
CHEMBL1201304 14493 5 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
1222 1664 49 None -17 33 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
3396 1664 49 None -17 33 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
85 1664 49 None -17 33 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL46516 1664 49 None -17 33 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
DB04842 1664 49 None -17 33 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
3180 14473 41 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 289 8 0 3 3.9 CCCCOc1ccc(C(=O)CCN2CCCCC2)cc1 10.1038/s41467-023-40064-9
CHEMBL1201217 14473 41 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 289 8 0 3 3.9 CCCCOc1ccc(C(=O)CCN2CCCCC2)cc1 10.1038/s41467-023-40064-9
2794 19380 85 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 472 4 1 4 7.5 CC(C)/N=c1\cc2n(-c3ccc(Cl)cc3)c3ccccc3nc-2cc1Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL1292 19380 85 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 472 4 1 4 7.5 CC(C)/N=c1\cc2n(-c3ccc(Cl)cc3)c3ccccc3nc-2cc1Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5284616 161627 55 None - 0 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 914 6 3 13 6.2 CO[C@H]1C[C@@H]2CC[C@@H](C)[C@@](O)(O2)C(=O)C(=O)N2CCCC[C@H]2C(=O)O[C@H]([C@H](C)C[C@@H]2CC[C@@H](O)[C@H](OC)C2)CC(=O)[C@H](C)/C=C(\C)[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)/C=C/C=C/C=C/1C 10.1038/s41467-023-40064-9
CHEMBL413 161627 55 None - 0 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 914 6 3 13 6.2 CO[C@H]1C[C@@H]2CC[C@@H](C)[C@@](O)(O2)C(=O)C(=O)N2CCCC[C@H]2C(=O)O[C@H]([C@H](C)C[C@@H]2CC[C@@H](O)[C@H](OC)C2)CC(=O)[C@H](C)/C=C(\C)[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)/C=C/C=C/C=C/1C 10.1038/s41467-023-40064-9
2351 4300 49 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
CHEMBL1008 4300 49 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
CHEMBL1257078 4300 49 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
213046 2385 59 None - 9 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
4168 2385 59 None - 9 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
7461 2385 59 None - 9 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
CHEMBL1237021 2385 59 None - 9 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
DB08815 2385 59 None - 9 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
135398735 136968 32 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 822 4 6 15 4.3 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
136262914 136968 32 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 822 4 6 15 4.3 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
CHEMBL374478 136968 32 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 822 4 6 15 4.3 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
202 1508 77 None -1 30 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
60835 1508 77 None -1 30 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
972 1508 77 None -1 30 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL1175 1508 77 None -1 30 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
DB00476 1508 77 None -1 30 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
2335 11848 22 None - 12 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
8478 11848 22 None - 12 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL1182210 11848 22 None - 12 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL221753 11848 22 None - 12 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
3547 141373 71 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 291 2 1 4 1.2 O=S(=O)(c1cccc2cnccc12)N1CCCNCC1 10.1038/s41467-023-40064-9
CHEMBL38380 141373 71 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 291 2 1 4 1.2 O=S(=O)(c1cccc2cnccc12)N1CCCNCC1 10.1038/s41467-023-40064-9
CHEMBL541388 141373 71 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 291 2 1 4 1.2 O=S(=O)(c1cccc2cnccc12)N1CCCNCC1 10.1038/s41467-023-40064-9
2179 167518 76 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 393 5 2 5 4.5 COc1cc(NS(C)(=O)=O)ccc1Nc1c2ccccc2nc2ccccc12 10.1038/s41467-023-40064-9
CHEMBL1256655 167518 76 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 393 5 2 5 4.5 COc1cc(NS(C)(=O)=O)ccc1Nc1c2ccccc2nc2ccccc12 10.1038/s41467-023-40064-9
CHEMBL43 167518 76 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 393 5 2 5 4.5 COc1cc(NS(C)(=O)=O)ccc1Nc1c2ccccc2nc2ccccc12 10.1038/s41467-023-40064-9
100 3805 58 None -7 55 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
2637 3805 58 None -7 55 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
5452 3805 58 None -7 55 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
CHEMBL479 3805 58 None -7 55 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
DB00679 3805 58 None -7 55 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
2448 99323 70 None -4 18 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 10.1038/s41467-023-40064-9
CHEMBL28218 99323 70 None -4 18 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 10.1038/s41467-023-40064-9
4642 41986 28 None - 0 Human 6.0 pAC50 = 6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 344 5 1 5 2.7 CN1CCCN=C1COC(=O)C(O)(c1ccccc1)C1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL1495 41986 28 None - 0 Human 6.0 pAC50 = 6 Binding
Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration
ChEMBL 344 5 1 5 2.7 CN1CCCN=C1COC(=O)C(O)(c1ccccc1)C1CCCCC1 10.1038/s41467-023-40064-9
135398737 958 93 None 2 89 Human 9.4 pEC50 = 9.4 Binding
Inverse agonist activity at human histamine H1 receptor by R-SAT assayInverse agonist activity at human histamine H1 receptor by R-SAT assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 958 93 None 2 89 Human 9.4 pEC50 = 9.4 Binding
Inverse agonist activity at human histamine H1 receptor by R-SAT assayInverse agonist activity at human histamine H1 receptor by R-SAT assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 958 93 None 2 89 Human 9.4 pEC50 = 9.4 Binding
Inverse agonist activity at human histamine H1 receptor by R-SAT assayInverse agonist activity at human histamine H1 receptor by R-SAT assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 958 93 None 2 89 Human 9.4 pEC50 = 9.4 Binding
Inverse agonist activity at human histamine H1 receptor by R-SAT assayInverse agonist activity at human histamine H1 receptor by R-SAT assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 958 93 None 2 89 Human 9.4 pEC50 = 9.4 Binding
Inverse agonist activity at human histamine H1 receptor by R-SAT assayInverse agonist activity at human histamine H1 receptor by R-SAT assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
11327353 165621 0 None - 0 Guinea pig 6.9 pEC50 = 6.9 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 410 11 2 3 4.9 c1ccc(C(CCc2nc(CCNCCc3ccncc3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
CHEMBL424336 165621 0 None - 0 Guinea pig 6.9 pEC50 = 6.9 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 410 11 2 3 4.9 c1ccc(C(CCc2nc(CCNCCc3ccncc3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
11201079 46218 0 None - 0 Guinea pig 6.9 pEC50 = 6.9 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 424 12 2 3 5.3 c1ccc(C(CCc2nc(CCNCCCc3cccnc3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
CHEMBL153474 46218 0 None - 0 Guinea pig 6.9 pEC50 = 6.9 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 424 12 2 3 5.3 c1ccc(C(CCc2nc(CCNCCCc3cccnc3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
11235688 119852 0 None - 1 Guinea pig 6.9 pEC50 = 6.9 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 427 13 3 3 5.1 c1ccc(C(CCc2nc(CCNCCCCc3c[nH]cn3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
CHEMBL348656 119852 0 None - 1 Guinea pig 6.9 pEC50 = 6.9 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 427 13 3 3 5.1 c1ccc(C(CCc2nc(CCNCCCCc3c[nH]cn3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
42625384 169773 0 None - 1 Human 4.9 pEC50 = 4.9 Binding
Agonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 209 4 3 2 -0.2 CC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL443896 169773 0 None - 1 Human 4.9 pEC50 = 4.9 Binding
Agonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 209 4 3 2 -0.2 CC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
1204 1932 119 None -501 24 Human 7.9 pEC50 = 7.9 Binding
Inhibition of human Histamine H1 receptor using [3H]pyrilamineInhibition of human Histamine H1 receptor using [3H]pyrilamine
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm020415q
1247 1932 119 None -501 24 Human 7.9 pEC50 = 7.9 Binding
Inhibition of human Histamine H1 receptor using [3H]pyrilamineInhibition of human Histamine H1 receptor using [3H]pyrilamine
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm020415q
1375 1932 119 None -501 24 Human 7.9 pEC50 = 7.9 Binding
Inhibition of human Histamine H1 receptor using [3H]pyrilamineInhibition of human Histamine H1 receptor using [3H]pyrilamine
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm020415q
774 1932 119 None -501 24 Human 7.9 pEC50 = 7.9 Binding
Inhibition of human Histamine H1 receptor using [3H]pyrilamineInhibition of human Histamine H1 receptor using [3H]pyrilamine
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm020415q
CHEMBL90 1932 119 None -501 24 Human 7.9 pEC50 = 7.9 Binding
Inhibition of human Histamine H1 receptor using [3H]pyrilamineInhibition of human Histamine H1 receptor using [3H]pyrilamine
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm020415q
DB05381 1932 119 None -501 24 Human 7.9 pEC50 = 7.9 Binding
Inhibition of human Histamine H1 receptor using [3H]pyrilamineInhibition of human Histamine H1 receptor using [3H]pyrilamine
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm020415q
11407994 46478 0 None - 0 Guinea pig 7.9 pEC50 = 7.9 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 438 13 2 3 5.7 c1ccc(C(CCc2nc(CCNCCCCc3cccnc3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
CHEMBL153736 46478 0 None - 0 Guinea pig 7.9 pEC50 = 7.9 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 438 13 2 3 5.7 c1ccc(C(CCc2nc(CCNCCCCc3cccnc3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
11269940 46531 1 None - 1 Guinea pig 7.9 pEC50 = 7.9 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 413 12 3 3 4.7 c1ccc(C(CCc2nc(CCNCCCc3c[nH]cn3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
CHEMBL153776 46531 1 None - 1 Guinea pig 7.9 pEC50 = 7.9 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 413 12 3 3 4.7 c1ccc(C(CCc2nc(CCNCCCc3c[nH]cn3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
10410901 119747 0 None 3 2 Guinea pig 7.9 pEC50 = 7.9 Binding
Effective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig AortaEffective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig Aorta
ChEMBL 438 13 2 3 5.7 c1ccc(C(CCc2nc(CCNCCCCc3ccccn3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
CHEMBL347796 119747 0 None 3 2 Guinea pig 7.9 pEC50 = 7.9 Binding
Effective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig AortaEffective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig Aorta
ChEMBL 438 13 2 3 5.7 c1ccc(C(CCc2nc(CCNCCCCc3ccccn3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
11166893 46214 0 None - 0 Guinea pig 7.8 pEC50 = 7.8 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 452 14 2 3 6.1 c1ccc(C(CCc2nc(CCNCCCCCc3ccccn3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
CHEMBL153468 46214 0 None - 0 Guinea pig 7.8 pEC50 = 7.8 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 452 14 2 3 6.1 c1ccc(C(CCc2nc(CCNCCCCCc3ccccn3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
10447834 1933 4 None 8 5 Guinea pig 6.8 pEC50 = 6.8 Binding
Effective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig AortaEffective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig Aorta
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm0309147
4026 1933 4 None 8 5 Guinea pig 6.8 pEC50 = 6.8 Binding
Effective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig AortaEffective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig Aorta
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm0309147
CHEMBL275507 1933 4 None 8 5 Guinea pig 6.8 pEC50 = 6.8 Binding
Effective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig AortaEffective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig Aorta
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm0309147
10403687 2511 3 None -7 5 Rat 6.8 pEC50 = 6.8 Binding
Effective concentration against histamine H1 receptor in rat aortaEffective concentration against histamine H1 receptor in rat aorta
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm0309147
1205 2511 3 None -7 5 Rat 6.8 pEC50 = 6.8 Binding
Effective concentration against histamine H1 receptor in rat aortaEffective concentration against histamine H1 receptor in rat aorta
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm0309147
CHEMBL275035 2511 3 None -7 5 Rat 6.8 pEC50 = 6.8 Binding
Effective concentration against histamine H1 receptor in rat aortaEffective concentration against histamine H1 receptor in rat aorta
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm0309147
1204 1932 119 None -46 24 Guinea pig 6.8 pEC50 = 6.8 Binding
Effective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig AortaEffective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig Aorta
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0309147
1247 1932 119 None -46 24 Guinea pig 6.8 pEC50 = 6.8 Binding
Effective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig AortaEffective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig Aorta
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0309147
1375 1932 119 None -46 24 Guinea pig 6.8 pEC50 = 6.8 Binding
Effective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig AortaEffective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig Aorta
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0309147
774 1932 119 None -46 24 Guinea pig 6.8 pEC50 = 6.8 Binding
Effective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig AortaEffective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig Aorta
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0309147
CHEMBL90 1932 119 None -46 24 Guinea pig 6.8 pEC50 = 6.8 Binding
Effective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig AortaEffective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig Aorta
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0309147
DB05381 1932 119 None -46 24 Guinea pig 6.8 pEC50 = 6.8 Binding
Effective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig AortaEffective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig Aorta
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0309147
42626110 179769 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 310 5 4 2 1.6 N/C(=N\C(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL474448 179769 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 310 5 4 2 1.6 N/C(=N\C(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1 10.1021/jm9000693
10447834 1933 4 None 8 5 Guinea pig 6.7 pEC50 = 6.7 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm0309147
4026 1933 4 None 8 5 Guinea pig 6.7 pEC50 = 6.7 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm0309147
CHEMBL275507 1933 4 None 8 5 Guinea pig 6.7 pEC50 = 6.7 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm0309147
1204 1932 119 None -501 24 Human 6.7 pEC50 = 6.7 Binding
Activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
1247 1932 119 None -501 24 Human 6.7 pEC50 = 6.7 Binding
Activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
1375 1932 119 None -501 24 Human 6.7 pEC50 = 6.7 Binding
Activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
774 1932 119 None -501 24 Human 6.7 pEC50 = 6.7 Binding
Activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
CHEMBL90 1932 119 None -501 24 Human 6.7 pEC50 = 6.7 Binding
Activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
DB05381 1932 119 None -501 24 Human 6.7 pEC50 = 6.7 Binding
Activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
1204 1932 119 None -501 24 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 or RGS9 assessed as increase in 32Pi level incubated for 20 mins by liquid scintillation counting in presence of [gamma32P]GTPAgonist activity at human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 or RGS9 assessed as increase in 32Pi level incubated for 20 mins by liquid scintillation counting in presence of [gamma32P]GTP
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
1247 1932 119 None -501 24 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 or RGS9 assessed as increase in 32Pi level incubated for 20 mins by liquid scintillation counting in presence of [gamma32P]GTPAgonist activity at human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 or RGS9 assessed as increase in 32Pi level incubated for 20 mins by liquid scintillation counting in presence of [gamma32P]GTP
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
1375 1932 119 None -501 24 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 or RGS9 assessed as increase in 32Pi level incubated for 20 mins by liquid scintillation counting in presence of [gamma32P]GTPAgonist activity at human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 or RGS9 assessed as increase in 32Pi level incubated for 20 mins by liquid scintillation counting in presence of [gamma32P]GTP
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
774 1932 119 None -501 24 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 or RGS9 assessed as increase in 32Pi level incubated for 20 mins by liquid scintillation counting in presence of [gamma32P]GTPAgonist activity at human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 or RGS9 assessed as increase in 32Pi level incubated for 20 mins by liquid scintillation counting in presence of [gamma32P]GTP
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
CHEMBL90 1932 119 None -501 24 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 or RGS9 assessed as increase in 32Pi level incubated for 20 mins by liquid scintillation counting in presence of [gamma32P]GTPAgonist activity at human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 or RGS9 assessed as increase in 32Pi level incubated for 20 mins by liquid scintillation counting in presence of [gamma32P]GTP
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
DB05381 1932 119 None -501 24 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 or RGS9 assessed as increase in 32Pi level incubated for 20 mins by liquid scintillation counting in presence of [gamma32P]GTPAgonist activity at human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 or RGS9 assessed as increase in 32Pi level incubated for 20 mins by liquid scintillation counting in presence of [gamma32P]GTP
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
1204 1932 119 None -501 24 Human 6.7 pEC50 = 6.7 Binding
Activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
1247 1932 119 None -501 24 Human 6.7 pEC50 = 6.7 Binding
Activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
1375 1932 119 None -501 24 Human 6.7 pEC50 = 6.7 Binding
Activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
774 1932 119 None -501 24 Human 6.7 pEC50 = 6.7 Binding
Activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
CHEMBL90 1932 119 None -501 24 Human 6.7 pEC50 = 6.7 Binding
Activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
DB05381 1932 119 None -501 24 Human 6.7 pEC50 = 6.7 Binding
Activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
1204 1932 119 None -501 24 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm9000693
1247 1932 119 None -501 24 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm9000693
1375 1932 119 None -501 24 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm9000693
774 1932 119 None -501 24 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm9000693
CHEMBL90 1932 119 None -501 24 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm9000693
DB05381 1932 119 None -501 24 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm9000693
1204 1932 119 None -501 24 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
1247 1932 119 None -501 24 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
1375 1932 119 None -501 24 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
774 1932 119 None -501 24 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
CHEMBL90 1932 119 None -501 24 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
DB05381 1932 119 None -501 24 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
1204 1932 119 None -46 24 Guinea pig 6.7 pEC50 = 6.7 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0309147
1247 1932 119 None -46 24 Guinea pig 6.7 pEC50 = 6.7 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0309147
1375 1932 119 None -46 24 Guinea pig 6.7 pEC50 = 6.7 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0309147
774 1932 119 None -46 24 Guinea pig 6.7 pEC50 = 6.7 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0309147
CHEMBL90 1932 119 None -46 24 Guinea pig 6.7 pEC50 = 6.7 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0309147
DB05381 1932 119 None -46 24 Guinea pig 6.7 pEC50 = 6.7 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0309147
1227 2489 43 None -2 12 Human 8.6 pEC50 = 8.6 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO-K1 cellsDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/np058114h
2331 2489 43 None -2 12 Human 8.6 pEC50 = 8.6 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO-K1 cellsDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/np058114h
3957 2489 43 None -2 12 Human 8.6 pEC50 = 8.6 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO-K1 cellsDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/np058114h
4992 2489 43 None -2 12 Human 8.6 pEC50 = 8.6 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO-K1 cellsDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/np058114h
CHEMBL511 2489 43 None -2 12 Human 8.6 pEC50 = 8.6 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO-K1 cellsDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/np058114h
DB06691 2489 43 None -2 12 Human 8.6 pEC50 = 8.6 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO-K1 cellsDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/np058114h
10364258 45769 0 None 2 2 Guinea pig 7.7 pEC50 = 7.7 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 410 11 2 3 4.9 c1ccc(C(CCc2nc(CCNCCc3ccccn3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
CHEMBL153067 45769 0 None 2 2 Guinea pig 7.7 pEC50 = 7.7 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 410 11 2 3 4.9 c1ccc(C(CCc2nc(CCNCCc3ccccn3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
11475781 46057 0 None - 0 Guinea pig 7.7 pEC50 = 7.7 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 424 12 2 3 5.3 c1ccc(C(CCc2nc(CCNCCCc3ccccn3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
CHEMBL153321 46057 0 None - 0 Guinea pig 7.7 pEC50 = 7.7 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 424 12 2 3 5.3 c1ccc(C(CCc2nc(CCNCCCc3ccccn3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
42625386 178353 0 None - 1 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 237 6 3 2 0.6 CCCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL465170 178353 0 None - 1 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 237 6 3 2 0.6 CCCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
11453438 45701 0 None - 0 Guinea pig 7.6 pEC50 = 7.6 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 438 13 2 3 5.7 c1ccc(C(CCc2nc(CCNCCCCc3ccncc3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
CHEMBL153010 45701 0 None - 0 Guinea pig 7.6 pEC50 = 7.6 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 438 13 2 3 5.7 c1ccc(C(CCc2nc(CCNCCCCc3ccncc3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
10410901 119747 0 None -3 2 Rat 6.6 pEC50 = 6.6 Binding
Effective concentration against histamine H1 receptor in rat aortaEffective concentration against histamine H1 receptor in rat aorta
ChEMBL 438 13 2 3 5.7 c1ccc(C(CCc2nc(CCNCCCCc3ccccn3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
CHEMBL347796 119747 0 None -3 2 Rat 6.6 pEC50 = 6.6 Binding
Effective concentration against histamine H1 receptor in rat aortaEffective concentration against histamine H1 receptor in rat aorta
ChEMBL 438 13 2 3 5.7 c1ccc(C(CCc2nc(CCNCCCCc3ccccn3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
42625304 179100 0 None - 1 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 237 5 3 2 0.4 CC(C)C(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL471724 179100 0 None - 1 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 237 5 3 2 0.4 CC(C)C(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
11775345 42176 0 None - 0 Guinea pig 7.6 pEC50 = 7.6 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 452 14 2 3 6.1 c1ccc(C(CCc2nc(CCNCCCCCc3cccnc3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
CHEMBL149684 42176 0 None - 0 Guinea pig 7.6 pEC50 = 7.6 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 452 14 2 3 6.1 c1ccc(C(CCc2nc(CCNCCCCCc3cccnc3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
11339274 119624 0 None - 0 Guinea pig 6.6 pEC50 = 6.6 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 424 12 2 3 5.3 c1ccc(C(CCc2nc(CCNCCCc3ccncc3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
CHEMBL346620 119624 0 None - 0 Guinea pig 6.6 pEC50 = 6.6 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 424 12 2 3 5.3 c1ccc(C(CCc2nc(CCNCCCc3ccncc3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
11741669 96753 0 None -2 2 Rat 6.5 pEC50 = 6.5 Binding
Effective concentration against histamine H1 receptor in rat aortaEffective concentration against histamine H1 receptor in rat aorta
ChEMBL 399 11 3 3 4.3 c1ccc(C(CCc2nc(CCNCCc3cnc[nH]3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
CHEMBL264491 96753 0 None -2 2 Rat 6.5 pEC50 = 6.5 Binding
Effective concentration against histamine H1 receptor in rat aortaEffective concentration against histamine H1 receptor in rat aorta
ChEMBL 399 11 3 3 4.3 c1ccc(C(CCc2nc(CCNCCc3cnc[nH]3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
42625303 180766 0 None - 1 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 223 5 3 2 0.2 CCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL475621 180766 0 None - 1 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 223 5 3 2 0.2 CCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
10403687 2511 3 None 7 5 Guinea pig 7.4 pEC50 = 7.4 Binding
Effective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig AortaEffective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig Aorta
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm0309147
1205 2511 3 None 7 5 Guinea pig 7.4 pEC50 = 7.4 Binding
Effective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig AortaEffective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig Aorta
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm0309147
CHEMBL275035 2511 3 None 7 5 Guinea pig 7.4 pEC50 = 7.4 Binding
Effective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig AortaEffective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig Aorta
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm0309147
1204 1932 119 None -309 24 Rat 5.4 pEC50 = 5.4 Binding
Effective concentration against histamine H1 receptor in rat aortaEffective concentration against histamine H1 receptor in rat aorta
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0309147
1247 1932 119 None -309 24 Rat 5.4 pEC50 = 5.4 Binding
Effective concentration against histamine H1 receptor in rat aortaEffective concentration against histamine H1 receptor in rat aorta
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0309147
1375 1932 119 None -309 24 Rat 5.4 pEC50 = 5.4 Binding
Effective concentration against histamine H1 receptor in rat aortaEffective concentration against histamine H1 receptor in rat aorta
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0309147
774 1932 119 None -309 24 Rat 5.4 pEC50 = 5.4 Binding
Effective concentration against histamine H1 receptor in rat aortaEffective concentration against histamine H1 receptor in rat aorta
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0309147
CHEMBL90 1932 119 None -309 24 Rat 5.4 pEC50 = 5.4 Binding
Effective concentration against histamine H1 receptor in rat aortaEffective concentration against histamine H1 receptor in rat aorta
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0309147
DB05381 1932 119 None -309 24 Rat 5.4 pEC50 = 5.4 Binding
Effective concentration against histamine H1 receptor in rat aortaEffective concentration against histamine H1 receptor in rat aorta
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0309147
11741669 96753 0 None 2 2 Guinea pig 8.3 pEC50 = 8.3 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 399 11 3 3 4.3 c1ccc(C(CCc2nc(CCNCCc3cnc[nH]3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
CHEMBL264491 96753 0 None 2 2 Guinea pig 8.3 pEC50 = 8.3 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 399 11 3 3 4.3 c1ccc(C(CCc2nc(CCNCCc3cnc[nH]3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
10364258 45769 0 None -2 2 Rat 6.3 pEC50 = 6.3 Binding
Effective concentration against histamine H1 receptor in rat aortaEffective concentration against histamine H1 receptor in rat aorta
ChEMBL 410 11 2 3 4.9 c1ccc(C(CCc2nc(CCNCCc3ccccn3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
CHEMBL153067 45769 0 None -2 2 Rat 6.3 pEC50 = 6.3 Binding
Effective concentration against histamine H1 receptor in rat aortaEffective concentration against histamine H1 receptor in rat aorta
ChEMBL 410 11 2 3 4.9 c1ccc(C(CCc2nc(CCNCCc3ccccn3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
10403687 2511 3 None 7 5 Guinea pig 7.2 pEC50 = 7.2 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm0309147
1205 2511 3 None 7 5 Guinea pig 7.2 pEC50 = 7.2 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm0309147
CHEMBL275035 2511 3 None 7 5 Guinea pig 7.2 pEC50 = 7.2 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm0309147
10410901 119747 0 None 3 2 Guinea pig 8.2 pEC50 = 8.2 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 438 13 2 3 5.7 c1ccc(C(CCc2nc(CCNCCCCc3ccccn3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
CHEMBL347796 119747 0 None 3 2 Guinea pig 8.2 pEC50 = 8.2 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 438 13 2 3 5.7 c1ccc(C(CCc2nc(CCNCCCCc3ccccn3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
46887041 8760 1 None - 0 Human 5.2 pEC50 = 5.2 Binding
Activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay
ChEMBL 313 7 4 3 2.2 C[C@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccc1 10.1016/j.bmcl.2010.03.082
CHEMBL1096428 8760 1 None - 0 Human 5.2 pEC50 = 5.2 Binding
Activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay
ChEMBL 313 7 4 3 2.2 C[C@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccc1 10.1016/j.bmcl.2010.03.082
46887043 8763 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay
ChEMBL 319 7 4 3 2.6 C[C@@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1 10.1016/j.bmcl.2010.03.082
CHEMBL1096431 8763 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay
ChEMBL 319 7 4 3 2.6 C[C@@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1 10.1016/j.bmcl.2010.03.082
11269875 121004 0 None - 1 Guinea pig 7.1 pEC50 = 7.1 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 410 11 2 3 4.9 c1ccc(C(CCc2nc(CCNCCc3cccnc3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
CHEMBL356449 121004 0 None - 1 Guinea pig 7.1 pEC50 = 7.1 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 410 11 2 3 4.9 c1ccc(C(CCc2nc(CCNCCc3cccnc3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
10364258 45769 0 None 2 2 Guinea pig 7.1 pEC50 = 7.1 Binding
Effective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig AortaEffective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig Aorta
ChEMBL 410 11 2 3 4.9 c1ccc(C(CCc2nc(CCNCCc3ccccn3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
CHEMBL153067 45769 0 None 2 2 Guinea pig 7.1 pEC50 = 7.1 Binding
Effective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig AortaEffective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig Aorta
ChEMBL 410 11 2 3 4.9 c1ccc(C(CCc2nc(CCNCCc3ccccn3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
11269875 121004 0 None - 1 Guinea pig 7.1 pEC50 = 7.1 Binding
Effective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig AortaEffective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig Aorta
ChEMBL 410 11 2 3 4.9 c1ccc(C(CCc2nc(CCNCCc3cccnc3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
CHEMBL356449 121004 0 None - 1 Guinea pig 7.1 pEC50 = 7.1 Binding
Effective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig AortaEffective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig Aorta
ChEMBL 410 11 2 3 4.9 c1ccc(C(CCc2nc(CCNCCc3cccnc3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
46830167 8761 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay
ChEMBL 313 7 4 3 2.2 C[C@@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccc1 10.1016/j.bmcl.2010.03.082
CHEMBL1096429 8761 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay
ChEMBL 313 7 4 3 2.2 C[C@@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccc1 10.1016/j.bmcl.2010.03.082
10447834 1933 4 None -8 5 Rat 6.1 pEC50 = 6.1 Binding
Effective concentration against histamine H1 receptor in rat aortaEffective concentration against histamine H1 receptor in rat aorta
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm0309147
4026 1933 4 None -8 5 Rat 6.1 pEC50 = 6.1 Binding
Effective concentration against histamine H1 receptor in rat aortaEffective concentration against histamine H1 receptor in rat aorta
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm0309147
CHEMBL275507 1933 4 None -8 5 Rat 6.1 pEC50 = 6.1 Binding
Effective concentration against histamine H1 receptor in rat aortaEffective concentration against histamine H1 receptor in rat aorta
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm0309147
10374457 28895 2 None - 2 Human 6.1 pEC50 = 6.1 Binding
Inhibition of human Histamine H1 receptor using [3H]pyrilamineInhibition of human Histamine H1 receptor using [3H]pyrilamine
ChEMBL 123 1 2 2 0.2 N[C@H]1C[C@@H]1c1c[nH]cn1 10.1021/jm020415q
CHEMBL13795 28895 2 None - 2 Human 6.1 pEC50 = 6.1 Binding
Inhibition of human Histamine H1 receptor using [3H]pyrilamineInhibition of human Histamine H1 receptor using [3H]pyrilamine
ChEMBL 123 1 2 2 0.2 N[C@H]1C[C@@H]1c1c[nH]cn1 10.1021/jm020415q
46887042 8762 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay
ChEMBL 319 7 4 3 2.6 C[C@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1 10.1016/j.bmcl.2010.03.082
CHEMBL1096430 8762 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay
ChEMBL 319 7 4 3 2.6 C[C@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1 10.1016/j.bmcl.2010.03.082
11741669 96753 0 None 2 2 Guinea pig 8.0 pEC50 = 8.0 Binding
Effective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig AortaEffective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig Aorta
ChEMBL 399 11 3 3 4.3 c1ccc(C(CCc2nc(CCNCCc3cnc[nH]3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
CHEMBL264491 96753 0 None 2 2 Guinea pig 8.0 pEC50 = 8.0 Binding
Effective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig AortaEffective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig Aorta
ChEMBL 399 11 3 3 4.3 c1ccc(C(CCc2nc(CCNCCc3cnc[nH]3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
11178495 168668 0 None - 0 Guinea pig 7.0 pEC50 = 7.0 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 452 14 2 3 6.1 c1ccc(C(CCc2nc(CCNCCCCCc3ccncc3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
CHEMBL436415 168668 0 None - 0 Guinea pig 7.0 pEC50 = 7.0 Binding
Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum
ChEMBL 452 14 2 3 6.1 c1ccc(C(CCc2nc(CCNCCCCCc3ccncc3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
1227 2489 43 None -2 12 Human 10.9 pIC50 = 10.9 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in HEK293 cellsDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in HEK293 cells
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmc.2016.03.006
2331 2489 43 None -2 12 Human 10.9 pIC50 = 10.9 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in HEK293 cellsDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in HEK293 cells
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmc.2016.03.006
3957 2489 43 None -2 12 Human 10.9 pIC50 = 10.9 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in HEK293 cellsDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in HEK293 cells
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmc.2016.03.006
4992 2489 43 None -2 12 Human 10.9 pIC50 = 10.9 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in HEK293 cellsDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in HEK293 cells
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmc.2016.03.006
CHEMBL511 2489 43 None -2 12 Human 10.9 pIC50 = 10.9 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in HEK293 cellsDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in HEK293 cells
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmc.2016.03.006
DB06691 2489 43 None -2 12 Human 10.9 pIC50 = 10.9 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in HEK293 cellsDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in HEK293 cells
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmc.2016.03.006
180 401 56 None -11 40 Rat 10.7 pIC50 = 10.7 Binding
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1021/jm9910369
200 401 56 None -11 40 Rat 10.7 pIC50 = 10.7 Binding
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1021/jm9910369
2160 401 56 None -11 40 Rat 10.7 pIC50 = 10.7 Binding
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1021/jm9910369
CHEMBL629 401 56 None -11 40 Rat 10.7 pIC50 = 10.7 Binding
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1021/jm9910369
DB00321 401 56 None -11 40 Rat 10.7 pIC50 = 10.7 Binding
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1021/jm9910369
1971 2866 38 None -9 30 Rat 10.3 pIC50 = 10.3 Binding
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1021/jm9910369
2404 2866 38 None -9 30 Rat 10.3 pIC50 = 10.3 Binding
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1021/jm9910369
4543 2866 38 None -9 30 Rat 10.3 pIC50 = 10.3 Binding
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1021/jm9910369
CHEMBL445 2866 38 None -9 30 Rat 10.3 pIC50 = 10.3 Binding
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1021/jm9910369
DB00540 2866 38 None -9 30 Rat 10.3 pIC50 = 10.3 Binding
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1021/jm9910369
1427 2013 54 None -1 27 Rat 10.2 pIC50 = 10.2 Binding
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1021/jm9910369
357 2013 54 None -1 27 Rat 10.2 pIC50 = 10.2 Binding
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1021/jm9910369
3696 2013 54 None -1 27 Rat 10.2 pIC50 = 10.2 Binding
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1021/jm9910369
CHEMBL11 2013 54 None -1 27 Rat 10.2 pIC50 = 10.2 Binding
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1021/jm9910369
DB00458 2013 54 None -1 27 Rat 10.2 pIC50 = 10.2 Binding
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1021/jm9910369
76316323 85629 0 None - 0 Guinea pig 10.2 pIC50 = 10.2 Binding
Inhibition of H1 receptor in Cavia porcellus (guinea pig) ileum assessed as inhibition of histamine-induced contractionInhibition of H1 receptor in Cavia porcellus (guinea pig) ileum assessed as inhibition of histamine-induced contraction
ChEMBL 314 2 1 6 1.6 NC(=O)c1c(N2CCCC2)nc2sc3ccccc3n2c1=O 10.1007/s00044-012-0100-4
CHEMBL2283398 85629 0 None - 0 Guinea pig 10.2 pIC50 = 10.2 Binding
Inhibition of H1 receptor in Cavia porcellus (guinea pig) ileum assessed as inhibition of histamine-induced contractionInhibition of H1 receptor in Cavia porcellus (guinea pig) ileum assessed as inhibition of histamine-induced contraction
ChEMBL 314 2 1 6 1.6 NC(=O)c1c(N2CCCC2)nc2sc3ccccc3n2c1=O 10.1007/s00044-012-0100-4
2398 954 62 None - 29 Rat 9.7 pIC50 = 9.7 Binding
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1021/jm9910369
2801 954 62 None - 29 Rat 9.7 pIC50 = 9.7 Binding
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1021/jm9910369
701 954 62 None - 29 Rat 9.7 pIC50 = 9.7 Binding
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1021/jm9910369
CHEMBL415 954 62 None - 29 Rat 9.7 pIC50 = 9.7 Binding
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1021/jm9910369
DB01242 954 62 None - 29 Rat 9.7 pIC50 = 9.7 Binding
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1021/jm9910369
13726621 95265 0 None - 0 Guinea pig 9.6 pIC50 = 9.6 Binding
Inhibition of [3H]mepyramine binding to the histamine receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the histamine receptor in guinea pig cortex
ChEMBL 311 3 0 4 2.2 CN1C[C@@H](CCN2CCC2)Oc2ncc(Cl)cc2C1=S 10.1021/jm00108a012
CHEMBL25626 95265 0 None - 0 Guinea pig 9.6 pIC50 = 9.6 Binding
Inhibition of [3H]mepyramine binding to the histamine receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the histamine receptor in guinea pig cortex
ChEMBL 311 3 0 4 2.2 CN1C[C@@H](CCN2CCC2)Oc2ncc(Cl)cc2C1=S 10.1021/jm00108a012
26987 949 33 None 16 21 Human 9.4 pIC50 = 9.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
6063 949 33 None 16 21 Human 9.4 pIC50 = 9.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
671 949 33 None 16 21 Human 9.4 pIC50 = 9.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
CHEMBL1626 949 33 None 16 21 Human 9.4 pIC50 = 9.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
DB00283 949 33 None 16 21 Human 9.4 pIC50 = 9.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
3158 56267 27 None 40 20 Human 9.2 pIC50 = 9.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
CHEMBL1628227 56267 27 None 40 20 Human 9.2 pIC50 = 9.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
2995 204405 53 None -42 23 Rat 9.1 pIC50 = 9.1 Binding
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1021/jm9910369
CHEMBL1696 204405 53 None -42 23 Rat 9.1 pIC50 = 9.1 Binding
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1021/jm9910369
CHEMBL72 204405 53 None -42 23 Rat 9.1 pIC50 = 9.1 Binding
Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1021/jm9910369
1227 2489 43 None -2 12 Human 9.1 pIC50 = 9.1 Binding
Binding affinity to human histamine H1 receptor by radioligand displacement assayBinding affinity to human histamine H1 receptor by radioligand displacement assay
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmc.2013.03.016
2331 2489 43 None -2 12 Human 9.1 pIC50 = 9.1 Binding
Binding affinity to human histamine H1 receptor by radioligand displacement assayBinding affinity to human histamine H1 receptor by radioligand displacement assay
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmc.2013.03.016
3957 2489 43 None -2 12 Human 9.1 pIC50 = 9.1 Binding
Binding affinity to human histamine H1 receptor by radioligand displacement assayBinding affinity to human histamine H1 receptor by radioligand displacement assay
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmc.2013.03.016
4992 2489 43 None -2 12 Human 9.1 pIC50 = 9.1 Binding
Binding affinity to human histamine H1 receptor by radioligand displacement assayBinding affinity to human histamine H1 receptor by radioligand displacement assay
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmc.2013.03.016
CHEMBL511 2489 43 None -2 12 Human 9.1 pIC50 = 9.1 Binding
Binding affinity to human histamine H1 receptor by radioligand displacement assayBinding affinity to human histamine H1 receptor by radioligand displacement assay
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmc.2013.03.016
DB06691 2489 43 None -2 12 Human 9.1 pIC50 = 9.1 Binding
Binding affinity to human histamine H1 receptor by radioligand displacement assayBinding affinity to human histamine H1 receptor by radioligand displacement assay
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmc.2013.03.016
1224 1432 83 None 1 13 Guinea pig 9.0 pIC50 = 9 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1021/jm00173a011
3100 1432 83 None 1 13 Guinea pig 9.0 pIC50 = 9 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1021/jm00173a011
8980 1432 83 None 1 13 Guinea pig 9.0 pIC50 = 9 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1021/jm00173a011
916 1432 83 None 1 13 Guinea pig 9.0 pIC50 = 9 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1021/jm00173a011
CHEMBL657 1432 83 None 1 13 Guinea pig 9.0 pIC50 = 9 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1021/jm00173a011
DB01075 1432 83 None 1 13 Guinea pig 9.0 pIC50 = 9 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1021/jm00173a011
1530 2182 50 None -5 21 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1016/j.bmc.2011.03.003
3827 2182 50 None -5 21 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1016/j.bmc.2011.03.003
7206 2182 50 None -5 21 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1016/j.bmc.2011.03.003
CHEMBL534 2182 50 None -5 21 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1016/j.bmc.2011.03.003
DB00920 2182 50 None -5 21 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1016/j.bmc.2011.03.003
1530 2182 50 None -5 21 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1016/j.bmcl.2009.03.124
3827 2182 50 None -5 21 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1016/j.bmcl.2009.03.124
7206 2182 50 None -5 21 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1016/j.bmcl.2009.03.124
CHEMBL534 2182 50 None -5 21 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1016/j.bmcl.2009.03.124
DB00920 2182 50 None -5 21 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1016/j.bmcl.2009.03.124
2600 3779 74 None 1 13 Human 9.0 pIC50 = 9 Binding
Inhibition of histamine H1 receptor (unknown origin)Inhibition of histamine H1 receptor (unknown origin)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1021/jm501535r
2608 3779 74 None 1 13 Human 9.0 pIC50 = 9 Binding
Inhibition of histamine H1 receptor (unknown origin)Inhibition of histamine H1 receptor (unknown origin)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1021/jm501535r
5405 3779 74 None 1 13 Human 9.0 pIC50 = 9 Binding
Inhibition of histamine H1 receptor (unknown origin)Inhibition of histamine H1 receptor (unknown origin)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1021/jm501535r
CHEMBL17157 3779 74 None 1 13 Human 9.0 pIC50 = 9 Binding
Inhibition of histamine H1 receptor (unknown origin)Inhibition of histamine H1 receptor (unknown origin)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1021/jm501535r
DB00342 3779 74 None 1 13 Human 9.0 pIC50 = 9 Binding
Inhibition of histamine H1 receptor (unknown origin)Inhibition of histamine H1 receptor (unknown origin)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1021/jm501535r
137125256 123051 0 None - 0 Human 9.0 pIC50 = 9 Binding
Inhibition of recombinant human histamine H1 receptorInhibition of recombinant human histamine H1 receptor
ChEMBL 328 0 1 4 3.3 CN1CCN(C2=Nc3cc(F)ccc3Nc3ccc(F)cc32)CC1 10.1021/acsmedchemlett.5b00102
CHEMBL3609328 123051 0 None - 0 Human 9.0 pIC50 = 9 Binding
Inhibition of recombinant human histamine H1 receptorInhibition of recombinant human histamine H1 receptor
ChEMBL 328 0 1 4 3.3 CN1CCN(C2=Nc3cc(F)ccc3Nc3ccc(F)cc32)CC1 10.1021/acsmedchemlett.5b00102
11976 920 59 None - 24 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1021/jm300671m
667467 920 59 None - 24 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1021/jm300671m
CHEMBL908 920 59 None - 24 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1021/jm300671m
DB01239 920 59 None - 24 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1021/jm300671m
1530 2182 50 None -5 21 Human 8.9 pIC50 = 8.9 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
3827 2182 50 None -5 21 Human 8.9 pIC50 = 8.9 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
7206 2182 50 None -5 21 Human 8.9 pIC50 = 8.9 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
CHEMBL534 2182 50 None -5 21 Human 8.9 pIC50 = 8.9 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
DB00920 2182 50 None -5 21 Human 8.9 pIC50 = 8.9 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
44318581 205916 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.
ChEMBL 312 2 0 3 3.5 CN(C)CC1CC2c3ccccc3Cc3cc(F)ccc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL84081 205916 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.
ChEMBL 312 2 0 3 3.5 CN(C)CC1CC2c3ccccc3Cc3cc(F)ccc3N2O1 10.1016/s0960-894x(01)00721-1
1227 2489 43 None -2 12 Human 8.9 pIC50 = 8.9 Binding
Percent inhibition against Histamine H1 receptor at 1 uMPercent inhibition against Histamine H1 receptor at 1 uM
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm058018d
2331 2489 43 None -2 12 Human 8.9 pIC50 = 8.9 Binding
Percent inhibition against Histamine H1 receptor at 1 uMPercent inhibition against Histamine H1 receptor at 1 uM
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm058018d
3957 2489 43 None -2 12 Human 8.9 pIC50 = 8.9 Binding
Percent inhibition against Histamine H1 receptor at 1 uMPercent inhibition against Histamine H1 receptor at 1 uM
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm058018d
4992 2489 43 None -2 12 Human 8.9 pIC50 = 8.9 Binding
Percent inhibition against Histamine H1 receptor at 1 uMPercent inhibition against Histamine H1 receptor at 1 uM
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm058018d
CHEMBL511 2489 43 None -2 12 Human 8.9 pIC50 = 8.9 Binding
Percent inhibition against Histamine H1 receptor at 1 uMPercent inhibition against Histamine H1 receptor at 1 uM
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm058018d
DB06691 2489 43 None -2 12 Human 8.9 pIC50 = 8.9 Binding
Percent inhibition against Histamine H1 receptor at 1 uMPercent inhibition against Histamine H1 receptor at 1 uM
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm058018d
1227 2489 43 None -2 12 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]pyrilamine from human recombinant H1 receptor expressed in HEK293 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human recombinant H1 receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmc.2016.11.014
2331 2489 43 None -2 12 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]pyrilamine from human recombinant H1 receptor expressed in HEK293 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human recombinant H1 receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmc.2016.11.014
3957 2489 43 None -2 12 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]pyrilamine from human recombinant H1 receptor expressed in HEK293 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human recombinant H1 receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmc.2016.11.014
4992 2489 43 None -2 12 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]pyrilamine from human recombinant H1 receptor expressed in HEK293 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human recombinant H1 receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmc.2016.11.014
CHEMBL511 2489 43 None -2 12 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]pyrilamine from human recombinant H1 receptor expressed in HEK293 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human recombinant H1 receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmc.2016.11.014
DB06691 2489 43 None -2 12 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]pyrilamine from human recombinant H1 receptor expressed in HEK293 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human recombinant H1 receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmc.2016.11.014
1227 2489 43 None -2 12 Human 8.8 pIC50 = 8.8 Binding
Binding affinity to human histamine H1 receptor by radioligand displacement assayBinding affinity to human histamine H1 receptor by radioligand displacement assay
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.ejmech.2013.01.044
2331 2489 43 None -2 12 Human 8.8 pIC50 = 8.8 Binding
Binding affinity to human histamine H1 receptor by radioligand displacement assayBinding affinity to human histamine H1 receptor by radioligand displacement assay
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.ejmech.2013.01.044
3957 2489 43 None -2 12 Human 8.8 pIC50 = 8.8 Binding
Binding affinity to human histamine H1 receptor by radioligand displacement assayBinding affinity to human histamine H1 receptor by radioligand displacement assay
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.ejmech.2013.01.044
4992 2489 43 None -2 12 Human 8.8 pIC50 = 8.8 Binding
Binding affinity to human histamine H1 receptor by radioligand displacement assayBinding affinity to human histamine H1 receptor by radioligand displacement assay
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.ejmech.2013.01.044
CHEMBL511 2489 43 None -2 12 Human 8.8 pIC50 = 8.8 Binding
Binding affinity to human histamine H1 receptor by radioligand displacement assayBinding affinity to human histamine H1 receptor by radioligand displacement assay
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.ejmech.2013.01.044
DB06691 2489 43 None -2 12 Human 8.8 pIC50 = 8.8 Binding
Binding affinity to human histamine H1 receptor by radioligand displacement assayBinding affinity to human histamine H1 receptor by radioligand displacement assay
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.ejmech.2013.01.044
1227 2489 43 None 2 12 Guinea pig 8.8 pIC50 = 8.8 Binding
Inhibition of guinea pig histamine H1 receptorInhibition of guinea pig histamine H1 receptor
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmc.2010.07.034
2331 2489 43 None 2 12 Guinea pig 8.8 pIC50 = 8.8 Binding
Inhibition of guinea pig histamine H1 receptorInhibition of guinea pig histamine H1 receptor
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmc.2010.07.034
3957 2489 43 None 2 12 Guinea pig 8.8 pIC50 = 8.8 Binding
Inhibition of guinea pig histamine H1 receptorInhibition of guinea pig histamine H1 receptor
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmc.2010.07.034
4992 2489 43 None 2 12 Guinea pig 8.8 pIC50 = 8.8 Binding
Inhibition of guinea pig histamine H1 receptorInhibition of guinea pig histamine H1 receptor
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmc.2010.07.034
CHEMBL511 2489 43 None 2 12 Guinea pig 8.8 pIC50 = 8.8 Binding
Inhibition of guinea pig histamine H1 receptorInhibition of guinea pig histamine H1 receptor
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmc.2010.07.034
DB06691 2489 43 None 2 12 Guinea pig 8.8 pIC50 = 8.8 Binding
Inhibition of guinea pig histamine H1 receptorInhibition of guinea pig histamine H1 receptor
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmc.2010.07.034
135 2532 43 None -1 58 Human 8.8 pIC50 = 8.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
1796 2532 43 None -1 58 Human 8.8 pIC50 = 8.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
4184 2532 43 None -1 58 Human 8.8 pIC50 = 8.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
CHEMBL6437 2532 43 None -1 58 Human 8.8 pIC50 = 8.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
DB06148 2532 43 None -1 58 Human 8.8 pIC50 = 8.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
1027 1576 73 None 6 2 Guinea pig 8.8 pIC50 = 8.8 Binding
Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum
ChEMBL 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 10.1021/jm00017a019
3241 1576 73 None 6 2 Guinea pig 8.8 pIC50 = 8.8 Binding
Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum
ChEMBL 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 10.1021/jm00017a019
7176 1576 73 None 6 2 Guinea pig 8.8 pIC50 = 8.8 Binding
Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum
ChEMBL 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 10.1021/jm00017a019
CHEMBL1106 1576 73 None 6 2 Guinea pig 8.8 pIC50 = 8.8 Binding
Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum
ChEMBL 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 10.1021/jm00017a019
DB00751 1576 73 None 6 2 Guinea pig 8.8 pIC50 = 8.8 Binding
Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum
ChEMBL 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 10.1021/jm00017a019
44461456 205749 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligandBinding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligand
ChEMBL 308 2 0 3 3.8 CN(C)CC1(C)CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL82714 205749 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligandBinding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligand
ChEMBL 308 2 0 3 3.8 CN(C)CC1(C)CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
72548703 161567 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor after 60 mins by scintillation counting analysisDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor after 60 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
CHEMBL4128926 161567 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor after 60 mins by scintillation counting analysisDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor after 60 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
44318554 107079 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.
ChEMBL 312 2 0 3 3.5 CN(C)CC1CC2c3ccccc3Cc3c(F)cccc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL315834 107079 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.
ChEMBL 312 2 0 3 3.5 CN(C)CC1CC2c3ccccc3Cc3c(F)cccc3N2O1 10.1016/s0960-894x(01)00721-1
1227 2489 43 None -2 12 Human 8.7 pIC50 = 8.7 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm701575k
2331 2489 43 None -2 12 Human 8.7 pIC50 = 8.7 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm701575k
3957 2489 43 None -2 12 Human 8.7 pIC50 = 8.7 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm701575k
4992 2489 43 None -2 12 Human 8.7 pIC50 = 8.7 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm701575k
CHEMBL511 2489 43 None -2 12 Human 8.7 pIC50 = 8.7 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm701575k
DB06691 2489 43 None -2 12 Human 8.7 pIC50 = 8.7 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm701575k
124087 1389 114 None 3 15 Human 8.7 pIC50 = 8.7 Binding
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1016/j.bmcl.2019.126712
7157 1389 114 None 3 15 Human 8.7 pIC50 = 8.7 Binding
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1016/j.bmcl.2019.126712
814 1389 114 None 3 15 Human 8.7 pIC50 = 8.7 Binding
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1016/j.bmcl.2019.126712
CHEMBL1172 1389 114 None 3 15 Human 8.7 pIC50 = 8.7 Binding
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1016/j.bmcl.2019.126712
DB00967 1389 114 None 3 15 Human 8.7 pIC50 = 8.7 Binding
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1016/j.bmcl.2019.126712
1227 2489 43 None -2 12 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor in HEK293 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor in HEK293 cells after 60 mins by scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/acs.jmedchem.6b01422
2331 2489 43 None -2 12 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor in HEK293 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor in HEK293 cells after 60 mins by scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/acs.jmedchem.6b01422
3957 2489 43 None -2 12 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor in HEK293 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor in HEK293 cells after 60 mins by scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/acs.jmedchem.6b01422
4992 2489 43 None -2 12 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor in HEK293 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor in HEK293 cells after 60 mins by scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/acs.jmedchem.6b01422
CHEMBL511 2489 43 None -2 12 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor in HEK293 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor in HEK293 cells after 60 mins by scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/acs.jmedchem.6b01422
DB06691 2489 43 None -2 12 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor in HEK293 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor in HEK293 cells after 60 mins by scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/acs.jmedchem.6b01422
13726596 93948 0 None - 0 Guinea pig 8.7 pIC50 = 8.7 Binding
Inhibition of [3H]mepyramine binding to the histamine receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the histamine receptor in guinea pig cortex
ChEMBL 299 3 0 4 2.1 CN(C)CC[C@@H]1CN(C)C(=S)c2cc(Cl)cnc2O1 10.1021/jm00108a012
CHEMBL24835 93948 0 None - 0 Guinea pig 8.7 pIC50 = 8.7 Binding
Inhibition of [3H]mepyramine binding to the histamine receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the histamine receptor in guinea pig cortex
ChEMBL 299 3 0 4 2.1 CN(C)CC[C@@H]1CN(C)C(=S)c2cc(Cl)cnc2O1 10.1021/jm00108a012
19426635 205593 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligandBinding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligand
ChEMBL 280 2 1 3 3.1 CNCC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL81485 205593 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligandBinding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligand
ChEMBL 280 2 1 3 3.1 CNCC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
9869791 63926 20 None - 1 Rat 7.0 pIC50 = 7 Binding
Concentration for 50% inhibition towards central histamine H1 receptor Concentration for 50% inhibition towards central histamine H1 receptor
ChEMBL 480 8 1 7 0.9 CN1CCN(S(=O)(=O)CCCN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)CC1 10.1016/j.bmcl.2005.01.039
CHEMBL180632 63926 20 None - 1 Rat 7.0 pIC50 = 7 Binding
Concentration for 50% inhibition towards central histamine H1 receptor Concentration for 50% inhibition towards central histamine H1 receptor
ChEMBL 480 8 1 7 0.9 CN1CCN(S(=O)(=O)CCCN2CCC(CNC(=O)c3cccc4c3OCCO4)CC2)CC1 10.1016/j.bmcl.2005.01.039
11453538 84744 0 None - 0 Guinea pig 7.0 pIC50 = 7 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 442 10 1 6 4.7 CCOCCn1cc(C2CCN(CCOc3ccsc3C(=O)O)CC2)c2ccccc21 10.1021/jm0498203
CHEMBL222927 84744 0 None - 0 Guinea pig 7.0 pIC50 = 7 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 442 10 1 6 4.7 CCOCCn1cc(C2CCN(CCOc3ccsc3C(=O)O)CC2)c2ccccc21 10.1021/jm0498203
11396873 136985 0 None - 0 Guinea pig 7.0 pIC50 = 7 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 454 10 1 5 4.8 CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cc(F)ccc21 10.1021/jm0498203
CHEMBL374585 136985 0 None - 0 Guinea pig 7.0 pIC50 = 7 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 454 10 1 5 4.8 CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cc(F)ccc21 10.1021/jm0498203
1853 3551 38 None - 1 Human 7.0 pIC50 = 7 Binding
Inhibitory concentration against histamine H1 receptorInhibitory concentration against histamine H1 receptor
ChEMBL 352 0 0 2 4.3 Clc1ccc2c(c1)CCc1c(C2=C2CCN(CC2)C(=O)C)nccc1 10.1021/jm058225d
60680 3551 38 None - 1 Human 7.0 pIC50 = 7 Binding
Inhibitory concentration against histamine H1 receptorInhibitory concentration against histamine H1 receptor
ChEMBL 352 0 0 2 4.3 Clc1ccc2c(c1)CCc1c(C2=C2CCN(CC2)C(=O)C)nccc1 10.1021/jm058225d
CHEMBL10971 3551 38 None - 1 Human 7.0 pIC50 = 7 Binding
Inhibitory concentration against histamine H1 receptorInhibitory concentration against histamine H1 receptor
ChEMBL 352 0 0 2 4.3 Clc1ccc2c(c1)CCc1c(C2=C2CCN(CC2)C(=O)C)nccc1 10.1021/jm058225d
1613 2348 53 None - 44 Rat 6.0 pIC50 = 6 Binding
Binding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligandBinding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligand
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm991005d
205 2348 53 None - 44 Rat 6.0 pIC50 = 6 Binding
Binding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligandBinding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligand
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm991005d
3964 2348 53 None - 44 Rat 6.0 pIC50 = 6 Binding
Binding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligandBinding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligand
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm991005d
CHEMBL831 2348 53 None - 44 Rat 6.0 pIC50 = 6 Binding
Binding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligandBinding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligand
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm991005d
DB00408 2348 53 None - 44 Rat 6.0 pIC50 = 6 Binding
Binding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligandBinding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligand
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm991005d
3689 102771 55 None - 0 Human 6.0 pIC50 = 6 Binding
Compound was tested for the binding affinity against histamine H1 receptor by using [3H]mepyramine as radioligandCompound was tested for the binding affinity against histamine H1 receptor by using [3H]mepyramine as radioligand
ChEMBL 325 5 2 3 3.8 CC(C(O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1021/jm00114a018
CHEMBL1372983 102771 55 None - 0 Human 6.0 pIC50 = 6 Binding
Compound was tested for the binding affinity against histamine H1 receptor by using [3H]mepyramine as radioligandCompound was tested for the binding affinity against histamine H1 receptor by using [3H]mepyramine as radioligand
ChEMBL 325 5 2 3 3.8 CC(C(O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1021/jm00114a018
CHEMBL305187 102771 55 None - 0 Human 6.0 pIC50 = 6 Binding
Compound was tested for the binding affinity against histamine H1 receptor by using [3H]mepyramine as radioligandCompound was tested for the binding affinity against histamine H1 receptor by using [3H]mepyramine as radioligand
ChEMBL 325 5 2 3 3.8 CC(C(O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1021/jm00114a018
11430418 18786 12 None - 1 Human 6.0 pIC50 = 6 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptorDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor
ChEMBL 432 6 1 7 2.5 Nn1c(CCCCN2CCN(c3ccc4ccccc4n3)CC2)nc2c(c1=O)CCCC2 10.1021/jm1002292
CHEMBL1278088 18786 12 None - 1 Human 6.0 pIC50 = 6 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptorDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor
ChEMBL 432 6 1 7 2.5 Nn1c(CCCCN2CCN(c3ccc4ccccc4n3)CC2)nc2c(c1=O)CCCC2 10.1021/jm1002292
11459394 48166 1 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 251 12 2 2 3.8 NCCCCCCCCCCCCc1c[nH]cn1 10.1021/jm030936t
CHEMBL155188 48166 1 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 251 12 2 2 3.8 NCCCCCCCCCCCCc1c[nH]cn1 10.1021/jm030936t
5310982 93612 4 None - 3 Human 6.0 pIC50 = 6 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 255 3 2 2 2.6 NCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1 10.1021/jm030936t
CHEMBL24665 93612 4 None - 3 Human 6.0 pIC50 = 6 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 255 3 2 2 2.6 NCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1 10.1021/jm030936t
107782 14468 18 None 1 5 Human 5.0 pIC50 = 5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O nan
67151996 14468 18 None 1 5 Human 5.0 pIC50 = 5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O nan
CHEMBL1201207 14468 18 None 1 5 Human 5.0 pIC50 = 5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O nan
44461357 104374 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligandBinding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligand
ChEMBL 330 2 0 4 4.3 CN(C)CC1CC2c3ccccc3Oc3ccc(Cl)cc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL310183 104374 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligandBinding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligand
ChEMBL 330 2 0 4 4.3 CN(C)CC1CC2c3ccccc3Oc3ccc(Cl)cc3N2O1 10.1016/s0960-894x(01)00721-1
10205121 66692 0 None - 0 Guinea pig 7.0 pIC50 = 7.0 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 464 6 1 4 6.5 O=C(O)c1cccc(CN2CCC(c3cn(Cc4ccc(Cl)s4)c4ccccc34)CC2)c1 10.1021/jm0498203
CHEMBL185489 66692 0 None - 0 Guinea pig 7.0 pIC50 = 7.0 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 464 6 1 4 6.5 O=C(O)c1cccc(CN2CCC(c3cn(Cc4ccc(Cl)s4)c4ccccc34)CC2)c1 10.1021/jm0498203
45268185 196107 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 535 8 1 9 2.9 Cn1c(N2CCN(CCCN3c4ccccc4Sc4ccc(CCC(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmcl.2009.03.124
CHEMBL560917 196107 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 535 8 1 9 2.9 Cn1c(N2CCN(CCCN3c4ccccc4Sc4ccc(CCC(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmcl.2009.03.124
14762577 4468 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 336 6 1 2 3.7 Cc1ccccc1C(=O)NCCN1CCC(Cc2ccccc2)CC1 10.1021/jm00173a011
CHEMBL101790 4468 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 336 6 1 2 3.7 Cc1ccccc1C(=O)NCCN1CCC(Cc2ccccc2)CC1 10.1021/jm00173a011
44318841 106927 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.
ChEMBL 308 2 0 3 3.7 Cc1cccc2c1C1CC(CN(C)C)ON1c1ccccc1C2 10.1016/s0960-894x(01)00721-1
CHEMBL314795 106927 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.
ChEMBL 308 2 0 3 3.7 Cc1cccc2c1C1CC(CN(C)C)ON1c1ccccc1C2 10.1016/s0960-894x(01)00721-1
155554175 175693 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 490 6 1 5 5.2 COc1ccc(OCC(O)CN2CCC(=C3c4ccc(Cl)cc4CCc4cccnc43)CC2)cc1 10.1016/j.bmcl.2019.126712
CHEMBL4581995 175693 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 490 6 1 5 5.2 COc1ccc(OCC(O)CN2CCC(=C3c4ccc(Cl)cc4CCc4cccnc43)CC2)cc1 10.1016/j.bmcl.2019.126712
9904236 14076 22 None - 1 Human 5.0 pIC50 = 5.0 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.
ChEMBL 295 0 1 3 3.7 O=C1Cc2ccccc2C(=C2CCNCC2)c2ccsc21 nan
CHEMBL1197564 14076 22 None - 1 Human 5.0 pIC50 = 5.0 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.
ChEMBL 295 0 1 3 3.7 O=C1Cc2ccccc2C(=C2CCNCC2)c2ccsc21 nan
9904236 14076 22 None - 1 Human 5.0 pIC50 = 5.0 Binding
Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 295 0 1 3 3.7 O=C1Cc2ccccc2C(=C2CCNCC2)c2ccsc21 nan
CHEMBL1197564 14076 22 None - 1 Human 5.0 pIC50 = 5.0 Binding
Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 295 0 1 3 3.7 O=C1Cc2ccccc2C(=C2CCNCC2)c2ccsc21 nan
118162109 186246 11 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of histamine H1 receptor (unknown origin)Inhibition of histamine H1 receptor (unknown origin)
ChEMBL 447 8 3 9 3.1 CC(F)(F)COc1ncncc1CNc1ncc(C#N)c(N[C@@H]2CC[C@H](O)C(C)(C)C2)n1 10.1021/acs.jmedchem.1c00388
CHEMBL4873647 186246 11 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of histamine H1 receptor (unknown origin)Inhibition of histamine H1 receptor (unknown origin)
ChEMBL 447 8 3 9 3.1 CC(F)(F)COc1ncncc1CNc1ncc(C#N)c(N[C@@H]2CC[C@H](O)C(C)(C)C2)n1 10.1021/acs.jmedchem.1c00388
736282 78142 12 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
ChEMBL 337 6 1 3 4.2 CN1[C@H](CC(=O)c2ccccc2)CCC[C@@H]1C[C@H](O)c1ccccc1 10.1021/jm300671m
CHEMBL2103769 78142 12 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
ChEMBL 337 6 1 3 4.2 CN1[C@H](CC(=O)c2ccccc2)CCC[C@@H]1C[C@H](O)c1ccccc1 10.1021/jm300671m
13726595 99573 0 None - 0 Guinea pig 4.9 pIC50 = 4.9 Binding
Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex
ChEMBL 299 3 0 4 2.1 CN(C)CC[C@H]1CN(C)C(=S)c2cc(Cl)cnc2O1 10.1021/jm00108a012
CHEMBL283760 99573 0 None - 0 Guinea pig 4.9 pIC50 = 4.9 Binding
Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex
ChEMBL 299 3 0 4 2.1 CN(C)CC[C@H]1CN(C)C(=S)c2cc(Cl)cnc2O1 10.1021/jm00108a012
2726 919 68 None -2 72 Human 7.9 pIC50 = 7.9 Binding
Binding affinity to histamine H1 receptor (unknown origin) by radioligand binding assayBinding affinity to histamine H1 receptor (unknown origin) by radioligand binding assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm400856t
621 919 68 None -2 72 Human 7.9 pIC50 = 7.9 Binding
Binding affinity to histamine H1 receptor (unknown origin) by radioligand binding assayBinding affinity to histamine H1 receptor (unknown origin) by radioligand binding assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm400856t
83 919 68 None -2 72 Human 7.9 pIC50 = 7.9 Binding
Binding affinity to histamine H1 receptor (unknown origin) by radioligand binding assayBinding affinity to histamine H1 receptor (unknown origin) by radioligand binding assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm400856t
CHEMBL71 919 68 None -2 72 Human 7.9 pIC50 = 7.9 Binding
Binding affinity to histamine H1 receptor (unknown origin) by radioligand binding assayBinding affinity to histamine H1 receptor (unknown origin) by radioligand binding assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm400856t
DB00477 919 68 None -2 72 Human 7.9 pIC50 = 7.9 Binding
Binding affinity to histamine H1 receptor (unknown origin) by radioligand binding assayBinding affinity to histamine H1 receptor (unknown origin) by radioligand binding assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm400856t
1227 2489 43 None -2 12 Human 7.9 pIC50 = 7.9 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm030936t
2331 2489 43 None -2 12 Human 7.9 pIC50 = 7.9 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm030936t
3957 2489 43 None -2 12 Human 7.9 pIC50 = 7.9 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm030936t
4992 2489 43 None -2 12 Human 7.9 pIC50 = 7.9 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm030936t
CHEMBL511 2489 43 None -2 12 Human 7.9 pIC50 = 7.9 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm030936t
DB06691 2489 43 None -2 12 Human 7.9 pIC50 = 7.9 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm030936t
10026300 167834 17 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligandBinding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligand
ChEMBL 441 2 0 7 3.3 CN1CCN(C2=Nc3ccccc3Oc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
CHEMBL430798 167834 17 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligandBinding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligand
ChEMBL 441 2 0 7 3.3 CN1CCN(C2=Nc3ccccc3Oc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
10141470 123557 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 494 8 1 5 6.4 O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccc(Cl)s3)c3ccccc23)CC1 10.1021/jm0498203
CHEMBL361805 123557 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 494 8 1 5 6.4 O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccc(Cl)s3)c3ccccc23)CC1 10.1021/jm0498203
44392633 65576 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 454 9 1 4 6.1 CCCCn1cc(C2CCN(CCOc3cc(Cl)ccc3C(=O)O)CC2)c2ccccc21 10.1016/j.bmcl.2004.12.008
CHEMBL183168 65576 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 454 9 1 4 6.1 CCCCn1cc(C2CCN(CCOc3cc(Cl)ccc3C(=O)O)CC2)c2ccccc21 10.1016/j.bmcl.2004.12.008
9932752 141983 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 436 8 1 4 5.1 O=C(O)c1ccccc1OCCN1CCC(c2cn(CC3CC3)c3cc(F)ccc23)CC1 10.1021/jm0498203
CHEMBL387391 141983 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 436 8 1 4 5.1 O=C(O)c1ccccc1OCCN1CCC(c2cn(CC3CC3)c3cc(F)ccc23)CC1 10.1021/jm0498203
45485061 198754 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptorDisplacement of [3H]pyrilamine from human histamine H1 receptor
ChEMBL 489 5 2 5 5.0 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL583014 198754 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptorDisplacement of [3H]pyrilamine from human histamine H1 receptor
ChEMBL 489 5 2 5 5.0 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
45269073 196388 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 563 7 1 9 3.7 Cn1c(N2CCCN(CCCN3c4ccccc4Sc4ccc(C(C)(C)C(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmcl.2009.03.124
CHEMBL562676 196388 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 563 7 1 9 3.7 Cn1c(N2CCCN(CCCN3c4ccccc4Sc4ccc(C(C)(C)C(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmcl.2009.03.124
45269070 196616 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 493 5 1 9 2.2 Cn1c(N2CCN(CCN3c4ccccc4Sc4ccc(C(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmcl.2009.03.124
CHEMBL564168 196616 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 493 5 1 9 2.2 Cn1c(N2CCN(CCN3c4ccccc4Sc4ccc(C(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmcl.2009.03.124
4601 206747 35 None -1 16 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL1201023 206747 35 None -1 16 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL900 206747 35 None -1 16 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
10226501 137874 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 460 7 1 5 5.8 COc1ccc(CN2CCC(c3cn(Cc4cccs4)c4ccccc34)CC2)cc1C(=O)O 10.1021/jm0498203
CHEMBL376202 137874 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 460 7 1 5 5.8 COc1ccc(CN2CCC(c3cn(Cc4cccs4)c4ccccc34)CC2)cc1C(=O)O 10.1021/jm0498203
2284 3182 33 None -10 29 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1021/jm300671m
4926 3182 33 None -10 29 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1021/jm300671m
7281 3182 33 None -10 29 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1021/jm300671m
CHEMBL564 3182 33 None -10 29 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1021/jm300671m
DB00420 3182 33 None -10 29 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1021/jm300671m
1197 88 120 None - 1 Human 5.9 pIC50 = 5.9 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 122 2 1 2 0.6 NCCc1ccccn1 10.1021/jm030936t
75919 88 120 None - 1 Human 5.9 pIC50 = 5.9 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 122 2 1 2 0.6 NCCc1ccccn1 10.1021/jm030936t
CHEMBL32813 88 120 None - 1 Human 5.9 pIC50 = 5.9 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 122 2 1 2 0.6 NCCc1ccccn1 10.1021/jm030936t
10890691 44716 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 262 12 1 2 4.5 NCCCCCCCCCCCCc1cccnc1 10.1021/jm030936t
CHEMBL152122 44716 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 262 12 1 2 4.5 NCCCCCCCCCCCCc1cccnc1 10.1021/jm030936t
11288570 49000 1 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 265 13 2 2 4.2 NCCCCCCCCCCCCCc1c[nH]cn1 10.1021/jm030936t
CHEMBL156071 49000 1 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 265 13 2 2 4.2 NCCCCCCCCCCCCCc1c[nH]cn1 10.1021/jm030936t
2142 3096 58 None -7585 36 Rat 4.9 pIC50 = 4.9 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm300671m
4920903 3096 58 None -7585 36 Rat 4.9 pIC50 = 4.9 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm300671m
502 3096 58 None -7585 36 Rat 4.9 pIC50 = 4.9 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm300671m
5775 3096 58 None -7585 36 Rat 4.9 pIC50 = 4.9 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm300671m
CHEMBL597 3096 58 None -7585 36 Rat 4.9 pIC50 = 4.9 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm300671m
DB00692 3096 58 None -7585 36 Rat 4.9 pIC50 = 4.9 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1021/jm300671m
9802248 166243 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 420 9 1 4 5.4 CCCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccccc21 10.1021/jm0498203
CHEMBL426786 166243 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 420 9 1 4 5.4 CCCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccccc21 10.1021/jm0498203
14762597 4343 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 392 4 2 3 3.4 O=C(CCN1CCN2Cc3[nH]c4ccccc4c3CC2C1)Nc1ccccc1F 10.1021/jm00173a011
CHEMBL101029 4343 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 392 4 2 3 3.4 O=C(CCN1CCN2Cc3[nH]c4ccccc4c3CC2C1)Nc1ccccc1F 10.1021/jm00173a011
54582401 61998 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 533 7 1 9 2.3 Cn1c(N2CCCN(CCCN3c4ccccc4COc4ccc(CC(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmc.2011.03.003
CHEMBL1774493 61998 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 533 7 1 9 2.3 Cn1c(N2CCCN(CCCN3c4ccccc4COc4ccc(CC(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmc.2011.03.003
54583384 61999 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 547 7 1 9 2.9 CC(C(=O)O)c1ccc2c(c1)N(CCCN1CCCN(c3cc(=O)n(C)c(=O)n3C)CC1)c1ccccc1CO2 10.1016/j.bmc.2011.03.003
CHEMBL1774494 61999 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 547 7 1 9 2.9 CC(C(=O)O)c1ccc2c(c1)N(CCCN1CCCN(c3cc(=O)n(C)c(=O)n3C)CC1)c1ccccc1CO2 10.1016/j.bmc.2011.03.003
11071079 110593 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 496 9 0 3 6.0 O=C(OCCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
CHEMBL325516 110593 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 496 9 0 3 6.0 O=C(OCCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
135398745 2914 112 None 1 65 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
47 2914 112 None 1 65 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
CHEMBL715 2914 112 None 1 65 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
DB00334 2914 112 None 1 65 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
135398745 2914 112 None -1 65 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [3H]mepyramine from H1R in rat brainDisplacement of [3H]mepyramine from H1R in rat brain
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1073/pnas.0611417104
47 2914 112 None -1 65 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [3H]mepyramine from H1R in rat brainDisplacement of [3H]mepyramine from H1R in rat brain
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1073/pnas.0611417104
CHEMBL715 2914 112 None -1 65 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [3H]mepyramine from H1R in rat brainDisplacement of [3H]mepyramine from H1R in rat brain
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1073/pnas.0611417104
DB00334 2914 112 None -1 65 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [3H]mepyramine from H1R in rat brainDisplacement of [3H]mepyramine from H1R in rat brain
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1073/pnas.0611417104
44461622 205943 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligandBinding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligand
ChEMBL 322 4 0 3 4.2 CCN(CC)CC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL84293 205943 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligandBinding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligand
ChEMBL 322 4 0 3 4.2 CCN(CC)CC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
11476077 136407 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 436 10 1 5 4.5 CCOCCn1cc(C2CCN(Cc3cccc(OCC(=O)O)c3)CC2)c2ccccc21 10.1021/jm0498203
CHEMBL373534 136407 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 436 10 1 5 4.5 CCOCCn1cc(C2CCN(Cc3cccc(OCC(=O)O)c3)CC2)c2ccccc21 10.1021/jm0498203
137125241 123063 30 None - 0 Human 4.9 pIC50 = 4.9 Binding
Selectivity interaction (Receptor panel (Novartis) ) EUB0000164c HRH1Selectivity interaction (Receptor panel (Novartis) ) EUB0000164c HRH1
ChEMBL 479 4 2 4 5.1 CC(C)NC(=O)N1CC[C@H](NC2=Nc3cc(F)ccc3N(CC(F)F)c3ccc(Cl)cc32)C1 10.6019/CHEMBL5212743
CHEMBL3609372 123063 30 None - 0 Human 4.9 pIC50 = 4.9 Binding
Selectivity interaction (Receptor panel (Novartis) ) EUB0000164c HRH1Selectivity interaction (Receptor panel (Novartis) ) EUB0000164c HRH1
ChEMBL 479 4 2 4 5.1 CC(C)NC(=O)N1CC[C@H](NC2=Nc3cc(F)ccc3N(CC(F)F)c3ccc(Cl)cc32)C1 10.6019/CHEMBL5212743
14762603 4196 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 380 5 1 5 2.7 O=C(CCN1CCN2Cc3ccccc3CC2C1)Nc1ccccc1[N+](=O)[O-] 10.1021/jm00173a011
CHEMBL100169 4196 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 380 5 1 5 2.7 O=C(CCN1CCN2Cc3ccccc3CC2C1)Nc1ccccc1[N+](=O)[O-] 10.1021/jm00173a011
14762570 4288 3 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 368 7 1 5 2.1 O=C(NCCN1CCN(Cc2ccccc2)CC1)c1ccccc1[N+](=O)[O-] 10.1021/jm00173a011
CHEMBL100695 4288 3 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 368 7 1 5 2.1 O=C(NCCN1CCN(Cc2ccccc2)CC1)c1ccccc1[N+](=O)[O-] 10.1021/jm00173a011
771426 4384 17 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 341 6 1 3 3.0 O=C(CCN1CCN(Cc2ccccc2)CC1)Nc1ccccc1F 10.1021/jm00173a011
CHEMBL101312 4384 17 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 341 6 1 3 3.0 O=C(CCN1CCN(Cc2ccccc2)CC1)Nc1ccccc1F 10.1021/jm00173a011
14762602 4171 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 335 4 1 3 2.8 O=C(CCN1CCN2Cc3ccccc3CC2C1)Nc1ccccc1 10.1021/jm00173a011
CHEMBL100064 4171 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 335 4 1 3 2.8 O=C(CCN1CCN2Cc3ccccc3CC2C1)Nc1ccccc1 10.1021/jm00173a011
3151 1462 97 None -41 27 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
945 1462 97 None -41 27 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
965 1462 97 None -41 27 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
CHEMBL219916 1462 97 None -41 27 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
DB01184 1462 97 None -41 27 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
54581387 62011 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 528 6 1 7 2.8 Cn1c(N2CCCN(CC/C=C3/c4ccccc4CCc4ccc(CC(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmc.2011.03.003
CHEMBL1774506 62011 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 528 6 1 7 2.8 Cn1c(N2CCCN(CC/C=C3/c4ccccc4CCc4ccc(CC(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmc.2011.03.003
44392585 122612 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 528 8 1 5 7.0 O=C(O)c1ccc(Cl)cc1OCCN1CCC(c2cn(Cc3ccc(Cl)s3)c3ccccc23)CC1 10.1016/j.bmcl.2004.12.008
CHEMBL360270 122612 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 528 8 1 5 7.0 O=C(O)c1ccc(Cl)cc1OCCN1CCC(c2cn(Cc3ccc(Cl)s3)c3ccccc23)CC1 10.1016/j.bmcl.2004.12.008
2247 505 81 None -4 42 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 505 81 None -4 42 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 505 81 None -4 42 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 505 81 None -4 42 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 505 81 None -4 42 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
44319119 106967 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.
ChEMBL 324 3 0 4 3.4 COc1ccc2c(c1)C1CC(CN(C)C)ON1c1ccccc1C2 10.1016/s0960-894x(01)00721-1
CHEMBL315044 106967 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.
ChEMBL 324 3 0 4 3.4 COc1ccc2c(c1)C1CC(CN(C)C)ON1c1ccccc1C2 10.1016/s0960-894x(01)00721-1
9823337 137264 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 418 8 1 4 5.0 O=C(O)c1ccccc1OCCN1CCC(c2cn(CC3CC3)c3ccccc23)CC1 10.1021/jm0498203
CHEMBL375208 137264 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 418 8 1 4 5.0 O=C(O)c1ccccc1OCCN1CCC(c2cn(CC3CC3)c3ccccc23)CC1 10.1021/jm0498203
11362693 141612 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 440 9 1 5 4.4 COCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccc(F)cc21 10.1021/jm0498203
CHEMBL385133 141612 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 440 9 1 5 4.4 COCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccc(F)cc21 10.1021/jm0498203
54581386 61995 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 505 6 1 9 2.0 Cn1c(N2CCN(CCCN3c4ccccc4COc4ccc(C(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmc.2011.03.003
CHEMBL1774490 61995 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 505 6 1 9 2.0 Cn1c(N2CCN(CCCN3c4ccccc4COc4ccc(C(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmc.2011.03.003
9889247 84761 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 436 10 1 5 4.6 CCOCCn1cc(C2CCN(CCOc3cccc(C(=O)O)c3)CC2)c2ccccc21 10.1021/jm0498203
CHEMBL223024 84761 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 436 10 1 5 4.6 CCOCCn1cc(C2CCN(CCOc3cccc(C(=O)O)c3)CC2)c2ccccc21 10.1021/jm0498203
10478188 122942 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 436 9 1 5 4.8 CCOCCn1cc(C2CCN(Cc3ccc(OC)c(C(=O)O)c3)CC2)c2ccccc21 10.1021/jm0498203
CHEMBL360712 122942 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 436 9 1 5 4.8 CCOCCn1cc(C2CCN(Cc3ccc(OC)c(C(=O)O)c3)CC2)c2ccccc21 10.1021/jm0498203
5624 32693 14 None -5 10 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 520 5 1 8 4.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2 nan
CHEMBL1203324 32693 14 None -5 10 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 520 5 1 8 4.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2 nan
CHEMBL141343 32693 14 None -5 10 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 520 5 1 8 4.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2 nan
1170 1633 75 None - 1 Human 7.8 pIC50 = 7.8 Binding
Inhibition of histamine H1 receptor (unknown origin)Inhibition of histamine H1 receptor (unknown origin)
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1021/jm501535r
3348 1633 75 None - 1 Human 7.8 pIC50 = 7.8 Binding
Inhibition of histamine H1 receptor (unknown origin)Inhibition of histamine H1 receptor (unknown origin)
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1021/jm501535r
4819 1633 75 None - 1 Human 7.8 pIC50 = 7.8 Binding
Inhibition of histamine H1 receptor (unknown origin)Inhibition of histamine H1 receptor (unknown origin)
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1021/jm501535r
74685737 1633 75 None - 1 Human 7.8 pIC50 = 7.8 Binding
Inhibition of histamine H1 receptor (unknown origin)Inhibition of histamine H1 receptor (unknown origin)
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1021/jm501535r
CHEMBL914 1633 75 None - 1 Human 7.8 pIC50 = 7.8 Binding
Inhibition of histamine H1 receptor (unknown origin)Inhibition of histamine H1 receptor (unknown origin)
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1021/jm501535r
DB00950 1633 75 None - 1 Human 7.8 pIC50 = 7.8 Binding
Inhibition of histamine H1 receptor (unknown origin)Inhibition of histamine H1 receptor (unknown origin)
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1021/jm501535r
44318834 106151 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.
ChEMBL 328 2 0 3 4.1 CN(C)CC1CC2c3ccccc3Cc3cccc(Cl)c3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL313604 106151 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.
ChEMBL 328 2 0 3 4.1 CN(C)CC1CC2c3ccccc3Cc3cccc(Cl)c3N2O1 10.1016/s0960-894x(01)00721-1
44318820 206038 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.
ChEMBL 308 2 0 3 3.7 Cc1ccc2c(c1)Cc1ccccc1N1OC(CN(C)C)CC21 10.1016/s0960-894x(01)00721-1
CHEMBL85155 206038 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.
ChEMBL 308 2 0 3 3.7 Cc1ccc2c(c1)Cc1ccccc1N1OC(CN(C)C)CC21 10.1016/s0960-894x(01)00721-1
2865 4143 73 None -1047 53 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [3H]mepyramine from H1R in rat brainDisplacement of [3H]mepyramine from H1R in rat brain
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1073/pnas.0611417104
59 4143 73 None -1047 53 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [3H]mepyramine from H1R in rat brainDisplacement of [3H]mepyramine from H1R in rat brain
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1073/pnas.0611417104
60854 4143 73 None -1047 53 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [3H]mepyramine from H1R in rat brainDisplacement of [3H]mepyramine from H1R in rat brain
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1073/pnas.0611417104
CHEMBL708 4143 73 None -1047 53 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [3H]mepyramine from H1R in rat brainDisplacement of [3H]mepyramine from H1R in rat brain
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1073/pnas.0611417104
DB00246 4143 73 None -1047 53 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [3H]mepyramine from H1R in rat brainDisplacement of [3H]mepyramine from H1R in rat brain
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1073/pnas.0611417104
10279311 84351 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 512 7 1 5 6.6 COc1ccc(CN2CCC(c3cn(Cc4ccc(Cl)s4)c4cc(F)ccc34)CC2)cc1C(=O)O 10.1021/jm0498203
CHEMBL221730 84351 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 512 7 1 5 6.6 COc1ccc(CN2CCC(c3cn(Cc4ccc(Cl)s4)c4cc(F)ccc34)CC2)cc1C(=O)O 10.1021/jm0498203
11212029 84619 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 410 7 1 4 4.5 COCCn1cc(C2CCN(Cc3cccc(C(=O)O)c3)CC2)c2ccc(F)cc21 10.1021/jm0498203
CHEMBL222142 84619 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 410 7 1 4 4.5 COCCn1cc(C2CCN(Cc3cccc(C(=O)O)c3)CC2)c2ccc(F)cc21 10.1021/jm0498203
9889248 84730 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 436 10 1 5 4.6 CCOCCn1cc(C2CCN(CCOc3ccc(C(=O)O)cc3)CC2)c2ccccc21 10.1021/jm0498203
CHEMBL222853 84730 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 436 10 1 5 4.6 CCOCCn1cc(C2CCN(CCOc3ccc(C(=O)O)cc3)CC2)c2ccccc21 10.1021/jm0498203
11329754 141982 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 514 10 1 5 5.4 CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cc(Br)ccc21 10.1021/jm0498203
CHEMBL387390 141982 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 514 10 1 5 5.4 CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cc(Br)ccc21 10.1021/jm0498203
1305 511 14 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptorDisplacement of [3H]pyrilamine from human histamine H1 receptor
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2009.09.003
9934033 511 14 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptorDisplacement of [3H]pyrilamine from human histamine H1 receptor
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL182150 511 14 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptorDisplacement of [3H]pyrilamine from human histamine H1 receptor
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2009.09.003
54586253 62000 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 561 7 1 9 3.1 Cn1c(N2CCCN(CCCN3c4ccccc4COc4ccc(C(C)(C)C(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmc.2011.03.003
CHEMBL1774495 62000 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 561 7 1 9 3.1 Cn1c(N2CCCN(CCCN3c4ccccc4COc4ccc(C(C)(C)C(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmc.2011.03.003
44461613 104223 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligandBinding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligand
ChEMBL 350 4 0 3 5.0 CC(C)N(CC1CC2c3ccccc3Cc3ccccc3N2O1)C(C)C 10.1016/s0960-894x(01)00721-1
CHEMBL309904 104223 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligandBinding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligand
ChEMBL 350 4 0 3 5.0 CC(C)N(CC1CC2c3ccccc3Cc3ccccc3N2O1)C(C)C 10.1016/s0960-894x(01)00721-1
14762593 4679 7 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 322 6 1 2 4.0 O=C(CCN1CCC(Cc2ccccc2)CC1)Nc1ccccc1 10.1021/jm00173a011
CHEMBL103303 4679 7 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 322 6 1 2 4.0 O=C(CCN1CCC(Cc2ccccc2)CC1)Nc1ccccc1 10.1021/jm00173a011
54587282 62012 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 514 5 1 7 2.9 Cn1c(N2CCCN(CC/C=C3/c4ccccc4CCc4ccc(C(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmc.2011.03.003
CHEMBL1774507 62012 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 514 5 1 7 2.9 Cn1c(N2CCCN(CC/C=C3/c4ccccc4CCc4ccc(C(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmc.2011.03.003
14762579 4398 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 322 6 1 2 3.4 O=C(NCCN1CCC(Cc2ccccc2)CC1)c1ccccc1 10.1021/jm00173a011
CHEMBL101388 4398 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 322 6 1 2 3.4 O=C(NCCN1CCC(Cc2ccccc2)CC1)c1ccccc1 10.1021/jm00173a011
11351801 84349 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 466 11 1 6 4.6 CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cc(OC)ccc21 10.1021/jm0498203
CHEMBL221716 84349 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 466 11 1 6 4.6 CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cc(OC)ccc21 10.1021/jm0498203
12488 1657 56 None -2 23 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
941361 1657 56 None -2 23 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
CHEMBL30008 1657 56 None -2 23 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
DB04841 1657 56 None -2 23 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
1204 1932 119 None -501 24 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm030936t
1247 1932 119 None -501 24 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm030936t
1375 1932 119 None -501 24 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm030936t
774 1932 119 None -501 24 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm030936t
CHEMBL90 1932 119 None -501 24 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm030936t
DB05381 1932 119 None -501 24 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm030936t
4098 32505 30 None 1 11 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 nan
CHEMBL1255739 32505 30 None 1 11 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 nan
CHEMBL1411979 32505 30 None 1 11 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 nan
44345317 113067 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity against Histamine H1 receptorBinding affinity against Histamine H1 receptor
ChEMBL 295 2 0 4 2.8 CN(C)CC1CC2c3cccnc3Cc3ccccc3N2O1 10.1016/s0960-894x(02)00796-5
CHEMBL331188 113067 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity against Histamine H1 receptorBinding affinity against Histamine H1 receptor
ChEMBL 295 2 0 4 2.8 CN(C)CC1CC2c3cccnc3Cc3ccccc3N2O1 10.1016/s0960-894x(02)00796-5
10246054 106544 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.
ChEMBL 330 2 0 3 3.7 CN(C)CC1CC2c3cc(F)ccc3Cc3ccc(F)cc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL314107 106544 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.
ChEMBL 330 2 0 3 3.7 CN(C)CC1CC2c3cc(F)ccc3Cc3ccc(F)cc3N2O1 10.1016/s0960-894x(01)00721-1
1588 2325 27 None -35 44 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
28864 2325 27 None -35 44 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
43 2325 27 None -35 44 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
CHEMBL157138 2325 27 None -35 44 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
DB00589 2325 27 None -35 44 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
45485062 197168 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptorDisplacement of [3H]pyrilamine from human histamine H1 receptor
ChEMBL 367 5 2 5 3.3 Cc1cccc(C(=O)N[C@H]2CC[C@@H](Nc3ncc(C)c(N(C)C)n3)CC2)c1 10.1016/j.bmcl.2009.09.003
CHEMBL567993 197168 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptorDisplacement of [3H]pyrilamine from human histamine H1 receptor
ChEMBL 367 5 2 5 3.3 Cc1cccc(C(=O)N[C@H]2CC[C@@H](Nc3ncc(C)c(N(C)C)n3)CC2)c1 10.1016/j.bmcl.2009.09.003
124087 1389 114 None 3 15 Human 4.8 pIC50 = 4.8 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
7157 1389 114 None 3 15 Human 4.8 pIC50 = 4.8 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
814 1389 114 None 3 15 Human 4.8 pIC50 = 4.8 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
CHEMBL1172 1389 114 None 3 15 Human 4.8 pIC50 = 4.8 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
DB00967 1389 114 None 3 15 Human 4.8 pIC50 = 4.8 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
124087 1389 114 None 3 15 Human 4.8 pIC50 = 4.8 Binding
Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
7157 1389 114 None 3 15 Human 4.8 pIC50 = 4.8 Binding
Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
814 1389 114 None 3 15 Human 4.8 pIC50 = 4.8 Binding
Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
CHEMBL1172 1389 114 None 3 15 Human 4.8 pIC50 = 4.8 Binding
Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
DB00967 1389 114 None 3 15 Human 4.8 pIC50 = 4.8 Binding
Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
14762598 4314 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 374 4 2 3 3.2 O=C(CCN1CCN2Cc3[nH]c4ccccc4c3CC2C1)Nc1ccccc1 10.1021/jm00173a011
CHEMBL100865 4314 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 374 4 2 3 3.2 O=C(CCN1CCN2Cc3[nH]c4ccccc4c3CC2C1)Nc1ccccc1 10.1021/jm00173a011
4601 206747 35 None - 16 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 10.1021/jm300671m
CHEMBL1201023 206747 35 None - 16 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 10.1021/jm300671m
CHEMBL900 206747 35 None - 16 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 10.1021/jm300671m
11113605 10507 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 480 9 0 2 5.8 O=C(CCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
CHEMBL116735 10507 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 480 9 0 2 5.8 O=C(CCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
2031 120433 31 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
ChEMBL 311 8 0 3 3.7 CCN(CC)CCOC(=O)C(c1ccccc1)c1ccccc1 10.1021/jm300671m
CHEMBL353846 120433 31 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
ChEMBL 311 8 0 3 3.7 CCN(CC)CCOC(=O)C(c1ccccc1)c1ccccc1 10.1021/jm300671m
2726 919 68 None -2 72 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 919 68 None -2 72 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 919 68 None -2 72 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 919 68 None -2 72 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 919 68 None -2 72 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
155536195 172164 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 504 7 1 5 5.6 CCOc1ccccc1OCC(O)CN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/j.bmcl.2019.126712
CHEMBL4473399 172164 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 504 7 1 5 5.6 CCOc1ccccc1OCC(O)CN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/j.bmcl.2019.126712
1605 2342 117 None -2 4 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 nan
3957 2342 117 None -2 4 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 nan
7216 2342 117 None -2 4 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 nan
CHEMBL998 2342 117 None -2 4 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 nan
DB00455 2342 117 None -2 4 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 nan
23027035 198547 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptorDisplacement of [3H]pyrilamine from human histamine H1 receptor
ChEMBL 367 5 2 5 3.3 Cc1ccc(C(=O)N[C@H]2CC[C@@H](Nc3ncc(C)c(N(C)C)n3)CC2)cc1 10.1016/j.bmcl.2009.09.003
CHEMBL578170 198547 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptorDisplacement of [3H]pyrilamine from human histamine H1 receptor
ChEMBL 367 5 2 5 3.3 Cc1ccc(C(=O)N[C@H]2CC[C@@H](Nc3ncc(C)c(N(C)C)n3)CC2)cc1 10.1016/j.bmcl.2009.09.003
44392612 66685 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 474 9 1 6 5.2 COc1ccc(C(=O)O)c(OCCN2CCC(c3cn(Cc4ccoc4)c4ccccc34)CC2)c1 10.1016/j.bmcl.2004.12.008
CHEMBL185454 66685 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 474 9 1 6 5.2 COc1ccc(C(=O)O)c(OCCN2CCC(c3cn(Cc4ccoc4)c4ccccc34)CC2)c1 10.1016/j.bmcl.2004.12.008
126963284 144774 0 None - 1 Human 4.8 pIC50 = 4.8 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.
ChEMBL 311 1 1 3 4.2 CO[C@H]1Cc2ccccc2C(=C2CCNCC2)c2ccsc21 nan
CHEMBL3909134 144774 0 None - 1 Human 4.8 pIC50 = 4.8 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.
ChEMBL 311 1 1 3 4.2 CO[C@H]1Cc2ccccc2C(=C2CCNCC2)c2ccsc21 nan
121237834 147359 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 297 0 2 3 3.5 O[C@H]1Cc2ccccc2C(=C2CCNCC2)c2ccsc21 nan
CHEMBL3929465 147359 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 297 0 2 3 3.5 O[C@H]1Cc2ccccc2C(=C2CCNCC2)c2ccsc21 nan
14762588 4360 2 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 368 7 1 5 2.7 O=C(CCN1CCN(Cc2ccccc2)CC1)Nc1ccccc1[N+](=O)[O-] 10.1021/jm00173a011
CHEMBL101122 4360 2 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 368 7 1 5 2.7 O=C(CCN1CCN(Cc2ccccc2)CC1)Nc1ccccc1[N+](=O)[O-] 10.1021/jm00173a011
1224 1432 83 None -2 13 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
3100 1432 83 None -2 13 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
8980 1432 83 None -2 13 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
916 1432 83 None -2 13 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
CHEMBL657 1432 83 None -2 13 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
DB01075 1432 83 None -2 13 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
14762599 4197 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 419 5 2 5 3.1 O=C(CCN1CCN2Cc3[nH]c4ccccc4c3CC2C1)Nc1ccccc1[N+](=O)[O-] 10.1021/jm00173a011
CHEMBL100170 4197 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 419 5 2 5 3.1 O=C(CCN1CCN2Cc3[nH]c4ccccc4c3CC2C1)Nc1ccccc1[N+](=O)[O-] 10.1021/jm00173a011
2712 916 34 None -5 4 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl nan
3370 916 34 None -5 4 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl nan
594 916 34 None -5 4 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl nan
CHEMBL451 916 34 None -5 4 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl nan
DB00475 916 34 None -5 4 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl nan
10907460 9828 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 521 11 1 3 5.8 CCOc1ccc(CCNC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
CHEMBL113956 9828 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 521 11 1 3 5.8 CCOc1ccc(CCNC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
11340290 64364 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 466 11 1 6 4.6 CCOCCn1cc(C2CCN(CCOc3cc(OC)ccc3C(=O)O)CC2)c2ccccc21 10.1016/j.bmcl.2004.12.008
CHEMBL181278 64364 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 466 11 1 6 4.6 CCOCCn1cc(C2CCN(CCOc3cc(OC)ccc3C(=O)O)CC2)c2ccccc21 10.1016/j.bmcl.2004.12.008
11282005 66066 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 436 10 1 5 4.6 CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccccc21 10.1016/j.bmcl.2004.12.008
CHEMBL183706 66066 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 436 10 1 5 4.6 CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccccc21 10.1016/j.bmcl.2004.12.008
11730467 11028 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 476 10 0 2 6.0 O=C(CCCc1ccccc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
CHEMBL117537 11028 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 476 10 0 2 6.0 O=C(CCCc1ccccc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
54586257 62010 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 514 6 1 7 2.5 Cn1c(N2CCN(CC/C=C3/c4ccccc4CCc4ccc(CC(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmc.2011.03.003
CHEMBL1774505 62010 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 514 6 1 7 2.5 Cn1c(N2CCN(CC/C=C3/c4ccccc4CCc4ccc(CC(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmc.2011.03.003
11430513 84631 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 436 10 1 5 4.5 CCOCCn1cc(C2CCN(Cc3ccccc3OCC(=O)O)CC2)c2ccccc21 10.1021/jm0498203
CHEMBL222217 84631 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 436 10 1 5 4.5 CCOCCn1cc(C2CCN(Cc3ccccc3OCC(=O)O)CC2)c2ccccc21 10.1021/jm0498203
19426632 205858 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligandBinding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligand
ChEMBL 266 1 1 3 2.8 NCC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL83731 205858 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligandBinding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligand
ChEMBL 266 1 1 3 2.8 NCC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
1195 46 5 None - 1 Human 5.7 pIC50 = 5.7 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 221 3 2 2 2.2 NCCc1cnc([nH]1)c1cccc(c1)Cl 10.1021/jm030936t
14827778 46 5 None - 1 Human 5.7 pIC50 = 5.7 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 221 3 2 2 2.2 NCCc1cnc([nH]1)c1cccc(c1)Cl 10.1021/jm030936t
CHEMBL287052 46 5 None - 1 Human 5.7 pIC50 = 5.7 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 221 3 2 2 2.2 NCCc1cnc([nH]1)c1cccc(c1)Cl 10.1021/jm030936t
11346501 48264 1 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 279 14 2 2 4.6 NCCCCCCCCCCCCCCc1c[nH]cn1 10.1021/jm030936t
CHEMBL155314 48264 1 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 279 14 2 2 4.6 NCCCCCCCCCCCCCCc1c[nH]cn1 10.1021/jm030936t
11264275 119468 2 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 209 9 2 2 2.6 NCCCCCCCCCc1c[nH]cn1 10.1021/jm030936t
CHEMBL345185 119468 2 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 209 9 2 2 2.6 NCCCCCCCCCc1c[nH]cn1 10.1021/jm030936t
1164 1630 26 None - 12 Rat 4.7 pIC50 = 4.7 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1021/jm300671m
1626 1630 26 None - 12 Rat 4.7 pIC50 = 4.7 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1021/jm300671m
3345 1630 26 None - 12 Rat 4.7 pIC50 = 4.7 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1021/jm300671m
CHEMBL596 1630 26 None - 12 Rat 4.7 pIC50 = 4.7 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1021/jm300671m
DB00813 1630 26 None - 12 Rat 4.7 pIC50 = 4.7 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1021/jm300671m
44290349 178537 0 None 131 2 Rat 8.7 pIC50 = 8.7 Binding
Compound was evaluated for binding activity against [3H]pyrilamine as radioligand for Histamine H1 receptorCompound was evaluated for binding activity against [3H]pyrilamine as radioligand for Histamine H1 receptor
ChEMBL 411 5 2 6 2.1 O=C(c1ccc(F)cc1)C1CCN(CCn2c(=O)[nH]c3cc(O)ccc3c2=O)CC1 10.1021/jm00159a017
CHEMBL46683 178537 0 None 131 2 Rat 8.7 pIC50 = 8.7 Binding
Compound was evaluated for binding activity against [3H]pyrilamine as radioligand for Histamine H1 receptorCompound was evaluated for binding activity against [3H]pyrilamine as radioligand for Histamine H1 receptor
ChEMBL 411 5 2 6 2.1 O=C(c1ccc(F)cc1)C1CCN(CCn2c(=O)[nH]c3cc(O)ccc3c2=O)CC1 10.1021/jm00159a017
44319120 205778 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.
ChEMBL 312 2 0 3 3.5 CN(C)CC1CC2c3cccc(F)c3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL82966 205778 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.
ChEMBL 312 2 0 3 3.5 CN(C)CC1CC2c3cccc(F)c3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
10381889 107069 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity against Histamine H1 receptorBinding affinity against Histamine H1 receptor
ChEMBL 328 2 0 3 4.1 CN(C)CC1CC2c3ccccc3Cc3ccc(Cl)cc3N2O1 10.1016/s0960-894x(02)00796-5
CHEMBL315772 107069 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity against Histamine H1 receptorBinding affinity against Histamine H1 receptor
ChEMBL 328 2 0 3 4.1 CN(C)CC1CC2c3ccccc3Cc3ccc(Cl)cc3N2O1 10.1016/s0960-894x(02)00796-5
10381889 107069 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.
ChEMBL 328 2 0 3 4.1 CN(C)CC1CC2c3ccccc3Cc3ccc(Cl)cc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL315772 107069 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.
ChEMBL 328 2 0 3 4.1 CN(C)CC1CC2c3ccccc3Cc3ccc(Cl)cc3N2O1 10.1016/s0960-894x(01)00721-1
44318454 206009 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.
ChEMBL 312 2 0 3 3.5 CN(C)CC1CC2c3ccccc3Cc3ccc(F)cc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL84931 206009 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.
ChEMBL 312 2 0 3 3.5 CN(C)CC1CC2c3ccccc3Cc3ccc(F)cc3N2O1 10.1016/s0960-894x(01)00721-1
2286 3183 51 None -2 30 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
4927 3183 51 None -2 30 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
7282 3183 51 None -2 30 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
CHEMBL643 3183 51 None -2 30 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
DB01069 3183 51 None -2 30 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
155518920 170324 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 490 6 1 5 5.2 COc1ccccc1OCC(O)CN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/j.bmcl.2019.126712
CHEMBL4446961 170324 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 490 6 1 5 5.2 COc1ccccc1OCC(O)CN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/j.bmcl.2019.126712
155541322 173008 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 502 6 1 5 5.4 CC(=O)c1ccccc1OCC(O)CN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/j.bmcl.2019.126712
CHEMBL4518271 173008 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 502 6 1 5 5.4 CC(=O)c1ccccc1OCC(O)CN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/j.bmcl.2019.126712
10114407 123326 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 444 7 1 5 5.4 COc1ccc(CN2CCC(c3cn(Cc4ccoc4)c4ccccc34)CC2)cc1C(=O)O 10.1016/j.bmcl.2004.12.008
CHEMBL361625 123326 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 444 7 1 5 5.4 COc1ccc(CN2CCC(c3cn(Cc4ccoc4)c4ccccc34)CC2)cc1C(=O)O 10.1016/j.bmcl.2004.12.008
44332016 4244 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 261 0 1 2 2.4 ClN1CCN2Cc3[nH]c4ccccc4c3CC2C1 10.1021/jm00173a011
CHEMBL100442 4244 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 261 0 1 2 2.4 ClN1CCN2Cc3[nH]c4ccccc4c3CC2C1 10.1021/jm00173a011
13726483 95255 2 None - 0 Guinea pig 4.7 pIC50 = 4.7 Binding
Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex
ChEMBL 265 3 0 4 1.4 CN(C)CC[C@H]1CN(C)C(=S)c2cccnc2O1 10.1021/jm00108a012
CHEMBL25622 95255 2 None - 0 Guinea pig 4.7 pIC50 = 4.7 Binding
Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex
ChEMBL 265 3 0 4 1.4 CN(C)CC[C@H]1CN(C)C(=S)c2cccnc2O1 10.1021/jm00108a012
44392549 65356 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 450 10 1 5 5.4 CCCCn1cc(C2CCN(CCOc3cc(OC)ccc3C(=O)O)CC2)c2ccccc21 10.1016/j.bmcl.2004.12.008
CHEMBL182922 65356 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 450 10 1 5 5.4 CCCCn1cc(C2CCN(CCOc3cc(OC)ccc3C(=O)O)CC2)c2ccccc21 10.1016/j.bmcl.2004.12.008
739984 107204 15 None - 0 Guinea pig 5.7 pIC50 = 5.7 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 323 6 1 3 2.8 O=C(CCN1CCN(Cc2ccccc2)CC1)Nc1ccccc1 10.1021/jm00173a011
CHEMBL316616 107204 15 None - 0 Guinea pig 5.7 pIC50 = 5.7 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 323 6 1 3 2.8 O=C(CCN1CCN(Cc2ccccc2)CC1)Nc1ccccc1 10.1021/jm00173a011
9822631 122959 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 406 8 1 4 4.8 CCOCCn1cc(C2CCN(Cc3cccc(C(=O)O)c3)CC2)c2ccccc21 10.1021/jm0498203
CHEMBL360791 122959 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 406 8 1 4 4.8 CCOCCn1cc(C2CCN(Cc3cccc(C(=O)O)c3)CC2)c2ccccc21 10.1021/jm0498203
11202401 137107 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 478 11 1 6 4.8 CCOCCn1cc(C2CCN(CCOc3ccc(C(C)=O)cc3C(=O)O)CC2)c2ccccc21 10.1021/jm0498203
CHEMBL374755 137107 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 478 11 1 6 4.8 CCOCCn1cc(C2CCN(CCOc3ccc(C(C)=O)cc3C(=O)O)CC2)c2ccccc21 10.1021/jm0498203
2600 3779 74 None 1 13 Human 7.7 pIC50 = 7.7 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
2608 3779 74 None 1 13 Human 7.7 pIC50 = 7.7 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
5405 3779 74 None 1 13 Human 7.7 pIC50 = 7.7 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
CHEMBL17157 3779 74 None 1 13 Human 7.7 pIC50 = 7.7 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
DB00342 3779 74 None 1 13 Human 7.7 pIC50 = 7.7 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
10369004 13688 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Compound is evaluated for in vitro receptor binding affinity against H1 receptorCompound is evaluated for in vitro receptor binding affinity against H1 receptor
ChEMBL 508 7 0 8 2.5 Cn1c(=O)c2c(ncn2CCCN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)n(C)c1=O 10.1021/jm00020a018
CHEMBL1194812 13688 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Compound is evaluated for in vitro receptor binding affinity against H1 receptorCompound is evaluated for in vitro receptor binding affinity against H1 receptor
ChEMBL 508 7 0 8 2.5 Cn1c(=O)c2c(ncn2CCCN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)n(C)c1=O 10.1021/jm00020a018
CHEMBL553331 13688 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Compound is evaluated for in vitro receptor binding affinity against H1 receptorCompound is evaluated for in vitro receptor binding affinity against H1 receptor
ChEMBL 508 7 0 8 2.5 Cn1c(=O)c2c(ncn2CCCN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)n(C)c1=O 10.1021/jm00020a018
11166846 84301 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 450 10 1 5 4.9 CCOCCn1cc(C2CCN(CCOc3ccc(C)cc3C(=O)O)CC2)c2ccccc21 10.1021/jm0498203
CHEMBL221462 84301 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 450 10 1 5 4.9 CCOCCn1cc(C2CCN(CCOc3ccc(C)cc3C(=O)O)CC2)c2ccccc21 10.1021/jm0498203
11238716 84292 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 592 10 1 5 6.2 CCOCCn1cc(C2CCN(CCOc3c(Br)cc(Br)cc3C(=O)O)CC2)c2ccccc21 10.1021/jm0498203
CHEMBL221414 84292 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 592 10 1 5 6.2 CCOCCn1cc(C2CCN(CCOc3c(Br)cc(Br)cc3C(=O)O)CC2)c2ccccc21 10.1021/jm0498203
10160717 168398 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 444 8 1 5 5.2 O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccoc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.12.008
CHEMBL434709 168398 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 444 8 1 5 5.2 O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccoc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.12.008
135398737 958 93 None -4 89 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligandBinding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991005d
38 958 93 None -4 89 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligandBinding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991005d
722 958 93 None -4 89 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligandBinding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991005d
CHEMBL42 958 93 None -4 89 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligandBinding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991005d
DB00363 958 93 None -4 89 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligandBinding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991005d
45267326 195966 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 535 7 1 9 2.9 Cn1c(N2CCCN(CCCN3c4ccccc4Sc4ccc(CC(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmcl.2009.03.124
CHEMBL559665 195966 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 535 7 1 9 2.9 Cn1c(N2CCCN(CCCN3c4ccccc4Sc4ccc(CC(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmcl.2009.03.124
45268181 196645 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 521 6 1 9 3.0 Cn1c(N2CCCN(CCCN3c4ccccc4Sc4ccc(C(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmcl.2009.03.124
CHEMBL564370 196645 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 521 6 1 9 3.0 Cn1c(N2CCCN(CCCN3c4ccccc4Sc4ccc(C(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmcl.2009.03.124
135398737 958 93 None -4 89 Rat 7.6 pIC50 = 7.6 Binding
Inhibitory binding of [3H]mepyramine to histamine H1 receptors in rat brain membranesInhibitory binding of [3H]mepyramine to histamine H1 receptors in rat brain membranes
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9704457
38 958 93 None -4 89 Rat 7.6 pIC50 = 7.6 Binding
Inhibitory binding of [3H]mepyramine to histamine H1 receptors in rat brain membranesInhibitory binding of [3H]mepyramine to histamine H1 receptors in rat brain membranes
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9704457
722 958 93 None -4 89 Rat 7.6 pIC50 = 7.6 Binding
Inhibitory binding of [3H]mepyramine to histamine H1 receptors in rat brain membranesInhibitory binding of [3H]mepyramine to histamine H1 receptors in rat brain membranes
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9704457
CHEMBL42 958 93 None -4 89 Rat 7.6 pIC50 = 7.6 Binding
Inhibitory binding of [3H]mepyramine to histamine H1 receptors in rat brain membranesInhibitory binding of [3H]mepyramine to histamine H1 receptors in rat brain membranes
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9704457
DB00363 958 93 None -4 89 Rat 7.6 pIC50 = 7.6 Binding
Inhibitory binding of [3H]mepyramine to histamine H1 receptors in rat brain membranesInhibitory binding of [3H]mepyramine to histamine H1 receptors in rat brain membranes
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9704457
1530 2182 50 None -5 21 Human 5.6 pIC50 = 5.6 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
3827 2182 50 None -5 21 Human 5.6 pIC50 = 5.6 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
7206 2182 50 None -5 21 Human 5.6 pIC50 = 5.6 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
CHEMBL534 2182 50 None -5 21 Human 5.6 pIC50 = 5.6 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
DB00920 2182 50 None -5 21 Human 5.6 pIC50 = 5.6 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
1530 2182 50 None -5 21 Human 5.6 pIC50 = 5.6 Binding
Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
3827 2182 50 None -5 21 Human 5.6 pIC50 = 5.6 Binding
Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
7206 2182 50 None -5 21 Human 5.6 pIC50 = 5.6 Binding
Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
CHEMBL534 2182 50 None -5 21 Human 5.6 pIC50 = 5.6 Binding
Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
DB00920 2182 50 None -5 21 Human 5.6 pIC50 = 5.6 Binding
Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
126963283 160963 0 None - 1 Human 4.6 pIC50 = 4.6 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.
ChEMBL 311 1 1 3 4.2 CO[C@@H]1Cc2ccccc2C(=C2CCNCC2)c2ccsc21 nan
CHEMBL4115677 160963 0 None - 1 Human 4.6 pIC50 = 4.6 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.
ChEMBL 311 1 1 3 4.2 CO[C@@H]1Cc2ccccc2C(=C2CCNCC2)c2ccsc21 nan
11638166 8147 0 None - 1 Human 4.6 pIC50 = 4.6 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 310 5 0 3 4.6 CC(c1ccncc1)c1c(CCN(C)C)sc2ccccc12 10.1016/j.bmcl.2010.01.134
CHEMBL1091790 8147 0 None - 1 Human 4.6 pIC50 = 4.6 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 310 5 0 3 4.6 CC(c1ccncc1)c1c(CCN(C)C)sc2ccccc12 10.1016/j.bmcl.2010.01.134
11335478 160965 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 297 0 2 3 3.5 O[C@@H]1Cc2ccccc2C(=C2CCNCC2)c2ccsc21 nan
CHEMBL4115693 160965 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 297 0 2 3 3.5 O[C@@H]1Cc2ccccc2C(=C2CCNCC2)c2ccsc21 nan
9802248 166243 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 420 9 1 4 5.4 CCCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccccc21 10.1016/j.bmcl.2004.12.008
CHEMBL426786 166243 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 420 9 1 4 5.4 CCCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccccc21 10.1016/j.bmcl.2004.12.008
2274 3173 58 None -3 31 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917 3173 58 None -3 31 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
7279 3173 58 None -3 31 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL728 3173 58 None -3 31 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
DB00433 3173 58 None -3 31 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
14842833 93303 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex
ChEMBL 275 5 0 3 3.2 CN(C)CCC(c1ccccn1)c1ccc(Cl)cn1 10.1021/jm00108a012
CHEMBL24517 93303 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex
ChEMBL 275 5 0 3 3.2 CN(C)CCC(c1ccccn1)c1ccc(Cl)cn1 10.1021/jm00108a012
44392620 126823 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 524 9 1 6 6.4 COc1ccc(C(=O)O)c(OCCN2CCC(c3cn(Cc4ccc(Cl)s4)c4ccccc34)CC2)c1 10.1016/j.bmcl.2004.12.008
CHEMBL365450 126823 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 524 9 1 6 6.4 COc1ccc(C(=O)O)c(OCCN2CCC(c3cn(Cc4ccc(Cl)s4)c4ccccc34)CC2)c1 10.1016/j.bmcl.2004.12.008
10003369 84336 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 440 8 1 5 4.5 COCCn1cc(C2CCN(Cc3ccc(OC)c(C(=O)O)c3)CC2)c2ccc(F)cc21 10.1021/jm0498203
CHEMBL221678 84336 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 440 8 1 5 4.5 COCCn1cc(C2CCN(Cc3ccc(OC)c(C(=O)O)c3)CC2)c2ccc(F)cc21 10.1021/jm0498203
2389 3331 118 None -46 67 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
5073 3331 118 None -46 67 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
96 3331 118 None -46 67 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
CHEMBL85 3331 118 None -46 67 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
DB00734 3331 118 None -46 67 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
11333854 51605 1 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 237 11 2 2 3.4 NCCCCCCCCCCCc1c[nH]cn1 10.1021/jm030936t
CHEMBL158352 51605 1 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 237 11 2 2 3.4 NCCCCCCCCCCCc1c[nH]cn1 10.1021/jm030936t
11241807 51010 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 234 10 1 2 3.7 NCCCCCCCCCCc1cccnc1 10.1021/jm030936t
CHEMBL157842 51010 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 234 10 1 2 3.7 NCCCCCCCCCCc1cccnc1 10.1021/jm030936t
11253315 121965 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 234 10 1 2 3.7 NCCCCCCCCCCc1ccncc1 10.1021/jm030936t
CHEMBL359122 121965 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 234 10 1 2 3.7 NCCCCCCCCCCc1ccncc1 10.1021/jm030936t
54586252 61997 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 519 7 1 9 2.0 Cn1c(N2CCN(CCCN3c4ccccc4COc4ccc(CC(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmc.2011.03.003
CHEMBL1774492 61997 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 519 7 1 9 2.0 Cn1c(N2CCN(CCCN3c4ccccc4COc4ccc(CC(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmc.2011.03.003
127049862 140257 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Antagonistic activity at histamine1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine1 receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 425 8 1 5 4.4 CNC(=O)c1cccc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)c1 10.1016/j.bmcl.2016.04.087
CHEMBL3805559 140257 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Antagonistic activity at histamine1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine1 receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 425 8 1 5 4.4 CNC(=O)c1cccc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)c1 10.1016/j.bmcl.2016.04.087
44461800 205297 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligandBinding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligand
ChEMBL 336 2 0 4 3.2 c1ccc2c(c1)Cc1ccccc1N1OC(CN3CCOCC3)CC21 10.1016/s0960-894x(01)00721-1
CHEMBL79249 205297 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligandBinding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligand
ChEMBL 336 2 0 4 3.2 c1ccc2c(c1)Cc1ccccc1N1OC(CN3CCOCC3)CC21 10.1016/s0960-894x(01)00721-1
1427 2013 54 None -5 27 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to histamine H1 receptor (unknown origin) by radioligand binding assayBinding affinity to histamine H1 receptor (unknown origin) by radioligand binding assay
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1021/jm400856t
357 2013 54 None -5 27 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to histamine H1 receptor (unknown origin) by radioligand binding assayBinding affinity to histamine H1 receptor (unknown origin) by radioligand binding assay
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1021/jm400856t
3696 2013 54 None -5 27 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to histamine H1 receptor (unknown origin) by radioligand binding assayBinding affinity to histamine H1 receptor (unknown origin) by radioligand binding assay
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1021/jm400856t
CHEMBL11 2013 54 None -5 27 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to histamine H1 receptor (unknown origin) by radioligand binding assayBinding affinity to histamine H1 receptor (unknown origin) by radioligand binding assay
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1021/jm400856t
DB00458 2013 54 None -5 27 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to histamine H1 receptor (unknown origin) by radioligand binding assayBinding affinity to histamine H1 receptor (unknown origin) by radioligand binding assay
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1021/jm400856t
6075 150108 42 None 2 16 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
CHEMBL395110 150108 42 None 2 16 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
155545724 173471 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 526 6 1 5 5.5 COc1c(OCC(O)CN2CCC(=C3c4ccc(Cl)cc4CCc4cccnc43)CC2)ccc(F)c1F 10.1016/j.bmcl.2019.126712
CHEMBL4529928 173471 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 526 6 1 5 5.5 COc1c(OCC(O)CN2CCC(=C3c4ccc(Cl)cc4CCc4cccnc43)CC2)ccc(F)c1F 10.1016/j.bmcl.2019.126712
44392599 65175 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 390 7 1 3 5.5 CCCCn1cc(C2CCN(Cc3cccc(C(=O)O)c3)CC2)c2ccccc21 10.1016/j.bmcl.2004.12.008
CHEMBL182474 65175 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 390 7 1 3 5.5 CCCCn1cc(C2CCN(Cc3cccc(C(=O)O)c3)CC2)c2ccccc21 10.1016/j.bmcl.2004.12.008
1353 1911 93 None -489 83 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
3559 1911 93 None -489 83 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
86 1911 93 None -489 83 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
CHEMBL54 1911 93 None -489 83 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
DB00502 1911 93 None -489 83 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
11785584 136964 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 512 8 1 5 6.5 O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccc(Cl)s3)c3cc(F)ccc23)CC1 10.1021/jm0498203
CHEMBL374459 136964 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 512 8 1 5 6.5 O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccc(Cl)s3)c3cc(F)ccc23)CC1 10.1021/jm0498203
22322323 196017 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 440 7 1 7 2.7 Cn1c(NCCCN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)cc(=O)n(C)c1=O 10.1016/j.bmcl.2009.03.124
CHEMBL560120 196017 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 440 7 1 7 2.7 Cn1c(NCCCN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)cc(=O)n(C)c1=O 10.1016/j.bmcl.2009.03.124
3191 102858 97 None 2 25 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
CHEMBL305660 102858 97 None 2 25 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
155549722 173849 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 494 5 1 4 5.8 OC(COc1ccccc1Cl)CN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/j.bmcl.2019.126712
CHEMBL4539056 173849 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 494 5 1 4 5.8 OC(COc1ccccc1Cl)CN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/j.bmcl.2019.126712
10894144 110559 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 377 7 0 4 3.5 N#Cc1ccc(CCOC(=O)N2CCN(CCCc3ccccc3)CC2)cc1 10.1021/jm010878g
CHEMBL325258 110559 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 377 7 0 4 3.5 N#Cc1ccc(CCOC(=O)N2CCN(CCCc3ccccc3)CC2)cc1 10.1021/jm010878g
3038952 108911 2 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 241 0 1 2 1.8 CN1CCN2Cc3[nH]c4ccccc4c3CC2C1 10.1021/jm00173a011
CHEMBL321104 108911 2 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 241 0 1 2 1.8 CN1CCN2Cc3[nH]c4ccccc4c3CC2C1 10.1021/jm00173a011
76319448 85388 2 None - 0 Guinea pig 4.5 pIC50 = 4.5 Binding
Inhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challengeInhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challenge
ChEMBL 221 4 4 4 0.7 CC(CO)(CO)Nc1nc2ccccc2[nH]1 10.1007/s00044-008-9119-y
CHEMBL2262478 85388 2 None - 0 Guinea pig 4.5 pIC50 = 4.5 Binding
Inhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challengeInhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challenge
ChEMBL 221 4 4 4 0.7 CC(CO)(CO)Nc1nc2ccccc2[nH]1 10.1007/s00044-008-9119-y
1605 2342 117 None -2 4 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against histamine H1 receptorInhibitory concentration against histamine H1 receptor
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1021/jm058225d
3957 2342 117 None -2 4 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against histamine H1 receptorInhibitory concentration against histamine H1 receptor
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1021/jm058225d
7216 2342 117 None -2 4 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against histamine H1 receptorInhibitory concentration against histamine H1 receptor
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1021/jm058225d
CHEMBL998 2342 117 None -2 4 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against histamine H1 receptorInhibitory concentration against histamine H1 receptor
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1021/jm058225d
DB00455 2342 117 None -2 4 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against histamine H1 receptorInhibitory concentration against histamine H1 receptor
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1021/jm058225d
2812 4779 101 None -28 34 Human 4.5 pIC50 = 4.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 4779 101 None -28 34 Human 4.5 pIC50 = 4.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
2600 3779 74 None -3 13 Guinea pig 6.5 pIC50 = 6.5 Binding
Inhibitory activity against Tritiated [3H]- mepyramine binding to histamine H1 receptor in guinea pig cerebral cortexInhibitory activity against Tritiated [3H]- mepyramine binding to histamine H1 receptor in guinea pig cerebral cortex
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1021/jm00121a022
2608 3779 74 None -3 13 Guinea pig 6.5 pIC50 = 6.5 Binding
Inhibitory activity against Tritiated [3H]- mepyramine binding to histamine H1 receptor in guinea pig cerebral cortexInhibitory activity against Tritiated [3H]- mepyramine binding to histamine H1 receptor in guinea pig cerebral cortex
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1021/jm00121a022
5405 3779 74 None -3 13 Guinea pig 6.5 pIC50 = 6.5 Binding
Inhibitory activity against Tritiated [3H]- mepyramine binding to histamine H1 receptor in guinea pig cerebral cortexInhibitory activity against Tritiated [3H]- mepyramine binding to histamine H1 receptor in guinea pig cerebral cortex
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1021/jm00121a022
CHEMBL17157 3779 74 None -3 13 Guinea pig 6.5 pIC50 = 6.5 Binding
Inhibitory activity against Tritiated [3H]- mepyramine binding to histamine H1 receptor in guinea pig cerebral cortexInhibitory activity against Tritiated [3H]- mepyramine binding to histamine H1 receptor in guinea pig cerebral cortex
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1021/jm00121a022
DB00342 3779 74 None -3 13 Guinea pig 6.5 pIC50 = 6.5 Binding
Inhibitory activity against Tritiated [3H]- mepyramine binding to histamine H1 receptor in guinea pig cerebral cortexInhibitory activity against Tritiated [3H]- mepyramine binding to histamine H1 receptor in guinea pig cerebral cortex
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1021/jm00121a022
10141470 123557 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 494 8 1 5 6.4 O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccc(Cl)s3)c3ccccc23)CC1 10.1016/j.bmcl.2004.12.008
CHEMBL361805 123557 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 494 8 1 5 6.4 O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccc(Cl)s3)c3ccccc23)CC1 10.1016/j.bmcl.2004.12.008
153996 112668 2 None - 3 Human 8.5 pIC50 = 8.5 Binding
Inhibitory concentration against histamine H1 receptorInhibitory concentration against histamine H1 receptor
ChEMBL 639 10 1 6 5.7 COc1cc(C(=O)N2CC[C@](CCN3CCC(C(N)=O)(c4ccccc4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC 10.1021/jm058225d
CHEMBL330366 112668 2 None - 3 Human 8.5 pIC50 = 8.5 Binding
Inhibitory concentration against histamine H1 receptorInhibitory concentration against histamine H1 receptor
ChEMBL 639 10 1 6 5.7 COc1cc(C(=O)N2CC[C@](CCN3CCC(C(N)=O)(c4ccccc4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC 10.1021/jm058225d
CHEMBL539021 112668 2 None - 3 Human 8.5 pIC50 = 8.5 Binding
Inhibitory concentration against histamine H1 receptorInhibitory concentration against histamine H1 receptor
ChEMBL 639 10 1 6 5.7 COc1cc(C(=O)N2CC[C@](CCN3CCC(C(N)=O)(c4ccccc4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC 10.1021/jm058225d
19426644 107174 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligandBinding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligand
ChEMBL 320 2 0 3 3.9 c1ccc2c(c1)Cc1ccccc1N1OC(CN3CCCC3)CC21 10.1016/s0960-894x(01)00721-1
CHEMBL316438 107174 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligandBinding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligand
ChEMBL 320 2 0 3 3.9 c1ccc2c(c1)Cc1ccccc1N1OC(CN3CCCC3)CC21 10.1016/s0960-894x(01)00721-1
1201549 597 24 None -1 20 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
333 597 24 None -1 20 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
7601 597 24 None -1 20 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL1201203 597 24 None -1 20 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL438151 597 24 None -1 20 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
DB00245 597 24 None -1 20 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
1227 2489 43 None -2 12 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells after 3 hrsDisplacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells after 3 hrs
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmcl.2013.01.025
2331 2489 43 None -2 12 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells after 3 hrsDisplacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells after 3 hrs
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmcl.2013.01.025
3957 2489 43 None -2 12 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells after 3 hrsDisplacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells after 3 hrs
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmcl.2013.01.025
4992 2489 43 None -2 12 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells after 3 hrsDisplacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells after 3 hrs
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmcl.2013.01.025
CHEMBL511 2489 43 None -2 12 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells after 3 hrsDisplacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells after 3 hrs
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmcl.2013.01.025
DB06691 2489 43 None -2 12 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells after 3 hrsDisplacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells after 3 hrs
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmcl.2013.01.025
45269436 196656 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 422 5 0 5 4.3 CN(C1CCOCC1)C1CCN(c2nc3ccccc3n2Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2009.05.086
CHEMBL564446 196656 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 422 5 0 5 4.3 CN(C1CCOCC1)C1CCN(c2nc3ccccc3n2Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2009.05.086
135 2532 43 None -1 58 Human 8.5 pIC50 = 8.5 Binding
Binding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligandBinding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligand
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
1796 2532 43 None -1 58 Human 8.5 pIC50 = 8.5 Binding
Binding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligandBinding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligand
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
4184 2532 43 None -1 58 Human 8.5 pIC50 = 8.5 Binding
Binding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligandBinding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligand
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
CHEMBL6437 2532 43 None -1 58 Human 8.5 pIC50 = 8.5 Binding
Binding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligandBinding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligand
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
DB06148 2532 43 None -1 58 Human 8.5 pIC50 = 8.5 Binding
Binding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligandBinding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligand
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
2284 3182 33 None 1 29 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
4926 3182 33 None 1 29 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
7281 3182 33 None 1 29 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
CHEMBL564 3182 33 None 1 29 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
DB00420 3182 33 None 1 29 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
11539632 70561 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibitory concentration against histamine H1 receptorInhibitory concentration against histamine H1 receptor
ChEMBL 447 8 1 5 4.8 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL194837 70561 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibitory concentration against histamine H1 receptorInhibitory concentration against histamine H1 receptor
ChEMBL 447 8 1 5 4.8 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
155568607 176112 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 490 6 1 5 5.2 COc1ccccc1OC[C@H](O)CN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/j.bmcl.2019.126712
CHEMBL4591702 176112 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 490 6 1 5 5.2 COc1ccccc1OC[C@H](O)CN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/j.bmcl.2019.126712
277 1301 62 None -2 50 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
2913 1301 62 None -2 50 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
765 1301 62 None -2 50 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
CHEMBL516 1301 62 None -2 50 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
DB00434 1301 62 None -2 50 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
1227 2489 43 None -2 12 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
2331 2489 43 None -2 12 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
3957 2489 43 None -2 12 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
4992 2489 43 None -2 12 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
CHEMBL511 2489 43 None -2 12 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
DB06691 2489 43 None -2 12 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
44319133 106941 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.
ChEMBL 312 2 0 3 3.5 CN(C)CC1CC2c3cc(F)ccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL314885 106941 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.
ChEMBL 312 2 0 3 3.5 CN(C)CC1CC2c3cc(F)ccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
10103 3416 72 None 25 3 Human 8.4 pIC50 = 8.4 Binding
Inhibitory concentration against histamine H1 receptorInhibitory concentration against histamine H1 receptor
ChEMBL 415 2 0 3 5.6 Cc1cncc(c1)CN1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1021/jm058225d
133017 3416 72 None 25 3 Human 8.4 pIC50 = 8.4 Binding
Inhibitory concentration against histamine H1 receptorInhibitory concentration against histamine H1 receptor
ChEMBL 415 2 0 3 5.6 Cc1cncc(c1)CN1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1021/jm058225d
2413 3416 72 None 25 3 Human 8.4 pIC50 = 8.4 Binding
Inhibitory concentration against histamine H1 receptorInhibitory concentration against histamine H1 receptor
ChEMBL 415 2 0 3 5.6 Cc1cncc(c1)CN1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1021/jm058225d
CHEMBL91397 3416 72 None 25 3 Human 8.4 pIC50 = 8.4 Binding
Inhibitory concentration against histamine H1 receptorInhibitory concentration against histamine H1 receptor
ChEMBL 415 2 0 3 5.6 Cc1cncc(c1)CN1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1021/jm058225d
DB11614 3416 72 None 25 3 Human 8.4 pIC50 = 8.4 Binding
Inhibitory concentration against histamine H1 receptorInhibitory concentration against histamine H1 receptor
ChEMBL 415 2 0 3 5.6 Cc1cncc(c1)CN1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1021/jm058225d
13726485 91424 1 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
Inhibition of [3H]mepyramine binding to the histamine receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the histamine receptor in guinea pig cortex
ChEMBL 265 3 0 4 1.4 CN(C)CC[C@@H]1CN(C)C(=S)c2cccnc2O1 10.1021/jm00108a012
CHEMBL24031 91424 1 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
Inhibition of [3H]mepyramine binding to the histamine receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the histamine receptor in guinea pig cortex
ChEMBL 265 3 0 4 1.4 CN(C)CC[C@@H]1CN(C)C(=S)c2cccnc2O1 10.1021/jm00108a012
11247290 136703 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 424 8 1 4 4.9 CCOCCn1cc(C2CCN(Cc3ccc(F)c(C(=O)O)c3)CC2)c2ccccc21 10.1021/jm0498203
CHEMBL374059 136703 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 424 8 1 4 4.9 CCOCCn1cc(C2CCN(Cc3ccc(F)c(C(=O)O)c3)CC2)c2ccccc21 10.1021/jm0498203
9918576 207337 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against histamine H1 receptorInhibitory concentration against histamine H1 receptor
ChEMBL 764 14 0 10 7.0 COc1ccc(C2(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C2)cc1OC 10.1021/jm058225d
CHEMBL93556 207337 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against histamine H1 receptorInhibitory concentration against histamine H1 receptor
ChEMBL 764 14 0 10 7.0 COc1ccc(C2(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C2)cc1OC 10.1021/jm058225d
10420190 206760 0 None - 3 Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 195 8 2 2 2.3 NCCCCCCCCc1c[nH]cn1 10.1021/jm030936t
CHEMBL90063 206760 0 None - 3 Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 195 8 2 2 2.3 NCCCCCCCCc1c[nH]cn1 10.1021/jm030936t
10660 14416 58 None 2 12 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 469 6 1 7 3.0 CN(C)CCOC(c1ccccc1)c1ccccc1.Cn1c(=O)c2[nH]c(Cl)nc2n(C)c1=O nan
CHEMBL1200406 14416 58 None 2 12 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 469 6 1 7 3.0 CN(C)CCOC(c1ccccc1)c1ccccc1.Cn1c(=O)c2[nH]c(Cl)nc2n(C)c1=O nan
2771 195017 74 None -2 27 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 nan
CHEMBL1200781 195017 74 None -2 27 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 nan
CHEMBL549 195017 74 None -2 27 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 nan
11259138 85012 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 436 10 1 5 4.5 CCOCCn1cc(C2CCN(Cc3ccc(OCC(=O)O)cc3)CC2)c2ccccc21 10.1021/jm0498203
CHEMBL223882 85012 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 436 10 1 5 4.5 CCOCCn1cc(C2CCN(Cc3ccc(OCC(=O)O)cc3)CC2)c2ccccc21 10.1021/jm0498203
45272487 196402 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 547 7 1 9 3.4 Cn1c(N2CCCN(CCCN3c4ccccc4Sc4ccc(/C=C\C(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmcl.2009.03.124
CHEMBL562792 196402 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 547 7 1 9 3.4 Cn1c(N2CCCN(CCCN3c4ccccc4Sc4ccc(/C=C\C(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmcl.2009.03.124
54582402 62008 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 502 5 1 8 2.3 Cn1c(N2CCN(CC/C=C3/c4ccccc4COc4ccc(C(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmc.2011.03.003
CHEMBL1774503 62008 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 502 5 1 8 2.3 Cn1c(N2CCN(CC/C=C3/c4ccccc4COc4ccc(C(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmc.2011.03.003
11211919 84753 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 406 8 1 4 4.8 CCOCCn1cc(C2CCN(Cc3ccccc3C(=O)O)CC2)c2ccccc21 10.1021/jm0498203
CHEMBL222984 84753 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 406 8 1 4 4.8 CCOCCn1cc(C2CCN(Cc3ccccc3C(=O)O)CC2)c2ccccc21 10.1021/jm0498203
10205121 66692 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 464 6 1 4 6.5 O=C(O)c1cccc(CN2CCC(c3cn(Cc4ccc(Cl)s4)c4ccccc34)CC2)c1 10.1016/j.bmcl.2004.12.008
CHEMBL185489 66692 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 464 6 1 4 6.5 O=C(O)c1cccc(CN2CCC(c3cn(Cc4ccc(Cl)s4)c4ccccc34)CC2)c1 10.1016/j.bmcl.2004.12.008
11340290 64364 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 466 11 1 6 4.6 CCOCCn1cc(C2CCN(CCOc3cc(OC)ccc3C(=O)O)CC2)c2ccccc21 10.1021/jm0498203
CHEMBL181278 64364 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 466 11 1 6 4.6 CCOCCn1cc(C2CCN(CCOc3cc(OC)ccc3C(=O)O)CC2)c2ccccc21 10.1021/jm0498203
14762564 4311 2 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 449 6 1 3 2.8 O=C(NCCN1CCN(Cc2ccccc2)CC1)c1ccccc1I 10.1021/jm00173a011
CHEMBL100858 4311 2 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 449 6 1 3 2.8 O=C(NCCN1CCN(Cc2ccccc2)CC1)c1ccccc1I 10.1021/jm00173a011
11363750 84630 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 484 8 1 4 5.5 CCOCCn1cc(C2CCN(Cc3cc(C(=O)O)ccc3Br)CC2)c2ccccc21 10.1021/jm0498203
CHEMBL222214 84630 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 484 8 1 4 5.5 CCOCCn1cc(C2CCN(Cc3cc(C(=O)O)ccc3Br)CC2)c2ccccc21 10.1021/jm0498203
45270753 195400 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 521 7 1 9 3.0 Cn1c(N2CCN(CCCCN3c4ccccc4Sc4ccc(C(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmcl.2009.03.124
CHEMBL552057 195400 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 521 7 1 9 3.0 Cn1c(N2CCN(CCCCN3c4ccccc4Sc4ccc(C(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmcl.2009.03.124
11659592 8143 0 None - 1 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 310 5 0 3 4.6 C[C@H](c1cccnc1)c1c(CCN(C)C)sc2ccccc12 10.1016/j.bmcl.2010.01.134
CHEMBL1091777 8143 0 None - 1 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 310 5 0 3 4.6 C[C@H](c1cccnc1)c1c(CCN(C)C)sc2ccccc12 10.1016/j.bmcl.2010.01.134
10161929 137187 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 464 9 1 6 4.4 O=C(O)c1ccccc1OCCN1CCC(c2cn(CCC3OCCO3)c3ccccc23)CC1 10.1021/jm0498203
CHEMBL374869 137187 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 464 9 1 6 4.4 O=C(O)c1ccccc1OCCN1CCC(c2cn(CCC3OCCO3)c3ccccc23)CC1 10.1021/jm0498203
149227688 174629 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 544 6 1 5 6.1 OC(COc1ccccc1OC(F)(F)F)CN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/j.bmcl.2019.126712
CHEMBL4557928 174629 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 544 6 1 5 6.1 OC(COc1ccccc1OC(F)(F)F)CN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/j.bmcl.2019.126712
44566054 187141 2 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cells
ChEMBL 350 9 0 3 5.1 CCN(CC)CCCCCCn1c2ccccc2c(=O)c2ccccc21 10.1128/aac.00669-07
CHEMBL491889 187141 2 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cells
ChEMBL 350 9 0 3 5.1 CCN(CC)CCCCCCn1c2ccccc2c(=O)c2ccccc21 10.1128/aac.00669-07
213 3853 55 None -8 44 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
2717 3853 55 None -8 44 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
5533 3853 55 None -8 44 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
CHEMBL621 3853 55 None -8 44 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
DB00656 3853 55 None -8 44 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
44332061 4415 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 257 1 1 3 1.8 CON1CCN2Cc3[nH]c4ccccc4c3CC2C1 10.1021/jm00173a011
CHEMBL101490 4415 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 257 1 1 3 1.8 CON1CCN2Cc3[nH]c4ccccc4c3CC2C1 10.1021/jm00173a011
44392588 66653 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 494 7 1 5 6.5 COc1ccc(CN2CCC(c3cn(Cc4ccc(Cl)s4)c4ccccc34)CC2)cc1C(=O)O 10.1016/j.bmcl.2004.12.008
CHEMBL185289 66653 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 494 7 1 5 6.5 COc1ccc(CN2CCC(c3cn(Cc4ccc(Cl)s4)c4ccccc34)CC2)cc1C(=O)O 10.1016/j.bmcl.2004.12.008
10139592 85004 0 None - 0 Guinea pig 7.4 pIC50 = 7.4 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 462 8 1 5 5.4 O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccco3)c3cc(F)ccc23)CC1 10.1021/jm0498203
CHEMBL223837 85004 0 None - 0 Guinea pig 7.4 pIC50 = 7.4 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 462 8 1 5 5.4 O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccco3)c3cc(F)ccc23)CC1 10.1021/jm0498203
45270750 195305 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 507 6 1 9 2.6 Cn1c(N2CCN(CCCN3c4ccccc4Sc4ccc(C(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmcl.2009.03.124
CHEMBL551457 195305 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 507 6 1 9 2.6 Cn1c(N2CCN(CCCN3c4ccccc4Sc4ccc(C(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmcl.2009.03.124
44319098 205785 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.
ChEMBL 362 2 0 3 4.4 CN(C)CC1CC2c3cccc(C(F)(F)F)c3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL83073 205785 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.
ChEMBL 362 2 0 3 4.4 CN(C)CC1CC2c3cccc(C(F)(F)F)c3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
44332031 208113 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 272 1 1 3 1.4 O=[N+]([O-])N1CCN2Cc3[nH]c4ccccc4c3CC2C1 10.1021/jm00173a011
CHEMBL97938 208113 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 272 1 1 3 1.4 O=[N+]([O-])N1CCN2Cc3[nH]c4ccccc4c3CC2C1 10.1021/jm00173a011
6726 1280 51 None 3 13 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
7151 1280 51 None 3 13 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
749 1280 51 None 3 13 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
CHEMBL648 1280 51 None 3 13 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
DB01176 1280 51 None 3 13 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
2337 3256 77 None 1 62 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
50 3256 77 None 1 62 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
5002 3256 77 None 1 62 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
CHEMBL716 3256 77 None 1 62 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
DB01224 3256 77 None 1 62 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
2762 3863 31 None -9 2 Human 7.4 pIC50 = 7.4 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 10.1021/jm030936t
5587 3863 31 None -9 2 Human 7.4 pIC50 = 7.4 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 10.1021/jm030936t
7318 3863 31 None -9 2 Human 7.4 pIC50 = 7.4 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 10.1021/jm030936t
CHEMBL1241 3863 31 None -9 2 Human 7.4 pIC50 = 7.4 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 10.1021/jm030936t
DB00792 3863 31 None -9 2 Human 7.4 pIC50 = 7.4 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 10.1021/jm030936t
10140544 141639 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 478 9 1 6 4.4 O=C(O)c1ccccc1OCCN1CCC(c2cn(CCC3COCCO3)c3ccccc23)CC1 10.1021/jm0498203
CHEMBL385311 141639 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 478 9 1 6 4.4 O=C(O)c1ccccc1OCCN1CCC(c2cn(CCC3COCCO3)c3ccccc23)CC1 10.1021/jm0498203
23027211 197250 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptorDisplacement of [3H]pyrilamine from human histamine H1 receptor
ChEMBL 421 5 2 5 4.3 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)c(Cl)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL568400 197250 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptorDisplacement of [3H]pyrilamine from human histamine H1 receptor
ChEMBL 421 5 2 5 4.3 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)c(Cl)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
11231249 50338 1 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 277 11 1 2 4.2 c1nc(CCCCCCCCCCN2CCCC2)c[nH]1 10.1021/jm030936t
CHEMBL157217 50338 1 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 277 11 1 2 4.2 c1nc(CCCCCCCCCCN2CCCC2)c[nH]1 10.1021/jm030936t
10264715 50398 1 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 262 12 1 2 4.5 NCCCCCCCCCCCCc1ccncc1 10.1021/jm030936t
CHEMBL157273 50398 1 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 262 12 1 2 4.5 NCCCCCCCCCCCCc1ccncc1 10.1021/jm030936t
11358657 44834 1 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 305 13 1 2 4.9 c1nc(CCCCCCCCCCCCN2CCCC2)c[nH]1 10.1021/jm030936t
CHEMBL152221 44834 1 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 305 13 1 2 4.9 c1nc(CCCCCCCCCCCCN2CCCC2)c[nH]1 10.1021/jm030936t
45270350 195074 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 434 6 0 4 5.7 CN(CC1CCCCC1)C1CCN(c2nc3ccccc3n2Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2009.05.086
CHEMBL549598 195074 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 434 6 0 4 5.7 CN(CC1CCCCC1)C1CCN(c2nc3ccccc3n2Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2009.05.086
155532375 171780 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 490 6 1 5 5.2 COc1ccccc1OC[C@@H](O)CN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/j.bmcl.2019.126712
CHEMBL4467816 171780 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 490 6 1 5 5.2 COc1ccccc1OC[C@@H](O)CN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/j.bmcl.2019.126712
155557098 174569 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 478 5 1 4 5.3 OC(COc1ccccc1F)CN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/j.bmcl.2019.126712
CHEMBL4556553 174569 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 478 5 1 4 5.3 OC(COc1ccccc1F)CN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/j.bmcl.2019.126712
180 401 56 None -1 40 Human 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
200 401 56 None -1 40 Human 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2160 401 56 None -1 40 Human 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
CHEMBL629 401 56 None -1 40 Human 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
DB00321 401 56 None -1 40 Human 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
135398737 958 93 None 2 89 Human 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 958 93 None 2 89 Human 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 958 93 None 2 89 Human 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 958 93 None 2 89 Human 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 958 93 None 2 89 Human 8.3 pIC50 = 8.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
11753159 547 6 None -1 2 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 525 5 1 5 4.7 Cc1ccc(cc1)S(=O)(=O)NC(=O)N1CCC(CC1)N1CCC(CC1)Oc1ccc(c(c1)Cl)Cl 10.1021/jm300682j
7679 547 6 None -1 2 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 525 5 1 5 4.7 Cc1ccc(cc1)S(=O)(=O)NC(=O)N1CCC(CC1)N1CCC(CC1)Oc1ccc(c(c1)Cl)Cl 10.1021/jm300682j
CHEMBL2158814 547 6 None -1 2 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 525 5 1 5 4.7 Cc1ccc(cc1)S(=O)(=O)NC(=O)N1CCC(CC1)N1CCC(CC1)Oc1ccc(c(c1)Cl)Cl 10.1021/jm300682j
1212 1662 50 None -41 65 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 1662 50 None -41 65 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 1662 50 None -41 65 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 1662 50 None -41 65 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 1662 50 None -41 65 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
2337 3256 77 None -1 62 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [3H]mepyramine from H1R in rat brainDisplacement of [3H]mepyramine from H1R in rat brain
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1073/pnas.0611417104
50 3256 77 None -1 62 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [3H]mepyramine from H1R in rat brainDisplacement of [3H]mepyramine from H1R in rat brain
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1073/pnas.0611417104
5002 3256 77 None -1 62 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [3H]mepyramine from H1R in rat brainDisplacement of [3H]mepyramine from H1R in rat brain
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1073/pnas.0611417104
CHEMBL716 3256 77 None -1 62 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [3H]mepyramine from H1R in rat brainDisplacement of [3H]mepyramine from H1R in rat brain
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1073/pnas.0611417104
DB01224 3256 77 None -1 62 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [3H]mepyramine from H1R in rat brainDisplacement of [3H]mepyramine from H1R in rat brain
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1073/pnas.0611417104
44189144 195965 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 521 7 1 9 2.5 Cn1c(N2CCN(CCCN3c4ccccc4Sc4ccc(CC(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmc.2011.03.003
CHEMBL559664 195965 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 521 7 1 9 2.5 Cn1c(N2CCN(CCCN3c4ccccc4Sc4ccc(CC(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmc.2011.03.003
44189144 195965 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 521 7 1 9 2.5 Cn1c(N2CCN(CCCN3c4ccccc4Sc4ccc(CC(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmcl.2009.03.124
CHEMBL559664 195965 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 521 7 1 9 2.5 Cn1c(N2CCN(CCCN3c4ccccc4Sc4ccc(CC(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmcl.2009.03.124
155526952 171176 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 538 5 1 4 5.9 OC(COc1ccccc1Br)CN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/j.bmcl.2019.126712
CHEMBL4458953 171176 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 538 5 1 4 5.9 OC(COc1ccccc1Br)CN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/j.bmcl.2019.126712
9822631 122959 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 406 8 1 4 4.8 CCOCCn1cc(C2CCN(Cc3cccc(C(=O)O)c3)CC2)c2ccccc21 10.1016/j.bmcl.2004.12.008
CHEMBL360791 122959 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 406 8 1 4 4.8 CCOCCn1cc(C2CCN(Cc3cccc(C(=O)O)c3)CC2)c2ccccc21 10.1016/j.bmcl.2004.12.008
16722760 61996 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 519 6 1 9 2.4 Cn1c(N2CCCN(CCCN3c4ccccc4COc4ccc(C(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmc.2011.03.003
CHEMBL1774491 61996 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 519 6 1 9 2.4 Cn1c(N2CCCN(CCCN3c4ccccc4COc4ccc(C(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmc.2011.03.003
45269933 195295 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 518 7 1 8 3.5 Cn1c(C2=CCN(CCCN3c4ccccc4Sc4ccc(CC(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmcl.2009.03.124
CHEMBL551394 195295 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 518 7 1 8 3.5 Cn1c(C2=CCN(CCCN3c4ccccc4Sc4ccc(CC(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmcl.2009.03.124
45268186 196530 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 563 8 1 9 3.9 CCC(C(=O)O)c1ccc2c(c1)N(CCCN1CCCN(c3cc(=O)n(C)c(=O)n3C)CC1)c1ccccc1S2 10.1016/j.bmcl.2009.03.124
CHEMBL563647 196530 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 563 8 1 9 3.9 CCC(C(=O)O)c1ccc2c(c1)N(CCCN1CCCN(c3cc(=O)n(C)c(=O)n3C)CC1)c1ccccc1S2 10.1016/j.bmcl.2009.03.124
133 2496 52 None -102 42 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
1723 2496 52 None -102 42 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
28693 2496 52 None -102 42 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
CHEMBL19215 2496 52 None -102 42 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
DB13520 2496 52 None -102 42 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
155544367 173374 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at human Gq-coupled HRH1 expressed in CHOK1 cells assessed as inhibition in Orexin A-induced beta-arrestin 2 recruitment incubated for 30 mins followed by Orexin A addition and measured after 90 or 180 mins by pathhunter beta-arrestin assayAntagonist activity at human Gq-coupled HRH1 expressed in CHOK1 cells assessed as inhibition in Orexin A-induced beta-arrestin 2 recruitment incubated for 30 mins followed by Orexin A addition and measured after 90 or 180 mins by pathhunter beta-arrestin assay
ChEMBL 508 3 0 4 6.0 CC[C@]12CCCN(C(=O)c3cccc(Br)c3)CCc3c(n(c4ccccc34)C(=O)C1)[C@@H]2OC 10.1021/acs.jmedchem.9b01924
CHEMBL4527708 173374 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at human Gq-coupled HRH1 expressed in CHOK1 cells assessed as inhibition in Orexin A-induced beta-arrestin 2 recruitment incubated for 30 mins followed by Orexin A addition and measured after 90 or 180 mins by pathhunter beta-arrestin assayAntagonist activity at human Gq-coupled HRH1 expressed in CHOK1 cells assessed as inhibition in Orexin A-induced beta-arrestin 2 recruitment incubated for 30 mins followed by Orexin A addition and measured after 90 or 180 mins by pathhunter beta-arrestin assay
ChEMBL 508 3 0 4 6.0 CC[C@]12CCCN(C(=O)c3cccc(Br)c3)CCc3c(n(c4ccccc34)C(=O)C1)[C@@H]2OC 10.1021/acs.jmedchem.9b01924
11385692 137049 0 None - 0 Guinea pig 7.4 pIC50 = 7.4 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 462 8 1 5 5.4 O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccoc3)c3cc(F)ccc23)CC1 10.1021/jm0498203
CHEMBL374675 137049 0 None - 0 Guinea pig 7.4 pIC50 = 7.4 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 462 8 1 5 5.4 O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccoc3)c3cc(F)ccc23)CC1 10.1021/jm0498203
14407121 60085 0 None - 0 Guinea pig 7.4 pIC50 = 7.4 Binding
Inhibitory activity against Tritiated [3H]- mepyramine binding to histamine H1 receptor in guinea pig cerebral cortexInhibitory activity against Tritiated [3H]- mepyramine binding to histamine H1 receptor in guinea pig cerebral cortex
ChEMBL 473 10 1 5 5.3 COc1cc(C(C)=O)ccc1OCCCN1CCC(C(O)(c2ccccc2)c2ccccc2)CC1 10.1021/jm00121a022
CHEMBL17390 60085 0 None - 0 Guinea pig 7.4 pIC50 = 7.4 Binding
Inhibitory activity against Tritiated [3H]- mepyramine binding to histamine H1 receptor in guinea pig cerebral cortexInhibitory activity against Tritiated [3H]- mepyramine binding to histamine H1 receptor in guinea pig cerebral cortex
ChEMBL 473 10 1 5 5.3 COc1cc(C(C)=O)ccc1OCCCN1CCC(C(O)(c2ccccc2)c2ccccc2)CC1 10.1021/jm00121a022
242 470 124 None -22 51 Human 6.4 pIC50 = 6.4 Binding
Antagonistic activity at histamine1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine1 receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2016.04.087
34 470 124 None -22 51 Human 6.4 pIC50 = 6.4 Binding
Antagonistic activity at histamine1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine1 receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2016.04.087
60795 470 124 None -22 51 Human 6.4 pIC50 = 6.4 Binding
Antagonistic activity at histamine1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine1 receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2016.04.087
CHEMBL1112 470 124 None -22 51 Human 6.4 pIC50 = 6.4 Binding
Antagonistic activity at histamine1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine1 receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2016.04.087
DB01238 470 124 None -22 51 Human 6.4 pIC50 = 6.4 Binding
Antagonistic activity at histamine1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine1 receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2016.04.087
14762566 107735 7 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 401 6 1 3 3.0 O=C(NCCN1CCN(Cc2ccccc2)CC1)c1ccccc1Br 10.1021/jm00173a011
CHEMBL319123 107735 7 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 401 6 1 3 3.0 O=C(NCCN1CCN(Cc2ccccc2)CC1)c1ccccc1Br 10.1021/jm00173a011
14842830 98986 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex
ChEMBL 308 5 0 2 4.5 CN(C)CCC(c1ccc(Cl)cc1)c1ccc(Cl)cn1 10.1021/jm00108a012
CHEMBL279907 98986 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex
ChEMBL 308 5 0 2 4.5 CN(C)CCC(c1ccc(Cl)cc1)c1ccc(Cl)cn1 10.1021/jm00108a012
15181802 12165 0 None - 0 Guinea pig 7.4 pIC50 = 7.4 Binding
Compound is evaluated for in vitro receptor binding affinity against H1 receptorCompound is evaluated for in vitro receptor binding affinity against H1 receptor
ChEMBL 471 7 0 7 3.4 Cn1c(=O)c2c(ncn2CCCN2CCC(C(c3ccccc3)c3ccccc3)CC2)n(C)c1=O 10.1021/jm00020a018
CHEMBL1184199 12165 0 None - 0 Guinea pig 7.4 pIC50 = 7.4 Binding
Compound is evaluated for in vitro receptor binding affinity against H1 receptorCompound is evaluated for in vitro receptor binding affinity against H1 receptor
ChEMBL 471 7 0 7 3.4 Cn1c(=O)c2c(ncn2CCCN2CCC(C(c3ccccc3)c3ccccc3)CC2)n(C)c1=O 10.1021/jm00020a018
CHEMBL338611 12165 0 None - 0 Guinea pig 7.4 pIC50 = 7.4 Binding
Compound is evaluated for in vitro receptor binding affinity against H1 receptorCompound is evaluated for in vitro receptor binding affinity against H1 receptor
ChEMBL 471 7 0 7 3.4 Cn1c(=O)c2c(ncn2CCCN2CCC(C(c3ccccc3)c3ccccc3)CC2)n(C)c1=O 10.1021/jm00020a018
3191 102858 97 None - 25 Guinea pig 7.4 pIC50 = 7.4 Binding
Compound is evaluated for in vitro receptor binding affinity against H1 receptorCompound is evaluated for in vitro receptor binding affinity against H1 receptor
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 10.1021/jm00020a018
CHEMBL305660 102858 97 None - 25 Guinea pig 7.4 pIC50 = 7.4 Binding
Compound is evaluated for in vitro receptor binding affinity against H1 receptorCompound is evaluated for in vitro receptor binding affinity against H1 receptor
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 10.1021/jm00020a018
3168 9262 92 None -87 21 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
CHEMBL1108 9262 92 None -87 21 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
11005810 10466 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 517 10 1 4 6.2 N#Cc1ccc(CCOC(=O)NC2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
CHEMBL116463 10466 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 517 10 1 4 6.2 N#Cc1ccc(CCOC(=O)NC2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
45269062 196512 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 535 8 2 9 3.6 Cn1c(NCCCN2CCC(CN3c4ccccc4Sc4ccc(C(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmcl.2009.03.124
CHEMBL563520 196512 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 535 8 2 9 3.6 Cn1c(NCCCN2CCC(CN3c4ccccc4Sc4ccc(C(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmcl.2009.03.124
9954899 204463 17 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Binding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligandBinding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligand
ChEMBL 440 2 1 7 3.3 CN1CCN(C2=Nc3ccccc3Nc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
CHEMBL72292 204463 17 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Binding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligandBinding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligand
ChEMBL 440 2 1 7 3.3 CN1CCN(C2=Nc3ccccc3Nc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
11189839 84334 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 438 9 1 4 5.5 CCCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccc(F)cc21 10.1021/jm0498203
CHEMBL221664 84334 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 438 9 1 4 5.5 CCCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccc(F)cc21 10.1021/jm0498203
9954899 204463 17 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory binding of [3H]mepyramine to histamine H1 receptors in rat brain membranesInhibitory binding of [3H]mepyramine to histamine H1 receptors in rat brain membranes
ChEMBL 440 2 1 7 3.3 CN1CCN(C2=Nc3ccccc3Nc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm9704457
CHEMBL72292 204463 17 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory binding of [3H]mepyramine to histamine H1 receptors in rat brain membranesInhibitory binding of [3H]mepyramine to histamine H1 receptors in rat brain membranes
ChEMBL 440 2 1 7 3.3 CN1CCN(C2=Nc3ccccc3Nc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm9704457
44319134 205993 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.
ChEMBL 362 2 0 3 4.4 CN(C)CC1CC2c3c(cccc3C(F)(F)F)Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL84810 205993 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.
ChEMBL 362 2 0 3 4.4 CN(C)CC1CC2c3c(cccc3C(F)(F)F)Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
9979651 84762 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 422 8 1 5 4.4 COCCn1cc(C2CCN(Cc3ccc(OC)c(C(=O)O)c3)CC2)c2ccccc21 10.1021/jm0498203
CHEMBL223025 84762 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 422 8 1 5 4.4 COCCn1cc(C2CCN(Cc3ccc(OC)c(C(=O)O)c3)CC2)c2ccccc21 10.1021/jm0498203
10409896 65577 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 420 8 1 4 5.5 CCCCn1cc(C2CCN(Cc3ccc(OC)c(C(=O)O)c3)CC2)c2ccccc21 10.1016/j.bmcl.2004.12.008
CHEMBL183169 65577 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 420 8 1 4 5.5 CCCCn1cc(C2CCN(Cc3ccc(OC)c(C(=O)O)c3)CC2)c2ccccc21 10.1016/j.bmcl.2004.12.008
14762590 4489 1 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 350 7 1 2 4.5 CCc1ccccc1NC(=O)CCN1CCC(Cc2ccccc2)CC1 10.1021/jm00173a011
CHEMBL101973 4489 1 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 350 7 1 2 4.5 CCc1ccccc1NC(=O)CCN1CCC(Cc2ccccc2)CC1 10.1021/jm00173a011
11811722 10065 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 413 5 1 4 4.4 O=C1NCN(c2ccccc2)C12CCN(Cc1cccc(Oc3ccccc3)c1)CC2 10.1021/jm010878g
CHEMBL115280 10065 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 413 5 1 4 4.4 O=C1NCN(c2ccccc2)C12CCN(Cc1cccc(Oc3ccccc3)c1)CC2 10.1021/jm010878g
2286 3183 51 None -2 30 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to histamine H1 receptor (unknown origin) by radioligand binding assayBinding affinity to histamine H1 receptor (unknown origin) by radioligand binding assay
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1021/jm400856t
4927 3183 51 None -2 30 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to histamine H1 receptor (unknown origin) by radioligand binding assayBinding affinity to histamine H1 receptor (unknown origin) by radioligand binding assay
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1021/jm400856t
7282 3183 51 None -2 30 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to histamine H1 receptor (unknown origin) by radioligand binding assayBinding affinity to histamine H1 receptor (unknown origin) by radioligand binding assay
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1021/jm400856t
CHEMBL643 3183 51 None -2 30 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to histamine H1 receptor (unknown origin) by radioligand binding assayBinding affinity to histamine H1 receptor (unknown origin) by radioligand binding assay
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1021/jm400856t
DB01069 3183 51 None -2 30 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to histamine H1 receptor (unknown origin) by radioligand binding assayBinding affinity to histamine H1 receptor (unknown origin) by radioligand binding assay
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1021/jm400856t
1227 2489 43 None -5 12 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm300671m
2331 2489 43 None -5 12 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm300671m
3957 2489 43 None -5 12 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm300671m
4992 2489 43 None -5 12 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm300671m
CHEMBL511 2489 43 None -5 12 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm300671m
DB06691 2489 43 None -5 12 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm300671m
44318842 206108 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.
ChEMBL 308 2 0 3 3.7 Cc1ccc2c(c1)N1OC(CN(C)C)CC1c1ccccc1C2 10.1016/s0960-894x(01)00721-1
CHEMBL85735 206108 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.
ChEMBL 308 2 0 3 3.7 Cc1ccc2c(c1)N1OC(CN(C)C)CC1c1ccccc1C2 10.1016/s0960-894x(01)00721-1
1971 2866 38 None -1 30 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
2404 2866 38 None -1 30 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
4543 2866 38 None -1 30 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
CHEMBL445 2866 38 None -1 30 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
DB00540 2866 38 None -1 30 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
11247939 137105 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 450 10 1 5 4.9 CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cccc(C)c21 10.1021/jm0498203
CHEMBL374754 137105 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 450 10 1 5 4.9 CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cccc(C)c21 10.1021/jm0498203
11328514 137858 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 454 10 1 5 4.8 CCOCCn1cc(C2CCN(CCOc3cccc(F)c3C(=O)O)CC2)c2ccccc21 10.1021/jm0498203
CHEMBL376025 137858 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 454 10 1 5 4.8 CCOCCn1cc(C2CCN(CCOc3cccc(F)c3C(=O)O)CC2)c2ccccc21 10.1021/jm0498203
11373970 141973 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 436 9 1 5 4.8 CCOCCn1cc(C2CCN(Cc3cccc(C(=O)O)c3)CC2)c2cc(OC)ccc21 10.1021/jm0498203
CHEMBL387325 141973 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 436 9 1 5 4.8 CCOCCn1cc(C2CCN(Cc3cccc(C(=O)O)c3)CC2)c2cc(OC)ccc21 10.1021/jm0498203
10263017 207462 2 None - 3 Human 6.3 pIC50 = 6.3 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 223 10 2 2 3.0 NCCCCCCCCCCc1c[nH]cn1 10.1021/jm030936t
CHEMBL94249 207462 2 None - 3 Human 6.3 pIC50 = 6.3 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 223 10 2 2 3.0 NCCCCCCCCCCc1c[nH]cn1 10.1021/jm030936t
44369359 46881 1 None - 0 Human 4.3 pIC50 = 4.3 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 255 3 2 2 2.9 NCCc1c[nH]c(-c2ccc(Cl)c(Cl)c2)n1 10.1021/jm030936t
CHEMBL154068 46881 1 None - 0 Human 4.3 pIC50 = 4.3 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 255 3 2 2 2.9 NCCc1c[nH]c(-c2ccc(Cl)c(Cl)c2)n1 10.1021/jm030936t
657255 199084 34 None -18 15 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 nan
CHEMBL588119 199084 34 None -18 15 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 nan
148123909 170233 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 505 6 1 6 5.1 O=[N+]([O-])c1ccccc1OCC(O)CN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/j.bmcl.2019.126712
CHEMBL4445636 170233 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 505 6 1 6 5.1 O=[N+]([O-])c1ccccc1OCC(O)CN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/j.bmcl.2019.126712
14762600 164451 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 363 5 1 3 3.3 CCc1ccccc1NC(=O)CCN1CCN2Cc3ccccc3CC2C1 10.1021/jm00173a011
CHEMBL421393 164451 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 363 5 1 3 3.3 CCc1ccccc1NC(=O)CCN1CCN2Cc3ccccc3CC2C1 10.1021/jm00173a011
45269063 196186 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 549 8 1 9 3.6 CN(CCCN1CCC(CN2c3ccccc3Sc3ccc(C(=O)O)cc32)CC1)c1cc(=O)n(C)c(=O)n1C 10.1016/j.bmcl.2009.03.124
CHEMBL561377 196186 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 549 8 1 9 3.6 CN(CCCN1CCC(CN2c3ccccc3Sc3ccc(C(=O)O)cc32)CC1)c1cc(=O)n(C)c(=O)n1C 10.1016/j.bmcl.2009.03.124
52953079 62001 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 519 6 1 9 2.4 Cn1c(N2CCCN(CCCN3c4cc(C(=O)O)ccc4COc4ccccc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmc.2011.03.003
CHEMBL1774496 62001 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 519 6 1 9 2.4 Cn1c(N2CCCN(CCCN3c4cc(C(=O)O)ccc4COc4ccccc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmc.2011.03.003
286016 4416 8 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 227 0 2 2 1.5 c1ccc2c3c([nH]c2c1)CN1CCNCC1C3 10.1021/jm00173a011
CHEMBL101491 4416 8 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 227 0 2 2 1.5 c1ccc2c3c([nH]c2c1)CN1CCNCC1C3 10.1021/jm00173a011
54586254 62003 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 531 7 1 8 2.6 Cn1c(N2CCCN(CCCN3c4ccccc4CCc4ccc(CC(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmc.2011.03.003
CHEMBL1774498 62003 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 531 7 1 8 2.6 Cn1c(N2CCCN(CCCN3c4ccccc4CCc4ccc(CC(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmc.2011.03.003
54584335 62006 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 516 6 1 8 2.2 Cn1c(N2CCN(CC/C=C3\c4ccccc4COc4ccc(CC(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmc.2011.03.003
CHEMBL1774501 62006 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 516 6 1 8 2.2 Cn1c(N2CCN(CC/C=C3\c4ccccc4COc4ccc(CC(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmc.2011.03.003
17964355 126453 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 414 6 1 4 5.4 O=C(O)c1cccc(CN2CCC(c3cn(Cc4ccoc4)c4ccccc34)CC2)c1 10.1016/j.bmcl.2004.12.008
CHEMBL365197 126453 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 414 6 1 4 5.4 O=C(O)c1cccc(CN2CCC(c3cn(Cc4ccoc4)c4ccccc34)CC2)c1 10.1016/j.bmcl.2004.12.008
14762591 4216 2 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 356 6 1 2 4.6 O=C(CCN1CCC(Cc2ccccc2)CC1)Nc1ccccc1Cl 10.1021/jm00173a011
CHEMBL100276 4216 2 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 356 6 1 2 4.6 O=C(CCN1CCC(Cc2ccccc2)CC1)Nc1ccccc1Cl 10.1021/jm00173a011
10298838 168794 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 469 9 1 5 5.2 O=C(O)c1ccccc1OCCN1CCC(c2cn(CCc3ccccn3)c3ccccc23)CC1 10.1021/jm0498203
CHEMBL437519 168794 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 469 9 1 5 5.2 O=C(O)c1ccccc1OCCN1CCC(c2cn(CCc3ccccn3)c3ccccc23)CC1 10.1021/jm0498203
22322323 196017 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 440 7 1 7 2.7 Cn1c(NCCCN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)cc(=O)n(C)c1=O 10.1016/j.bmcl.2009.03.124
CHEMBL560120 196017 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 440 7 1 7 2.7 Cn1c(NCCCN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)cc(=O)n(C)c1=O 10.1016/j.bmcl.2009.03.124
10917690 207605 1 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against histamine H1 receptorInhibitory concentration against histamine H1 receptor
ChEMBL 471 8 0 5 5.4 COc1ccc(CCN2CCC(C(=O)c3nc4ccccc4n3Cc3ccc(F)cc3)CC2)cc1 10.1021/jm058225d
CHEMBL95051 207605 1 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against histamine H1 receptorInhibitory concentration against histamine H1 receptor
ChEMBL 471 8 0 5 5.4 COc1ccc(CCN2CCC(C(=O)c3nc4ccccc4n3Cc3ccc(F)cc3)CC2)cc1 10.1021/jm058225d
44318461 205735 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.
ChEMBL 308 2 0 3 3.7 Cc1cccc2c1Cc1ccccc1C1CC(CN(C)C)ON21 10.1016/s0960-894x(01)00721-1
CHEMBL82635 205735 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.
ChEMBL 308 2 0 3 3.7 Cc1cccc2c1Cc1ccccc1C1CC(CN(C)C)ON21 10.1016/s0960-894x(01)00721-1
1227 2489 43 None -2 12 Human 8.2 pIC50 = 8.2 Binding
Displacement of radiolabeled pyrilamine from human histamine H1 receptorDisplacement of radiolabeled pyrilamine from human histamine H1 receptor
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm8007618
2331 2489 43 None -2 12 Human 8.2 pIC50 = 8.2 Binding
Displacement of radiolabeled pyrilamine from human histamine H1 receptorDisplacement of radiolabeled pyrilamine from human histamine H1 receptor
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm8007618
3957 2489 43 None -2 12 Human 8.2 pIC50 = 8.2 Binding
Displacement of radiolabeled pyrilamine from human histamine H1 receptorDisplacement of radiolabeled pyrilamine from human histamine H1 receptor
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm8007618
4992 2489 43 None -2 12 Human 8.2 pIC50 = 8.2 Binding
Displacement of radiolabeled pyrilamine from human histamine H1 receptorDisplacement of radiolabeled pyrilamine from human histamine H1 receptor
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm8007618
CHEMBL511 2489 43 None -2 12 Human 8.2 pIC50 = 8.2 Binding
Displacement of radiolabeled pyrilamine from human histamine H1 receptorDisplacement of radiolabeled pyrilamine from human histamine H1 receptor
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm8007618
DB06691 2489 43 None -2 12 Human 8.2 pIC50 = 8.2 Binding
Displacement of radiolabeled pyrilamine from human histamine H1 receptorDisplacement of radiolabeled pyrilamine from human histamine H1 receptor
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm8007618
147863431 175939 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 460 5 1 4 5.2 OC(COc1ccccc1)CN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/j.bmcl.2019.126712
CHEMBL4587694 175939 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 460 5 1 4 5.2 OC(COc1ccccc1)CN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/j.bmcl.2019.126712
1210 918 51 None -20 21 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
1213 918 51 None -20 21 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
2725 918 51 None -20 21 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
33036 918 51 None -20 21 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
4411 918 51 None -20 21 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
616 918 51 None -20 21 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
6976 918 51 None -20 21 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
716121 918 51 None -20 21 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL1201353 918 51 None -20 21 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL1554789 918 51 None -20 21 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL505 918 51 None -20 21 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
DB01114 918 51 None -20 21 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
DB13679 918 51 None -20 21 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
9904205 205850 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity against Histamine H1 receptorBinding affinity against Histamine H1 receptor
ChEMBL 294 2 0 3 3.4 CN(C)CC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(02)00796-5
CHEMBL83658 205850 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity against Histamine H1 receptorBinding affinity against Histamine H1 receptor
ChEMBL 294 2 0 3 3.4 CN(C)CC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(02)00796-5
9904205 205850 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.
ChEMBL 294 2 0 3 3.4 CN(C)CC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL83658 205850 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.
ChEMBL 294 2 0 3 3.4 CN(C)CC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
9904205 205850 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligandBinding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligand
ChEMBL 294 2 0 3 3.4 CN(C)CC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL83658 205850 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligandBinding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligand
ChEMBL 294 2 0 3 3.4 CN(C)CC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
16005860 187406 7 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 388 5 1 2 4.8 CC(C)(C)CCN1CC[C@H](CNC(=O)c2cc(Cl)cc(Cl)c2)[C@H](F)C1 10.1021/jm800830n
CHEMBL493677 187406 7 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 388 5 1 2 4.8 CC(C)(C)CCN1CC[C@H](CNC(=O)c2cc(Cl)cc(Cl)c2)[C@H](F)C1 10.1021/jm800830n
44461456 205749 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligandBinding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligand
ChEMBL 308 2 0 3 3.8 CN(C)CC1(C)CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL82714 205749 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligandBinding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligand
ChEMBL 308 2 0 3 3.8 CN(C)CC1(C)CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
11508317 8140 0 None - 1 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 336 5 0 3 5.1 C[C@@H](c1ccccn1)c1c(CCN2CCCC2)sc2ccccc12 10.1016/j.bmcl.2010.01.134
CHEMBL1091774 8140 0 None - 1 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 336 5 0 3 5.1 C[C@@H](c1ccccn1)c1c(CCN2CCCC2)sc2ccccc12 10.1016/j.bmcl.2010.01.134
40466858 16155 67 None - 0 Guinea pig 5.2 pIC50 = 5.2 Binding
Inhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challengeInhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challenge
ChEMBL 348 6 1 3 4.0 Cc1ccc(/C(=C\CN2CCCC2)c2cccc(/C=C/C(=O)O)n2)cc1 10.1007/s00044-008-9119-y
5284514 16155 67 None - 0 Guinea pig 5.2 pIC50 = 5.2 Binding
Inhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challengeInhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challenge
ChEMBL 348 6 1 3 4.0 Cc1ccc(/C(=C\CN2CCCC2)c2cccc(/C=C/C(=O)O)n2)cc1 10.1007/s00044-008-9119-y
CHEMBL1224 16155 67 None - 0 Guinea pig 5.2 pIC50 = 5.2 Binding
Inhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challengeInhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challenge
ChEMBL 348 6 1 3 4.0 Cc1ccc(/C(=C\CN2CCCC2)c2cccc(/C=C/C(=O)O)n2)cc1 10.1007/s00044-008-9119-y
136224310 85389 0 None - 0 Guinea pig 5.2 pIC50 = 5.2 Binding
Inhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challengeInhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challenge
ChEMBL 227 3 4 5 -1.4 CC(C)(CO)NC=C1C(=O)NC(=O)NC1=O 10.1007/s00044-008-9119-y
CHEMBL2262481 85389 0 None - 0 Guinea pig 5.2 pIC50 = 5.2 Binding
Inhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challengeInhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challenge
ChEMBL 227 3 4 5 -1.4 CC(C)(CO)NC=C1C(=O)NC(=O)NC1=O 10.1007/s00044-008-9119-y
54586256 62009 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 516 5 1 8 2.7 Cn1c(N2CCCN(CC/C=C3/c4ccccc4COc4ccc(C(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmc.2011.03.003
CHEMBL1774504 62009 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 516 5 1 8 2.7 Cn1c(N2CCCN(CC/C=C3/c4ccccc4COc4ccc(C(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmc.2011.03.003
44271504 59717 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
Inhibitory activity against Tritiated [3H]- mepyramine binding to histamine H1 receptor in guinea pig cerebral cortexInhibitory activity against Tritiated [3H]- mepyramine binding to histamine H1 receptor in guinea pig cerebral cortex
ChEMBL 495 9 1 5 5.2 COC(=O)c1ccc(OCCCN2CCC(C(O)(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm00121a022
CHEMBL17237 59717 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
Inhibitory activity against Tritiated [3H]- mepyramine binding to histamine H1 receptor in guinea pig cerebral cortexInhibitory activity against Tritiated [3H]- mepyramine binding to histamine H1 receptor in guinea pig cerebral cortex
ChEMBL 495 9 1 5 5.2 COC(=O)c1ccc(OCCCN2CCC(C(O)(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm00121a022
11230427 44721 1 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 249 9 1 2 3.4 c1nc(CCCCCCCCN2CCCC2)c[nH]1 10.1021/jm030936t
CHEMBL152126 44721 1 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 249 9 1 2 3.4 c1nc(CCCCCCCCN2CCCC2)c[nH]1 10.1021/jm030936t
14762595 4444 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 402 5 2 3 3.8 CCc1ccccc1NC(=O)CCN1CCN2Cc3[nH]c4ccccc4c3CC2C1 10.1021/jm00173a011
CHEMBL101625 4444 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 402 5 2 3 3.8 CCc1ccccc1NC(=O)CCN1CCN2Cc3[nH]c4ccccc4c3CC2C1 10.1021/jm00173a011
1210 918 51 None -20 21 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cells
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1128/aac.00669-07
1213 918 51 None -20 21 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cells
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1128/aac.00669-07
2725 918 51 None -20 21 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cells
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1128/aac.00669-07
33036 918 51 None -20 21 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cells
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1128/aac.00669-07
4411 918 51 None -20 21 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cells
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1128/aac.00669-07
616 918 51 None -20 21 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cells
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1128/aac.00669-07
6976 918 51 None -20 21 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cells
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1128/aac.00669-07
716121 918 51 None -20 21 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cells
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1128/aac.00669-07
CHEMBL1201353 918 51 None -20 21 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cells
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1128/aac.00669-07
CHEMBL1554789 918 51 None -20 21 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cells
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1128/aac.00669-07
CHEMBL505 918 51 None -20 21 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cells
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1128/aac.00669-07
DB01114 918 51 None -20 21 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cells
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1128/aac.00669-07
DB13679 918 51 None -20 21 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cells
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1128/aac.00669-07
14762575 4184 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 400 6 1 2 4.1 O=C(NCCN1CCC(Cc2ccccc2)CC1)c1ccccc1Br 10.1021/jm00173a011
CHEMBL100125 4184 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 400 6 1 2 4.1 O=C(NCCN1CCC(Cc2ccccc2)CC1)c1ccccc1Br 10.1021/jm00173a011
44461565 104350 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligandBinding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligand
ChEMBL 322 4 0 3 4.2 CN(C)CCCC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL310018 104350 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligandBinding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligand
ChEMBL 322 4 0 3 4.2 CN(C)CCCC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
4919 206234 23 None - 8 Rat 5.2 pIC50 = 5.2 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
ChEMBL 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 10.1021/jm300671m
CHEMBL86715 206234 23 None - 8 Rat 5.2 pIC50 = 5.2 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
ChEMBL 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 10.1021/jm300671m
14762601 108361 1 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 369 4 1 3 3.4 O=C(CCN1CCN2Cc3ccccc3CC2C1)Nc1ccccc1Cl 10.1021/jm00173a011
CHEMBL319817 108361 1 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 369 4 1 3 3.4 O=C(CCN1CCN2Cc3ccccc3CC2C1)Nc1ccccc1Cl 10.1021/jm00173a011
45267329 196008 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 549 8 1 9 3.3 Cn1c(N2CCCN(CCCN3c4ccccc4Sc4ccc(CCC(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmcl.2009.03.124
CHEMBL560061 196008 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 549 8 1 9 3.3 Cn1c(N2CCCN(CCCN3c4ccccc4Sc4ccc(CCC(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmcl.2009.03.124
10478188 122942 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 436 9 1 5 4.8 CCOCCn1cc(C2CCN(Cc3ccc(OC)c(C(=O)O)c3)CC2)c2ccccc21 10.1016/j.bmcl.2004.12.008
CHEMBL360712 122942 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 436 9 1 5 4.8 CCOCCn1cc(C2CCN(Cc3ccc(OC)c(C(=O)O)c3)CC2)c2ccccc21 10.1016/j.bmcl.2004.12.008
14762573 4482 2 None - 0 Guinea pig 5.2 pIC50 = 5.2 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 323 6 1 3 2.2 O=C(NCCN1CCN(Cc2ccccc2)CC1)c1ccccc1 10.1021/jm00173a011
CHEMBL101927 4482 2 None - 0 Guinea pig 5.2 pIC50 = 5.2 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 323 6 1 3 2.2 O=C(NCCN1CCN(Cc2ccccc2)CC1)c1ccccc1 10.1021/jm00173a011
14762568 109222 2 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 357 6 1 3 2.9 O=C(NCCN1CCN(Cc2ccccc2)CC1)c1ccccc1Cl 10.1021/jm00173a011
CHEMBL321738 109222 2 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 357 6 1 3 2.9 O=C(NCCN1CCN(Cc2ccccc2)CC1)c1ccccc1Cl 10.1021/jm00173a011
44318695 107005 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.
ChEMBL 370 3 0 3 5.1 CN(C)CC1CC2c3ccccc3Cc3ccc(-c4ccccc4)cc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL315308 107005 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.Binding affinity at human cloned Histamine H1 receptor expressed in CHO cells by [3H]pyrilamine displacement.
ChEMBL 370 3 0 3 5.1 CN(C)CC1CC2c3ccccc3Cc3ccc(-c4ccccc4)cc3N2O1 10.1016/s0960-894x(01)00721-1
16722761 62002 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 517 6 1 8 2.6 Cn1c(N2CCCN(CCCN3c4ccccc4CCc4ccc(C(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmc.2011.03.003
CHEMBL1774497 62002 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 517 6 1 8 2.6 Cn1c(N2CCCN(CCCN3c4ccccc4CCc4ccc(C(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmc.2011.03.003
44392642 65252 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 478 8 1 5 5.9 O=C(O)c1ccc(Cl)cc1OCCN1CCC(c2cn(Cc3ccoc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.12.008
CHEMBL182758 65252 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 478 8 1 5 5.9 O=C(O)c1ccc(Cl)cc1OCCN1CCC(c2cn(Cc3ccoc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.12.008
2253940 67254 11 None - 0 Guinea pig 5.2 pIC50 = 5.2 Binding
Inhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challengeInhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challenge
ChEMBL 237 2 3 4 0.2 O=C1NC(=O)C(=CNC2CCCCC2)C(=O)N1 10.1007/s00044-008-9119-y
CHEMBL1880624 67254 11 None - 0 Guinea pig 5.2 pIC50 = 5.2 Binding
Inhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challengeInhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challenge
ChEMBL 237 2 3 4 0.2 O=C1NC(=O)C(=CNC2CCCCC2)C(=O)N1 10.1007/s00044-008-9119-y
14762572 111578 1 None - 0 Guinea pig 5.2 pIC50 = 5.2 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 337 6 1 3 2.5 Cc1ccccc1C(=O)NCCN1CCN(Cc2ccccc2)CC1 10.1021/jm00173a011
CHEMBL328170 111578 1 None - 0 Guinea pig 5.2 pIC50 = 5.2 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 337 6 1 3 2.5 Cc1ccccc1C(=O)NCCN1CCN(Cc2ccccc2)CC1 10.1021/jm00173a011
100 3805 58 None -7 55 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
2637 3805 58 None -7 55 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
5452 3805 58 None -7 55 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
CHEMBL479 3805 58 None -7 55 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
DB00679 3805 58 None -7 55 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
45270755 196736 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 549 7 1 9 3.5 CC(C(=O)O)c1ccc2c(c1)N(CCCN1CCCN(c3cc(=O)n(C)c(=O)n3C)CC1)c1ccccc1S2 10.1016/j.bmcl.2009.03.124
CHEMBL565083 196736 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 549 7 1 9 3.5 CC(C(=O)O)c1ccc2c(c1)N(CCCN1CCCN(c3cc(=O)n(C)c(=O)n3C)CC1)c1ccccc1S2 10.1016/j.bmcl.2009.03.124
135515198 104750 8 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Binding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligandBinding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligand
ChEMBL 440 2 1 7 3.3 CN1CCN(C2=Nc3cc(OS(=O)(=O)C(F)(F)F)ccc3Nc3ccccc32)CC1 10.1021/jm991005d
CHEMBL310712 104750 8 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Binding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligandBinding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligand
ChEMBL 440 2 1 7 3.3 CN1CCN(C2=Nc3cc(OS(=O)(=O)C(F)(F)F)ccc3Nc3ccccc32)CC1 10.1021/jm991005d
135515198 104750 8 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory binding of [3H]mepyramine to histamine H1 receptors in rat brain membranesInhibitory binding of [3H]mepyramine to histamine H1 receptors in rat brain membranes
ChEMBL 440 2 1 7 3.3 CN1CCN(C2=Nc3cc(OS(=O)(=O)C(F)(F)F)ccc3Nc3ccccc32)CC1 10.1021/jm9704457
CHEMBL310712 104750 8 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory binding of [3H]mepyramine to histamine H1 receptors in rat brain membranesInhibitory binding of [3H]mepyramine to histamine H1 receptors in rat brain membranes
ChEMBL 440 2 1 7 3.3 CN1CCN(C2=Nc3cc(OS(=O)(=O)C(F)(F)F)ccc3Nc3ccccc32)CC1 10.1021/jm9704457
1547484 940 74 None -1 20 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
654 940 74 None -1 20 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
9072 940 74 None -1 20 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
CHEMBL43064 940 74 None -1 20 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
DB00568 940 74 None -1 20 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
54586255 62004 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 559 7 1 8 3.3 Cn1c(N2CCCN(CCCN3c4ccccc4CCc4ccc(C(C)(C)C(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmc.2011.03.003
CHEMBL1774499 62004 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 559 7 1 8 3.3 Cn1c(N2CCCN(CCCN3c4ccccc4CCc4ccc(C(C)(C)C(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmc.2011.03.003
11293983 84291 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 454 10 1 5 4.8 CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccc(F)cc21 10.1021/jm0498203
CHEMBL221413 84291 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 454 10 1 5 4.8 CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccc(F)cc21 10.1021/jm0498203
23027411 198520 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptorDisplacement of [3H]pyrilamine from human histamine H1 receptor
ChEMBL 387 5 2 5 3.7 Cc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)cc3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL577912 198520 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptorDisplacement of [3H]pyrilamine from human histamine H1 receptor
ChEMBL 387 5 2 5 3.7 Cc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)cc3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
14762584 4357 1 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 351 7 1 3 3.4 CCc1ccccc1NC(=O)CCN1CCN(Cc2ccccc2)CC1 10.1021/jm00173a011
CHEMBL101088 4357 1 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 351 7 1 3 3.4 CCc1ccccc1NC(=O)CCN1CCN(Cc2ccccc2)CC1 10.1021/jm00173a011
1170 1633 75 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1016/j.bmc.2011.03.003
3348 1633 75 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1016/j.bmc.2011.03.003
4819 1633 75 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1016/j.bmc.2011.03.003
74685737 1633 75 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1016/j.bmc.2011.03.003
CHEMBL914 1633 75 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1016/j.bmc.2011.03.003
DB00950 1633 75 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1016/j.bmc.2011.03.003
1170 1633 75 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1016/j.bmcl.2009.03.124
3348 1633 75 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1016/j.bmcl.2009.03.124
4819 1633 75 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1016/j.bmcl.2009.03.124
74685737 1633 75 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1016/j.bmcl.2009.03.124
CHEMBL914 1633 75 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1016/j.bmcl.2009.03.124
DB00950 1633 75 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1016/j.bmcl.2009.03.124
1170 1633 75 None - 1 Human 7.1 pIC50 = 7.1 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1016/j.bmcl.2009.03.124
3348 1633 75 None - 1 Human 7.1 pIC50 = 7.1 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1016/j.bmcl.2009.03.124
4819 1633 75 None - 1 Human 7.1 pIC50 = 7.1 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1016/j.bmcl.2009.03.124
74685737 1633 75 None - 1 Human 7.1 pIC50 = 7.1 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1016/j.bmcl.2009.03.124
CHEMBL914 1633 75 None - 1 Human 7.1 pIC50 = 7.1 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1016/j.bmcl.2009.03.124
DB00950 1633 75 None - 1 Human 7.1 pIC50 = 7.1 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1016/j.bmcl.2009.03.124
10447834 1933 4 None -1862 5 Human 6.1 pIC50 = 6.1 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm030936t
4026 1933 4 None -1862 5 Human 6.1 pIC50 = 6.1 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm030936t
CHEMBL275507 1933 4 None -1862 5 Human 6.1 pIC50 = 6.1 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm030936t
11816882 47504 1 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 220 9 1 2 3.3 NCCCCCCCCCc1ccccn1 10.1021/jm030936t
CHEMBL154566 47504 1 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor
ChEMBL 220 9 1 2 3.3 NCCCCCCCCCc1ccccn1 10.1021/jm030936t
10885636 111016 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 503 9 0 4 5.7 N#Cc1ccc(CCOC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
CHEMBL326263 111016 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 503 9 0 4 5.7 N#Cc1ccc(CCOC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
14762576 4465 1 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 356 6 1 2 4.0 O=C(NCCN1CCC(Cc2ccccc2)CC1)c1ccccc1Cl 10.1021/jm00173a011
CHEMBL101758 4465 1 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 356 6 1 2 4.0 O=C(NCCN1CCC(Cc2ccccc2)CC1)c1ccccc1Cl 10.1021/jm00173a011
173727 60299 15 None - 0 Guinea pig 8.1 pIC50 = 8.1 Binding
Inhibitory activity against Tritiated [3H]- mepyramine binding to histamine H1 receptor in guinea pig cerebral cortexInhibitory activity against Tritiated [3H]- mepyramine binding to histamine H1 receptor in guinea pig cerebral cortex
ChEMBL 509 10 1 5 5.6 COc1cc(C(C)=O)ccc1OCCCN1CCC(C(O)(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm00121a022
CHEMBL17436 60299 15 None - 0 Guinea pig 8.1 pIC50 = 8.1 Binding
Inhibitory activity against Tritiated [3H]- mepyramine binding to histamine H1 receptor in guinea pig cerebral cortexInhibitory activity against Tritiated [3H]- mepyramine binding to histamine H1 receptor in guinea pig cerebral cortex
ChEMBL 509 10 1 5 5.6 COc1cc(C(C)=O)ccc1OCCCN1CCC(C(O)(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm00121a022
155522480 170649 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 490 6 1 5 5.2 COc1cccc(OCC(O)CN2CCC(=C3c4ccc(Cl)cc4CCc4cccnc43)CC2)c1 10.1016/j.bmcl.2019.126712
CHEMBL4451332 170649 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 490 6 1 5 5.2 COc1cccc(OCC(O)CN2CCC(=C3c4ccc(Cl)cc4CCc4cccnc43)CC2)c1 10.1016/j.bmcl.2019.126712
4011 82408 49 None 6 24 Human 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
CHEMBL21731 82408 49 None 6 24 Human 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
1210 918 51 None 9 21 Guinea pig 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm00108a012
1213 918 51 None 9 21 Guinea pig 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm00108a012
2725 918 51 None 9 21 Guinea pig 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm00108a012
33036 918 51 None 9 21 Guinea pig 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm00108a012
4411 918 51 None 9 21 Guinea pig 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm00108a012
616 918 51 None 9 21 Guinea pig 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm00108a012
6976 918 51 None 9 21 Guinea pig 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm00108a012
716121 918 51 None 9 21 Guinea pig 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm00108a012
CHEMBL1201353 918 51 None 9 21 Guinea pig 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm00108a012
CHEMBL1554789 918 51 None 9 21 Guinea pig 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm00108a012
CHEMBL505 918 51 None 9 21 Guinea pig 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm00108a012
DB01114 918 51 None 9 21 Guinea pig 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm00108a012
DB13679 918 51 None 9 21 Guinea pig 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm00108a012
155549599 173853 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 474 5 1 4 5.5 Cc1ccccc1OCC(O)CN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/j.bmcl.2019.126712
CHEMBL4539150 173853 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 474 5 1 4 5.5 Cc1ccccc1OCC(O)CN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/j.bmcl.2019.126712
2389 3331 118 None -346 67 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [3H]mepyramine from H1R in rat brainDisplacement of [3H]mepyramine from H1R in rat brain
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1073/pnas.0611417104
5073 3331 118 None -346 67 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [3H]mepyramine from H1R in rat brainDisplacement of [3H]mepyramine from H1R in rat brain
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1073/pnas.0611417104
96 3331 118 None -346 67 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [3H]mepyramine from H1R in rat brainDisplacement of [3H]mepyramine from H1R in rat brain
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1073/pnas.0611417104
CHEMBL85 3331 118 None -346 67 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [3H]mepyramine from H1R in rat brainDisplacement of [3H]mepyramine from H1R in rat brain
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1073/pnas.0611417104
DB00734 3331 118 None -346 67 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [3H]mepyramine from H1R in rat brainDisplacement of [3H]mepyramine from H1R in rat brain
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1073/pnas.0611417104
11329753 84563 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 514 10 1 5 5.4 CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cccc(Br)c21 10.1021/jm0498203
CHEMBL222083 84563 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 514 10 1 5 5.4 CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cccc(Br)c21 10.1021/jm0498203
45267775 196232 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 414 5 0 4 5.3 CN(c1ccccc1)C1CCN(c2nc3ccccc3n2Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2009.05.086
CHEMBL561690 196232 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 414 5 0 4 5.3 CN(c1ccccc1)C1CCN(c2nc3ccccc3n2Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2009.05.086
23027245 197128 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptorDisplacement of [3H]pyrilamine from human histamine H1 receptor
ChEMBL 387 5 2 5 3.7 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)cc3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL567791 197128 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptorDisplacement of [3H]pyrilamine from human histamine H1 receptor
ChEMBL 387 5 2 5 3.7 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)cc3)CC2)n1 10.1016/j.bmcl.2009.09.003
10915140 29474 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of mepyramine binding to Histamine H1 receptorInhibition of mepyramine binding to Histamine H1 receptor
ChEMBL 351 5 0 3 4.2 COC1Cc2ccccc2C2(CCN(CCCc3ccccc3)CC2)O1 10.1021/jm010992z
CHEMBL138458 29474 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of mepyramine binding to Histamine H1 receptorInhibition of mepyramine binding to Histamine H1 receptor
ChEMBL 351 5 0 3 4.2 COC1Cc2ccccc2C2(CCN(CCCc3ccccc3)CC2)O1 10.1021/jm010992z
76323071 85391 0 None - 0 Guinea pig 4.1 pIC50 = 4.1 Binding
Inhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challengeInhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challenge
ChEMBL 292 7 3 5 0.0 CC(CO)(CO)NCCCN1C(=O)c2ccccc2C1=O 10.1007/s00044-008-9119-y
CHEMBL2262485 85391 0 None - 0 Guinea pig 4.1 pIC50 = 4.1 Binding
Inhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challengeInhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challenge
ChEMBL 292 7 3 5 0.0 CC(CO)(CO)NCCCN1C(=O)c2ccccc2C1=O 10.1007/s00044-008-9119-y
155545274 174953 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 528 5 1 4 6.2 OC(COc1ccccc1C(F)(F)F)CN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/j.bmcl.2019.126712
CHEMBL4565774 174953 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 528 5 1 4 6.2 OC(COc1ccccc1C(F)(F)F)CN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/j.bmcl.2019.126712
23027527 196792 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptorDisplacement of [3H]pyrilamine from human histamine H1 receptor
ChEMBL 371 5 2 5 3.1 Cc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)cc3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL565551 196792 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptorDisplacement of [3H]pyrilamine from human histamine H1 receptor
ChEMBL 371 5 2 5 3.1 Cc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)cc3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
46182745 57327 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of radioligand binding to human histamine H1 receptorInhibition of radioligand binding to human histamine H1 receptor
ChEMBL 461 6 1 3 6.2 O=C(O)c1cc(-c2cccc(COc3ccc4c(c3)CN(C3CCCC3)C4=O)c2)ccc1Cl 10.1021/jm3005306
CHEMBL1651208 57327 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of radioligand binding to human histamine H1 receptorInhibition of radioligand binding to human histamine H1 receptor
ChEMBL 461 6 1 3 6.2 O=C(O)c1cc(-c2cccc(COc3ccc4c(c3)CN(C3CCCC3)C4=O)c2)ccc1Cl 10.1021/jm3005306
11487026 85015 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 422 9 1 5 4.2 COCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccccc21 10.1021/jm0498203
CHEMBL223889 85015 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 422 9 1 5 4.2 COCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccccc21 10.1021/jm0498203
44461606 105995 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligandBinding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligand
ChEMBL 308 3 0 3 3.8 CN(C)CCC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL313189 105995 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligandBinding affinity for human cloned Histamine H1 receptor expressed in CHO cells using [3H]pyrilamine as radioligand
ChEMBL 308 3 0 3 3.8 CN(C)CCC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
14762592 4363 4 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 340 6 1 2 4.1 O=C(CCN1CCC(Cc2ccccc2)CC1)Nc1ccccc1F 10.1021/jm00173a011
CHEMBL101133 4363 4 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 340 6 1 2 4.1 O=C(CCN1CCC(Cc2ccccc2)CC1)Nc1ccccc1F 10.1021/jm00173a011
1342605 4397 16 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 357 6 1 3 3.5 O=C(CCN1CCN(Cc2ccccc2)CC1)Nc1ccccc1Cl 10.1021/jm00173a011
CHEMBL101387 4397 16 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 357 6 1 3 3.5 O=C(CCN1CCN(Cc2ccccc2)CC1)Nc1ccccc1Cl 10.1021/jm00173a011
54587281 62005 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 516 6 1 8 2.2 Cn1c(N2CCN(CC/C=C3/c4ccccc4COc4ccc(CC(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmc.2011.03.003
CHEMBL1774500 62005 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 516 6 1 8 2.2 Cn1c(N2CCN(CC/C=C3/c4ccccc4COc4ccc(CC(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmc.2011.03.003
1224 1432 83 None -2 13 Human 4.1 pIC50 = 4.1 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
3100 1432 83 None -2 13 Human 4.1 pIC50 = 4.1 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
8980 1432 83 None -2 13 Human 4.1 pIC50 = 4.1 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
916 1432 83 None -2 13 Human 4.1 pIC50 = 4.1 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
CHEMBL657 1432 83 None -2 13 Human 4.1 pIC50 = 4.1 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
DB01075 1432 83 None -2 13 Human 4.1 pIC50 = 4.1 Binding
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand.
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
1224 1432 83 None -2 13 Human 4.1 pIC50 = 4.1 Binding
Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
3100 1432 83 None -2 13 Human 4.1 pIC50 = 4.1 Binding
Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
8980 1432 83 None -2 13 Human 4.1 pIC50 = 4.1 Binding
Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
916 1432 83 None -2 13 Human 4.1 pIC50 = 4.1 Binding
Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
CHEMBL657 1432 83 None -2 13 Human 4.1 pIC50 = 4.1 Binding
Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
DB01075 1432 83 None -2 13 Human 4.1 pIC50 = 4.1 Binding
Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Histamine H1 Receptors Binding Assay: Affinities of the test compounds for peripheral human histamine H-1-receptors were assessed using receptor-binding assays. The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
2398 954 62 None -1 29 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
2801 954 62 None -1 29 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
701 954 62 None -1 29 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
CHEMBL415 954 62 None -1 29 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
DB01242 954 62 None -1 29 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
11282005 66066 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 436 10 1 5 4.6 CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccccc21 10.1021/jm0498203
CHEMBL183706 66066 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 436 10 1 5 4.6 CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccccc21 10.1021/jm0498203
44392621 66324 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 420 10 0 5 4.7 CCOCCn1cc(C2CCN(CCOc3ccccc3C=O)CC2)c2ccccc21 10.1016/j.bmcl.2004.12.008
CHEMBL184989 66324 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against histamine-H1 receptorInhibitory concentration against histamine-H1 receptor
ChEMBL 420 10 0 5 4.7 CCOCCn1cc(C2CCN(CCOc3ccccc3C=O)CC2)c2ccccc21 10.1016/j.bmcl.2004.12.008
2389 3331 118 None -46 67 Human 6.1 pIC50 = 6.1 Binding
Antagonistic activity at histamine1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine1 receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2016.04.087
5073 3331 118 None -46 67 Human 6.1 pIC50 = 6.1 Binding
Antagonistic activity at histamine1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine1 receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2016.04.087
96 3331 118 None -46 67 Human 6.1 pIC50 = 6.1 Binding
Antagonistic activity at histamine1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine1 receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2016.04.087
CHEMBL85 3331 118 None -46 67 Human 6.1 pIC50 = 6.1 Binding
Antagonistic activity at histamine1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine1 receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2016.04.087
DB00734 3331 118 None -46 67 Human 6.1 pIC50 = 6.1 Binding
Antagonistic activity at histamine1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine1 receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2016.04.087
21177786 85390 0 None - 0 Guinea pig 4.1 pIC50 = 4.1 Binding
Inhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challengeInhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challenge
ChEMBL 225 1 2 5 -1.4 O=C1NC(=O)C(=CN2CCOCC2)C(=O)N1 10.1007/s00044-008-9119-y
CHEMBL2262482 85390 0 None - 0 Guinea pig 4.1 pIC50 = 4.1 Binding
Inhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challengeInhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challenge
ChEMBL 225 1 2 5 -1.4 O=C1NC(=O)C(=CN2CCOCC2)C(=O)N1 10.1007/s00044-008-9119-y
10273238 84754 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 414 6 1 4 5.4 O=C(O)c1cccc(CN2CCC(c3cn(Cc4ccco4)c4ccccc34)CC2)c1 10.1021/jm0498203
CHEMBL222985 84754 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 414 6 1 4 5.4 O=C(O)c1cccc(CN2CCC(c3cn(Cc4ccco4)c4ccccc34)CC2)c1 10.1021/jm0498203
13726622 94578 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex
ChEMBL 311 3 0 4 2.2 CN1C[C@H](CCN2CCC2)Oc2ncc(Cl)cc2C1=S 10.1021/jm00108a012
CHEMBL25198 94578 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex
ChEMBL 311 3 0 4 2.2 CN1C[C@H](CCN2CCC2)Oc2ncc(Cl)cc2C1=S 10.1021/jm00108a012
45273362 196473 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 551 8 1 10 2.8 Cn1c(N2CCCN(CCCN3c4ccccc4Sc4ccc(OCC(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmcl.2009.03.124
CHEMBL563271 196473 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 551 8 1 10 2.8 Cn1c(N2CCCN(CCCN3c4ccccc4Sc4ccc(OCC(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmcl.2009.03.124
135398737 958 93 None -4 89 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]mepyramine from H1R in rat brainDisplacement of [3H]mepyramine from H1R in rat brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1073/pnas.0611417104
38 958 93 None -4 89 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]mepyramine from H1R in rat brainDisplacement of [3H]mepyramine from H1R in rat brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1073/pnas.0611417104
722 958 93 None -4 89 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]mepyramine from H1R in rat brainDisplacement of [3H]mepyramine from H1R in rat brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1073/pnas.0611417104
CHEMBL42 958 93 None -4 89 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]mepyramine from H1R in rat brainDisplacement of [3H]mepyramine from H1R in rat brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1073/pnas.0611417104
DB00363 958 93 None -4 89 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]mepyramine from H1R in rat brainDisplacement of [3H]mepyramine from H1R in rat brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1073/pnas.0611417104
1385580 29276 76 None - 5 Guinea pig 8.1 pIC50 = 8.1 Binding
Inhibitory activity against Tritiated [3H]- mepyramine binding to Histamine H1 receptor in guinea pig cerebral cortexInhibitory activity against Tritiated [3H]- mepyramine binding to Histamine H1 receptor in guinea pig cerebral cortex
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1021/jm00121a022
4615 29276 76 None - 5 Guinea pig 8.1 pIC50 = 8.1 Binding
Inhibitory activity against Tritiated [3H]- mepyramine binding to Histamine H1 receptor in guinea pig cerebral cortexInhibitory activity against Tritiated [3H]- mepyramine binding to Histamine H1 receptor in guinea pig cerebral cortex
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1021/jm00121a022
CHEMBL13828 29276 76 None - 5 Guinea pig 8.1 pIC50 = 8.1 Binding
Inhibitory activity against Tritiated [3H]- mepyramine binding to Histamine H1 receptor in guinea pig cerebral cortexInhibitory activity against Tritiated [3H]- mepyramine binding to Histamine H1 receptor in guinea pig cerebral cortex
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1021/jm00121a022
150575506 172171 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 474 6 0 4 6.2 COc1ccccc1OCCCN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/j.bmcl.2019.126712
CHEMBL4473466 172171 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)
ChEMBL 474 6 0 4 6.2 COc1ccccc1OCCCN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/j.bmcl.2019.126712
6761 67799 19 None -1 18 Human 8.0 pIC50 = 8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
CHEMBL1909072 67799 19 None -1 18 Human 8.0 pIC50 = 8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
124087 1389 114 None 3 15 Human 8.0 pIC50 = 8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
7157 1389 114 None 3 15 Human 8.0 pIC50 = 8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
814 1389 114 None 3 15 Human 8.0 pIC50 = 8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
CHEMBL1172 1389 114 None 3 15 Human 8.0 pIC50 = 8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
DB00967 1389 114 None 3 15 Human 8.0 pIC50 = 8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
10202996 84642 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 430 6 1 4 5.8 O=C(O)c1cccc(CN2CCC(c3cn(Cc4cccs4)c4ccccc34)CC2)c1 10.1021/jm0498203
CHEMBL222372 84642 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 430 6 1 4 5.8 O=C(O)c1cccc(CN2CCC(c3cn(Cc4cccs4)c4ccccc34)CC2)c1 10.1021/jm0498203
10162727 84618 0 None - 0 Guinea pig 7.0 pIC50 = 7.0 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 478 7 1 5 6.0 COc1ccc(CN2CCC(c3cn(Cc4cccs4)c4cc(F)ccc34)CC2)cc1C(=O)O 10.1021/jm0498203
CHEMBL222139 84618 0 None - 0 Guinea pig 7.0 pIC50 = 7.0 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 478 7 1 5 6.0 COc1ccc(CN2CCC(c3cn(Cc4cccs4)c4cc(F)ccc34)CC2)cc1C(=O)O 10.1021/jm0498203
54580386 62007 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 530 6 1 8 2.6 Cn1c(N2CCCN(CC/C=C3/c4ccccc4COc4ccc(CC(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmc.2011.03.003
CHEMBL1774502 62007 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
ChEMBL 530 6 1 8 2.6 Cn1c(N2CCCN(CC/C=C3/c4ccccc4COc4ccc(CC(=O)O)cc43)CC2)cc(=O)n(C)c1=O 10.1016/j.bmc.2011.03.003
45484995 198519 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptorDisplacement of [3H]pyrilamine from human histamine H1 receptor
ChEMBL 403 6 2 5 3.5 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3ccc(F)c(F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL577904 198519 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptorDisplacement of [3H]pyrilamine from human histamine H1 receptor
ChEMBL 403 6 2 5 3.5 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3ccc(F)c(F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
44332030 111488 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 242 0 2 3 1.1 NN1CCN2Cc3[nH]c4ccccc4c3CC2C1 10.1021/jm00173a011
CHEMBL327724 111488 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 242 0 2 3 1.1 NN1CCN2Cc3[nH]c4ccccc4c3CC2C1 10.1021/jm00173a011
2600 3779 74 None -3 13 Guinea pig 7.0 pIC50 = 7.0 Binding
Compound is evaluated for in vitro receptor binding affinity against H1 receptorCompound is evaluated for in vitro receptor binding affinity against H1 receptor
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1021/jm00020a018
2608 3779 74 None -3 13 Guinea pig 7.0 pIC50 = 7.0 Binding
Compound is evaluated for in vitro receptor binding affinity against H1 receptorCompound is evaluated for in vitro receptor binding affinity against H1 receptor
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1021/jm00020a018
5405 3779 74 None -3 13 Guinea pig 7.0 pIC50 = 7.0 Binding
Compound is evaluated for in vitro receptor binding affinity against H1 receptorCompound is evaluated for in vitro receptor binding affinity against H1 receptor
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1021/jm00020a018
CHEMBL17157 3779 74 None -3 13 Guinea pig 7.0 pIC50 = 7.0 Binding
Compound is evaluated for in vitro receptor binding affinity against H1 receptorCompound is evaluated for in vitro receptor binding affinity against H1 receptor
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1021/jm00020a018
DB00342 3779 74 None -3 13 Guinea pig 7.0 pIC50 = 7.0 Binding
Compound is evaluated for in vitro receptor binding affinity against H1 receptorCompound is evaluated for in vitro receptor binding affinity against H1 receptor
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1021/jm00020a018
14407102 13854 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
Inhibitory activity against Tritiated [3H]- mepyramine binding to histamine H1 receptor in guinea pig cerebral cortexInhibitory activity against Tritiated [3H]- mepyramine binding to histamine H1 receptor in guinea pig cerebral cortex
ChEMBL 509 10 1 5 5.6 CCOC(=O)c1ccc(OCCCN2CCC(C(O)(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm00121a022
CHEMBL1195925 13854 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
Inhibitory activity against Tritiated [3H]- mepyramine binding to histamine H1 receptor in guinea pig cerebral cortexInhibitory activity against Tritiated [3H]- mepyramine binding to histamine H1 receptor in guinea pig cerebral cortex
ChEMBL 509 10 1 5 5.6 CCOC(=O)c1ccc(OCCCN2CCC(C(O)(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm00121a022
CHEMBL555593 13854 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
Inhibitory activity against Tritiated [3H]- mepyramine binding to histamine H1 receptor in guinea pig cerebral cortexInhibitory activity against Tritiated [3H]- mepyramine binding to histamine H1 receptor in guinea pig cerebral cortex
ChEMBL 509 10 1 5 5.6 CCOC(=O)c1ccc(OCCCN2CCC(C(O)(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm00121a022
10139591 84640 0 None - 0 Guinea pig 7.0 pIC50 = 7.0 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 462 7 1 5 5.5 COc1ccc(CN2CCC(c3cn(Cc4ccoc4)c4cc(F)ccc34)CC2)cc1C(=O)O 10.1021/jm0498203
CHEMBL222356 84640 0 None - 0 Guinea pig 7.0 pIC50 = 7.0 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 462 7 1 5 5.5 COc1ccc(CN2CCC(c3cn(Cc4ccoc4)c4cc(F)ccc34)CC2)cc1C(=O)O 10.1021/jm0498203
14762594 111442 3 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 352 7 1 3 4.0 COc1ccccc1NC(=O)CCN1CCC(Cc2ccccc2)CC1 10.1021/jm00173a011
CHEMBL327517 111442 3 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 352 7 1 3 4.0 COc1ccccc1NC(=O)CCN1CCC(Cc2ccccc2)CC1 10.1021/jm00173a011
11338659 84302 0 None - 0 Guinea pig 7.0 pIC50 = 7.0 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 404 8 1 4 4.8 C=CCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccccc21 10.1021/jm0498203
CHEMBL221463 84302 0 None - 0 Guinea pig 7.0 pIC50 = 7.0 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 404 8 1 4 4.8 C=CCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccccc21 10.1021/jm0498203
127049863 140252 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonistic activity at histamine1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine1 receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 443 8 1 5 4.5 CNC(=O)c1cc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)ccc1F 10.1016/j.bmcl.2016.04.087
CHEMBL3805518 140252 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonistic activity at histamine1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine1 receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 443 8 1 5 4.5 CNC(=O)c1cc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)ccc1F 10.1016/j.bmcl.2016.04.087
14762596 4373 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 408 4 2 3 3.9 O=C(CCN1CCN2Cc3[nH]c4ccccc4c3CC2C1)Nc1ccccc1Cl 10.1021/jm00173a011
CHEMBL101217 4373 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
ChEMBL 408 4 2 3 3.9 O=C(CCN1CCN2Cc3[nH]c4ccccc4c3CC2C1)Nc1ccccc1Cl 10.1021/jm00173a011
10204866 84736 0 None - 0 Guinea pig 7.0 pIC50 = 7.0 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 460 8 1 5 5.7 O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3cccs3)c3ccccc23)CC1 10.1021/jm0498203
CHEMBL222881 84736 0 None - 0 Guinea pig 7.0 pIC50 = 7.0 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 460 8 1 5 5.7 O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3cccs3)c3ccccc23)CC1 10.1021/jm0498203
10138404 136882 0 None - 0 Guinea pig 7.0 pIC50 = 7.0 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 444 8 1 5 5.2 O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccco3)c3ccccc23)CC1 10.1021/jm0498203
CHEMBL374218 136882 0 None - 0 Guinea pig 7.0 pIC50 = 7.0 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranesDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 444 8 1 5 5.2 O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccco3)c3ccccc23)CC1 10.1021/jm0498203
100 3805 58 None -23 55 Rat 7.0 pIC50 = 7 Binding
Binding affinity against Histamine H1 receptor was measured using radioligand ([3H]pyrilamine) binding assayBinding affinity against Histamine H1 receptor was measured using radioligand ([3H]pyrilamine) binding assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1021/jm00153a010
2637 3805 58 None -23 55 Rat 7.0 pIC50 = 7 Binding
Binding affinity against Histamine H1 receptor was measured using radioligand ([3H]pyrilamine) binding assayBinding affinity against Histamine H1 receptor was measured using radioligand ([3H]pyrilamine) binding assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1021/jm00153a010
5452 3805 58 None -23 55 Rat 7.0 pIC50 = 7 Binding
Binding affinity against Histamine H1 receptor was measured using radioligand ([3H]pyrilamine) binding assayBinding affinity against Histamine H1 receptor was measured using radioligand ([3H]pyrilamine) binding assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1021/jm00153a010
CHEMBL479 3805 58 None -23 55 Rat 7.0 pIC50 = 7 Binding
Binding affinity against Histamine H1 receptor was measured using radioligand ([3H]pyrilamine) binding assayBinding affinity against Histamine H1 receptor was measured using radioligand ([3H]pyrilamine) binding assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1021/jm00153a010
DB00679 3805 58 None -23 55 Rat 7.0 pIC50 = 7 Binding
Binding affinity against Histamine H1 receptor was measured using radioligand ([3H]pyrilamine) binding assayBinding affinity against Histamine H1 receptor was measured using radioligand ([3H]pyrilamine) binding assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1021/jm00153a010
191 403 98 None -56 29 Human 7.0 pIC50 = 7 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
201 403 98 None -56 29 Human 7.0 pIC50 = 7 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
2170 403 98 None -56 29 Human 7.0 pIC50 = 7 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
CHEMBL1113 403 98 None -56 29 Human 7.0 pIC50 = 7 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
DB00543 403 98 None -56 29 Human 7.0 pIC50 = 7 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
135398745 2914 112 None 1 65 Human 10.1 pKd = 10.1 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm100064d
47 2914 112 None 1 65 Human 10.1 pKd = 10.1 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm100064d
CHEMBL715 2914 112 None 1 65 Human 10.1 pKd = 10.1 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm100064d
DB00334 2914 112 None 1 65 Human 10.1 pKd = 10.1 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm100064d
CHEMBL5284242 194615 0 None 56 3 Human 10.0 pKd = 10 Binding
Antagonist potency at human H1 receptorAntagonist potency at human H1 receptor
ChEMBL 510 11 0 6 4.0 COCCCC(=O)N(C)CCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL5315342 194615 0 None 56 3 Human 10.0 pKd = 10 Binding
Antagonist potency at human H1 receptorAntagonist potency at human H1 receptor
ChEMBL 510 11 0 6 4.0 COCCCC(=O)N(C)CCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
1228 3866 34 None 5 4 Guinea pig 9.9 pKd = 9.9 Binding
Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum
ChEMBL 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 10.1021/jm00017a019
2763 3866 34 None 5 4 Guinea pig 9.9 pKd = 9.9 Binding
Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum
ChEMBL 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 10.1021/jm00017a019
5282443 3866 34 None 5 4 Guinea pig 9.9 pKd = 9.9 Binding
Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum
ChEMBL 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 10.1021/jm00017a019
CHEMBL855 3866 34 None 5 4 Guinea pig 9.9 pKd = 9.9 Binding
Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum
ChEMBL 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 10.1021/jm00017a019
DB00427 3866 34 None 5 4 Guinea pig 9.9 pKd = 9.9 Binding
Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum
ChEMBL 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 10.1021/jm00017a019
CHEMBL5275284 194654 0 None 5 3 Human 9.9 pKd = 9.9 Binding
Antagonist potency at human H1 receptorAntagonist potency at human H1 receptor
ChEMBL 466 8 1 5 3.9 CC(C)C(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL5315872 194654 0 None 5 3 Human 9.9 pKd = 9.9 Binding
Antagonist potency at human H1 receptorAntagonist potency at human H1 receptor
ChEMBL 466 8 1 5 3.9 CC(C)C(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL5272464 194625 0 None 11 3 Human 9.8 pKd = 9.8 Binding
Antagonist potency at human H1 receptorAntagonist potency at human H1 receptor
ChEMBL 480 10 1 5 4.4 CCCNC(=O)CCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL5315453 194625 0 None 11 3 Human 9.8 pKd = 9.8 Binding
Antagonist potency at human H1 receptorAntagonist potency at human H1 receptor
ChEMBL 480 10 1 5 4.4 CCCNC(=O)CCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
24824726 161109 1 None 2 6 Human 9.7 pKd = 9.7 Binding
Antagonist potency at human H1 receptorAntagonist potency at human H1 receptor
ChEMBL 496 11 1 6 3.6 COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL4060529 161109 1 None 2 6 Human 9.7 pKd = 9.7 Binding
Antagonist potency at human H1 receptorAntagonist potency at human H1 receptor
ChEMBL 496 11 1 6 3.6 COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL4117079 161109 1 None 2 6 Human 9.7 pKd = 9.7 Binding
Antagonist potency at human H1 receptorAntagonist potency at human H1 receptor
ChEMBL 496 11 1 6 3.6 COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL5282336 161109 1 None 2 6 Human 9.7 pKd = 9.7 Binding
Antagonist potency at human H1 receptorAntagonist potency at human H1 receptor
ChEMBL 496 11 1 6 3.6 COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL5286389 161109 1 None 2 6 Human 9.7 pKd = 9.7 Binding
Antagonist potency at human H1 receptorAntagonist potency at human H1 receptor
ChEMBL 496 11 1 6 3.6 COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
2267 559 71 None 10 7 Human 9.7 pKd = 9.7 Binding
Antagonist potency at human H1 receptorAntagonist potency at human H1 receptor
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1021/acsmedchemlett.7b00112
271 559 71 None 10 7 Human 9.7 pKd = 9.7 Binding
Antagonist potency at human H1 receptorAntagonist potency at human H1 receptor
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1021/acsmedchemlett.7b00112
7121 559 71 None 10 7 Human 9.7 pKd = 9.7 Binding
Antagonist potency at human H1 receptorAntagonist potency at human H1 receptor
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1021/acsmedchemlett.7b00112
CHEMBL639 559 71 None 10 7 Human 9.7 pKd = 9.7 Binding
Antagonist potency at human H1 receptorAntagonist potency at human H1 receptor
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1021/acsmedchemlett.7b00112
DB00972 559 71 None 10 7 Human 9.7 pKd = 9.7 Binding
Antagonist potency at human H1 receptorAntagonist potency at human H1 receptor
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1021/acsmedchemlett.7b00112
CHEMBL5273244 194616 0 None 63 3 Human 9.7 pKd = 9.7 Binding
Antagonist potency at human H1 receptorAntagonist potency at human H1 receptor
ChEMBL 468 9 1 6 2.9 COCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL5315364 194616 0 None 63 3 Human 9.7 pKd = 9.7 Binding
Antagonist potency at human H1 receptorAntagonist potency at human H1 receptor
ChEMBL 468 9 1 6 2.9 COCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL5270515 194609 0 None 39 3 Human 9.6 pKd = 9.6 Binding
Antagonist potency at human H1 receptorAntagonist potency at human H1 receptor
ChEMBL 452 8 1 5 3.6 CCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL5315265 194609 0 None 39 3 Human 9.6 pKd = 9.6 Binding
Antagonist potency at human H1 receptorAntagonist potency at human H1 receptor
ChEMBL 452 8 1 5 3.6 CCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
1227 2489 43 None 2 12 Guinea pig 9.5 pKd = 9.5 Binding
Antagonist activity at histamine H1 receptor in Cavia porcellus (guinea pig) ileum assessed as inhibition of electrically-induced contractionAntagonist activity at histamine H1 receptor in Cavia porcellus (guinea pig) ileum assessed as inhibition of electrically-induced contraction
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1007/s00044-012-0090-2
2331 2489 43 None 2 12 Guinea pig 9.5 pKd = 9.5 Binding
Antagonist activity at histamine H1 receptor in Cavia porcellus (guinea pig) ileum assessed as inhibition of electrically-induced contractionAntagonist activity at histamine H1 receptor in Cavia porcellus (guinea pig) ileum assessed as inhibition of electrically-induced contraction
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1007/s00044-012-0090-2
3957 2489 43 None 2 12 Guinea pig 9.5 pKd = 9.5 Binding
Antagonist activity at histamine H1 receptor in Cavia porcellus (guinea pig) ileum assessed as inhibition of electrically-induced contractionAntagonist activity at histamine H1 receptor in Cavia porcellus (guinea pig) ileum assessed as inhibition of electrically-induced contraction
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1007/s00044-012-0090-2
4992 2489 43 None 2 12 Guinea pig 9.5 pKd = 9.5 Binding
Antagonist activity at histamine H1 receptor in Cavia porcellus (guinea pig) ileum assessed as inhibition of electrically-induced contractionAntagonist activity at histamine H1 receptor in Cavia porcellus (guinea pig) ileum assessed as inhibition of electrically-induced contraction
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1007/s00044-012-0090-2
CHEMBL511 2489 43 None 2 12 Guinea pig 9.5 pKd = 9.5 Binding
Antagonist activity at histamine H1 receptor in Cavia porcellus (guinea pig) ileum assessed as inhibition of electrically-induced contractionAntagonist activity at histamine H1 receptor in Cavia porcellus (guinea pig) ileum assessed as inhibition of electrically-induced contraction
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1007/s00044-012-0090-2
DB06691 2489 43 None 2 12 Guinea pig 9.5 pKd = 9.5 Binding
Antagonist activity at histamine H1 receptor in Cavia porcellus (guinea pig) ileum assessed as inhibition of electrically-induced contractionAntagonist activity at histamine H1 receptor in Cavia porcellus (guinea pig) ileum assessed as inhibition of electrically-induced contraction
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1007/s00044-012-0090-2
CHEMBL5276489 194643 0 None 70 3 Human 9.5 pKd = 9.5 Binding
Antagonist potency at human H1 receptorAntagonist potency at human H1 receptor
ChEMBL 492 8 1 5 4.4 O=C(NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O)C1CCCC1 10.1021/acsmedchemlett.7b00112
CHEMBL5315725 194643 0 None 70 3 Human 9.5 pKd = 9.5 Binding
Antagonist potency at human H1 receptorAntagonist potency at human H1 receptor
ChEMBL 492 8 1 5 4.4 O=C(NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O)C1CCCC1 10.1021/acsmedchemlett.7b00112
24824726 161109 1 None 2 6 Human 9.4 pKd = 9.4 Binding
Antagonist potency at human histamine H1 receptorAntagonist potency at human histamine H1 receptor
ChEMBL 496 11 1 6 3.6 COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL4060529 161109 1 None 2 6 Human 9.4 pKd = 9.4 Binding
Antagonist potency at human histamine H1 receptorAntagonist potency at human histamine H1 receptor
ChEMBL 496 11 1 6 3.6 COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL4117079 161109 1 None 2 6 Human 9.4 pKd = 9.4 Binding
Antagonist potency at human histamine H1 receptorAntagonist potency at human histamine H1 receptor
ChEMBL 496 11 1 6 3.6 COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL5282336 161109 1 None 2 6 Human 9.4 pKd = 9.4 Binding
Antagonist potency at human histamine H1 receptorAntagonist potency at human histamine H1 receptor
ChEMBL 496 11 1 6 3.6 COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL5286389 161109 1 None 2 6 Human 9.4 pKd = 9.4 Binding
Antagonist potency at human histamine H1 receptorAntagonist potency at human histamine H1 receptor
ChEMBL 496 11 1 6 3.6 COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL5272034 194611 0 None 10 3 Human 9.3 pKd = 9.3 Binding
Antagonist potency at human H1 receptorAntagonist potency at human H1 receptor
ChEMBL 496 11 1 6 3.6 COCCNC(=O)CCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL5315277 194611 0 None 10 3 Human 9.3 pKd = 9.3 Binding
Antagonist potency at human H1 receptorAntagonist potency at human H1 receptor
ChEMBL 496 11 1 6 3.6 COCCNC(=O)CCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL5286701 194629 0 None 12 3 Human 9.3 pKd = 9.3 Binding
Antagonist potency at human H1 receptorAntagonist potency at human H1 receptor
ChEMBL 482 10 1 6 3.3 COCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL5315483 194629 0 None 12 3 Human 9.3 pKd = 9.3 Binding
Antagonist potency at human H1 receptorAntagonist potency at human H1 receptor
ChEMBL 482 10 1 6 3.3 COCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL5269671 194600 0 None 44 3 Human 9.2 pKd = 9.2 Binding
Antagonist potency at human H1 receptorAntagonist potency at human H1 receptor
ChEMBL 466 9 1 5 4.0 CCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL5315170 194600 0 None 44 3 Human 9.2 pKd = 9.2 Binding
Antagonist potency at human H1 receptorAntagonist potency at human H1 receptor
ChEMBL 466 9 1 5 4.0 CCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
1227 2489 43 None 2 12 Guinea pig 9.2 pKd = 9.2 Binding
Antagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 minsAntagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 mins
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1039/C8MD00527C
2331 2489 43 None 2 12 Guinea pig 9.2 pKd = 9.2 Binding
Antagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 minsAntagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 mins
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1039/C8MD00527C
3957 2489 43 None 2 12 Guinea pig 9.2 pKd = 9.2 Binding
Antagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 minsAntagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 mins
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1039/C8MD00527C
4992 2489 43 None 2 12 Guinea pig 9.2 pKd = 9.2 Binding
Antagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 minsAntagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 mins
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1039/C8MD00527C
CHEMBL511 2489 43 None 2 12 Guinea pig 9.2 pKd = 9.2 Binding
Antagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 minsAntagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 mins
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1039/C8MD00527C
DB06691 2489 43 None 2 12 Guinea pig 9.2 pKd = 9.2 Binding
Antagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 minsAntagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 mins
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1039/C8MD00527C
CHEMBL5291469 194640 0 None 70 2 Human 9.1 pKd = 9.1 Binding
Antagonist potency at human H1 receptorAntagonist potency at human H1 receptor
ChEMBL 508 8 1 6 3.6 O=C(NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O)C1CCOCC1 10.1021/acsmedchemlett.7b00112
CHEMBL5315702 194640 0 None 70 2 Human 9.1 pKd = 9.1 Binding
Antagonist potency at human H1 receptorAntagonist potency at human H1 receptor
ChEMBL 508 8 1 6 3.6 O=C(NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O)C1CCOCC1 10.1021/acsmedchemlett.7b00112
277 1301 62 None 2 50 Guinea pig 9.0 pKd = 9 Binding
Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 10.1021/jm00017a019
2913 1301 62 None 2 50 Guinea pig 9.0 pKd = 9 Binding
Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 10.1021/jm00017a019
765 1301 62 None 2 50 Guinea pig 9.0 pKd = 9 Binding
Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 10.1021/jm00017a019
CHEMBL516 1301 62 None 2 50 Guinea pig 9.0 pKd = 9 Binding
Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 10.1021/jm00017a019
DB00434 1301 62 None 2 50 Guinea pig 9.0 pKd = 9 Binding
Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 10.1021/jm00017a019
1227 2489 43 None 2 12 Guinea pig 8.8 pKd = 8.8 Binding
Antagonist activity at histamine H1 receptor in guinea pig jejunum assessed as reduction in histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig jejunum assessed as reduction in histamine-induced contractions
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmcl.2015.02.037
2331 2489 43 None 2 12 Guinea pig 8.8 pKd = 8.8 Binding
Antagonist activity at histamine H1 receptor in guinea pig jejunum assessed as reduction in histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig jejunum assessed as reduction in histamine-induced contractions
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmcl.2015.02.037
3957 2489 43 None 2 12 Guinea pig 8.8 pKd = 8.8 Binding
Antagonist activity at histamine H1 receptor in guinea pig jejunum assessed as reduction in histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig jejunum assessed as reduction in histamine-induced contractions
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmcl.2015.02.037
4992 2489 43 None 2 12 Guinea pig 8.8 pKd = 8.8 Binding
Antagonist activity at histamine H1 receptor in guinea pig jejunum assessed as reduction in histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig jejunum assessed as reduction in histamine-induced contractions
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmcl.2015.02.037
CHEMBL511 2489 43 None 2 12 Guinea pig 8.8 pKd = 8.8 Binding
Antagonist activity at histamine H1 receptor in guinea pig jejunum assessed as reduction in histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig jejunum assessed as reduction in histamine-induced contractions
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmcl.2015.02.037
DB06691 2489 43 None 2 12 Guinea pig 8.8 pKd = 8.8 Binding
Antagonist activity at histamine H1 receptor in guinea pig jejunum assessed as reduction in histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig jejunum assessed as reduction in histamine-induced contractions
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmcl.2015.02.037
11291 98796 25 None 4 2 Guinea pig 8.8 pKd = 8.8 Binding
Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum
ChEMBL 261 1 0 1 3.9 CN1CCC2=C(C1)C(c1ccccc1)c1ccccc12 10.1021/jm00017a019
CHEMBL278398 98796 25 None 4 2 Guinea pig 8.8 pKd = 8.8 Binding
Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum
ChEMBL 261 1 0 1 3.9 CN1CCC2=C(C1)C(c1ccccc1)c1ccccc12 10.1021/jm00017a019
24824726 161109 1 None -2 6 Guinea pig 8.7 pKd = 8.7 Binding
Antagonist activity at histamine H1 receptor in guinea pig isolated trachea assessed as change in histamine-induced contractionAntagonist activity at histamine H1 receptor in guinea pig isolated trachea assessed as change in histamine-induced contraction
ChEMBL 496 11 1 6 3.6 COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL4060529 161109 1 None -2 6 Guinea pig 8.7 pKd = 8.7 Binding
Antagonist activity at histamine H1 receptor in guinea pig isolated trachea assessed as change in histamine-induced contractionAntagonist activity at histamine H1 receptor in guinea pig isolated trachea assessed as change in histamine-induced contraction
ChEMBL 496 11 1 6 3.6 COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL4117079 161109 1 None -2 6 Guinea pig 8.7 pKd = 8.7 Binding
Antagonist activity at histamine H1 receptor in guinea pig isolated trachea assessed as change in histamine-induced contractionAntagonist activity at histamine H1 receptor in guinea pig isolated trachea assessed as change in histamine-induced contraction
ChEMBL 496 11 1 6 3.6 COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL5282336 161109 1 None -2 6 Guinea pig 8.7 pKd = 8.7 Binding
Antagonist activity at histamine H1 receptor in guinea pig isolated trachea assessed as change in histamine-induced contractionAntagonist activity at histamine H1 receptor in guinea pig isolated trachea assessed as change in histamine-induced contraction
ChEMBL 496 11 1 6 3.6 COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL5286389 161109 1 None -2 6 Guinea pig 8.7 pKd = 8.7 Binding
Antagonist activity at histamine H1 receptor in guinea pig isolated trachea assessed as change in histamine-induced contractionAntagonist activity at histamine H1 receptor in guinea pig isolated trachea assessed as change in histamine-induced contraction
ChEMBL 496 11 1 6 3.6 COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
11097588 202138 2 None - 1 Guinea pig 8.7 pKd = 8.7 Binding
Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum
ChEMBL 269 6 0 2 3.7 Cc1ccc([C@H](OCCN(C)C)c2ccccc2)cc1 10.1021/jm00017a019
CHEMBL609131 202138 2 None - 1 Guinea pig 8.7 pKd = 8.7 Binding
Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum
ChEMBL 269 6 0 2 3.7 Cc1ccc([C@H](OCCN(C)C)c2ccccc2)cc1 10.1021/jm00017a019
168279703 191138 0 None - 1 Human 8.0 pKd = 8 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1372 37 8 13 7.6 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5188259 191138 0 None - 1 Human 8.0 pKd = 8 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1372 37 8 13 7.6 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
168279703 191138 0 None - 1 Human 8.0 pKd = 8.0 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1372 37 8 13 7.6 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5188259 191138 0 None - 1 Human 8.0 pKd = 8.0 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1372 37 8 13 7.6 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
168282752 191096 0 None - 1 Human 8.0 pKd = 8.0 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1303 32 8 13 7.3 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5187728 191096 0 None - 1 Human 8.0 pKd = 8.0 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1303 32 8 13 7.3 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
11826604 39706 0 None -7585 3 Guinea pig 5.0 pKd = 5 Binding
Activity at Histamine H1 receptor using functional H1 receptor assay on guinea pig ileumActivity at Histamine H1 receptor using functional H1 receptor assay on guinea pig ileum
ChEMBL 457 10 1 4 6.4 c1ccc2c(NCCCc3ccc(OCCCN4CCCCC4)cc3)c3c(nc2c1)CCCC3 10.1021/jm0110845
CHEMBL14754 39706 0 None -7585 3 Guinea pig 5.0 pKd = 5 Binding
Activity at Histamine H1 receptor using functional H1 receptor assay on guinea pig ileumActivity at Histamine H1 receptor using functional H1 receptor assay on guinea pig ileum
ChEMBL 457 10 1 4 6.4 c1ccc2c(NCCCc3ccc(OCCCN4CCCCC4)cc3)c3c(nc2c1)CCCC3 10.1021/jm0110845
11004759 43164 1 None -30902 3 Guinea pig 5.0 pKd = 5 Binding
Activity at Histamine H1 receptor using functional H1 receptor assay on guinea pig ileumActivity at Histamine H1 receptor using functional H1 receptor assay on guinea pig ileum
ChEMBL 443 9 1 4 6.0 c1ccc2c(NCCc3ccc(OCCCN4CCCCC4)cc3)c3c(nc2c1)CCCC3 10.1021/jm0110845
CHEMBL15056 43164 1 None -30902 3 Guinea pig 5.0 pKd = 5 Binding
Activity at Histamine H1 receptor using functional H1 receptor assay on guinea pig ileumActivity at Histamine H1 receptor using functional H1 receptor assay on guinea pig ileum
ChEMBL 443 9 1 4 6.0 c1ccc2c(NCCc3ccc(OCCCN4CCCCC4)cc3)c3c(nc2c1)CCCC3 10.1021/jm0110845
44352460 20957 0 None -707 3 Guinea pig 5.0 pKd = 5 Binding
Receptor profile was evaluated at Histamine H1 receptor of guinea pig ileumReceptor profile was evaluated at Histamine H1 receptor of guinea pig ileum
ChEMBL 238 8 1 2 3.6 CC(C)(C)CCCCOCCCc1c[nH]cn1 10.1021/jm020910m
CHEMBL131117 20957 0 None -707 3 Guinea pig 5.0 pKd = 5 Binding
Receptor profile was evaluated at Histamine H1 receptor of guinea pig ileumReceptor profile was evaluated at Histamine H1 receptor of guinea pig ileum
ChEMBL 238 8 1 2 3.6 CC(C)(C)CCCCOCCCc1c[nH]cn1 10.1021/jm020910m
155541141 176664 0 None -2 2 Guinea pig 7.0 pKd = 7.0 Binding
Antagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 minsAntagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 mins
ChEMBL 504 16 1 5 4.7 N#C/N=C(\N)N(CCCCN1CCN(CCCCCCCOc2ccccc2)CC1)Cc1ccccc1 10.1039/C8MD00527C
CHEMBL4517581 176664 0 None -2 2 Guinea pig 7.0 pKd = 7.0 Binding
Antagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 minsAntagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 mins
ChEMBL 504 16 1 5 4.7 N#C/N=C(\N)N(CCCCN1CCN(CCCCCCCOc2ccccc2)CC1)Cc1ccccc1 10.1039/C8MD00527C
CHEMBL4598140 176664 0 None -2 2 Guinea pig 7.0 pKd = 7.0 Binding
Antagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 minsAntagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 mins
ChEMBL 504 16 1 5 4.7 N#C/N=C(\N)N(CCCCN1CCN(CCCCCCCOc2ccccc2)CC1)Cc1ccccc1 10.1039/C8MD00527C
168282752 191096 0 None - 1 Human 8.0 pKd = 8.0 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1303 32 8 13 7.3 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5187728 191096 0 None - 1 Human 8.0 pKd = 8.0 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1303 32 8 13 7.3 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
90667434 109489 0 None - 1 Guinea pig 6.0 pKd = 6.0 Binding
Antagonist activity at guinea pig ileum histamine H1 receptor assessed as inhibition of histamine-induced response after 10 to 15 minsAntagonist activity at guinea pig ileum histamine H1 receptor assessed as inhibition of histamine-induced response after 10 to 15 mins
ChEMBL 313 7 2 3 1.9 CC(CC(=O)/N=C(\N)NCCCn1ccnc1)c1ccccc1 10.1039/C3MD00245D
CHEMBL3220892 109489 0 None - 1 Guinea pig 6.0 pKd = 6.0 Binding
Antagonist activity at guinea pig ileum histamine H1 receptor assessed as inhibition of histamine-induced response after 10 to 15 minsAntagonist activity at guinea pig ileum histamine H1 receptor assessed as inhibition of histamine-induced response after 10 to 15 mins
ChEMBL 313 7 2 3 1.9 CC(CC(=O)/N=C(\N)NCCCn1ccnc1)c1ccccc1 10.1039/C3MD00245D
168288124 191727 0 None - 1 Human 7.9 pKd = 7.9 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1259 31 7 12 6.9 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5197183 191727 0 None - 1 Human 7.9 pKd = 7.9 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1259 31 7 12 6.9 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
168288124 191727 0 None - 1 Human 7.9 pKd = 7.9 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1259 31 7 12 6.9 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5197183 191727 0 None - 1 Human 7.9 pKd = 7.9 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1259 31 7 12 6.9 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
155540438 172541 0 None -7 2 Guinea pig 5.9 pKd = 5.9 Binding
Antagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions after 15 minsAntagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions after 15 mins
ChEMBL 290 3 1 6 1.3 CN1CCN(c2nc(N)nc(CC3CCCCC3)n2)CC1 10.1016/j.bmc.2019.02.020
CHEMBL4483783 172541 0 None -7 2 Guinea pig 5.9 pKd = 5.9 Binding
Antagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions after 15 minsAntagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions after 15 mins
ChEMBL 290 3 1 6 1.3 CN1CCN(c2nc(N)nc(CC3CCCCC3)n2)CC1 10.1016/j.bmc.2019.02.020
155561756 176416 0 None -28 2 Guinea pig 6.9 pKd = 6.9 Binding
Antagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 minsAntagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 mins
ChEMBL 546 16 2 3 7.3 N=C(N)N(CCCCC1CCN(CCCCCCCOc2ccccc2)CC1)Cc1ccc(C(F)(F)F)cc1 10.1039/C8MD00527C
CHEMBL4585110 176416 0 None -28 2 Guinea pig 6.9 pKd = 6.9 Binding
Antagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 minsAntagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 mins
ChEMBL 546 16 2 3 7.3 N=C(N)N(CCCCC1CCN(CCCCCCCOc2ccccc2)CC1)Cc1ccc(C(F)(F)F)cc1 10.1039/C8MD00527C
CHEMBL4596105 176416 0 None -28 2 Guinea pig 6.9 pKd = 6.9 Binding
Antagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 minsAntagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 mins
ChEMBL 546 16 2 3 7.3 N=C(N)N(CCCCC1CCN(CCCCCCCOc2ccccc2)CC1)Cc1ccc(C(F)(F)F)cc1 10.1039/C8MD00527C
10902522 18976 0 None -1000 3 Guinea pig 4.9 pKd = 4.9 Binding
Receptor profile was evaluated at Histamine H1 receptor of guinea pig ileumReceptor profile was evaluated at Histamine H1 receptor of guinea pig ileum
ChEMBL 295 5 2 3 3.5 CC(C)(C)C(NC(=O)OCCCc1c[nH]cn1)C(C)(C)C 10.1021/jm020910m
CHEMBL128773 18976 0 None -1000 3 Guinea pig 4.9 pKd = 4.9 Binding
Receptor profile was evaluated at Histamine H1 receptor of guinea pig ileumReceptor profile was evaluated at Histamine H1 receptor of guinea pig ileum
ChEMBL 295 5 2 3 3.5 CC(C)(C)C(NC(=O)OCCCc1c[nH]cn1)C(C)(C)C 10.1021/jm020910m
168284216 190877 0 None - 1 Human 5.9 pKd = 5.9 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1112 30 9 12 1.8 Cc1cc(C)n2c1C=C1C=CC(CCC(=O)NCCCC[C@H](NC(=O)CCNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)CCN3CCC(Oc4ccccc4Cc4ccccc4)CC3)C(C)C)C(N)=O)=[N+]1[B-]2(F)F 10.1021/acs.jmedchem.2c00125
CHEMBL5184842 190877 0 None - 1 Human 5.9 pKd = 5.9 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1112 30 9 12 1.8 Cc1cc(C)n2c1C=C1C=CC(CCC(=O)NCCCC[C@H](NC(=O)CCNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)CCN3CCC(Oc4ccccc4Cc4ccccc4)CC3)C(C)C)C(N)=O)=[N+]1[B-]2(F)F 10.1021/acs.jmedchem.2c00125
168284216 190877 0 None - 1 Human 5.9 pKd = 5.9 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1112 30 9 12 1.8 Cc1cc(C)n2c1C=C1C=CC(CCC(=O)NCCCC[C@H](NC(=O)CCNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)CCN3CCC(Oc4ccccc4Cc4ccccc4)CC3)C(C)C)C(N)=O)=[N+]1[B-]2(F)F 10.1021/acs.jmedchem.2c00125
CHEMBL5184842 190877 0 None - 1 Human 5.9 pKd = 5.9 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1112 30 9 12 1.8 Cc1cc(C)n2c1C=C1C=CC(CCC(=O)NCCCC[C@H](NC(=O)CCNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)CCN3CCC(Oc4ccccc4Cc4ccccc4)CC3)C(C)C)C(N)=O)=[N+]1[B-]2(F)F 10.1021/acs.jmedchem.2c00125
168269144 189998 0 None - 1 Human 7.9 pKd = 7.9 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1193 28 6 14 6.0 C[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)NCCC(=O)N[C@@H](CCCn1cc(COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)nn1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5171227 189998 0 None - 1 Human 7.9 pKd = 7.9 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1193 28 6 14 6.0 C[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)NCCC(=O)N[C@@H](CCCn1cc(COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)nn1)C(N)=O 10.1021/acs.jmedchem.2c00125
25149335 184225 0 None - 1 Guinea pig 5.9 pKd = 5.9 Binding
Antagonist activity at guinea pig ileum histamine H1 receptor assessed as inhibition of histamine-induced response after 10 to 15 minsAntagonist activity at guinea pig ileum histamine H1 receptor assessed as inhibition of histamine-induced response after 10 to 15 mins
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1039/C3MD00245D
CHEMBL483406 184225 0 None - 1 Guinea pig 5.9 pKd = 5.9 Binding
Antagonist activity at guinea pig ileum histamine H1 receptor assessed as inhibition of histamine-induced response after 10 to 15 minsAntagonist activity at guinea pig ileum histamine H1 receptor assessed as inhibition of histamine-induced response after 10 to 15 mins
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1039/C3MD00245D
168269144 189998 0 None - 1 Human 7.9 pKd = 7.9 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1193 28 6 14 6.0 C[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)NCCC(=O)N[C@@H](CCCn1cc(COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)nn1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5171227 189998 0 None - 1 Human 7.9 pKd = 7.9 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1193 28 6 14 6.0 C[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)NCCC(=O)N[C@@H](CCCn1cc(COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)nn1)C(N)=O 10.1021/acs.jmedchem.2c00125
168282405 191207 0 None - 1 Human 5.8 pKd = 5.8 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1101 28 7 10 4.5 Cc1cc(C)n2c1C=C1C=CC(CCC(=O)NCCCC[C@H](NC(=O)CCNC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc3ccccc3)NC(=O)CCN3CCC(Oc4ccccc4Cc4ccccc4)CC3)C(N)=O)=[N+]1[B-]2(F)F 10.1021/acs.jmedchem.2c00125
CHEMBL5189492 191207 0 None - 1 Human 5.8 pKd = 5.8 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1101 28 7 10 4.5 Cc1cc(C)n2c1C=C1C=CC(CCC(=O)NCCCC[C@H](NC(=O)CCNC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc3ccccc3)NC(=O)CCN3CCC(Oc4ccccc4Cc4ccccc4)CC3)C(N)=O)=[N+]1[B-]2(F)F 10.1021/acs.jmedchem.2c00125
168282405 191207 0 None - 1 Human 5.8 pKd = 5.8 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1101 28 7 10 4.5 Cc1cc(C)n2c1C=C1C=CC(CCC(=O)NCCCC[C@H](NC(=O)CCNC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc3ccccc3)NC(=O)CCN3CCC(Oc4ccccc4Cc4ccccc4)CC3)C(N)=O)=[N+]1[B-]2(F)F 10.1021/acs.jmedchem.2c00125
CHEMBL5189492 191207 0 None - 1 Human 5.8 pKd = 5.8 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1101 28 7 10 4.5 Cc1cc(C)n2c1C=C1C=CC(CCC(=O)NCCCC[C@H](NC(=O)CCNC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc3ccccc3)NC(=O)CCN3CCC(Oc4ccccc4Cc4ccccc4)CC3)C(N)=O)=[N+]1[B-]2(F)F 10.1021/acs.jmedchem.2c00125
90667234 109473 0 None - 1 Guinea pig 5.8 pKd = 5.8 Binding
Antagonist activity at guinea pig ileum histamine H1 receptor assessed as inhibition of histamine-induced response after 10 to 15 minsAntagonist activity at guinea pig ileum histamine H1 receptor assessed as inhibition of histamine-induced response after 10 to 15 mins
ChEMBL 314 7 3 3 1.4 CC(CC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1039/C3MD00245D
CHEMBL3220635 109473 0 None - 1 Guinea pig 5.8 pKd = 5.8 Binding
Antagonist activity at guinea pig ileum histamine H1 receptor assessed as inhibition of histamine-induced response after 10 to 15 minsAntagonist activity at guinea pig ileum histamine H1 receptor assessed as inhibition of histamine-induced response after 10 to 15 mins
ChEMBL 314 7 3 3 1.4 CC(CC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1039/C3MD00245D
168281594 191269 0 None - 1 Human 7.8 pKd = 7.8 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1319 33 9 14 6.2 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5190566 191269 0 None - 1 Human 7.8 pKd = 7.8 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1319 33 9 14 6.2 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
102596130 117699 21 None - 1 Guinea pig 6.8 pKd = 6.8 Binding
Antagonist activity at histamine H1 receptor in guinea pig jejunum assessed as reduction in histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig jejunum assessed as reduction in histamine-induced contractions
ChEMBL 405 0 0 5 4.0 O=C(N1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1)n1cncn1 10.1016/j.bmcl.2015.02.037
CHEMBL3401455 117699 21 None - 1 Guinea pig 6.8 pKd = 6.8 Binding
Antagonist activity at histamine H1 receptor in guinea pig jejunum assessed as reduction in histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig jejunum assessed as reduction in histamine-induced contractions
ChEMBL 405 0 0 5 4.0 O=C(N1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1)n1cncn1 10.1016/j.bmcl.2015.02.037
155554852 176612 0 None 10 2 Guinea pig 6.8 pKd = 6.8 Binding
Antagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 minsAntagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 mins
ChEMBL 339 11 2 2 4.4 N=C(N)N(CCCCCCCOc1ccccc1)Cc1ccccc1 10.1039/C8MD00527C
CHEMBL4550675 176612 0 None 10 2 Guinea pig 6.8 pKd = 6.8 Binding
Antagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 minsAntagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 mins
ChEMBL 339 11 2 2 4.4 N=C(N)N(CCCCCCCOc1ccccc1)Cc1ccccc1 10.1039/C8MD00527C
CHEMBL4597766 176612 0 None 10 2 Guinea pig 6.8 pKd = 6.8 Binding
Antagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 minsAntagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 mins
ChEMBL 339 11 2 2 4.4 N=C(N)N(CCCCCCCOc1ccccc1)Cc1ccccc1 10.1039/C8MD00527C
11437142 202606 2 None - 1 Guinea pig 6.8 pKd = 6.8 Binding
Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum
ChEMBL 269 6 0 2 3.7 Cc1ccc([C@@H](OCCN(C)C)c2ccccc2)cc1 10.1021/jm00017a019
CHEMBL612084 202606 2 None - 1 Guinea pig 6.8 pKd = 6.8 Binding
Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum
ChEMBL 269 6 0 2 3.7 Cc1ccc([C@@H](OCCN(C)C)c2ccccc2)cc1 10.1021/jm00017a019
168281594 191269 0 None - 1 Human 7.8 pKd = 7.8 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1319 33 9 14 6.2 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5190566 191269 0 None - 1 Human 7.8 pKd = 7.8 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1319 33 9 14 6.2 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
168297910 192453 0 None - 1 Human 6.8 pKd = 6.8 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1223 29 7 15 5.0 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cn1cc(COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)nn1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5208512 192453 0 None - 1 Human 6.8 pKd = 6.8 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1223 29 7 15 5.0 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cn1cc(COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)nn1)C(N)=O 10.1021/acs.jmedchem.2c00125
168297910 192453 0 None - 1 Human 6.8 pKd = 6.8 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1223 29 7 15 5.0 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cn1cc(COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)nn1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5208512 192453 0 None - 1 Human 6.8 pKd = 6.8 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1223 29 7 15 5.0 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cn1cc(COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)nn1)C(N)=O 10.1021/acs.jmedchem.2c00125
90667235 109474 0 None - 1 Guinea pig 5.8 pKd = 5.8 Binding
Antagonist activity at guinea pig ileum histamine H1 receptor assessed as inhibition of histamine-induced response after 10 to 15 minsAntagonist activity at guinea pig ileum histamine H1 receptor assessed as inhibition of histamine-induced response after 10 to 15 mins
ChEMBL 376 8 3 3 2.4 N/C(=N\C(=O)CC(c1ccccc1)c1ccccc1)NCCCc1ncn[nH]1 10.1039/C3MD00245D
CHEMBL3220636 109474 0 None - 1 Guinea pig 5.8 pKd = 5.8 Binding
Antagonist activity at guinea pig ileum histamine H1 receptor assessed as inhibition of histamine-induced response after 10 to 15 minsAntagonist activity at guinea pig ileum histamine H1 receptor assessed as inhibition of histamine-induced response after 10 to 15 mins
ChEMBL 376 8 3 3 2.4 N/C(=N\C(=O)CC(c1ccccc1)c1ccccc1)NCCCc1ncn[nH]1 10.1039/C3MD00245D
168280897 190786 0 None - 1 Human 7.8 pKd = 7.8 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1383 39 10 15 4.9 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5183511 190786 0 None - 1 Human 7.8 pKd = 7.8 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1383 39 10 15 4.9 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
168280897 190786 0 None - 1 Human 7.7 pKd = 7.7 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1383 39 10 15 4.9 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5183511 190786 0 None - 1 Human 7.7 pKd = 7.7 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1383 39 10 15 4.9 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
168285825 191547 0 None - 1 Human 7.7 pKd = 7.7 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1278 31 8 16 4.7 CC(C)[C@H](NC(=O)CCN(C)CC/C=C1\c2ccccc2COc2ccccc21)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCn1cc(COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)nn1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5194541 191547 0 None - 1 Human 7.7 pKd = 7.7 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1278 31 8 16 4.7 CC(C)[C@H](NC(=O)CCN(C)CC/C=C1\c2ccccc2COc2ccccc21)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCn1cc(COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)nn1)C(N)=O 10.1021/acs.jmedchem.2c00125
168285825 191547 0 None - 1 Human 7.7 pKd = 7.7 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1278 31 8 16 4.7 CC(C)[C@H](NC(=O)CCN(C)CC/C=C1\c2ccccc2COc2ccccc21)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCn1cc(COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)nn1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5194541 191547 0 None - 1 Human 7.7 pKd = 7.7 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1278 31 8 16 4.7 CC(C)[C@H](NC(=O)CCN(C)CC/C=C1\c2ccccc2COc2ccccc21)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCn1cc(COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)nn1)C(N)=O 10.1021/acs.jmedchem.2c00125
168280529 190784 0 None - 1 Human 7.7 pKd = 7.7 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1280 32 8 16 4.5 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCn1cc(COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)nn1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5183487 190784 0 None - 1 Human 7.7 pKd = 7.7 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1280 32 8 16 4.5 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCn1cc(COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)nn1)C(N)=O 10.1021/acs.jmedchem.2c00125
168292310 191974 0 None - 1 Human 7.7 pKd = 7.7 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1093 23 5 13 5.7 C[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cn1cc(COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)nn1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5201153 191974 0 None - 1 Human 7.7 pKd = 7.7 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1093 23 5 13 5.7 C[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cn1cc(COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)nn1)C(N)=O 10.1021/acs.jmedchem.2c00125
1605 2342 117 None -2 4 Human 6.7 pKd = 6.7 Binding
Binding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assayBinding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assay
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1021/acs.jmedchem.0c00483
3957 2342 117 None -2 4 Human 6.7 pKd = 6.7 Binding
Binding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assayBinding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assay
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1021/acs.jmedchem.0c00483
7216 2342 117 None -2 4 Human 6.7 pKd = 6.7 Binding
Binding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assayBinding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assay
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1021/acs.jmedchem.0c00483
CHEMBL998 2342 117 None -2 4 Human 6.7 pKd = 6.7 Binding
Binding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assayBinding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assay
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1021/acs.jmedchem.0c00483
DB00455 2342 117 None -2 4 Human 6.7 pKd = 6.7 Binding
Binding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assayBinding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assay
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1021/acs.jmedchem.0c00483
4161540 116089 26 None - 1 Human 6.7 pKd = 6.7 Binding
Binding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assayBinding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assay
ChEMBL 412 2 1 4 4.4 CCOC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3c(CO)ccnc32)CC1 10.1021/acs.jmedchem.0c00483
CHEMBL3357022 116089 26 None - 1 Human 6.7 pKd = 6.7 Binding
Binding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assayBinding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assay
ChEMBL 412 2 1 4 4.4 CCOC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3c(CO)ccnc32)CC1 10.1021/acs.jmedchem.0c00483
60150162 173866 0 None -32 5 Guinea pig 6.7 pKd = 6.7 Binding
Antagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 5 mins followed by histamine addition during 30 mins equilibration period with washing every 10 minsAntagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 5 mins followed by histamine addition during 30 mins equilibration period with washing every 10 mins
ChEMBL 479 16 2 4 4.8 N=C(N)N(CCCCN1CCN(CCCCCCCOc2ccccc2)CC1)Cc1ccccc1 10.1039/C8MD00527C
CHEMBL4539444 173866 0 None -32 5 Guinea pig 6.7 pKd = 6.7 Binding
Antagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 5 mins followed by histamine addition during 30 mins equilibration period with washing every 10 minsAntagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 5 mins followed by histamine addition during 30 mins equilibration period with washing every 10 mins
ChEMBL 479 16 2 4 4.8 N=C(N)N(CCCCN1CCN(CCCCCCCOc2ccccc2)CC1)Cc1ccccc1 10.1039/C8MD00527C
10933521 163465 0 None -100 3 Guinea pig 5.7 pKd = 5.7 Binding
Receptor profile was evaluated at Histamine H1 receptor of guinea pig ileumReceptor profile was evaluated at Histamine H1 receptor of guinea pig ileum
ChEMBL 237 6 2 3 1.9 CC(NC(=O)OCCCc1c[nH]cn1)C1CC1 10.1021/jm020910m
CHEMBL419975 163465 0 None -100 3 Guinea pig 5.7 pKd = 5.7 Binding
Receptor profile was evaluated at Histamine H1 receptor of guinea pig ileumReceptor profile was evaluated at Histamine H1 receptor of guinea pig ileum
ChEMBL 237 6 2 3 1.9 CC(NC(=O)OCCCc1c[nH]cn1)C1CC1 10.1021/jm020910m
10977121 20784 2 None -3715 3 Guinea pig 4.7 pKd = 4.7 Binding
Receptor profile was evaluated at Histamine H1 receptor of guinea pig ileumReceptor profile was evaluated at Histamine H1 receptor of guinea pig ileum
ChEMBL 224 7 1 2 3.2 CC(C)(C)CCCOCCCc1c[nH]cn1 10.1021/jm020910m
CHEMBL130958 20784 2 None -3715 3 Guinea pig 4.7 pKd = 4.7 Binding
Receptor profile was evaluated at Histamine H1 receptor of guinea pig ileumReceptor profile was evaluated at Histamine H1 receptor of guinea pig ileum
ChEMBL 224 7 1 2 3.2 CC(C)(C)CCCOCCCc1c[nH]cn1 10.1021/jm020910m
168280529 190784 0 None - 1 Human 7.7 pKd = 7.7 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1280 32 8 16 4.5 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCn1cc(COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)nn1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5183487 190784 0 None - 1 Human 7.7 pKd = 7.7 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1280 32 8 16 4.5 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCn1cc(COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)nn1)C(N)=O 10.1021/acs.jmedchem.2c00125
168292310 191974 0 None - 1 Human 7.7 pKd = 7.7 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1093 23 5 13 5.7 C[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cn1cc(COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)nn1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5201153 191974 0 None - 1 Human 7.7 pKd = 7.7 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1093 23 5 13 5.7 C[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cn1cc(COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)nn1)C(N)=O 10.1021/acs.jmedchem.2c00125
12884174 177738 2 None - 1 Human 6.7 pKd = 6.7 Binding
Binding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assayBinding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assay
ChEMBL 348 1 0 3 4.2 CCOC(=O)N1CCC(=C2c3ccccc3CCc3cccnc32)CC1 10.1021/acs.jmedchem.0c00483
CHEMBL4642460 177738 2 None - 1 Human 6.7 pKd = 6.7 Binding
Binding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assayBinding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assay
ChEMBL 348 1 0 3 4.2 CCOC(=O)N1CCC(=C2c3ccccc3CCc3cccnc32)CC1 10.1021/acs.jmedchem.0c00483
168269973 189926 0 None - 1 Human 6.7 pKd = 6.7 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1166 31 9 13 2.9 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)CCC1=[N+]2C(=Cc3ccc(-c4cccs4)n3[B-]2(F)F)C=C1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5169978 189926 0 None - 1 Human 6.7 pKd = 6.7 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1166 31 9 13 2.9 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)CCC1=[N+]2C(=Cc3ccc(-c4cccs4)n3[B-]2(F)F)C=C1)C(N)=O 10.1021/acs.jmedchem.2c00125
168269973 189926 0 None - 1 Human 6.7 pKd = 6.7 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1166 31 9 13 2.9 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)CCC1=[N+]2C(=Cc3ccc(-c4cccs4)n3[B-]2(F)F)C=C1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5169978 189926 0 None - 1 Human 6.7 pKd = 6.7 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1166 31 9 13 2.9 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)CCC1=[N+]2C(=Cc3ccc(-c4cccs4)n3[B-]2(F)F)C=C1)C(N)=O 10.1021/acs.jmedchem.2c00125
6604035 168075 6 None - 1 Guinea pig 6.7 pKd = 6.7 Binding
Inhibition of specific binding of [3H]mepyramine to Histamine 1 receptors in guinea-pigInhibition of specific binding of [3H]mepyramine to Histamine 1 receptors in guinea-pig
ChEMBL 471 8 2 3 6.4 CC(C)(C)c1ccc([C@@H](O)CCCN2CCC(C(O)(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/S0960-894X(00)80261-9
CHEMBL432527 168075 6 None - 1 Guinea pig 6.7 pKd = 6.7 Binding
Inhibition of specific binding of [3H]mepyramine to Histamine 1 receptors in guinea-pigInhibition of specific binding of [3H]mepyramine to Histamine 1 receptors in guinea-pig
ChEMBL 471 8 2 3 6.4 CC(C)(C)c1ccc([C@@H](O)CCCN2CCC(C(O)(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/S0960-894X(00)80261-9
168280244 190971 0 None - 1 Human 5.7 pKd = 5.7 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1462 38 10 17 4.5 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)CCCCC[N+]1=C(/C=C/C=C/C=C2/N(C)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(C)c2cc(S(=O)(=O)O)ccc21)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5186049 190971 0 None - 1 Human 5.7 pKd = 5.7 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1462 38 10 17 4.5 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)CCCCC[N+]1=C(/C=C/C=C/C=C2/N(C)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(C)c2cc(S(=O)(=O)O)ccc21)C(N)=O 10.1021/acs.jmedchem.2c00125
168284928 191384 0 None - 1 Human 5.7 pKd = 5.7 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1451 36 8 15 7.2 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)CCCCC[N+]1=C(/C=C/C=C/C=C2/N(C)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(C)c2cc(S(=O)(=O)O)ccc21)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5192377 191384 0 None - 1 Human 5.7 pKd = 5.7 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1451 36 8 15 7.2 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)CCCCC[N+]1=C(/C=C/C=C/C=C2/N(C)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(C)c2cc(S(=O)(=O)O)ccc21)C(N)=O 10.1021/acs.jmedchem.2c00125
168280244 190971 0 None - 1 Human 5.7 pKd = 5.7 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1462 38 10 17 4.5 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)CCCCC[N+]1=C(/C=C/C=C/C=C2/N(C)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(C)c2cc(S(=O)(=O)O)ccc21)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5186049 190971 0 None - 1 Human 5.7 pKd = 5.7 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1462 38 10 17 4.5 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)CCCCC[N+]1=C(/C=C/C=C/C=C2/N(C)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(C)c2cc(S(=O)(=O)O)ccc21)C(N)=O 10.1021/acs.jmedchem.2c00125
168284928 191384 0 None - 1 Human 5.7 pKd = 5.7 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1451 36 8 15 7.2 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)CCCCC[N+]1=C(/C=C/C=C/C=C2/N(C)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(C)c2cc(S(=O)(=O)O)ccc21)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5192377 191384 0 None - 1 Human 5.7 pKd = 5.7 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1451 36 8 15 7.2 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)CCCCC[N+]1=C(/C=C/C=C/C=C2/N(C)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(C)c2cc(S(=O)(=O)O)ccc21)C(N)=O 10.1021/acs.jmedchem.2c00125
60150166 174724 0 None -60 5 Guinea pig 6.7 pKd = 6.7 Binding
Antagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 5 mins followed by histamine addition during 30 mins equilibration period with washing every 10 minsAntagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 5 mins followed by histamine addition during 30 mins equilibration period with washing every 10 mins
ChEMBL 524 17 2 6 4.7 N=C(N)N(CCCCN1CCN(CCCCCCCOc2ccccc2)CC1)Cc1ccc([N+](=O)[O-])cc1 10.1039/C8MD00527C
CHEMBL4560123 174724 0 None -60 5 Guinea pig 6.7 pKd = 6.7 Binding
Antagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 5 mins followed by histamine addition during 30 mins equilibration period with washing every 10 minsAntagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 5 mins followed by histamine addition during 30 mins equilibration period with washing every 10 mins
ChEMBL 524 17 2 6 4.7 N=C(N)N(CCCCN1CCN(CCCCCCCOc2ccccc2)CC1)Cc1ccc([N+](=O)[O-])cc1 10.1039/C8MD00527C
156012610 177394 0 None - 1 Human 6.6 pKd = 6.6 Binding
Binding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assayBinding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assay
ChEMBL 400 1 0 3 5.4 CCOC(=O)N1CCC(=C2c3ccc(Cl)cc3CC(F)c3cccnc32)CC1 10.1021/acs.jmedchem.0c00483
CHEMBL4638183 177394 0 None - 1 Human 6.6 pKd = 6.6 Binding
Binding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assayBinding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assay
ChEMBL 400 1 0 3 5.4 CCOC(=O)N1CCC(=C2c3ccc(Cl)cc3CC(F)c3cccnc32)CC1 10.1021/acs.jmedchem.0c00483
90667227 109468 0 None - 1 Guinea pig 5.6 pKd = 5.6 Binding
Antagonist activity at guinea pig ileum histamine H1 receptor assessed as inhibition of histamine-induced response after 10 to 15 minsAntagonist activity at guinea pig ileum histamine H1 receptor assessed as inhibition of histamine-induced response after 10 to 15 mins
ChEMBL 375 8 2 3 2.9 N/C(=N\C(=O)CC(c1ccccc1)c1ccccc1)NCCCn1ccnc1 10.1039/C3MD00245D
CHEMBL3220628 109468 0 None - 1 Guinea pig 5.6 pKd = 5.6 Binding
Antagonist activity at guinea pig ileum histamine H1 receptor assessed as inhibition of histamine-induced response after 10 to 15 minsAntagonist activity at guinea pig ileum histamine H1 receptor assessed as inhibition of histamine-induced response after 10 to 15 mins
ChEMBL 375 8 2 3 2.9 N/C(=N\C(=O)CC(c1ccccc1)c1ccccc1)NCCCn1ccnc1 10.1039/C3MD00245D
155540201 172908 0 None -15 5 Guinea pig 6.6 pKd = 6.6 Binding
Antagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 5 mins followed by histamine addition during 30 mins equilibration period with washing every 10 minsAntagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 5 mins followed by histamine addition during 30 mins equilibration period with washing every 10 mins
ChEMBL 513 16 2 4 5.5 N=C(N)N(CCCCN1CCN(CCCCCCCOc2ccccc2)CC1)Cc1ccc(Cl)cc1 10.1039/C8MD00527C
CHEMBL4516173 172908 0 None -15 5 Guinea pig 6.6 pKd = 6.6 Binding
Antagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 5 mins followed by histamine addition during 30 mins equilibration period with washing every 10 minsAntagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 5 mins followed by histamine addition during 30 mins equilibration period with washing every 10 mins
ChEMBL 513 16 2 4 5.5 N=C(N)N(CCCCN1CCN(CCCCCCCOc2ccccc2)CC1)Cc1ccc(Cl)cc1 10.1039/C8MD00527C
124087 1389 114 None 3 15 Human 7.6 pKd = 7.6 Binding
Binding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assayBinding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1021/acs.jmedchem.0c00483
7157 1389 114 None 3 15 Human 7.6 pKd = 7.6 Binding
Binding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assayBinding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1021/acs.jmedchem.0c00483
814 1389 114 None 3 15 Human 7.6 pKd = 7.6 Binding
Binding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assayBinding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1021/acs.jmedchem.0c00483
CHEMBL1172 1389 114 None 3 15 Human 7.6 pKd = 7.6 Binding
Binding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assayBinding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1021/acs.jmedchem.0c00483
DB00967 1389 114 None 3 15 Human 7.6 pKd = 7.6 Binding
Binding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assayBinding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1021/acs.jmedchem.0c00483
10916261 35292 0 None -30902 3 Guinea pig 5.6 pKd = 5.6 Binding
Activity at Histamine H1 receptor using functional H1 receptor assay on guinea pig ileumActivity at Histamine H1 receptor using functional H1 receptor assay on guinea pig ileum
ChEMBL 395 7 1 4 5.9 Clc1ccc2c(Nc3ccc(OCCCN4CCCCC4)cc3)ccnc2c1 10.1021/jm0110845
CHEMBL14364 35292 0 None -30902 3 Guinea pig 5.6 pKd = 5.6 Binding
Activity at Histamine H1 receptor using functional H1 receptor assay on guinea pig ileumActivity at Histamine H1 receptor using functional H1 receptor assay on guinea pig ileum
ChEMBL 395 7 1 4 5.9 Clc1ccc2c(Nc3ccc(OCCCN4CCCCC4)cc3)ccnc2c1 10.1021/jm0110845
9794557 19999 0 None -83 3 Guinea pig 4.6 pKd = 4.6 Binding
Receptor profile was evaluated at Histamine H1 receptor of guinea pig ileumReceptor profile was evaluated at Histamine H1 receptor of guinea pig ileum
ChEMBL 227 6 0 2 3.3 CC(C)(C)CCOCCCN1CCCCC1 10.1021/jm020910m
CHEMBL130331 19999 0 None -83 3 Guinea pig 4.6 pKd = 4.6 Binding
Receptor profile was evaluated at Histamine H1 receptor of guinea pig ileumReceptor profile was evaluated at Histamine H1 receptor of guinea pig ileum
ChEMBL 227 6 0 2 3.3 CC(C)(C)CCOCCCN1CCCCC1 10.1021/jm020910m
156013234 177503 0 None - 1 Human 6.6 pKd = 6.6 Binding
Binding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assayBinding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assay
ChEMBL 398 1 1 4 4.4 CCOC(=O)N1CCC(=C2c3ccc(Cl)cc3C(O)Cc3cccnc32)CC1 10.1021/acs.jmedchem.0c00483
CHEMBL4639563 177503 0 None - 1 Human 6.6 pKd = 6.6 Binding
Binding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assayBinding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assay
ChEMBL 398 1 1 4 4.4 CCOC(=O)N1CCC(=C2c3ccc(Cl)cc3C(O)Cc3cccnc32)CC1 10.1021/acs.jmedchem.0c00483
90667233 109472 0 None - 1 Guinea pig 5.6 pKd = 5.6 Binding
Antagonist activity at guinea pig ileum histamine H1 receptor assessed as inhibition of histamine-induced response after 10 to 15 minsAntagonist activity at guinea pig ileum histamine H1 receptor assessed as inhibition of histamine-induced response after 10 to 15 mins
ChEMBL 375 8 3 2 3.0 N/C(=N\C(=O)CC(c1ccccc1)c1ccccc1)NCCCc1cn[nH]c1 10.1039/C3MD00245D
CHEMBL3220634 109472 0 None - 1 Guinea pig 5.6 pKd = 5.6 Binding
Antagonist activity at guinea pig ileum histamine H1 receptor assessed as inhibition of histamine-induced response after 10 to 15 minsAntagonist activity at guinea pig ileum histamine H1 receptor assessed as inhibition of histamine-induced response after 10 to 15 mins
ChEMBL 375 8 3 2 3.0 N/C(=N\C(=O)CC(c1ccccc1)c1ccccc1)NCCCc1cn[nH]c1 10.1039/C3MD00245D
168281433 190959 0 None - 1 Human 5.6 pKd = 5.6 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1214 34 8 11 5.2 Cc1cc(C)n2c1C=C1C=CC(CCC(=O)NCCCCCC(=O)NCCCC[C@H](NC(=O)CCNC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc3ccccc3)NC(=O)CCN3CCC(Oc4ccccc4Cc4ccccc4)CC3)C(N)=O)=[N+]1[B-]2(F)F 10.1021/acs.jmedchem.2c00125
CHEMBL5185960 190959 0 None - 1 Human 5.6 pKd = 5.6 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1214 34 8 11 5.2 Cc1cc(C)n2c1C=C1C=CC(CCC(=O)NCCCCCC(=O)NCCCC[C@H](NC(=O)CCNC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc3ccccc3)NC(=O)CCN3CCC(Oc4ccccc4Cc4ccccc4)CC3)C(N)=O)=[N+]1[B-]2(F)F 10.1021/acs.jmedchem.2c00125
168281433 190959 0 None - 1 Human 5.6 pKd = 5.6 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1214 34 8 11 5.2 Cc1cc(C)n2c1C=C1C=CC(CCC(=O)NCCCCCC(=O)NCCCC[C@H](NC(=O)CCNC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc3ccccc3)NC(=O)CCN3CCC(Oc4ccccc4Cc4ccccc4)CC3)C(N)=O)=[N+]1[B-]2(F)F 10.1021/acs.jmedchem.2c00125
CHEMBL5185960 190959 0 None - 1 Human 5.6 pKd = 5.6 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1214 34 8 11 5.2 Cc1cc(C)n2c1C=C1C=CC(CCC(=O)NCCCCCC(=O)NCCCC[C@H](NC(=O)CCNC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc3ccccc3)NC(=O)CCN3CCC(Oc4ccccc4Cc4ccccc4)CC3)C(N)=O)=[N+]1[B-]2(F)F 10.1021/acs.jmedchem.2c00125
156010880 177143 0 None - 1 Human 6.6 pKd = 6.6 Binding
Binding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assayBinding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assay
ChEMBL 432 2 0 3 5.8 CCOC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3c(C(F)F)ccnc32)CC1 10.1021/acs.jmedchem.0c00483
CHEMBL4633975 177143 0 None - 1 Human 6.6 pKd = 6.6 Binding
Binding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assayBinding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assay
ChEMBL 432 2 0 3 5.8 CCOC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3c(C(F)F)ccnc32)CC1 10.1021/acs.jmedchem.0c00483
168290008 191817 0 None - 1 Human 7.6 pKd = 7.6 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1180 27 7 15 4.2 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cn1cc(COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)nn1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5198557 191817 0 None - 1 Human 7.6 pKd = 7.6 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1180 27 7 15 4.2 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cn1cc(COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)nn1)C(N)=O 10.1021/acs.jmedchem.2c00125
14637775 178038 25 None - 1 Human 7.6 pKd = 7.6 Binding
Binding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assayBinding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assay
ChEMBL 326 0 2 3 3.5 OC1Cc2cc(Cl)ccc2C(=C2CCNCC2)c2ncccc21 10.1021/acs.jmedchem.0c00483
CHEMBL4647038 178038 25 None - 1 Human 7.6 pKd = 7.6 Binding
Binding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assayBinding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assay
ChEMBL 326 0 2 3 3.5 OC1Cc2cc(Cl)ccc2C(=C2CCNCC2)c2ncccc21 10.1021/acs.jmedchem.0c00483
168290008 191817 0 None - 1 Human 7.6 pKd = 7.6 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1180 27 7 15 4.2 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cn1cc(COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)nn1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5198557 191817 0 None - 1 Human 7.6 pKd = 7.6 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1180 27 7 15 4.2 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cn1cc(COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)nn1)C(N)=O 10.1021/acs.jmedchem.2c00125
155550732 176629 0 None -11 3 Guinea pig 6.5 pKd = 6.5 Binding
Antagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions incubated for 15 minsAntagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions incubated for 15 mins
ChEMBL 323 8 0 2 5.4 c1ccc(-c2ccc(OCCCCCN3CCCCC3)cc2)cc1 10.1016/j.bmc.2017.07.058
CHEMBL4540849 176629 0 None -11 3 Guinea pig 6.5 pKd = 6.5 Binding
Antagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions incubated for 15 minsAntagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions incubated for 15 mins
ChEMBL 323 8 0 2 5.4 c1ccc(-c2ccc(OCCCCCN3CCCCC3)cc2)cc1 10.1016/j.bmc.2017.07.058
CHEMBL4597895 176629 0 None -11 3 Guinea pig 6.5 pKd = 6.5 Binding
Antagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions incubated for 15 minsAntagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions incubated for 15 mins
ChEMBL 323 8 0 2 5.4 c1ccc(-c2ccc(OCCCCCN3CCCCC3)cc2)cc1 10.1016/j.bmc.2017.07.058
135398737 958 93 None 2 89 Human 8.5 pKd = 8.5 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm100064d
38 958 93 None 2 89 Human 8.5 pKd = 8.5 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm100064d
722 958 93 None 2 89 Human 8.5 pKd = 8.5 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm100064d
CHEMBL42 958 93 None 2 89 Human 8.5 pKd = 8.5 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm100064d
DB00363 958 93 None 2 89 Human 8.5 pKd = 8.5 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm100064d
168280938 190830 0 None - 1 Human 8.4 pKd = 8.4 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1270 33 9 14 4.2 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5184108 190830 0 None - 1 Human 8.4 pKd = 8.4 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1270 33 9 14 4.2 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
90667430 109488 0 None - 1 Guinea pig 5.5 pKd = 5.5 Binding
Antagonist activity at guinea pig ileum histamine H1 receptor assessed as inhibition of histamine-induced response after 10 to 15 minsAntagonist activity at guinea pig ileum histamine H1 receptor assessed as inhibition of histamine-induced response after 10 to 15 mins
ChEMBL 370 9 2 3 2.9 CC(CC(=O)/N=C(\N)NCCCc1ccc(CN(C)C)o1)c1ccccc1 10.1039/C3MD00245D
CHEMBL3220888 109488 0 None - 1 Guinea pig 5.5 pKd = 5.5 Binding
Antagonist activity at guinea pig ileum histamine H1 receptor assessed as inhibition of histamine-induced response after 10 to 15 minsAntagonist activity at guinea pig ileum histamine H1 receptor assessed as inhibition of histamine-induced response after 10 to 15 mins
ChEMBL 370 9 2 3 2.9 CC(CC(=O)/N=C(\N)NCCCc1ccc(CN(C)C)o1)c1ccccc1 10.1039/C3MD00245D
2600 3779 74 None -3 13 Guinea pig 6.5 pKd = 6.5 Binding
Inhibition of specific binding of [3H]mepyramine to Histamine 1 receptors in guinea-pigInhibition of specific binding of [3H]mepyramine to Histamine 1 receptors in guinea-pig
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1016/S0960-894X(00)80261-9
2608 3779 74 None -3 13 Guinea pig 6.5 pKd = 6.5 Binding
Inhibition of specific binding of [3H]mepyramine to Histamine 1 receptors in guinea-pigInhibition of specific binding of [3H]mepyramine to Histamine 1 receptors in guinea-pig
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1016/S0960-894X(00)80261-9
5405 3779 74 None -3 13 Guinea pig 6.5 pKd = 6.5 Binding
Inhibition of specific binding of [3H]mepyramine to Histamine 1 receptors in guinea-pigInhibition of specific binding of [3H]mepyramine to Histamine 1 receptors in guinea-pig
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1016/S0960-894X(00)80261-9
CHEMBL17157 3779 74 None -3 13 Guinea pig 6.5 pKd = 6.5 Binding
Inhibition of specific binding of [3H]mepyramine to Histamine 1 receptors in guinea-pigInhibition of specific binding of [3H]mepyramine to Histamine 1 receptors in guinea-pig
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1016/S0960-894X(00)80261-9
DB00342 3779 74 None -3 13 Guinea pig 6.5 pKd = 6.5 Binding
Inhibition of specific binding of [3H]mepyramine to Histamine 1 receptors in guinea-pigInhibition of specific binding of [3H]mepyramine to Histamine 1 receptors in guinea-pig
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1016/S0960-894X(00)80261-9
118729369 117846 0 None - 1 Guinea pig 6.5 pKd = 6.5 Binding
Antagonist activity at histamine H1 receptor in guinea pig jejunum assessed as reduction in histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig jejunum assessed as reduction in histamine-induced contractions
ChEMBL 368 0 0 4 4.3 O=C(N1CCC(=C2c3ccccc3C=Cc3ccccc32)CC1)n1cncn1 10.1016/j.bmcl.2015.02.037
CHEMBL3402827 117846 0 None - 1 Guinea pig 6.5 pKd = 6.5 Binding
Antagonist activity at histamine H1 receptor in guinea pig jejunum assessed as reduction in histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig jejunum assessed as reduction in histamine-induced contractions
ChEMBL 368 0 0 4 4.3 O=C(N1CCC(=C2c3ccccc3C=Cc3ccccc32)CC1)n1cncn1 10.1016/j.bmcl.2015.02.037
11080253 36582 0 None -2041 3 Guinea pig 5.5 pKd = 5.5 Binding
Activity at Histamine H1 receptor using functional H1 receptor assay on guinea pig ileumActivity at Histamine H1 receptor using functional H1 receptor assay on guinea pig ileum
ChEMBL 417 11 1 4 5.9 c1ccc2c(NCCCCc3ccc(OCCCN4CCCCC4)cc3)ccnc2c1 10.1021/jm0110845
CHEMBL14484 36582 0 None -2041 3 Guinea pig 5.5 pKd = 5.5 Binding
Activity at Histamine H1 receptor using functional H1 receptor assay on guinea pig ileumActivity at Histamine H1 receptor using functional H1 receptor assay on guinea pig ileum
ChEMBL 417 11 1 4 5.9 c1ccc2c(NCCCCc3ccc(OCCCN4CCCCC4)cc3)ccnc2c1 10.1021/jm0110845
11748564 18933 0 None -1584 3 Guinea pig 4.5 pKd = 4.5 Binding
Receptor profile was evaluated at Histamine H1 receptor of guinea pig ileumReceptor profile was evaluated at Histamine H1 receptor of guinea pig ileum
ChEMBL 299 7 2 3 3.2 O=C(NC(c1ccccc1)C1CC1)OCCCc1c[nH]cn1 10.1021/jm020910m
CHEMBL128585 18933 0 None -1584 3 Guinea pig 4.5 pKd = 4.5 Binding
Receptor profile was evaluated at Histamine H1 receptor of guinea pig ileumReceptor profile was evaluated at Histamine H1 receptor of guinea pig ileum
ChEMBL 299 7 2 3 3.2 O=C(NC(c1ccccc1)C1CC1)OCCCc1c[nH]cn1 10.1021/jm020910m
60150164 175759 0 None -107 2 Guinea pig 6.5 pKd = 6.5 Binding
Antagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 5 mins followed by histamine addition during 30 mins equilibration period with washing every 10 minsAntagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 5 mins followed by histamine addition during 30 mins equilibration period with washing every 10 mins
ChEMBL 547 16 2 4 5.8 N=C(N)N(CCCCN1CCN(CCCCCCCOc2ccccc2)CC1)Cc1ccc(C(F)(F)F)cc1 10.1039/C8MD00527C
CHEMBL4583515 175759 0 None -107 2 Guinea pig 6.5 pKd = 6.5 Binding
Antagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 5 mins followed by histamine addition during 30 mins equilibration period with washing every 10 minsAntagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 5 mins followed by histamine addition during 30 mins equilibration period with washing every 10 mins
ChEMBL 547 16 2 4 5.8 N=C(N)N(CCCCN1CCN(CCCCCCCOc2ccccc2)CC1)Cc1ccc(C(F)(F)F)cc1 10.1039/C8MD00527C
11725577 11183 0 None -26 3 Guinea pig 5.5 pKd = 5.5 Binding
Potency at histamine H1 receptor subtype, was tested on guinea pig right ileumPotency at histamine H1 receptor subtype, was tested on guinea pig right ileum
ChEMBL 352 7 0 4 4.6 CO/N=C(\C)c1ccc(OCc2ccc(CN3CCCCC3)cc2)cc1 10.1021/jm021084k
CHEMBL1178642 11183 0 None -26 3 Guinea pig 5.5 pKd = 5.5 Binding
Potency at histamine H1 receptor subtype, was tested on guinea pig right ileumPotency at histamine H1 receptor subtype, was tested on guinea pig right ileum
ChEMBL 352 7 0 4 4.6 CO/N=C(\C)c1ccc(OCc2ccc(CN3CCCCC3)cc2)cc1 10.1021/jm021084k
CHEMBL35869 11183 0 None -26 3 Guinea pig 5.5 pKd = 5.5 Binding
Potency at histamine H1 receptor subtype, was tested on guinea pig right ileumPotency at histamine H1 receptor subtype, was tested on guinea pig right ileum
ChEMBL 352 7 0 4 4.6 CO/N=C(\C)c1ccc(OCc2ccc(CN3CCCCC3)cc2)cc1 10.1021/jm021084k
2600 3779 74 None -3 13 Guinea pig 7.5 pKd = 7.5 Binding
Dissociation constant was determined against H1 receptor of guinea pig lung membranes using radioligand binding assays.Dissociation constant was determined against H1 receptor of guinea pig lung membranes using radioligand binding assays.
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1021/jm00013a023
2608 3779 74 None -3 13 Guinea pig 7.5 pKd = 7.5 Binding
Dissociation constant was determined against H1 receptor of guinea pig lung membranes using radioligand binding assays.Dissociation constant was determined against H1 receptor of guinea pig lung membranes using radioligand binding assays.
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1021/jm00013a023
5405 3779 74 None -3 13 Guinea pig 7.5 pKd = 7.5 Binding
Dissociation constant was determined against H1 receptor of guinea pig lung membranes using radioligand binding assays.Dissociation constant was determined against H1 receptor of guinea pig lung membranes using radioligand binding assays.
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1021/jm00013a023
CHEMBL17157 3779 74 None -3 13 Guinea pig 7.5 pKd = 7.5 Binding
Dissociation constant was determined against H1 receptor of guinea pig lung membranes using radioligand binding assays.Dissociation constant was determined against H1 receptor of guinea pig lung membranes using radioligand binding assays.
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1021/jm00013a023
DB00342 3779 74 None -3 13 Guinea pig 7.5 pKd = 7.5 Binding
Dissociation constant was determined against H1 receptor of guinea pig lung membranes using radioligand binding assays.Dissociation constant was determined against H1 receptor of guinea pig lung membranes using radioligand binding assays.
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1021/jm00013a023
7048803 102303 4 None - 1 Guinea pig 6.4 pKd = 6.4 Binding
Inhibition of specific binding of [3H]mepyramine to Histamine 1 receptors in guinea-pigInhibition of specific binding of [3H]mepyramine to Histamine 1 receptors in guinea-pig
ChEMBL 471 8 2 3 6.4 CC(C)(C)c1ccc([C@H](O)CCCN2CCC(C(O)(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/S0960-894X(00)80261-9
CHEMBL303454 102303 4 None - 1 Guinea pig 6.4 pKd = 6.4 Binding
Inhibition of specific binding of [3H]mepyramine to Histamine 1 receptors in guinea-pigInhibition of specific binding of [3H]mepyramine to Histamine 1 receptors in guinea-pig
ChEMBL 471 8 2 3 6.4 CC(C)(C)c1ccc([C@H](O)CCCN2CCC(C(O)(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/S0960-894X(00)80261-9
90667232 109471 0 None - 1 Guinea pig 5.4 pKd = 5.4 Binding
Antagonist activity at guinea pig ileum histamine H1 receptor assessed as inhibition of histamine-induced response after 10 to 15 minsAntagonist activity at guinea pig ileum histamine H1 receptor assessed as inhibition of histamine-induced response after 10 to 15 mins
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1cn[nH]c1)c1ccccc1 10.1039/C3MD00245D
CHEMBL3220633 109471 0 None - 1 Guinea pig 5.4 pKd = 5.4 Binding
Antagonist activity at guinea pig ileum histamine H1 receptor assessed as inhibition of histamine-induced response after 10 to 15 minsAntagonist activity at guinea pig ileum histamine H1 receptor assessed as inhibition of histamine-induced response after 10 to 15 mins
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1cn[nH]c1)c1ccccc1 10.1039/C3MD00245D
10949464 98189 0 None -5128 3 Guinea pig 5.4 pKd = 5.4 Binding
Activity at Histamine H1 receptor using functional H1 receptor assay on guinea pig ileumActivity at Histamine H1 receptor using functional H1 receptor assay on guinea pig ileum
ChEMBL 403 10 1 4 5.5 c1ccc2c(NCCCc3ccc(OCCCN4CCCCC4)cc3)ccnc2c1 10.1021/jm0110845
CHEMBL274041 98189 0 None -5128 3 Guinea pig 5.4 pKd = 5.4 Binding
Activity at Histamine H1 receptor using functional H1 receptor assay on guinea pig ileumActivity at Histamine H1 receptor using functional H1 receptor assay on guinea pig ileum
ChEMBL 403 10 1 4 5.5 c1ccc2c(NCCCc3ccc(OCCCN4CCCCC4)cc3)ccnc2c1 10.1021/jm0110845
44352410 19585 0 None -10 2 Guinea pig 4.4 pKd = 4.4 Binding
Receptor profile was evaluated at Histamine H1 receptor of guinea pig ileumReceptor profile was evaluated at Histamine H1 receptor of guinea pig ileum
ChEMBL 270 5 1 3 3.0 CC(NC(=O)OCCCN1CCCCC1)C(C)(C)C 10.1021/jm020910m
CHEMBL130005 19585 0 None -10 2 Guinea pig 4.4 pKd = 4.4 Binding
Receptor profile was evaluated at Histamine H1 receptor of guinea pig ileumReceptor profile was evaluated at Histamine H1 receptor of guinea pig ileum
ChEMBL 270 5 1 3 3.0 CC(NC(=O)OCCCN1CCCCC1)C(C)(C)C 10.1021/jm020910m
168280938 190830 0 None - 1 Human 8.4 pKd = 8.4 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1270 33 9 14 4.2 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5184108 190830 0 None - 1 Human 8.4 pKd = 8.4 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1270 33 9 14 4.2 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
1204 1932 119 None -501 24 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
1247 1932 119 None -501 24 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
1375 1932 119 None -501 24 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
774 1932 119 None -501 24 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
CHEMBL90 1932 119 None -501 24 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
DB05381 1932 119 None -501 24 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
119570 3159 96 None -162 40 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
2233 3159 96 None -162 40 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
953 3159 96 None -162 40 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
CHEMBL301265 3159 96 None -162 40 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
DB00413 3159 96 None -162 40 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
168268716 192762 0 None -1 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 372 3 4 4 3.5 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NC2CCCCC2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5170276 192762 0 None -1 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 372 3 4 4 3.5 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NC2CCCCC2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5221176 192762 0 None -1 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 372 3 4 4 3.5 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NC2CCCCC2)cc1 10.1021/acs.jmedchem.1c00692
168268680 192766 0 None -1 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 662 11 8 8 4.8 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5172675 192766 0 None -1 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 662 11 8 8 4.8 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5221210 192766 0 None -1 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 662 11 8 8 4.8 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1 10.1021/acs.jmedchem.1c00692
168268827 192779 0 None -4 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 450 8 4 4 4.8 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5179906 192779 0 None -4 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 450 8 4 4 4.8 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5221314 192779 0 None -4 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 450 8 4 4 4.8 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)c1 10.1021/acs.jmedchem.1c00692
168268853 192785 0 None -19 6 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 389 8 4 5 1.9 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5180504 192785 0 None -19 6 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 389 8 4 5 1.9 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5221353 192785 0 None -19 6 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 389 8 4 5 1.9 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
168273471 192801 0 None -12 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 596 17 8 10 0.7 N/C(=N\C(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5173079 192801 0 None -12 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 596 17 8 10 0.7 N/C(=N\C(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221433 192801 0 None -12 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 596 17 8 10 0.7 N/C(=N\C(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168273549 192803 0 None -1 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 436 6 4 4 4.3 Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5174342 192803 0 None -1 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 436 6 4 4 4.3 Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5221438 192803 0 None -1 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 436 6 4 4 4.3 Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1 10.1021/acs.jmedchem.1c00692
168273640 192805 0 None -100 6 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 568 15 8 10 -0.1 N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5176229 192805 0 None -100 6 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 568 15 8 10 -0.1 N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221444 192805 0 None -100 6 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 568 15 8 10 -0.1 N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168273745 192808 0 None -114 6 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 332 6 4 4 1.5 N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5178472 192808 0 None -114 6 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 332 6 4 4 1.5 N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221451 192808 0 None -114 6 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 332 6 4 4 1.5 N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
168274129 192809 0 None -16 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 370 12 5 6 1.0 NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5176780 192809 0 None -16 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 370 12 5 6 1.0 NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221468 192809 0 None -16 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 370 12 5 6 1.0 NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168275750 192826 0 None -72 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 332 6 3 4 1.6 Cc1nnc(CCCN/C(N)=N/C(=O)NCc2ccccc2)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5175558 192826 0 None -72 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 332 6 3 4 1.6 Cc1nnc(CCCN/C(N)=N/C(=O)NCc2ccccc2)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221581 192826 0 None -72 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 332 6 3 4 1.6 Cc1nnc(CCCN/C(N)=N/C(=O)NCc2ccccc2)s1 10.1021/acs.jmedchem.1c00692
168276867 192835 0 None -1 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 662 11 8 8 4.8 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5174278 192835 0 None -1 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 662 11 8 8 4.8 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5221653 192835 0 None -1 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 662 11 8 8 4.8 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)c1 10.1021/acs.jmedchem.1c00692
168277996 192846 0 None -60 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 380 4 4 4 3.3 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCc2ccccc2)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5173373 192846 0 None -60 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 380 4 4 4 3.3 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCc2ccccc2)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5221736 192846 0 None -60 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 380 4 4 4 3.3 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCc2ccccc2)c1 10.1021/acs.jmedchem.1c00692
168278471 192848 0 None -229 6 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 312 8 4 4 1.5 CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5183205 192848 0 None -229 6 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 312 8 4 4 1.5 CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221757 192848 0 None -229 6 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 312 8 4 4 1.5 CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
168278543 192851 0 None -2 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 358 4 4 4 1.6 N/C(=N\C(=O)NCc1ccccc1)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
CHEMBL5184846 192851 0 None -2 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 358 4 4 4 1.6 N/C(=N\C(=O)NCc1ccccc1)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
CHEMBL5221764 192851 0 None -2 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 358 4 4 4 1.6 N/C(=N\C(=O)NCc1ccccc1)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
168280339 192865 0 None 3 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 372 8 3 5 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCn1cc(CN(C)C)nn1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5188592 192865 0 None 3 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 372 8 3 5 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCn1cc(CN(C)C)nn1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5221885 192865 0 None 3 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 372 8 3 5 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCn1cc(CN(C)C)nn1)c1ccccc1 10.1021/acs.jmedchem.1c00692
168281536 192881 0 None -2 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 369 12 4 5 1.7 Cc1nnc(CCCN/C(N)=N/C(=O)NCCCCCCCCN)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5189006 192881 0 None -2 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 369 12 4 5 1.7 Cc1nnc(CCCN/C(N)=N/C(=O)NCCCCCCCCN)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221966 192881 0 None -2 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 369 12 4 5 1.7 Cc1nnc(CCCN/C(N)=N/C(=O)NCCCCCCCCN)s1 10.1021/acs.jmedchem.1c00692
168281746 192882 0 None -14454 6 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 365 6 4 5 1.6 CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5184911 192882 0 None -14454 6 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 365 6 4 5 1.6 CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5221974 192882 0 None -14454 6 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 365 6 4 5 1.6 CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1 10.1021/acs.jmedchem.1c00692
168283097 192893 0 None -66 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 311 9 4 5 0.8 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)o1 10.1021/acs.jmedchem.1c00692
CHEMBL5186770 192893 0 None -66 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 311 9 4 5 0.8 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)o1 10.1021/acs.jmedchem.1c00692
CHEMBL5222043 192893 0 None -66 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 311 9 4 5 0.8 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)o1 10.1021/acs.jmedchem.1c00692
168283321 192895 0 None -2 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 364 7 4 4 2.3 Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1 10.1021/acs.jmedchem.1c00692
CHEMBL5183015 192895 0 None -2 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 364 7 4 4 2.3 Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1 10.1021/acs.jmedchem.1c00692
CHEMBL5222057 192895 0 None -2 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 364 7 4 4 2.3 Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1 10.1021/acs.jmedchem.1c00692
168283536 192900 0 None -1 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 312 8 3 4 1.6 CCCCCNC(=O)/N=C(/N)NCCCc1nnc(C)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5187758 192900 0 None -1 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 312 8 3 4 1.6 CCCCCNC(=O)/N=C(/N)NCCCc1nnc(C)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222074 192900 0 None -1 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 312 8 3 4 1.6 CCCCCNC(=O)/N=C(/N)NCCCc1nnc(C)s1 10.1021/acs.jmedchem.1c00692
168284289 192906 0 None -3 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 428 8 4 4 3.1 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
CHEMBL5194860 192906 0 None -3 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 428 8 4 4 3.1 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
CHEMBL5222123 192906 0 None -3 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 428 8 4 4 3.1 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
168284480 192910 0 None -66 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 330 6 4 4 1.3 Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCc1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5197548 192910 0 None -66 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 330 6 4 4 1.3 Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCc1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222137 192910 0 None -66 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 330 6 4 4 1.3 Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCc1ccccc1 10.1021/acs.jmedchem.1c00692
168286141 192924 0 None -3 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 450 8 4 4 4.8 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5192993 192924 0 None -3 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 450 8 4 4 4.8 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222231 192924 0 None -3 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 450 8 4 4 4.8 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
168286426 192926 0 None -58 6 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 403 10 4 5 2.3 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5198795 192926 0 None -58 6 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 403 10 4 5 2.3 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222241 192926 0 None -58 6 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 403 10 4 5 2.3 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168290235 192968 0 None -12882 20 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5201074 192968 0 None -12882 20 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222491 192968 0 None -12882 20 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
168290815 192973 0 None -10232 6 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 327 9 4 5 1.2 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5200771 192973 0 None -10232 6 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 327 9 4 5 1.2 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222529 192973 0 None -10232 6 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 327 9 4 5 1.2 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168291233 192979 0 None -6 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 373 8 4 5 1.4 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)o2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5200106 192979 0 None -6 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 373 8 4 5 1.4 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)o2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222556 192979 0 None -6 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 373 8 4 5 1.4 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)o2)cc1 10.1021/acs.jmedchem.1c00692
168292954 192997 0 None -44 6 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 388 8 4 4 2.5 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5202592 192997 0 None -44 6 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 388 8 4 4 2.5 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222660 192997 0 None -44 6 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 388 8 4 4 2.5 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
168294161 193006 0 None -3 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 360 6 4 4 3.3 CCCCCNC(=O)/N=C(\N)Nc1cccc(-c2sc(N)nc2C)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5204739 193006 0 None -3 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 360 6 4 4 3.3 CCCCCNC(=O)/N=C(\N)Nc1cccc(-c2sc(N)nc2C)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5222742 193006 0 None -3 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 360 6 4 4 3.3 CCCCCNC(=O)/N=C(\N)Nc1cccc(-c2sc(N)nc2C)c1 10.1021/acs.jmedchem.1c00692
168294445 193010 0 None 1 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 414 6 4 4 2.6 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCC2CCc3nc(N)sc3C2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5208113 193010 0 None 1 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 414 6 4 4 2.6 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCC2CCc3nc(N)sc3C2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222768 193010 0 None 1 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 414 6 4 4 2.6 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCC2CCc3nc(N)sc3C2)cc1 10.1021/acs.jmedchem.1c00692
168294166 193014 0 None -1 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 360 6 4 4 3.3 CCCCCNC(=O)/N=C(\N)Nc1ccc(-c2sc(N)nc2C)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5209081 193014 0 None -1 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 360 6 4 4 3.3 CCCCCNC(=O)/N=C(\N)Nc1ccc(-c2sc(N)nc2C)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222775 193014 0 None -1 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 360 6 4 4 3.3 CCCCCNC(=O)/N=C(\N)Nc1ccc(-c2sc(N)nc2C)cc1 10.1021/acs.jmedchem.1c00692
168294449 193018 0 None -74 6 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 367 7 4 5 1.9 CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1 10.1021/acs.jmedchem.1c00692
CHEMBL5204599 193018 0 None -74 6 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 367 7 4 5 1.9 CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1 10.1021/acs.jmedchem.1c00692
CHEMBL5222793 193018 0 None -74 6 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 367 7 4 5 1.9 CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1 10.1021/acs.jmedchem.1c00692
168294767 193019 0 None -3235 20 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5207281 193019 0 None -3235 20 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222802 193019 0 None -3235 20 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168294770 193020 0 None -2 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 436 6 4 4 4.3 Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5208327 193020 0 None -2 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 436 6 4 4 4.3 Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222806 193020 0 None -2 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 436 6 4 4 4.3 Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)cc1 10.1021/acs.jmedchem.1c00692
168294776 193026 0 None -11 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 366 7 3 4 2.6 Cc1nnc(CCCN/C(N)=N/C(=O)NCC(C)C2CCCCC2)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5209479 193026 0 None -11 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 366 7 3 4 2.6 Cc1nnc(CCCN/C(N)=N/C(=O)NCC(C)C2CCCCC2)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222831 193026 0 None -11 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 366 7 3 4 2.6 Cc1nnc(CCCN/C(N)=N/C(=O)NCC(C)C2CCCCC2)s1 10.1021/acs.jmedchem.1c00692
168295528 193031 0 None -2951 20 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5206565 193031 0 None -2951 20 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222872 193031 0 None -2951 20 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168294178 193035 0 None -1 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 414 5 4 4 4.4 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)C2CCCCC2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5205197 193035 0 None -1 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 414 5 4 4 4.4 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)C2CCCCC2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222887 193035 0 None -1 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 414 5 4 4 4.4 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)C2CCCCC2)cc1 10.1021/acs.jmedchem.1c00692
168295541 193040 0 None -301 6 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 347 6 4 5 1.4 C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5208845 193040 0 None -301 6 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 347 6 4 5 1.4 C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222926 193040 0 None -301 6 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 347 6 4 5 1.4 C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1 10.1021/acs.jmedchem.1c00692
168295543 193041 0 None -1 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 380 4 4 4 3.3 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5209021 193041 0 None -1 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 380 4 4 4 3.3 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222929 193041 0 None -1 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 380 4 4 4 3.3 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
168295803 193045 0 None -3 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 338 6 4 4 1.6 CCCCCNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
CHEMBL5207206 193045 0 None -3 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 338 6 4 4 1.6 CCCCCNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
CHEMBL5222937 193045 0 None -3 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 338 6 4 4 1.6 CCCCCNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
168294182 193048 0 None -57 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 314 6 4 2 1.7 C[C@@H](NC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5208722 193048 0 None -57 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 314 6 4 2 1.7 C[C@@H](NC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222960 193048 0 None -57 4 Human 8.4 pKd = 8.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 314 6 4 2 1.7 C[C@@H](NC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/acs.jmedchem.1c00692
168286984 191392 0 None - 1 Human 8.3 pKd = 8.3 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1254 32 8 13 5.2 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5192474 191392 0 None - 1 Human 8.3 pKd = 8.3 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1254 32 8 13 5.2 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
168289844 191333 0 None - 1 Human 8.3 pKd = 8.3 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1284 34 9 14 4.6 CC[C@H](C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5191552 191333 0 None - 1 Human 8.3 pKd = 8.3 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1284 34 9 14 4.6 CC[C@H](C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
10744393 71464 0 None - 1 Human 6.4 pKd = 6.4 Binding
Dissociation constant against histamine H1 receptorDissociation constant against histamine H1 receptor
ChEMBL 514 8 2 5 4.7 O=C(N[C@H](CN1CCC(OC2c3ccccc3CCc3ccccc32)CC1)C(=O)O)OCc1ccccc1 10.1021/jm058225d
CHEMBL196220 71464 0 None - 1 Human 6.4 pKd = 6.4 Binding
Dissociation constant against histamine H1 receptorDissociation constant against histamine H1 receptor
ChEMBL 514 8 2 5 4.7 O=C(N[C@H](CN1CCC(OC2c3ccccc3CCc3ccccc32)CC1)C(=O)O)OCc1ccccc1 10.1021/jm058225d
156021916 178190 0 None - 1 Human 6.4 pKd = 6.4 Binding
Binding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assayBinding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assay
ChEMBL 398 1 1 4 3.9 CCOC(=O)N1CC/C(=C2/c3ccc(Cl)cc3CCc3cccnc32)C(O)C1 10.1021/acs.jmedchem.0c00483
CHEMBL4649344 178190 0 None - 1 Human 6.4 pKd = 6.4 Binding
Binding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assayBinding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assay
ChEMBL 398 1 1 4 3.9 CCOC(=O)N1CC/C(=C2/c3ccc(Cl)cc3CCc3cccnc32)C(O)C1 10.1021/acs.jmedchem.0c00483
168269233 189915 0 None - 1 Human 7.4 pKd = 7.4 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1205 30 7 11 5.8 Cc1cc(C)n2c1C=C1C=CC(/C=C/c3ccc(OCC(=O)NCCCC[C@H](NC(=O)CCNC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc4ccccc4)NC(=O)CCN4CCC(Oc5ccccc5Cc5ccccc5)CC4)C(N)=O)cc3)=[N+]1[B-]2(F)F 10.1021/acs.jmedchem.2c00125
CHEMBL5169872 189915 0 None - 1 Human 7.4 pKd = 7.4 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1205 30 7 11 5.8 Cc1cc(C)n2c1C=C1C=CC(/C=C/c3ccc(OCC(=O)NCCCC[C@H](NC(=O)CCNC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc4ccccc4)NC(=O)CCN4CCC(Oc5ccccc5Cc5ccccc5)CC4)C(N)=O)cc3)=[N+]1[B-]2(F)F 10.1021/acs.jmedchem.2c00125
168269233 189915 0 None - 1 Human 7.4 pKd = 7.4 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1205 30 7 11 5.8 Cc1cc(C)n2c1C=C1C=CC(/C=C/c3ccc(OCC(=O)NCCCC[C@H](NC(=O)CCNC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc4ccccc4)NC(=O)CCN4CCC(Oc5ccccc5Cc5ccccc5)CC4)C(N)=O)cc3)=[N+]1[B-]2(F)F 10.1021/acs.jmedchem.2c00125
CHEMBL5169872 189915 0 None - 1 Human 7.4 pKd = 7.4 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1205 30 7 11 5.8 Cc1cc(C)n2c1C=C1C=CC(/C=C/c3ccc(OCC(=O)NCCCC[C@H](NC(=O)CCNC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc4ccccc4)NC(=O)CCN4CCC(Oc5ccccc5Cc5ccccc5)CC4)C(N)=O)cc3)=[N+]1[B-]2(F)F 10.1021/acs.jmedchem.2c00125
156016191 177700 2 None - 1 Human 6.3 pKd = 6.3 Binding
Binding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assayBinding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assay
ChEMBL 380 1 0 3 5.0 CCOC(=O)N1C=C/C(=C2/c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/acs.jmedchem.0c00483
CHEMBL4642056 177700 2 None - 1 Human 6.3 pKd = 6.3 Binding
Binding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assayBinding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assay
ChEMBL 380 1 0 3 5.0 CCOC(=O)N1C=C/C(=C2/c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/acs.jmedchem.0c00483
156019460 177943 0 None - 1 Human 6.3 pKd = 6.3 Binding
Binding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assayBinding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assay
ChEMBL 398 1 1 4 4.4 CCOC(=O)N1CCC(=C2c3ccc(Cl)cc3CC(O)c3cccnc32)CC1 10.1021/acs.jmedchem.0c00483
CHEMBL4645629 177943 0 None - 1 Human 6.3 pKd = 6.3 Binding
Binding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assayBinding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assay
ChEMBL 398 1 1 4 4.4 CCOC(=O)N1CCC(=C2c3ccc(Cl)cc3CC(O)c3cccnc32)CC1 10.1021/acs.jmedchem.0c00483
10936212 11211 1 None -74 3 Guinea pig 5.3 pKd = 5.3 Binding
Potency at histamine H1 receptor subtype, was tested on guinea pig right ileumPotency at histamine H1 receptor subtype, was tested on guinea pig right ileum
ChEMBL 323 6 0 3 4.5 CC(=O)c1ccc(OCc2ccc(CN3CCCCC3)cc2)cc1 10.1021/jm021084k
CHEMBL1178750 11211 1 None -74 3 Guinea pig 5.3 pKd = 5.3 Binding
Potency at histamine H1 receptor subtype, was tested on guinea pig right ileumPotency at histamine H1 receptor subtype, was tested on guinea pig right ileum
ChEMBL 323 6 0 3 4.5 CC(=O)c1ccc(OCc2ccc(CN3CCCCC3)cc2)cc1 10.1021/jm021084k
CHEMBL39603 11211 1 None -74 3 Guinea pig 5.3 pKd = 5.3 Binding
Potency at histamine H1 receptor subtype, was tested on guinea pig right ileumPotency at histamine H1 receptor subtype, was tested on guinea pig right ileum
ChEMBL 323 6 0 3 4.5 CC(=O)c1ccc(OCc2ccc(CN3CCCCC3)cc2)cc1 10.1021/jm021084k
14637770 178097 25 None - 1 Human 7.3 pKd = 7.3 Binding
Binding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assayBinding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assay
ChEMBL 326 0 2 3 3.5 OC1Cc2cccnc2C(=C2CCNCC2)c2ccc(Cl)cc21 10.1021/acs.jmedchem.0c00483
CHEMBL4647890 178097 25 None - 1 Human 7.3 pKd = 7.3 Binding
Binding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assayBinding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assay
ChEMBL 326 0 2 3 3.5 OC1Cc2cccnc2C(=C2CCNCC2)c2ccc(Cl)cc21 10.1021/acs.jmedchem.0c00483
168272779 190564 0 None - 1 Human 8.3 pKd = 8.3 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1191 27 6 14 6.2 C[C@H](NC(=O)CCN(C)CC/C=C1\c2ccccc2COc2ccccc21)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)NCCC(=O)N[C@@H](CCCn1cc(COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)nn1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5180096 190564 0 None - 1 Human 8.3 pKd = 8.3 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1191 27 6 14 6.2 C[C@H](NC(=O)CCN(C)CC/C=C1\c2ccccc2COc2ccccc21)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)NCCC(=O)N[C@@H](CCCn1cc(COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)nn1)C(N)=O 10.1021/acs.jmedchem.2c00125
168283831 190930 0 None - 1 Human 8.3 pKd = 8.3 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1256 32 9 14 3.9 C[C@H](NC(=O)[C@@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5185508 190930 0 None - 1 Human 8.3 pKd = 8.3 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1256 32 9 14 3.9 C[C@H](NC(=O)[C@@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
168289844 191333 0 None - 1 Human 8.3 pKd = 8.3 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1284 34 9 14 4.6 CC[C@H](C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5191552 191333 0 None - 1 Human 8.3 pKd = 8.3 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1284 34 9 14 4.6 CC[C@H](C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
168286984 191392 0 None - 1 Human 8.3 pKd = 8.3 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1254 32 8 13 5.2 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5192474 191392 0 None - 1 Human 8.3 pKd = 8.3 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1254 32 8 13 5.2 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
168283831 190930 0 None - 1 Human 8.3 pKd = 8.3 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1256 32 9 14 3.9 C[C@H](NC(=O)[C@@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5185508 190930 0 None - 1 Human 8.3 pKd = 8.3 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1256 32 9 14 3.9 C[C@H](NC(=O)[C@@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
168272779 190564 0 None - 1 Human 8.3 pKd = 8.3 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1191 27 6 14 6.2 C[C@H](NC(=O)CCN(C)CC/C=C1\c2ccccc2COc2ccccc21)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)NCCC(=O)N[C@@H](CCCn1cc(COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)nn1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5180096 190564 0 None - 1 Human 8.3 pKd = 8.3 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1191 27 6 14 6.2 C[C@H](NC(=O)CCN(C)CC/C=C1\c2ccccc2COc2ccccc21)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)NCCC(=O)N[C@@H](CCCn1cc(COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)nn1)C(N)=O 10.1021/acs.jmedchem.2c00125
168289771 191813 0 None - 1 Human 8.2 pKd = 8.2 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1284 34 9 14 4.6 CC(C)C[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5198492 191813 0 None - 1 Human 8.2 pKd = 8.2 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1284 34 9 14 4.6 CC(C)C[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
168297510 192479 0 None - 1 Human 8.2 pKd = 8.2 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1305 32 9 14 6.0 C[C@H](NC(=O)[C@@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)[C@@H](C)O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5208869 192479 0 None - 1 Human 8.2 pKd = 8.2 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1305 32 9 14 6.0 C[C@H](NC(=O)[C@@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)[C@@H](C)O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
44461723 205955 0 None 398 2 Guinea pig 8.2 pKd = 8.2 Binding
dissociation constant was determined against H1 receptor of guinea pig lung membranes using radioligand binding assays.dissociation constant was determined against H1 receptor of guinea pig lung membranes using radioligand binding assays.
ChEMBL 519 8 0 8 7.0 O=c1cc(C2N=NN=N2)oc2cc(OCCCN3CCC(=C(c4ccccc4)c4ccccc4)CC3)ccc12 10.1021/jm00013a023
CHEMBL84407 205955 0 None 398 2 Guinea pig 8.2 pKd = 8.2 Binding
dissociation constant was determined against H1 receptor of guinea pig lung membranes using radioligand binding assays.dissociation constant was determined against H1 receptor of guinea pig lung membranes using radioligand binding assays.
ChEMBL 519 8 0 8 7.0 O=c1cc(C2N=NN=N2)oc2cc(OCCCN3CCC(=C(c4ccccc4)c4ccccc4)CC3)ccc12 10.1021/jm00013a023
10435880 205360 0 None 707 2 Guinea pig 8.2 pKd = 8.2 Binding
Dissociation constant was determined against H1 receptor of guinea pig lung membranes using radioligand binding assays.Dissociation constant was determined against H1 receptor of guinea pig lung membranes using radioligand binding assays.
ChEMBL 495 8 1 5 5.9 O=C(O)c1cc(=O)c2cc(OCCCN3CCC(=C(c4ccccc4)c4ccccc4)CC3)ccc2o1 10.1021/jm00013a023
CHEMBL79732 205360 0 None 707 2 Guinea pig 8.2 pKd = 8.2 Binding
Dissociation constant was determined against H1 receptor of guinea pig lung membranes using radioligand binding assays.Dissociation constant was determined against H1 receptor of guinea pig lung membranes using radioligand binding assays.
ChEMBL 495 8 1 5 5.9 O=C(O)c1cc(=O)c2cc(OCCCN3CCC(=C(c4ccccc4)c4ccccc4)CC3)ccc2o1 10.1021/jm00013a023
10067161 44119 1 None -30199 3 Guinea pig 5.3 pKd = 5.3 Binding
Activity at Histamine H1 receptor using functional H1 receptor assay on guinea pig ileumActivity at Histamine H1 receptor using functional H1 receptor assay on guinea pig ileum
ChEMBL 361 7 1 4 5.2 c1ccc2c(Nc3ccc(OCCCN4CCCCC4)cc3)ccnc2c1 10.1021/jm0110845
CHEMBL15153 44119 1 None -30199 3 Guinea pig 5.3 pKd = 5.3 Binding
Activity at Histamine H1 receptor using functional H1 receptor assay on guinea pig ileumActivity at Histamine H1 receptor using functional H1 receptor assay on guinea pig ileum
ChEMBL 361 7 1 4 5.2 c1ccc2c(Nc3ccc(OCCCN4CCCCC4)cc3)ccnc2c1 10.1021/jm0110845
11107010 18965 2 None -1000 3 Guinea pig 4.3 pKd = 4.3 Binding
Receptor profile was evaluated at Histamine H1 receptor of guinea pig ileumReceptor profile was evaluated at Histamine H1 receptor of guinea pig ileum
ChEMBL 224 6 1 2 3.2 CC(CC(C)(C)C)OCCCc1c[nH]cn1 10.1021/jm020910m
CHEMBL128714 18965 2 None -1000 3 Guinea pig 4.3 pKd = 4.3 Binding
Receptor profile was evaluated at Histamine H1 receptor of guinea pig ileumReceptor profile was evaluated at Histamine H1 receptor of guinea pig ileum
ChEMBL 224 6 1 2 3.2 CC(CC(C)(C)C)OCCCc1c[nH]cn1 10.1021/jm020910m
10956869 63052 0 None -5128 3 Guinea pig 4.3 pKd = 4.3 Binding
Receptor profile was evaluated at Histamine H1 receptor of guinea pig ileumReceptor profile was evaluated at Histamine H1 receptor of guinea pig ileum
ChEMBL 279 6 2 3 3.0 C[C@@H](NC(=O)OCCCc1c[nH]cn1)C1CCCCC1 10.1021/jm020910m
CHEMBL1788247 63052 0 None -5128 3 Guinea pig 4.3 pKd = 4.3 Binding
Receptor profile was evaluated at Histamine H1 receptor of guinea pig ileumReceptor profile was evaluated at Histamine H1 receptor of guinea pig ileum
ChEMBL 279 6 2 3 3.0 C[C@@H](NC(=O)OCCCc1c[nH]cn1)C1CCCCC1 10.1021/jm020910m
156012578 177359 0 None - 1 Human 7.3 pKd = 7.3 Binding
Binding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assayBinding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assay
ChEMBL 414 1 2 5 3.5 CCOC(=O)N1C(O)CC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1O 10.1021/acs.jmedchem.0c00483
CHEMBL4637657 177359 0 None - 1 Human 7.3 pKd = 7.3 Binding
Binding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assayBinding affinity to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assay
ChEMBL 414 1 2 5 3.5 CCOC(=O)N1C(O)CC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1O 10.1021/acs.jmedchem.0c00483
168297282 192477 0 None - 1 Human 5.3 pKd = 5.3 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1225 36 10 13 2.4 Cc1cc(C)n2c1C=C1C=CC(CCC(=O)NCCCCCC(=O)NCCCC[C@H](NC(=O)CCNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)CCN3CCC(Oc4ccccc4Cc4ccccc4)CC3)C(C)C)C(N)=O)=[N+]1[B-]2(F)F 10.1021/acs.jmedchem.2c00125
CHEMBL5208850 192477 0 None - 1 Human 5.3 pKd = 5.3 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1225 36 10 13 2.4 Cc1cc(C)n2c1C=C1C=CC(CCC(=O)NCCCCCC(=O)NCCCC[C@H](NC(=O)CCNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)CCN3CCC(Oc4ccccc4Cc4ccccc4)CC3)C(C)C)C(N)=O)=[N+]1[B-]2(F)F 10.1021/acs.jmedchem.2c00125
168297282 192477 0 None - 1 Human 5.3 pKd = 5.3 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1225 36 10 13 2.4 Cc1cc(C)n2c1C=C1C=CC(CCC(=O)NCCCCCC(=O)NCCCC[C@H](NC(=O)CCNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)CCN3CCC(Oc4ccccc4Cc4ccccc4)CC3)C(C)C)C(N)=O)=[N+]1[B-]2(F)F 10.1021/acs.jmedchem.2c00125
CHEMBL5208850 192477 0 None - 1 Human 5.3 pKd = 5.3 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1225 36 10 13 2.4 Cc1cc(C)n2c1C=C1C=CC(CCC(=O)NCCCCCC(=O)NCCCC[C@H](NC(=O)CCNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)CCN3CCC(Oc4ccccc4Cc4ccccc4)CC3)C(C)C)C(N)=O)=[N+]1[B-]2(F)F 10.1021/acs.jmedchem.2c00125
277 1301 62 None -2 50 Human 5.3 pKd = 5.3 Binding
Dissociation constant against histamine H1 receptorDissociation constant against histamine H1 receptor
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 10.1021/jm058225d
2913 1301 62 None -2 50 Human 5.3 pKd = 5.3 Binding
Dissociation constant against histamine H1 receptorDissociation constant against histamine H1 receptor
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 10.1021/jm058225d
765 1301 62 None -2 50 Human 5.3 pKd = 5.3 Binding
Dissociation constant against histamine H1 receptorDissociation constant against histamine H1 receptor
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 10.1021/jm058225d
CHEMBL516 1301 62 None -2 50 Human 5.3 pKd = 5.3 Binding
Dissociation constant against histamine H1 receptorDissociation constant against histamine H1 receptor
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 10.1021/jm058225d
DB00434 1301 62 None -2 50 Human 5.3 pKd = 5.3 Binding
Dissociation constant against histamine H1 receptorDissociation constant against histamine H1 receptor
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 10.1021/jm058225d
168289021 191777 0 None - 1 Human 8.2 pKd = 8.2 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1272 33 10 15 2.9 C[C@@H](O)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5197990 191777 0 None - 1 Human 8.2 pKd = 8.2 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1272 33 10 15 2.9 C[C@@H](O)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
168289771 191813 0 None - 1 Human 8.2 pKd = 8.2 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1284 34 9 14 4.6 CC(C)C[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5198492 191813 0 None - 1 Human 8.2 pKd = 8.2 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1284 34 9 14 4.6 CC(C)C[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
168297510 192479 0 None - 1 Human 8.2 pKd = 8.2 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1305 32 9 14 6.0 C[C@H](NC(=O)[C@@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)[C@@H](C)O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5208869 192479 0 None - 1 Human 8.2 pKd = 8.2 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1305 32 9 14 6.0 C[C@H](NC(=O)[C@@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)[C@@H](C)O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
24824726 161109 1 None 2 6 Human 8.2 pKd = 8.2 Binding
Antagonist activity at histamine H1 receptor in human isolated trachea assessed as change in histamine-induced contractionAntagonist activity at histamine H1 receptor in human isolated trachea assessed as change in histamine-induced contraction
ChEMBL 496 11 1 6 3.6 COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL4060529 161109 1 None 2 6 Human 8.2 pKd = 8.2 Binding
Antagonist activity at histamine H1 receptor in human isolated trachea assessed as change in histamine-induced contractionAntagonist activity at histamine H1 receptor in human isolated trachea assessed as change in histamine-induced contraction
ChEMBL 496 11 1 6 3.6 COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL4117079 161109 1 None 2 6 Human 8.2 pKd = 8.2 Binding
Antagonist activity at histamine H1 receptor in human isolated trachea assessed as change in histamine-induced contractionAntagonist activity at histamine H1 receptor in human isolated trachea assessed as change in histamine-induced contraction
ChEMBL 496 11 1 6 3.6 COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL5282336 161109 1 None 2 6 Human 8.2 pKd = 8.2 Binding
Antagonist activity at histamine H1 receptor in human isolated trachea assessed as change in histamine-induced contractionAntagonist activity at histamine H1 receptor in human isolated trachea assessed as change in histamine-induced contraction
ChEMBL 496 11 1 6 3.6 COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL5286389 161109 1 None 2 6 Human 8.2 pKd = 8.2 Binding
Antagonist activity at histamine H1 receptor in human isolated trachea assessed as change in histamine-induced contractionAntagonist activity at histamine H1 receptor in human isolated trachea assessed as change in histamine-induced contraction
ChEMBL 496 11 1 6 3.6 COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
168289021 191777 0 None - 1 Human 8.2 pKd = 8.2 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1272 33 10 15 2.9 C[C@@H](O)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5197990 191777 0 None - 1 Human 8.2 pKd = 8.2 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1272 33 10 15 2.9 C[C@@H](O)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
168295200 192389 0 None - 1 Human 8.2 pKd = 8.2 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1321 33 10 15 5.0 C[C@@H](O)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5207609 192389 0 None - 1 Human 8.2 pKd = 8.2 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1321 33 10 15 5.0 C[C@@H](O)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
155539314 176380 0 None -5 2 Guinea pig 7.2 pKd = 7.2 Binding
Antagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 minsAntagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 mins
ChEMBL 628 14 4 4 5.0 N=C(N)N(CCCCN1CCN(CCCCN(Cc2ccc(C(F)(F)F)cc2)C(=N)N)CC1)Cc1ccc(C(F)(F)F)cc1 10.1039/C8MD00527C
CHEMBL4514561 176380 0 None -5 2 Guinea pig 7.2 pKd = 7.2 Binding
Antagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 minsAntagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 mins
ChEMBL 628 14 4 4 5.0 N=C(N)N(CCCCN1CCN(CCCCN(Cc2ccc(C(F)(F)F)cc2)C(=N)N)CC1)Cc1ccc(C(F)(F)F)cc1 10.1039/C8MD00527C
CHEMBL4595855 176380 0 None -5 2 Guinea pig 7.2 pKd = 7.2 Binding
Antagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 minsAntagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 mins
ChEMBL 628 14 4 4 5.0 N=C(N)N(CCCCN1CCN(CCCCN(Cc2ccc(C(F)(F)F)cc2)C(=N)N)CC1)Cc1ccc(C(F)(F)F)cc1 10.1039/C8MD00527C
155553524 176519 0 None -5 2 Guinea pig 7.2 pKd = 7.2 Binding
Antagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 minsAntagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 mins
ChEMBL 546 16 2 3 7.3 N=C(N)N(CCCCN1CCC(CCCCCCCOc2ccccc2)CC1)Cc1ccc(C(F)(F)F)cc1 10.1039/C8MD00527C
CHEMBL4546027 176519 0 None -5 2 Guinea pig 7.2 pKd = 7.2 Binding
Antagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 minsAntagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 mins
ChEMBL 546 16 2 3 7.3 N=C(N)N(CCCCN1CCC(CCCCCCCOc2ccccc2)CC1)Cc1ccc(C(F)(F)F)cc1 10.1039/C8MD00527C
CHEMBL4596938 176519 0 None -5 2 Guinea pig 7.2 pKd = 7.2 Binding
Antagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 minsAntagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 mins
ChEMBL 546 16 2 3 7.3 N=C(N)N(CCCCN1CCC(CCCCCCCOc2ccccc2)CC1)Cc1ccc(C(F)(F)F)cc1 10.1039/C8MD00527C
168283519 191064 0 None - 1 Human 7.2 pKd = 7.2 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1216 32 9 13 3.1 Cc1cc(C)n2c1C=C1C=CC(/C=C/c3ccc(OCC(=O)NCCCC[C@H](NC(=O)CCNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)CCN4CCC(Oc5ccccc5Cc5ccccc5)CC4)C(C)C)C(N)=O)cc3)=[N+]1[B-]2(F)F 10.1021/acs.jmedchem.2c00125
CHEMBL5187345 191064 0 None - 1 Human 7.2 pKd = 7.2 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1216 32 9 13 3.1 Cc1cc(C)n2c1C=C1C=CC(/C=C/c3ccc(OCC(=O)NCCCC[C@H](NC(=O)CCNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)CCN4CCC(Oc5ccccc5Cc5ccccc5)CC4)C(C)C)C(N)=O)cc3)=[N+]1[B-]2(F)F 10.1021/acs.jmedchem.2c00125
155565680 176245 0 None -6 2 Guinea pig 7.2 pKd = 7.2 Binding
Antagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 minsAntagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 mins
ChEMBL 547 16 3 4 5.7 N=C(NCCCCN1CCN(CCCCCCCOc2ccccc2)CC1)NCc1ccc(C(F)(F)F)cc1 10.1039/C8MD00527C
CHEMBL4579190 176245 0 None -6 2 Guinea pig 7.2 pKd = 7.2 Binding
Antagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 minsAntagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 mins
ChEMBL 547 16 3 4 5.7 N=C(NCCCCN1CCN(CCCCCCCOc2ccccc2)CC1)NCc1ccc(C(F)(F)F)cc1 10.1039/C8MD00527C
CHEMBL4594800 176245 0 None -6 2 Guinea pig 7.2 pKd = 7.2 Binding
Antagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 minsAntagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 mins
ChEMBL 547 16 3 4 5.7 N=C(NCCCCN1CCN(CCCCCCCOc2ccccc2)CC1)NCc1ccc(C(F)(F)F)cc1 10.1039/C8MD00527C
168283519 191064 0 None - 1 Human 7.2 pKd = 7.2 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1216 32 9 13 3.1 Cc1cc(C)n2c1C=C1C=CC(/C=C/c3ccc(OCC(=O)NCCCC[C@H](NC(=O)CCNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)CCN4CCC(Oc5ccccc5Cc5ccccc5)CC4)C(C)C)C(N)=O)cc3)=[N+]1[B-]2(F)F 10.1021/acs.jmedchem.2c00125
CHEMBL5187345 191064 0 None - 1 Human 7.2 pKd = 7.2 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1216 32 9 13 3.1 Cc1cc(C)n2c1C=C1C=CC(/C=C/c3ccc(OCC(=O)NCCCC[C@H](NC(=O)CCNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)CCN4CCC(Oc5ccccc5Cc5ccccc5)CC4)C(C)C)C(N)=O)cc3)=[N+]1[B-]2(F)F 10.1021/acs.jmedchem.2c00125
168295200 192389 0 None - 1 Human 8.2 pKd = 8.2 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1321 33 10 15 5.0 C[C@@H](O)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5207609 192389 0 None - 1 Human 8.2 pKd = 8.2 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1321 33 10 15 5.0 C[C@@H](O)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)C(N)=O 10.1021/acs.jmedchem.2c00125
168276508 190266 0 None - 1 Human 8.1 pKd = 8.1 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells incubated for 1 hr using furimazine as substrate measured after 5 mins by NanoBRET binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells incubated for 1 hr using furimazine as substrate measured after 5 mins by NanoBRET binding assay
ChEMBL 1140 28 6 11 6.9 C[C@@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@H](C)C(=O)N[C@H](C)C(=O)NCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1 10.1021/acs.jmedchem.2c00125
CHEMBL5175488 190266 0 None - 1 Human 8.1 pKd = 8.1 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells incubated for 1 hr using furimazine as substrate measured after 5 mins by NanoBRET binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells incubated for 1 hr using furimazine as substrate measured after 5 mins by NanoBRET binding assay
ChEMBL 1140 28 6 11 6.9 C[C@@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@H](C)C(=O)N[C@H](C)C(=O)NCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1 10.1021/acs.jmedchem.2c00125
2200 20203 61 None 26 2 Guinea pig 7.1 pKd = 7.1 Binding
Antagonist activity at H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced ileum contraction measured after 15 minsAntagonist activity at H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced ileum contraction measured after 15 mins
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1016/j.ejmech.2018.04.043
CHEMBL1256819 20203 61 None 26 2 Guinea pig 7.1 pKd = 7.1 Binding
Antagonist activity at H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced ileum contraction measured after 15 minsAntagonist activity at H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced ileum contraction measured after 15 mins
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1016/j.ejmech.2018.04.043
CHEMBL1305 20203 61 None 26 2 Guinea pig 7.1 pKd = 7.1 Binding
Antagonist activity at H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced ileum contraction measured after 15 minsAntagonist activity at H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced ileum contraction measured after 15 mins
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1016/j.ejmech.2018.04.043
1605 2342 117 None 1 4 Guinea pig 7.1 pKd = 7.1 Binding
Antagonist activity at histamine H1 receptor in guinea pig jejunum assessed as reduction in histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig jejunum assessed as reduction in histamine-induced contractions
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1016/j.bmcl.2015.02.037
3957 2342 117 None 1 4 Guinea pig 7.1 pKd = 7.1 Binding
Antagonist activity at histamine H1 receptor in guinea pig jejunum assessed as reduction in histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig jejunum assessed as reduction in histamine-induced contractions
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1016/j.bmcl.2015.02.037
7216 2342 117 None 1 4 Guinea pig 7.1 pKd = 7.1 Binding
Antagonist activity at histamine H1 receptor in guinea pig jejunum assessed as reduction in histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig jejunum assessed as reduction in histamine-induced contractions
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1016/j.bmcl.2015.02.037
CHEMBL998 2342 117 None 1 4 Guinea pig 7.1 pKd = 7.1 Binding
Antagonist activity at histamine H1 receptor in guinea pig jejunum assessed as reduction in histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig jejunum assessed as reduction in histamine-induced contractions
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1016/j.bmcl.2015.02.037
DB00455 2342 117 None 1 4 Guinea pig 7.1 pKd = 7.1 Binding
Antagonist activity at histamine H1 receptor in guinea pig jejunum assessed as reduction in histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig jejunum assessed as reduction in histamine-induced contractions
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1016/j.bmcl.2015.02.037
2200 20203 61 None 26 2 Guinea pig 7.1 pKd = 7.1 Binding
Antagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions after 15 minsAntagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions after 15 mins
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1016/j.bmc.2019.02.020
CHEMBL1256819 20203 61 None 26 2 Guinea pig 7.1 pKd = 7.1 Binding
Antagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions after 15 minsAntagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions after 15 mins
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1016/j.bmc.2019.02.020
CHEMBL1305 20203 61 None 26 2 Guinea pig 7.1 pKd = 7.1 Binding
Antagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions after 15 minsAntagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions after 15 mins
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1016/j.bmc.2019.02.020
2200 20203 61 None 26 2 Guinea pig 7.1 pKd = 7.1 Binding
Antagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions incubated for 15 minsAntagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions incubated for 15 mins
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1016/j.bmc.2017.07.058
CHEMBL1256819 20203 61 None 26 2 Guinea pig 7.1 pKd = 7.1 Binding
Antagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions incubated for 15 minsAntagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions incubated for 15 mins
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1016/j.bmc.2017.07.058
CHEMBL1305 20203 61 None 26 2 Guinea pig 7.1 pKd = 7.1 Binding
Antagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions incubated for 15 minsAntagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions incubated for 15 mins
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1016/j.bmc.2017.07.058
168296109 192423 0 None - 1 Human 6.1 pKd = 6.1 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1155 29 7 11 5.6 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)CCC1=[N+]2C(=Cc3ccc(-c4cccs4)n3[B-]2(F)F)C=C1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5208169 192423 0 None - 1 Human 6.1 pKd = 6.1 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1155 29 7 11 5.6 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)CCC1=[N+]2C(=Cc3ccc(-c4cccs4)n3[B-]2(F)F)C=C1)C(N)=O 10.1021/acs.jmedchem.2c00125
155567030 176417 0 None -21 4 Guinea pig 6.1 pKd = 6.1 Binding
Antagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions incubated for 15 minsAntagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions incubated for 15 mins
ChEMBL 337 8 0 2 5.8 c1ccc(-c2ccc(OCCCCCN3CCCCCC3)cc2)cc1 10.1016/j.bmc.2017.07.058
CHEMBL4586133 176417 0 None -21 4 Guinea pig 6.1 pKd = 6.1 Binding
Antagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions incubated for 15 minsAntagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions incubated for 15 mins
ChEMBL 337 8 0 2 5.8 c1ccc(-c2ccc(OCCCCCN3CCCCCC3)cc2)cc1 10.1016/j.bmc.2017.07.058
CHEMBL4596108 176417 0 None -21 4 Guinea pig 6.1 pKd = 6.1 Binding
Antagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions incubated for 15 minsAntagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions incubated for 15 mins
ChEMBL 337 8 0 2 5.8 c1ccc(-c2ccc(OCCCCCN3CCCCCC3)cc2)cc1 10.1016/j.bmc.2017.07.058
168296109 192423 0 None - 1 Human 6.1 pKd = 6.1 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1155 29 7 11 5.6 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)CCC1=[N+]2C(=Cc3ccc(-c4cccs4)n3[B-]2(F)F)C=C1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5208169 192423 0 None - 1 Human 6.1 pKd = 6.1 Binding
Binding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H1R expressed in HEK293T cells using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 1155 29 7 11 5.6 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)CCC1=[N+]2C(=Cc3ccc(-c4cccs4)n3[B-]2(F)F)C=C1)C(N)=O 10.1021/acs.jmedchem.2c00125
1278 2150 84 None -288 8 Guinea pig 6.1 pKd = 6.1 Binding
Antagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions after 15 minsAntagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions after 15 mins
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmc.2019.02.020
1279 2150 84 None -288 8 Guinea pig 6.1 pKd = 6.1 Binding
Antagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions after 15 minsAntagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions after 15 mins
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmc.2019.02.020
4908365 2150 84 None -288 8 Guinea pig 6.1 pKd = 6.1 Binding
Antagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions after 15 minsAntagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions after 15 mins
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmc.2019.02.020
CHEMBL129198 2150 84 None -288 8 Guinea pig 6.1 pKd = 6.1 Binding
Antagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions after 15 minsAntagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions after 15 mins
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmc.2019.02.020
155540474 176273 0 None -10 2 Guinea pig 7.1 pKd = 7.1 Binding
Antagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 minsAntagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 mins
ChEMBL 479 16 3 4 4.7 N=C(NCCCCN1CCN(CCCCCCCOc2ccccc2)CC1)NCc1ccccc1 10.1039/C8MD00527C
CHEMBL4482871 176273 0 None -10 2 Guinea pig 7.1 pKd = 7.1 Binding
Antagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 minsAntagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 mins
ChEMBL 479 16 3 4 4.7 N=C(NCCCCN1CCN(CCCCCCCOc2ccccc2)CC1)NCc1ccccc1 10.1039/C8MD00527C
CHEMBL4595050 176273 0 None -10 2 Guinea pig 7.1 pKd = 7.1 Binding
Antagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 minsAntagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 mins
ChEMBL 479 16 3 4 4.7 N=C(NCCCCN1CCN(CCCCCCCOc2ccccc2)CC1)NCc1ccccc1 10.1039/C8MD00527C
10873565 37836 0 None -1584 3 Guinea pig 6.1 pKd = 6.1 Binding
Activity at Histamine H1 receptor using functional H1 receptor assay on guinea pig ileumActivity at Histamine H1 receptor using functional H1 receptor assay on guinea pig ileum
ChEMBL 423 9 1 4 5.8 Clc1ccc2c(NCCc3ccc(OCCCN4CCCCC4)cc3)ccnc2c1 10.1021/jm0110845
CHEMBL14587 37836 0 None -1584 3 Guinea pig 6.1 pKd = 6.1 Binding
Activity at Histamine H1 receptor using functional H1 receptor assay on guinea pig ileumActivity at Histamine H1 receptor using functional H1 receptor assay on guinea pig ileum
ChEMBL 423 9 1 4 5.8 Clc1ccc2c(NCCc3ccc(OCCCN4CCCCC4)cc3)ccnc2c1 10.1021/jm0110845
11048988 40949 0 None -3981 3 Guinea pig 5.1 pKd = 5.1 Binding
Activity at Histamine H1 receptor using functional H1 receptor assay on guinea pig ileumActivity at Histamine H1 receptor using functional H1 receptor assay on guinea pig ileum
ChEMBL 471 11 1 4 6.8 c1ccc2c(NCCCCc3ccc(OCCCN4CCCCC4)cc3)c3c(nc2c1)CCCC3 10.1021/jm0110845
CHEMBL14868 40949 0 None -3981 3 Guinea pig 5.1 pKd = 5.1 Binding
Activity at Histamine H1 receptor using functional H1 receptor assay on guinea pig ileumActivity at Histamine H1 receptor using functional H1 receptor assay on guinea pig ileum
ChEMBL 471 11 1 4 6.8 c1ccc2c(NCCCCc3ccc(OCCCN4CCCCC4)cc3)c3c(nc2c1)CCCC3 10.1021/jm0110845
11046028 152538 0 None -144 3 Guinea pig 5.1 pKd = 5.1 Binding
Potency at histamine H1 receptor subtype, was tested on guinea pig right ileumPotency at histamine H1 receptor subtype, was tested on guinea pig right ileum
ChEMBL 338 6 1 4 4.5 C/C(=N\O)c1ccc(OCc2ccc(CN3CCCCC3)cc2)cc1 10.1021/jm021084k
CHEMBL39716 152538 0 None -144 3 Guinea pig 5.1 pKd = 5.1 Binding
Potency at histamine H1 receptor subtype, was tested on guinea pig right ileumPotency at histamine H1 receptor subtype, was tested on guinea pig right ileum
ChEMBL 338 6 1 4 4.5 C/C(=N\O)c1ccc(OCc2ccc(CN3CCCCC3)cc2)cc1 10.1021/jm021084k
11089134 21404 0 None -151 3 Guinea pig 5.1 pKd = 5.1 Binding
Receptor profile was evaluated at Histamine H1 receptor of guinea pig ileumReceptor profile was evaluated at Histamine H1 receptor of guinea pig ileum
ChEMBL 341 7 2 3 4.4 O=C(NC(c1ccccc1)C1CCCCC1)OCCCc1c[nH]cn1 10.1021/jm020910m
CHEMBL131476 21404 0 None -151 3 Guinea pig 5.1 pKd = 5.1 Binding
Receptor profile was evaluated at Histamine H1 receptor of guinea pig ileumReceptor profile was evaluated at Histamine H1 receptor of guinea pig ileum
ChEMBL 341 7 2 3 4.4 O=C(NC(c1ccccc1)C1CCCCC1)OCCCc1c[nH]cn1 10.1021/jm020910m
9866657 12018 0 None -512 3 Guinea pig 5.0 pKd = 5.0 Binding
Potency at histamine H1 receptor subtype, was tested on guinea pig right ileumPotency at histamine H1 receptor subtype, was tested on guinea pig right ileum
ChEMBL 309 6 0 3 4.1 CC(=O)c1ccc(OCc2ccc(CN3CCCC3)cc2)cc1 10.1021/jm021084k
CHEMBL1183328 12018 0 None -512 3 Guinea pig 5.0 pKd = 5.0 Binding
Potency at histamine H1 receptor subtype, was tested on guinea pig right ileumPotency at histamine H1 receptor subtype, was tested on guinea pig right ileum
ChEMBL 309 6 0 3 4.1 CC(=O)c1ccc(OCc2ccc(CN3CCCC3)cc2)cc1 10.1021/jm021084k
CHEMBL290613 12018 0 None -512 3 Guinea pig 5.0 pKd = 5.0 Binding
Potency at histamine H1 receptor subtype, was tested on guinea pig right ileumPotency at histamine H1 receptor subtype, was tested on guinea pig right ileum
ChEMBL 309 6 0 3 4.1 CC(=O)c1ccc(OCc2ccc(CN3CCCC3)cc2)cc1 10.1021/jm021084k
26987 949 33 None 16 21 Human 10.3 pKi = 10.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
6063 949 33 None 16 21 Human 10.3 pKi = 10.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
671 949 33 None 16 21 Human 10.3 pKi = 10.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
CHEMBL1626 949 33 None 16 21 Human 10.3 pKi = 10.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
DB00283 949 33 None 16 21 Human 10.3 pKi = 10.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
3158 56267 27 None 40 20 Human 10.2 pKi = 10.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
CHEMBL1628227 56267 27 None 40 20 Human 10.2 pKi = 10.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
15749406 12274 0 None - 1 Guinea pig 9.9 pKi = 9.9 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 293 3 0 2 4.3 Cc1ccc2c(c1)/C(=C/CCN(C)C)c1ccccc1CO2 10.1021/jm00089a020
CHEMBL1184758 12274 0 None - 1 Guinea pig 9.9 pKi = 9.9 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 293 3 0 2 4.3 Cc1ccc2c(c1)/C(=C/CCN(C)C)c1ccccc1CO2 10.1021/jm00089a020
CHEMBL366965 12274 0 None - 1 Guinea pig 9.9 pKi = 9.9 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 293 3 0 2 4.3 Cc1ccc2c(c1)/C(=C/CCN(C)C)c1ccccc1CO2 10.1021/jm00089a020
1530 2182 50 None -5 21 Human 9.9 pKi = 9.9 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
3827 2182 50 None -5 21 Human 9.9 pKi = 9.9 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
7206 2182 50 None -5 21 Human 9.9 pKi = 9.9 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
CHEMBL534 2182 50 None -5 21 Human 9.9 pKi = 9.9 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
DB00920 2182 50 None -5 21 Human 9.9 pKi = 9.9 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
135 2532 43 None -1 58 Human 9.8 pKi = 9.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
1796 2532 43 None -1 58 Human 9.8 pKi = 9.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
4184 2532 43 None -1 58 Human 9.8 pKi = 9.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
CHEMBL6437 2532 43 None -1 58 Human 9.8 pKi = 9.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
DB06148 2532 43 None -1 58 Human 9.8 pKi = 9.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
1225 1471 26 None -1 22 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]mepyramine from human H1R expressed in HEK293T cell homogenates incubated for 1 hr by radioligand binding assay based liquid scintillation counterDisplacement of [3H]mepyramine from human H1R expressed in HEK293T cell homogenates incubated for 1 hr by radioligand binding assay based liquid scintillation counter
ChEMBL 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C 10.1021/acs.jmedchem.2c00125
3958 1471 26 None -1 22 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]mepyramine from human H1R expressed in HEK293T cell homogenates incubated for 1 hr by radioligand binding assay based liquid scintillation counterDisplacement of [3H]mepyramine from human H1R expressed in HEK293T cell homogenates incubated for 1 hr by radioligand binding assay based liquid scintillation counter
ChEMBL 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C 10.1021/acs.jmedchem.2c00125
667477 1471 26 None -1 22 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]mepyramine from human H1R expressed in HEK293T cell homogenates incubated for 1 hr by radioligand binding assay based liquid scintillation counterDisplacement of [3H]mepyramine from human H1R expressed in HEK293T cell homogenates incubated for 1 hr by radioligand binding assay based liquid scintillation counter
ChEMBL 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C 10.1021/acs.jmedchem.2c00125
CHEMBL860 1471 26 None -1 22 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]mepyramine from human H1R expressed in HEK293T cell homogenates incubated for 1 hr by radioligand binding assay based liquid scintillation counterDisplacement of [3H]mepyramine from human H1R expressed in HEK293T cell homogenates incubated for 1 hr by radioligand binding assay based liquid scintillation counter
ChEMBL 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C 10.1021/acs.jmedchem.2c00125
DB01142 1471 26 None -1 22 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]mepyramine from human H1R expressed in HEK293T cell homogenates incubated for 1 hr by radioligand binding assay based liquid scintillation counterDisplacement of [3H]mepyramine from human H1R expressed in HEK293T cell homogenates incubated for 1 hr by radioligand binding assay based liquid scintillation counter
ChEMBL 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C 10.1021/acs.jmedchem.2c00125
3158 56267 27 None 40 20 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1021/jm2011589
CHEMBL1628227 56267 27 None 40 20 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1021/jm2011589
1238 203174 24 None -38 16 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cellsDisplacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm100652h
CHEMBL64249 203174 24 None -38 16 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cellsDisplacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm100652h
3158 56267 27 None 40 20 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1021/acs.jmedchem.6b00981
CHEMBL1628227 56267 27 None 40 20 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1021/acs.jmedchem.6b00981
46884735 7973 0 None 11481 2 Human 9.5 pKi = 9.5 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 316 5 0 3 4.3 C[C@H](C1=C(CCN(C)C)Cc2cc(F)ccc21)c1nccs1 10.1016/j.bmcl.2010.02.055
CHEMBL1090527 7973 0 None 11481 2 Human 9.5 pKi = 9.5 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 316 5 0 3 4.3 C[C@H](C1=C(CCN(C)C)Cc2cc(F)ccc21)c1nccs1 10.1016/j.bmcl.2010.02.055
135398745 2914 112 None -1 65 Rat 9.5 pKi = 9.5 Binding
Half-maximal inhibition of [3H]7-OH-DPAT binding to Histamine H1 receptor in rat tissue homogenateHalf-maximal inhibition of [3H]7-OH-DPAT binding to Histamine H1 receptor in rat tissue homogenate
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm010982y
47 2914 112 None -1 65 Rat 9.5 pKi = 9.5 Binding
Half-maximal inhibition of [3H]7-OH-DPAT binding to Histamine H1 receptor in rat tissue homogenateHalf-maximal inhibition of [3H]7-OH-DPAT binding to Histamine H1 receptor in rat tissue homogenate
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm010982y
CHEMBL715 2914 112 None -1 65 Rat 9.5 pKi = 9.5 Binding
Half-maximal inhibition of [3H]7-OH-DPAT binding to Histamine H1 receptor in rat tissue homogenateHalf-maximal inhibition of [3H]7-OH-DPAT binding to Histamine H1 receptor in rat tissue homogenate
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm010982y
DB00334 2914 112 None -1 65 Rat 9.5 pKi = 9.5 Binding
Half-maximal inhibition of [3H]7-OH-DPAT binding to Histamine H1 receptor in rat tissue homogenateHalf-maximal inhibition of [3H]7-OH-DPAT binding to Histamine H1 receptor in rat tissue homogenate
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm010982y
1530 2182 50 None 5 21 Guinea pig 9.5 pKi = 9.5 Binding
The compound was tested in vitro for binding affinity against histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMThe compound was tested in vitro for binding affinity against histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1021/jm00089a020
3827 2182 50 None 5 21 Guinea pig 9.5 pKi = 9.5 Binding
The compound was tested in vitro for binding affinity against histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMThe compound was tested in vitro for binding affinity against histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1021/jm00089a020
7206 2182 50 None 5 21 Guinea pig 9.5 pKi = 9.5 Binding
The compound was tested in vitro for binding affinity against histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMThe compound was tested in vitro for binding affinity against histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1021/jm00089a020
CHEMBL534 2182 50 None 5 21 Guinea pig 9.5 pKi = 9.5 Binding
The compound was tested in vitro for binding affinity against histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMThe compound was tested in vitro for binding affinity against histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1021/jm00089a020
DB00920 2182 50 None 5 21 Guinea pig 9.5 pKi = 9.5 Binding
The compound was tested in vitro for binding affinity against histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMThe compound was tested in vitro for binding affinity against histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1021/jm00089a020
71452601 84207 0 None 100 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 434 8 1 5 4.5 N#Cc1cccc(OC[C@@H](O)CCN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)c1 10.1016/j.bmcl.2012.09.113
CHEMBL2208424 84207 0 None 100 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 434 8 1 5 4.5 N#Cc1cccc(OC[C@@H](O)CCN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)c1 10.1016/j.bmcl.2012.09.113
2286 3183 51 None -2 30 Human 9.5 pKi = 9.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
4927 3183 51 None -2 30 Human 9.5 pKi = 9.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
7282 3183 51 None -2 30 Human 9.5 pKi = 9.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
CHEMBL643 3183 51 None -2 30 Human 9.5 pKi = 9.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
DB01069 3183 51 None -2 30 Human 9.5 pKi = 9.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
1201549 597 24 None -1 20 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
333 597 24 None -1 20 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
7601 597 24 None -1 20 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL1201203 597 24 None -1 20 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL438151 597 24 None -1 20 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
DB00245 597 24 None -1 20 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
31843 163565 83 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 324 0 0 2 4.4 CN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/acs.jmedchem.9b00447
CHEMBL420316 163565 83 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 324 0 0 2 4.4 CN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/acs.jmedchem.9b00447
CHEMBL4551989 163565 83 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 324 0 0 2 4.4 CN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/acs.jmedchem.9b00447
2284 3182 33 None 1 29 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
4926 3182 33 None 1 29 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
7281 3182 33 None 1 29 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
CHEMBL564 3182 33 None 1 29 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
DB00420 3182 33 None 1 29 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
12963076 196625 4 None 162 7 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation counting
ChEMBL 292 5 0 2 4.1 C[C@H](C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm900933k
CHEMBL564226 196625 4 None 162 7 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation counting
ChEMBL 292 5 0 2 4.1 C[C@H](C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm900933k
10315110 171857 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 338 1 0 2 4.8 CCN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/acs.jmedchem.9b00447
CHEMBL4469024 171857 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 338 1 0 2 4.8 CCN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/acs.jmedchem.9b00447
277 1301 62 None -2 50 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
2913 1301 62 None -2 50 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
765 1301 62 None -2 50 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
CHEMBL516 1301 62 None -2 50 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
DB00434 1301 62 None -2 50 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
9839050 112379 0 None 1 9 Human 9.4 pKi = 9.4 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 293 2 0 2 3.8 CN(C)C[C@H]1C[C@@H]2c3ccccc3Cc3ccccc3[C@H]2O1 10.1021/jm049632c
CHEMBL329566 112379 0 None 1 9 Human 9.4 pKi = 9.4 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 293 2 0 2 3.8 CN(C)C[C@H]1C[C@@H]2c3ccccc3Cc3ccccc3[C@H]2O1 10.1021/jm049632c
1227 2489 43 None -2 12 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
2331 2489 43 None -2 12 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
3957 2489 43 None -2 12 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
4992 2489 43 None -2 12 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
CHEMBL511 2489 43 None -2 12 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
DB06691 2489 43 None -2 12 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C nan
12963076 196625 4 None 162 7 Human 9.4 pKi = 9.4 Binding
Compound was evaluated for binding affinity towards cloned human histamine H1 receptors stably expressed in CHO-K1 cells using [3H]mepyramineCompound was evaluated for binding affinity towards cloned human histamine H1 receptors stably expressed in CHO-K1 cells using [3H]mepyramine
ChEMBL 292 5 0 2 4.1 C[C@H](C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL564226 196625 4 None 162 7 Human 9.4 pKi = 9.4 Binding
Compound was evaluated for binding affinity towards cloned human histamine H1 receptors stably expressed in CHO-K1 cells using [3H]mepyramineCompound was evaluated for binding affinity towards cloned human histamine H1 receptors stably expressed in CHO-K1 cells using [3H]mepyramine
ChEMBL 292 5 0 2 4.1 C[C@H](C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
15749404 203414 3 None - 1 Guinea pig 9.3 pKi = 9.3 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 323 5 1 3 3.5 CN(C)CC/C=C1\c2ccccc2COc2ccc(CCO)cc21 10.1021/jm00089a020
CHEMBL65612 203414 3 None - 1 Guinea pig 9.3 pKi = 9.3 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 323 5 1 3 3.5 CN(C)CC/C=C1\c2ccccc2COc2ccc(CCO)cc21 10.1021/jm00089a020
10333104 119589 0 None 43 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cellsDisplacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cells
ChEMBL 265 4 0 1 4.1 CN(C)CCCC1c2ccccc2Cc2ccccc21 10.1016/j.bmc.2009.08.016
CHEMBL346230 119589 0 None 43 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cellsDisplacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cells
ChEMBL 265 4 0 1 4.1 CN(C)CCCC1c2ccccc2Cc2ccccc21 10.1016/j.bmc.2009.08.016
11832931 161791 1 None - 1 Rat 9.3 pKi = 9.3 Binding
Tested for displacement of H-1 in rat brain by radioligand binding studiesTested for displacement of H-1 in rat brain by radioligand binding studies
ChEMBL 283 3 1 2 3.0 Cc1[nH]cnc1CCC(=O)N1CC(C)(C)c2ccccc21 10.1016/S0960-894X(00)80418-7
CHEMBL414174 161791 1 None - 1 Rat 9.3 pKi = 9.3 Binding
Tested for displacement of H-1 in rat brain by radioligand binding studiesTested for displacement of H-1 in rat brain by radioligand binding studies
ChEMBL 283 3 1 2 3.0 Cc1[nH]cnc1CCC(=O)N1CC(C)(C)c2ccccc21 10.1016/S0960-894X(00)80418-7
2435 3590 83 None -95 48 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cellsDisplacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm100652h
60149 3590 83 None -95 48 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cellsDisplacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm100652h
98 3590 83 None -95 48 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cellsDisplacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm100652h
CHEMBL12713 3590 83 None -95 48 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cellsDisplacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm100652h
DB06144 3590 83 None -95 48 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cellsDisplacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm100652h
44401164 69816 0 None -2 9 Human 9.3 pKi = 9.3 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 329 2 0 3 4.5 CN(C)C[C@H]1CC2c3ccccc3Sc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL193639 69816 0 None -2 9 Human 9.3 pKi = 9.3 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 329 2 0 3 4.5 CN(C)C[C@H]1CC2c3ccccc3Sc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
277 1301 62 None 2 50 Guinea pig 9.3 pKi = 9.3 Binding
Inhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 minInhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 min
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 10.1021/jm00017a019
2913 1301 62 None 2 50 Guinea pig 9.3 pKi = 9.3 Binding
Inhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 minInhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 min
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 10.1021/jm00017a019
765 1301 62 None 2 50 Guinea pig 9.3 pKi = 9.3 Binding
Inhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 minInhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 min
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 10.1021/jm00017a019
CHEMBL516 1301 62 None 2 50 Guinea pig 9.3 pKi = 9.3 Binding
Inhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 minInhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 min
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 10.1021/jm00017a019
DB00434 1301 62 None 2 50 Guinea pig 9.3 pKi = 9.3 Binding
Inhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 minInhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 min
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 10.1021/jm00017a019
9839050 112379 0 None 1 9 Human 9.3 pKi = 9.3 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 293 2 0 2 3.8 CN(C)C[C@H]1C[C@@H]2c3ccccc3Cc3ccccc3[C@H]2O1 10.1016/j.bmcl.2004.03.069
CHEMBL329566 112379 0 None 1 9 Human 9.3 pKi = 9.3 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 293 2 0 2 3.8 CN(C)C[C@H]1C[C@@H]2c3ccccc3Cc3ccccc3[C@H]2O1 10.1016/j.bmcl.2004.03.069
180 401 56 None -1 40 Human 9.3 pKi = 9.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
200 401 56 None -1 40 Human 9.3 pKi = 9.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2160 401 56 None -1 40 Human 9.3 pKi = 9.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
CHEMBL629 401 56 None -1 40 Human 9.3 pKi = 9.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
DB00321 401 56 None -1 40 Human 9.3 pKi = 9.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
135398737 958 93 None 2 89 Human 9.2 pKi = 9.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 958 93 None 2 89 Human 9.2 pKi = 9.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 958 93 None 2 89 Human 9.2 pKi = 9.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 958 93 None 2 89 Human 9.2 pKi = 9.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 958 93 None 2 89 Human 9.2 pKi = 9.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
42631003 199618 13 None -2 8 Human 9.2 pKi = 9.2 Binding
Binding affinity to histamine H1 receptor (unknown origin) assessed as inhibition constantBinding affinity to histamine H1 receptor (unknown origin) assessed as inhibition constant
ChEMBL 304 3 0 2 4.2 Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1016/j.ejmech.2022.114464
CHEMBL592752 199618 13 None -2 8 Human 9.2 pKi = 9.2 Binding
Binding affinity to histamine H1 receptor (unknown origin) assessed as inhibition constantBinding affinity to histamine H1 receptor (unknown origin) assessed as inhibition constant
ChEMBL 304 3 0 2 4.2 Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1016/j.ejmech.2022.114464
44247803 196086 0 None -4 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation counting
ChEMBL 295 5 0 1 4.3 CN(C)CCC1=C(Cc2ccc(F)cc2)c2ccccc2C1 10.1021/jm900933k
CHEMBL560741 196086 0 None -4 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation counting
ChEMBL 295 5 0 1 4.3 CN(C)CCC1=C(Cc2ccc(F)cc2)c2ccccc2C1 10.1021/jm900933k
44401164 69816 0 None -2 9 Human 9.2 pKi = 9.2 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 329 2 0 3 4.5 CN(C)C[C@H]1CC2c3ccccc3Sc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL193639 69816 0 None -2 9 Human 9.2 pKi = 9.2 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 329 2 0 3 4.5 CN(C)C[C@H]1CC2c3ccccc3Sc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
103 4153 61 None -1 53 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human H1 receptorBinding affinity towards human H1 receptor
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm0002432
2875 4153 61 None -1 53 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human H1 receptorBinding affinity towards human H1 receptor
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm0002432
5736 4153 61 None -1 53 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human H1 receptorBinding affinity towards human H1 receptor
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm0002432
CHEMBL285802 4153 61 None -1 53 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human H1 receptorBinding affinity towards human H1 receptor
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm0002432
DB09225 4153 61 None -1 53 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human H1 receptorBinding affinity towards human H1 receptor
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm0002432
44326705 112323 0 None 5 3 Human 9.2 pKi = 9.2 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 293 2 0 2 3.8 CN(C)C[C@@H]1C[C@@H]2c3ccccc3Cc3ccccc3[C@H]2O1 10.1016/j.bmcl.2004.03.069
CHEMBL329268 112323 0 None 5 3 Human 9.2 pKi = 9.2 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 293 2 0 2 3.8 CN(C)C[C@@H]1C[C@@H]2c3ccccc3Cc3ccccc3[C@H]2O1 10.1016/j.bmcl.2004.03.069
15749405 101063 14 None - 1 Guinea pig 9.2 pKi = 9.2 Binding
The compound was tested in vitro for binding affinity against histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMThe compound was tested in vitro for binding affinity against histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 323 5 1 3 3.5 CN(C)CC/C=C1/c2ccccc2COc2ccc(CCO)cc21 10.1021/jm00089a020
CHEMBL294777 101063 14 None - 1 Guinea pig 9.2 pKi = 9.2 Binding
The compound was tested in vitro for binding affinity against histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMThe compound was tested in vitro for binding affinity against histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 323 5 1 3 3.5 CN(C)CC/C=C1/c2ccccc2COc2ccc(CCO)cc21 10.1021/jm00089a020
CHEMBL5270515 194609 0 None 39 3 Human 9.2 pKi = 9.2 Binding
Antagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysisAntagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysis
ChEMBL 452 8 1 5 3.6 CCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL5315265 194609 0 None 39 3 Human 9.2 pKi = 9.2 Binding
Antagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysisAntagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysis
ChEMBL 452 8 1 5 3.6 CCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
155519275 170433 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 364 2 0 2 5.1 Clc1ccc2c(c1)CCc1cccnc1C2=C1CCN(CC2CC2)CC1 10.1021/acs.jmedchem.9b00447
CHEMBL4448535 170433 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 364 2 0 2 5.1 Clc1ccc2c(c1)CCc1cccnc1C2=C1CCN(CC2CC2)CC1 10.1021/acs.jmedchem.9b00447
9839081 111646 0 None 1 3 Human 9.2 pKi = 9.2 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 294 2 0 3 3.4 CN(C)C[C@@H]1C[C@@H]2c3ccccc3Cc3ccccc3N2O1 10.1016/j.bmcl.2004.03.069
CHEMBL328573 111646 0 None 1 3 Human 9.2 pKi = 9.2 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 294 2 0 3 3.4 CN(C)C[C@@H]1C[C@@H]2c3ccccc3Cc3ccccc3N2O1 10.1016/j.bmcl.2004.03.069
21855 84246 42 None 7 6 Human 9.2 pKi = 9.2 Binding
Compound was evaluated for binding affinity towards cloned human histamine H1 receptors stably expressed in CHO-K1 cells using [3H]mepyramineCompound was evaluated for binding affinity towards cloned human histamine H1 receptors stably expressed in CHO-K1 cells using [3H]mepyramine
ChEMBL 292 5 0 2 4.1 CC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL22108 84246 42 None 7 6 Human 9.2 pKi = 9.2 Binding
Compound was evaluated for binding affinity towards cloned human histamine H1 receptors stably expressed in CHO-K1 cells using [3H]mepyramineCompound was evaluated for binding affinity towards cloned human histamine H1 receptors stably expressed in CHO-K1 cells using [3H]mepyramine
ChEMBL 292 5 0 2 4.1 CC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
44326319 207211 0 None 9 3 Human 9.2 pKi = 9.2 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 293 2 0 2 3.8 CN(C)CC1C[C@@H]2c3ccccc3Cc3ccccc3[C@H]2O1 10.1016/j.bmcl.2004.03.069
CHEMBL92667 207211 0 None 9 3 Human 9.2 pKi = 9.2 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 293 2 0 2 3.8 CN(C)CC1C[C@@H]2c3ccccc3Cc3ccccc3[C@H]2O1 10.1016/j.bmcl.2004.03.069
46884734 7972 0 None 6 2 Human 9.2 pKi = 9.2 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 341 6 0 4 3.7 COc1nccnc1[C@H](C)C1=C(CCN(C)C)Cc2cc(F)ccc21 10.1016/j.bmcl.2010.02.055
CHEMBL1090526 7972 0 None 6 2 Human 9.2 pKi = 9.2 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 341 6 0 4 3.7 COc1nccnc1[C@H](C)C1=C(CCN(C)C)Cc2cc(F)ccc21 10.1016/j.bmcl.2010.02.055
46884734 7972 0 None 6 2 Human 9.2 pKi = 9.2 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 341 6 0 4 3.7 COc1nccnc1[C@H](C)C1=C(CCN(C)C)Cc2cc(F)ccc21 10.1016/j.bmcl.2010.07.117
CHEMBL1090526 7972 0 None 6 2 Human 9.2 pKi = 9.2 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 341 6 0 4 3.7 COc1nccnc1[C@H](C)C1=C(CCN(C)C)Cc2cc(F)ccc21 10.1016/j.bmcl.2010.07.117
1227 2489 43 None -2 12 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor in HEK293 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor in HEK293 cells after 60 mins by scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/acs.jmedchem.6b01422
2331 2489 43 None -2 12 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor in HEK293 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor in HEK293 cells after 60 mins by scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/acs.jmedchem.6b01422
3957 2489 43 None -2 12 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor in HEK293 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor in HEK293 cells after 60 mins by scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/acs.jmedchem.6b01422
4992 2489 43 None -2 12 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor in HEK293 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor in HEK293 cells after 60 mins by scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/acs.jmedchem.6b01422
CHEMBL511 2489 43 None -2 12 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor in HEK293 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor in HEK293 cells after 60 mins by scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/acs.jmedchem.6b01422
DB06691 2489 43 None -2 12 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor in HEK293 cells after 60 mins by scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor in HEK293 cells after 60 mins by scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/acs.jmedchem.6b01422
1210 918 51 None -20 21 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
1213 918 51 None -20 21 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
2725 918 51 None -20 21 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
33036 918 51 None -20 21 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
4411 918 51 None -20 21 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
616 918 51 None -20 21 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
6976 918 51 None -20 21 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
716121 918 51 None -20 21 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL1201353 918 51 None -20 21 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL1554789 918 51 None -20 21 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL505 918 51 None -20 21 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
DB01114 918 51 None -20 21 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
DB13679 918 51 None -20 21 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL5269671 194600 0 None 44 3 Human 9.1 pKi = 9.1 Binding
Antagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysisAntagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysis
ChEMBL 466 9 1 5 4.0 CCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL5315170 194600 0 None 44 3 Human 9.1 pKi = 9.1 Binding
Antagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysisAntagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysis
ChEMBL 466 9 1 5 4.0 CCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL5272034 194611 0 None 10 3 Human 9.1 pKi = 9.1 Binding
Antagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysisAntagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysis
ChEMBL 496 11 1 6 3.6 COCCNC(=O)CCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL5315277 194611 0 None 10 3 Human 9.1 pKi = 9.1 Binding
Antagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysisAntagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysis
ChEMBL 496 11 1 6 3.6 COCCNC(=O)CCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL5286701 194629 0 None 12 3 Human 9.1 pKi = 9.1 Binding
Antagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysisAntagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysis
ChEMBL 482 10 1 6 3.3 COCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL5315483 194629 0 None 12 3 Human 9.1 pKi = 9.1 Binding
Antagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysisAntagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysis
ChEMBL 482 10 1 6 3.3 COCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
155567541 175992 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 378 2 0 2 5.5 Clc1ccc2c(c1)CCc1cccnc1C2=C1CCN(CC2CCC2)CC1 10.1021/acs.jmedchem.9b00447
CHEMBL4588983 175992 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 378 2 0 2 5.5 Clc1ccc2c(c1)CCc1cccnc1C2=C1CCN(CC2CCC2)CC1 10.1021/acs.jmedchem.9b00447
46884666 8286 0 None 3019 2 Human 9.1 pKi = 9.1 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 298 5 0 3 4.2 C[C@H](C1=C(CCN(C)C)Cc2ccccc21)c1nccs1 10.1016/j.bmcl.2010.02.055
CHEMBL1092598 8286 0 None 3019 2 Human 9.1 pKi = 9.1 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 298 5 0 3 4.2 C[C@H](C1=C(CCN(C)C)Cc2ccccc21)c1nccs1 10.1016/j.bmcl.2010.02.055
11515387 8301 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 327 6 0 4 3.1 COc1nccnc1CC1=C(CCN(C)C)Cc2cc(F)ccc21 10.1016/j.bmcl.2010.02.055
CHEMBL1092651 8301 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 327 6 0 4 3.1 COc1nccnc1CC1=C(CCN(C)C)Cc2cc(F)ccc21 10.1016/j.bmcl.2010.02.055
652557 59458 13 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 330 6 1 5 2.3 O=C(CCN1CCN(Cc2ccccc2)CC1)Nc1nccs1 10.1021/acs.jmedchem.8b00718
CHEMBL1712377 59458 13 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 330 6 1 5 2.3 O=C(CCN1CCN(Cc2ccccc2)CC1)Nc1nccs1 10.1021/acs.jmedchem.8b00718
11759212 57892 0 None 40 6 Human 9.1 pKi = 9.1 Binding
Compound was evaluated for binding affinity towards cloned human histamine H1 receptors stably expressed in CHO-K1 cells using [3H]mepyramineCompound was evaluated for binding affinity towards cloned human histamine H1 receptors stably expressed in CHO-K1 cells using [3H]mepyramine
ChEMBL 326 5 0 2 4.8 CC(C1=C(CCN(C)C)Cc2cc(Cl)ccc21)c1ccccn1 10.1021/jm020895l
CHEMBL167223 57892 0 None 40 6 Human 9.1 pKi = 9.1 Binding
Compound was evaluated for binding affinity towards cloned human histamine H1 receptors stably expressed in CHO-K1 cells using [3H]mepyramineCompound was evaluated for binding affinity towards cloned human histamine H1 receptors stably expressed in CHO-K1 cells using [3H]mepyramine
ChEMBL 326 5 0 2 4.8 CC(C1=C(CCN(C)C)Cc2cc(Cl)ccc21)c1ccccn1 10.1021/jm020895l
135 2532 43 None -1 58 Guinea pig 9.1 pKi = 9.1 Binding
Inhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 minInhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 min
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00017a019
1796 2532 43 None -1 58 Guinea pig 9.1 pKi = 9.1 Binding
Inhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 minInhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 min
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00017a019
4184 2532 43 None -1 58 Guinea pig 9.1 pKi = 9.1 Binding
Inhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 minInhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 min
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00017a019
CHEMBL6437 2532 43 None -1 58 Guinea pig 9.1 pKi = 9.1 Binding
Inhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 minInhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 min
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00017a019
DB06148 2532 43 None -1 58 Guinea pig 9.1 pKi = 9.1 Binding
Inhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 minInhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 min
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00017a019
44247935 196577 0 None -2 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation counting
ChEMBL 294 5 0 3 4.1 C[C@@H](c1ccccn1)c1c(CCN(C)C)oc2ccccc12 10.1021/jm900933k
CHEMBL563920 196577 0 None -2 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation counting
ChEMBL 294 5 0 3 4.1 C[C@@H](c1ccccn1)c1c(CCN(C)C)oc2ccccc12 10.1021/jm900933k
1210 918 51 None -20 21 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/j.bmcl.2013.12.024
1213 918 51 None -20 21 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/j.bmcl.2013.12.024
2725 918 51 None -20 21 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/j.bmcl.2013.12.024
33036 918 51 None -20 21 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/j.bmcl.2013.12.024
4411 918 51 None -20 21 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/j.bmcl.2013.12.024
616 918 51 None -20 21 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/j.bmcl.2013.12.024
6976 918 51 None -20 21 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/j.bmcl.2013.12.024
716121 918 51 None -20 21 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/j.bmcl.2013.12.024
CHEMBL1201353 918 51 None -20 21 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/j.bmcl.2013.12.024
CHEMBL1554789 918 51 None -20 21 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/j.bmcl.2013.12.024
CHEMBL505 918 51 None -20 21 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/j.bmcl.2013.12.024
DB01114 918 51 None -20 21 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/j.bmcl.2013.12.024
DB13679 918 51 None -20 21 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/j.bmcl.2013.12.024
1227 2489 43 None -2 12 Human 9.0 pKi = 9.0 Binding
Binding affinity to human histamine H1 receptor by radioligand displacement assayBinding affinity to human histamine H1 receptor by radioligand displacement assay
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.ejmech.2013.01.044
2331 2489 43 None -2 12 Human 9.0 pKi = 9.0 Binding
Binding affinity to human histamine H1 receptor by radioligand displacement assayBinding affinity to human histamine H1 receptor by radioligand displacement assay
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.ejmech.2013.01.044
3957 2489 43 None -2 12 Human 9.0 pKi = 9.0 Binding
Binding affinity to human histamine H1 receptor by radioligand displacement assayBinding affinity to human histamine H1 receptor by radioligand displacement assay
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.ejmech.2013.01.044
4992 2489 43 None -2 12 Human 9.0 pKi = 9.0 Binding
Binding affinity to human histamine H1 receptor by radioligand displacement assayBinding affinity to human histamine H1 receptor by radioligand displacement assay
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.ejmech.2013.01.044
CHEMBL511 2489 43 None -2 12 Human 9.0 pKi = 9.0 Binding
Binding affinity to human histamine H1 receptor by radioligand displacement assayBinding affinity to human histamine H1 receptor by radioligand displacement assay
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.ejmech.2013.01.044
DB06691 2489 43 None -2 12 Human 9.0 pKi = 9.0 Binding
Binding affinity to human histamine H1 receptor by radioligand displacement assayBinding affinity to human histamine H1 receptor by radioligand displacement assay
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.ejmech.2013.01.044
124087 1389 114 None 3 15 Human 9.0 pKi = 9.0 Binding
Binding affinity towards human histamine H1 receptor expressed in CHO-K1 cellsBinding affinity towards human histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1016/j.bmcl.2004.08.060
7157 1389 114 None 3 15 Human 9.0 pKi = 9.0 Binding
Binding affinity towards human histamine H1 receptor expressed in CHO-K1 cellsBinding affinity towards human histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1016/j.bmcl.2004.08.060
814 1389 114 None 3 15 Human 9.0 pKi = 9.0 Binding
Binding affinity towards human histamine H1 receptor expressed in CHO-K1 cellsBinding affinity towards human histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1016/j.bmcl.2004.08.060
CHEMBL1172 1389 114 None 3 15 Human 9.0 pKi = 9.0 Binding
Binding affinity towards human histamine H1 receptor expressed in CHO-K1 cellsBinding affinity towards human histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1016/j.bmcl.2004.08.060
DB00967 1389 114 None 3 15 Human 9.0 pKi = 9.0 Binding
Binding affinity towards human histamine H1 receptor expressed in CHO-K1 cellsBinding affinity towards human histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1016/j.bmcl.2004.08.060
135398737 958 93 None 2 89 Human 9.0 pKi = 9 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 958 93 None 2 89 Human 9.0 pKi = 9 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 958 93 None 2 89 Human 9.0 pKi = 9 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 958 93 None 2 89 Human 9.0 pKi = 9 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 958 93 None 2 89 Human 9.0 pKi = 9 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
46865650 8285 0 None 3715 2 Human 9.0 pKi = 9 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 323 6 0 4 3.6 COc1nccnc1[C@H](C)C1=C(CCN(C)C)Cc2ccccc21 10.1016/j.bmcl.2010.02.055
CHEMBL1092597 8285 0 None 3715 2 Human 9.0 pKi = 9 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 323 6 0 4 3.6 COc1nccnc1[C@H](C)C1=C(CCN(C)C)Cc2ccccc21 10.1016/j.bmcl.2010.02.055
163091 494 34 None -6 10 Human 9.0 pKi = 9 Binding
Binding affinity to H1 histamine receptor (unknown origin)Binding affinity to H1 histamine receptor (unknown origin)
ChEMBL 285 0 0 2 4.3 Clc1ccc2c(c1)[C@H]1CN(C[C@@H]1c1c(O2)cccc1)C 10.1016/j.bmcl.2020.127681
22 494 34 None -6 10 Human 9.0 pKi = 9 Binding
Binding affinity to H1 histamine receptor (unknown origin)Binding affinity to H1 histamine receptor (unknown origin)
ChEMBL 285 0 0 2 4.3 Clc1ccc2c(c1)[C@H]1CN(C[C@@H]1c1c(O2)cccc1)C 10.1016/j.bmcl.2020.127681
CHEMBL504548 494 34 None -6 10 Human 9.0 pKi = 9 Binding
Binding affinity to H1 histamine receptor (unknown origin)Binding affinity to H1 histamine receptor (unknown origin)
ChEMBL 285 0 0 2 4.3 Clc1ccc2c(c1)[C@H]1CN(C[C@@H]1c1c(O2)cccc1)C 10.1016/j.bmcl.2020.127681
68168663 175695 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 352 1 0 2 5.1 CC(C)N1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/acs.jmedchem.9b00447
CHEMBL4582006 175695 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 352 1 0 2 5.1 CC(C)N1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/acs.jmedchem.9b00447
15662541 67772 0 None - 1 Guinea pig 9.0 pKi = 9 Binding
Inhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranesInhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 322 2 0 3 4.8 c1ccc2c(c1)Sc1ccccc1N2CC12CCN(CC1)CC2 10.1021/jm00017a019
CHEMBL1908311 67772 0 None - 1 Guinea pig 9.0 pKi = 9 Binding
Inhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranesInhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 322 2 0 3 4.8 c1ccc2c(c1)Sc1ccccc1N2CC12CCN(CC1)CC2 10.1021/jm00017a019
135398737 958 93 None 2 89 Human 9.0 pKi = 9 Binding
Inhibition of histamine H1 receptor (unknown origin)Inhibition of histamine H1 receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401958n
38 958 93 None 2 89 Human 9.0 pKi = 9 Binding
Inhibition of histamine H1 receptor (unknown origin)Inhibition of histamine H1 receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401958n
722 958 93 None 2 89 Human 9.0 pKi = 9 Binding
Inhibition of histamine H1 receptor (unknown origin)Inhibition of histamine H1 receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401958n
CHEMBL42 958 93 None 2 89 Human 9.0 pKi = 9 Binding
Inhibition of histamine H1 receptor (unknown origin)Inhibition of histamine H1 receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401958n
DB00363 958 93 None 2 89 Human 9.0 pKi = 9 Binding
Inhibition of histamine H1 receptor (unknown origin)Inhibition of histamine H1 receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401958n
4011 82408 49 None 6 24 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
CHEMBL21731 82408 49 None 6 24 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
135398737 958 93 None 2 89 Human 9.0 pKi = 9.0 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm049632c
38 958 93 None 2 89 Human 9.0 pKi = 9.0 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm049632c
722 958 93 None 2 89 Human 9.0 pKi = 9.0 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm049632c
CHEMBL42 958 93 None 2 89 Human 9.0 pKi = 9.0 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm049632c
DB00363 958 93 None 2 89 Human 9.0 pKi = 9.0 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm049632c
180 401 56 None -1 40 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1016/j.bmcl.2008.09.012
200 401 56 None -1 40 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1016/j.bmcl.2008.09.012
2160 401 56 None -1 40 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1016/j.bmcl.2008.09.012
CHEMBL629 401 56 None -1 40 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1016/j.bmcl.2008.09.012
DB00321 401 56 None -1 40 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1016/j.bmcl.2008.09.012
6761 67799 19 None -1 18 Human 8.9 pKi = 8.9 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
CHEMBL1909072 67799 19 None -1 18 Human 8.9 pKi = 8.9 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
124087 1389 114 None 3 15 Human 8.9 pKi = 8.9 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
7157 1389 114 None 3 15 Human 8.9 pKi = 8.9 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
814 1389 114 None 3 15 Human 8.9 pKi = 8.9 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
CHEMBL1172 1389 114 None 3 15 Human 8.9 pKi = 8.9 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
DB00967 1389 114 None 3 15 Human 8.9 pKi = 8.9 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
44326442 107120 0 None 14 3 Human 8.9 pKi = 8.9 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 366 2 0 4 4.0 CN1CCN(CC2C[C@@H]3c4ccccc4Sc4ccccc4[C@H]3O2)CC1 10.1016/j.bmcl.2004.03.069
CHEMBL316068 107120 0 None 14 3 Human 8.9 pKi = 8.9 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 366 2 0 4 4.0 CN1CCN(CC2C[C@@H]3c4ccccc4Sc4ccccc4[C@H]3O2)CC1 10.1016/j.bmcl.2004.03.069
135398745 2914 112 None 1 65 Human 8.9 pKi = 8.9 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm049632c
47 2914 112 None 1 65 Human 8.9 pKi = 8.9 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm049632c
CHEMBL715 2914 112 None 1 65 Human 8.9 pKi = 8.9 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm049632c
DB00334 2914 112 None 1 65 Human 8.9 pKi = 8.9 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm049632c
44401106 124327 0 None -1 9 Human 8.9 pKi = 8.9 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 329 2 0 3 4.5 CN(C)C[C@@H]1CC2c3ccccc3Sc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL363581 124327 0 None -1 9 Human 8.9 pKi = 8.9 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 329 2 0 3 4.5 CN(C)C[C@@H]1CC2c3ccccc3Sc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
44290349 178537 0 None 131 2 Rat 8.9 pKi = 8.9 Binding
Compound was evaluated for binding activity against [3H]pyrilamine as radioligand for Histamine H1 receptorCompound was evaluated for binding activity against [3H]pyrilamine as radioligand for Histamine H1 receptor
ChEMBL 411 5 2 6 2.1 O=C(c1ccc(F)cc1)C1CCN(CCn2c(=O)[nH]c3cc(O)ccc3c2=O)CC1 10.1021/jm00159a017
CHEMBL46683 178537 0 None 131 2 Rat 8.9 pKi = 8.9 Binding
Compound was evaluated for binding activity against [3H]pyrilamine as radioligand for Histamine H1 receptorCompound was evaluated for binding activity against [3H]pyrilamine as radioligand for Histamine H1 receptor
ChEMBL 411 5 2 6 2.1 O=C(c1ccc(F)cc1)C1CCN(CCn2c(=O)[nH]c3cc(O)ccc3c2=O)CC1 10.1021/jm00159a017
2267 559 71 None 10 7 Human 8.9 pKi = 8.9 Binding
Antagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysisAntagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysis
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1021/acsmedchemlett.7b00112
271 559 71 None 10 7 Human 8.9 pKi = 8.9 Binding
Antagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysisAntagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysis
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1021/acsmedchemlett.7b00112
7121 559 71 None 10 7 Human 8.9 pKi = 8.9 Binding
Antagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysisAntagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysis
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1021/acsmedchemlett.7b00112
CHEMBL639 559 71 None 10 7 Human 8.9 pKi = 8.9 Binding
Antagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysisAntagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysis
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1021/acsmedchemlett.7b00112
DB00972 559 71 None 10 7 Human 8.9 pKi = 8.9 Binding
Antagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysisAntagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysis
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1021/acsmedchemlett.7b00112
CHEMBL5273244 194616 0 None 63 3 Human 8.9 pKi = 8.9 Binding
Antagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysisAntagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysis
ChEMBL 468 9 1 6 2.9 COCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL5315364 194616 0 None 63 3 Human 8.9 pKi = 8.9 Binding
Antagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysisAntagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysis
ChEMBL 468 9 1 6 2.9 COCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
155536963 172238 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 392 2 0 2 5.9 Clc1ccc2c(c1)CCc1cccnc1C2=C1CCN(CC2CCCC2)CC1 10.1021/acs.jmedchem.9b00447
CHEMBL4474226 172238 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 392 2 0 2 5.9 Clc1ccc2c(c1)CCc1cccnc1C2=C1CCN(CC2CCCC2)CC1 10.1021/acs.jmedchem.9b00447
1227 2489 43 None -2 12 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/acs.jmedchem.6b00981
2331 2489 43 None -2 12 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/acs.jmedchem.6b00981
3957 2489 43 None -2 12 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/acs.jmedchem.6b00981
4992 2489 43 None -2 12 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/acs.jmedchem.6b00981
CHEMBL511 2489 43 None -2 12 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/acs.jmedchem.6b00981
DB06691 2489 43 None -2 12 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/acs.jmedchem.6b00981
46884733 7911 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 353 7 0 5 3.6 COc1ccc2c(c1)CC(CCN(C)C)=C2[C@@H](C)c1nccnc1OC 10.1016/j.bmcl.2010.02.055
CHEMBL1090186 7911 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 353 7 0 5 3.6 COc1ccc2c(c1)CC(CCN(C)C)=C2[C@@H](C)c1nccnc1OC 10.1016/j.bmcl.2010.02.055
44247806 195668 2 None 14454 2 Human 8.9 pKi = 8.9 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 293 5 0 3 3.5 C[C@H](C1=C(CCN(C)C)Cc2ccccc21)c1cnccn1 10.1016/j.bmcl.2010.02.055
CHEMBL556506 195668 2 None 14454 2 Human 8.9 pKi = 8.9 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 293 5 0 3 3.5 C[C@H](C1=C(CCN(C)C)Cc2ccccc21)c1cnccn1 10.1016/j.bmcl.2010.02.055
44247806 195668 2 None 14454 2 Human 8.9 pKi = 8.9 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 293 5 0 3 3.5 C[C@H](C1=C(CCN(C)C)Cc2ccccc21)c1cnccn1 10.1016/j.bmcl.2010.12.053
CHEMBL556506 195668 2 None 14454 2 Human 8.9 pKi = 8.9 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 293 5 0 3 3.5 C[C@H](C1=C(CCN(C)C)Cc2ccccc21)c1cnccn1 10.1016/j.bmcl.2010.12.053
45272894 195655 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 375 4 0 5 4.3 Fc1ccc(Cn2c(N3CCC(n4ccnc4)CC3)nc3ccccc32)cc1 10.1016/j.bmcl.2009.05.086
CHEMBL556449 195655 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 375 4 0 5 4.3 Fc1ccc(Cn2c(N3CCC(n4ccnc4)CC3)nc3ccccc32)cc1 10.1016/j.bmcl.2009.05.086
44247806 195668 2 None 14454 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation counting
ChEMBL 293 5 0 3 3.5 C[C@H](C1=C(CCN(C)C)Cc2ccccc21)c1cnccn1 10.1021/jm900933k
CHEMBL556506 195668 2 None 14454 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation counting
ChEMBL 293 5 0 3 3.5 C[C@H](C1=C(CCN(C)C)Cc2ccccc21)c1cnccn1 10.1021/jm900933k
46884670 8223 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 313 5 0 3 3.6 CN(C)CCC1=C(Cc2cnccn2)c2ccc(Cl)cc2C1 10.1016/j.bmcl.2010.02.055
CHEMBL1092259 8223 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 313 5 0 3 3.6 CN(C)CCC1=C(Cc2cnccn2)c2ccc(Cl)cc2C1 10.1016/j.bmcl.2010.02.055
11702114 8299 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 297 5 0 3 3.1 CN(C)CCC1=C(Cc2cnccn2)c2ccc(F)cc2C1 10.1016/j.bmcl.2010.02.055
CHEMBL1092649 8299 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 297 5 0 3 3.1 CN(C)CCC1=C(Cc2cnccn2)c2ccc(F)cc2C1 10.1016/j.bmcl.2010.02.055
11186523 127511 0 None 1 9 Human 8.9 pKi = 8.9 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 329 2 0 3 4.5 CN(C)C[C@H]1C[C@@H]2c3ccccc3Sc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL366164 127511 0 None 1 9 Human 8.9 pKi = 8.9 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 329 2 0 3 4.5 CN(C)C[C@H]1C[C@@H]2c3ccccc3Sc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
1027 1576 73 None 6 2 Guinea pig 8.9 pKi = 8.9 Binding
Inhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 minInhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 min
ChEMBL 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 10.1021/jm00017a019
3241 1576 73 None 6 2 Guinea pig 8.9 pKi = 8.9 Binding
Inhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 minInhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 min
ChEMBL 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 10.1021/jm00017a019
7176 1576 73 None 6 2 Guinea pig 8.9 pKi = 8.9 Binding
Inhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 minInhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 min
ChEMBL 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 10.1021/jm00017a019
CHEMBL1106 1576 73 None 6 2 Guinea pig 8.9 pKi = 8.9 Binding
Inhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 minInhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 min
ChEMBL 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 10.1021/jm00017a019
DB00751 1576 73 None 6 2 Guinea pig 8.9 pKi = 8.9 Binding
Inhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 minInhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 min
ChEMBL 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 10.1021/jm00017a019
135398745 2914 112 None 1 65 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
47 2914 112 None 1 65 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
CHEMBL715 2914 112 None 1 65 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
DB00334 2914 112 None 1 65 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
46884698 8300 0 None 1318 2 Human 8.8 pKi = 8.8 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 343 6 0 4 3.6 COc1nccnc1CC1=C(CCN(C)C)Cc2cc(Cl)ccc21 10.1016/j.bmcl.2010.02.055
CHEMBL1092650 8300 0 None 1318 2 Human 8.8 pKi = 8.8 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 343 6 0 4 3.6 COc1nccnc1CC1=C(CCN(C)C)Cc2cc(Cl)ccc21 10.1016/j.bmcl.2010.02.055
45272876 196503 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 348 4 0 4 3.9 Cc1ccc(Cn2c(N3CCC(N(C)C)CC3)nc3ccccc32)cc1 10.1016/j.bmcl.2009.05.086
CHEMBL563451 196503 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 348 4 0 4 3.9 Cc1ccc(Cn2c(N3CCC(N(C)C)CC3)nc3ccccc32)cc1 10.1016/j.bmcl.2009.05.086
44247806 195668 2 None 14454 2 Human 8.8 pKi = 8.8 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 293 5 0 3 3.5 C[C@H](C1=C(CCN(C)C)Cc2ccccc21)c1cnccn1 10.1016/j.bmcl.2010.07.117
CHEMBL556506 195668 2 None 14454 2 Human 8.8 pKi = 8.8 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 293 5 0 3 3.5 C[C@H](C1=C(CCN(C)C)Cc2ccccc21)c1cnccn1 10.1016/j.bmcl.2010.07.117
124087 1389 114 None 3 15 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1021/acs.jmedchem.9b00447
7157 1389 114 None 3 15 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1021/acs.jmedchem.9b00447
814 1389 114 None 3 15 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1021/acs.jmedchem.9b00447
CHEMBL1172 1389 114 None 3 15 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1021/acs.jmedchem.9b00447
DB00967 1389 114 None 3 15 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1021/acs.jmedchem.9b00447
1227 2489 43 None -2 12 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells after 3 hrsDisplacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells after 3 hrs
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmcl.2013.01.025
2331 2489 43 None -2 12 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells after 3 hrsDisplacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells after 3 hrs
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmcl.2013.01.025
3957 2489 43 None -2 12 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells after 3 hrsDisplacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells after 3 hrs
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmcl.2013.01.025
4992 2489 43 None -2 12 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells after 3 hrsDisplacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells after 3 hrs
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmcl.2013.01.025
CHEMBL511 2489 43 None -2 12 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells after 3 hrsDisplacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells after 3 hrs
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmcl.2013.01.025
DB06691 2489 43 None -2 12 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells after 3 hrsDisplacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells after 3 hrs
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmcl.2013.01.025
1228 3866 34 None -5 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]pyrilamine from histamine H1 receptorDisplacement of [3H]pyrilamine from histamine H1 receptor
ChEMBL 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 10.1021/np50094a001
2763 3866 34 None -5 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]pyrilamine from histamine H1 receptorDisplacement of [3H]pyrilamine from histamine H1 receptor
ChEMBL 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 10.1021/np50094a001
5282443 3866 34 None -5 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]pyrilamine from histamine H1 receptorDisplacement of [3H]pyrilamine from histamine H1 receptor
ChEMBL 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 10.1021/np50094a001
CHEMBL855 3866 34 None -5 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]pyrilamine from histamine H1 receptorDisplacement of [3H]pyrilamine from histamine H1 receptor
ChEMBL 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 10.1021/np50094a001
DB00427 3866 34 None -5 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]pyrilamine from histamine H1 receptorDisplacement of [3H]pyrilamine from histamine H1 receptor
ChEMBL 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 10.1021/np50094a001
1816 2540 102 None -3 18 Human 8.8 pKi = 8.8 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1021/jm049632c
4205 2540 102 None -3 18 Human 8.8 pKi = 8.8 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1021/jm049632c
7241 2540 102 None -3 18 Human 8.8 pKi = 8.8 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1021/jm049632c
CHEMBL654 2540 102 None -3 18 Human 8.8 pKi = 8.8 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1021/jm049632c
DB00370 2540 102 None -3 18 Human 8.8 pKi = 8.8 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1021/jm049632c
2247 505 81 None -4 42 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 505 81 None -4 42 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 505 81 None -4 42 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 505 81 None -4 42 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 505 81 None -4 42 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
1228 3866 34 None 5 4 Guinea pig 8.8 pKi = 8.8 Binding
Inhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 minInhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 min
ChEMBL 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 10.1021/jm00017a019
2763 3866 34 None 5 4 Guinea pig 8.8 pKi = 8.8 Binding
Inhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 minInhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 min
ChEMBL 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 10.1021/jm00017a019
5282443 3866 34 None 5 4 Guinea pig 8.8 pKi = 8.8 Binding
Inhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 minInhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 min
ChEMBL 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 10.1021/jm00017a019
CHEMBL855 3866 34 None 5 4 Guinea pig 8.8 pKi = 8.8 Binding
Inhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 minInhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 min
ChEMBL 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 10.1021/jm00017a019
DB00427 3866 34 None 5 4 Guinea pig 8.8 pKi = 8.8 Binding
Inhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 minInhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 min
ChEMBL 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 10.1021/jm00017a019
4011 82408 49 None 6 24 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 10.1016/j.bmcl.2008.09.012
CHEMBL21731 82408 49 None 6 24 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 10.1016/j.bmcl.2008.09.012
11702115 8304 2 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 297 5 0 3 3.1 CN(C)CCC1=C(Cc2cccnn2)c2ccc(F)cc2C1 10.1016/j.bmcl.2010.02.055
CHEMBL1092662 8304 2 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 297 5 0 3 3.1 CN(C)CCC1=C(Cc2cccnn2)c2ccc(F)cc2C1 10.1016/j.bmcl.2010.02.055
11695591 8321 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 328 5 0 3 4.7 C[C@H](c1cccnc1F)c1c(CCN(C)C)sc2ccccc12 10.1016/j.bmcl.2010.01.134
CHEMBL1092765 8321 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 328 5 0 3 4.7 C[C@H](c1cccnc1F)c1c(CCN(C)C)sc2ccccc12 10.1016/j.bmcl.2010.01.134
1227 2489 43 None -2 12 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in HEK-293 cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in HEK-293 cells
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.ejmech.2014.12.045
2331 2489 43 None -2 12 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in HEK-293 cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in HEK-293 cells
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.ejmech.2014.12.045
3957 2489 43 None -2 12 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in HEK-293 cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in HEK-293 cells
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.ejmech.2014.12.045
4992 2489 43 None -2 12 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in HEK-293 cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in HEK-293 cells
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.ejmech.2014.12.045
CHEMBL511 2489 43 None -2 12 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in HEK-293 cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in HEK-293 cells
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.ejmech.2014.12.045
DB06691 2489 43 None -2 12 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in HEK-293 cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in HEK-293 cells
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.ejmech.2014.12.045
1227 2489 43 None -2 12 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]pyrilamine from human recombinant H1 receptor expressed in HEK293 cellsDisplacement of [3H]pyrilamine from human recombinant H1 receptor expressed in HEK293 cells
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm401895u
2331 2489 43 None -2 12 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]pyrilamine from human recombinant H1 receptor expressed in HEK293 cellsDisplacement of [3H]pyrilamine from human recombinant H1 receptor expressed in HEK293 cells
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm401895u
3957 2489 43 None -2 12 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]pyrilamine from human recombinant H1 receptor expressed in HEK293 cellsDisplacement of [3H]pyrilamine from human recombinant H1 receptor expressed in HEK293 cells
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm401895u
4992 2489 43 None -2 12 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]pyrilamine from human recombinant H1 receptor expressed in HEK293 cellsDisplacement of [3H]pyrilamine from human recombinant H1 receptor expressed in HEK293 cells
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm401895u
CHEMBL511 2489 43 None -2 12 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]pyrilamine from human recombinant H1 receptor expressed in HEK293 cellsDisplacement of [3H]pyrilamine from human recombinant H1 receptor expressed in HEK293 cells
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm401895u
DB06691 2489 43 None -2 12 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]pyrilamine from human recombinant H1 receptor expressed in HEK293 cellsDisplacement of [3H]pyrilamine from human recombinant H1 receptor expressed in HEK293 cells
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm401895u
135 2532 43 None -1 58 Human 8.8 pKi = 8.8 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm049632c
1796 2532 43 None -1 58 Human 8.8 pKi = 8.8 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm049632c
4184 2532 43 None -1 58 Human 8.8 pKi = 8.8 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm049632c
CHEMBL6437 2532 43 None -1 58 Human 8.8 pKi = 8.8 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm049632c
DB06148 2532 43 None -1 58 Human 8.8 pKi = 8.8 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm049632c
11702115 8304 2 None - 1 Human 8.8 pKi = 8.8 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 297 5 0 3 3.1 CN(C)CCC1=C(Cc2cccnn2)c2ccc(F)cc2C1 10.1016/j.bmcl.2010.07.117
CHEMBL1092662 8304 2 None - 1 Human 8.8 pKi = 8.8 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 297 5 0 3 3.1 CN(C)CCC1=C(Cc2cccnn2)c2ccc(F)cc2C1 10.1016/j.bmcl.2010.07.117
155539495 172846 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 394 4 0 2 6.2 CCC(CC)CN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/acs.jmedchem.9b00447
CHEMBL4514700 172846 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 394 4 0 2 6.2 CCC(CC)CN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/acs.jmedchem.9b00447
135398737 958 93 None 2 89 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2008.06.030
38 958 93 None 2 89 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2008.06.030
722 958 93 None 2 89 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2008.06.030
CHEMBL42 958 93 None 2 89 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2008.06.030
DB00363 958 93 None 2 89 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2008.06.030
135398737 958 93 None 2 89 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]pyrilamine from human H1 receptor by liquid scintillation countingDisplacement of [3H]pyrilamine from human H1 receptor by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2011.12.019
38 958 93 None 2 89 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]pyrilamine from human H1 receptor by liquid scintillation countingDisplacement of [3H]pyrilamine from human H1 receptor by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2011.12.019
722 958 93 None 2 89 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]pyrilamine from human H1 receptor by liquid scintillation countingDisplacement of [3H]pyrilamine from human H1 receptor by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2011.12.019
CHEMBL42 958 93 None 2 89 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]pyrilamine from human H1 receptor by liquid scintillation countingDisplacement of [3H]pyrilamine from human H1 receptor by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2011.12.019
DB00363 958 93 None 2 89 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]pyrilamine from human H1 receptor by liquid scintillation countingDisplacement of [3H]pyrilamine from human H1 receptor by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2011.12.019
45272875 195844 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 352 4 0 4 3.8 CN(C)C1CCN(c2nc3ccccc3n2Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2009.05.086
CHEMBL558467 195844 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 352 4 0 4 3.8 CN(C)C1CCN(c2nc3ccccc3n2Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2009.05.086
4098 32505 30 None 1 11 Human 8.7 pKi = 8.7 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 nan
CHEMBL1255739 32505 30 None 1 11 Human 8.7 pKi = 8.7 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 nan
CHEMBL1411979 32505 30 None 1 11 Human 8.7 pKi = 8.7 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 nan
44326125 111701 0 None 8 3 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 455 4 0 3 5.9 O=C(c1ccc(F)cc1)C1CCN(CC2C[C@@H]3c4ccccc4Cc4ccccc4[C@H]3O2)CC1 10.1016/j.bmcl.2004.03.069
CHEMBL328662 111701 0 None 8 3 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 455 4 0 3 5.9 O=C(c1ccc(F)cc1)C1CCN(CC2C[C@@H]3c4ccccc4Cc4ccccc4[C@H]3O2)CC1 10.1016/j.bmcl.2004.03.069
2726 919 68 None -2 72 Human 8.7 pKi = 8.7 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 919 68 None -2 72 Human 8.7 pKi = 8.7 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 919 68 None -2 72 Human 8.7 pKi = 8.7 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 919 68 None -2 72 Human 8.7 pKi = 8.7 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 919 68 None -2 72 Human 8.7 pKi = 8.7 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
134135966 154445 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 281 4 0 2 3.8 CN1CCC(Oc2ccccc2Cc2ccccc2)CC1 10.1021/acs.jmedchem.6b00981
CHEMBL3906929 154445 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 281 4 0 2 3.8 CN1CCC(Oc2ccccc2Cc2ccccc2)CC1 10.1021/acs.jmedchem.6b00981
CHEMBL3990109 154445 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 281 4 0 2 3.8 CN1CCC(Oc2ccccc2Cc2ccccc2)CC1 10.1021/acs.jmedchem.6b00981
18715379 9143 0 None - 1 Rat 8.0 pKi = 8 Binding
Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.
ChEMBL 430 0 0 2 5.0 CC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3cc(Br)cnc32)CC1 10.1016/S0960-894X(00)80290-5
CHEMBL11001 9143 0 None - 1 Rat 8.0 pKi = 8 Binding
Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.
ChEMBL 430 0 0 2 5.0 CC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3cc(Br)cnc32)CC1 10.1016/S0960-894X(00)80290-5
10177103 171347 0 None 12 2 Rat 8.0 pKi = 8 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
ChEMBL 368 9 1 3 4.5 CN(CCCc1c[nH]cn1)CCC(c1ccc(Cl)cc1)c1ccccn1 10.1016/s0960-894x(03)00357-3
CHEMBL446147 171347 0 None 12 2 Rat 8.0 pKi = 8 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
ChEMBL 368 9 1 3 4.5 CN(CCCc1c[nH]cn1)CCC(c1ccc(Cl)cc1)c1ccccn1 10.1016/s0960-894x(03)00357-3
CHEMBL5291469 194640 0 None 70 2 Human 8.0 pKi = 8 Binding
Antagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysisAntagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysis
ChEMBL 508 8 1 6 3.6 O=C(NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O)C1CCOCC1 10.1021/acsmedchemlett.7b00112
CHEMBL5315702 194640 0 None 70 2 Human 8.0 pKi = 8 Binding
Antagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysisAntagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysis
ChEMBL 508 8 1 6 3.6 O=C(NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O)C1CCOCC1 10.1021/acsmedchemlett.7b00112
2337 3256 77 None 1 62 Human 8.0 pKi = 8 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
50 3256 77 None 1 62 Human 8.0 pKi = 8 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
5002 3256 77 None 1 62 Human 8.0 pKi = 8 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
CHEMBL716 3256 77 None 1 62 Human 8.0 pKi = 8 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
DB01224 3256 77 None 1 62 Human 8.0 pKi = 8 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
14127193 11286 0 None - 1 Guinea pig 8.0 pKi = 8 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 351 6 1 3 4.4 CCN(CC)CC/C=C1/c2ccccc2COc2ccc(C(=O)O)cc21 10.1021/jm00089a020
CHEMBL1179179 11286 0 None - 1 Guinea pig 8.0 pKi = 8 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 351 6 1 3 4.4 CCN(CC)CC/C=C1/c2ccccc2COc2ccc(C(=O)O)cc21 10.1021/jm00089a020
CHEMBL63596 11286 0 None - 1 Guinea pig 8.0 pKi = 8 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 351 6 1 3 4.4 CCN(CC)CC/C=C1/c2ccccc2COc2ccc(C(=O)O)cc21 10.1021/jm00089a020
135398737 958 93 None 2 89 Human 8.0 pKi = 8 Binding
Binding affinity to H1 histamine receptor (unknown origin) by PDSP assayBinding affinity to H1 histamine receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
38 958 93 None 2 89 Human 8.0 pKi = 8 Binding
Binding affinity to H1 histamine receptor (unknown origin) by PDSP assayBinding affinity to H1 histamine receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
722 958 93 None 2 89 Human 8.0 pKi = 8 Binding
Binding affinity to H1 histamine receptor (unknown origin) by PDSP assayBinding affinity to H1 histamine receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
CHEMBL42 958 93 None 2 89 Human 8.0 pKi = 8 Binding
Binding affinity to H1 histamine receptor (unknown origin) by PDSP assayBinding affinity to H1 histamine receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
DB00363 958 93 None 2 89 Human 8.0 pKi = 8 Binding
Binding affinity to H1 histamine receptor (unknown origin) by PDSP assayBinding affinity to H1 histamine receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
135398745 2914 112 None 1 65 Human 8.0 pKi = 8 Binding
Binding affinity to H1 histamine receptor (unknown origin) by PDSP assayBinding affinity to H1 histamine receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
47 2914 112 None 1 65 Human 8.0 pKi = 8 Binding
Binding affinity to H1 histamine receptor (unknown origin) by PDSP assayBinding affinity to H1 histamine receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
CHEMBL715 2914 112 None 1 65 Human 8.0 pKi = 8 Binding
Binding affinity to H1 histamine receptor (unknown origin) by PDSP assayBinding affinity to H1 histamine receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
DB00334 2914 112 None 1 65 Human 8.0 pKi = 8 Binding
Binding affinity to H1 histamine receptor (unknown origin) by PDSP assayBinding affinity to H1 histamine receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
2337 3256 77 None 1 62 Human 8.0 pKi = 8 Binding
Binding affinity to H1 histamine receptor (unknown origin) by PDSP assayBinding affinity to H1 histamine receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
50 3256 77 None 1 62 Human 8.0 pKi = 8 Binding
Binding affinity to H1 histamine receptor (unknown origin) by PDSP assayBinding affinity to H1 histamine receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
5002 3256 77 None 1 62 Human 8.0 pKi = 8 Binding
Binding affinity to H1 histamine receptor (unknown origin) by PDSP assayBinding affinity to H1 histamine receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
CHEMBL716 3256 77 None 1 62 Human 8.0 pKi = 8 Binding
Binding affinity to H1 histamine receptor (unknown origin) by PDSP assayBinding affinity to H1 histamine receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
DB01224 3256 77 None 1 62 Human 8.0 pKi = 8 Binding
Binding affinity to H1 histamine receptor (unknown origin) by PDSP assayBinding affinity to H1 histamine receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
1427 2013 54 None -5 27 Human 8.0 pKi = 8 Binding
Binding affinity to H1 receptor (unknown origin)Binding affinity to H1 receptor (unknown origin)
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1016/j.bmcl.2020.127493
357 2013 54 None -5 27 Human 8.0 pKi = 8 Binding
Binding affinity to H1 receptor (unknown origin)Binding affinity to H1 receptor (unknown origin)
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1016/j.bmcl.2020.127493
3696 2013 54 None -5 27 Human 8.0 pKi = 8 Binding
Binding affinity to H1 receptor (unknown origin)Binding affinity to H1 receptor (unknown origin)
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1016/j.bmcl.2020.127493
CHEMBL11 2013 54 None -5 27 Human 8.0 pKi = 8 Binding
Binding affinity to H1 receptor (unknown origin)Binding affinity to H1 receptor (unknown origin)
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1016/j.bmcl.2020.127493
DB00458 2013 54 None -5 27 Human 8.0 pKi = 8 Binding
Binding affinity to H1 receptor (unknown origin)Binding affinity to H1 receptor (unknown origin)
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1016/j.bmcl.2020.127493
1524 2181 96 None -2 52 Guinea pig 8.0 pKi = 8 Binding
Binding affinity to guinea pig cerebellum homogenate membrane H1 receptor incubated for 30 minsBinding affinity to guinea pig cerebellum homogenate membrane H1 receptor incubated for 30 mins
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/acs.jmedchem.2c00633
197 2181 96 None -2 52 Guinea pig 8.0 pKi = 8 Binding
Binding affinity to guinea pig cerebellum homogenate membrane H1 receptor incubated for 30 minsBinding affinity to guinea pig cerebellum homogenate membrane H1 receptor incubated for 30 mins
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/acs.jmedchem.2c00633
3822 2181 96 None -2 52 Guinea pig 8.0 pKi = 8 Binding
Binding affinity to guinea pig cerebellum homogenate membrane H1 receptor incubated for 30 minsBinding affinity to guinea pig cerebellum homogenate membrane H1 receptor incubated for 30 mins
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/acs.jmedchem.2c00633
88 2181 96 None -2 52 Guinea pig 8.0 pKi = 8 Binding
Binding affinity to guinea pig cerebellum homogenate membrane H1 receptor incubated for 30 minsBinding affinity to guinea pig cerebellum homogenate membrane H1 receptor incubated for 30 mins
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/acs.jmedchem.2c00633
CHEMBL51 2181 96 None -2 52 Guinea pig 8.0 pKi = 8 Binding
Binding affinity to guinea pig cerebellum homogenate membrane H1 receptor incubated for 30 minsBinding affinity to guinea pig cerebellum homogenate membrane H1 receptor incubated for 30 mins
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/acs.jmedchem.2c00633
DB12465 2181 96 None -2 52 Guinea pig 8.0 pKi = 8 Binding
Binding affinity to guinea pig cerebellum homogenate membrane H1 receptor incubated for 30 minsBinding affinity to guinea pig cerebellum homogenate membrane H1 receptor incubated for 30 mins
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/acs.jmedchem.2c00633
69260079 81306 2 None 63 2 Human 8.0 pKi = 8 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 463 6 1 5 4.8 O=C(O)c1cccnc1N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158834 81306 2 None 63 2 Human 8.0 pKi = 8 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 463 6 1 5 4.8 O=C(O)c1cccnc1N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
17867053 99010 0 None 10 3 Rat 8.0 pKi = 8 Binding
Displacement of [3H]- pyrilamine from rat brain membrane Histamine H1 receptorDisplacement of [3H]- pyrilamine from rat brain membrane Histamine H1 receptor
ChEMBL 435 5 0 5 4.3 Cn1c(=O)sc2cc(CCN3CCN(Cc4ccc(Cl)cc4Cl)CC3)ccc21 10.1016/s0960-894x(02)00123-3
CHEMBL280063 99010 0 None 10 3 Rat 8.0 pKi = 8 Binding
Displacement of [3H]- pyrilamine from rat brain membrane Histamine H1 receptorDisplacement of [3H]- pyrilamine from rat brain membrane Histamine H1 receptor
ChEMBL 435 5 0 5 4.3 Cn1c(=O)sc2cc(CCN3CCN(Cc4ccc(Cl)cc4Cl)CC3)ccc21 10.1016/s0960-894x(02)00123-3
59296066 84093 0 None -5 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 487 7 3 5 3.0 Cc1cc(Cl)ccc1OC1CCN(C[C@H](O)CNC(=O)c2c[nH]c(=O)cc2C(F)(F)F)CC1 10.1016/j.bmcl.2012.09.112
CHEMBL2207663 84093 0 None -5 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 487 7 3 5 3.0 Cc1cc(Cl)ccc1OC1CCN(C[C@H](O)CNC(=O)c2c[nH]c(=O)cc2C(F)(F)F)CC1 10.1016/j.bmcl.2012.09.112
59295938 84094 0 None -7 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 521 7 3 5 3.6 Cc1c(Cl)ccc(OC2CCN(C[C@H](O)CNC(=O)c3c[nH]c(=O)cc3C(F)(F)F)CC2)c1Cl 10.1016/j.bmcl.2012.09.112
CHEMBL2207664 84094 0 None -7 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 521 7 3 5 3.6 Cc1c(Cl)ccc(OC2CCN(C[C@H](O)CNC(=O)c3c[nH]c(=O)cc3C(F)(F)F)CC2)c1Cl 10.1016/j.bmcl.2012.09.112
11335419 67100 1 None 11 6 Human 8.0 pKi = 8 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 295 7 0 2 4.1 c1ccc(Cc2ccccc2OCCCN2CCCC2)cc1 10.1021/acs.jmedchem.6b00981
CHEMBL187367 67100 1 None 11 6 Human 8.0 pKi = 8 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 295 7 0 2 4.1 c1ccc(Cc2ccccc2OCCCN2CCCC2)cc1 10.1021/acs.jmedchem.6b00981
15662541 67772 0 None - 1 Guinea pig 8.0 pKi = 8 Binding
Inhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 minInhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 min
ChEMBL 322 2 0 3 4.8 c1ccc2c(c1)Sc1ccccc1N2CC12CCN(CC1)CC2 10.1021/jm00017a019
CHEMBL1908311 67772 0 None - 1 Guinea pig 8.0 pKi = 8 Binding
Inhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 minInhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 min
ChEMBL 322 2 0 3 4.8 c1ccc2c(c1)Sc1ccccc1N2CC12CCN(CC1)CC2 10.1021/jm00017a019
44450154 95836 0 None - 1 Human 8.0 pKi = 8 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 311 4 1 4 2.7 c1ccc([C@@H](Oc2cccc3c2OCC3)[C@H]2CNCCO2)cc1 10.1016/j.bmcl.2008.03.050
CHEMBL258930 95836 0 None - 1 Human 8.0 pKi = 8 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 311 4 1 4 2.7 c1ccc([C@@H](Oc2cccc3c2OCC3)[C@H]2CNCCO2)cc1 10.1016/j.bmcl.2008.03.050
44449768 96023 0 None - 1 Human 8.0 pKi = 8 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 317 5 1 4 2.9 COc1cc(F)ccc1O[C@H](c1ccccc1)[C@H]1CNCCO1 10.1016/j.bmcl.2008.03.050
CHEMBL259765 96023 0 None - 1 Human 8.0 pKi = 8 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 317 5 1 4 2.9 COc1cc(F)ccc1O[C@H](c1ccccc1)[C@H]1CNCCO1 10.1016/j.bmcl.2008.03.050
44450212 96219 0 None - 1 Human 8.0 pKi = 8 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 321 4 1 3 3.6 Fc1ccc(O[C@H](c2ccccc2)[C@H]2CNCCO2)c(Cl)c1 10.1016/j.bmcl.2008.03.050
CHEMBL260823 96219 0 None - 1 Human 8.0 pKi = 8 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 321 4 1 3 3.6 Fc1ccc(O[C@H](c2ccccc2)[C@H]2CNCCO2)c(Cl)c1 10.1016/j.bmcl.2008.03.050
44450181 96743 0 None - 1 Human 8.0 pKi = 8 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 305 4 1 3 3.1 Fc1cccc(O[C@H](c2ccccc2)[C@H]2CNCCO2)c1F 10.1016/j.bmcl.2008.03.050
CHEMBL264418 96743 0 None - 1 Human 8.0 pKi = 8 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 305 4 1 3 3.1 Fc1cccc(O[C@H](c2ccccc2)[C@H]2CNCCO2)c1F 10.1016/j.bmcl.2008.03.050
44450184 155676 0 None - 1 Human 8.0 pKi = 8 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 301 4 1 3 3.2 Cc1cc(F)ccc1O[C@H](c1ccccc1)[C@H]1CNCCO1 10.1016/j.bmcl.2008.03.050
CHEMBL404956 155676 0 None - 1 Human 8.0 pKi = 8 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 301 4 1 3 3.2 Cc1cc(F)ccc1O[C@H](c1ccccc1)[C@H]1CNCCO1 10.1016/j.bmcl.2008.03.050
10458170 116526 0 None - 1 Guinea pig 8.0 pKi = 8 Binding
Inhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptorInhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptor
ChEMBL 487 8 1 4 6.0 O=C(O)Cc1ccc2c(c1)C(SCCN1CCC(Cc3ccccc3)CC1)c1ccccc1CO2 10.1021/jm00055a013
CHEMBL336198 116526 0 None - 1 Guinea pig 8.0 pKi = 8 Binding
Inhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptorInhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptor
ChEMBL 487 8 1 4 6.0 O=C(O)Cc1ccc2c(c1)C(SCCN1CCC(Cc3ccccc3)CC1)c1ccccc1CO2 10.1021/jm00055a013
51039227 57760 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 323 5 0 3 3.5 FC1CCN(CCC2=C(Cc3cnccn3)c3ccccc3C2)C1 10.1016/j.bmcl.2010.12.053
CHEMBL1669417 57760 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 323 5 0 3 3.5 FC1CCN(CCC2=C(Cc3cnccn3)c3ccccc3C2)C1 10.1016/j.bmcl.2010.12.053
22621911 9408 0 None - 1 Rat 7.0 pKi = 7 Binding
Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.
ChEMBL 386 0 0 2 4.9 CC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3cc(Cl)cnc32)CC1 10.1016/S0960-894X(00)80290-5
CHEMBL11159 9408 0 None - 1 Rat 7.0 pKi = 7 Binding
Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.
ChEMBL 386 0 0 2 4.9 CC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3cc(Cl)cnc32)CC1 10.1016/S0960-894X(00)80290-5
242 470 124 None -22 51 Human 7.0 pKi = 7 Binding
Binding affinity to H1 histamine receptor (unknown origin) by PDSP assayBinding affinity to H1 histamine receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
34 470 124 None -22 51 Human 7.0 pKi = 7 Binding
Binding affinity to H1 histamine receptor (unknown origin) by PDSP assayBinding affinity to H1 histamine receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
60795 470 124 None -22 51 Human 7.0 pKi = 7 Binding
Binding affinity to H1 histamine receptor (unknown origin) by PDSP assayBinding affinity to H1 histamine receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
CHEMBL1112 470 124 None -22 51 Human 7.0 pKi = 7 Binding
Binding affinity to H1 histamine receptor (unknown origin) by PDSP assayBinding affinity to H1 histamine receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
DB01238 470 124 None -22 51 Human 7.0 pKi = 7 Binding
Binding affinity to H1 histamine receptor (unknown origin) by PDSP assayBinding affinity to H1 histamine receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
2389 3331 118 None -46 67 Human 7.0 pKi = 7 Binding
Binding affinity to H1 histamine receptor (unknown origin) by PDSP assayBinding affinity to H1 histamine receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
5073 3331 118 None -46 67 Human 7.0 pKi = 7 Binding
Binding affinity to H1 histamine receptor (unknown origin) by PDSP assayBinding affinity to H1 histamine receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
96 3331 118 None -46 67 Human 7.0 pKi = 7 Binding
Binding affinity to H1 histamine receptor (unknown origin) by PDSP assayBinding affinity to H1 histamine receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
CHEMBL85 3331 118 None -46 67 Human 7.0 pKi = 7 Binding
Binding affinity to H1 histamine receptor (unknown origin) by PDSP assayBinding affinity to H1 histamine receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
DB00734 3331 118 None -46 67 Human 7.0 pKi = 7 Binding
Binding affinity to H1 histamine receptor (unknown origin) by PDSP assayBinding affinity to H1 histamine receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
66615705 81267 0 None -19 2 Human 7.0 pKi = 7 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 508 8 1 4 5.4 O=C(O)[C@H](Cc1ccc(F)cc1)N1CCC(CN2CCC(Oc3ccc(Cl)cc3Cl)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158779 81267 0 None -19 2 Human 7.0 pKi = 7 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 508 8 1 4 5.4 O=C(O)[C@H](Cc1ccc(F)cc1)N1CCC(CN2CCC(Oc3ccc(Cl)cc3Cl)CC2)CC1 10.1016/j.bmcl.2012.08.103
71453204 81270 0 None -12 2 Human 7.0 pKi = 7 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 488 8 1 4 5.0 Cc1cc(OC2CCN(CC3CCN([C@@H](Cc4ccc(F)cc4)C(=O)O)CC3)CC2)ccc1Cl 10.1016/j.bmcl.2012.08.103
CHEMBL2158782 81270 0 None -12 2 Human 7.0 pKi = 7 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 488 8 1 4 5.0 Cc1cc(OC2CCN(CC3CCN([C@@H](Cc4ccc(F)cc4)C(=O)O)CC3)CC2)ccc1Cl 10.1016/j.bmcl.2012.08.103
71451392 81274 0 None -31 2 Human 7.0 pKi = 7 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 504 8 1 4 5.6 C[C@](Cc1ccccc1)(C(=O)O)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158786 81274 0 None -31 2 Human 7.0 pKi = 7 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 504 8 1 4 5.6 C[C@](Cc1ccccc1)(C(=O)O)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
68849581 81289 0 None -3 2 Human 7.0 pKi = 7 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 478 7 1 5 4.4 O=C(O)C(c1ccccc1)N1CCO[C@H](CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.08.103
CHEMBL2158818 81289 0 None -3 2 Human 7.0 pKi = 7 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 478 7 1 5 4.4 O=C(O)C(c1ccccc1)N1CCO[C@H](CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.08.103
69347575 81292 0 None -10 2 Human 7.0 pKi = 7 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 476 7 1 4 5.4 O=C(O)[C@@H](c1ccccc1)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158821 81292 0 None -10 2 Human 7.0 pKi = 7 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 476 7 1 4 5.4 O=C(O)[C@@H](c1ccccc1)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
71072034 81308 0 None -3 2 Human 7.0 pKi = 7 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 490 8 1 4 5.2 O=C(O)[C@@H](Cc1ccccc1)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158836 81308 0 None -3 2 Human 7.0 pKi = 7 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 490 8 1 4 5.2 O=C(O)[C@@H](Cc1ccccc1)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
127036932 137348 0 None -3 22 Human 7.0 pKi = 7 Binding
Binding affinity to histamine H1 receptor (unknown origin) by competition binding assayBinding affinity to histamine H1 receptor (unknown origin) by competition binding assay
ChEMBL 274 7 1 1 4.0 C=CCN(CC=C)CCc1c[nH]c2ccc(Cl)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3752900 137348 0 None -3 22 Human 7.0 pKi = 7 Binding
Binding affinity to histamine H1 receptor (unknown origin) by competition binding assayBinding affinity to histamine H1 receptor (unknown origin) by competition binding assay
ChEMBL 274 7 1 1 4.0 C=CCN(CC=C)CCc1c[nH]c2ccc(Cl)cc12 10.1016/j.bmcl.2015.12.053
127036953 137515 0 None -10 22 Human 7.0 pKi = 7 Binding
Binding affinity to histamine H1 receptor (unknown origin) by competition binding assayBinding affinity to histamine H1 receptor (unknown origin) by competition binding assay
ChEMBL 318 7 1 1 4.1 C=CCN(CC=C)CCc1c[nH]c2ccc(Br)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3754166 137515 0 None -10 22 Human 7.0 pKi = 7 Binding
Binding affinity to histamine H1 receptor (unknown origin) by competition binding assayBinding affinity to histamine H1 receptor (unknown origin) by competition binding assay
ChEMBL 318 7 1 1 4.1 C=CCN(CC=C)CCc1c[nH]c2ccc(Br)cc12 10.1016/j.bmcl.2015.12.053
59296085 84209 0 None 2 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 506 8 2 7 3.1 CS(=O)(=O)c1ccc(C(=O)NC[C@@H](O)CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)s1 10.1016/j.bmcl.2012.09.113
CHEMBL2208426 84209 0 None 2 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 506 8 2 7 3.1 CS(=O)(=O)c1ccc(C(=O)NC[C@@H](O)CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)s1 10.1016/j.bmcl.2012.09.113
57397301 67880 0 None -13 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
ChEMBL 560 11 1 6 4.6 COc1ccc(CN(CCN(C)CCN2CCN(C(=O)c3cc4cc(Cl)ccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
CHEMBL1910382 67880 0 None -13 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
ChEMBL 560 11 1 6 4.6 COc1ccc(CN(CCN(C)CCN2CCN(C(=O)c3cc4cc(Cl)ccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
12660328 13406 16 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 241 6 1 2 2.9 CNCCOc1ccccc1Cc1ccccc1 10.1021/acs.jmedchem.6b00981
CHEMBL1192719 13406 16 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 241 6 1 2 2.9 CNCCOc1ccccc1Cc1ccccc1 10.1021/acs.jmedchem.6b00981
CHEMBL3953343 13406 16 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 241 6 1 2 2.9 CNCCOc1ccccc1Cc1ccccc1 10.1021/acs.jmedchem.6b00981
242 470 124 None -23 51 Guinea pig 7.0 pKi = 7 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm070516u
34 470 124 None -23 51 Guinea pig 7.0 pKi = 7 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm070516u
60795 470 124 None -23 51 Guinea pig 7.0 pKi = 7 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm070516u
CHEMBL1112 470 124 None -23 51 Guinea pig 7.0 pKi = 7 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm070516u
DB01238 470 124 None -23 51 Guinea pig 7.0 pKi = 7 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm070516u
23102733 82233 0 None -1 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 511 6 1 5 4.0 O=C(NS(=O)(=O)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1)c1ccccc1 10.1016/j.bmcl.2012.08.124
CHEMBL2171015 82233 0 None -1 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 511 6 1 5 4.0 O=C(NS(=O)(=O)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1)c1ccccc1 10.1016/j.bmcl.2012.08.124
71458869 82241 0 None 2 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 506 7 1 5 4.6 O=C(O)COc1cccc(C(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.124
CHEMBL2171022 82241 0 None 2 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 506 7 1 5 4.6 O=C(O)COc1cccc(C(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.124
11709314 104111 0 None -100 2 Human 6.0 pKi = 6 Binding
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced effect by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced effect by FLIPR assay
ChEMBL 307 5 0 2 4.1 c1ccc(COc2ccc3c(c2)CCN(CC2CC2)CC3)cc1 10.1016/j.bmcl.2013.09.089
CHEMBL3094114 104111 0 None -100 2 Human 6.0 pKi = 6 Binding
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced effect by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced effect by FLIPR assay
ChEMBL 307 5 0 2 4.1 c1ccc(COc2ccc3c(c2)CCN(CC2CC2)CC3)cc1 10.1016/j.bmcl.2013.09.089
10067368 104132 0 None -100 2 Human 6.0 pKi = 6 Binding
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced effect by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced effect by FLIPR assay
ChEMBL 364 6 0 3 4.5 c1ccc(N2CCc3ccc(OCCCN4CCCCC4)cc3CC2)cc1 10.1016/j.bmcl.2013.09.089
CHEMBL3094214 104132 0 None -100 2 Human 6.0 pKi = 6 Binding
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced effect by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced effect by FLIPR assay
ChEMBL 364 6 0 3 4.5 c1ccc(N2CCc3ccc(OCCCN4CCCCC4)cc3CC2)cc1 10.1016/j.bmcl.2013.09.089
10064805 102376 0 None -54 4 Human 6.0 pKi = 6 Binding
Compound was tested for its binding affinity towards human H1 receptorCompound was tested for its binding affinity towards human H1 receptor
ChEMBL 323 4 1 3 4.4 CN1CCCC1CCNc1c2c(nc3ccccc13)CCCCC2 10.1016/s0960-894x(03)00356-1
CHEMBL303824 102376 0 None -54 4 Human 6.0 pKi = 6 Binding
Compound was tested for its binding affinity towards human H1 receptorCompound was tested for its binding affinity towards human H1 receptor
ChEMBL 323 4 1 3 4.4 CN1CCCC1CCNc1c2c(nc3ccccc13)CCCCC2 10.1016/s0960-894x(03)00356-1
33630 178957 99 None -13 28 Human 6.0 pKi = 6 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Pyrilamine from human H1 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL47050 178957 99 None -13 28 Human 6.0 pKi = 6 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Pyrilamine from human H1 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
71454295 84079 0 None -1258 7 Human 6.0 pKi = 6 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis
ChEMBL 536 8 0 6 5.5 COc1ccccc1N1CCN(Cc2cc(CN3CCN(c4ccccc4OC)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207641 84079 0 None -1258 7 Human 6.0 pKi = 6 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis
ChEMBL 536 8 0 6 5.5 COc1ccccc1N1CCN(Cc2cc(CN3CCN(c4ccccc4OC)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
17963199 82270 0 None -1 2 Human 6.0 pKi = 6 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 493 5 1 5 3.7 Cc1ccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(F)c(F)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.124
CHEMBL2171050 82270 0 None -1 2 Human 6.0 pKi = 6 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 493 5 1 5 3.7 Cc1ccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(F)c(F)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.124
25025581 201996 0 None -15 8 Human 6.0 pKi = 6 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 285 4 1 2 3.1 CCOC[C@H]1[C@@H]2CNC[C@@]21c1ccc(Cl)c(Cl)c1 10.1021/jm901818u
CHEMBL608151 201996 0 None -15 8 Human 6.0 pKi = 6 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 285 4 1 2 3.1 CCOC[C@H]1[C@@H]2CNC[C@@]21c1ccc(Cl)c(Cl)c1 10.1021/jm901818u
10060425 54935 0 None -758 2 Guinea pig 5.0 pKi = 5 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 245 5 2 3 2.6 O=C(Nc1ccccc1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL16142 54935 0 None -758 2 Guinea pig 5.0 pKi = 5 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 245 5 2 3 2.6 O=C(Nc1ccccc1)OCCCc1c[nH]cn1 10.1021/jm9507688
14554146 119119 0 None - 1 Rat 5.0 pKi = 5 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 354 0 0 2 3.9 CC(=O)N1CCC(=C2c3cc(F)c(F)cc3CCc3cccnc32)CC1 10.1021/jm00105a069
CHEMBL342747 119119 0 None - 1 Rat 5.0 pKi = 5 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 354 0 0 2 3.9 CC(=O)N1CCC(=C2c3cc(F)c(F)cc3CCc3cccnc32)CC1 10.1021/jm00105a069
44334265 109683 0 None -50 3 Human 5.0 pKi = 5 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 368 8 1 6 2.0 CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)c3cnccn3)C2)cc1 10.1016/s0960-894x(02)00685-6
CHEMBL322695 109683 0 None -50 3 Human 5.0 pKi = 5 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 368 8 1 6 2.0 CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)c3cnccn3)C2)cc1 10.1016/s0960-894x(02)00685-6
44304295 202869 0 None -2290 3 Human 5.0 pKi = 5 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 357 8 1 5 1.5 O=C1C[C@@H](N2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)CC2)N1 10.1016/s0960-894x(02)00310-4
CHEMBL62596 202869 0 None -2290 3 Human 5.0 pKi = 5 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 357 8 1 5 1.5 O=C1C[C@@H](N2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)CC2)N1 10.1016/s0960-894x(02)00310-4
44304331 203121 0 None -2187 3 Human 5.0 pKi = 5 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 449 11 1 5 3.2 N[C@H](CCc1ccccc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL64059 203121 0 None -2187 3 Human 5.0 pKi = 5 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 449 11 1 5 3.2 N[C@H](CCc1ccccc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
44304303 203329 0 None -776 3 Human 5.0 pKi = 5 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 371 8 1 5 1.6 O=C(c1ccc(OCCCN2CCN(C(=O)[C@@H]3CCN3)CC2)cc1)C1CC1 10.1016/s0960-894x(02)00310-4
CHEMBL64896 203329 0 None -776 3 Human 5.0 pKi = 5 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 371 8 1 5 1.6 O=C(c1ccc(OCCCN2CCN(C(=O)[C@@H]3CCN3)CC2)cc1)C1CC1 10.1016/s0960-894x(02)00310-4
26191740 151582 9 None - 1 Human 5.0 pKi = 5 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 267 4 1 2 3.4 c1ccc(Cc2ccc(OC3CCNCC3)cc2)cc1 10.1021/acs.jmedchem.6b00981
CHEMBL3963375 151582 9 None - 1 Human 5.0 pKi = 5 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 267 4 1 2 3.4 c1ccc(Cc2ccc(OC3CCNCC3)cc2)cc1 10.1021/acs.jmedchem.6b00981
11623756 8142 0 None - 1 Human 5.0 pKi = 5 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 310 5 0 3 4.6 CC(c1cccnc1)c1c(CCN(C)C)sc2ccccc12 10.1016/j.bmcl.2010.01.134
CHEMBL1091776 8142 0 None - 1 Human 5.0 pKi = 5 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 310 5 0 3 4.6 CC(c1cccnc1)c1c(CCN(C)C)sc2ccccc12 10.1016/j.bmcl.2010.01.134
10731042 98650 0 None -194 2 Guinea pig 4.0 pKi = 4 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 274 6 3 4 1.9 Nc1ccc(CNC(=O)OCCCc2c[nH]cn2)cc1 10.1021/jm9507688
CHEMBL277285 98650 0 None -194 2 Guinea pig 4.0 pKi = 4 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 274 6 3 4 1.9 Nc1ccc(CNC(=O)OCCCc2c[nH]cn2)cc1 10.1021/jm9507688
44304311 200293 0 None -17378 3 Human 4.0 pKi = 4 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 442 10 1 7 2.2 N[C@H](Cc1nccs1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL59733 200293 0 None -17378 3 Human 4.0 pKi = 4 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 442 10 1 7 2.2 N[C@H](Cc1nccs1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
44304067 201283 0 None -43651 3 Human 4.0 pKi = 4 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 359 9 1 5 1.4 CNCC(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL60401 201283 0 None -43651 3 Human 4.0 pKi = 4 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 359 9 1 5 1.4 CNCC(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
44334521 107836 0 None -85 3 Human 4.0 pKi = 4 Binding
Binding affinity towards human Histamine H1 receptor (For compound 11)Binding affinity towards human Histamine H1 receptor (For compound 11)
ChEMBL 262 6 1 4 1.7 CC(=O)c1ccc(OCCCN2CC[C@H](N)C2)cc1 10.1016/s0960-894x(02)00685-6
CHEMBL319231 107836 0 None -85 3 Human 4.0 pKi = 4 Binding
Binding affinity towards human Histamine H1 receptor (For compound 11)Binding affinity towards human Histamine H1 receptor (For compound 11)
ChEMBL 262 6 1 4 1.7 CC(=O)c1ccc(OCCCN2CC[C@H](N)C2)cc1 10.1016/s0960-894x(02)00685-6
118709751 113541 0 None -776 10 Human 6.0 pKi = 6 Binding
Displacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation countingDisplacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1ccccc1F 10.1016/j.bmcl.2014.07.018
CHEMBL3321792 113541 0 None -776 10 Human 6.0 pKi = 6 Binding
Displacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation countingDisplacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1ccccc1F 10.1016/j.bmcl.2014.07.018
46882664 5717 0 None -2 5 Human 6.0 pKi = 6.0 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 494 8 2 8 3.6 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)c(S(N)(=O)=O)cc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
CHEMBL1078240 5717 0 None -2 5 Human 6.0 pKi = 6.0 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 494 8 2 8 3.6 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)c(S(N)(=O)=O)cc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
11545813 181194 0 None -24 7 Human 6.0 pKi = 6.0 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 400 6 0 3 5.2 O=C(CCCN1C2CCC1CN(c1ccc(Cl)cc1)CC2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL476109 181194 0 None -24 7 Human 6.0 pKi = 6.0 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 400 6 0 3 5.2 O=C(CCCN1C2CCC1CN(c1ccc(Cl)cc1)CC2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
168284748 191648 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 742 19 6 8 1.7 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5196026 191648 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 742 19 6 8 1.7 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
44304308 102485 0 None -40 3 Human 6.0 pKi = 6.0 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 432 8 0 5 3.7 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3cccc(F)c3F)cc2)CC1 10.1016/s0960-894x(02)00309-8
CHEMBL304027 102485 0 None -40 3 Human 6.0 pKi = 6.0 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 432 8 0 5 3.7 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3cccc(F)c3F)cc2)CC1 10.1016/s0960-894x(02)00309-8
168284748 191648 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 742 19 6 8 1.7 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5196026 191648 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 742 19 6 8 1.7 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
44304357 200610 0 None -851 3 Human 5.0 pKi = 5.0 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 415 9 1 5 3.0 CC(C)(C)C[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL59931 200610 0 None -851 3 Human 5.0 pKi = 5.0 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 415 9 1 5 3.0 CC(C)(C)C[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
164614907 184584 0 None -323 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 378 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(F)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4848697 184584 0 None -323 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 378 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(F)cc1 10.1016/j.ejmech.2021.113190
44267109 7171 0 None - 1 Rat 6.0 pKi = 6.0 Binding
Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.
ChEMBL 366 0 0 2 4.6 CC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3ccc(C)nc32)CC1 10.1016/S0960-894X(00)80290-5
CHEMBL10855 7171 0 None - 1 Rat 6.0 pKi = 6.0 Binding
Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.
ChEMBL 366 0 0 2 4.6 CC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3ccc(C)nc32)CC1 10.1016/S0960-894X(00)80290-5
21830793 91835 10 None -6760 45 Human 6.0 pKi = 6.0 Binding
Binding affinity to histamine H1 receptor (unknown origin)Binding affinity to histamine H1 receptor (unknown origin)
ChEMBL 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 10.1016/j.bmc.2013.05.050
CHEMBL2413154 91835 10 None -6760 45 Human 6.0 pKi = 6.0 Binding
Binding affinity to histamine H1 receptor (unknown origin)Binding affinity to histamine H1 receptor (unknown origin)
ChEMBL 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 10.1016/j.bmc.2013.05.050
44304246 202651 0 None -12 3 Human 7.0 pKi = 7.0 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 426 11 0 5 4.6 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3occc3C)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL61396 202651 0 None -12 3 Human 7.0 pKi = 7.0 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 426 11 0 5 4.6 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3occc3C)CC2)cc1 10.1016/s0960-894x(02)00309-8
44304310 203274 0 None -141 3 Human 6.0 pKi = 6.0 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 415 10 0 4 4.1 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)N3CCCC3)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL64667 203274 0 None -141 3 Human 6.0 pKi = 6.0 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 415 10 0 4 4.1 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)N3CCCC3)CC2)cc1 10.1016/s0960-894x(02)00309-8
168281746 192882 0 None -14454 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 365 6 4 5 1.6 CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5184911 192882 0 None -14454 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 365 6 4 5 1.6 CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5221974 192882 0 None -14454 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 365 6 4 5 1.6 CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1 10.1021/acs.jmedchem.1c00692
71712245 110310 0 None -43651 2 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 377 7 0 6 3.9 Cc1nnc(-c2cccnc2)n1-c1ccc(OCCCN2CCCCC2)cc1 10.1016/j.ejmech.2014.03.014
CHEMBL3238445 110310 0 None -43651 2 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 377 7 0 6 3.9 Cc1nnc(-c2cccnc2)n1-c1ccc(OCCCN2CCCCC2)cc1 10.1016/j.ejmech.2014.03.014
56835171 69740 0 None -645 9 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]histamine from human H1 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H1 receptor expressed in HEK cell membranes
ChEMBL 295 2 2 6 1.9 Nc1nc(N2CCNCC2)c2ccc(-c3ccco3)cc2n1 10.1016/j.bmcl.2011.10.104
CHEMBL1935574 69740 0 None -645 9 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]histamine from human H1 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H1 receptor expressed in HEK cell membranes
ChEMBL 295 2 2 6 1.9 Nc1nc(N2CCNCC2)c2ccc(-c3ccco3)cc2n1 10.1016/j.bmcl.2011.10.104
132060752 162926 0 None -3 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-Pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 437 7 0 6 3.4 CCOC(=O)CCN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)C3)CC1 10.1016/j.ejmech.2018.02.024
CHEMBL4174189 162926 0 None -3 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-Pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 437 7 0 6 3.4 CCOC(=O)CCN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)C3)CC1 10.1016/j.ejmech.2018.02.024
44304457 203213 0 None -354 3 Human 6.0 pKi = 6.0 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 376 10 0 5 3.6 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OC)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL64408 203213 0 None -354 3 Human 6.0 pKi = 6.0 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 376 10 0 5 3.6 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OC)CC2)cc1 10.1016/s0960-894x(02)00309-8
127026017 137358 0 None 12 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 415 5 1 6 3.6 COc1ccc(CNc2nc3c(c(N4CCN(C)CC4)n2)-c2ccccc2CC3)cc1 10.1016/j.bmcl.2015.12.035
CHEMBL3752972 137358 0 None 12 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 415 5 1 6 3.6 COc1ccc(CNc2nc3c(c(N4CCN(C)CC4)n2)-c2ccccc2CC3)cc1 10.1016/j.bmcl.2015.12.035
12192007 168408 44 None -407 3 Human 5.0 pKi = 5.0 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 191 2 2 2 0.8 N[C@@H](C(=O)O)C1Cc2ccccc2C1 10.1016/s0960-894x(02)00310-4
CHEMBL434785 168408 44 None -407 3 Human 5.0 pKi = 5.0 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 191 2 2 2 0.8 N[C@@H](C(=O)O)C1Cc2ccccc2C1 10.1016/s0960-894x(02)00310-4
168275750 192826 0 None -72 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 332 6 3 4 1.6 Cc1nnc(CCCN/C(N)=N/C(=O)NCc2ccccc2)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5175558 192826 0 None -72 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 332 6 3 4 1.6 Cc1nnc(CCCN/C(N)=N/C(=O)NCc2ccccc2)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221581 192826 0 None -72 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 332 6 3 4 1.6 Cc1nnc(CCCN/C(N)=N/C(=O)NCc2ccccc2)s1 10.1021/acs.jmedchem.1c00692
867637 55187 4 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 291 5 1 4 3.0 C=CCn1c(=N)n(CC(=O)c2ccccc2)c2ccccc21 10.1021/jm2011589
CHEMBL1617548 55187 4 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 291 5 1 4 3.0 C=CCn1c(=N)n(CC(=O)c2ccccc2)c2ccccc21 10.1021/jm2011589
164612037 185377 0 None -204173 20 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
CHEMBL4860528 185377 0 None -204173 20 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
44288874 101095 0 None -107 7 Human 7.0 pKi = 7.0 Binding
Selectivity screen against human Histamine H1 receptorSelectivity screen against human Histamine H1 receptor
ChEMBL 528 7 2 4 4.2 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3F)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1 10.1016/s0960-894x(99)00696-4
CHEMBL295001 101095 0 None -107 7 Human 7.0 pKi = 7.0 Binding
Selectivity screen against human Histamine H1 receptorSelectivity screen against human Histamine H1 receptor
ChEMBL 528 7 2 4 4.2 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3F)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1 10.1016/s0960-894x(99)00696-4
168287539 191559 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity to H1 receptor (unknown origin)Binding affinity to H1 receptor (unknown origin)
ChEMBL 392 7 2 4 3.7 CCOc1ccc(F)cc1NC(=O)c1cc(C)ccc1NS(=O)(=O)C1CC1 10.1021/acsmedchemlett.2c00100
CHEMBL5194692 191559 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity to H1 receptor (unknown origin)Binding affinity to H1 receptor (unknown origin)
ChEMBL 392 7 2 4 3.7 CCOc1ccc(F)cc1NC(=O)c1cc(C)ccc1NS(=O)(=O)C1CC1 10.1021/acsmedchemlett.2c00100
53326724 57753 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 332 7 0 4 3.8 C[C@H](C1=C(CCN(C)CCC#N)Cc2ccccc21)c1cnccn1 10.1016/j.bmcl.2010.12.053
CHEMBL1669410 57753 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 332 7 0 4 3.8 C[C@H](C1=C(CCN(C)CCC#N)Cc2ccccc21)c1cnccn1 10.1016/j.bmcl.2010.12.053
23381046 66754 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human histamine H1 receptor expressed in CHO-K1 cellsBinding affinity towards human histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 548 10 2 5 4.7 NC(=O)N(O)CCC#Cc1ccc(OCCCN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2004.08.060
CHEMBL185825 66754 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human histamine H1 receptor expressed in CHO-K1 cellsBinding affinity towards human histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 548 10 2 5 4.7 NC(=O)N(O)CCC#Cc1ccc(OCCCN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2004.08.060
168269382 189920 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 818 21 6 8 3.1 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5169902 189920 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 818 21 6 8 3.1 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
44304438 203168 0 None -100 3 Human 6.0 pKi = 6.0 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 420 13 0 5 4.1 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)CSCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL64235 203168 0 None -100 3 Human 6.0 pKi = 6.0 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 420 13 0 5 4.1 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)CSCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
3570228 69033 67 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 213 4 1 2 3.0 NCCc1ccccc1Oc1ccccc1 10.1021/jm2011589
CHEMBL1923535 69033 67 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 213 4 1 2 3.0 NCCc1ccccc1Oc1ccccc1 10.1021/jm2011589
141485890 173280 0 None - 1 Guinea pig 6.0 pKi = 6.0 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysisDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysis
ChEMBL 331 6 0 4 1.7 CCN1CCN(CCCOc2ccc3c(c2)C(=O)N(C)CC3)CC1 10.1016/j.bmcl.2019.04.015
CHEMBL4525456 173280 0 None - 1 Guinea pig 6.0 pKi = 6.0 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysisDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysis
ChEMBL 331 6 0 4 1.7 CCN1CCN(CCCOc2ccc3c(c2)C(=O)N(C)CC3)CC1 10.1016/j.bmcl.2019.04.015
2337 3256 77 None 1 62 Human 8.0 pKi = 8.0 Binding
Binding affinity to H1 histamine receptor (unknown origin)Binding affinity to H1 histamine receptor (unknown origin)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmcl.2020.127681
50 3256 77 None 1 62 Human 8.0 pKi = 8.0 Binding
Binding affinity to H1 histamine receptor (unknown origin)Binding affinity to H1 histamine receptor (unknown origin)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmcl.2020.127681
5002 3256 77 None 1 62 Human 8.0 pKi = 8.0 Binding
Binding affinity to H1 histamine receptor (unknown origin)Binding affinity to H1 histamine receptor (unknown origin)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmcl.2020.127681
CHEMBL716 3256 77 None 1 62 Human 8.0 pKi = 8.0 Binding
Binding affinity to H1 histamine receptor (unknown origin)Binding affinity to H1 histamine receptor (unknown origin)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmcl.2020.127681
DB01224 3256 77 None 1 62 Human 8.0 pKi = 8.0 Binding
Binding affinity to H1 histamine receptor (unknown origin)Binding affinity to H1 histamine receptor (unknown origin)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmcl.2020.127681
15749427 102059 0 None 1 2 Human 8.0 pKi = 8.0 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 323 4 1 3 3.2 CN(C)C/C=C1\c2ccccc2COc2ccc(CC(=O)O)cc21 10.1021/jm300682j
CHEMBL302005 102059 0 None 1 2 Human 8.0 pKi = 8.0 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 323 4 1 3 3.2 CN(C)C/C=C1\c2ccccc2COc2ccc(CC(=O)O)cc21 10.1021/jm300682j
191 403 98 None -56 29 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
201 403 98 None -56 29 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
2170 403 98 None -56 29 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
CHEMBL1113 403 98 None -56 29 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
DB00543 403 98 None -56 29 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
11544156 194901 0 None -123 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation counting
ChEMBL 313 5 0 2 4.7 CN(C)CCc1sc2ccccc2c1Cc1ccc(F)cc1 10.1021/jm900933k
CHEMBL540982 194901 0 None -123 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation counting
ChEMBL 313 5 0 2 4.7 CN(C)CCc1sc2ccccc2c1Cc1ccc(F)cc1 10.1021/jm900933k
15749427 102059 0 None 1 2 Human 8.0 pKi = 8.0 Binding
Inhibition constant against histamine H1 receptorInhibition constant against histamine H1 receptor
ChEMBL 323 4 1 3 3.2 CN(C)C/C=C1\c2ccccc2COc2ccc(CC(=O)O)cc21 10.1021/jm058225d
CHEMBL302005 102059 0 None 1 2 Human 8.0 pKi = 8.0 Binding
Inhibition constant against histamine H1 receptorInhibition constant against histamine H1 receptor
ChEMBL 323 4 1 3 3.2 CN(C)C/C=C1\c2ccccc2COc2ccc(CC(=O)O)cc21 10.1021/jm058225d
15749427 102059 0 None -1 2 Guinea pig 8.0 pKi = 8.0 Binding
Inhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptorInhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptor
ChEMBL 323 4 1 3 3.2 CN(C)C/C=C1\c2ccccc2COc2ccc(CC(=O)O)cc21 10.1021/jm00055a013
CHEMBL302005 102059 0 None -1 2 Guinea pig 8.0 pKi = 8.0 Binding
Inhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptorInhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptor
ChEMBL 323 4 1 3 3.2 CN(C)C/C=C1\c2ccccc2COc2ccc(CC(=O)O)cc21 10.1021/jm00055a013
15749427 102059 0 None -1 2 Guinea pig 8.0 pKi = 8.0 Binding
The compound was tested in vitro for binding affinity against histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMThe compound was tested in vitro for binding affinity against histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 323 4 1 3 3.2 CN(C)C/C=C1\c2ccccc2COc2ccc(CC(=O)O)cc21 10.1021/jm00089a020
CHEMBL302005 102059 0 None -1 2 Guinea pig 8.0 pKi = 8.0 Binding
The compound was tested in vitro for binding affinity against histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMThe compound was tested in vitro for binding affinity against histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 323 4 1 3 3.2 CN(C)C/C=C1\c2ccccc2COc2ccc(CC(=O)O)cc21 10.1021/jm00089a020
46884668 8289 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 293 5 0 3 3.3 Cc1ccc2c(c1)CC(CCN(C)C)=C2Cc1cnccn1 10.1016/j.bmcl.2010.02.055
CHEMBL1092600 8289 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 293 5 0 3 3.3 Cc1ccc2c(c1)CC(CCN(C)C)=C2Cc1cnccn1 10.1016/j.bmcl.2010.02.055
24769156 116217 0 None -181 4 Human 7.0 pKi = 7.0 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 388 7 1 4 3.6 O=C(NCCCCN1CCN(c2ccccc2)CC1)c1ccc2ncccc2c1 10.1021/jm501119j
CHEMBL3358509 116217 0 None -181 4 Human 7.0 pKi = 7.0 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 388 7 1 4 3.6 O=C(NCCCCN1CCN(c2ccccc2)CC1)c1ccc2ncccc2c1 10.1021/jm501119j
168269382 189920 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 818 21 6 8 3.1 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5169902 189920 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 818 21 6 8 3.1 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
16006492 97469 7 None -275 6 Human 6.0 pKi = 6.0 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 195 0 2 3 2.0 CC1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.080
CHEMBL270177 97469 7 None -275 6 Human 6.0 pKi = 6.0 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 195 0 2 3 2.0 CC1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.080
44334037 4446 0 None -199 3 Human 5.0 pKi = 5.0 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 450 9 1 7 3.7 CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)c3csc(-c4cccnc4)n3)C2)cc1 10.1016/s0960-894x(02)00685-6
CHEMBL101634 4446 0 None -199 3 Human 5.0 pKi = 5.0 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 450 9 1 7 3.7 CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)c3csc(-c4cccnc4)n3)C2)cc1 10.1016/s0960-894x(02)00685-6
95339350 162882 1 None 3 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 277 4 0 4 1.9 COC[C@@H](C)N1CCN(c2cccc(F)c2C#N)CC1 10.1021/acs.jmedchem.8b00718
CHEMBL4173442 162882 1 None 3 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 277 4 0 4 1.9 COC[C@@H](C)N1CCN(c2cccc(F)c2C#N)CC1 10.1021/acs.jmedchem.8b00718
141485895 175197 0 None - 1 Guinea pig 7.0 pKi = 7.0 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysisDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysis
ChEMBL 304 5 1 4 1.2 CN1CCc2ccc(OCCCN3CCC(O)C3)cc2C1=O 10.1016/j.bmcl.2019.04.015
CHEMBL4570965 175197 0 None - 1 Guinea pig 7.0 pKi = 7.0 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysisDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysis
ChEMBL 304 5 1 4 1.2 CN1CCc2ccc(OCCCN3CCC(O)C3)cc2C1=O 10.1016/j.bmcl.2019.04.015
112936251 137266 1 None -1 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 359 5 1 5 3.5 CN1CCN(c2cc(-c3ccccc3)nc(NCc3ccccc3)n2)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3752085 137266 1 None -1 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 359 5 1 5 3.5 CN1CCN(c2cc(-c3ccccc3)nc(NCc3ccccc3)n2)CC1 10.1016/j.bmcl.2015.12.035
44304991 203061 0 None -891 3 Human 5.0 pKi = 5.0 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 424 12 0 5 3.6 CCCCCC(=O)c1ccc(OCCCN2CCN(S(=O)(=O)C(C)C)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL63631 203061 0 None -891 3 Human 5.0 pKi = 5.0 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 424 12 0 5 3.6 CCCCCC(=O)c1ccc(OCCCN2CCN(S(=O)(=O)C(C)C)CC2)cc1 10.1016/s0960-894x(02)00309-8
71525679 89726 0 None -794 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]histamine from human histamine H1 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H1 receptor expressed in HEK cells
ChEMBL 272 3 2 6 1.0 CCc1cnc2c(N3CC[C@@H](NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
CHEMBL2376801 89726 0 None -794 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]histamine from human histamine H1 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H1 receptor expressed in HEK cells
ChEMBL 272 3 2 6 1.0 CCc1cnc2c(N3CC[C@@H](NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
57334553 90475 0 None -3715 13 Guinea pig 6.0 pKi = 6.0 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysisDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysis
ChEMBL 484 7 0 6 6.1 Cc1cc(=O)oc2c(Cl)c(OCCCCN3CCC(c4noc5cc(F)ccc45)CC3)ccc12 10.1021/jm400408r
CHEMBL2387229 90475 0 None -3715 13 Guinea pig 6.0 pKi = 6.0 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysisDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysis
ChEMBL 484 7 0 6 6.1 Cc1cc(=O)oc2c(Cl)c(OCCCCN3CCC(c4noc5cc(F)ccc45)CC3)ccc12 10.1021/jm400408r
44324800 206948 0 None -371 7 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]pyrilamine binding to Histamine H1 receptorInhibition of [3H]pyrilamine binding to Histamine H1 receptor
ChEMBL 463 7 0 7 3.5 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4ccccc4)CC3)[C@@H]1CO2 10.1021/jm049619s
CHEMBL91157 206948 0 None -371 7 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]pyrilamine binding to Histamine H1 receptorInhibition of [3H]pyrilamine binding to Histamine H1 receptor
ChEMBL 463 7 0 7 3.5 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4ccccc4)CC3)[C@@H]1CO2 10.1021/jm049619s
94496003 162865 1 None -20 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 331 5 1 5 2.8 C[C@H](CNc1cncc(Cl)n1)N1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00718
CHEMBL4173176 162865 1 None -20 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 331 5 1 5 2.8 C[C@H](CNc1cncc(Cl)n1)N1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00718
5048 3133 64 None -109 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1016/j.ejmech.2014.03.014
8924 3133 64 None -109 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1016/j.ejmech.2014.03.014
9948102 3133 64 None -109 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1016/j.ejmech.2014.03.014
CHEMBL462605 3133 64 None -109 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1016/j.ejmech.2014.03.014
DB11642 3133 64 None -109 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1016/j.ejmech.2014.03.014
21533446 70155 0 None -30 10 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation countingDisplacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation counting
ChEMBL 379 6 1 3 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
CHEMBL1940403 70155 0 None -30 10 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation countingDisplacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation counting
ChEMBL 379 6 1 3 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
44267115 9903 0 None - 1 Rat 5.9 pKi = 5.9 Binding
Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.
ChEMBL 394 1 0 3 4.5 CC(=O)c1cnc2c(c1)CCc1cc(Cl)ccc1C2=C1CCN(C(C)=O)CC1 10.1016/S0960-894X(00)80290-5
CHEMBL11435 9903 0 None - 1 Rat 5.9 pKi = 5.9 Binding
Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.
ChEMBL 394 1 0 3 4.5 CC(=O)c1cnc2c(c1)CCc1cc(Cl)ccc1C2=C1CCN(C(C)=O)CC1 10.1016/S0960-894X(00)80290-5
107782 14468 18 None 1 5 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O nan
67151996 14468 18 None 1 5 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O nan
CHEMBL1201207 14468 18 None 1 5 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O nan
127026019 137460 0 None 6 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 378 2 0 6 1.7 CN1CCN(c2nc3c(c(N4CCN(C)CC4)n2)-c2ccccc2CC3)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3753705 137460 0 None 6 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 378 2 0 6 1.7 CN1CCN(c2nc3c(c(N4CCN(C)CC4)n2)-c2ccccc2CC3)CC1 10.1016/j.bmcl.2015.12.035
168276112 190272 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 790 19 6 8 3.2 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5175594 190272 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 790 19 6 8 3.2 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
168276112 190272 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 790 19 6 8 3.2 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5175594 190272 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 790 19 6 8 3.2 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
45815848 162304 5 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 330 4 0 5 3.2 CC(C)(C)c1nc(CN2CCN(Cc3ccccn3)CC2)cs1 10.1021/acs.jmedchem.8b00718
CHEMBL4164366 162304 5 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 330 4 0 5 3.2 CC(C)(C)c1nc(CN2CCN(Cc3ccccn3)CC2)cs1 10.1021/acs.jmedchem.8b00718
46884600 7719 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 293 5 0 3 3.3 Cc1cncc(CC2=C(CCN(C)C)Cc3ccccc32)n1 10.1016/j.bmcl.2010.02.055
CHEMBL1088882 7719 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 293 5 0 3 3.3 Cc1cncc(CC2=C(CCN(C)C)Cc3ccccc32)n1 10.1016/j.bmcl.2010.02.055
11277528 170102 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for H1 histamine receptor expressed in CHO cellsBinding affinity for H1 histamine receptor expressed in CHO cells
ChEMBL 282 0 1 5 1.6 Cn1ccc2c1C(=O)Cn1ccnc1C2=C1CCNCC1 10.1021/jm049495j
CHEMBL444353 170102 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for H1 histamine receptor expressed in CHO cellsBinding affinity for H1 histamine receptor expressed in CHO cells
ChEMBL 282 0 1 5 1.6 Cn1ccc2c1C(=O)Cn1ccnc1C2=C1CCNCC1 10.1021/jm049495j
15749426 11284 0 None - 1 Guinea pig 7.9 pKi = 7.9 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 309 3 1 3 3.3 CN(C)C/C=C1\c2ccccc2COc2ccc(C(=O)O)cc21 10.1021/jm00089a020
CHEMBL1179173 11284 0 None - 1 Guinea pig 7.9 pKi = 7.9 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 309 3 1 3 3.3 CN(C)C/C=C1\c2ccccc2COc2ccc(C(=O)O)cc21 10.1021/jm00089a020
CHEMBL63424 11284 0 None - 1 Guinea pig 7.9 pKi = 7.9 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 309 3 1 3 3.3 CN(C)C/C=C1\c2ccccc2COc2ccc(C(=O)O)cc21 10.1021/jm00089a020
6603950 203324 9 None -19 8 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cellsDisplacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 344 1 0 3 4.3 CN1CCN([C@@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm100652h
CHEMBL64875 203324 9 None -19 8 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cellsDisplacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 344 1 0 3 4.3 CN1CCN([C@@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm100652h
11580426 7944 3 None 117 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 310 5 0 3 4.6 CC(c1ccccn1)c1c(CCN(C)C)sc2ccccc12 10.1016/j.bmcl.2010.01.134
CHEMBL1090432 7944 3 None 117 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 310 5 0 3 4.6 CC(c1ccccn1)c1c(CCN(C)C)sc2ccccc12 10.1016/j.bmcl.2010.01.134
10028980 24697 0 None - 1 Guinea pig 7.9 pKi = 7.9 Binding
Inhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptorInhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptor
ChEMBL 501 9 1 4 6.4 O=C(O)CCc1ccc2c(c1)C(SCCN1CCC(Cc3ccccc3)CC1)c1ccccc1CO2 10.1021/jm00055a013
CHEMBL134377 24697 0 None - 1 Guinea pig 7.9 pKi = 7.9 Binding
Inhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptorInhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptor
ChEMBL 501 9 1 4 6.4 O=C(O)CCc1ccc2c(c1)C(SCCN1CCC(Cc3ccccc3)CC1)c1ccccc1CO2 10.1021/jm00055a013
135398737 958 93 None -2 89 Guinea pig 7.9 pKi = 7.9 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates after 60 mins by liquid scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates after 60 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2015.09.045
38 958 93 None -2 89 Guinea pig 7.9 pKi = 7.9 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates after 60 mins by liquid scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates after 60 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2015.09.045
722 958 93 None -2 89 Guinea pig 7.9 pKi = 7.9 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates after 60 mins by liquid scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates after 60 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2015.09.045
CHEMBL42 958 93 None -2 89 Guinea pig 7.9 pKi = 7.9 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates after 60 mins by liquid scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates after 60 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2015.09.045
DB00363 958 93 None -2 89 Guinea pig 7.9 pKi = 7.9 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates after 60 mins by liquid scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates after 60 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2015.09.045
49836410 18735 0 None 3 4 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]pyrilamine from histamine H1 receptor in Sprague-Dawley rat cortical membrane by liquid scintillation countingDisplacement of [3H]pyrilamine from histamine H1 receptor in Sprague-Dawley rat cortical membrane by liquid scintillation counting
ChEMBL 393 2 1 2 4.5 O=C(O)C1(F)CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)CC1 10.1021/jm100856p
CHEMBL1277678 18735 0 None 3 4 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]pyrilamine from histamine H1 receptor in Sprague-Dawley rat cortical membrane by liquid scintillation countingDisplacement of [3H]pyrilamine from histamine H1 receptor in Sprague-Dawley rat cortical membrane by liquid scintillation counting
ChEMBL 393 2 1 2 4.5 O=C(O)C1(F)CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)CC1 10.1021/jm100856p
11437142 202606 2 None - 1 Guinea pig 7.9 pKi = 7.9 Binding
Inhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranesInhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 269 6 0 2 3.7 Cc1ccc([C@@H](OCCN(C)C)c2ccccc2)cc1 10.1021/jm00017a019
CHEMBL612084 202606 2 None - 1 Guinea pig 7.9 pKi = 7.9 Binding
Inhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranesInhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes
ChEMBL 269 6 0 2 3.7 Cc1ccc([C@@H](OCCN(C)C)c2ccccc2)cc1 10.1021/jm00017a019
11097588 202138 2 None - 1 Guinea pig 7.9 pKi = 7.9 Binding
Inhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 minInhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 min
ChEMBL 269 6 0 2 3.7 Cc1ccc([C@H](OCCN(C)C)c2ccccc2)cc1 10.1021/jm00017a019
CHEMBL609131 202138 2 None - 1 Guinea pig 7.9 pKi = 7.9 Binding
Inhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 minInhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 min
ChEMBL 269 6 0 2 3.7 Cc1ccc([C@H](OCCN(C)C)c2ccccc2)cc1 10.1021/jm00017a019
16202149 80633 1 None 3 2 Human 7.9 pKi = 7.9 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 556 10 1 4 6.8 CC1(C)CCCN(CCCOc2ccc(C3CCN(C(=O)c4ccc(CCC(=O)O)c5ccccc45)CC3)cc2)C1 10.1021/jm100064d
CHEMBL2151156 80633 1 None 3 2 Human 7.9 pKi = 7.9 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 556 10 1 4 6.8 CC1(C)CCCN(CCCOc2ccc(C3CCN(C(=O)c4ccc(CCC(=O)O)c5ccccc45)CC3)cc2)C1 10.1021/jm100064d
71450777 84203 0 None 63 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 404 7 0 4 5.2 N#Cc1cccc(OCCCN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)c1 10.1016/j.bmcl.2012.09.113
CHEMBL2208420 84203 0 None 63 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 404 7 0 4 5.2 N#Cc1cccc(OCCCN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)c1 10.1016/j.bmcl.2012.09.113
59295926 84218 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 474 7 2 6 3.6 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1cnnc2ccccc12 10.1016/j.bmcl.2012.09.113
CHEMBL2208435 84218 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 474 7 2 6 3.6 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1cnnc2ccccc12 10.1016/j.bmcl.2012.09.113
59295984 84011 0 None -3 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 487 7 3 5 3.3 Cc1cc(Cl)ccc1OC1CCN(C[C@H](O)CNC(=O)c2c[nH]c(=O)c3cc(F)ccc23)CC1 10.1016/j.bmcl.2012.09.112
CHEMBL2207279 84011 0 None -3 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 487 7 3 5 3.3 Cc1cc(Cl)ccc1OC1CCN(C[C@H](O)CNC(=O)c2c[nH]c(=O)c3cc(F)ccc23)CC1 10.1016/j.bmcl.2012.09.112
59296033 84018 0 None -15 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 596 9 3 7 2.7 CN(C)S(=O)(=O)c1ccc2c(C(=O)NC[C@@H](O)CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)c[nH]c(=O)c2c1 10.1016/j.bmcl.2012.09.112
CHEMBL2207286 84018 0 None -15 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 596 9 3 7 2.7 CN(C)S(=O)(=O)c1ccc2c(C(=O)NC[C@@H](O)CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)c[nH]c(=O)c2c1 10.1016/j.bmcl.2012.09.112
71459762 84091 0 None -7 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 452 8 3 5 3.2 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]nc1C1CC1 10.1016/j.bmcl.2012.09.112
CHEMBL2207661 84091 0 None -7 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 452 8 3 5 3.2 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]nc1C1CC1 10.1016/j.bmcl.2012.09.112
7077 66959 27 None 3 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 10.1021/acs.jmedchem.6b00981
CHEMBL186720 66959 27 None 3 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 10.1021/acs.jmedchem.6b00981
CHEMBL3925724 66959 27 None 3 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 10.1021/acs.jmedchem.6b00981
3359700 143095 2 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 309 7 0 2 4.5 c1ccc(Cc2ccccc2OCCCN2CCCCC2)cc1 10.1021/acs.jmedchem.6b00981
CHEMBL3895427 143095 2 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 309 7 0 2 4.5 c1ccc(Cc2ccccc2OCCCN2CCCCC2)cc1 10.1021/acs.jmedchem.6b00981
11742610 207029 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 415 2 0 3 5.6 Cc1ccncc1CN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/acs.jmedchem.9b00447
CHEMBL91565 207029 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 415 2 0 3 5.6 Cc1ccncc1CN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/acs.jmedchem.9b00447
144950987 179970 0 None 95 6 Human 6.9 pKi = 6.9 Binding
Binding affinity to H1 receptor (unknown origin)Binding affinity to H1 receptor (unknown origin)
ChEMBL 292 3 0 2 3.4 CN(C)CCN1C(=O)c2ccccc2/C=C\c2ccccc21 10.1016/j.bmcl.2020.127493
CHEMBL4746800 179970 0 None 95 6 Human 6.9 pKi = 6.9 Binding
Binding affinity to H1 receptor (unknown origin)Binding affinity to H1 receptor (unknown origin)
ChEMBL 292 3 0 2 3.4 CN(C)CCN1C(=O)c2ccccc2/C=C\c2ccccc21 10.1016/j.bmcl.2020.127493
46884154 8325 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 340 6 0 4 4.6 COc1ccc(C(C)c2c(CCN(C)C)sc3ccccc23)cn1 10.1016/j.bmcl.2010.01.134
CHEMBL1092812 8325 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 340 6 0 4 4.6 COc1ccc(C(C)c2c(CCN(C)C)sc3ccccc23)cn1 10.1016/j.bmcl.2010.01.134
14885639 118569 0 None - 1 Rat 5.9 pKi = 5.9 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 351 1 0 2 5.4 CC(=O)C1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/jm00105a069
CHEMBL341584 118569 0 None - 1 Rat 5.9 pKi = 5.9 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 351 1 0 2 5.4 CC(=O)C1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/jm00105a069
44352308 117487 0 None -1479 12 Rat 4.9 pKi = 4.9 Binding
Binding affinity towards rat histamine H1 receptor was determined using [3H]pyrilamine as radioligandBinding affinity towards rat histamine H1 receptor was determined using [3H]pyrilamine as radioligand
ChEMBL 339 5 2 2 4.0 Cc1[nH]c2cccc(NC(=O)c3ccc(F)cc3)c2c1CCN(C)C 10.1021/jm0155190
CHEMBL339980 117487 0 None -1479 12 Rat 4.9 pKi = 4.9 Binding
Binding affinity towards rat histamine H1 receptor was determined using [3H]pyrilamine as radioligandBinding affinity towards rat histamine H1 receptor was determined using [3H]pyrilamine as radioligand
ChEMBL 339 5 2 2 4.0 Cc1[nH]c2cccc(NC(=O)c3ccc(F)cc3)c2c1CCN(C)C 10.1021/jm0155190
44304382 203302 0 None -125 3 Human 5.9 pKi = 5.9 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 403 11 1 4 4.0 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)NC(C)C)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL64773 203302 0 None -125 3 Human 5.9 pKi = 5.9 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 403 11 1 4 4.0 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)NC(C)C)CC2)cc1 10.1016/s0960-894x(02)00309-8
164627774 186565 0 None -2 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 344 3 4 4 1.4 N/C(=N\C(=O)NCc1ccccc1)NC1CCc2nc(N)sc2C1 10.1016/j.ejmech.2021.113190
CHEMBL4878215 186565 0 None -2 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 344 3 4 4 1.4 N/C(=N\C(=O)NCc1ccccc1)NC1CCc2nc(N)sc2C1 10.1016/j.ejmech.2021.113190
44304030 200962 0 None -91 3 Human 4.9 pKi = 4.9 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 511 11 1 5 4.4 N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL60189 200962 0 None -91 3 Human 4.9 pKi = 4.9 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 511 11 1 5 4.4 N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
118709750 113540 0 None -109 9 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation countingDisplacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1cccc(F)c1 10.1016/j.bmcl.2014.07.018
CHEMBL3321791 113540 0 None -109 9 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation countingDisplacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1cccc(F)c1 10.1016/j.bmcl.2014.07.018
155564280 175423 0 None - 1 Guinea pig 5.9 pKi = 5.9 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysisDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysis
ChEMBL 290 4 0 4 1.0 CN1CCc2ccc(OCCN3CCOCC3)cc2C1=O 10.1016/j.bmcl.2019.04.015
CHEMBL4576048 175423 0 None - 1 Guinea pig 5.9 pKi = 5.9 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysisDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysis
ChEMBL 290 4 0 4 1.0 CN1CCc2ccc(OCCN3CCOCC3)cc2C1=O 10.1016/j.bmcl.2019.04.015
45485525 197799 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation counting
ChEMBL 337 7 1 2 4.8 Cc1ccc(CCCCN2CCC(C(O)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2009.07.047
CHEMBL572034 197799 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation counting
ChEMBL 337 7 1 2 4.8 Cc1ccc(CCCCN2CCC(C(O)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2009.07.047
46884239 8436 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 299 5 0 4 3.8 CC(c1c(CCN(C)C)sc2ccccc12)n1ccnc1 10.1016/j.bmcl.2010.01.134
CHEMBL1093607 8436 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 299 5 0 4 3.8 CC(c1c(CCN(C)C)sc2ccccc12)n1ccnc1 10.1016/j.bmcl.2010.01.134
57345619 70464 0 None -13 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-Pyrilamine from human histamine H1 receptor by liquid scintillation counterDisplacement of [3H]-Pyrilamine from human histamine H1 receptor by liquid scintillation counter
ChEMBL 360 6 0 2 5.0 Fc1ccc(CCCCN2CCCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2012.01.022
CHEMBL1946253 70464 0 None -13 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-Pyrilamine from human histamine H1 receptor by liquid scintillation counterDisplacement of [3H]-Pyrilamine from human histamine H1 receptor by liquid scintillation counter
ChEMBL 360 6 0 2 5.0 Fc1ccc(CCCCN2CCCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2012.01.022
28390601 162972 0 None -2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 377 4 0 5 3.9 Cc1oc(-c2ccco2)nc1CN1CCN([C@@H]2CCc3ccccc3C2)CC1 10.1021/acs.jmedchem.8b00718
CHEMBL4175018 162972 0 None -2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 377 4 0 5 3.9 Cc1oc(-c2ccco2)nc1CN1CCN([C@@H]2CCc3ccccc3C2)CC1 10.1021/acs.jmedchem.8b00718
69347707 81305 1 None 5 2 Human 6.9 pKi = 6.9 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 476 7 1 4 5.4 O=C(O)c1ccc(CN2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.103
CHEMBL2158833 81305 1 None 5 2 Human 6.9 pKi = 6.9 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 476 7 1 4 5.4 O=C(O)c1ccc(CN2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.103
71072057 81312 0 None -5 2 Human 6.9 pKi = 6.9 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 508 8 1 4 5.4 O=C(O)[C@H](Cc1cccc(F)c1)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158840 81312 0 None -5 2 Human 6.9 pKi = 6.9 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 508 8 1 4 5.4 O=C(O)[C@H](Cc1cccc(F)c1)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
24839550 137315 14 None -2 15 Human 6.9 pKi = 6.9 Binding
Binding affinity to histamine H1 receptor (unknown origin) by competition binding assayBinding affinity to histamine H1 receptor (unknown origin) by competition binding assay
ChEMBL 240 7 1 1 3.4 C=CCN(CC=C)CCc1c[nH]c2ccccc12 10.1016/j.bmcl.2015.12.053
CHEMBL3752576 137315 14 None -2 15 Human 6.9 pKi = 6.9 Binding
Binding affinity to histamine H1 receptor (unknown origin) by competition binding assayBinding affinity to histamine H1 receptor (unknown origin) by competition binding assay
ChEMBL 240 7 1 1 3.4 C=CCN(CC=C)CCc1c[nH]c2ccccc12 10.1016/j.bmcl.2015.12.053
59296094 84099 0 None -31 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 480 7 3 6 2.7 N#Cc1ccc(OC2CCN(C[C@H](O)CNC(=O)c3c[nH]c(=O)c4ccccc34)CC2)cc1Cl 10.1016/j.bmcl.2012.09.112
CHEMBL2207669 84099 0 None -31 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 480 7 3 6 2.7 N#Cc1ccc(OC2CCN(C[C@H](O)CNC(=O)c3c[nH]c(=O)c4ccccc34)CC2)cc1Cl 10.1016/j.bmcl.2012.09.112
9954003 71700 24 None -251 9 Guinea pig 6.9 pKi = 6.9 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 422 5 2 4 3.8 C[C@H]1Oc2c(cccc2N2CCN(CCCc3c[nH]c4ccc(F)cc34)CC2)NC1=O 10.1021/jm070516u
CHEMBL196514 71700 24 None -251 9 Guinea pig 6.9 pKi = 6.9 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 422 5 2 4 3.8 C[C@H]1Oc2c(cccc2N2CCN(CCCc3c[nH]c4ccc(F)cc34)CC2)NC1=O 10.1021/jm070516u
71462389 82243 0 None 1 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 476 5 1 4 4.8 O=C(O)c1cccc(C(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.124
CHEMBL2171024 82243 0 None 1 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 476 5 1 4 4.8 O=C(O)c1cccc(C(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.124
17963141 82268 0 None 1 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 491 5 1 5 4.1 Cc1ccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(Cl)cc4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.124
CHEMBL2171049 82268 0 None 1 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 491 5 1 5 4.1 Cc1ccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(Cl)cc4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.124
168296182 192227 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 808 21 7 9 1.8 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5204985 192227 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 808 21 7 9 1.8 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
9971374 104126 0 None -316 2 Human 5.9 pKi = 5.9 Binding
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced effect by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced effect by FLIPR assay
ChEMBL 288 5 1 3 2.6 c1cc2c(cc1OCCCN1CCCCC1)CCNCC2 10.1016/j.bmcl.2013.09.089
CHEMBL3094130 104126 0 None -316 2 Human 5.9 pKi = 5.9 Binding
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced effect by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced effect by FLIPR assay
ChEMBL 288 5 1 3 2.6 c1cc2c(cc1OCCCN1CCCCC1)CCNCC2 10.1016/j.bmcl.2013.09.089
50898777 56440 0 None -11748 8 Human 5.9 pKi = 5.9 Binding
Binding affinity to Histamine receptor H1Binding affinity to Histamine receptor H1
ChEMBL 441 9 1 6 3.6 COC(=O)CCCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2010.10.011
CHEMBL1632158 56440 0 None -11748 8 Human 5.9 pKi = 5.9 Binding
Binding affinity to Histamine receptor H1Binding affinity to Histamine receptor H1
ChEMBL 441 9 1 6 3.6 COC(=O)CCCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2010.10.011
71461541 84220 0 None -15 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 513 9 3 6 2.7 CS(=O)(=O)c1ccccc1C(=O)NCC(O)CNC1CCN(Cc2ccc(Cl)c(Cl)c2)CC1 10.1016/j.bmcl.2012.09.113
CHEMBL2208437 84220 0 None -15 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 513 9 3 6 2.7 CS(=O)(=O)c1ccccc1C(=O)NCC(O)CNC1CCN(Cc2ccc(Cl)c(Cl)c2)CC1 10.1016/j.bmcl.2012.09.113
50878551 90745 61 None -21 18 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
CHEMBL2391541 90745 61 None -21 18 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
10662264 56494 0 None -812 2 Guinea pig 4.9 pKi = 4.9 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 304 7 2 5 2.2 O=C(NCc1ccc([N+](=O)[O-])cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL16338 56494 0 None -812 2 Guinea pig 4.9 pKi = 4.9 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 304 7 2 5 2.2 O=C(NCc1ccc([N+](=O)[O-])cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
10660952 98123 0 None -190 2 Guinea pig 4.9 pKi = 4.9 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 287 7 1 3 3.0 CCN(Cc1ccccc1)C(=O)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL273549 98123 0 None -190 2 Guinea pig 4.9 pKi = 4.9 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 287 7 1 3 3.0 CCN(Cc1ccccc1)C(=O)OCCCc1c[nH]cn1 10.1021/jm9507688
10732219 98944 0 None -602 2 Guinea pig 4.9 pKi = 4.9 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 290 6 2 5 2.5 O=C(Nc1cccc([N+](=O)[O-])c1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL279617 98944 0 None -602 2 Guinea pig 4.9 pKi = 4.9 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 290 6 2 5 2.5 O=C(Nc1cccc([N+](=O)[O-])c1)OCCCc1c[nH]cn1 10.1021/jm9507688
1204 1932 119 None -46 24 Guinea pig 4.9 pKi = 4.9 Binding
Binding affinity against H1 receptor of guinea pig by the displacement of [3H]mepyramine, bound to membranes of CHO cellsBinding affinity against H1 receptor of guinea pig by the displacement of [3H]mepyramine, bound to membranes of CHO cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm00002a008
1247 1932 119 None -46 24 Guinea pig 4.9 pKi = 4.9 Binding
Binding affinity against H1 receptor of guinea pig by the displacement of [3H]mepyramine, bound to membranes of CHO cellsBinding affinity against H1 receptor of guinea pig by the displacement of [3H]mepyramine, bound to membranes of CHO cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm00002a008
1375 1932 119 None -46 24 Guinea pig 4.9 pKi = 4.9 Binding
Binding affinity against H1 receptor of guinea pig by the displacement of [3H]mepyramine, bound to membranes of CHO cellsBinding affinity against H1 receptor of guinea pig by the displacement of [3H]mepyramine, bound to membranes of CHO cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm00002a008
774 1932 119 None -46 24 Guinea pig 4.9 pKi = 4.9 Binding
Binding affinity against H1 receptor of guinea pig by the displacement of [3H]mepyramine, bound to membranes of CHO cellsBinding affinity against H1 receptor of guinea pig by the displacement of [3H]mepyramine, bound to membranes of CHO cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm00002a008
CHEMBL90 1932 119 None -46 24 Guinea pig 4.9 pKi = 4.9 Binding
Binding affinity against H1 receptor of guinea pig by the displacement of [3H]mepyramine, bound to membranes of CHO cellsBinding affinity against H1 receptor of guinea pig by the displacement of [3H]mepyramine, bound to membranes of CHO cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm00002a008
DB05381 1932 119 None -46 24 Guinea pig 4.9 pKi = 4.9 Binding
Binding affinity against H1 receptor of guinea pig by the displacement of [3H]mepyramine, bound to membranes of CHO cellsBinding affinity against H1 receptor of guinea pig by the displacement of [3H]mepyramine, bound to membranes of CHO cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm00002a008
44304560 102763 0 None -9549 3 Human 4.9 pKi = 4.9 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 371 8 1 5 1.6 O=C(c1ccc(OCCCN2CCN(C(=O)[C@H]3CCN3)CC2)cc1)C1CC1 10.1016/s0960-894x(02)00310-4
CHEMBL305144 102763 0 None -9549 3 Human 4.9 pKi = 4.9 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 371 8 1 5 1.6 O=C(c1ccc(OCCCN2CCN(C(=O)[C@H]3CCN3)CC2)cc1)C1CC1 10.1016/s0960-894x(02)00310-4
10422468 204158 0 None -630 3 Guinea pig 4.9 pKi = 4.9 Binding
Displacement of [3H]mepyramine bound to membranes of CHO cells expressing guinea pig H1 receptorsDisplacement of [3H]mepyramine bound to membranes of CHO cells expressing guinea pig H1 receptors
ChEMBL 254 7 3 2 2.4 CC(C)/N=C(\S)NCCCCCc1c[nH]cn1 10.1021/jm00012a025
CHEMBL70603 204158 0 None -630 3 Guinea pig 4.9 pKi = 4.9 Binding
Displacement of [3H]mepyramine bound to membranes of CHO cells expressing guinea pig H1 receptorsDisplacement of [3H]mepyramine bound to membranes of CHO cells expressing guinea pig H1 receptors
ChEMBL 254 7 3 2 2.4 CC(C)/N=C(\S)NCCCCCc1c[nH]cn1 10.1021/jm00012a025
1204 1932 119 None -501 24 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor N7.45S mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor N7.45S mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1038/nchembio714
1247 1932 119 None -501 24 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor N7.45S mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor N7.45S mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1038/nchembio714
1375 1932 119 None -501 24 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor N7.45S mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor N7.45S mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1038/nchembio714
774 1932 119 None -501 24 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor N7.45S mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor N7.45S mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1038/nchembio714
CHEMBL90 1932 119 None -501 24 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor N7.45S mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor N7.45S mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1038/nchembio714
DB05381 1932 119 None -501 24 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor N7.45S mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor N7.45S mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1038/nchembio714
164620678 186019 0 None -199 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 374 7 4 4 2.7 CCC(NC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4870510 186019 0 None -199 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 374 7 4 4 2.7 CCC(NC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1 10.1016/j.ejmech.2021.113190
168296182 192227 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 808 21 7 9 1.8 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5204985 192227 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 808 21 7 9 1.8 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
155567030 176417 0 None -37 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells incubated for 60 mins by microbeta scintillation counter methodDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells incubated for 60 mins by microbeta scintillation counter method
ChEMBL 337 8 0 2 5.8 c1ccc(-c2ccc(OCCCCCN3CCCCCC3)cc2)cc1 10.1016/j.bmc.2017.07.058
CHEMBL4586133 176417 0 None -37 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells incubated for 60 mins by microbeta scintillation counter methodDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells incubated for 60 mins by microbeta scintillation counter method
ChEMBL 337 8 0 2 5.8 c1ccc(-c2ccc(OCCCCCN3CCCCCC3)cc2)cc1 10.1016/j.bmc.2017.07.058
CHEMBL4596108 176417 0 None -37 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells incubated for 60 mins by microbeta scintillation counter methodDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells incubated for 60 mins by microbeta scintillation counter method
ChEMBL 337 8 0 2 5.8 c1ccc(-c2ccc(OCCCCCN3CCCCCC3)cc2)cc1 10.1016/j.bmc.2017.07.058
18337331 116091 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting method
ChEMBL 410 2 0 3 5.5 CC(C)COC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/jm501086v
CHEMBL3357035 116091 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting method
ChEMBL 410 2 0 3 5.5 CC(C)COC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/jm501086v
57403525 70154 0 None -85 10 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation countingDisplacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation counting
ChEMBL 361 6 1 2 4.8 OC1(c2ccc(Cl)cc2)CCN(CCCCc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
CHEMBL1940402 70154 0 None -85 10 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation countingDisplacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation counting
ChEMBL 361 6 1 2 4.8 OC1(c2ccc(Cl)cc2)CCN(CCCCc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
168295543 193041 0 None -1 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 380 4 4 4 3.3 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5209021 193041 0 None -1 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 380 4 4 4 3.3 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222929 193041 0 None -1 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 380 4 4 4 3.3 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
57390695 70467 0 None 3 8 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-Pyrilamine from human histamine H1 receptor by liquid scintillation counterDisplacement of [3H]-Pyrilamine from human histamine H1 receptor by liquid scintillation counter
ChEMBL 427 7 0 5 5.5 O=C(CCCCN1CCCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.bmc.2012.01.022
CHEMBL1946257 70467 0 None 3 8 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-Pyrilamine from human histamine H1 receptor by liquid scintillation counterDisplacement of [3H]-Pyrilamine from human histamine H1 receptor by liquid scintillation counter
ChEMBL 427 7 0 5 5.5 O=C(CCCCN1CCCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.bmc.2012.01.022
127035062 136451 0 None -44 19 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]Pyrilamine from human H1 Histamine receptors stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]Pyrilamine from human H1 Histamine receptors stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 447 12 0 5 5.2 COc1ccc(CCN(CCCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
CHEMBL3735756 136451 0 None -44 19 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]Pyrilamine from human H1 Histamine receptors stably expressed in HEK cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]Pyrilamine from human H1 Histamine receptors stably expressed in HEK cell membrane after 90 mins by scintillation counting method
ChEMBL 447 12 0 5 5.2 COc1ccc(CCN(CCCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
53322959 57750 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 325 7 0 3 3.9 C[C@H](C1=C(CCN(C)CCF)Cc2ccccc21)c1cnccn1 10.1016/j.bmcl.2010.12.053
CHEMBL1669408 57750 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 325 7 0 3 3.9 C[C@H](C1=C(CCN(C)CCF)Cc2ccccc21)c1cnccn1 10.1016/j.bmcl.2010.12.053
11493620 8268 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 328 5 0 3 4.7 C[C@@H](c1ccc(F)cn1)c1c(CCN(C)C)sc2ccccc12 10.1016/j.bmcl.2010.01.134
CHEMBL1092495 8268 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 328 5 0 3 4.7 C[C@@H](c1ccc(F)cn1)c1c(CCN(C)C)sc2ccccc12 10.1016/j.bmcl.2010.01.134
76332519 105477 0 None -1 4 Guinea pig 7.9 pKi = 7.9 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation counting
ChEMBL 510 7 0 6 6.3 O=c1oc2c(Cl)c(OCCCCN3CCC(c4noc5cc(F)ccc45)CC3)ccc2c2c1CCC2 10.1016/j.ejmech.2014.01.012
CHEMBL3120697 105477 0 None -1 4 Guinea pig 7.9 pKi = 7.9 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation counting
ChEMBL 510 7 0 6 6.3 O=c1oc2c(Cl)c(OCCCCN3CCC(c4noc5cc(F)ccc45)CC3)ccc2c2c1CCC2 10.1016/j.ejmech.2014.01.012
53324167 57767 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 370 7 0 4 4.5 C[C@H](C1=C(CCN(C)Cc2ccccn2)Cc2ccccc21)c1cnccn1 10.1016/j.bmcl.2010.12.053
CHEMBL1669424 57767 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 370 7 0 4 4.5 C[C@H](C1=C(CCN(C)Cc2ccccn2)Cc2ccccc21)c1cnccn1 10.1016/j.bmcl.2010.12.053
44334036 167792 0 None -323 3 Human 4.9 pKi = 4.9 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 391 8 1 5 3.0 CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)c3ccc(C#N)cc3)C2)cc1 10.1016/s0960-894x(02)00685-6
CHEMBL430502 167792 0 None -323 3 Human 4.9 pKi = 4.9 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 391 8 1 5 3.0 CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)c3ccc(C#N)cc3)C2)cc1 10.1016/s0960-894x(02)00685-6
168271050 189932 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 774 19 5 7 3.5 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5170060 189932 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 774 19 5 7 3.5 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
168271050 189932 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 774 19 5 7 3.5 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5170060 189932 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 774 19 5 7 3.5 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL4576555 214017 5 None -1 19 Human 5.9 pKi = 5.9 Binding
GPCRScan assay: inhibition of H1GPCRScan assay: inhibition of H1
ChEMBL None None None CN1CCN(C(=O)C(C)(C)c2ccc(C(=O)Nc3cn4cc(-c5cc(C(C)(C)C)cc(C(C)(C)C)c5)ccc4n3)cc2)CC1 10.6019/CHEMBL4507307
168268827 192779 0 None -4 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 450 8 4 4 4.8 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5179906 192779 0 None -4 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 450 8 4 4 4.8 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5221314 192779 0 None -4 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 450 8 4 4 4.8 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)c1 10.1021/acs.jmedchem.1c00692
72138721 162229 3 None -3 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 349 6 1 5 2.9 Fc1ccccc1N1CCN(CCCNc2cncc(Cl)n2)CC1 10.1021/acs.jmedchem.8b00718
CHEMBL4163265 162229 3 None -3 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 349 6 1 5 2.9 Fc1ccccc1N1CCN(CCCNc2cncc(Cl)n2)CC1 10.1021/acs.jmedchem.8b00718
168268853 192785 0 None -19 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 389 8 4 5 1.9 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5180504 192785 0 None -19 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 389 8 4 5 1.9 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5221353 192785 0 None -19 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 389 8 4 5 1.9 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
164624107 185722 0 None -29 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 402 9 4 4 2.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCc1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4865765 185722 0 None -29 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 402 9 4 4 2.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCc1ccccc1 10.1016/j.ejmech.2021.113190
44304990 203062 0 None -363 3 Human 4.9 pKi = 4.9 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 483 12 0 6 4.1 CCCCCC(=O)c1ccc(OCCCN2CCN(S(=O)(=O)c3ccc(C#N)cc3)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL63632 203062 0 None -363 3 Human 4.9 pKi = 4.9 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 483 12 0 6 4.1 CCCCCC(=O)c1ccc(OCCCN2CCN(S(=O)(=O)c3ccc(C#N)cc3)CC2)cc1 10.1016/s0960-894x(02)00309-8
44304066 202765 0 None -309 3 Human 4.9 pKi = 4.9 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 449 11 1 5 3.0 CN[C@H](Cc1ccccc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL62050 202765 0 None -309 3 Human 4.9 pKi = 4.9 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 449 11 1 5 3.0 CN[C@H](Cc1ccccc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
73347825 92540 0 None 1 3 Human 5.9 pKi = 5.9 Binding
Inhibition of histamine H1 receptor (unknown origin) by PDSP assayInhibition of histamine H1 receptor (unknown origin) by PDSP assay
ChEMBL 311 5 1 3 2.9 COc1ccc(CN[C@H]2C3C4CC5C6C4CC3C6C52)cc1OC 10.1016/j.bmc.2013.07.045
CHEMBL2432046 92540 0 None 1 3 Human 5.9 pKi = 5.9 Binding
Inhibition of histamine H1 receptor (unknown origin) by PDSP assayInhibition of histamine H1 receptor (unknown origin) by PDSP assay
ChEMBL 311 5 1 3 2.9 COc1ccc(CN[C@H]2C3C4CC5C6C4CC3C6C52)cc1OC 10.1016/j.bmc.2013.07.045
18715381 97351 0 None - 1 Rat 5.9 pKi = 5.9 Binding
Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.
ChEMBL 386 0 0 2 4.9 CC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3ccc(Cl)nc32)CC1 10.1016/S0960-894X(00)80290-5
CHEMBL269460 97351 0 None - 1 Rat 5.9 pKi = 5.9 Binding
Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.
ChEMBL 386 0 0 2 4.9 CC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3ccc(Cl)nc32)CC1 10.1016/S0960-894X(00)80290-5
CHEMBL4520788 213975 10 None -63 25 Human 5.9 pKi = 5.9 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a HRH1Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a HRH1
ChEMBL None None None CNCc1ccccc1-c1csc([C@H](C)Nc2nc(C)nc3cc(OC)c(OC)cc23)c1 10.6019/CHEMBL5212743
44373221 54388 0 None 3 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cellsDisplacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cells
ChEMBL 223 2 1 1 3.1 NCCC1c2ccccc2Cc2ccccc21 10.1016/j.bmc.2009.08.016
CHEMBL160893 54388 0 None 3 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cellsDisplacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cells
ChEMBL 223 2 1 1 3.1 NCCC1c2ccccc2Cc2ccccc21 10.1016/j.bmc.2009.08.016
46882180 5841 0 None -5 6 Human 5.9 pKi = 5.9 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 482 7 2 7 3.7 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)c(S(N)(=O)=O)cc4o3)CC2)ccc1F 10.1016/j.bmcl.2009.09.024
CHEMBL1079180 5841 0 None -5 6 Human 5.9 pKi = 5.9 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 482 7 2 7 3.7 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)c(S(N)(=O)=O)cc4o3)CC2)ccc1F 10.1016/j.bmcl.2009.09.024
9923147 5049 0 None -2238 4 Human 4.9 pKi = 4.9 Binding
Binding affinity at human cortical Histamine 1 receptorBinding affinity at human cortical Histamine 1 receptor
ChEMBL 321 6 1 4 3.0 N#Cc1ccc(-c2ccc(OCCCN3CC[C@@H](N)C3)cc2)cc1 10.1016/s0960-894x(02)00648-0
CHEMBL105267 5049 0 None -2238 4 Human 4.9 pKi = 4.9 Binding
Binding affinity at human cortical Histamine 1 receptorBinding affinity at human cortical Histamine 1 receptor
ChEMBL 321 6 1 4 3.0 N#Cc1ccc(-c2ccc(OCCCN3CC[C@@H](N)C3)cc2)cc1 10.1016/s0960-894x(02)00648-0
44326321 207796 0 None 2 3 Human 7.9 pKi = 7.9 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 295 2 0 3 4.0 CN(C)CC1C[C@@H]2c3ccccc3Oc3ccccc3[C@H]2O1 10.1016/j.bmcl.2004.03.069
CHEMBL96158 207796 0 None 2 3 Human 7.9 pKi = 7.9 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 295 2 0 3 4.0 CN(C)CC1C[C@@H]2c3ccccc3Oc3ccccc3[C@H]2O1 10.1016/j.bmcl.2004.03.069
2389 3331 118 None -46 67 Human 7.9 pKi = 7.9 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
5073 3331 118 None -46 67 Human 7.9 pKi = 7.9 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
96 3331 118 None -46 67 Human 7.9 pKi = 7.9 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
CHEMBL85 3331 118 None -46 67 Human 7.9 pKi = 7.9 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
DB00734 3331 118 None -46 67 Human 7.9 pKi = 7.9 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
10382839 116552 0 None - 1 Guinea pig 7.9 pKi = 7.9 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 343 5 1 4 3.7 CN(C)CCSC1c2ccccc2COc2ccc(C(=O)O)cc21 10.1021/jm00089a020
CHEMBL336317 116552 0 None - 1 Guinea pig 7.9 pKi = 7.9 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 343 5 1 4 3.7 CN(C)CCSC1c2ccccc2COc2ccc(C(=O)O)cc21 10.1021/jm00089a020
CHEMBL538750 116552 0 None - 1 Guinea pig 7.9 pKi = 7.9 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 343 5 1 4 3.7 CN(C)CCSC1c2ccccc2COc2ccc(C(=O)O)cc21 10.1021/jm00089a020
1222 881 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human histamine H1 receptor expressed in CHO-K1 cellsBinding affinity towards human histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1016/j.bmcl.2004.08.060
2678 881 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human histamine H1 receptor expressed in CHO-K1 cellsBinding affinity towards human histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1016/j.bmcl.2004.08.060
581 881 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human histamine H1 receptor expressed in CHO-K1 cellsBinding affinity towards human histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1016/j.bmcl.2004.08.060
CHEMBL1000 881 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human histamine H1 receptor expressed in CHO-K1 cellsBinding affinity towards human histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1016/j.bmcl.2004.08.060
DB00341 881 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human histamine H1 receptor expressed in CHO-K1 cellsBinding affinity towards human histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1016/j.bmcl.2004.08.060
12992627 67247 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human histamine H1 receptor expressed in CHO-K1 cellsBinding affinity towards human histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 570 7 2 5 5.7 NC(=O)N(O)CCC#Cc1ccc(OCCCN2CCC(=C3c4ccc(Cl)cc4CCc4cccnc43)CC2)cc1 10.1016/j.bmcl.2004.08.060
CHEMBL188021 67247 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human histamine H1 receptor expressed in CHO-K1 cellsBinding affinity towards human histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 570 7 2 5 5.7 NC(=O)N(O)CCC#Cc1ccc(OCCCN2CCC(=C3c4ccc(Cl)cc4CCc4cccnc43)CC2)cc1 10.1016/j.bmcl.2004.08.060
135398737 958 93 None -4 89 Rat 7.9 pKi = 7.9 Binding
Half-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenateHalf-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenate
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm010982y
38 958 93 None -4 89 Rat 7.9 pKi = 7.9 Binding
Half-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenateHalf-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenate
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm010982y
722 958 93 None -4 89 Rat 7.9 pKi = 7.9 Binding
Half-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenateHalf-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenate
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm010982y
CHEMBL42 958 93 None -4 89 Rat 7.9 pKi = 7.9 Binding
Half-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenateHalf-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenate
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm010982y
DB00363 958 93 None -4 89 Rat 7.9 pKi = 7.9 Binding
Half-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenateHalf-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenate
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm010982y
1222 881 0 None -1 2 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cellsIn vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1016/j.bmcl.2004.02.005
2678 881 0 None -1 2 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cellsIn vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1016/j.bmcl.2004.02.005
581 881 0 None -1 2 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cellsIn vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1016/j.bmcl.2004.02.005
CHEMBL1000 881 0 None -1 2 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cellsIn vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1016/j.bmcl.2004.02.005
DB00341 881 0 None -1 2 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cellsIn vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1016/j.bmcl.2004.02.005
1222 881 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Inhibition constant against histamine H1 receptorInhibition constant against histamine H1 receptor
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1021/jm058225d
2678 881 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Inhibition constant against histamine H1 receptorInhibition constant against histamine H1 receptor
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1021/jm058225d
581 881 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Inhibition constant against histamine H1 receptorInhibition constant against histamine H1 receptor
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1021/jm058225d
CHEMBL1000 881 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Inhibition constant against histamine H1 receptorInhibition constant against histamine H1 receptor
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1021/jm058225d
DB00341 881 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Inhibition constant against histamine H1 receptorInhibition constant against histamine H1 receptor
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1021/jm058225d
44401042 124829 0 None -3 9 Human 7.9 pKi = 7.9 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 329 2 0 3 4.6 CN(C)C[C@@H]1CC2c3ccccc3Oc3ccc(Cl)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL364270 124829 0 None -3 9 Human 7.9 pKi = 7.9 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 329 2 0 3 4.6 CN(C)C[C@@H]1CC2c3ccccc3Oc3ccc(Cl)cc3[C@H]2O1 10.1021/jm049632c
10344845 24883 0 None - 1 Guinea pig 7.9 pKi = 7.9 Binding
Inhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptorInhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptor
ChEMBL 474 7 1 5 4.9 O=C(O)c1ccc2c(c1)C(SCCN1CCN(Cc3ccccc3)CC1)c1ccccc1CO2 10.1021/jm00055a013
CHEMBL134543 24883 0 None - 1 Guinea pig 7.9 pKi = 7.9 Binding
Inhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptorInhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptor
ChEMBL 474 7 1 5 4.9 O=C(O)c1ccc2c(c1)C(SCCN1CCN(Cc3ccccc3)CC1)c1ccccc1CO2 10.1021/jm00055a013
45272878 195861 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 448 7 0 6 4.4 COc1ccc(Cn2c(N3CCC(N(C)CC4CCOCC4)CC3)nc3ccccc32)cc1 10.1016/j.bmcl.2009.05.086
CHEMBL558663 195861 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 448 7 0 6 4.4 COc1ccc(Cn2c(N3CCC(N(C)CC4CCOCC4)CC3)nc3ccccc32)cc1 10.1016/j.bmcl.2009.05.086
45270330 196447 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 434 7 1 6 4.1 COc1ccc(Cn2c(N3CCC(NCC4CCOCC4)CC3)nc3ccccc32)cc1 10.1016/j.bmcl.2009.05.086
CHEMBL563055 196447 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 434 7 1 6 4.1 COc1ccc(Cn2c(N3CCC(NCC4CCOCC4)CC3)nc3ccccc32)cc1 10.1016/j.bmcl.2009.05.086
25184832 18695 0 None 2 5 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]pyrilamine from histamine H1 receptor in Sprague-Dawley rat cortical membrane by liquid scintillation countingDisplacement of [3H]pyrilamine from histamine H1 receptor in Sprague-Dawley rat cortical membrane by liquid scintillation counting
ChEMBL 349 2 1 3 3.8 O=C(O)C1CN(C2CCC3(Cc4ccccc4Oc4ccccc43)C2)C1 10.1021/jm100856p
CHEMBL1277312 18695 0 None 2 5 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]pyrilamine from histamine H1 receptor in Sprague-Dawley rat cortical membrane by liquid scintillation countingDisplacement of [3H]pyrilamine from histamine H1 receptor in Sprague-Dawley rat cortical membrane by liquid scintillation counting
ChEMBL 349 2 1 3 3.8 O=C(O)C1CN(C2CCC3(Cc4ccccc4Oc4ccccc43)C2)C1 10.1021/jm100856p
1224 1432 83 None -2 13 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1016/j.bmcl.2011.09.001
3100 1432 83 None -2 13 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1016/j.bmcl.2011.09.001
8980 1432 83 None -2 13 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1016/j.bmcl.2011.09.001
916 1432 83 None -2 13 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1016/j.bmcl.2011.09.001
CHEMBL657 1432 83 None -2 13 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1016/j.bmcl.2011.09.001
DB01075 1432 83 None -2 13 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1016/j.bmcl.2011.09.001
44343629 159949 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 327 1 1 3 2.4 O=C1CN(C2c3ccc(Cl)cc3CCc3cccnc32)CCN1 10.1016/s0960-894x(98)00626-x
CHEMBL410734 159949 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 327 1 1 3 2.4 O=C1CN(C2c3ccc(Cl)cc3CCc3cccnc32)CCN1 10.1016/s0960-894x(98)00626-x
10474964 130471 0 None -181 7 Rat 6.9 pKi = 6.9 Binding
Inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat cortexInhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat cortex
ChEMBL 381 5 1 3 3.3 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
CHEMBL368061 130471 0 None -181 7 Rat 6.9 pKi = 6.9 Binding
Inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat cortexInhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat cortex
ChEMBL 381 5 1 3 3.3 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
CHEMBL5206021 130471 0 None -181 7 Rat 6.9 pKi = 6.9 Binding
Inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat cortexInhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat cortex
ChEMBL 381 5 1 3 3.3 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
46782362 150451 27 None -10 2 Human 6.9 pKi = 6.9 Binding
Radioligand Binding Assay: The pharmacological profile of metopimazine, metopimazine acid (MPZA), domperidone, and metoclopramide were assessed by radioligand binding and by a functional antagonist assay. For the radioligand binding assay, cell membranes of dopamine D2 receptor expressing cells were incubated with [3H]spiperone and competing drugs in buffer. The assay was terminated by rapid filtration, and the bound radioactive signal was determined by liquid scintillation counting.Radioligand Binding Assay: The pharmacological profile of metopimazine, metopimazine acid (MPZA), domperidone, and metoclopramide were assessed by radioligand binding and by a functional antagonist assay. For the radioligand binding assay, cell membranes of dopamine D2 receptor expressing cells were incubated with [3H]spiperone and competing drugs in buffer. The assay was terminated by rapid filtration, and the bound radioactive signal was determined by liquid scintillation counting.
ChEMBL 446 6 1 6 3.9 CS(=O)(=O)c1ccc2c(c1)N(CCCN1CCC(C(=O)O)CC1)c1ccccc1S2 nan
CHEMBL3954123 150451 27 None -10 2 Human 6.9 pKi = 6.9 Binding
Radioligand Binding Assay: The pharmacological profile of metopimazine, metopimazine acid (MPZA), domperidone, and metoclopramide were assessed by radioligand binding and by a functional antagonist assay. For the radioligand binding assay, cell membranes of dopamine D2 receptor expressing cells were incubated with [3H]spiperone and competing drugs in buffer. The assay was terminated by rapid filtration, and the bound radioactive signal was determined by liquid scintillation counting.Radioligand Binding Assay: The pharmacological profile of metopimazine, metopimazine acid (MPZA), domperidone, and metoclopramide were assessed by radioligand binding and by a functional antagonist assay. For the radioligand binding assay, cell membranes of dopamine D2 receptor expressing cells were incubated with [3H]spiperone and competing drugs in buffer. The assay was terminated by rapid filtration, and the bound radioactive signal was determined by liquid scintillation counting.
ChEMBL 446 6 1 6 3.9 CS(=O)(=O)c1ccc2c(c1)N(CCCN1CCC(C(=O)O)CC1)c1ccccc1S2 nan
11121216 30139 0 None -707 14 Human 5.9 pKi = 5.9 Binding
Binding affinity towards Histamine H1 receptorBinding affinity towards Histamine H1 receptor
ChEMBL 335 1 1 2 3.0 C[C@@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
CHEMBL138989 30139 0 None -707 14 Human 5.9 pKi = 5.9 Binding
Binding affinity towards Histamine H1 receptorBinding affinity towards Histamine H1 receptor
ChEMBL 335 1 1 2 3.0 C[C@@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
71456045 84073 0 None -1995 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis
ChEMBL 362 5 1 4 3.6 COc1ccccc1N1CCN(Cc2cc(CO)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207635 84073 0 None -1995 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis
ChEMBL 362 5 1 4 3.6 COc1ccccc1N1CCN(Cc2cc(CO)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
44334214 4615 0 None -2344 3 Human 4.9 pKi = 4.9 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 427 9 1 6 2.6 CC(=O)c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccc(C#N)cc3)C2)cc1 10.1016/s0960-894x(02)00685-6
CHEMBL102840 4615 0 None -2344 3 Human 4.9 pKi = 4.9 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 427 9 1 6 2.6 CC(=O)c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccc(C#N)cc3)C2)cc1 10.1016/s0960-894x(02)00685-6
44304090 202950 0 None -301 3 Human 5.9 pKi = 5.9 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 360 8 0 5 2.8 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00309-8
CHEMBL62948 202950 0 None -301 3 Human 5.9 pKi = 5.9 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 360 8 0 5 2.8 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00309-8
53245590 92399 43 None -3 4 Human 5.9 pKi = 5.9 Binding
Binding affinity to histamine H1 receptor (unknown origin)Binding affinity to histamine H1 receptor (unknown origin)
ChEMBL 420 6 0 7 3.9 COc1cc2nc(C3CC3)nc(N3CCN(c4ccccc4OC)CC3)c2cc1OC 10.1021/ml400176n
CHEMBL2431120 92399 43 None -3 4 Human 5.9 pKi = 5.9 Binding
Binding affinity to histamine H1 receptor (unknown origin)Binding affinity to histamine H1 receptor (unknown origin)
ChEMBL 420 6 0 7 3.9 COc1cc2nc(C3CC3)nc(N3CCN(c4ccccc4OC)CC3)c2cc1OC 10.1021/ml400176n
16726095 84637 2 None -1 4 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]pyrilamine from rat cortex histamine H1 receptorDisplacement of [3H]pyrilamine from rat cortex histamine H1 receptor
ChEMBL 379 5 1 4 3.4 COC(=O)C1(c2ccc(C)cc2)CC1CN1CCC(O)(c2ccccc2)CC1 10.1021/jm0611197
CHEMBL222301 84637 2 None -1 4 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]pyrilamine from rat cortex histamine H1 receptorDisplacement of [3H]pyrilamine from rat cortex histamine H1 receptor
ChEMBL 379 5 1 4 3.4 COC(=O)C1(c2ccc(C)cc2)CC1CN1CCC(O)(c2ccccc2)CC1 10.1021/jm0611197
127051844 140847 0 None -125 9 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 322 6 1 3 2.8 NC(=O)c1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819427 140847 0 None -125 9 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 322 6 1 3 2.8 NC(=O)c1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
4601 206747 35 None -1 16 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL1201023 206747 35 None -1 16 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL900 206747 35 None -1 16 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
168276867 192835 0 None -1 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 662 11 8 8 4.8 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5174278 192835 0 None -1 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 662 11 8 8 4.8 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5221653 192835 0 None -1 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 662 11 8 8 4.8 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)c1 10.1021/acs.jmedchem.1c00692
44304068 102347 0 None -89 3 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 441 10 1 5 3.5 N[C@H](CC1CCCCC1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL303737 102347 0 None -89 3 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 441 10 1 5 3.5 N[C@H](CC1CCCCC1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
44304760 202901 0 None -234 3 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 431 13 1 5 3.7 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](N)CC(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
CHEMBL62741 202901 0 None -234 3 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 431 13 1 5 3.7 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](N)CC(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
9906978 42711 2 None -28 12 Human 5.8 pKi = 5.8 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL150161 42711 2 None -28 12 Human 5.8 pKi = 5.8 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
9906978 42711 2 None -28 12 Human 5.8 pKi = 5.8 Binding
Binding affinity to human cloned histamine H1 receptor by radioligand binding assayBinding affinity to human cloned histamine H1 receptor by radioligand binding assay
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmcl.2006.03.057
CHEMBL150161 42711 2 None -28 12 Human 5.8 pKi = 5.8 Binding
Binding affinity to human cloned histamine H1 receptor by radioligand binding assayBinding affinity to human cloned histamine H1 receptor by radioligand binding assay
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmcl.2006.03.057
118721930 116094 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting method
ChEMBL 394 3 0 2 5.4 CCCCC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/jm501086v
CHEMBL3357043 116094 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting method
ChEMBL 394 3 0 2 5.4 CCCCC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/jm501086v
44335428 4984 0 None -1 3 Human 5.8 pKi = 5.8 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 358 7 1 5 2.6 CCOC(=O)N1CCN(CCCOc2ccc(-c3c[nH]cn3)cc2)CC1 10.1016/s0960-894x(02)00648-0
CHEMBL104947 4984 0 None -1 3 Human 5.8 pKi = 5.8 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 358 7 1 5 2.6 CCOC(=O)N1CCN(CCCOc2ccc(-c3c[nH]cn3)cc2)CC1 10.1016/s0960-894x(02)00648-0
2865 4143 73 None -58 53 Human 7.8 pKi = 7.8 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 nan
59 4143 73 None -58 53 Human 7.8 pKi = 7.8 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 nan
60854 4143 73 None -58 53 Human 7.8 pKi = 7.8 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 nan
CHEMBL708 4143 73 None -58 53 Human 7.8 pKi = 7.8 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 nan
DB00246 4143 73 None -58 53 Human 7.8 pKi = 7.8 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 nan
46884641 7914 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 279 5 0 3 3.0 CN(C)CCC1=C(Cc2ncccn2)c2ccccc2C1 10.1016/j.bmcl.2010.02.055
CHEMBL1090198 7914 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 279 5 0 3 3.0 CN(C)CCC1=C(Cc2ncccn2)c2ccccc2C1 10.1016/j.bmcl.2010.02.055
12765746 102280 4 None -69 9 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cellsDisplacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 344 1 0 3 4.3 CN1CCN([C@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm100652h
CHEMBL303313 102280 4 None -69 9 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cellsDisplacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 344 1 0 3 4.3 CN1CCN([C@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm100652h
11696813 187918 12 None -3 9 Guinea pig 7.8 pKi = 7.8 Binding
Displacement of [3H]pyrilamine from histamine H1 receptor in guinea pig cerebellumDisplacement of [3H]pyrilamine from histamine H1 receptor in guinea pig cerebellum
ChEMBL 391 7 1 4 4.1 Cc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4o3)CC2)c1 10.1021/jm800689g
CHEMBL496739 187918 12 None -3 9 Guinea pig 7.8 pKi = 7.8 Binding
Displacement of [3H]pyrilamine from histamine H1 receptor in guinea pig cerebellumDisplacement of [3H]pyrilamine from histamine H1 receptor in guinea pig cerebellum
ChEMBL 391 7 1 4 4.1 Cc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4o3)CC2)c1 10.1021/jm800689g
44404954 135265 0 None 1 3 Guinea pig 7.8 pKi = 7.8 Binding
Inhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptorInhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptor
ChEMBL 453 6 1 3 5.6 O=C(O)Cc1ccc2c(c1)/C(=C\CN1CCC(Cc3ccccc3)CC1)c1ccccc1CO2 10.1021/jm00055a013
CHEMBL372588 135265 0 None 1 3 Guinea pig 7.8 pKi = 7.8 Binding
Inhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptorInhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptor
ChEMBL 453 6 1 3 5.6 O=C(O)Cc1ccc2c(c1)/C(=C\CN1CCC(Cc3ccccc3)CC1)c1ccccc1CO2 10.1021/jm00055a013
15749429 202913 0 None - 1 Guinea pig 7.8 pKi = 7.8 Binding
The compound was tested in vitro for binding affinity against histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMThe compound was tested in vitro for binding affinity against histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 351 6 1 3 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccc(CCC(=O)O)cc21 10.1021/jm00089a020
CHEMBL62790 202913 0 None - 1 Guinea pig 7.8 pKi = 7.8 Binding
The compound was tested in vitro for binding affinity against histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMThe compound was tested in vitro for binding affinity against histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 351 6 1 3 4.0 CN(C)CC/C=C1/c2ccccc2COc2ccc(CCC(=O)O)cc21 10.1021/jm00089a020
53326727 57770 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 377 7 0 4 4.3 C[C@H](C1=C(CCN(C)CC2CCOCC2)Cc2ccccc21)c1cnccn1 10.1016/j.bmcl.2010.12.053
CHEMBL1669427 57770 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 377 7 0 4 4.3 C[C@H](C1=C(CCN(C)CC2CCOCC2)Cc2ccccc21)c1cnccn1 10.1016/j.bmcl.2010.12.053
9914506 81257 0 None -3 2 Human 7.8 pKi = 7.8 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 515 8 1 5 5.1 N#Cc1ccccc1C[C@@H](C(=O)O)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158769 81257 0 None -3 2 Human 7.8 pKi = 7.8 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 515 8 1 5 5.1 N#Cc1ccccc1C[C@@H](C(=O)O)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
71072052 81259 0 None -1 2 Human 7.8 pKi = 7.8 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 515 8 1 5 5.1 N#Cc1ccc(C[C@@H](C(=O)O)N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.103
CHEMBL2158771 81259 0 None -1 2 Human 7.8 pKi = 7.8 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 515 8 1 5 5.1 N#Cc1ccc(C[C@@H](C(=O)O)N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.103
71072081 81261 0 None 1 2 Human 7.8 pKi = 7.8 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 504 8 1 4 5.6 Cc1cccc(C[C@@H](C(=O)O)N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.103
CHEMBL2158773 81261 0 None 1 2 Human 7.8 pKi = 7.8 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 504 8 1 4 5.6 Cc1cccc(C[C@@H](C(=O)O)N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.103
71449584 81296 1 None 1 2 Human 7.8 pKi = 7.8 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 476 7 1 4 5.4 O=C(O)Cc1ccccc1N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158825 81296 1 None 1 2 Human 7.8 pKi = 7.8 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 476 7 1 4 5.4 O=C(O)Cc1ccccc1N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
69272932 81299 0 None 1 2 Human 7.8 pKi = 7.8 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 492 8 1 5 5.2 O=C(O)COc1ccccc1N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158828 81299 0 None 1 2 Human 7.8 pKi = 7.8 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 492 8 1 5 5.2 O=C(O)COc1ccccc1N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
17747460 61329 12 None -19 4 Human 7.8 pKi = 7.8 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 640 14 0 6 7.8 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1021/jm100064d
CHEMBL1767164 61329 12 None -19 4 Human 7.8 pKi = 7.8 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 640 14 0 6 7.8 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1021/jm100064d
59296114 84208 0 None 12 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 480 7 2 6 3.4 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1cn2cc(F)ccc2n1 10.1016/j.bmcl.2012.09.113
CHEMBL2208425 84208 0 None 12 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 480 7 2 6 3.4 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1cn2cc(F)ccc2n1 10.1016/j.bmcl.2012.09.113
59296111 84087 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 480 7 3 5 3.4 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]nc1C(F)(F)F 10.1016/j.bmcl.2012.09.112
CHEMBL2207658 84087 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 480 7 3 5 3.4 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]nc1C(F)(F)F 10.1016/j.bmcl.2012.09.112
23722970 69020 21 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 267 4 1 2 3.4 c1ccc(Cc2ccccc2OC2CCNCC2)cc1 10.1021/acs.jmedchem.6b00981
CHEMBL1923521 69020 21 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 267 4 1 2 3.4 c1ccc(Cc2ccccc2OC2CCNCC2)cc1 10.1021/acs.jmedchem.6b00981
CHEMBL3977546 69020 21 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 267 4 1 2 3.4 c1ccc(Cc2ccccc2OC2CCNCC2)cc1 10.1021/acs.jmedchem.6b00981
44396235 168537 1 None 23 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 281 6 0 2 3.8 c1ccc(Cc2ccccc2OCCN2CCCC2)cc1 10.1021/acs.jmedchem.6b00981
CHEMBL435505 168537 1 None 23 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 281 6 0 2 3.8 c1ccc(Cc2ccccc2OCCN2CCCC2)cc1 10.1021/acs.jmedchem.6b00981
2865 4143 73 None -17 53 Guinea pig 7.8 pKi = 7.8 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm070516u
59 4143 73 None -17 53 Guinea pig 7.8 pKi = 7.8 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm070516u
60854 4143 73 None -17 53 Guinea pig 7.8 pKi = 7.8 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm070516u
CHEMBL708 4143 73 None -17 53 Guinea pig 7.8 pKi = 7.8 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm070516u
DB00246 4143 73 None -17 53 Guinea pig 7.8 pKi = 7.8 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm070516u
136229178 82244 0 None 19 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 516 5 1 6 4.5 O=C(c1ccc(-c2noc(=O)[nH]2)cc1)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
CHEMBL2171025 82244 0 None 19 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 516 5 1 6 4.5 O=C(c1ccc(-c2noc(=O)[nH]2)cc1)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
71451671 82247 0 None 31 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 519 8 2 5 5.0 O=C(O)CCNc1ccccc1C(=O)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
CHEMBL2171028 82247 0 None 31 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 519 8 2 5 5.0 O=C(O)CCNc1ccccc1C(=O)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
17963153 82265 0 None 1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 525 5 1 5 4.7 Cc1ccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(Cl)cc4Cl)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.124
CHEMBL2171046 82265 0 None 1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 525 5 1 5 4.7 Cc1ccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(Cl)cc4Cl)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.124
10324985 76781 8 None -112 17 Human 6.8 pKi = 6.8 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
CHEMBL199824 76781 8 None -112 17 Human 6.8 pKi = 6.8 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
CHEMBL2068762 76781 8 None -112 17 Human 6.8 pKi = 6.8 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
9913604 204586 0 None - 1 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cellsIn vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 492 7 2 5 4.4 NC(=O)N(O)CCC#Cc1ccc(CN2CCN([C@H](c3ccccc3)c3ccc(Cl)cc3)CC2)o1 10.1016/j.bmcl.2004.02.005
CHEMBL73135 204586 0 None - 1 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cellsIn vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 492 7 2 5 4.4 NC(=O)N(O)CCC#Cc1ccc(CN2CCN([C@H](c3ccccc3)c3ccc(Cl)cc3)CC2)o1 10.1016/j.bmcl.2004.02.005
9913604 204586 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition constant against histamine H1 receptorInhibition constant against histamine H1 receptor
ChEMBL 492 7 2 5 4.4 NC(=O)N(O)CCC#Cc1ccc(CN2CCN([C@H](c3ccccc3)c3ccc(Cl)cc3)CC2)o1 10.1021/jm058225d
CHEMBL73135 204586 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition constant against histamine H1 receptorInhibition constant against histamine H1 receptor
ChEMBL 492 7 2 5 4.4 NC(=O)N(O)CCC#Cc1ccc(CN2CCN([C@H](c3ccccc3)c3ccc(Cl)cc3)CC2)o1 10.1021/jm058225d
14885627 114820 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 352 0 0 2 4.3 CC(=O)N1CCC(=C2c3cc(Cl)ccc3CCc3cccnc32)CC1 10.1021/jm00105a069
CHEMBL334127 114820 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 352 0 0 2 4.3 CC(=O)N1CCC(=C2c3cc(Cl)ccc3CCc3cccnc32)CC1 10.1021/jm00105a069
44334368 109217 0 None -301 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 506 10 1 5 3.9 O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccc(Br)cc3)C2)cc1)C1CC1 10.1016/s0960-894x(02)00685-6
CHEMBL321709 109217 0 None -301 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 506 10 1 5 3.9 O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccc(Br)cc3)C2)cc1)C1CC1 10.1016/s0960-894x(02)00685-6
9848303 111580 0 None -501 9 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cellsDisplacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 487 6 1 6 3.8 Cn1cc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)nn1 10.1021/jm100652h
CHEMBL328187 111580 0 None -501 9 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cellsDisplacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 487 6 1 6 3.8 Cn1cc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)nn1 10.1021/jm100652h
168276544 190321 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 742 19 6 8 1.8 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5176319 190321 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 742 19 6 8 1.8 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
168276544 190321 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 742 19 6 8 1.8 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5176319 190321 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 742 19 6 8 1.8 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
44304318 203261 0 None -234 3 Human 5.8 pKi = 5.8 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 373 9 1 5 1.8 C[C@@H](CN)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL64608 203261 0 None -234 3 Human 5.8 pKi = 5.8 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 373 9 1 5 1.8 C[C@@H](CN)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
118721928 116092 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting method
ChEMBL 378 1 0 2 4.8 C/C=C/C(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/jm501086v
CHEMBL3357041 116092 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting method
ChEMBL 378 1 0 2 4.8 C/C=C/C(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/jm501086v
1621 2429 17 None -301 45 Human 5.8 pKi = 5.8 Binding
Binding affinity towards Histamine H1 receptorBinding affinity towards Histamine H1 receptor
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
17 2429 17 None -301 45 Human 5.8 pKi = 5.8 Binding
Binding affinity towards Histamine H1 receptorBinding affinity towards Histamine H1 receptor
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
5761 2429 17 None -301 45 Human 5.8 pKi = 5.8 Binding
Binding affinity towards Histamine H1 receptorBinding affinity towards Histamine H1 receptor
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
CHEMBL263881 2429 17 None -301 45 Human 5.8 pKi = 5.8 Binding
Binding affinity towards Histamine H1 receptorBinding affinity towards Histamine H1 receptor
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
DB04829 2429 17 None -301 45 Human 5.8 pKi = 5.8 Binding
Binding affinity towards Histamine H1 receptorBinding affinity towards Histamine H1 receptor
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
45485535 197621 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation counting
ChEMBL 399 7 1 2 5.6 Cc1ccc(CCCN2CCC(C(O)(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2009.07.047
CHEMBL570695 197621 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation counting
ChEMBL 399 7 1 2 5.6 Cc1ccc(CCCN2CCC(C(O)(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2009.07.047
3151 1462 97 None -41 27 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
945 1462 97 None -41 27 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
965 1462 97 None -41 27 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
CHEMBL219916 1462 97 None -41 27 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
DB01184 1462 97 None -41 27 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 nan
44395741 181581 0 None -10 10 Human 6.8 pKi = 6.8 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL476935 181581 0 None -10 10 Human 6.8 pKi = 6.8 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL558392 181581 0 None -10 10 Human 6.8 pKi = 6.8 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
44307779 203559 0 None -1348 4 Human 4.8 pKi = 4.8 Binding
Compound was tested for its binding affinity towards human H1 receptorCompound was tested for its binding affinity towards human H1 receptor
ChEMBL 332 2 0 2 4.7 C(#Cc1c2c(nc3ccccc13)CCCCC2)CCN1CCCCC1 10.1016/s0960-894x(03)00356-1
CHEMBL66660 203559 0 None -1348 4 Human 4.8 pKi = 4.8 Binding
Compound was tested for its binding affinity towards human H1 receptorCompound was tested for its binding affinity towards human H1 receptor
ChEMBL 332 2 0 2 4.7 C(#Cc1c2c(nc3ccccc13)CCCCC2)CCN1CCCCC1 10.1016/s0960-894x(03)00356-1
168279725 191155 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 728 19 6 8 1.5 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5188589 191155 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 728 19 6 8 1.5 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
168292703 192060 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 726 18 5 7 2.9 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5202570 192060 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 726 18 5 7 2.9 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
44335387 108550 0 None -5 4 Human 6.8 pKi = 6.8 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 393 7 0 5 3.8 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)CC1 10.1016/s0960-894x(02)00648-0
CHEMBL320178 108550 0 None -5 4 Human 6.8 pKi = 6.8 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 393 7 0 5 3.8 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)CC1 10.1016/s0960-894x(02)00648-0
11444350 81265 0 None -7 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 558 8 1 4 6.3 O=C(O)[C@H](Cc1cccc(C(F)(F)F)c1)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158777 81265 0 None -7 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 558 8 1 4 6.3 O=C(O)[C@H](Cc1cccc(C(F)(F)F)c1)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
71451391 81269 0 None -12 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 472 8 1 4 4.5 Cc1cc(F)ccc1OC1CCN(CC2CCN([C@@H](Cc3ccc(F)cc3)C(=O)O)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158781 81269 0 None -12 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 472 8 1 4 4.5 Cc1cc(F)ccc1OC1CCN(CC2CCN([C@@H](Cc3ccc(F)cc3)C(=O)O)CC2)CC1 10.1016/j.bmcl.2012.08.103
16040671 81279 0 None -56 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 502 8 1 4 5.4 Cc1cc(Cl)ccc1OC1CCN(CC2CCN([C@@](C)(Cc3ccc(F)cc3)C(=O)O)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158791 81279 0 None -56 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 502 8 1 4 5.4 Cc1cc(Cl)ccc1OC1CCN(CC2CCN([C@@](C)(Cc3ccc(F)cc3)C(=O)O)CC2)CC1 10.1016/j.bmcl.2012.08.103
127051843 140751 0 None -7 9 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 0 3 3.6 N#Cc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818200 140751 0 None -7 9 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 0 3 3.6 N#Cc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
168279725 191155 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 728 19 6 8 1.5 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5188589 191155 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 728 19 6 8 1.5 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
168292703 192060 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 726 18 5 7 2.9 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5202570 192060 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 726 18 5 7 2.9 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
44267106 98490 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.
ChEMBL 368 0 1 3 4.0 CC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3cc(O)cnc32)CC1 10.1016/S0960-894X(00)80290-5
CHEMBL275993 98490 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.
ChEMBL 368 0 1 3 4.0 CC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3cc(O)cnc32)CC1 10.1016/S0960-894X(00)80290-5
44304325 201678 0 None -74 3 Human 5.8 pKi = 5.8 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 389 11 1 4 3.6 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)NCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL60620 201678 0 None -74 3 Human 5.8 pKi = 5.8 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 389 11 1 4 3.6 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)NCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
10473209 62674 3 None -6456 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 352 4 1 5 2.6 CNC(=O)c1cnc(Oc2ccc3c(c2)CCN(C2CCC2)CC3)cn1 10.1016/j.bmcl.2013.09.090
CHEMBL1783890 62674 3 None -6456 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 352 4 1 5 2.6 CNC(=O)c1cnc(Oc2ccc3c(c2)CCN(C2CCC2)CC3)cn1 10.1016/j.bmcl.2013.09.090
127051844 140847 0 None -125 9 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 322 6 1 3 2.8 NC(=O)c1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819427 140847 0 None -125 9 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 322 6 1 3 2.8 NC(=O)c1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
9974306 204474 0 None -199 4 Guinea pig 5.8 pKi = 5.8 Binding
Displacement of [3H]mepyramine bound to membranes of CHO cells expressing guinea pig H1 receptorsDisplacement of [3H]mepyramine bound to membranes of CHO cells expressing guinea pig H1 receptors
ChEMBL 336 8 3 2 3.4 S=C(NCCCCCc1c[nH]cn1)NCc1ccc(Cl)cc1 10.1021/jm00012a025
CHEMBL72372 204474 0 None -199 4 Guinea pig 5.8 pKi = 5.8 Binding
Displacement of [3H]mepyramine bound to membranes of CHO cells expressing guinea pig H1 receptorsDisplacement of [3H]mepyramine bound to membranes of CHO cells expressing guinea pig H1 receptors
ChEMBL 336 8 3 2 3.4 S=C(NCCCCCc1c[nH]cn1)NCc1ccc(Cl)cc1 10.1021/jm00012a025
2061019 55103 17 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 227 5 1 2 2.6 NCCOc1ccccc1Cc1ccccc1 10.1021/acs.jmedchem.6b00981
CHEMBL1616890 55103 17 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 227 5 1 2 2.6 NCCOc1ccccc1Cc1ccccc1 10.1021/acs.jmedchem.6b00981
CHEMBL3916710 55103 17 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 227 5 1 2 2.6 NCCOc1ccccc1Cc1ccccc1 10.1021/acs.jmedchem.6b00981
134142912 154522 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 267 4 1 2 3.4 c1ccc(Cc2cccc(OC3CCNCC3)c2)cc1 10.1021/acs.jmedchem.6b00981
CHEMBL3913361 154522 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 267 4 1 2 3.4 c1ccc(Cc2cccc(OC3CCNCC3)c2)cc1 10.1021/acs.jmedchem.6b00981
CHEMBL3990797 154522 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 267 4 1 2 3.4 c1ccc(Cc2cccc(OC3CCNCC3)c2)cc1 10.1021/acs.jmedchem.6b00981
10802230 56559 0 None -389 2 Guinea pig 4.8 pKi = 4.8 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 273 6 1 3 2.6 CN(Cc1ccccc1)C(=O)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL16404 56559 0 None -389 2 Guinea pig 4.8 pKi = 4.8 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 273 6 1 3 2.6 CN(Cc1ccccc1)C(=O)OCCCc1c[nH]cn1 10.1021/jm9507688
10358195 57460 0 None -1023 2 Guinea pig 4.8 pKi = 4.8 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 313 5 2 3 3.6 O=C(Nc1ccc(C(F)(F)F)cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL16565 57460 0 None -1023 2 Guinea pig 4.8 pKi = 4.8 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 313 5 2 3 3.6 O=C(Nc1ccc(C(F)(F)F)cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
10520238 57564 0 None -1288 2 Guinea pig 4.8 pKi = 4.8 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 327 6 2 3 3.3 O=C(NCc1ccc(C(F)(F)F)cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL16654 57564 0 None -1288 2 Guinea pig 4.8 pKi = 4.8 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 327 6 2 3 3.3 O=C(NCc1ccc(C(F)(F)F)cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
10708894 98633 0 None -1202 2 Guinea pig 4.8 pKi = 4.8 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 293 6 2 3 2.9 O=C(NCc1ccc(Cl)cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL277149 98633 0 None -1202 2 Guinea pig 4.8 pKi = 4.8 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 293 6 2 3 2.9 O=C(NCc1ccc(Cl)cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
10466840 204481 0 None -1584 4 Guinea pig 4.8 pKi = 4.8 Binding
Displacement of [3H]mepyramine bound to membranes of CHO cells expressing guinea pig H1 receptorsDisplacement of [3H]mepyramine bound to membranes of CHO cells expressing guinea pig H1 receptors
ChEMBL 240 7 3 2 2.0 CC/N=C(\S)NCCCCCc1c[nH]cn1 10.1021/jm00012a025
CHEMBL72424 204481 0 None -1584 4 Guinea pig 4.8 pKi = 4.8 Binding
Displacement of [3H]mepyramine bound to membranes of CHO cells expressing guinea pig H1 receptorsDisplacement of [3H]mepyramine bound to membranes of CHO cells expressing guinea pig H1 receptors
ChEMBL 240 7 3 2 2.0 CC/N=C(\S)NCCCCCc1c[nH]cn1 10.1021/jm00012a025
164627020 186408 0 None -363 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 422 7 4 4 3.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4876025 186408 0 None -363 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 422 7 4 4 3.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
25271818 12967 58 None -1 2 Guinea pig 7.8 pKi = 7.8 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 337 5 1 3 3.6 CN(C)CC/C=C1/c2ccccc2COc2ccc(CC(=O)O)cc21 10.1021/jm00089a020
5281071 12967 58 None -1 2 Guinea pig 7.8 pKi = 7.8 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 337 5 1 3 3.6 CN(C)CC/C=C1/c2ccccc2COc2ccc(CC(=O)O)cc21 10.1021/jm00089a020
CHEMBL1189432 12967 58 None -1 2 Guinea pig 7.8 pKi = 7.8 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 337 5 1 3 3.6 CN(C)CC/C=C1/c2ccccc2COc2ccc(CC(=O)O)cc21 10.1021/jm00089a020
CHEMBL1719 12967 58 None -1 2 Guinea pig 7.8 pKi = 7.8 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 337 5 1 3 3.6 CN(C)CC/C=C1/c2ccccc2COc2ccc(CC(=O)O)cc21 10.1021/jm00089a020
44622869 197717 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation counting
ChEMBL 371 5 1 2 5.1 Cc1ccc(CN2CCC(C(O)(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2009.07.047
CHEMBL571390 197717 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation counting
ChEMBL 371 5 1 2 5.1 Cc1ccc(CN2CCC(C(O)(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2009.07.047
71151588 118258 0 None -1584 10 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in HEK-293 cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in HEK-293 cells
ChEMBL 518 9 1 7 3.6 NC(=O)c1ccccc1OCCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2014.12.045
CHEMBL3409256 118258 0 None -1584 10 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in HEK-293 cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in HEK-293 cells
ChEMBL 518 9 1 7 3.6 NC(=O)c1ccccc1OCCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2014.12.045
14885632 21003 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 348 1 0 3 3.6 COc1ccc2c(c1)CCc1cccnc1C2=C1CCN(C(C)=O)CC1 10.1021/jm00105a069
CHEMBL131155 21003 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 348 1 0 3 3.6 COc1ccc2c(c1)CCc1cccnc1C2=C1CCN(C(C)=O)CC1 10.1021/jm00105a069
44334235 4631 0 None -1445 3 Human 4.8 pKi = 4.8 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 442 10 1 5 3.4 Cc1ccccc1S(=O)(=O)N[C@H]1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)C1 10.1016/s0960-894x(02)00685-6
CHEMBL102929 4631 0 None -1445 3 Human 4.8 pKi = 4.8 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 442 10 1 5 3.4 Cc1ccccc1S(=O)(=O)N[C@H]1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)C1 10.1016/s0960-894x(02)00685-6
53318873 57764 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 360 7 0 5 4.1 C[C@H](C1=C(CCN(C)Cc2ncco2)Cc2ccccc21)c1cnccn1 10.1016/j.bmcl.2010.12.053
CHEMBL1669421 57764 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 360 7 0 5 4.1 C[C@H](C1=C(CCN(C)Cc2ncco2)Cc2ccccc21)c1cnccn1 10.1016/j.bmcl.2010.12.053
44335389 5167 0 None 3 3 Human 6.8 pKi = 6.8 Binding
Binding affinity at human cortical Histamine 1 receptorBinding affinity at human cortical Histamine 1 receptor
ChEMBL 413 8 0 6 3.8 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccccc3[N+](=O)[O-])cc2)CC1 10.1016/s0960-894x(02)00648-0
CHEMBL105952 5167 0 None 3 3 Human 6.8 pKi = 6.8 Binding
Binding affinity at human cortical Histamine 1 receptorBinding affinity at human cortical Histamine 1 receptor
ChEMBL 413 8 0 6 3.8 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccccc3[N+](=O)[O-])cc2)CC1 10.1016/s0960-894x(02)00648-0
168277076 190474 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 755 21 6 8 2.3 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5178882 190474 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 755 21 6 8 2.3 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
44304014 100785 0 None -1905 3 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 431 10 1 6 2.3 CC(C)(C)OC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL293033 100785 0 None -1905 3 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 431 10 1 6 2.3 CC(C)(C)OC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
168277076 190474 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 755 21 6 8 2.3 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5178882 190474 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 755 21 6 8 2.3 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
155528188 171321 0 None - 1 Guinea pig 6.8 pKi = 6.8 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysisDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysis
ChEMBL 316 5 0 3 3.0 CC1CCCCN1CCCOc1ccc2c(c1)C(=O)N(C)CC2 10.1016/j.bmcl.2019.04.015
CHEMBL4461154 171321 0 None - 1 Guinea pig 6.8 pKi = 6.8 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysisDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysis
ChEMBL 316 5 0 3 3.0 CC1CCCCN1CCCOc1ccc2c(c1)C(=O)N(C)CC2 10.1016/j.bmcl.2019.04.015
44304475 202767 0 None -309 3 Human 5.8 pKi = 5.8 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 348 8 0 5 2.8 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)CC)cc2)CC1 10.1016/s0960-894x(02)00309-8
CHEMBL62066 202767 0 None -309 3 Human 5.8 pKi = 5.8 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 348 8 0 5 2.8 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)CC)cc2)CC1 10.1016/s0960-894x(02)00309-8
164611757 184903 0 None -22 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 402 8 4 4 2.8 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4853107 184903 0 None -22 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 402 8 4 4 2.8 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1 10.1016/j.ejmech.2021.113190
44304451 102290 0 None -977 3 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 417 12 1 5 3.3 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](N)C(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
CHEMBL303369 102290 0 None -977 3 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 417 12 1 5 3.3 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](N)C(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
71525681 89728 0 None -2041 6 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]histamine from human histamine H1 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H1 receptor expressed in HEK cells
ChEMBL 298 3 2 6 1.7 CNC1CN(c2nc(N)nc3cc(C4CCCC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
CHEMBL2376803 89728 0 None -2041 6 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]histamine from human histamine H1 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H1 receptor expressed in HEK cells
ChEMBL 298 3 2 6 1.7 CNC1CN(c2nc(N)nc3cc(C4CCCC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
71528209 86972 0 None -257 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 465 6 0 3 5.8 CC1=CC(C)=[N+]2C1=C(c1ccc(OCCCN3CCCCC3)cc1)c1c(C)cc(C)n1[B-]2(F)F 10.1021/ml300383n
CHEMBL2323582 86972 0 None -257 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 465 6 0 3 5.8 CC1=CC(C)=[N+]2C1=C(c1ccc(OCCCN3CCCCC3)cc1)c1c(C)cc(C)n1[B-]2(F)F 10.1021/ml300383n
44209480 70170 0 None -151 11 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]pyrilamine from human H1 receptor by liquid scintillation countingDisplacement of [3H]pyrilamine from human H1 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940418 70170 0 None -151 11 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]pyrilamine from human H1 receptor by liquid scintillation countingDisplacement of [3H]pyrilamine from human H1 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
3015863 199757 10 None 1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cellsDisplacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cells
ChEMBL 225 5 1 1 3.6 NCCCC(c1ccccc1)c1ccccc1 10.1016/j.bmc.2009.08.016
CHEMBL593734 199757 10 None 1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cellsDisplacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cells
ChEMBL 225 5 1 1 3.6 NCCCC(c1ccccc1)c1ccccc1 10.1016/j.bmc.2009.08.016
57402471 67876 0 None -15 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
ChEMBL 469 8 1 5 4.0 COc1ccc(CN(CCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
CHEMBL1910378 67876 0 None -15 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
ChEMBL 469 8 1 5 4.0 COc1ccc(CN(CCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
44304415 202028 0 None -7079 3 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 505 13 2 7 3.2 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](CO)NC(=O)OC(C)(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
CHEMBL60837 202028 0 None -7079 3 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 505 13 2 7 3.2 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](CO)NC(=O)OC(C)(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
44304431 202941 0 None -724 3 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 566 14 1 7 4.9 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](Cc3ccncc3)NC(=O)OC(C)(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
CHEMBL62903 202941 0 None -724 3 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 566 14 1 7 4.9 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](Cc3ccncc3)NC(=O)OC(C)(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
164619208 185662 0 None -588 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 378 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccccc1F 10.1016/j.ejmech.2021.113190
CHEMBL4864852 185662 0 None -588 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 378 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccccc1F 10.1016/j.ejmech.2021.113190
135398737 958 93 None 2 89 Human 7.8 pKi = 7.8 Binding
Binding affinity against histamine H1 receptorBinding affinity against histamine H1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0002432
38 958 93 None 2 89 Human 7.8 pKi = 7.8 Binding
Binding affinity against histamine H1 receptorBinding affinity against histamine H1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0002432
722 958 93 None 2 89 Human 7.8 pKi = 7.8 Binding
Binding affinity against histamine H1 receptorBinding affinity against histamine H1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0002432
CHEMBL42 958 93 None 2 89 Human 7.8 pKi = 7.8 Binding
Binding affinity against histamine H1 receptorBinding affinity against histamine H1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0002432
DB00363 958 93 None 2 89 Human 7.8 pKi = 7.8 Binding
Binding affinity against histamine H1 receptorBinding affinity against histamine H1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0002432
46884155 8326 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 324 5 0 3 4.9 Cc1ncccc1[C@@H](C)c1c(CCN(C)C)sc2ccccc12 10.1016/j.bmcl.2010.01.134
CHEMBL1092813 8326 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 324 5 0 3 4.9 Cc1ncccc1[C@@H](C)c1c(CCN(C)C)sc2ccccc12 10.1016/j.bmcl.2010.01.134
10075223 23190 0 None - 1 Guinea pig 7.8 pKi = 7.8 Binding
Inhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptorInhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptor
ChEMBL 515 8 1 4 6.7 CC(C)(C(=O)O)c1ccc2c(c1)C(SCCN1CCC(Cc3ccccc3)CC1)c1ccccc1CO2 10.1021/jm00055a013
CHEMBL133127 23190 0 None - 1 Guinea pig 7.8 pKi = 7.8 Binding
Inhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptorInhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptor
ChEMBL 515 8 1 4 6.7 CC(C)(C(=O)O)c1ccc2c(c1)C(SCCN1CCC(Cc3ccccc3)CC1)c1ccccc1CO2 10.1021/jm00055a013
44389302 122933 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for human Histamine H1 receptor in CHO K1 cellsBinding affinity for human Histamine H1 receptor in CHO K1 cells
ChEMBL 653 13 1 6 7.3 O=C(OCc1ccccc1)N(O)CCC#Cc1ccc(OCCCCN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2004.12.023
CHEMBL360666 122933 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for human Histamine H1 receptor in CHO K1 cellsBinding affinity for human Histamine H1 receptor in CHO K1 cells
ChEMBL 653 13 1 6 7.3 O=C(OCc1ccccc1)N(O)CCC#Cc1ccc(OCCCCN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2004.12.023
135356876 174074 0 None 7 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to human H1 histamine receptor expressed in HEK cells by PDSP assayBinding affinity to human H1 histamine receptor expressed in HEK cells by PDSP assay
ChEMBL 464 5 2 6 5.5 O=C(O)c1cc(-c2ccc(C3CCNCC3)cc2)cc(-n2cc(-c3ccc(Cl)s3)nn2)c1 10.1021/acs.jmedchem.6b00044
CHEMBL4544251 174074 0 None 7 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to human H1 histamine receptor expressed in HEK cells by PDSP assayBinding affinity to human H1 histamine receptor expressed in HEK cells by PDSP assay
ChEMBL 464 5 2 6 5.5 O=C(O)c1cc(-c2ccc(C3CCNCC3)cc2)cc(-n2cc(-c3ccc(Cl)s3)nn2)c1 10.1021/acs.jmedchem.6b00044
14554127 113325 0 None -3 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting method
ChEMBL 380 2 0 2 5.1 CCCC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/jm501086v
CHEMBL331603 113325 0 None -3 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting method
ChEMBL 380 2 0 2 5.1 CCCC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/jm501086v
5624 32693 14 None -5 10 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 520 5 1 8 4.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2 nan
CHEMBL1203324 32693 14 None -5 10 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 520 5 1 8 4.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2 nan
CHEMBL141343 32693 14 None -5 10 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 520 5 1 8 4.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2 nan
57345617 70456 0 None -186 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-Pyrilamine from human histamine H1 receptor by liquid scintillation counterDisplacement of [3H]-Pyrilamine from human histamine H1 receptor by liquid scintillation counter
ChEMBL 387 6 1 2 5.3 OC1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2CCCCc1ccc(F)cc1 10.1016/j.bmc.2012.01.022
CHEMBL1946123 70456 0 None -186 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-Pyrilamine from human histamine H1 receptor by liquid scintillation counterDisplacement of [3H]-Pyrilamine from human histamine H1 receptor by liquid scintillation counter
ChEMBL 387 6 1 2 5.3 OC1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2CCCCc1ccc(F)cc1 10.1016/j.bmc.2012.01.022
76518514 113537 0 None -186 9 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation countingDisplacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation counting
ChEMBL 387 6 1 2 5.3 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCCc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
CHEMBL3321788 113537 0 None -186 9 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation countingDisplacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation counting
ChEMBL 387 6 1 2 5.3 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCCc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
168290077 191413 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 786 21 7 9 1.3 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5192678 191413 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 786 21 7 9 1.3 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
44304319 202634 0 None -194 3 Human 5.8 pKi = 5.8 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 373 9 1 5 1.8 C[C@H](CN)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL61288 202634 0 None -194 3 Human 5.8 pKi = 5.8 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 373 9 1 5 1.8 C[C@H](CN)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
132075278 162644 0 None -30 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-Pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 308 3 0 3 3.1 c1ccc(CN2CCc3cc(N4CCOCC4)ccc3C2)cc1 10.1016/j.ejmech.2018.02.024
CHEMBL4169752 162644 0 None -30 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-Pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 308 3 0 3 3.1 c1ccc(CN2CCc3cc(N4CCOCC4)ccc3C2)cc1 10.1016/j.ejmech.2018.02.024
168290077 191413 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 786 21 7 9 1.3 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5192678 191413 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 786 21 7 9 1.3 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
10354158 52138 0 None -5 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cellsDisplacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cells
ChEMBL 237 3 1 1 3.5 NCCCC1c2ccccc2Cc2ccccc21 10.1016/j.bmc.2009.08.016
CHEMBL158780 52138 0 None -5 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cellsDisplacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cells
ChEMBL 237 3 1 1 3.5 NCCCC1c2ccccc2Cc2ccccc21 10.1016/j.bmc.2009.08.016
155536609 172219 0 None - 1 Guinea pig 6.8 pKi = 6.8 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysisDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysis
ChEMBL 316 5 0 4 1.7 CN1CCc2ccc(OCCCN3CCC(=O)CC3)cc2C1=O 10.1016/j.bmcl.2019.04.015
CHEMBL4474007 172219 0 None - 1 Guinea pig 6.8 pKi = 6.8 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysisDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysis
ChEMBL 316 5 0 4 1.7 CN1CCc2ccc(OCCCN3CCC(=O)CC3)cc2C1=O 10.1016/j.bmcl.2019.04.015
127051843 140751 0 None -7 9 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 0 3 3.6 N#Cc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818200 140751 0 None -7 9 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 0 3 3.6 N#Cc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
44304288 102207 0 None -831 3 Human 5.8 pKi = 5.8 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 386 11 0 4 3.8 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)C3CC3)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL302886 102207 0 None -831 3 Human 5.8 pKi = 5.8 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 386 11 0 4 3.8 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)C3CC3)CC2)cc1 10.1016/s0960-894x(02)00309-8
46967967 120817 5 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 299 4 0 4 3.4 c1cnc2c(c1)cc([C@@H]1CCCO1)n2CCN1CCCCC1 10.1021/jm2011589
CHEMBL3557423 120817 5 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 299 4 0 4 3.4 c1cnc2c(c1)cc([C@@H]1CCCO1)n2CCN1CCCCC1 10.1021/jm2011589
12488 1657 56 None -2 23 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
941361 1657 56 None -2 23 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
CHEMBL30008 1657 56 None -2 23 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
DB04841 1657 56 None -2 23 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
132356 14677 1 None - 1 Guinea pig 7.8 pKi = 7.8 Binding
Inhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptorInhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptor
ChEMBL 473 7 1 4 6.1 O=C(O)c1ccc2c(c1)C(SCCN1CCC(Cc3ccccc3)CC1)c1ccccc1CO2 10.1021/jm00055a013
CHEMBL1205688 14677 1 None - 1 Guinea pig 7.8 pKi = 7.8 Binding
Inhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptorInhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptor
ChEMBL 473 7 1 4 6.1 O=C(O)c1ccc2c(c1)C(SCCN1CCC(Cc3ccccc3)CC1)c1ccccc1CO2 10.1021/jm00055a013
CHEMBL133778 14677 1 None - 1 Guinea pig 7.8 pKi = 7.8 Binding
Inhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptorInhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptor
ChEMBL 473 7 1 4 6.1 O=C(O)c1ccc2c(c1)C(SCCN1CCC(Cc3ccccc3)CC1)c1ccccc1CO2 10.1021/jm00055a013
135458410 167189 0 None -3 6 Human 7.7 pKi = 7.7 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 293 2 2 3 3.5 CC1NC(NCC(F)F)=Nc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL429136 167189 0 None -3 6 Human 7.7 pKi = 7.7 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 293 2 2 3 3.5 CC1NC(NCC(F)F)=Nc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2007.10.078
45272070 195284 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 375 4 0 5 4.3 Fc1ccc(Cn2c(N3CCC(n4cccn4)CC3)nc3ccccc32)cc1 10.1016/j.bmcl.2009.05.086
CHEMBL551347 195284 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 375 4 0 5 4.3 Fc1ccc(Cn2c(N3CCC(n4cccn4)CC3)nc3ccccc32)cc1 10.1016/j.bmcl.2009.05.086
4806 4008 88 None -5 13 Human 6.8 pKi = 6.8 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
7351 4008 88 None -5 13 Human 6.8 pKi = 6.8 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
9966051 4008 88 None -5 13 Human 6.8 pKi = 6.8 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
CHEMBL2104993 4008 88 None -5 13 Human 6.8 pKi = 6.8 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
DB09068 4008 88 None -5 13 Human 6.8 pKi = 6.8 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
44312748 204765 0 None - 1 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cellsIn vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 496 7 2 5 3.8 NC(=O)N(O)CCC#C[C@H]1CC[C@H](CN2CCN([C@H](c3ccccc3)c3ccc(Cl)cc3)CC2)O1 10.1016/j.bmcl.2004.02.005
CHEMBL74688 204765 0 None - 1 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cellsIn vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 496 7 2 5 3.8 NC(=O)N(O)CCC#C[C@H]1CC[C@H](CN2CCN([C@H](c3ccccc3)c3ccc(Cl)cc3)CC2)O1 10.1016/j.bmcl.2004.02.005
44335185 107391 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 446 7 0 4 4.7 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(Br)cc3)cc2)CC1 10.1016/s0960-894x(02)00648-0
CHEMBL317900 107391 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 446 7 0 4 4.7 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(Br)cc3)cc2)CC1 10.1016/s0960-894x(02)00648-0
168294445 193010 0 None 1 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 414 6 4 4 2.6 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCC2CCc3nc(N)sc3C2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5208113 193010 0 None 1 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 414 6 4 4 2.6 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCC2CCc3nc(N)sc3C2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222768 193010 0 None 1 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 414 6 4 4 2.6 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCC2CCc3nc(N)sc3C2)cc1 10.1021/acs.jmedchem.1c00692
168273471 192801 0 None -12 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 596 17 8 10 0.7 N/C(=N\C(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5173079 192801 0 None -12 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 596 17 8 10 0.7 N/C(=N\C(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221433 192801 0 None -12 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 596 17 8 10 0.7 N/C(=N\C(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168273549 192803 0 None -1 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 436 6 4 4 4.3 Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5174342 192803 0 None -1 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 436 6 4 4 4.3 Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5221438 192803 0 None -1 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 436 6 4 4 4.3 Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1 10.1021/acs.jmedchem.1c00692
76325295 105476 0 None -234 4 Guinea pig 5.7 pKi = 5.7 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation counting
ChEMBL 490 7 0 6 5.9 Cc1c(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)ccc2c3c(c(=O)oc12)CCC3 10.1016/j.ejmech.2014.01.012
CHEMBL3120696 105476 0 None -234 4 Guinea pig 5.7 pKi = 5.7 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation counting
ChEMBL 490 7 0 6 5.9 Cc1c(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)ccc2c3c(c(=O)oc12)CCC3 10.1016/j.ejmech.2014.01.012
168288713 191377 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 799 23 7 9 2.0 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5192305 191377 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 799 23 7 9 2.0 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
168288713 191377 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 799 23 7 9 2.0 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5192305 191377 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 799 23 7 9 2.0 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
127026018 137492 0 None 3 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 399 5 1 5 3.6 CN1CCN(c2nc(NCCc3ccccc3)nc3c2-c2ccccc2CC3)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3753985 137492 0 None 3 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 399 5 1 5 3.6 CN1CCN(c2nc(NCCc3ccccc3)nc3c2-c2ccccc2CC3)CC1 10.1016/j.bmcl.2015.12.035
95198280 162091 0 None -1 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 351 5 1 5 3.4 Cc1oc(-c2ccc3ccccc3c2)nc1CN1CCO[C@H](CCN)C1 10.1021/acs.jmedchem.8b00718
CHEMBL4160967 162091 0 None -1 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 351 5 1 5 3.4 Cc1oc(-c2ccc3ccccc3c2)nc1CN1CCO[C@H](CCN)C1 10.1021/acs.jmedchem.8b00718
57403981 70495 0 None -14 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-Pyrilamine from human histamine H1 receptor by liquid scintillation counterDisplacement of [3H]-Pyrilamine from human histamine H1 receptor by liquid scintillation counter
ChEMBL 426 6 1 4 5.8 OC1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2CCCCc1nc2ccccc2s1 10.1016/j.bmc.2012.01.022
CHEMBL1946745 70495 0 None -14 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-Pyrilamine from human histamine H1 receptor by liquid scintillation counterDisplacement of [3H]-Pyrilamine from human histamine H1 receptor by liquid scintillation counter
ChEMBL 426 6 1 4 5.8 OC1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2CCCCc1nc2ccccc2s1 10.1016/j.bmc.2012.01.022
11653679 181191 1 None -28 11 Human 6.7 pKi = 6.7 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 374 6 0 3 4.7 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL476108 181191 1 None -28 11 Human 6.7 pKi = 6.7 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 374 6 0 3 4.7 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
10251906 2743 18 None -1548 8 Human 6.7 pKi = 6.7 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 427 8 1 4 3.6 IC1=CC(=C(C=C1OC)CCNCC2=C(C=CC=C2)OC)OC 10.1016/j.bmc.2008.04.050
13550 2743 18 None -1548 8 Human 6.7 pKi = 6.7 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 427 8 1 4 3.6 IC1=CC(=C(C=C1OC)CCNCC2=C(C=CC=C2)OC)OC 10.1016/j.bmc.2008.04.050
CHEMBL1908863 2743 18 None -1548 8 Human 6.7 pKi = 6.7 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 427 8 1 4 3.6 IC1=CC(=C(C=C1OC)CCNCC2=C(C=CC=C2)OC)OC 10.1016/j.bmc.2008.04.050
44313266 204613 0 None -3 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cellsDisplacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cells
ChEMBL 223 2 1 1 2.9 CNCC1c2ccccc2Cc2ccccc21 10.1016/j.bmc.2009.08.016
CHEMBL73307 204613 0 None -3 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cellsDisplacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cells
ChEMBL 223 2 1 1 2.9 CNCC1c2ccccc2Cc2ccccc21 10.1016/j.bmc.2009.08.016
9842252 131443 18 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for H1 histamine receptor expressed in CHO cellsBinding affinity for H1 histamine receptor expressed in CHO cells
ChEMBL 296 1 2 4 1.2 NC(=O)c1cnc2n1CCc1ccccc1C21CCNCC1 10.1021/jm049495j
CHEMBL369075 131443 18 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for H1 histamine receptor expressed in CHO cellsBinding affinity for H1 histamine receptor expressed in CHO cells
ChEMBL 296 1 2 4 1.2 NC(=O)c1cnc2n1CCc1ccccc1C21CCNCC1 10.1021/jm049495j
CHEMBL539843 131443 18 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for H1 histamine receptor expressed in CHO cellsBinding affinity for H1 histamine receptor expressed in CHO cells
ChEMBL 296 1 2 4 1.2 NC(=O)c1cnc2n1CCc1ccccc1C21CCNCC1 10.1021/jm049495j
2389 3331 118 None -46 67 Human 7.7 pKi = 7.7 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmc.2008.06.030
5073 3331 118 None -46 67 Human 7.7 pKi = 7.7 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmc.2008.06.030
96 3331 118 None -46 67 Human 7.7 pKi = 7.7 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmc.2008.06.030
CHEMBL85 3331 118 None -46 67 Human 7.7 pKi = 7.7 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmc.2008.06.030
DB00734 3331 118 None -46 67 Human 7.7 pKi = 7.7 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmc.2008.06.030
2337 3256 77 None 1 62 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human histamine H1 receptorBinding affinity towards human histamine H1 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm030480f
50 3256 77 None 1 62 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human histamine H1 receptorBinding affinity towards human histamine H1 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm030480f
5002 3256 77 None 1 62 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human histamine H1 receptorBinding affinity towards human histamine H1 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm030480f
CHEMBL716 3256 77 None 1 62 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human histamine H1 receptorBinding affinity towards human histamine H1 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm030480f
DB01224 3256 77 None 1 62 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human histamine H1 receptorBinding affinity towards human histamine H1 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm030480f
9872445 66779 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human histamine H1 receptor expressed in CHO-K1 cellsBinding affinity towards human histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 556 6 2 5 5.3 NC(=O)N(O)CCC#Cc1ccc(OCCN2CCC(=C3c4ccc(Cl)cc4CCc4cccnc43)CC2)cc1 10.1016/j.bmcl.2004.08.060
CHEMBL185905 66779 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human histamine H1 receptor expressed in CHO-K1 cellsBinding affinity towards human histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 556 6 2 5 5.3 NC(=O)N(O)CCC#Cc1ccc(OCCN2CCC(=C3c4ccc(Cl)cc4CCc4cccnc43)CC2)cc1 10.1016/j.bmcl.2004.08.060
1588 2325 27 None -35 44 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
28864 2325 27 None -35 44 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
43 2325 27 None -35 44 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
CHEMBL157138 2325 27 None -35 44 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
DB00589 2325 27 None -35 44 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
56820088 162118 4 None 169 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 340 4 0 6 3.5 c1ccc(-c2nc(CN3CCCN(c4nccs4)CC3)co2)cc1 10.1021/acs.jmedchem.8b00718
CHEMBL4161436 162118 4 None 169 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 340 4 0 6 3.5 c1ccc(-c2nc(CN3CCCN(c4nccs4)CC3)co2)cc1 10.1021/acs.jmedchem.8b00718
59652086 114592 0 None 85 2 Human 7.7 pKi = 7.7 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000726a HRH1Selectivity interaction (GPCR panel (PDSP screen)) EUB0000726a HRH1
ChEMBL 448 8 2 6 3.6 COc1cccc(CNC(=O)c2nc3scc(CN(C)Cc4ccccc4)c3c(=O)[nH]2)c1 10.6019/CHEMBL5212743
CHEMBL3337895 114592 0 None 85 2 Human 7.7 pKi = 7.7 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000726a HRH1Selectivity interaction (GPCR panel (PDSP screen)) EUB0000726a HRH1
ChEMBL 448 8 2 6 3.6 COc1cccc(CNC(=O)c2nc3scc(CN(C)Cc4ccccc4)c3c(=O)[nH]2)c1 10.6019/CHEMBL5212743
44288945 168915 0 None -47 7 Human 7.7 pKi = 7.7 Binding
Selectivity screen against human Histamine H1 receptorSelectivity screen against human Histamine H1 receptor
ChEMBL 485 7 2 3 4.4 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1 10.1016/s0960-894x(99)00696-4
CHEMBL43860 168915 0 None -47 7 Human 7.7 pKi = 7.7 Binding
Selectivity screen against human Histamine H1 receptorSelectivity screen against human Histamine H1 receptor
ChEMBL 485 7 2 3 4.4 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1 10.1016/s0960-894x(99)00696-4
57334102 90508 0 None -5 5 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysisDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysis
ChEMBL 450 7 0 6 5.4 Cc1cc(=O)oc2cc(OCCCCN3CCC(c4noc5cc(F)ccc45)CC3)ccc12 10.1021/jm400408r
CHEMBL2387260 90508 0 None -5 5 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysisDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysis
ChEMBL 450 7 0 6 5.4 Cc1cc(=O)oc2cc(OCCCCN3CCC(c4noc5cc(F)ccc45)CC3)ccc12 10.1021/jm400408r
71462102 81288 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 478 7 1 5 4.4 O=C(O)C(c1ccccc1)N1CCO[C@@H](CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.08.103
CHEMBL2158817 81288 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 478 7 1 5 4.4 O=C(O)C(c1ccccc1)N1CCO[C@@H](CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.08.103
71456725 81298 1 None 1 2 Human 7.7 pKi = 7.7 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 476 7 1 4 5.4 O=C(O)Cc1ccc(N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.103
CHEMBL2158827 81298 1 None 1 2 Human 7.7 pKi = 7.7 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 476 7 1 4 5.4 O=C(O)Cc1ccc(N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.103
71463288 84204 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 441 8 1 5 5.0 COc1cccc(SC[C@@H](O)CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)c1 10.1016/j.bmcl.2012.09.113
CHEMBL2208421 84204 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 441 8 1 5 5.0 COc1cccc(SC[C@@H](O)CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)c1 10.1016/j.bmcl.2012.09.113
59296064 84206 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 447 7 2 5 3.5 N#Cc1cccc(C(=O)NC[C@@H](O)CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)c1 10.1016/j.bmcl.2012.09.113
CHEMBL2208423 84206 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 447 7 2 5 3.5 N#Cc1cccc(C(=O)NC[C@@H](O)CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)c1 10.1016/j.bmcl.2012.09.113
59296000 84215 0 None -7 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 478 6 3 6 3.1 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)n1c(=O)[nH]c2ccccc21 10.1016/j.bmcl.2012.09.113
CHEMBL2208432 84215 0 None -7 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 478 6 3 6 3.1 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)n1c(=O)[nH]c2ccccc21 10.1016/j.bmcl.2012.09.113
59295982 84014 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 568 8 4 7 2.1 NS(=O)(=O)c1ccc2c(C(=O)NC[C@@H](O)CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)c[nH]c(=O)c2c1 10.1016/j.bmcl.2012.09.112
CHEMBL2207282 84014 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 568 8 4 7 2.1 NS(=O)(=O)c1ccc2c(C(=O)NC[C@@H](O)CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)c[nH]c(=O)c2c1 10.1016/j.bmcl.2012.09.112
59295925 84101 0 None -2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 567 8 3 7 2.9 CS(=O)(=O)c1ccc2c(C(=O)NC[C@@H](O)CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)c[nH]c(=O)c2c1 10.1016/j.bmcl.2012.09.112
CHEMBL2207671 84101 0 None -2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 567 8 3 7 2.9 CS(=O)(=O)c1ccc2c(C(=O)NC[C@@H](O)CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)c[nH]c(=O)c2c1 10.1016/j.bmcl.2012.09.112
71723301 91009 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 392 1 0 2 6.1 Clc1ccc2c(c1)CCc1cccnc1C2=C1CCN(C2CCCCC2)CC1 10.1021/acs.jmedchem.9b00447
CHEMBL2396897 91009 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 392 1 0 2 6.1 Clc1ccc2c(c1)CCc1cccnc1C2=C1CCN(C2CCCCC2)CC1 10.1021/acs.jmedchem.9b00447
25147772 173409 9 None -6 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in NIH3T3 cellsDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in NIH3T3 cells
ChEMBL 373 4 1 6 3.7 CN1CCN(c2nc(NCc3cccs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL452847 173409 9 None -6 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in NIH3T3 cellsDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in NIH3T3 cells
ChEMBL 373 4 1 6 3.7 CN1CCN(c2nc(NCc3cccs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
134151839 152978 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 323 7 0 2 4.9 c1ccc(Cc2ccccc2OCCCN2CCCCCC2)cc1 10.1021/acs.jmedchem.6b00981
CHEMBL3975229 152978 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 323 7 0 2 4.9 c1ccc(Cc2ccccc2OCCCN2CCCCCC2)cc1 10.1021/acs.jmedchem.6b00981
49836637 18678 0 None 1 4 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]pyrilamine from histamine H1 receptor in Sprague-Dawley rat cortical membrane by liquid scintillation countingDisplacement of [3H]pyrilamine from histamine H1 receptor in Sprague-Dawley rat cortical membrane by liquid scintillation counting
ChEMBL 375 2 1 3 4.5 O=C(O)C1=CCN(C2CCC3(Cc4ccccc4Oc4ccccc43)C2)CC1 10.1021/jm100856p
CHEMBL1277126 18678 0 None 1 4 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]pyrilamine from histamine H1 receptor in Sprague-Dawley rat cortical membrane by liquid scintillation countingDisplacement of [3H]pyrilamine from histamine H1 receptor in Sprague-Dawley rat cortical membrane by liquid scintillation counting
ChEMBL 375 2 1 3 4.5 O=C(O)C1=CCN(C2CCC3(Cc4ccccc4Oc4ccccc43)C2)CC1 10.1021/jm100856p
71458868 82232 0 None -6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 568 6 1 6 4.8 Cc1c(Cl)ccc(OC2CCN(C3CCN(C(=O)NS(=O)(=O)c4ccc(N(C)C)cc4)CC3)CC2)c1Cl 10.1016/j.bmcl.2012.08.124
CHEMBL2171014 82232 0 None -6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 568 6 1 6 4.8 Cc1c(Cl)ccc(OC2CCN(C3CCN(C(=O)NS(=O)(=O)c4ccc(N(C)C)cc4)CC3)CC2)c1Cl 10.1016/j.bmcl.2012.08.124
17963363 82254 0 None -2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 545 5 1 5 5.1 O=C(NS(=O)(=O)c1ccc(Cl)cc1)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
CHEMBL2171035 82254 0 None -2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 545 5 1 5 5.1 O=C(NS(=O)(=O)c1ccc(Cl)cc1)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
17963196 82255 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 541 6 1 6 4.4 COc1ccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.124
CHEMBL2171036 82255 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 541 6 1 6 4.4 COc1ccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.124
17963258 82256 0 None 2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 554 6 1 6 4.5 CN(C)c1ccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.124
CHEMBL2171037 82256 0 None 2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 554 6 1 6 4.5 CN(C)c1ccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.124
17963332 82259 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 541 6 1 6 4.4 COc1ccccc1S(=O)(=O)NC(=O)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
CHEMBL2171040 82259 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 541 6 1 6 4.4 COc1ccccc1S(=O)(=O)NC(=O)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
17963336 82263 0 None 5 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 536 5 1 6 4.3 N#Cc1cccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.124
CHEMBL2171044 82263 0 None 5 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 536 5 1 6 4.3 N#Cc1cccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.124
17963201 82266 0 None -31 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 539 5 1 5 5.0 Cc1ccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(C)c4Cl)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.124
CHEMBL2171047 82266 0 None -31 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 539 5 1 5 5.0 Cc1ccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(C)c4Cl)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.124
14885626 32172 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 414 1 0 2 5.6 O=C(c1ccccc1)N1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/jm00105a069
CHEMBL140924 32172 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 414 1 0 2 5.6 O=C(c1ccccc1)N1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/jm00105a069
14885631 34940 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 332 0 0 2 3.9 CC(=O)N1CCC(=C2c3ccc(C)cc3CCc3cccnc32)CC1 10.1021/jm00105a069
CHEMBL143242 34940 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 332 0 0 2 3.9 CC(=O)N1CCC(=C2c3ccc(C)cc3CCc3cccnc32)CC1 10.1021/jm00105a069
135986088 178115 0 None -57 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 543 7 1 6 6.5 Clc1ccc2c(c1)N=C(N1CCN(Cc3ccc(OCCCN4CCCCC4)cc3)CC1)c1ccccc1N2 10.1016/j.bmcl.2008.09.012
CHEMBL464811 178115 0 None -57 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 543 7 1 6 6.5 Clc1ccc2c(c1)N=C(N1CCN(Cc3ccc(OCCCN4CCCCC4)cc3)CC1)c1ccccc1N2 10.1016/j.bmcl.2008.09.012
44312371 105483 0 None - 1 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cellsIn vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 492 6 2 5 4.4 CC(C#Cc1ccc(CN2CCN([C@H](c3ccccc3)c3ccc(Cl)cc3)CC2)o1)N(O)C(N)=O 10.1016/j.bmcl.2004.02.005
CHEMBL312082 105483 0 None - 1 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cellsIn vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 492 6 2 5 4.4 CC(C#Cc1ccc(CN2CCN([C@H](c3ccccc3)c3ccc(Cl)cc3)CC2)o1)N(O)C(N)=O 10.1016/j.bmcl.2004.02.005
CHEMBL4576555 214017 5 None -1 19 Human 5.7 pKi = 5.7 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000705a HRH1Selectivity interaction (GPCR panel (PDSP screen)) EUB0000705a HRH1
ChEMBL None None None CN1CCN(C(=O)C(C)(C)c2ccc(C(=O)Nc3cn4cc(-c5cc(C(C)(C)C)cc(C(C)(C)C)c5)ccc4n3)cc2)CC1 10.6019/CHEMBL5212743
CHEMBL4576555 214017 5 None -1 19 Human 5.7 pKi = 5.7 Binding
GPCRScan assay: inhibition of H1GPCRScan assay: inhibition of H1
ChEMBL None None None CN1CCN(C(=O)C(C)(C)c2ccc(C(=O)Nc3cn4cc(-c5cc(C(C)(C)C)cc(C(C)(C)C)c5)ccc4n3)cc2)CC1 10.6019/CHEMBL4507307
44304558 101019 0 None -602 3 Human 5.7 pKi = 5.7 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 374 11 0 4 3.8 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)CC)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL294502 101019 0 None -602 3 Human 5.7 pKi = 5.7 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 374 11 0 4 3.8 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)CC)CC2)cc1 10.1016/s0960-894x(02)00309-8
4023 198 24 None -660 4 Human 5.7 pKi = 5.7 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 349 7 0 4 3.6 N#Cc1ccc(cc1)c1ccc(cc1)OCCCN1CC[C@H](C1)N(C)C 10.1016/s0960-894x(02)00648-0
9884746 198 24 None -660 4 Human 5.7 pKi = 5.7 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 349 7 0 4 3.6 N#Cc1ccc(cc1)c1ccc(cc1)OCCCN1CC[C@H](C1)N(C)C 10.1016/s0960-894x(02)00648-0
CHEMBL319000 198 24 None -660 4 Human 5.7 pKi = 5.7 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 349 7 0 4 3.6 N#Cc1ccc(cc1)c1ccc(cc1)OCCCN1CC[C@H](C1)N(C)C 10.1016/s0960-894x(02)00648-0
127026016 137489 0 None 13 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 385 4 1 5 3.6 CN1CCN(c2nc(NCc3ccccc3)nc3c2-c2ccccc2CC3)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3753967 137489 0 None 13 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 385 4 1 5 3.6 CN1CCN(c2nc(NCc3ccccc3)nc3c2-c2ccccc2CC3)CC1 10.1016/j.bmcl.2015.12.035
649745 31482 54 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 303 3 1 7 0.5 C1CCN(c2nc(N3CCCC3)nc(N3CCNCC3)n2)C1 10.1021/jm2011589
CHEMBL1403257 31482 54 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 303 3 1 7 0.5 C1CCN(c2nc(N3CCCC3)nc(N3CCNCC3)n2)C1 10.1021/jm2011589
44304450 202867 0 None -239 3 Human 4.7 pKi = 4.7 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 417 12 1 5 3.3 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](N)C(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
CHEMBL62592 202867 0 None -239 3 Human 4.7 pKi = 4.7 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 417 12 1 5 3.3 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](N)C(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
162665485 182357 0 None -58 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-pyrilamine from human H1 histamine receptor expressed in human HEK293 cellsDisplacement of [3H]-pyrilamine from human H1 histamine receptor expressed in human HEK293 cells
ChEMBL 468 4 0 3 5.3 C[C@H]1CN(CC[C@H]2CC[C@H](N3C(=O)[C@H]4[C@H]5CC[C@H](C5)[C@H]4C3=O)CC2)CCc2ccc(Cl)cc21 10.1016/j.bmcl.2020.127681
CHEMBL4784751 182357 0 None -58 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-pyrilamine from human H1 histamine receptor expressed in human HEK293 cellsDisplacement of [3H]-pyrilamine from human H1 histamine receptor expressed in human HEK293 cells
ChEMBL 468 4 0 3 5.3 C[C@H]1CN(CC[C@H]2CC[C@H](N3C(=O)[C@H]4[C@H]5CC[C@H](C5)[C@H]4C3=O)CC2)CCc2ccc(Cl)cc21 10.1016/j.bmcl.2020.127681
112936357 137359 1 None 18 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 373 6 1 5 3.6 CN1CCN(c2nc(NCCc3ccccc3)cc(-c3ccccc3)n2)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3752978 137359 1 None 18 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 373 6 1 5 3.6 CN1CCN(c2nc(NCCc3ccccc3)cc(-c3ccccc3)n2)CC1 10.1016/j.bmcl.2015.12.035
127035837 137417 0 None 5 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 403 4 1 5 3.7 CN1CCN(c2nc(NCc3ccc(F)cc3)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3753334 137417 0 None 5 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 403 4 1 5 3.7 CN1CCN(c2nc(NCc3ccc(F)cc3)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
164626370 186473 0 None -1 6 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 338 6 4 4 1.8 CCCCCCNC(=O)/N=C(\N)NC1CCc2nc(N)sc2C1 10.1016/j.ejmech.2021.113190
CHEMBL4876799 186473 0 None -1 6 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 338 6 4 4 1.8 CCCCCCNC(=O)/N=C(\N)NC1CCc2nc(N)sc2C1 10.1016/j.ejmech.2021.113190
18382725 116090 27 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting method
ChEMBL 412 2 0 4 4.9 CCOC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3cc(OC)cnc32)CC1 10.1021/jm501086v
CHEMBL3357024 116090 27 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting method
ChEMBL 412 2 0 4 4.9 CCOC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3cc(OC)cnc32)CC1 10.1021/jm501086v
10398175 180091 7 None -6 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cellsDisplacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cells
ChEMBL 209 1 1 1 2.7 NCC1c2ccccc2Cc2ccccc21 10.1016/j.bmc.2009.08.016
CHEMBL47482 180091 7 None -6 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cellsDisplacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cells
ChEMBL 209 1 1 1 2.7 NCC1c2ccccc2Cc2ccccc21 10.1016/j.bmc.2009.08.016
162644910 179411 0 None -18 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cell membranes co-expressing RGS4 measured after 60 mins by scintillation counting analysisDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cell membranes co-expressing RGS4 measured after 60 mins by scintillation counting analysis
ChEMBL 407 7 0 4 5.0 Clc1cccc(-c2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)c1 10.1016/j.ejmech.2020.113041
CHEMBL4740135 179411 0 None -18 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cell membranes co-expressing RGS4 measured after 60 mins by scintillation counting analysisDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cell membranes co-expressing RGS4 measured after 60 mins by scintillation counting analysis
ChEMBL 407 7 0 4 5.0 Clc1cccc(-c2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)c1 10.1016/j.ejmech.2020.113041
46882181 5681 0 None 1 5 Human 6.7 pKi = 6.7 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 536 10 2 8 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(NS(=O)(=O)c5ccccc5)ccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
CHEMBL1077908 5681 0 None 1 5 Human 6.7 pKi = 6.7 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 536 10 2 8 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(NS(=O)(=O)c5ccccc5)ccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
66615691 81277 0 None -125 2 Human 6.7 pKi = 6.7 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 518 8 1 4 5.9 Cc1c(OC2CCN(CC3CCN([C@@](C)(Cc4ccccc4)C(=O)O)CC3)CC2)ccc(Cl)c1Cl 10.1016/j.bmcl.2012.08.103
CHEMBL2158789 81277 0 None -125 2 Human 6.7 pKi = 6.7 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 518 8 1 4 5.9 Cc1c(OC2CCN(CC3CCN([C@@](C)(Cc4ccccc4)C(=O)O)CC3)CC2)ccc(Cl)c1Cl 10.1016/j.bmcl.2012.08.103
59296109 84211 0 None -12 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 500 8 2 6 3.0 CS(=O)(=O)c1ccccc1C(=O)NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1 10.1016/j.bmcl.2012.09.113
CHEMBL2208428 84211 0 None -12 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 500 8 2 6 3.0 CS(=O)(=O)c1ccccc1C(=O)NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1 10.1016/j.bmcl.2012.09.113
127051845 140729 0 None -12 9 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 309 6 0 3 3.7 COc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3817898 140729 0 None -12 9 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 309 6 0 3 3.7 COc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
71462391 82251 0 None 1 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 554 6 1 6 3.9 CS(=O)(=O)c1cccc(C(=O)N2CC[C@@H](N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)[C@H](C(=O)O)C2)c1 10.1016/j.bmcl.2012.08.124
CHEMBL2171032 82251 0 None 1 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 554 6 1 6 3.9 CS(=O)(=O)c1cccc(C(=O)N2CC[C@@H](N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)[C@H](C(=O)O)C2)c1 10.1016/j.bmcl.2012.08.124
46881463 7218 0 None -501 5 Human 5.7 pKi = 5.7 Binding
Activity at histamine H1 receptorActivity at histamine H1 receptor
ChEMBL 293 3 1 2 2.7 O=C1N(CC2CCCCN2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2010.01.090
CHEMBL1085672 7218 0 None -501 5 Human 5.7 pKi = 5.7 Binding
Activity at histamine H1 receptorActivity at histamine H1 receptor
ChEMBL 293 3 1 2 2.7 O=C1N(CC2CCCCN2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2010.01.090
9798145 104133 0 None -3981 2 Human 5.7 pKi = 5.7 Binding
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced effect by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced effect by FLIPR assay
ChEMBL 342 7 0 3 3.8 c1cc2c(cc1OCCCN1CCCCC1)CCN(CC1CC1)CC2 10.1016/j.bmcl.2013.09.089
CHEMBL3094215 104133 0 None -3981 2 Human 5.7 pKi = 5.7 Binding
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced effect by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced effect by FLIPR assay
ChEMBL 342 7 0 3 3.8 c1cc2c(cc1OCCCN1CCCCC1)CCN(CC1CC1)CC2 10.1016/j.bmcl.2013.09.089
10429386 104134 0 None -3981 2 Human 5.7 pKi = 5.7 Binding
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced effect by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced effect by FLIPR assay
ChEMBL 372 7 0 4 3.5 c1cc2c(cc1OCCCN1CCCCC1)CCN(CC1CCCO1)CC2 10.1016/j.bmcl.2013.09.089
CHEMBL3094216 104134 0 None -3981 2 Human 5.7 pKi = 5.7 Binding
Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced effect by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced effect by FLIPR assay
ChEMBL 372 7 0 4 3.5 c1cc2c(cc1OCCCN1CCCCC1)CCN(CC1CCCO1)CC2 10.1016/j.bmcl.2013.09.089
44304294 202963 0 None -9 3 Human 5.7 pKi = 5.7 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 485 10 1 5 3.9 N[C@H](Cc1cccc2ccccc12)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL63003 202963 0 None -9 3 Human 5.7 pKi = 5.7 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 485 10 1 5 3.9 N[C@H](Cc1cccc2ccccc12)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
10565409 52189 0 None -977 2 Guinea pig 4.7 pKi = 4.7 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 290 6 2 5 2.5 O=C(Nc1ccc([N+](=O)[O-])cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL15883 52189 0 None -977 2 Guinea pig 4.7 pKi = 4.7 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 290 6 2 5 2.5 O=C(Nc1ccc([N+](=O)[O-])cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
5250783 169387 3 None -1995 3 Guinea pig 4.7 pKi = 4.7 Binding
Displacement of [3H]mepyramine bound to membranes of CHO cells expressing guinea pig H1 receptorsDisplacement of [3H]mepyramine bound to membranes of CHO cells expressing guinea pig H1 receptors
ChEMBL 226 6 3 2 1.6 C/N=C(\S)NCCCCCc1c[nH]cn1 10.1021/jm00012a025
CHEMBL44220 169387 3 None -1995 3 Guinea pig 4.7 pKi = 4.7 Binding
Displacement of [3H]mepyramine bound to membranes of CHO cells expressing guinea pig H1 receptorsDisplacement of [3H]mepyramine bound to membranes of CHO cells expressing guinea pig H1 receptors
ChEMBL 226 6 3 2 1.6 C/N=C(\S)NCCCCCc1c[nH]cn1 10.1021/jm00012a025
1204 1932 119 None -501 24 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor N7.45C mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor N7.45C mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1038/nchembio714
1247 1932 119 None -501 24 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor N7.45C mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor N7.45C mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1038/nchembio714
1375 1932 119 None -501 24 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor N7.45C mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor N7.45C mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1038/nchembio714
774 1932 119 None -501 24 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor N7.45C mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor N7.45C mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1038/nchembio714
CHEMBL90 1932 119 None -501 24 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor N7.45C mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor N7.45C mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1038/nchembio714
DB05381 1932 119 None -501 24 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor N7.45C mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor N7.45C mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1038/nchembio714
1210 918 51 None -9 21 Rat 8.7 pKi = 8.7 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/s0960-894x(03)00357-3
1213 918 51 None -9 21 Rat 8.7 pKi = 8.7 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/s0960-894x(03)00357-3
2725 918 51 None -9 21 Rat 8.7 pKi = 8.7 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/s0960-894x(03)00357-3
33036 918 51 None -9 21 Rat 8.7 pKi = 8.7 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/s0960-894x(03)00357-3
4411 918 51 None -9 21 Rat 8.7 pKi = 8.7 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/s0960-894x(03)00357-3
616 918 51 None -9 21 Rat 8.7 pKi = 8.7 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/s0960-894x(03)00357-3
6976 918 51 None -9 21 Rat 8.7 pKi = 8.7 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/s0960-894x(03)00357-3
716121 918 51 None -9 21 Rat 8.7 pKi = 8.7 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/s0960-894x(03)00357-3
CHEMBL1201353 918 51 None -9 21 Rat 8.7 pKi = 8.7 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/s0960-894x(03)00357-3
CHEMBL1554789 918 51 None -9 21 Rat 8.7 pKi = 8.7 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/s0960-894x(03)00357-3
CHEMBL505 918 51 None -9 21 Rat 8.7 pKi = 8.7 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/s0960-894x(03)00357-3
DB01114 918 51 None -9 21 Rat 8.7 pKi = 8.7 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/s0960-894x(03)00357-3
DB13679 918 51 None -9 21 Rat 8.7 pKi = 8.7 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/s0960-894x(03)00357-3
135398745 2914 112 None 1 65 Human 8.7 pKi = 8.7 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
47 2914 112 None 1 65 Human 8.7 pKi = 8.7 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
CHEMBL715 2914 112 None 1 65 Human 8.7 pKi = 8.7 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
DB00334 2914 112 None 1 65 Human 8.7 pKi = 8.7 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
1400 1957 70 None 2 3 Human 8.7 pKi = 8.7 Binding
Binding affinity to histamine H1 receptor (unknown origin)Binding affinity to histamine H1 receptor (unknown origin)
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1016/j.bmcl.2018.04.059
3658 1957 70 None 2 3 Human 8.7 pKi = 8.7 Binding
Binding affinity to histamine H1 receptor (unknown origin)Binding affinity to histamine H1 receptor (unknown origin)
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1016/j.bmcl.2018.04.059
7199 1957 70 None 2 3 Human 8.7 pKi = 8.7 Binding
Binding affinity to histamine H1 receptor (unknown origin)Binding affinity to histamine H1 receptor (unknown origin)
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1016/j.bmcl.2018.04.059
91513 1957 70 None 2 3 Human 8.7 pKi = 8.7 Binding
Binding affinity to histamine H1 receptor (unknown origin)Binding affinity to histamine H1 receptor (unknown origin)
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1016/j.bmcl.2018.04.059
CHEMBL896 1957 70 None 2 3 Human 8.7 pKi = 8.7 Binding
Binding affinity to histamine H1 receptor (unknown origin)Binding affinity to histamine H1 receptor (unknown origin)
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1016/j.bmcl.2018.04.059
DB00557 1957 70 None 2 3 Human 8.7 pKi = 8.7 Binding
Binding affinity to histamine H1 receptor (unknown origin)Binding affinity to histamine H1 receptor (unknown origin)
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1016/j.bmcl.2018.04.059
135398745 2914 112 None 1 65 Human 8.7 pKi = 8.7 Binding
Inhibition of histamine H1 receptor (unknown origin)Inhibition of histamine H1 receptor (unknown origin)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm401958n
47 2914 112 None 1 65 Human 8.7 pKi = 8.7 Binding
Inhibition of histamine H1 receptor (unknown origin)Inhibition of histamine H1 receptor (unknown origin)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm401958n
CHEMBL715 2914 112 None 1 65 Human 8.7 pKi = 8.7 Binding
Inhibition of histamine H1 receptor (unknown origin)Inhibition of histamine H1 receptor (unknown origin)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm401958n
DB00334 2914 112 None 1 65 Human 8.7 pKi = 8.7 Binding
Inhibition of histamine H1 receptor (unknown origin)Inhibition of histamine H1 receptor (unknown origin)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm401958n
2247 505 81 None -4 42 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1016/j.bmcl.2011.09.001
249 505 81 None -4 42 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1016/j.bmcl.2011.09.001
2603 505 81 None -4 42 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1016/j.bmcl.2011.09.001
CHEMBL296419 505 81 None -4 42 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1016/j.bmcl.2011.09.001
DB00637 505 81 None -4 42 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1016/j.bmcl.2011.09.001
1227 2489 43 None -2 12 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm2011589
2331 2489 43 None -2 12 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm2011589
3957 2489 43 None -2 12 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm2011589
4992 2489 43 None -2 12 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm2011589
CHEMBL511 2489 43 None -2 12 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm2011589
DB06691 2489 43 None -2 12 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm2011589
11688223 8302 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 313 5 0 3 3.6 CN(C)CCC1=C(Cc2cccnn2)c2ccc(Cl)cc2C1 10.1016/j.bmcl.2010.02.055
CHEMBL1092652 8302 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 313 5 0 3 3.6 CN(C)CCC1=C(Cc2cccnn2)c2ccc(Cl)cc2C1 10.1016/j.bmcl.2010.02.055
135398737 958 93 None 2 89 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human histamine H1 receptorBinding affinity towards human histamine H1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030480f
38 958 93 None 2 89 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human histamine H1 receptorBinding affinity towards human histamine H1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030480f
722 958 93 None 2 89 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human histamine H1 receptorBinding affinity towards human histamine H1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030480f
CHEMBL42 958 93 None 2 89 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human histamine H1 receptorBinding affinity towards human histamine H1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030480f
DB00363 958 93 None 2 89 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human histamine H1 receptorBinding affinity towards human histamine H1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030480f
155561547 175656 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 364 1 0 2 5.3 Clc1ccc2c(c1)CCc1cccnc1C2=C1CCN(C2CCC2)CC1 10.1021/acs.jmedchem.9b00447
CHEMBL4581343 175656 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 364 1 0 2 5.3 Clc1ccc2c(c1)CCc1cccnc1C2=C1CCN(C2CCC2)CC1 10.1021/acs.jmedchem.9b00447
46884639 7725 0 None 6918 2 Human 8.7 pKi = 8.7 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 309 6 0 4 3.0 COc1nccnc1CC1=C(CCN(C)C)Cc2ccccc21 10.1016/j.bmcl.2010.02.055
CHEMBL1088900 7725 0 None 6918 2 Human 8.7 pKi = 8.7 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 309 6 0 4 3.0 COc1nccnc1CC1=C(CCN(C)C)Cc2ccccc21 10.1016/j.bmcl.2010.02.055
46884736 7974 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 312 5 0 3 4.5 Cc1ccc2c(c1)CC(CCN(C)C)=C2[C@@H](C)c1nccs1 10.1016/j.bmcl.2010.02.055
CHEMBL1090528 7974 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 312 5 0 3 4.5 Cc1ccc2c(c1)CC(CCN(C)C)=C2[C@@H](C)c1nccs1 10.1016/j.bmcl.2010.02.055
45272046 195161 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 396 7 0 5 3.8 COCCN(C)C1CCN(c2nc3ccccc3n2Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2009.05.086
CHEMBL550337 195161 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 396 7 0 5 3.8 COCCN(C)C1CCN(c2nc3ccccc3n2Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2009.05.086
1227 2489 43 None -2 12 Human 8.7 pKi = 8.7 Binding
Displacement of radiolabeled pyrilamine from human histamine H1 receptorDisplacement of radiolabeled pyrilamine from human histamine H1 receptor
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm8007618
2331 2489 43 None -2 12 Human 8.7 pKi = 8.7 Binding
Displacement of radiolabeled pyrilamine from human histamine H1 receptorDisplacement of radiolabeled pyrilamine from human histamine H1 receptor
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm8007618
3957 2489 43 None -2 12 Human 8.7 pKi = 8.7 Binding
Displacement of radiolabeled pyrilamine from human histamine H1 receptorDisplacement of radiolabeled pyrilamine from human histamine H1 receptor
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm8007618
4992 2489 43 None -2 12 Human 8.7 pKi = 8.7 Binding
Displacement of radiolabeled pyrilamine from human histamine H1 receptorDisplacement of radiolabeled pyrilamine from human histamine H1 receptor
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm8007618
CHEMBL511 2489 43 None -2 12 Human 8.7 pKi = 8.7 Binding
Displacement of radiolabeled pyrilamine from human histamine H1 receptorDisplacement of radiolabeled pyrilamine from human histamine H1 receptor
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm8007618
DB06691 2489 43 None -2 12 Human 8.7 pKi = 8.7 Binding
Displacement of radiolabeled pyrilamine from human histamine H1 receptorDisplacement of radiolabeled pyrilamine from human histamine H1 receptor
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1021/jm8007618
44326390 207847 0 None 11 3 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 335 2 0 3 3.5 c1ccc2c(c1)Cc1ccccc1[C@H]1CC(CN3CCOCC3)O[C@H]21 10.1016/j.bmcl.2004.03.069
CHEMBL96429 207847 0 None 11 3 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 335 2 0 3 3.5 c1ccc2c(c1)Cc1ccccc1[C@H]1CC(CN3CCOCC3)O[C@H]21 10.1016/j.bmcl.2004.03.069
135398737 958 93 None 2 89 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2008.09.012
38 958 93 None 2 89 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2008.09.012
722 958 93 None 2 89 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2008.09.012
CHEMBL42 958 93 None 2 89 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2008.09.012
DB00363 958 93 None 2 89 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2008.09.012
15595033 195075 20 None 416 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 338 4 1 4 3.4 CNC1CCN(c2nc3ccccc3n2Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2009.05.086
CHEMBL549599 195075 20 None 416 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 338 4 1 4 3.4 CNC1CCN(c2nc3ccccc3n2Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2009.05.086
45272877 195845 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 364 5 0 5 3.6 COc1ccc(Cn2c(N3CCC(N(C)C)CC3)nc3ccccc32)cc1 10.1016/j.bmcl.2009.05.086
CHEMBL558468 195845 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 364 5 0 5 3.6 COc1ccc(Cn2c(N3CCC(N(C)C)CC3)nc3ccccc32)cc1 10.1016/j.bmcl.2009.05.086
45268662 195950 0 None 37 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 442 7 0 4 5.4 CN(CCc1ccccc1)C1CCN(c2nc3ccccc3n2Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2009.05.086
CHEMBL559557 195950 0 None 37 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 442 7 0 4 5.4 CN(CCc1ccccc1)C1CCN(c2nc3ccccc3n2Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2009.05.086
46865978 8439 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 328 6 0 4 4.2 COc1ccc2c(c1)CC(CCN(C)C)=C2[C@@H](C)c1nccs1 10.1016/j.bmcl.2010.02.055
CHEMBL1093623 8439 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 328 6 0 4 4.2 COc1ccc2c(c1)CC(CCN(C)C)=C2[C@@H](C)c1nccs1 10.1016/j.bmcl.2010.02.055
49782792 17911 0 None -7 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cellsDisplacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 381 3 1 4 3.3 CC(=O)NCc1ccc2c(c1)[C@@H](N1CCN(C)CC1)Cc1ccccc1S2 10.1021/jm100652h
CHEMBL1259174 17911 0 None -7 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cellsDisplacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 381 3 1 4 3.3 CC(=O)NCc1ccc2c(c1)[C@@H](N1CCN(C)CC1)Cc1ccccc1S2 10.1021/jm100652h
59296081 84083 0 None -7 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 608 9 3 7 2.9 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c(=O)c2cc(S(=O)(=O)N3CCC3)ccc12 10.1016/j.bmcl.2012.09.112
CHEMBL2207654 84083 0 None -7 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 608 9 3 7 2.9 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c(=O)c2cc(S(=O)(=O)N3CCC3)ccc12 10.1016/j.bmcl.2012.09.112
59295978 84085 0 None -1 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 507 7 3 5 3.6 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c(=O)c2c(F)cccc12 10.1016/j.bmcl.2012.09.112
CHEMBL2207656 84085 0 None -1 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 507 7 3 5 3.6 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c(=O)c2c(F)cccc12 10.1016/j.bmcl.2012.09.112
59295968 84086 0 None -3 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 487 7 3 5 3.3 Cc1cc(Cl)ccc1OC1CCN(C[C@H](O)CNC(=O)c2c[nH]c(=O)c3c(F)cccc23)CC1 10.1016/j.bmcl.2012.09.112
CHEMBL2207657 84086 0 None -3 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 487 7 3 5 3.3 Cc1cc(Cl)ccc1OC1CCN(C[C@H](O)CNC(=O)c2c[nH]c(=O)c3c(F)cccc23)CC1 10.1016/j.bmcl.2012.09.112
155556183 174488 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 406 2 0 2 6.3 Clc1ccc2c(c1)CCc1cccnc1C2=C1CCN(CC2CCCCC2)CC1 10.1021/acs.jmedchem.9b00447
CHEMBL4554533 174488 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 406 2 0 2 6.3 Clc1ccc2c(c1)CCc1cccnc1C2=C1CCN(CC2CCCCC2)CC1 10.1021/acs.jmedchem.9b00447
134134675 154583 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 315 4 0 2 4.4 CN1CCC(Oc2ccccc2Cc2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.6b00981
CHEMBL3905009 154583 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 315 4 0 2 4.4 CN1CCC(Oc2ccccc2Cc2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.6b00981
CHEMBL3991348 154583 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 315 4 0 2 4.4 CN1CCC(Oc2ccccc2Cc2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.6b00981
17963227 82231 0 None 39 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 539 5 0 5 5.1 Cc1ccc(S(=O)(=O)N(C)C(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.124
CHEMBL2171013 82231 0 None 39 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 539 5 0 5 5.1 Cc1ccc(S(=O)(=O)N(C)C(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.124
2600 3779 74 None 1 13 Human 8.6 pKi = 8.6 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
2608 3779 74 None 1 13 Human 8.6 pKi = 8.6 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
5405 3779 74 None 1 13 Human 8.6 pKi = 8.6 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
CHEMBL17157 3779 74 None 1 13 Human 8.6 pKi = 8.6 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
DB00342 3779 74 None 1 13 Human 8.6 pKi = 8.6 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
136152971 95357 0 None -1 6 Human 8.6 pKi = 8.6 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 293 2 2 3 3.5 C[C@@H]1NC(NCC(F)F)=Nc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL256694 95357 0 None -1 6 Human 8.6 pKi = 8.6 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 293 2 2 3 3.5 C[C@@H]1NC(NCC(F)F)=Nc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2007.10.078
2389 3331 118 None -46 67 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human histamine H1 receptorBinding affinity towards human histamine H1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm030480f
5073 3331 118 None -46 67 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human histamine H1 receptorBinding affinity towards human histamine H1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm030480f
96 3331 118 None -46 67 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human histamine H1 receptorBinding affinity towards human histamine H1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm030480f
CHEMBL85 3331 118 None -46 67 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human histamine H1 receptorBinding affinity towards human histamine H1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm030480f
DB00734 3331 118 None -46 67 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human histamine H1 receptorBinding affinity towards human histamine H1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm030480f
46884732 7910 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 337 6 0 4 3.9 COc1nccnc1[C@H](C)C1=C(CCN(C)C)Cc2cc(C)ccc21 10.1016/j.bmcl.2010.02.055
CHEMBL1090176 7910 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 337 6 0 4 3.9 COc1nccnc1[C@H](C)C1=C(CCN(C)C)Cc2cc(C)ccc21 10.1016/j.bmcl.2010.02.055
46884152 8252 0 None 812 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 328 5 0 3 4.7 C[C@@H](c1ncccc1F)c1c(CCN(C)C)sc2ccccc12 10.1016/j.bmcl.2010.01.134
CHEMBL1092377 8252 0 None 812 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 328 5 0 3 4.7 C[C@@H](c1ncccc1F)c1c(CCN(C)C)sc2ccccc12 10.1016/j.bmcl.2010.01.134
10102 2546 88 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 432 5 1 6 3.4 Fc1ccc(cc1)Cn1c(nc2c1cccc2)N1CCC(CC1)N(c1nccc(=O)[nH]1)C 10.1016/j.bmcl.2009.05.086
1824 2546 88 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 432 5 1 6 3.4 Fc1ccc(cc1)Cn1c(nc2c1cccc2)N1CCC(CC1)N(c1nccc(=O)[nH]1)C 10.1016/j.bmcl.2009.05.086
65906 2546 88 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 432 5 1 6 3.4 Fc1ccc(cc1)Cn1c(nc2c1cccc2)N1CCC(CC1)N(c1nccc(=O)[nH]1)C 10.1016/j.bmcl.2009.05.086
CHEMBL94454 2546 88 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 432 5 1 6 3.4 Fc1ccc(cc1)Cn1c(nc2c1cccc2)N1CCC(CC1)N(c1nccc(=O)[nH]1)C 10.1016/j.bmcl.2009.05.086
DB12523 2546 88 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 432 5 1 6 3.4 Fc1ccc(cc1)Cn1c(nc2c1cccc2)N1CCC(CC1)N(c1nccc(=O)[nH]1)C 10.1016/j.bmcl.2009.05.086
9857902 60804 0 None 6 5 Rat 8.6 pKi = 8.6 Binding
In vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamineIn vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamine
ChEMBL 311 1 0 4 3.5 Cc1ccc2n1C=C(N1CCN(C)CC1)c1ccccc1S2 10.1021/jm0309811
CHEMBL176169 60804 0 None 6 5 Rat 8.6 pKi = 8.6 Binding
In vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamineIn vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamine
ChEMBL 311 1 0 4 3.5 Cc1ccc2n1C=C(N1CCN(C)CC1)c1ccccc1S2 10.1021/jm0309811
9796255 129048 0 None -2 8 Rat 8.6 pKi = 8.6 Binding
In vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamineIn vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamine
ChEMBL 297 1 0 4 3.2 CN1CCN(C2=Cn3cccc3Sc3ccccc32)CC1 10.1021/jm0309811
CHEMBL367045 129048 0 None -2 8 Rat 8.6 pKi = 8.6 Binding
In vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamineIn vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamine
ChEMBL 297 1 0 4 3.2 CN1CCN(C2=Cn3cccc3Sc3ccccc32)CC1 10.1021/jm0309811
46884732 7910 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 337 6 0 4 3.9 COc1nccnc1[C@H](C)C1=C(CCN(C)C)Cc2cc(C)ccc21 10.1016/j.bmcl.2010.07.117
CHEMBL1090176 7910 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 337 6 0 4 3.9 COc1nccnc1[C@H](C)C1=C(CCN(C)C)Cc2cc(C)ccc21 10.1016/j.bmcl.2010.07.117
2274 3173 58 None -3 31 Human 8.6 pKi = 8.6 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917 3173 58 None -3 31 Human 8.6 pKi = 8.6 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
7279 3173 58 None -3 31 Human 8.6 pKi = 8.6 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL728 3173 58 None -3 31 Human 8.6 pKi = 8.6 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
DB00433 3173 58 None -3 31 Human 8.6 pKi = 8.6 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
53318872 57756 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 305 5 0 3 3.5 c1ccc2c(c1)CC(CCN1CCCC1)=C2Cc1cnccn1 10.1016/j.bmcl.2010.12.053
CHEMBL1669413 57756 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 305 5 0 3 3.5 c1ccc2c(c1)CC(CCN1CCCC1)=C2Cc1cnccn1 10.1016/j.bmcl.2010.12.053
135398745 2914 112 None 1 65 Human 8.6 pKi = 8.6 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmc.2008.06.030
47 2914 112 None 1 65 Human 8.6 pKi = 8.6 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmc.2008.06.030
CHEMBL715 2914 112 None 1 65 Human 8.6 pKi = 8.6 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmc.2008.06.030
DB00334 2914 112 None 1 65 Human 8.6 pKi = 8.6 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmc.2008.06.030
45273833 195888 0 None 977 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 420 5 0 4 5.5 CN(C1CCCCC1)C1CCN(c2nc3ccccc3n2Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2009.05.086
CHEMBL558933 195888 0 None 977 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 420 5 0 4 5.5 CN(C1CCCCC1)C1CCN(c2nc3ccccc3n2Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2009.05.086
2389 3331 118 None -46 67 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
5073 3331 118 None -46 67 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
96 3331 118 None -46 67 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
CHEMBL85 3331 118 None -46 67 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
DB00734 3331 118 None -46 67 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
46884200 8322 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 344 5 0 3 5.2 C[C@H](c1cccnc1Cl)c1c(CCN(C)C)sc2ccccc12 10.1016/j.bmcl.2010.01.134
CHEMBL1092766 8322 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 344 5 0 3 5.2 C[C@H](c1cccnc1Cl)c1c(CCN(C)C)sc2ccccc12 10.1016/j.bmcl.2010.01.134
11695811 8391 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 340 6 0 4 4.6 COc1ncccc1[C@@H](C)c1c(CCN(C)C)sc2ccccc12 10.1016/j.bmcl.2010.01.134
CHEMBL1093294 8391 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 340 6 0 4 4.6 COc1ncccc1[C@@H](C)c1c(CCN(C)C)sc2ccccc12 10.1016/j.bmcl.2010.01.134
45272890 195901 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 409 7 0 5 3.7 CN(C)CCN(C)C1CCN(c2nc3ccccc3n2Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2009.05.086
CHEMBL559061 195901 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 409 7 0 5 3.7 CN(C)CCN(C)C1CCN(c2nc3ccccc3n2Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2009.05.086
135398737 958 93 None -4 89 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamineIn vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamine
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0309811
38 958 93 None -4 89 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamineIn vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamine
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0309811
722 958 93 None -4 89 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamineIn vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamine
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0309811
CHEMBL42 958 93 None -4 89 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamineIn vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamine
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0309811
DB00363 958 93 None -4 89 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamineIn vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamine
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0309811
44266958 97241 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.
ChEMBL 382 1 1 3 3.8 CC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3cc(CO)cnc32)CC1 10.1016/S0960-894X(00)80290-5
CHEMBL268695 97241 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.
ChEMBL 382 1 1 3 3.8 CC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3cc(CO)cnc32)CC1 10.1016/S0960-894X(00)80290-5
11485192 203123 0 None - 1 Guinea pig 7.7 pKi = 7.7 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 323 4 1 3 3.7 CN(C)CC/C=C1/c2ccccc2COc2ccc(C(=O)O)cc21 10.1021/jm00089a020
CHEMBL64067 203123 0 None - 1 Guinea pig 7.7 pKi = 7.7 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 323 4 1 3 3.7 CN(C)CC/C=C1/c2ccccc2COc2ccc(C(=O)O)cc21 10.1021/jm00089a020
2389 3331 118 None -46 67 Human 7.7 pKi = 7.7 Binding
Binding affinity to H1 histamine receptor (unknown origin)Binding affinity to H1 histamine receptor (unknown origin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2020.127681
5073 3331 118 None -46 67 Human 7.7 pKi = 7.7 Binding
Binding affinity to H1 histamine receptor (unknown origin)Binding affinity to H1 histamine receptor (unknown origin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2020.127681
96 3331 118 None -46 67 Human 7.7 pKi = 7.7 Binding
Binding affinity to H1 histamine receptor (unknown origin)Binding affinity to H1 histamine receptor (unknown origin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2020.127681
CHEMBL85 3331 118 None -46 67 Human 7.7 pKi = 7.7 Binding
Binding affinity to H1 histamine receptor (unknown origin)Binding affinity to H1 histamine receptor (unknown origin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2020.127681
DB00734 3331 118 None -46 67 Human 7.7 pKi = 7.7 Binding
Binding affinity to H1 histamine receptor (unknown origin)Binding affinity to H1 histamine receptor (unknown origin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2020.127681
9419 35922 35 None 125 6 Human 7.7 pKi = 7.7 Binding
Binding affinity to H1 receptor (unknown origin)Binding affinity to H1 receptor (unknown origin)
ChEMBL 295 3 0 3 3.0 CN(C)CCN1C(=O)c2ccccc2N(C)c2ccccc21 10.1016/j.bmcl.2020.127493
CHEMBL1442422 35922 35 None 125 6 Human 7.7 pKi = 7.7 Binding
Binding affinity to H1 receptor (unknown origin)Binding affinity to H1 receptor (unknown origin)
ChEMBL 295 3 0 3 3.0 CN(C)CCN1C(=O)c2ccccc2N(C)c2ccccc21 10.1016/j.bmcl.2020.127493
71450058 82574 0 None 37 2 Human 7.7 pKi = 7.7 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 453 6 1 3 5.6 O=C(O)Cc1ccc2c(c1)/C(=C/CN1CCCC(Cc3ccccc3)C1)c1ccccc1CO2 10.1021/jm300682j
CHEMBL2178582 82574 0 None 37 2 Human 7.7 pKi = 7.7 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 453 6 1 3 5.6 O=C(O)Cc1ccc2c(c1)/C(=C/CN1CCCC(Cc3ccccc3)C1)c1ccccc1CO2 10.1021/jm300682j
1224 1432 83 None -2 13 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
3100 1432 83 None -2 13 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
8980 1432 83 None -2 13 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
916 1432 83 None -2 13 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
CHEMBL657 1432 83 None -2 13 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
DB01075 1432 83 None -2 13 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
1605 2342 117 None -2 4 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 nan
3957 2342 117 None -2 4 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 nan
7216 2342 117 None -2 4 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 nan
CHEMBL998 2342 117 None -2 4 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 nan
DB00455 2342 117 None -2 4 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 nan
9863340 162027 0 None -5 4 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]- pyrilamine from rat brain membrane Histamine H1 receptorDisplacement of [3H]- pyrilamine from rat brain membrane Histamine H1 receptor
ChEMBL 352 4 0 4 4.0 Cn1c(=O)sc2cc(CCN3CCC(c4ccccc4)CC3)ccc21 10.1016/s0960-894x(02)00123-3
CHEMBL415985 162027 0 None -5 4 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]- pyrilamine from rat brain membrane Histamine H1 receptorDisplacement of [3H]- pyrilamine from rat brain membrane Histamine H1 receptor
ChEMBL 352 4 0 4 4.0 Cn1c(=O)sc2cc(CCN3CCC(c4ccccc4)CC3)ccc21 10.1016/s0960-894x(02)00123-3
45485473 197335 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation counting
ChEMBL 457 9 1 4 5.4 COC(=O)c1ccc(CCCCN2CCC(C(O)(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2009.07.047
CHEMBL568892 197335 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation counting
ChEMBL 457 9 1 4 5.4 COC(=O)c1ccc(CCCCN2CCC(C(O)(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2009.07.047
44404954 135265 0 None -1 3 Human 7.7 pKi = 7.7 Binding
Inhibition constant against histamine H1 receptorInhibition constant against histamine H1 receptor
ChEMBL 453 6 1 3 5.6 O=C(O)Cc1ccc2c(c1)/C(=C\CN1CCC(Cc3ccccc3)CC1)c1ccccc1CO2 10.1021/jm058225d
CHEMBL372588 135265 0 None -1 3 Human 7.7 pKi = 7.7 Binding
Inhibition constant against histamine H1 receptorInhibition constant against histamine H1 receptor
ChEMBL 453 6 1 3 5.6 O=C(O)Cc1ccc2c(c1)/C(=C\CN1CCC(Cc3ccccc3)CC1)c1ccccc1CO2 10.1021/jm058225d
9937936 23115 0 None - 1 Guinea pig 7.7 pKi = 7.7 Binding
Inhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptorInhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptor
ChEMBL 453 6 1 3 5.6 O=C(O)Cc1ccc2c(c1)/C(=C/CN1CCC(Cc3ccccc3)CC1)c1ccccc1CO2 10.1021/jm00055a013
CHEMBL133080 23115 0 None - 1 Guinea pig 7.7 pKi = 7.7 Binding
Inhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptorInhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptor
ChEMBL 453 6 1 3 5.6 O=C(O)Cc1ccc2c(c1)/C(=C/CN1CCC(Cc3ccccc3)CC1)c1ccccc1CO2 10.1021/jm00055a013
10049865 24748 0 None - 1 Guinea pig 7.7 pKi = 7.7 Binding
Inhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptorInhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptor
ChEMBL 459 6 1 4 6.0 O=C(O)c1ccc2c(c1)C(SCCN1CCC(c3ccccc3)CC1)c1ccccc1CO2 10.1021/jm00055a013
CHEMBL134424 24748 0 None - 1 Guinea pig 7.7 pKi = 7.7 Binding
Inhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptorInhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptor
ChEMBL 459 6 1 4 6.0 O=C(O)c1ccc2c(c1)C(SCCN1CCC(c3ccccc3)CC1)c1ccccc1CO2 10.1021/jm00055a013
44326405 111585 0 None 6 3 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 309 2 0 3 3.8 CN(C)CC1C[C@@H]2c3ccccc3COc3ccccc3[C@H]2O1 10.1016/j.bmcl.2004.03.069
CHEMBL328209 111585 0 None 6 3 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 309 2 0 3 3.8 CN(C)CC1C[C@@H]2c3ccccc3COc3ccccc3[C@H]2O1 10.1016/j.bmcl.2004.03.069
71212556 143562 0 None -7 6 Human 7.7 pKi = 7.7 Binding
Scintillation Proximity Assay: [3H]-Pyrilamine binding experiments are carried out in SPA (scintillation proximity assay) 96-well format. Membranes used in this assay are prepared from HEK-293 cells stably expressing recombinant H1 receptor (human). The incubation is initiated by the addition of a mixture of WGA PVT SPA beads (1 mg/well, Perkin Elmer (MA, USA) RPNQ0001) and 3 μg membranes to assay buffer (67 mM Tris; pH 7.6) containing 3.5 nM [3H]-Pyrilamine and varying concentrations of the test compound (10 point concentration response curves). Non-specific binding is determined in the presence of 10 μM Triprolidine. Samples are incubated for 4 hr. at room temperature (22° C.) and then read in a Microbeta Trilux.Scintillation Proximity Assay: [3H]-Pyrilamine binding experiments are carried out in SPA (scintillation proximity assay) 96-well format. Membranes used in this assay are prepared from HEK-293 cells stably expressing recombinant H1 receptor (human). The incubation is initiated by the addition of a mixture of WGA PVT SPA beads (1 mg/well, Perkin Elmer (MA, USA) RPNQ0001) and 3 μg membranes to assay buffer (67 mM Tris; pH 7.6) containing 3.5 nM [3H]-Pyrilamine and varying concentrations of the test compound (10 point concentration response curves). Non-specific binding is determined in the presence of 10 μM Triprolidine. Samples are incubated for 4 hr. at room temperature (22° C.) and then read in a Microbeta Trilux.
ChEMBL 433 3 1 6 4.6 Cc1ccc2c(c1)Oc1sc(Cl)cc1C(N1CCN(CC(C)(C)C(=O)O)CC1)=N2 nan
CHEMBL3899169 143562 0 None -7 6 Human 7.7 pKi = 7.7 Binding
Scintillation Proximity Assay: [3H]-Pyrilamine binding experiments are carried out in SPA (scintillation proximity assay) 96-well format. Membranes used in this assay are prepared from HEK-293 cells stably expressing recombinant H1 receptor (human). The incubation is initiated by the addition of a mixture of WGA PVT SPA beads (1 mg/well, Perkin Elmer (MA, USA) RPNQ0001) and 3 μg membranes to assay buffer (67 mM Tris; pH 7.6) containing 3.5 nM [3H]-Pyrilamine and varying concentrations of the test compound (10 point concentration response curves). Non-specific binding is determined in the presence of 10 μM Triprolidine. Samples are incubated for 4 hr. at room temperature (22° C.) and then read in a Microbeta Trilux.Scintillation Proximity Assay: [3H]-Pyrilamine binding experiments are carried out in SPA (scintillation proximity assay) 96-well format. Membranes used in this assay are prepared from HEK-293 cells stably expressing recombinant H1 receptor (human). The incubation is initiated by the addition of a mixture of WGA PVT SPA beads (1 mg/well, Perkin Elmer (MA, USA) RPNQ0001) and 3 μg membranes to assay buffer (67 mM Tris; pH 7.6) containing 3.5 nM [3H]-Pyrilamine and varying concentrations of the test compound (10 point concentration response curves). Non-specific binding is determined in the presence of 10 μM Triprolidine. Samples are incubated for 4 hr. at room temperature (22° C.) and then read in a Microbeta Trilux.
ChEMBL 433 3 1 6 4.6 Cc1ccc2c(c1)Oc1sc(Cl)cc1C(N1CCN(CC(C)(C)C(=O)O)CC1)=N2 nan
524022 31644 1 None - 1 Rat 5.7 pKi = 5.7 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 318 0 0 2 3.6 CC(=O)N1CCC(=C2c3ccccc3CCc3cccnc32)CC1 10.1021/jm00105a069
CHEMBL140483 31644 1 None - 1 Rat 5.7 pKi = 5.7 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 318 0 0 2 3.6 CC(=O)N1CCC(=C2c3ccccc3CCc3cccnc32)CC1 10.1021/jm00105a069
71452695 78683 0 None -5011 3 Human 4.7 pKi = 4.7 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 453 10 1 6 3.0 N#Cc1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1 10.1016/s0960-894x(02)00685-6
CHEMBL2112451 78683 0 None -5011 3 Human 4.7 pKi = 4.7 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 453 10 1 6 3.0 N#Cc1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1 10.1016/s0960-894x(02)00685-6
44270248 47973 0 None - 1 Rat 4.7 pKi = 4.7 Binding
Displacement of [3H]- pyrilamine from rat brain membrane Histamine H1 receptorDisplacement of [3H]- pyrilamine from rat brain membrane Histamine H1 receptor
ChEMBL 305 3 1 5 1.8 C[C@H]1CN(CCc2ccc3c(c2)sc(=O)n3C)C[C@@H](C)N1 10.1016/s0960-894x(02)00123-3
CHEMBL15499 47973 0 None - 1 Rat 4.7 pKi = 4.7 Binding
Displacement of [3H]- pyrilamine from rat brain membrane Histamine H1 receptorDisplacement of [3H]- pyrilamine from rat brain membrane Histamine H1 receptor
ChEMBL 305 3 1 5 1.8 C[C@H]1CN(CCc2ccc3c(c2)sc(=O)n3C)C[C@@H](C)N1 10.1016/s0960-894x(02)00123-3
10156707 202642 0 None -6 2 Rat 6.7 pKi = 6.7 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
ChEMBL 381 9 3 3 4.6 N=C(CCCc1c[nH]cn1)NCCC(c1ccc(Cl)cc1)c1ccccn1 10.1016/s0960-894x(03)00357-3
CHEMBL61348 202642 0 None -6 2 Rat 6.7 pKi = 6.7 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
ChEMBL 381 9 3 3 4.6 N=C(CCCc1c[nH]cn1)NCCC(c1ccc(Cl)cc1)c1ccccn1 10.1016/s0960-894x(03)00357-3
10456093 197509 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation counting
ChEMBL 443 9 2 3 5.4 O=C(O)c1ccc(CCCCN2CCC(C(O)(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2009.07.047
CHEMBL570033 197509 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation counting
ChEMBL 443 9 2 3 5.4 O=C(O)c1ccc(CCCCN2CCC(C(O)(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2009.07.047
44304377 202777 0 None -112 3 Human 5.7 pKi = 5.7 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 424 11 0 6 3.5 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cnccn3)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL62115 202777 0 None -112 3 Human 5.7 pKi = 5.7 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 424 11 0 6 3.5 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cnccn3)CC2)cc1 10.1016/s0960-894x(02)00309-8
44591134 176200 0 None -169 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 535 11 0 5 7.7 CN(CCCN1c2ccccc2Sc2ccc(Cl)cc21)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
CHEMBL459373 176200 0 None -169 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 535 11 0 5 7.7 CN(CCCN1c2ccccc2Sc2ccc(Cl)cc21)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
2712 916 34 None -5 4 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl nan
3370 916 34 None -5 4 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl nan
594 916 34 None -5 4 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl nan
CHEMBL451 916 34 None -5 4 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl nan
DB00475 916 34 None -5 4 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl nan
44304309 169216 0 None -3 3 Human 6.7 pKi = 6.7 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 414 8 0 5 3.6 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3ccc(F)cc3)cc2)CC1 10.1016/s0960-894x(02)00309-8
CHEMBL440864 169216 0 None -3 3 Human 6.7 pKi = 6.7 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 414 8 0 5 3.6 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3ccc(F)cc3)cc2)CC1 10.1016/s0960-894x(02)00309-8
44304211 102197 0 None -6918 3 Human 5.7 pKi = 5.7 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 373 9 1 5 1.9 CC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL302829 102197 0 None -6918 3 Human 5.7 pKi = 5.7 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 373 9 1 5 1.9 CC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
127035835 137285 0 None -1 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 385 4 1 5 3.6 CN1CCN(c2nc(NCc3ccccc3)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3752270 137285 0 None -1 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 385 4 1 5 3.6 CN1CCN(c2nc(NCc3ccccc3)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
71519674 89729 0 None -2454 5 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human histamine H1 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H1 receptor expressed in HEK cells
ChEMBL 270 3 2 6 0.9 CNC1CN(c2nc(N)nc3cc(C4CC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
CHEMBL2376804 89729 0 None -2454 5 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human histamine H1 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H1 receptor expressed in HEK cells
ChEMBL 270 3 2 6 0.9 CNC1CN(c2nc(N)nc3cc(C4CC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
14554138 110662 37 None - 1 Rat 7.7 pKi = 7.7 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 338 1 0 2 3.9 O=CN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/jm00105a069
CHEMBL325909 110662 37 None - 1 Rat 7.7 pKi = 7.7 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 338 1 0 2 3.9 O=CN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/jm00105a069
2337 3256 77 None 1 62 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human H1 receptorBinding affinity towards human H1 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm0002432
50 3256 77 None 1 62 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human H1 receptorBinding affinity towards human H1 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm0002432
5002 3256 77 None 1 62 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human H1 receptorBinding affinity towards human H1 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm0002432
CHEMBL716 3256 77 None 1 62 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human H1 receptorBinding affinity towards human H1 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm0002432
DB01224 3256 77 None 1 62 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human H1 receptorBinding affinity towards human H1 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm0002432
57334707 90476 0 None -4 5 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysisDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysis
ChEMBL 464 7 0 6 5.7 Cc1cc(=O)oc2c(C)c(OCCCCN3CCC(c4noc5cc(F)ccc45)CC3)ccc12 10.1021/jm400408r
CHEMBL2387230 90476 0 None -4 5 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysisDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysis
ChEMBL 464 7 0 6 5.7 Cc1cc(=O)oc2c(C)c(OCCCCN3CCC(c4noc5cc(F)ccc45)CC3)ccc12 10.1021/jm400408r
56966478 105468 0 None 1 4 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation counting
ChEMBL 476 7 0 6 5.6 O=c1oc2cc(OCCCCN3CCC(c4noc5cc(F)ccc45)CC3)ccc2c2c1CCC2 10.1016/j.ejmech.2014.01.012
CHEMBL3120688 105468 0 None 1 4 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation counting
ChEMBL 476 7 0 6 5.6 O=c1oc2cc(OCCCCN3CCC(c4noc5cc(F)ccc45)CC3)ccc2c2c1CCC2 10.1016/j.ejmech.2014.01.012
9844271 130682 1 None -1 5 Rat 7.7 pKi = 7.7 Binding
Half-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenateHalf-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenate
ChEMBL 333 1 0 4 3.6 CN1CCN([C@@H]2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
CHEMBL368324 130682 1 None -1 5 Rat 7.7 pKi = 7.7 Binding
Half-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenateHalf-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenate
ChEMBL 333 1 0 4 3.6 CN1CCN([C@@H]2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
9844271 130682 1 None -1 5 Rat 7.7 pKi = 7.7 Binding
In vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamineIn vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamine
ChEMBL 333 1 0 4 3.6 CN1CCN([C@@H]2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm0309811
CHEMBL368324 130682 1 None -1 5 Rat 7.7 pKi = 7.7 Binding
In vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamineIn vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamine
ChEMBL 333 1 0 4 3.6 CN1CCN([C@@H]2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm0309811
2389 3331 118 None -52 67 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysisDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysis
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm400408r
5073 3331 118 None -52 67 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysisDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysis
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm400408r
96 3331 118 None -52 67 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysisDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysis
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm400408r
CHEMBL85 3331 118 None -52 67 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysisDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysis
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm400408r
DB00734 3331 118 None -52 67 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysisDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysis
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm400408r
44267047 9405 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.
ChEMBL 398 1 0 3 5.0 CSc1cnc2c(c1)CCc1cc(Cl)ccc1C2=C1CCN(C(C)=O)CC1 10.1016/S0960-894X(00)80290-5
CHEMBL11158 9405 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.
ChEMBL 398 1 0 3 5.0 CSc1cnc2c(c1)CCc1cc(Cl)ccc1C2=C1CCN(C(C)=O)CC1 10.1016/S0960-894X(00)80290-5
1353 1911 93 None -602 83 Rat 5.7 pKi = 5.7 Binding
Compound was tested for the binding affinity against rat cortical H1 receptor by Radio ligand [3H]pyrilamine binding assay.Compound was tested for the binding affinity against rat cortical H1 receptor by Radio ligand [3H]pyrilamine binding assay.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9601720
3559 1911 93 None -602 83 Rat 5.7 pKi = 5.7 Binding
Compound was tested for the binding affinity against rat cortical H1 receptor by Radio ligand [3H]pyrilamine binding assay.Compound was tested for the binding affinity against rat cortical H1 receptor by Radio ligand [3H]pyrilamine binding assay.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9601720
86 1911 93 None -602 83 Rat 5.7 pKi = 5.7 Binding
Compound was tested for the binding affinity against rat cortical H1 receptor by Radio ligand [3H]pyrilamine binding assay.Compound was tested for the binding affinity against rat cortical H1 receptor by Radio ligand [3H]pyrilamine binding assay.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9601720
CHEMBL54 1911 93 None -602 83 Rat 5.7 pKi = 5.7 Binding
Compound was tested for the binding affinity against rat cortical H1 receptor by Radio ligand [3H]pyrilamine binding assay.Compound was tested for the binding affinity against rat cortical H1 receptor by Radio ligand [3H]pyrilamine binding assay.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9601720
DB00502 1911 93 None -602 83 Rat 5.7 pKi = 5.7 Binding
Compound was tested for the binding affinity against rat cortical H1 receptor by Radio ligand [3H]pyrilamine binding assay.Compound was tested for the binding affinity against rat cortical H1 receptor by Radio ligand [3H]pyrilamine binding assay.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9601720
57401706 70171 0 None -37 11 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]pyrilamine from human H1 receptor by liquid scintillation countingDisplacement of [3H]pyrilamine from human H1 receptor by liquid scintillation counting
ChEMBL 331 6 0 4 3.5 Fc1ccc(SCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940419 70171 0 None -37 11 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]pyrilamine from human H1 receptor by liquid scintillation countingDisplacement of [3H]pyrilamine from human H1 receptor by liquid scintillation counting
ChEMBL 331 6 0 4 3.5 Fc1ccc(SCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
57398985 67883 0 None -16 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
ChEMBL 569 12 2 7 4.4 COc1ccc(CN(CCN(C)CC(C)Nc2ccc3[nH]c(C(=O)N4CCN(C)CC4)cc3c2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
CHEMBL1910385 67883 0 None -16 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
ChEMBL 569 12 2 7 4.4 COc1ccc(CN(CCN(C)CC(C)Nc2ccc3[nH]c(C(=O)N4CCN(C)CC4)cc3c2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
168268680 192766 0 None -1 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 662 11 8 8 4.8 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5172675 192766 0 None -1 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 662 11 8 8 4.8 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5221210 192766 0 None -1 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 662 11 8 8 4.8 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1 10.1021/acs.jmedchem.1c00692
44304437 100996 0 None -371 3 Human 4.7 pKi = 4.7 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 404 11 1 5 3.1 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)C(C)(C)O)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL294349 100996 0 None -371 3 Human 4.7 pKi = 4.7 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 404 11 1 5 3.1 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)C(C)(C)O)CC2)cc1 10.1016/s0960-894x(02)00309-8
44304393 105957 0 None -218 3 Human 4.7 pKi = 4.7 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 517 13 1 6 4.9 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](NC(=O)OC(C)(C)C)C(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
CHEMBL312958 105957 0 None -218 3 Human 4.7 pKi = 4.7 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 517 13 1 6 4.9 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](NC(=O)OC(C)(C)C)C(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
164622330 185862 0 None -870 6 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 360 6 4 4 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4867962 185862 0 None -870 6 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 360 6 4 4 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4531334 213985 31 None - 1 Human 5.7 pKi = 5.7 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000321b HRH1Selectivity interaction (GPCR panel (PDSP screen)) EUB0000321b HRH1
ChEMBL None None None CN1CCN(C(=O)C(C)(C)c2ccc(C(=O)Nc3cn4cc(-c5ccncc5)ccc4n3)cc2)CC1 10.6019/CHEMBL5212743
127051845 140729 0 None -12 9 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 309 6 0 3 3.7 COc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3817898 140729 0 None -12 9 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 309 6 0 3 3.7 COc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
10066369 120258 0 None -8 6 Human 6.7 pKi = 6.7 Binding
Compound was evaluated for binding affinity towards cloned human histamine H1 receptors stably expressed in CHO-K1 cells using [3H]mepyramineCompound was evaluated for binding affinity towards cloned human histamine H1 receptors stably expressed in CHO-K1 cells using [3H]mepyramine
ChEMBL 348 7 0 2 5.7 CC(C1=C(CCN(C(C)C)C(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL352375 120258 0 None -8 6 Human 6.7 pKi = 6.7 Binding
Compound was evaluated for binding affinity towards cloned human histamine H1 receptors stably expressed in CHO-K1 cells using [3H]mepyramineCompound was evaluated for binding affinity towards cloned human histamine H1 receptors stably expressed in CHO-K1 cells using [3H]mepyramine
ChEMBL 348 7 0 2 5.7 CC(C1=C(CCN(C(C)C)C(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
44304516 165356 0 None -512 3 Human 4.7 pKi = 4.7 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 357 8 1 5 1.5 O=C1C[C@H](N2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)CC2)N1 10.1016/s0960-894x(02)00310-4
CHEMBL423666 165356 0 None -512 3 Human 4.7 pKi = 4.7 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 357 8 1 5 1.5 O=C1C[C@H](N2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)CC2)N1 10.1016/s0960-894x(02)00310-4
44304013 202894 0 None -416 3 Human 4.7 pKi = 4.7 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 401 8 1 5 2.6 CC(C)(C)[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL62716 202894 0 None -416 3 Human 4.7 pKi = 4.7 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 401 8 1 5 2.6 CC(C)(C)[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
164621681 185580 0 None -173 4 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 444 7 4 5 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(OC(F)(F)F)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4863523 185580 0 None -173 4 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 444 7 4 5 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(OC(F)(F)F)cc1 10.1016/j.ejmech.2021.113190
11230971 123065 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for H1 histamine receptor expressed in CHO cellsBinding affinity for H1 histamine receptor expressed in CHO cells
ChEMBL 268 0 1 4 2.0 Cn1ccc2c1CCn1ccnc1C2=C1CCNCC1 10.1021/jm049495j
CHEMBL360953 123065 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for H1 histamine receptor expressed in CHO cellsBinding affinity for H1 histamine receptor expressed in CHO cells
ChEMBL 268 0 1 4 2.0 Cn1ccc2c1CCn1ccnc1C2=C1CCNCC1 10.1021/jm049495j
135446209 9585 58 None -2 3 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity of compound against histamine H1 neuronal receptorIn vitro binding affinity of compound against histamine H1 neuronal receptor
ChEMBL 298 0 2 5 3.1 Cc1cc2c(s1)Nc1ccccc1N=C2N1CCNCC1 10.1016/S0960-894X(96)00567-7
CHEMBL1125 9585 58 None -2 3 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity of compound against histamine H1 neuronal receptorIn vitro binding affinity of compound against histamine H1 neuronal receptor
ChEMBL 298 0 2 5 3.1 Cc1cc2c(s1)Nc1ccccc1N=C2N1CCNCC1 10.1016/S0960-894X(96)00567-7
2389 3331 118 None -52 67 Guinea pig 7.6 pKi = 7.6 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2014.01.012
5073 3331 118 None -52 67 Guinea pig 7.6 pKi = 7.6 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2014.01.012
96 3331 118 None -52 67 Guinea pig 7.6 pKi = 7.6 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2014.01.012
CHEMBL85 3331 118 None -52 67 Guinea pig 7.6 pKi = 7.6 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2014.01.012
DB00734 3331 118 None -52 67 Guinea pig 7.6 pKi = 7.6 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2014.01.012
90469115 185842 4 None -72 17 Human 6.7 pKi = 6.7 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 410 3 1 6 3.0 O=S(=O)(c1cccc(F)c1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
CHEMBL4867565 185842 4 None -72 17 Human 6.7 pKi = 6.7 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 410 3 1 6 3.0 O=S(=O)(c1cccc(F)c1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
10575070 67881 0 None 79 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
ChEMBL 439 7 1 3 4.7 O=C(c1cc2ccccc2[nH]1)N1CCN(CCOC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2011.09.001
CHEMBL1910383 67881 0 None 79 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
ChEMBL 439 7 1 3 4.7 O=C(c1cc2ccccc2[nH]1)N1CCN(CCOC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2011.09.001
44304387 202928 0 None -446 3 Human 5.7 pKi = 5.7 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 334 7 0 5 2.4 CCOC(=O)N1CCN(CCCOc2ccc(C(C)=O)cc2)CC1 10.1016/s0960-894x(02)00309-8
CHEMBL62840 202928 0 None -446 3 Human 5.7 pKi = 5.7 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 334 7 0 5 2.4 CCOC(=O)N1CCN(CCCOc2ccc(C(C)=O)cc2)CC1 10.1016/s0960-894x(02)00309-8
44304244 203176 0 None -141 3 Human 5.7 pKi = 5.7 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 372 12 0 4 4.2 CCCCCC(=O)c1ccc(OCCCN2CCN(CC3CC3)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL64253 203176 0 None -141 3 Human 5.7 pKi = 5.7 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 372 12 0 4 4.2 CCCCCC(=O)c1ccc(OCCCN2CCN(CC3CC3)CC2)cc1 10.1016/s0960-894x(02)00309-8
90654503 110312 0 None -29 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 483 9 1 4 4.9 O=C1NC(c2ccccc2)(c2ccccc2)C(=O)N1Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.ejmech.2014.03.014
CHEMBL3238447 110312 0 None -29 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 483 9 1 4 4.9 O=C1NC(c2ccccc2)(c2ccccc2)C(=O)N1Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.ejmech.2014.03.014
44304741 202917 0 None -223 3 Human 5.6 pKi = 5.6 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 466 13 1 6 3.3 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](N)Cc3ccncc3)CC2)cc1 10.1016/s0960-894x(02)00310-4
CHEMBL62808 202917 0 None -223 3 Human 5.6 pKi = 5.6 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 466 13 1 6 3.3 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](N)Cc3ccncc3)CC2)cc1 10.1016/s0960-894x(02)00310-4
57402933 69026 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 260 4 2 3 2.1 CNCC(O)CN1c2ccccc2C2CCCCC21 10.1021/jm2011589
CHEMBL1923528 69026 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 260 4 2 3 2.1 CNCC(O)CN1c2ccccc2C2CCCCC21 10.1021/jm2011589
155537890 172341 0 None 8 2 Guinea pig 7.6 pKi = 7.6 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysisDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysis
ChEMBL 302 5 0 3 2.6 CN1CCc2ccc(OCCCN3CCCCC3)cc2C1=O 10.1016/j.bmcl.2019.04.015
CHEMBL4475658 172341 0 None 8 2 Guinea pig 7.6 pKi = 7.6 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysisDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysis
ChEMBL 302 5 0 3 2.6 CN1CCc2ccc(OCCCN3CCCCC3)cc2C1=O 10.1016/j.bmcl.2019.04.015
11154555 800 62 None -56 12 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-pyrilamine from human H1 histamine receptor expressed in human HEK293 cellsDisplacement of [3H]-pyrilamine from human H1 histamine receptor expressed in human HEK293 cells
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2020.127681
5037 800 62 None -56 12 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-pyrilamine from human H1 histamine receptor expressed in human HEK293 cellsDisplacement of [3H]-pyrilamine from human H1 histamine receptor expressed in human HEK293 cells
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2020.127681
7671 800 62 None -56 12 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-pyrilamine from human H1 histamine receptor expressed in human HEK293 cellsDisplacement of [3H]-pyrilamine from human H1 histamine receptor expressed in human HEK293 cells
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2020.127681
CHEMBL2028019 800 62 None -56 12 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-pyrilamine from human H1 histamine receptor expressed in human HEK293 cellsDisplacement of [3H]-pyrilamine from human H1 histamine receptor expressed in human HEK293 cells
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2020.127681
CHEMBL3085826 800 62 None -56 12 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-pyrilamine from human H1 histamine receptor expressed in human HEK293 cellsDisplacement of [3H]-pyrilamine from human H1 histamine receptor expressed in human HEK293 cells
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2020.127681
DB06016 800 62 None -56 12 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-pyrilamine from human H1 histamine receptor expressed in human HEK293 cellsDisplacement of [3H]-pyrilamine from human H1 histamine receptor expressed in human HEK293 cells
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2020.127681
44267053 6462 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.
ChEMBL 428 1 0 2 5.9 CC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3cc(-c4ccccc4)cnc32)CC1 10.1016/S0960-894X(00)80290-5
CHEMBL10826 6462 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.
ChEMBL 428 1 0 2 5.9 CC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3cc(-c4ccccc4)cnc32)CC1 10.1016/S0960-894X(00)80290-5
44267061 98228 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.
ChEMBL 366 0 0 2 4.6 CC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3c(C)ccnc32)CC1 10.1016/S0960-894X(00)80290-5
CHEMBL274357 98228 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.
ChEMBL 366 0 0 2 4.6 CC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3c(C)ccnc32)CC1 10.1016/S0960-894X(00)80290-5
44334212 4629 0 None -501 3 Human 5.6 pKi = 5.6 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 456 11 1 5 3.7 CCc1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1 10.1016/s0960-894x(02)00685-6
CHEMBL102925 4629 0 None -501 3 Human 5.6 pKi = 5.6 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 456 11 1 5 3.7 CCc1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1 10.1016/s0960-894x(02)00685-6
44334369 5014 0 None -436 3 Human 5.6 pKi = 5.6 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 484 10 1 5 4.4 CC(C)(C)c1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1 10.1016/s0960-894x(02)00685-6
CHEMBL105071 5014 0 None -436 3 Human 5.6 pKi = 5.6 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 484 10 1 5 4.4 CC(C)(C)c1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1 10.1016/s0960-894x(02)00685-6
44275807 98970 0 None -2137 10 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human histaminergic (H1) receptorBinding affinity towards human histaminergic (H1) receptor
ChEMBL 422 7 0 4 4.5 C[C@H]1CC[C@H](C)N1CCCOc1ccc(-c2ccc(C(=O)N3CCOCC3)cc2)cc1 10.1016/s0960-894x(03)00118-5
CHEMBL27979 98970 0 None -2137 10 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human histaminergic (H1) receptorBinding affinity towards human histaminergic (H1) receptor
ChEMBL 422 7 0 4 4.5 C[C@H]1CC[C@H](C)N1CCCOc1ccc(-c2ccc(C(=O)N3CCOCC3)cc2)cc1 10.1016/s0960-894x(03)00118-5
164608815 184454 0 None -58 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 380 7 4 4 2.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1 10.1016/j.ejmech.2021.113190
CHEMBL4846638 184454 0 None -58 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 380 7 4 4 2.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1 10.1016/j.ejmech.2021.113190
53359025 62353 0 None -25 5 Human 5.6 pKi = 5.6 Binding
Binding affinity to Histamine H1 receptorBinding affinity to Histamine H1 receptor
ChEMBL 339 5 1 3 2.5 O=C(CCCN1C2C3C4CC5C6C4C2C6C1(O)C53)c1ccc(F)cc1 10.1016/j.bmcl.2012.08.046
CHEMBL1779058 62353 0 None -25 5 Human 5.6 pKi = 5.6 Binding
Binding affinity to Histamine H1 receptorBinding affinity to Histamine H1 receptor
ChEMBL 339 5 1 3 2.5 O=C(CCCN1C2C3C4CC5C6C4C2C6C1(O)C53)c1ccc(F)cc1 10.1016/j.bmcl.2012.08.046
53324553 56855 0 None -3 10 Human 5.6 pKi = 5.6 Binding
Inhibition of H1 receptorInhibition of H1 receptor
ChEMBL 283 4 1 1 3.1 Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1 10.1016/j.bmcl.2010.11.075
CHEMBL1643900 56855 0 None -3 10 Human 5.6 pKi = 5.6 Binding
Inhibition of H1 receptorInhibition of H1 receptor
ChEMBL 283 4 1 1 3.1 Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1 10.1016/j.bmcl.2010.11.075
53324553 56855 0 None -3 10 Human 5.6 pKi = 5.6 Binding
Inhibition of histamine H1 receptor (unknown origin) by PDSP assayInhibition of histamine H1 receptor (unknown origin) by PDSP assay
ChEMBL 283 4 1 1 3.1 Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1 10.1016/j.bmc.2013.07.045
CHEMBL1643900 56855 0 None -3 10 Human 5.6 pKi = 5.6 Binding
Inhibition of histamine H1 receptor (unknown origin) by PDSP assayInhibition of histamine H1 receptor (unknown origin) by PDSP assay
ChEMBL 283 4 1 1 3.1 Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1 10.1016/j.bmc.2013.07.045
1204 1932 119 None -501 24 Human 5.6 pKi = 5.6 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
1247 1932 119 None -501 24 Human 5.6 pKi = 5.6 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
1375 1932 119 None -501 24 Human 5.6 pKi = 5.6 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
774 1932 119 None -501 24 Human 5.6 pKi = 5.6 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
CHEMBL90 1932 119 None -501 24 Human 5.6 pKi = 5.6 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
DB05381 1932 119 None -501 24 Human 5.6 pKi = 5.6 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
1204 1932 119 None -501 24 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
1247 1932 119 None -501 24 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
1375 1932 119 None -501 24 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
774 1932 119 None -501 24 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
CHEMBL90 1932 119 None -501 24 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
DB05381 1932 119 None -501 24 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
168269877 190027 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 783 22 6 8 3.0 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5171683 190027 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 783 22 6 8 3.0 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
164622259 185730 0 None -2290 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 336 6 4 5 1.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccco1 10.1016/j.ejmech.2021.113190
CHEMBL4865965 185730 0 None -2290 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 336 6 4 5 1.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccco1 10.1016/j.ejmech.2021.113190
168269877 190027 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 783 22 6 8 3.0 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5171683 190027 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 783 22 6 8 3.0 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
15749417 102097 0 None - 1 Guinea pig 7.6 pKi = 7.6 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 323 4 1 3 3.7 CN(C)CC/C=C1/c2ccccc2COc2cc(C(=O)O)ccc21 10.1021/jm00089a020
CHEMBL302215 102097 0 None - 1 Guinea pig 7.6 pKi = 7.6 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 323 4 1 3 3.7 CN(C)CC/C=C1/c2ccccc2COc2cc(C(=O)O)ccc21 10.1021/jm00089a020
53321494 57749 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 311 7 0 3 3.3 CN(CCF)CCC1=C(Cc2cnccn2)c2ccccc2C1 10.1016/j.bmcl.2010.12.053
CHEMBL1669407 57749 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 311 7 0 3 3.3 CN(CCF)CCC1=C(Cc2cnccn2)c2ccccc2C1 10.1016/j.bmcl.2010.12.053
53318874 57769 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 371 7 0 5 3.9 C[C@H](C1=C(CCN(C)Cc2cnccn2)Cc2ccccc21)c1cnccn1 10.1016/j.bmcl.2010.12.053
CHEMBL1669426 57769 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 371 7 0 5 3.9 C[C@H](C1=C(CCN(C)Cc2cnccn2)Cc2ccccc21)c1cnccn1 10.1016/j.bmcl.2010.12.053
18715382 8955 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.
ChEMBL 386 0 0 2 4.9 CC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3c(Cl)ccnc32)CC1 10.1016/S0960-894X(00)80290-5
CHEMBL10981 8955 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.
ChEMBL 386 0 0 2 4.9 CC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3c(Cl)ccnc32)CC1 10.1016/S0960-894X(00)80290-5
46216770 199269 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]Pyrilamine from human cloned histamine H1 receptorDisplacement of [3H]Pyrilamine from human cloned histamine H1 receptor
ChEMBL 313 5 1 1 4.6 c1ccc(CCNCC2c3ccccc3Cc3ccccc32)cc1 10.1016/j.bmcl.2009.12.064
CHEMBL590241 199269 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]Pyrilamine from human cloned histamine H1 receptorDisplacement of [3H]Pyrilamine from human cloned histamine H1 receptor
ChEMBL 313 5 1 1 4.6 c1ccc(CCNCC2c3ccccc3Cc3ccccc32)cc1 10.1016/j.bmcl.2009.12.064
10066369 120258 0 None -8 6 Human 5.6 pKi = 5.6 Binding
Compound was evaluated for binding affinity towards cloned human histamine H1 receptors stably expressed in CHO-K1 cells using [3H]mepyramineCompound was evaluated for binding affinity towards cloned human histamine H1 receptors stably expressed in CHO-K1 cells using [3H]mepyramine
ChEMBL 348 7 0 2 5.7 CC(C1=C(CCN(C(C)C)C(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL352375 120258 0 None -8 6 Human 5.6 pKi = 5.6 Binding
Compound was evaluated for binding affinity towards cloned human histamine H1 receptors stably expressed in CHO-K1 cells using [3H]mepyramineCompound was evaluated for binding affinity towards cloned human histamine H1 receptors stably expressed in CHO-K1 cells using [3H]mepyramine
ChEMBL 348 7 0 2 5.7 CC(C1=C(CCN(C(C)C)C(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
164614841 185274 0 None -691 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 388 7 4 4 3.0 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)C(C)C 10.1016/j.ejmech.2021.113190
CHEMBL4858849 185274 0 None -691 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 388 7 4 4 3.0 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)C(C)C 10.1016/j.ejmech.2021.113190
164628701 186467 0 None -144 3 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 338 5 4 4 1.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC1CCCCC1 10.1016/j.ejmech.2021.113190
CHEMBL4876743 186467 0 None -144 3 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 338 5 4 4 1.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC1CCCCC1 10.1016/j.ejmech.2021.113190
72152558 162404 5 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 331 5 1 5 2.7 Cc1cccc(N2CCN(CCNc3cncc(Cl)n3)CC2)c1 10.1021/acs.jmedchem.8b00718
CHEMBL4165881 162404 5 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 331 5 1 5 2.7 Cc1cccc(N2CCN(CCNc3cncc(Cl)n3)CC2)c1 10.1021/acs.jmedchem.8b00718
657255 199084 34 None -18 15 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 nan
CHEMBL588119 199084 34 None -18 15 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 nan
53317595 57759 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 341 5 0 3 3.8 FC1(F)CCN(CCC2=C(Cc3cnccn3)c3ccccc3C2)C1 10.1016/j.bmcl.2010.12.053
CHEMBL1669416 57759 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 341 5 0 3 3.8 FC1(F)CCN(CCC2=C(Cc3cnccn3)c3ccccc3C2)C1 10.1016/j.bmcl.2010.12.053
60785 205893 48 None -204 7 Guinea pig 7.6 pKi = 7.6 Binding
Binding constant against histamine H1 receptor (in vivo)Binding constant against histamine H1 receptor (in vivo)
ChEMBL 425 5 0 4 3.7 O=S1(=O)c2cccc3cccc(c23)N1CCCN1CCN(c2ccc(F)cc2)CC1 10.1021/jm00112a025
CHEMBL83894 205893 48 None -204 7 Guinea pig 7.6 pKi = 7.6 Binding
Binding constant against histamine H1 receptor (in vivo)Binding constant against histamine H1 receptor (in vivo)
ChEMBL 425 5 0 4 3.7 O=S1(=O)c2cccc3cccc(c23)N1CCCN1CCN(c2ccc(F)cc2)CC1 10.1021/jm00112a025
14248602 54442 0 None 21 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cellsDisplacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cells
ChEMBL 237 2 0 1 3.3 CN(C)CC1c2ccccc2Cc2ccccc21 10.1016/j.bmc.2009.08.016
CHEMBL160933 54442 0 None 21 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cellsDisplacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cells
ChEMBL 237 2 0 1 3.3 CN(C)CC1c2ccccc2Cc2ccccc21 10.1016/j.bmc.2009.08.016
242 470 124 None -22 51 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-pyrilamine from human histamine H1 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2021.113931
34 470 124 None -22 51 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-pyrilamine from human histamine H1 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2021.113931
60795 470 124 None -22 51 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-pyrilamine from human histamine H1 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2021.113931
CHEMBL1112 470 124 None -22 51 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-pyrilamine from human histamine H1 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2021.113931
DB01238 470 124 None -22 51 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-pyrilamine from human histamine H1 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2021.113931
242 470 124 None -22 51 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2016.05.053
34 470 124 None -22 51 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2016.05.053
60795 470 124 None -22 51 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2016.05.053
CHEMBL1112 470 124 None -22 51 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2016.05.053
DB01238 470 124 None -22 51 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2016.05.053
71072115 81258 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 515 8 1 5 5.1 N#Cc1cccc(C[C@@H](C(=O)O)N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.103
CHEMBL2158770 81258 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 515 8 1 5 5.1 N#Cc1cccc(C[C@@H](C(=O)O)N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.103
69348078 81291 0 None 1 2 Human 7.6 pKi = 7.6 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 476 7 1 4 5.4 O=C(O)[C@H](c1ccccc1)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158820 81291 0 None 1 2 Human 7.6 pKi = 7.6 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 476 7 1 4 5.4 O=C(O)[C@H](c1ccccc1)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
59296048 84016 0 None -6 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 582 9 4 7 2.4 CNS(=O)(=O)c1ccc2c(C(=O)NC[C@@H](O)CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)c[nH]c(=O)c2c1 10.1016/j.bmcl.2012.09.112
CHEMBL2207284 84016 0 None -6 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 582 9 4 7 2.4 CNS(=O)(=O)c1ccc2c(C(=O)NC[C@@H](O)CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)c[nH]c(=O)c2c1 10.1016/j.bmcl.2012.09.112
59295914 84084 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 638 9 4 8 2.2 CC1(O)CN(S(=O)(=O)c2ccc3c(C(=O)NC[C@@H](O)CN4CCC(Oc5ccc(Cl)c(Cl)c5)CC4)c[nH]c(=O)c3c2)C1 10.1016/j.bmcl.2012.09.112
CHEMBL2207655 84084 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 638 9 4 8 2.2 CC1(O)CN(S(=O)(=O)c2ccc3c(C(=O)NC[C@@H](O)CN4CCC(Oc5ccc(Cl)c(Cl)c5)CC4)c[nH]c(=O)c3c2)C1 10.1016/j.bmcl.2012.09.112
59296100 84088 0 None -7 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 460 7 3 5 3.0 Cc1cc(Cl)ccc1OC1CCN(C[C@H](O)CNC(=O)c2c[nH]nc2C(F)(F)F)CC1 10.1016/j.bmcl.2012.09.112
CHEMBL2207659 84088 0 None -7 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 460 7 3 5 3.0 Cc1cc(Cl)ccc1OC1CCN(C[C@H](O)CNC(=O)c2c[nH]nc2C(F)(F)F)CC1 10.1016/j.bmcl.2012.09.112
44396220 125423 1 None 1 6 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 295 6 0 2 4.1 c1ccc(Cc2ccccc2OCCN2CCCCC2)cc1 10.1021/acs.jmedchem.6b00981
CHEMBL364565 125423 1 None 1 6 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 295 6 0 2 4.1 c1ccc(Cc2ccccc2OCCN2CCCCC2)cc1 10.1021/acs.jmedchem.6b00981
134145957 154511 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 296 4 0 1 3.9 C[N+]1(C)CCC(Oc2ccccc2Cc2ccccc2)CC1 10.1021/acs.jmedchem.6b00981
CHEMBL3944629 154511 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 296 4 0 1 3.9 C[N+]1(C)CCC(Oc2ccccc2Cc2ccccc2)CC1 10.1021/acs.jmedchem.6b00981
CHEMBL3990701 154511 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 296 4 0 1 3.9 C[N+]1(C)CCC(Oc2ccccc2Cc2ccccc2)CC1 10.1021/acs.jmedchem.6b00981
23102749 82234 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 525 6 1 5 4.3 Cc1c(Cl)ccc(OC2CCN(C3CCN(S(=O)(=O)NC(=O)c4ccccc4)CC3)CC2)c1Cl 10.1016/j.bmcl.2012.08.124
CHEMBL2171016 82234 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 525 6 1 5 4.3 Cc1c(Cl)ccc(OC2CCN(C3CCN(S(=O)(=O)NC(=O)c4ccccc4)CC3)CC2)c1Cl 10.1016/j.bmcl.2012.08.124
22397445 82239 0 None -2 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 499 4 1 4 5.0 O=C(c1c[nH]c(=O)c2ccccc12)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
CHEMBL2171020 82239 0 None -2 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 499 4 1 4 5.0 O=C(c1c[nH]c(=O)c2ccccc12)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
69826668 82240 0 None -5 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 524 5 0 5 4.9 Cc1c(Cl)ccc(OC2CCN(C3CCN(C(=O)c4cccc(S(C)(=O)=O)c4)CC3)CC2)c1Cl 10.1016/j.bmcl.2012.08.124
CHEMBL2171021 82240 0 None -5 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 524 5 0 5 4.9 Cc1c(Cl)ccc(OC2CCN(C3CCN(C(=O)c4cccc(S(C)(=O)=O)c4)CC3)CC2)c1Cl 10.1016/j.bmcl.2012.08.124
71449857 82242 0 None 10 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 476 5 1 4 4.8 O=C(O)c1ccccc1C(=O)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
CHEMBL2171023 82242 0 None 10 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 476 5 1 4 4.8 O=C(O)c1ccccc1C(=O)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
71453505 82260 0 None 1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 554 6 1 6 4.5 CN(C)c1ccccc1S(=O)(=O)NC(=O)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
CHEMBL2171041 82260 0 None 1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 554 6 1 6 4.5 CN(C)c1ccccc1S(=O)(=O)NC(=O)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
17963226 82267 0 None -3 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 505 5 1 5 4.4 Cc1ccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(Cl)cc4C)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.124
CHEMBL2171048 82267 0 None -3 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 505 5 1 5 4.4 Cc1ccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(Cl)cc4C)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.124
44343573 111057 0 None - 1 Rat 5.6 pKi = 5.6 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 369 2 0 3 3.5 CCC(=O)N1CCN(C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/s0960-894x(98)00626-x
CHEMBL326289 111057 0 None - 1 Rat 5.6 pKi = 5.6 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 369 2 0 3 3.5 CCC(=O)N1CCN(C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/s0960-894x(98)00626-x
44334406 4863 0 None -660 3 Human 5.6 pKi = 5.6 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 462 10 1 5 3.8 O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccc(Cl)cc3)C2)cc1)C1CC1 10.1016/s0960-894x(02)00685-6
CHEMBL104344 4863 0 None -660 3 Human 5.6 pKi = 5.6 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 462 10 1 5 3.8 O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccc(Cl)cc3)C2)cc1)C1CC1 10.1016/s0960-894x(02)00685-6
10472143 119277 0 None -5623 16 Human 5.6 pKi = 5.6 Binding
Binding affinity towards Histamine H1 receptorBinding affinity towards Histamine H1 receptor
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
CHEMBL343755 119277 0 None -5623 16 Human 5.6 pKi = 5.6 Binding
Binding affinity towards Histamine H1 receptorBinding affinity towards Histamine H1 receptor
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
59295960 84097 0 None -12 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 532 8 4 6 2.6 NC(=O)c1c(OC2CCN(C[C@H](O)CNC(=O)c3c[nH]c(=O)c4ccccc34)CC2)ccc(Cl)c1Cl 10.1016/j.bmcl.2012.09.112
CHEMBL2207667 84097 0 None -12 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 532 8 4 6 2.6 NC(=O)c1c(OC2CCN(C[C@H](O)CNC(=O)c3c[nH]c(=O)c4ccccc34)CC2)ccc(Cl)c1Cl 10.1016/j.bmcl.2012.09.112
59296041 84100 0 None -3 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 558 8 3 8 2.1 CS(=O)(=O)c1ccc2c(C(=O)NC[C@@H](O)CN3CCC(Oc4ccc(C#N)c(Cl)c4)CC3)c[nH]c(=O)c2c1 10.1016/j.bmcl.2012.09.112
CHEMBL2207670 84100 0 None -3 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 558 8 3 8 2.1 CS(=O)(=O)c1ccc2c(C(=O)NC[C@@H](O)CN3CCC(Oc4ccc(C#N)c(Cl)c4)CC3)c[nH]c(=O)c2c1 10.1016/j.bmcl.2012.09.112
18722998 154474 2 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 191 2 0 2 2.2 CN1CCC(Oc2ccccc2)CC1 10.1021/acs.jmedchem.6b00981
CHEMBL3983211 154474 2 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 191 2 0 2 2.2 CN1CCC(Oc2ccccc2)CC1 10.1021/acs.jmedchem.6b00981
CHEMBL3990343 154474 2 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 191 2 0 2 2.2 CN1CCC(Oc2ccccc2)CC1 10.1021/acs.jmedchem.6b00981
46881468 6859 0 None -10 3 Human 5.6 pKi = 5.6 Binding
Activity at histamine H1 receptorActivity at histamine H1 receptor
ChEMBL 245 3 1 3 1.9 c1ccc(N2CCN(CC3CCCCN3)C2)cc1 10.1016/j.bmcl.2010.01.090
CHEMBL1084132 6859 0 None -10 3 Human 5.6 pKi = 5.6 Binding
Activity at histamine H1 receptorActivity at histamine H1 receptor
ChEMBL 245 3 1 3 1.9 c1ccc(N2CCN(CC3CCCCN3)C2)cc1 10.1016/j.bmcl.2010.01.090
10420190 206760 0 None -2 3 Guinea pig 5.6 pKi = 5.6 Binding
Binding affinity against H1 receptor of guinea pig by the displacement of [3H]mepyramine, bound to membranes of CHO cellsBinding affinity against H1 receptor of guinea pig by the displacement of [3H]mepyramine, bound to membranes of CHO cells
ChEMBL 195 8 2 2 2.3 NCCCCCCCCc1c[nH]cn1 10.1021/jm00002a008
CHEMBL90063 206760 0 None -2 3 Guinea pig 5.6 pKi = 5.6 Binding
Binding affinity against H1 receptor of guinea pig by the displacement of [3H]mepyramine, bound to membranes of CHO cellsBinding affinity against H1 receptor of guinea pig by the displacement of [3H]mepyramine, bound to membranes of CHO cells
ChEMBL 195 8 2 2 2.3 NCCCCCCCCc1c[nH]cn1 10.1021/jm00002a008
11533362 80632 0 None -7943 2 Human 5.6 pKi = 5.6 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 497 6 0 6 3.4 CS(=O)(=O)c1ccc(C(=O)N2CCN(c3ccc(OC4CCN(C5CCC5)CC4)cc3)CC2)cc1 10.1021/jm100064d
CHEMBL2151155 80632 0 None -7943 2 Human 5.6 pKi = 5.6 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 497 6 0 6 3.4 CS(=O)(=O)c1ccc(C(=O)N2CCN(c3ccc(OC4CCN(C5CCC5)CC4)cc3)CC2)cc1 10.1021/jm100064d
9976892 103954 42 None -10715 3 Human 5.6 pKi = 5.6 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 377 4 0 4 4.0 O=C1CCCN1c1ccc(Oc2ccc3c(c2)CCN(C2CCC2)CC3)nc1 10.1016/j.bmcl.2013.09.090
CHEMBL3092650 103954 42 None -10715 3 Human 5.6 pKi = 5.6 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 377 4 0 4 4.0 O=C1CCCN1c1ccc(Oc2ccc3c(c2)CCN(C2CCC2)CC3)nc1 10.1016/j.bmcl.2013.09.090
168292954 192997 0 None -44 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 388 8 4 4 2.5 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5202592 192997 0 None -44 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 388 8 4 4 2.5 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222660 192997 0 None -44 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 388 8 4 4 2.5 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
10039772 104361 0 None -100 3 Guinea pig 5.6 pKi = 5.6 Binding
Displacement of [3H]mepyramine bound to membranes of CHO cells expressing guinea pig H1 receptorsDisplacement of [3H]mepyramine bound to membranes of CHO cells expressing guinea pig H1 receptors
ChEMBL 288 7 3 2 3.1 S=C(NCCCCCc1c[nH]cn1)Nc1ccccc1 10.1021/jm00012a025
CHEMBL310087 104361 0 None -100 3 Guinea pig 5.6 pKi = 5.6 Binding
Displacement of [3H]mepyramine bound to membranes of CHO cells expressing guinea pig H1 receptorsDisplacement of [3H]mepyramine bound to membranes of CHO cells expressing guinea pig H1 receptors
ChEMBL 288 7 3 2 3.1 S=C(NCCCCCc1c[nH]cn1)Nc1ccccc1 10.1021/jm00012a025
112936341 137474 1 None 12 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 359 5 1 5 3.5 CN1CCN(c2nc(NCc3ccccc3)cc(-c3ccccc3)n2)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3753849 137474 1 None 12 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 359 5 1 5 3.5 CN1CCN(c2nc(NCc3ccccc3)cc(-c3ccccc3)n2)CC1 10.1016/j.bmcl.2015.12.035
10711079 98741 0 None -1318 2 Guinea pig 4.6 pKi = 4.6 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 323 5 2 3 3.4 O=C(Nc1ccc(Br)cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL277989 98741 0 None -1318 2 Guinea pig 4.6 pKi = 4.6 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 323 5 2 3 3.4 O=C(Nc1ccc(Br)cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
155515780 170024 0 None - 1 Guinea pig 6.6 pKi = 6.6 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysisDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysis
ChEMBL 318 6 0 4 1.8 CCN1CCc2ccc(OCCCN3CCOCC3)cc2C1=O 10.1016/j.bmcl.2019.04.015
CHEMBL4442619 170024 0 None - 1 Guinea pig 6.6 pKi = 6.6 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysisDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysis
ChEMBL 318 6 0 4 1.8 CCN1CCc2ccc(OCCCN3CCOCC3)cc2C1=O 10.1016/j.bmcl.2019.04.015
9947477 199968 0 None -25 2 Rat 6.6 pKi = 6.6 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
ChEMBL 368 10 2 3 4.6 Clc1ccc(C(CCNCCCCc2c[nH]cn2)c2ccccn2)cc1 10.1016/s0960-894x(03)00357-3
CHEMBL59512 199968 0 None -25 2 Rat 6.6 pKi = 6.6 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
ChEMBL 368 10 2 3 4.6 Clc1ccc(C(CCNCCCCc2c[nH]cn2)c2ccccn2)cc1 10.1016/s0960-894x(03)00357-3
95214051 162423 0 None 1 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 331 6 2 5 1.7 O=C(CO)NC[C@H]1CCN(Cc2csc(-c3ccccc3)n2)C1 10.1021/acs.jmedchem.8b00718
CHEMBL4166178 162423 0 None 1 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 331 6 2 5 1.7 O=C(CO)NC[C@H]1CCN(Cc2csc(-c3ccccc3)n2)C1 10.1021/acs.jmedchem.8b00718
44478385 5776 6 None -446 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cellsDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells
ChEMBL 342 9 3 4 2.5 N#C/N=C(/NCCCCc1c[nH]cn1)NCCSc1ccccc1 10.1021/jm900526h
CHEMBL1078642 5776 6 None -446 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cellsDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells
ChEMBL 342 9 3 4 2.5 N#C/N=C(/NCCCCc1c[nH]cn1)NCCSc1ccccc1 10.1021/jm900526h
164611474 185452 0 None -407 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 366 6 4 5 2.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1cccs1 10.1016/j.ejmech.2021.113190
CHEMBL4861704 185452 0 None -407 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 366 6 4 5 2.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1cccs1 10.1016/j.ejmech.2021.113190
9906978 42711 2 None -28 12 Human 6.6 pKi = 6.6 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL150161 42711 2 None -28 12 Human 6.6 pKi = 6.6 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
9906978 42711 2 None -28 12 Human 6.6 pKi = 6.6 Binding
Binding affinity to human cloned histamine H1 receptor by radioligand binding assayBinding affinity to human cloned histamine H1 receptor by radioligand binding assay
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmcl.2006.03.057
CHEMBL150161 42711 2 None -28 12 Human 6.6 pKi = 6.6 Binding
Binding affinity to human cloned histamine H1 receptor by radioligand binding assayBinding affinity to human cloned histamine H1 receptor by radioligand binding assay
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmcl.2006.03.057
9850828 169902 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human histamine H1 receptor expressed in CHO-K1 cellsBinding affinity towards human histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 562 11 2 5 5.0 NC(=O)N(O)CCC#Cc1ccc(OCCCCN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2004.08.060
CHEMBL444083 169902 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human histamine H1 receptor expressed in CHO-K1 cellsBinding affinity towards human histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 562 11 2 5 5.0 NC(=O)N(O)CCC#Cc1ccc(OCCCCN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2004.08.060
155547818 173568 0 None 2 2 Guinea pig 7.6 pKi = 7.6 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysisDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysis
ChEMBL 302 5 0 3 2.6 CC1CCCN1CCCOc1ccc2c(c1)C(=O)N(C)CC2 10.1016/j.bmcl.2019.04.015
CHEMBL4532574 173568 0 None 2 2 Guinea pig 7.6 pKi = 7.6 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysisDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysis
ChEMBL 302 5 0 3 2.6 CC1CCCN1CCCOc1ccc2c(c1)C(=O)N(C)CC2 10.1016/j.bmcl.2019.04.015
44449794 158262 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 333 5 1 4 3.5 COc1cc(Cl)ccc1O[C@H](c1ccccc1)[C@H]1CNCCO1 10.1016/j.bmcl.2008.03.050
CHEMBL408868 158262 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 333 5 1 4 3.5 COc1cc(Cl)ccc1O[C@H](c1ccccc1)[C@H]1CNCCO1 10.1016/j.bmcl.2008.03.050
11848679 89244 0 None -204 6 Human 5.6 pKi = 5.6 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 489 9 3 9 2.9 CCOc1cc(CN2CCC(Nc3nc4cc(S(N)(=O)=O)ccc4o3)CC2)cc(OCC)c1N 10.1016/j.bmcl.2009.09.024
CHEMBL236788 89244 0 None -204 6 Human 5.6 pKi = 5.6 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 489 9 3 9 2.9 CCOc1cc(CN2CCC(Nc3nc4cc(S(N)(=O)=O)ccc4o3)CC2)cc(OCC)c1N 10.1016/j.bmcl.2009.09.024
146025727 171685 0 None -97 27 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4466483 171685 0 None -97 27 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
71456046 84075 0 None -1737 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis
ChEMBL 389 6 0 4 4.2 COc1ccccc1N1CCN(Cc2cc(CN(C)C)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207637 84075 0 None -1737 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis
ChEMBL 389 6 0 4 4.2 COc1ccccc1N1CCN(Cc2cc(CN(C)C)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
44209472 70172 2 None -144 11 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]pyrilamine from human H1 receptor by liquid scintillation countingDisplacement of [3H]pyrilamine from human H1 receptor by liquid scintillation counting
ChEMBL 315 6 0 4 2.8 Fc1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940420 70172 2 None -144 11 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]pyrilamine from human H1 receptor by liquid scintillation countingDisplacement of [3H]pyrilamine from human H1 receptor by liquid scintillation counting
ChEMBL 315 6 0 4 2.8 Fc1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
1072350 69027 5 None -4 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 269 3 0 5 2.2 c1ccc2c(c1)nc1n(CCN3CCCCC3)cnn21 10.1021/jm2011589
CHEMBL1923529 69027 5 None -4 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 269 3 0 5 2.2 c1ccc2c(c1)nc1n(CCN3CCCCC3)cnn21 10.1021/jm2011589
44304978 167889 0 None -1230 3 Human 4.6 pKi = 4.6 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 396 11 0 5 2.8 CCCCCC(=O)c1ccc(OCCCN2CCN(S(C)(=O)=O)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL431172 167889 0 None -1230 3 Human 4.6 pKi = 4.6 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 396 11 0 5 2.8 CCCCCC(=O)c1ccc(OCCCN2CCN(S(C)(=O)=O)CC2)cc1 10.1016/s0960-894x(02)00309-8
46230651 200508 0 None -125 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]Pyrilamine from human cloned histamine H1 receptorDisplacement of [3H]Pyrilamine from human cloned histamine H1 receptor
ChEMBL 289 2 1 2 3.8 COc1ccc2c3c(ccc2c1)Cc1ccccc1C3CN 10.1016/j.bmcl.2009.12.064
CHEMBL598753 200508 0 None -125 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]Pyrilamine from human cloned histamine H1 receptorDisplacement of [3H]Pyrilamine from human cloned histamine H1 receptor
ChEMBL 289 2 1 2 3.8 COc1ccc2c3c(ccc2c1)Cc1ccccc1C3CN 10.1016/j.bmcl.2009.12.064
164585622 184928 0 None 1 2 Human 5.6 pKi = 5.6 Binding
Binding affinity to H1 receptor (unknown origin)Binding affinity to H1 receptor (unknown origin)
ChEMBL 506 6 2 7 5.5 O=C(O)c1cc(-c2ccc(-c3cc(CO)on3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.1c00164
CHEMBL4853466 184928 0 None 1 2 Human 5.6 pKi = 5.6 Binding
Binding affinity to H1 receptor (unknown origin)Binding affinity to H1 receptor (unknown origin)
ChEMBL 506 6 2 7 5.5 O=C(O)c1cc(-c2ccc(-c3cc(CO)on3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.1c00164
24740863 89158 0 None -3 6 Human 6.6 pKi = 6.6 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 385 6 1 5 5.0 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1Cl 10.1016/j.bmcl.2009.09.024
CHEMBL236610 89158 0 None -3 6 Human 6.6 pKi = 6.6 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 385 6 1 5 5.0 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1Cl 10.1016/j.bmcl.2009.09.024
56781741 162635 4 None 1 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 337 6 0 6 3.0 Cc1cc(C)n(C2CN(CCCc3nc(-c4ccccc4)no3)C2)n1 10.1021/acs.jmedchem.8b00718
CHEMBL4169603 162635 4 None 1 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 337 6 0 6 3.0 Cc1cc(C)n(C2CN(CCCc3nc(-c4ccccc4)no3)C2)n1 10.1021/acs.jmedchem.8b00718
168291233 192979 0 None -6 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 373 8 4 5 1.4 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)o2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5200106 192979 0 None -6 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 373 8 4 5 1.4 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)o2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222556 192979 0 None -6 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 373 8 4 5 1.4 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)o2)cc1 10.1021/acs.jmedchem.1c00692
44326298 207909 0 None 3 3 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 293 2 0 2 3.8 CN(C)CC1C[C@H]2c3ccccc3Cc3ccccc3[C@H]2O1 10.1016/j.bmcl.2004.03.069
CHEMBL96732 207909 0 None 3 3 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 293 2 0 2 3.8 CN(C)CC1C[C@H]2c3ccccc3Cc3ccccc3[C@H]2O1 10.1016/j.bmcl.2004.03.069
1170 1633 75 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation counting
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1016/j.bmcl.2009.07.047
3348 1633 75 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation counting
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1016/j.bmcl.2009.07.047
4819 1633 75 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation counting
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1016/j.bmcl.2009.07.047
74685737 1633 75 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation counting
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1016/j.bmcl.2009.07.047
CHEMBL914 1633 75 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation counting
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1016/j.bmcl.2009.07.047
DB00950 1633 75 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation counting
ChEMBL 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 10.1016/j.bmcl.2009.07.047
44335237 5121 0 None 3 3 Human 7.6 pKi = 7.6 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 407 7 0 5 4.1 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(C#N)cc3C)cc2)CC1 10.1016/s0960-894x(02)00648-0
CHEMBL105669 5121 0 None 3 3 Human 7.6 pKi = 7.6 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 407 7 0 5 4.1 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(C#N)cc3C)cc2)CC1 10.1016/s0960-894x(02)00648-0
11963995 91865 0 None -15 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 387 6 1 4 3.8 CCOc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)ccc1Cl 10.1021/jm701144e
CHEMBL241329 91865 0 None -15 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 387 6 1 4 3.8 CCOc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)ccc1Cl 10.1021/jm701144e
49783209 17609 0 None -1380 26 Guinea pig 5.6 pKi = 5.6 Binding
Binding affinity to guinea pig histamine H1 receptorBinding affinity to guinea pig histamine H1 receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258223 17609 0 None -1380 26 Guinea pig 5.6 pKi = 5.6 Binding
Binding affinity to guinea pig histamine H1 receptorBinding affinity to guinea pig histamine H1 receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
409544 202914 4 None -194 3 Human 6.6 pKi = 6.6 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 390 11 0 5 4.0 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL62803 202914 4 None -194 3 Human 6.6 pKi = 6.6 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 390 11 0 5 4.0 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
44304383 203303 0 None -27 3 Human 6.6 pKi = 6.6 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 418 12 0 5 4.6 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC(C)C)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL64775 203303 0 None -27 3 Human 6.6 pKi = 6.6 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 418 12 0 5 4.6 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC(C)C)CC2)cc1 10.1016/s0960-894x(02)00309-8
44335559 109709 0 None -162 4 Human 6.6 pKi = 6.6 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 334 6 0 3 4.7 CC1CCCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)C1 10.1016/s0960-894x(02)00648-0
CHEMBL322873 109709 0 None -162 4 Human 6.6 pKi = 6.6 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 334 6 0 3 4.7 CC1CCCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)C1 10.1016/s0960-894x(02)00648-0
79698 202192 95 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cellsDisplacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cells
ChEMBL 211 4 1 1 3.2 NCCC(c1ccccc1)c1ccccc1 10.1016/j.bmc.2009.08.016
CHEMBL609579 202192 95 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cellsDisplacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cells
ChEMBL 211 4 1 1 3.2 NCCC(c1ccccc1)c1ccccc1 10.1016/j.bmc.2009.08.016
25450664 161996 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 392 6 0 6 3.9 COC(=O)c1ccc(-c2nc(CN(C)C[C@@H]3Cc4ccccc4O3)c(C)o2)cc1 10.1021/acs.jmedchem.8b00718
CHEMBL4159365 161996 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 392 6 0 6 3.9 COC(=O)c1ccc(-c2nc(CN(C)C[C@@H]3Cc4ccccc4O3)c(C)o2)cc1 10.1021/acs.jmedchem.8b00718
242 470 124 None -22 51 Human 7.6 pKi = 7.6 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
34 470 124 None -22 51 Human 7.6 pKi = 7.6 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
60795 470 124 None -22 51 Human 7.6 pKi = 7.6 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
CHEMBL1112 470 124 None -22 51 Human 7.6 pKi = 7.6 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
DB01238 470 124 None -22 51 Human 7.6 pKi = 7.6 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
53322839 57766 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 373 7 0 5 3.8 C[C@H](C1=C(CCN(C)Cc2nccn2C)Cc2ccccc21)c1cnccn1 10.1016/j.bmcl.2010.12.053
CHEMBL1669423 57766 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 373 7 0 5 3.8 C[C@H](C1=C(CCN(C)Cc2nccn2C)Cc2ccccc21)c1cnccn1 10.1016/j.bmcl.2010.12.053
11808040 168395 0 None -2 6 Human 7.5 pKi = 7.5 Binding
Compound was evaluated for binding affinity towards cloned human histamine H1 receptors stably expressed in CHO-K1 cells using [3H]mepyramineCompound was evaluated for binding affinity towards cloned human histamine H1 receptors stably expressed in CHO-K1 cells using [3H]mepyramine
ChEMBL 278 4 0 2 3.8 CC(C1=C(CN(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL434684 168395 0 None -2 6 Human 7.5 pKi = 7.5 Binding
Compound was evaluated for binding affinity towards cloned human histamine H1 receptors stably expressed in CHO-K1 cells using [3H]mepyramineCompound was evaluated for binding affinity towards cloned human histamine H1 receptors stably expressed in CHO-K1 cells using [3H]mepyramine
ChEMBL 278 4 0 2 3.8 CC(C1=C(CN(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
46929647 16758 0 None -19 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 355 5 2 3 4.3 FC(F)(F)c1ccc(SC[C@H](c2c[nH]cn2)C2CCNCC2)cc1 10.1021/jm100643t
CHEMBL1243394 16758 0 None -19 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 355 5 2 3 4.3 FC(F)(F)c1ccc(SC[C@H](c2c[nH]cn2)C2CCNCC2)cc1 10.1021/jm100643t
28357663 162144 2 None 1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 301 5 0 3 3.3 Cc1ccn(CCN2CCC(Cc3ccccc3F)CC2)n1 10.1021/acs.jmedchem.8b00718
CHEMBL4161837 162144 2 None 1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 301 5 0 3 3.3 Cc1ccn(CCN2CCC(Cc3ccccc3F)CC2)n1 10.1021/acs.jmedchem.8b00718
49841846 69738 0 None -812 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human H1 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H1 receptor expressed in HEK cell membranes
ChEMBL 325 2 1 6 2.7 CN1CCN(c2nc(N)nc3cc(-c4ccsc4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL1935572 69738 0 None -812 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human H1 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H1 receptor expressed in HEK cell membranes
ChEMBL 325 2 1 6 2.7 CN1CCN(c2nc(N)nc3cc(-c4ccsc4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
10451094 202473 0 None -56234 3 Human 4.6 pKi = 4.6 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 359 9 1 5 1.5 NCCC(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL61120 202473 0 None -56234 3 Human 4.6 pKi = 4.6 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 359 9 1 5 1.5 NCCC(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
127038376 136783 0 None -323 5 Guinea pig 5.6 pKi = 5.6 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellumDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum
ChEMBL 502 6 0 7 4.2 O=[N+]([O-])c1ccc(S(=O)(=O)N2CCC(CN3CCC(c4noc5cc(F)ccc45)CC3)CC2)cc1 10.1039/C4MD00578C
CHEMBL3741292 136783 0 None -323 5 Guinea pig 5.6 pKi = 5.6 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellumDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum
ChEMBL 502 6 0 7 4.2 O=[N+]([O-])c1ccc(S(=O)(=O)N2CCC(CN3CCC(c4noc5cc(F)ccc45)CC3)CC2)cc1 10.1039/C4MD00578C
44304751 101023 0 None -7 3 Human 6.5 pKi = 6.5 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 422 11 0 4 4.7 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccccc3)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL294519 101023 0 None -7 3 Human 6.5 pKi = 6.5 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 422 11 0 4 4.7 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccccc3)CC2)cc1 10.1016/s0960-894x(02)00309-8
44335225 164155 0 None -190 4 Human 5.5 pKi = 5.5 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 347 6 1 4 3.1 N#Cc1ccc(-c2ccc(OCCCN3CC4CNCC4C3)cc2)cc1 10.1016/s0960-894x(02)00648-0
CHEMBL421026 164155 0 None -190 4 Human 5.5 pKi = 5.5 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 347 6 1 4 3.1 N#Cc1ccc(-c2ccc(OCCCN3CC4CNCC4C3)cc2)cc1 10.1016/s0960-894x(02)00648-0
168294178 193035 0 None -1 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 414 5 4 4 4.4 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)C2CCCCC2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5205197 193035 0 None -1 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 414 5 4 4 4.4 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)C2CCCCC2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222887 193035 0 None -1 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 414 5 4 4 4.4 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)C2CCCCC2)cc1 10.1021/acs.jmedchem.1c00692
164627241 186429 0 None -95 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 438 6 4 4 3.1 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(Br)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4876267 186429 0 None -95 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 438 6 4 4 3.1 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(Br)cc1 10.1016/j.ejmech.2021.113190
164627189 186321 0 None -275 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 298 6 4 4 1.0 CCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
CHEMBL4874758 186321 0 None -275 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 298 6 4 4 1.0 CCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
118721929 116093 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting method
ChEMBL 394 2 0 2 5.3 CC(C)CC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/jm501086v
CHEMBL3357042 116093 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting method
ChEMBL 394 2 0 2 5.3 CC(C)CC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/jm501086v
162645254 179683 3 None -371 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cell membranes co-expressing RGS4 measured after 60 mins by scintillation counting analysisDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cell membranes co-expressing RGS4 measured after 60 mins by scintillation counting analysis
ChEMBL 398 7 0 5 4.2 N#Cc1ccc(-c2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)cc1 10.1016/j.ejmech.2020.113041
CHEMBL4743583 179683 3 None -371 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cell membranes co-expressing RGS4 measured after 60 mins by scintillation counting analysisDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cell membranes co-expressing RGS4 measured after 60 mins by scintillation counting analysis
ChEMBL 398 7 0 5 4.2 N#Cc1ccc(-c2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)cc1 10.1016/j.ejmech.2020.113041
24841480 183899 0 None -14 20 Human 7.5 pKi = 7.5 Binding
Antagonist activity at histamine H1 receptor (unknown origin) by PDSP assayAntagonist activity at histamine H1 receptor (unknown origin) by PDSP assay
ChEMBL 340 3 0 4 4.5 O=C(OCCN1CCCC1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
CHEMBL481153 183899 0 None -14 20 Human 7.5 pKi = 7.5 Binding
Antagonist activity at histamine H1 receptor (unknown origin) by PDSP assayAntagonist activity at histamine H1 receptor (unknown origin) by PDSP assay
ChEMBL 340 3 0 4 4.5 O=C(OCCN1CCCC1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
9928323 11937 0 None - 1 Guinea pig 7.5 pKi = 7.5 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 349 5 1 3 4.1 CN(C)CC/C=C1/c2ccccc2COc2ccc(/C=C/C(=O)O)cc21 10.1021/jm00089a020
CHEMBL1182766 11937 0 None - 1 Guinea pig 7.5 pKi = 7.5 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 349 5 1 3 4.1 CN(C)CC/C=C1/c2ccccc2COc2ccc(/C=C/C(=O)O)cc21 10.1021/jm00089a020
CHEMBL264979 11937 0 None - 1 Guinea pig 7.5 pKi = 7.5 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 349 5 1 3 4.1 CN(C)CC/C=C1/c2ccccc2COc2ccc(/C=C/C(=O)O)cc21 10.1021/jm00089a020
44326433 207858 0 None 1 3 Human 7.5 pKi = 7.5 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 409 3 0 2 6.1 c1ccc(C2CCN(CC3C[C@@H]4c5ccccc5Cc5ccccc5[C@H]4O3)CC2)cc1 10.1016/j.bmcl.2004.03.069
CHEMBL96471 207858 0 None 1 3 Human 7.5 pKi = 7.5 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 409 3 0 2 6.1 c1ccc(C2CCN(CC3C[C@@H]4c5ccccc5Cc5ccccc5[C@H]4O3)CC2)cc1 10.1016/j.bmcl.2004.03.069
23551948 110396 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 341 2 0 3 2.7 O=CN1CCN(C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/s0960-894x(98)00626-x
CHEMBL324336 110396 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 341 2 0 3 2.7 O=CN1CCN(C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/s0960-894x(98)00626-x
162647537 179804 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to H1 receptor (unknown origin)Binding affinity to H1 receptor (unknown origin)
ChEMBL 294 3 0 2 3.0 CN(C)CCN1C(=O)c2ccccc2CCc2ccccc21 10.1016/j.bmcl.2020.127493
CHEMBL4744893 179804 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to H1 receptor (unknown origin)Binding affinity to H1 receptor (unknown origin)
ChEMBL 294 3 0 2 3.0 CN(C)CCN1C(=O)c2ccccc2CCc2ccccc21 10.1016/j.bmcl.2020.127493
14885640 16778 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 340 3 0 2 4.1 CC(=O)N(C)CC/C=C1\c2ccc(Cl)cc2CCc2cccnc21 10.1021/jm00105a069
CHEMBL124466 16778 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 340 3 0 2 4.1 CC(=O)N(C)CC/C=C1\c2ccc(Cl)cc2CCc2cccnc21 10.1021/jm00105a069
9928224 134357 0 None -1621 3 Guinea pig 6.5 pKi = 6.5 Binding
Displacement of [3H]N-alpha-methylhistamine from histamine H1 receptor in guinea pig brainDisplacement of [3H]N-alpha-methylhistamine from histamine H1 receptor in guinea pig brain
ChEMBL 346 6 2 3 3.3 O=C(CCN1CCC(Cc2c[nH]cn2)CC1)Nc1ccc(Cl)cc1 10.1016/j.bmcl.2005.09.076
CHEMBL371730 134357 0 None -1621 3 Guinea pig 6.5 pKi = 6.5 Binding
Displacement of [3H]N-alpha-methylhistamine from histamine H1 receptor in guinea pig brainDisplacement of [3H]N-alpha-methylhistamine from histamine H1 receptor in guinea pig brain
ChEMBL 346 6 2 3 3.3 O=C(CCN1CCC(Cc2c[nH]cn2)CC1)Nc1ccc(Cl)cc1 10.1016/j.bmcl.2005.09.076
14885629 34978 0 None - 1 Rat 5.5 pKi = 5.5 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 336 0 0 2 3.8 CC(=O)N1CCC(=C2c3cc(F)ccc3CCc3cccnc32)CC1 10.1021/jm00105a069
CHEMBL143272 34978 0 None - 1 Rat 5.5 pKi = 5.5 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 336 0 0 2 3.8 CC(=O)N1CCC(=C2c3cc(F)ccc3CCc3cccnc32)CC1 10.1021/jm00105a069
162653991 180547 0 None -245 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-pyrilamine from human H1 histamine receptor expressed in human HEK293 cellsDisplacement of [3H]-pyrilamine from human H1 histamine receptor expressed in human HEK293 cells
ChEMBL 470 4 0 3 6.0 C[C@H]1CN(CC[C@H]2CC[C@H](N3C(=O)CC4(CCCC4)CC3=O)CC2)CCc2ccc(Cl)cc21 10.1016/j.bmcl.2020.127681
CHEMBL4753808 180547 0 None -245 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-pyrilamine from human H1 histamine receptor expressed in human HEK293 cellsDisplacement of [3H]-pyrilamine from human H1 histamine receptor expressed in human HEK293 cells
ChEMBL 470 4 0 3 6.0 C[C@H]1CN(CC[C@H]2CC[C@H](N3C(=O)CC4(CCCC4)CC3=O)CC2)CCc2ccc(Cl)cc21 10.1016/j.bmcl.2020.127681
10347051 67161 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human histamine H1 receptor expressed in CHO-K1 cellsBinding affinity towards human histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 534 9 2 5 4.3 NC(=O)N(O)CCC#Cc1ccc(OCCN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2004.08.060
CHEMBL187637 67161 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human histamine H1 receptor expressed in CHO-K1 cellsBinding affinity towards human histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 534 9 2 5 4.3 NC(=O)N(O)CCC#Cc1ccc(OCCN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2004.08.060
44591135 190177 0 None -190 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 532 10 0 4 8.0 CN(CC/C=C1\c2ccccc2Sc2ccc(Cl)cc21)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
CHEMBL517407 190177 0 None -190 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 532 10 0 4 8.0 CN(CC/C=C1\c2ccccc2Sc2ccc(Cl)cc21)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
90654501 110309 0 None -31622 3 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 314 6 0 5 3.1 Cc1nnc(C)n1-c1ccc(OCCCN2CCCCC2)cc1 10.1016/j.ejmech.2014.03.014
CHEMBL3238444 110309 0 None -31622 3 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 314 6 0 5 3.1 Cc1nnc(C)n1-c1ccc(OCCCN2CCCCC2)cc1 10.1016/j.ejmech.2014.03.014
132060734 163124 0 None 3 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-Pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 391 5 0 4 4.0 C=C(C)CN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)C3)CC1 10.1016/j.ejmech.2018.02.024
CHEMBL4177497 163124 0 None 3 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-Pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 391 5 0 4 4.0 C=C(C)CN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)C3)CC1 10.1016/j.ejmech.2018.02.024
44326427 107516 0 None 144 3 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 348 2 0 3 3.5 CN1CCN(CC2C[C@@H]3c4ccccc4Cc4ccccc4[C@H]3O2)CC1 10.1016/j.bmcl.2004.03.069
CHEMBL318659 107516 0 None 144 3 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 348 2 0 3 3.5 CN1CCN(CC2C[C@@H]3c4ccccc4Cc4ccccc4[C@H]3O2)CC1 10.1016/j.bmcl.2004.03.069
2247 505 81 None -4 42 Human 8.5 pKi = 8.5 Binding
Binding affinity towards histamine H1 receptorBinding affinity towards histamine H1 receptor
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1021/jm0205651
249 505 81 None -4 42 Human 8.5 pKi = 8.5 Binding
Binding affinity towards histamine H1 receptorBinding affinity towards histamine H1 receptor
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1021/jm0205651
2603 505 81 None -4 42 Human 8.5 pKi = 8.5 Binding
Binding affinity towards histamine H1 receptorBinding affinity towards histamine H1 receptor
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1021/jm0205651
CHEMBL296419 505 81 None -4 42 Human 8.5 pKi = 8.5 Binding
Binding affinity towards histamine H1 receptorBinding affinity towards histamine H1 receptor
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1021/jm0205651
DB00637 505 81 None -4 42 Human 8.5 pKi = 8.5 Binding
Binding affinity towards histamine H1 receptorBinding affinity towards histamine H1 receptor
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1021/jm0205651
10361564 51292 0 None 1 3 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]- pyrilamine from rat brain membrane Histamine H1 receptorDisplacement of [3H]- pyrilamine from rat brain membrane Histamine H1 receptor
ChEMBL 366 5 0 4 4.1 Cn1c(=O)sc2cc(CCN3CCC(Cc4ccccc4)CC3)ccc21 10.1016/s0960-894x(02)00123-3
CHEMBL15809 51292 0 None 1 3 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]- pyrilamine from rat brain membrane Histamine H1 receptorDisplacement of [3H]- pyrilamine from rat brain membrane Histamine H1 receptor
ChEMBL 366 5 0 4 4.1 Cn1c(=O)sc2cc(CCN3CCC(Cc4ccccc4)CC3)ccc21 10.1016/s0960-894x(02)00123-3
10399921 119805 0 None 4 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cellsDisplacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cells
ChEMBL 251 4 1 1 3.7 CNCCCC1c2ccccc2Cc2ccccc21 10.1016/j.bmc.2009.08.016
CHEMBL348302 119805 0 None 4 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cellsDisplacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cells
ChEMBL 251 4 1 1 3.7 CNCCCC1c2ccccc2Cc2ccccc21 10.1016/j.bmc.2009.08.016
46884731 7909 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 323 6 0 4 3.6 COc1ccc2c(c1)CC(CCN(C)C)=C2[C@@H](C)c1cnccn1 10.1016/j.bmcl.2010.02.055
CHEMBL1090175 7909 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 323 6 0 4 3.6 COc1ccc2c(c1)CC(CCN(C)C)=C2[C@@H](C)c1cnccn1 10.1016/j.bmcl.2010.02.055
46884667 8287 0 None 1174 2 Human 8.5 pKi = 8.5 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 312 5 0 3 4.5 Cc1csc([C@H](C)C2=C(CCN(C)C)Cc3ccccc32)n1 10.1016/j.bmcl.2010.02.055
CHEMBL1092599 8287 0 None 1174 2 Human 8.5 pKi = 8.5 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 312 5 0 3 4.5 Cc1csc([C@H](C)C2=C(CCN(C)C)Cc3ccccc32)n1 10.1016/j.bmcl.2010.02.055
6075 150108 42 None 2 16 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
CHEMBL395110 150108 42 None 2 16 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
24824726 161109 1 None 2 6 Human 8.5 pKi = 8.5 Binding
Antagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysisAntagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysis
ChEMBL 496 11 1 6 3.6 COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL4060529 161109 1 None 2 6 Human 8.5 pKi = 8.5 Binding
Antagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysisAntagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysis
ChEMBL 496 11 1 6 3.6 COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL4117079 161109 1 None 2 6 Human 8.5 pKi = 8.5 Binding
Antagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysisAntagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysis
ChEMBL 496 11 1 6 3.6 COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL5282336 161109 1 None 2 6 Human 8.5 pKi = 8.5 Binding
Antagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysisAntagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysis
ChEMBL 496 11 1 6 3.6 COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL5286389 161109 1 None 2 6 Human 8.5 pKi = 8.5 Binding
Antagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysisAntagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysis
ChEMBL 496 11 1 6 3.6 COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL5284242 194615 0 None 56 3 Human 8.5 pKi = 8.5 Binding
Antagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysisAntagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysis
ChEMBL 510 11 0 6 4.0 COCCCC(=O)N(C)CCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL5315342 194615 0 None 56 3 Human 8.5 pKi = 8.5 Binding
Antagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysisAntagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysis
ChEMBL 510 11 0 6 4.0 COCCCC(=O)N(C)CCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
75306277 109254 0 None -1 23 Human 8.5 pKi = 8.5 Binding
Binding affinity to H1 histamine receptor (unknown origin) by PDSP assayBinding affinity to H1 histamine receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
CHEMBL3217984 109254 0 None -1 23 Human 8.5 pKi = 8.5 Binding
Binding affinity to H1 histamine receptor (unknown origin) by PDSP assayBinding affinity to H1 histamine receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
71463287 84202 0 None 79 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 420 7 1 5 4.1 N#Cc1cccc(OC[C@@H](O)CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)c1 10.1016/j.bmcl.2012.09.113
CHEMBL2208419 84202 0 None 79 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 420 7 1 5 4.1 N#Cc1cccc(OC[C@@H](O)CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)c1 10.1016/j.bmcl.2012.09.113
155515934 170015 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 402 2 0 4 4.7 Clc1ccc2c(c1)CCc1cccnc1C2=C1CCN(Cc2ncccn2)CC1 10.1021/acs.jmedchem.9b00447
CHEMBL4442502 170015 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 402 2 0 4 4.7 Clc1ccc2c(c1)CCc1cccnc1C2=C1CCN(Cc2ncccn2)CC1 10.1021/acs.jmedchem.9b00447
89474811 172906 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 401 2 0 3 5.3 Clc1ccc2c(c1)CCc1cccnc1C2=C1CCN(Cc2ccccn2)CC1 10.1021/acs.jmedchem.9b00447
CHEMBL4516137 172906 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 401 2 0 3 5.3 Clc1ccc2c(c1)CCc1cccnc1C2=C1CCN(Cc2ccccn2)CC1 10.1021/acs.jmedchem.9b00447
155567448 175982 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 350 1 0 2 4.9 Clc1ccc2c(c1)CCc1cccnc1C2=C1CCN(C2CC2)CC1 10.1021/acs.jmedchem.9b00447
CHEMBL4588726 175982 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 350 1 0 2 4.9 Clc1ccc2c(c1)CCc1cccnc1C2=C1CCN(C2CC2)CC1 10.1021/acs.jmedchem.9b00447
4671324 13196 2 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 269 7 0 2 3.6 CN(C)CCCOc1ccccc1Cc1ccccc1 10.1021/acs.jmedchem.6b00981
CHEMBL1191054 13196 2 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 269 7 0 2 3.6 CN(C)CCCOc1ccccc1Cc1ccccc1 10.1021/acs.jmedchem.6b00981
CHEMBL3955589 13196 2 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 269 7 0 2 3.6 CN(C)CCCOc1ccccc1Cc1ccccc1 10.1021/acs.jmedchem.6b00981
45268653 195729 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 382 6 1 5 3.1 CN(CCO)C1CCN(c2nc3ccccc3n2Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2009.05.086
CHEMBL557210 195729 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 382 6 1 5 3.1 CN(CCO)C1CCN(c2nc3ccccc3n2Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2009.05.086
3191 102858 97 None 2 25 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
CHEMBL305660 102858 97 None 2 25 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
103 4153 61 None -1 53 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human histamine H1 receptorBinding affinity towards human histamine H1 receptor
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
2875 4153 61 None -1 53 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human histamine H1 receptorBinding affinity towards human histamine H1 receptor
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
5736 4153 61 None -1 53 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human histamine H1 receptorBinding affinity towards human histamine H1 receptor
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
CHEMBL285802 4153 61 None -1 53 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human histamine H1 receptorBinding affinity towards human histamine H1 receptor
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
DB09225 4153 61 None -1 53 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human histamine H1 receptorBinding affinity towards human histamine H1 receptor
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
69314950 78660 0 None 4 3 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 279 2 1 2 3.4 CNC[C@@H]1C[C@H]2c3ccccc3Cc3ccccc3[C@@H]2O1 10.1016/j.bmcl.2004.03.069
CHEMBL2112371 78660 0 None 4 3 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 279 2 1 2 3.4 CNC[C@@H]1C[C@H]2c3ccccc3Cc3ccccc3[C@@H]2O1 10.1016/j.bmcl.2004.03.069
135398745 2914 112 None 1 65 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human histamine H1 receptorBinding affinity towards human histamine H1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm030480f
47 2914 112 None 1 65 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human histamine H1 receptorBinding affinity towards human histamine H1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm030480f
CHEMBL715 2914 112 None 1 65 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human histamine H1 receptorBinding affinity towards human histamine H1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm030480f
DB00334 2914 112 None 1 65 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human histamine H1 receptorBinding affinity towards human histamine H1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm030480f
70941112 175390 5 None 117 2 Guinea pig 8.4 pKi = 8.4 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysisDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysis
ChEMBL 288 6 1 3 2.3 NC(=O)c1ccc(OCCCN2C[C@H]3CCC[C@H]3C2)cc1 10.1016/j.bmcl.2019.04.015
CHEMBL4575319 175390 5 None 117 2 Guinea pig 8.4 pKi = 8.4 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysisDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysis
ChEMBL 288 6 1 3 2.3 NC(=O)c1ccc(OCCCN2C[C@H]3CCC[C@H]3C2)cc1 10.1016/j.bmcl.2019.04.015
49782791 17910 0 None -8 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cellsDisplacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 381 3 1 4 3.3 CC(=O)NCc1ccc2c(c1)[C@H](N1CCN(C)CC1)Cc1ccccc1S2 10.1021/jm100652h
CHEMBL1259173 17910 0 None -8 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cellsDisplacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 381 3 1 4 3.3 CC(=O)NCc1ccc2c(c1)[C@H](N1CCN(C)CC1)Cc1ccccc1S2 10.1021/jm100652h
45271167 195364 0 None 977 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 428 6 0 4 5.3 CN(Cc1ccccc1)C1CCN(c2nc3ccccc3n2Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2009.05.086
CHEMBL551888 195364 0 None 977 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 428 6 0 4 5.3 CN(Cc1ccccc1)C1CCN(c2nc3ccccc3n2Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2009.05.086
9850828 169902 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity for recombinant human Histamine H1 receptor expressed in CHO K1 cellsBinding affinity for recombinant human Histamine H1 receptor expressed in CHO K1 cells
ChEMBL 562 11 2 5 5.0 NC(=O)N(O)CCC#Cc1ccc(OCCCCN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2004.12.023
CHEMBL444083 169902 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity for recombinant human Histamine H1 receptor expressed in CHO K1 cellsBinding affinity for recombinant human Histamine H1 receptor expressed in CHO K1 cells
ChEMBL 562 11 2 5 5.0 NC(=O)N(O)CCC#Cc1ccc(OCCCCN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2004.12.023
44326407 207159 0 None 23 3 Human 8.4 pKi = 8.4 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 378 4 1 4 2.8 OCCN1CCN(CC2C[C@@H]3c4ccccc4Cc4ccccc4[C@H]3O2)CC1 10.1016/j.bmcl.2004.03.069
CHEMBL92337 207159 0 None 23 3 Human 8.4 pKi = 8.4 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 378 4 1 4 2.8 OCCN1CCN(CC2C[C@@H]3c4ccccc4Cc4ccccc4[C@H]3O2)CC1 10.1016/j.bmcl.2004.03.069
44326690 111472 0 None 7 3 Human 8.4 pKi = 8.4 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 293 2 0 2 3.8 CN(C)C[C@@H]1C[C@H]2c3ccccc3Cc3ccccc3[C@@H]2O1 10.1016/j.bmcl.2004.03.069
CHEMBL327651 111472 0 None 7 3 Human 8.4 pKi = 8.4 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 293 2 0 2 3.8 CN(C)C[C@@H]1C[C@H]2c3ccccc3Cc3ccccc3[C@@H]2O1 10.1016/j.bmcl.2004.03.069
11976 920 59 None -4 24 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1016/j.bmcl.2008.09.012
667467 920 59 None -4 24 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1016/j.bmcl.2008.09.012
CHEMBL908 920 59 None -4 24 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1016/j.bmcl.2008.09.012
DB01239 920 59 None -4 24 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1016/j.bmcl.2008.09.012
135398737 958 93 None -2 89 Guinea pig 8.4 pKi = 8.4 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysisDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysis
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm400408r
38 958 93 None -2 89 Guinea pig 8.4 pKi = 8.4 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysisDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysis
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm400408r
722 958 93 None -2 89 Guinea pig 8.4 pKi = 8.4 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysisDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysis
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm400408r
CHEMBL42 958 93 None -2 89 Guinea pig 8.4 pKi = 8.4 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysisDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysis
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm400408r
DB00363 958 93 None -2 89 Guinea pig 8.4 pKi = 8.4 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysisDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysis
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm400408r
19861 207523 50 None - 1 Rat 8.4 pKi = 8.4 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 290 0 0 2 3.7 CN1CCC(=C2c3ccccc3CCc3cccnc32)CC1 10.1021/jm00105a069
CHEMBL946 207523 50 None - 1 Rat 8.4 pKi = 8.4 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 290 0 0 2 3.7 CN1CCC(=C2c3ccccc3CCc3cccnc32)CC1 10.1021/jm00105a069
46884063 8141 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 322 5 0 3 4.7 C[C@@H](c1ccccn1)c1c(CCN2CCC2)sc2ccccc12 10.1016/j.bmcl.2010.01.134
CHEMBL1091775 8141 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 322 5 0 3 4.7 C[C@@H](c1ccccn1)c1c(CCN2CCC2)sc2ccccc12 10.1016/j.bmcl.2010.01.134
44250284 195222 0 None 1230 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 436 6 0 5 4.6 CN(CC1CCOCC1)C1CCN(c2nc3ccccc3n2Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2009.05.086
CHEMBL550818 195222 0 None 1230 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 436 6 0 5 4.6 CN(CC1CCOCC1)C1CCN(c2nc3ccccc3n2Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2009.05.086
44250284 195222 0 None 1230 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation counting
ChEMBL 436 6 0 5 4.6 CN(CC1CCOCC1)C1CCN(c2nc3ccccc3n2Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2010.03.027
CHEMBL550818 195222 0 None 1230 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation counting
ChEMBL 436 6 0 5 4.6 CN(CC1CCOCC1)C1CCN(c2nc3ccccc3n2Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2010.03.027
CHEMBL5276489 194643 0 None 70 3 Human 8.4 pKi = 8.4 Binding
Antagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysisAntagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysis
ChEMBL 492 8 1 5 4.4 O=C(NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O)C1CCCC1 10.1021/acsmedchemlett.7b00112
CHEMBL5315725 194643 0 None 70 3 Human 8.4 pKi = 8.4 Binding
Antagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysisAntagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysis
ChEMBL 492 8 1 5 4.4 O=C(NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O)C1CCCC1 10.1021/acsmedchemlett.7b00112
CHEMBL5275284 194654 0 None 5 3 Human 8.4 pKi = 8.4 Binding
Antagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysisAntagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysis
ChEMBL 466 8 1 5 3.9 CC(C)C(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL5315872 194654 0 None 5 3 Human 8.4 pKi = 8.4 Binding
Antagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysisAntagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysis
ChEMBL 466 8 1 5 3.9 CC(C)C(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
9870185 84096 0 None -2 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 489 7 3 5 3.5 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c(=O)c2ccccc12 10.1016/j.bmcl.2012.09.113
CHEMBL2207666 84096 0 None -2 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 489 7 3 5 3.5 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c(=O)c2ccccc12 10.1016/j.bmcl.2012.09.113
59296104 84216 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 503 7 2 5 3.8 CN(C[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)C(=O)c1c[nH]c(=O)c2ccccc12 10.1016/j.bmcl.2012.09.113
CHEMBL2208433 84216 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 503 7 2 5 3.8 CN(C[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)C(=O)c1c[nH]c(=O)c2ccccc12 10.1016/j.bmcl.2012.09.113
59295994 84217 0 None 1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 489 7 3 5 3.5 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1cc(=O)[nH]c2ccccc12 10.1016/j.bmcl.2012.09.113
CHEMBL2208434 84217 0 None 1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 489 7 3 5 3.5 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1cc(=O)[nH]c2ccccc12 10.1016/j.bmcl.2012.09.113
59296090 84092 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 507 7 3 5 3.3 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c(=O)cc1C(F)(F)F 10.1016/j.bmcl.2012.09.112
CHEMBL2207662 84092 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 507 7 3 5 3.3 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c(=O)cc1C(F)(F)F 10.1016/j.bmcl.2012.09.112
9870185 84096 0 None -2 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 489 7 3 5 3.5 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c(=O)c2ccccc12 10.1016/j.bmcl.2012.09.112
CHEMBL2207666 84096 0 None -2 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 489 7 3 5 3.5 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c(=O)c2ccccc12 10.1016/j.bmcl.2012.09.112
10103 3416 72 None 25 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 415 2 0 3 5.6 Cc1cncc(c1)CN1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1021/acs.jmedchem.9b00447
133017 3416 72 None 25 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 415 2 0 3 5.6 Cc1cncc(c1)CN1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1021/acs.jmedchem.9b00447
2413 3416 72 None 25 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 415 2 0 3 5.6 Cc1cncc(c1)CN1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1021/acs.jmedchem.9b00447
CHEMBL91397 3416 72 None 25 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 415 2 0 3 5.6 Cc1cncc(c1)CN1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1021/acs.jmedchem.9b00447
DB11614 3416 72 None 25 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 415 2 0 3 5.6 Cc1cncc(c1)CN1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1021/acs.jmedchem.9b00447
155523802 170857 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 400 2 0 2 5.9 Clc1ccc2c(c1)CCc1cccnc1C2=C1CCN(Cc2ccccc2)CC1 10.1021/acs.jmedchem.9b00447
CHEMBL4454015 170857 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 400 2 0 2 5.9 Clc1ccc2c(c1)CCc1cccnc1C2=C1CCN(Cc2ccccc2)CC1 10.1021/acs.jmedchem.9b00447
155537274 172263 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 378 1 0 2 5.7 Clc1ccc2c(c1)CCc1cccnc1C2=C1CCN(C2CCCC2)CC1 10.1021/acs.jmedchem.9b00447
CHEMBL4474559 172263 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 378 1 0 2 5.7 Clc1ccc2c(c1)CCc1cccnc1C2=C1CCN(C2CCCC2)CC1 10.1021/acs.jmedchem.9b00447
168276508 190266 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]mepyramine from human H1R expressed in HEK293T cells by radioligand competition binding assayDisplacement of [3H]mepyramine from human H1R expressed in HEK293T cells by radioligand competition binding assay
ChEMBL 1140 28 6 11 6.9 C[C@@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@H](C)C(=O)N[C@H](C)C(=O)NCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1 10.1021/acs.jmedchem.2c00125
CHEMBL5175488 190266 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]mepyramine from human H1R expressed in HEK293T cells by radioligand competition binding assayDisplacement of [3H]mepyramine from human H1R expressed in HEK293T cells by radioligand competition binding assay
ChEMBL 1140 28 6 11 6.9 C[C@@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@H](C)C(=O)N[C@H](C)C(=O)NCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1 10.1021/acs.jmedchem.2c00125
44395497 66832 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human histamine H1 receptor expressed in CHO-K1 cellsBinding affinity towards human histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 560 11 2 5 5.4 NC(=O)N(O)CCC#Cc1ccc(OCCCCN2CCN([C@H](c3ccccc3)c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmcl.2004.08.060
CHEMBL186125 66832 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human histamine H1 receptor expressed in CHO-K1 cellsBinding affinity towards human histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 560 11 2 5 5.4 NC(=O)N(O)CCC#Cc1ccc(OCCCCN2CCN([C@H](c3ccccc3)c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmcl.2004.08.060
9998826 120477 0 None -69 5 Rat 7.5 pKi = 7.5 Binding
Inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat cortexInhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat cortex
ChEMBL 363 5 1 3 3.1 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccccc1 10.1021/jm950759z
CHEMBL354210 120477 0 None -69 5 Rat 7.5 pKi = 7.5 Binding
Inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat cortexInhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat cortex
ChEMBL 363 5 1 3 3.1 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccccc1 10.1021/jm950759z
72152556 162938 4 None -2 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 335 5 1 5 2.5 Fc1ccc(N2CCN(CCNc3cncc(Cl)n3)CC2)cc1 10.1021/acs.jmedchem.8b00718
CHEMBL4174330 162938 4 None -2 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 335 5 1 5 2.5 Fc1ccc(N2CCN(CCNc3cncc(Cl)n3)CC2)cc1 10.1021/acs.jmedchem.8b00718
44288769 101148 0 None -275 7 Human 6.5 pKi = 6.5 Binding
Selectivity screen against human Histamine H1 receptorSelectivity screen against human Histamine H1 receptor
ChEMBL 542 7 1 4 4.5 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3F)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1C 10.1016/s0960-894x(99)00696-4
CHEMBL295395 101148 0 None -275 7 Human 6.5 pKi = 6.5 Binding
Selectivity screen against human Histamine H1 receptorSelectivity screen against human Histamine H1 receptor
ChEMBL 542 7 1 4 4.5 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3F)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1C 10.1016/s0960-894x(99)00696-4
9958732 165991 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human histamine H1 receptor expressed in CHO-K1 cellsBinding affinity towards human histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 532 9 2 5 4.6 NC(=O)N(O)CCC#Cc1ccc(OCCN2CCN([C@H](c3ccccc3)c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmcl.2004.08.060
CHEMBL425358 165991 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human histamine H1 receptor expressed in CHO-K1 cellsBinding affinity towards human histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 532 9 2 5 4.6 NC(=O)N(O)CCC#Cc1ccc(OCCN2CCN([C@H](c3ccccc3)c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmcl.2004.08.060
127052294 140302 0 None -15 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 incubated for 60 mins by liquid scintillation counting method
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3806079 140302 0 None -15 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 incubated for 60 mins by liquid scintillation counting method
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
168290397 191971 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 770 20 6 8 2.5 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@H](Cc1ccccc1)C(N)=O)C(C)C 10.1021/acs.jmedchem.2c00125
CHEMBL5201087 191971 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 770 20 6 8 2.5 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@H](Cc1ccccc1)C(N)=O)C(C)C 10.1021/acs.jmedchem.2c00125
44304385 203178 0 None -61 3 Human 6.5 pKi = 6.5 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 404 11 0 5 4.4 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OC(C)C)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL64259 203178 0 None -61 3 Human 6.5 pKi = 6.5 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 404 11 0 5 4.4 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OC(C)C)CC2)cc1 10.1016/s0960-894x(02)00309-8
168281536 192881 0 None -2 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 369 12 4 5 1.7 Cc1nnc(CCCN/C(N)=N/C(=O)NCCCCCCCCN)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5189006 192881 0 None -2 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 369 12 4 5 1.7 Cc1nnc(CCCN/C(N)=N/C(=O)NCCCCCCCCN)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221966 192881 0 None -2 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 369 12 4 5 1.7 Cc1nnc(CCCN/C(N)=N/C(=O)NCCCCCCCCN)s1 10.1021/acs.jmedchem.1c00692
168290397 191971 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 770 20 6 8 2.5 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@H](Cc1ccccc1)C(N)=O)C(C)C 10.1021/acs.jmedchem.2c00125
CHEMBL5201087 191971 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 770 20 6 8 2.5 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@H](Cc1ccccc1)C(N)=O)C(C)C 10.1021/acs.jmedchem.2c00125
11753159 547 6 None -1 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 525 5 1 5 4.7 Cc1ccc(cc1)S(=O)(=O)NC(=O)N1CCC(CC1)N1CCC(CC1)Oc1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2012.08.103
7679 547 6 None -1 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 525 5 1 5 4.7 Cc1ccc(cc1)S(=O)(=O)NC(=O)N1CCC(CC1)N1CCC(CC1)Oc1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2012.08.103
CHEMBL2158814 547 6 None -1 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 525 5 1 5 4.7 Cc1ccc(cc1)S(=O)(=O)NC(=O)N1CCC(CC1)N1CCC(CC1)Oc1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2012.08.103
68938028 81260 0 None -6 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 504 8 1 4 5.6 Cc1ccccc1C[C@@H](C(=O)O)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158772 81260 0 None -6 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 504 8 1 4 5.6 Cc1ccccc1C[C@@H](C(=O)O)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
12001832 81272 0 None -63 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 522 8 1 4 5.7 Cc1c(OC2CCN(CC3CCN([C@@H](Cc4ccc(F)cc4)C(=O)O)CC3)CC2)ccc(Cl)c1Cl 10.1016/j.bmcl.2012.08.103
CHEMBL2158784 81272 0 None -63 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 522 8 1 4 5.7 Cc1c(OC2CCN(CC3CCN([C@@H](Cc4ccc(F)cc4)C(=O)O)CC3)CC2)ccc(Cl)c1Cl 10.1016/j.bmcl.2012.08.103
66615627 81278 0 None -158 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 536 8 1 4 6.1 Cc1c(OC2CCN(CC3CCN([C@@](C)(Cc4ccc(F)cc4)C(=O)O)CC3)CC2)ccc(Cl)c1Cl 10.1016/j.bmcl.2012.08.103
CHEMBL2158790 81278 0 None -158 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 536 8 1 4 6.1 Cc1c(OC2CCN(CC3CCN([C@@](C)(Cc4ccc(F)cc4)C(=O)O)CC3)CC2)ccc(Cl)c1Cl 10.1016/j.bmcl.2012.08.103
71460419 81310 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 524 8 1 4 5.9 O=C(O)[C@H](Cc1ccc(Cl)cc1)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158838 81310 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 524 8 1 4 5.9 O=C(O)[C@H](Cc1ccc(Cl)cc1)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
59295939 84213 0 None -12 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 461 7 3 4 4.1 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c2ccccc12 10.1016/j.bmcl.2012.09.113
CHEMBL2208430 84213 0 None -12 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 461 7 3 4 4.1 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c2ccccc12 10.1016/j.bmcl.2012.09.113
1222 881 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor S3.36C mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor S3.36C mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/nchembio714
2678 881 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor S3.36C mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor S3.36C mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/nchembio714
581 881 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor S3.36C mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor S3.36C mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/nchembio714
CHEMBL1000 881 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor S3.36C mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor S3.36C mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/nchembio714
DB00341 881 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor S3.36C mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor S3.36C mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/nchembio714
1222 881 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor S3.36T mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor S3.36T mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/nchembio714
2678 881 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor S3.36T mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor S3.36T mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/nchembio714
581 881 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor S3.36T mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor S3.36T mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/nchembio714
CHEMBL1000 881 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor S3.36T mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor S3.36T mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/nchembio714
DB00341 881 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor S3.36T mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor S3.36T mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/nchembio714
12660330 154590 3 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 255 7 1 2 3.3 CNCCCOc1ccccc1Cc1ccccc1 10.1021/acs.jmedchem.6b00981
CHEMBL3964404 154590 3 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 255 7 1 2 3.3 CNCCCOc1ccccc1Cc1ccccc1 10.1021/acs.jmedchem.6b00981
CHEMBL3991396 154590 3 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 255 7 1 2 3.3 CNCCCOc1ccccc1Cc1ccccc1 10.1021/acs.jmedchem.6b00981
9888211 21416 13 None -39 10 Guinea pig 7.5 pKi = 7.5 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 417 6 1 3 4.5 O=C1c2ccccc2C(=O)N1CCCCN1CC=C(c2c[nH]c3ccc(F)cc23)CC1 10.1021/jm070516u
CHEMBL131495 21416 13 None -39 10 Guinea pig 7.5 pKi = 7.5 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 417 6 1 3 4.5 O=C1c2ccccc2C(=O)N1CCCCN1CC=C(c2c[nH]c3ccc(F)cc23)CC1 10.1021/jm070516u
11753159 547 6 None -1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 525 5 1 5 4.7 Cc1ccc(cc1)S(=O)(=O)NC(=O)N1CCC(CC1)N1CCC(CC1)Oc1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2012.08.124
7679 547 6 None -1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 525 5 1 5 4.7 Cc1ccc(cc1)S(=O)(=O)NC(=O)N1CCC(CC1)N1CCC(CC1)Oc1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2012.08.124
CHEMBL2158814 547 6 None -1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 525 5 1 5 4.7 Cc1ccc(cc1)S(=O)(=O)NC(=O)N1CCC(CC1)N1CCC(CC1)Oc1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2012.08.124
71462390 82245 0 None 6 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 500 5 1 6 4.3 O=C(c1ccc(-c2nn[nH]n2)cc1)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
CHEMBL2171026 82245 0 None 6 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 500 5 1 6 4.3 O=C(c1ccc(-c2nn[nH]n2)cc1)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
17963315 82252 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 511 5 1 5 4.4 O=C(NS(=O)(=O)c1ccccc1)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
CHEMBL2171033 82252 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 511 5 1 5 4.4 O=C(NS(=O)(=O)c1ccccc1)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
71455217 82261 0 None 3 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 525 5 1 5 4.7 Cc1cccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.124
CHEMBL2171042 82261 0 None 3 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 525 5 1 5 4.7 Cc1cccc(S(=O)(=O)NC(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.124
95338888 162526 1 None 1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 286 5 0 3 4.1 CCCc1nc(CN2CC[C@H](c3ccccc3)C2)cs1 10.1021/acs.jmedchem.8b00718
CHEMBL4167807 162526 1 None 1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 286 5 0 3 4.1 CCCc1nc(CN2CC[C@H](c3ccccc3)C2)cs1 10.1021/acs.jmedchem.8b00718
14554145 30890 0 None - 1 Rat 5.5 pKi = 5.5 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 386 0 0 2 4.9 CC(=O)N1CCC(=C2c3cc(Cl)c(Cl)cc3CCc3cccnc32)CC1 10.1021/jm00105a069
CHEMBL139760 30890 0 None - 1 Rat 5.5 pKi = 5.5 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 386 0 0 2 4.9 CC(=O)N1CCC(=C2c3cc(Cl)c(Cl)cc3CCc3cccnc32)CC1 10.1021/jm00105a069
9549064 98011 3 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to histamine H1 (unknown origin)Binding affinity to histamine H1 (unknown origin)
ChEMBL 318 5 0 4 3.9 CCCc1ccc2c(c1)sc(=O)n2CCN1CCCCCC1 10.1007/s00044-005-0131-1
CHEMBL272899 98011 3 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to histamine H1 (unknown origin)Binding affinity to histamine H1 (unknown origin)
ChEMBL 318 5 0 4 3.9 CCCc1ccc2c(c1)sc(=O)n2CCN1CCCCCC1 10.1007/s00044-005-0131-1
1605 2342 117 None -2 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting method
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1021/jm501086v
3957 2342 117 None -2 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting method
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1021/jm501086v
7216 2342 117 None -2 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting method
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1021/jm501086v
CHEMBL998 2342 117 None -2 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting method
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1021/jm501086v
DB00455 2342 117 None -2 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting method
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1021/jm501086v
162669496 182595 0 None -45 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-pyrilamine from human H1 histamine receptor expressed in human HEK293 cellsDisplacement of [3H]-pyrilamine from human H1 histamine receptor expressed in human HEK293 cells
ChEMBL 466 4 0 3 5.1 C[C@H]1CN(CC[C@H]2CC[C@H](N3C(=O)[C@H]4[C@H]5C=C[C@H](C5)[C@H]4C3=O)CC2)CCc2ccc(Cl)cc21 10.1016/j.bmcl.2020.127681
CHEMBL4788140 182595 0 None -45 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-pyrilamine from human H1 histamine receptor expressed in human HEK293 cellsDisplacement of [3H]-pyrilamine from human H1 histamine receptor expressed in human HEK293 cells
ChEMBL 466 4 0 3 5.1 C[C@H]1CN(CC[C@H]2CC[C@H](N3C(=O)[C@H]4[C@H]5C=C[C@H](C5)[C@H]4C3=O)CC2)CCc2ccc(Cl)cc21 10.1016/j.bmcl.2020.127681
122196381 124295 0 None -295 5 Guinea pig 5.5 pKi = 5.5 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates after 60 mins by liquid scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates after 60 mins by liquid scintillation counting
ChEMBL 485 8 0 6 6.3 Fc1ccc2c(C3CCN(CCCOc4ccc(Cc5nc6ccccc6o5)cc4)CC3)noc2c1 10.1016/j.bmcl.2015.09.045
CHEMBL3634821 124295 0 None -295 5 Guinea pig 5.5 pKi = 5.5 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates after 60 mins by liquid scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates after 60 mins by liquid scintillation counting
ChEMBL 485 8 0 6 6.3 Fc1ccc2c(C3CCN(CCCOc4ccc(Cc5nc6ccccc6o5)cc4)CC3)noc2c1 10.1016/j.bmcl.2015.09.045
71454365 84201 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 465 8 2 6 4.6 O[C@@H](CNC1CCN(Cc2ccc(Cl)c(Cl)c2)CC1)COc1ccc2ncsc2c1 10.1016/j.bmcl.2012.09.113
CHEMBL2208418 84201 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 465 8 2 6 4.6 O[C@@H](CNC1CCN(Cc2ccc(Cl)c(Cl)c2)CC1)COc1ccc2ncsc2c1 10.1016/j.bmcl.2012.09.113
17178058 146487 26 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 253 3 1 2 3.5 c1ccc(-c2ccccc2OC2CCNCC2)cc1 10.1021/acs.jmedchem.6b00981
CHEMBL3922367 146487 26 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 253 3 1 2 3.5 c1ccc(-c2ccccc2OC2CCNCC2)cc1 10.1021/acs.jmedchem.6b00981
20252868 154482 1 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 241 6 1 2 3.0 NCCCOc1ccccc1Cc1ccccc1 10.1021/acs.jmedchem.6b00981
CHEMBL3981091 154482 1 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 241 6 1 2 3.0 NCCCOc1ccccc1Cc1ccccc1 10.1021/acs.jmedchem.6b00981
CHEMBL3990430 154482 1 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 241 6 1 2 3.0 NCCCOc1ccccc1Cc1ccccc1 10.1021/acs.jmedchem.6b00981
44270793 51343 0 None -30 2 Guinea pig 5.5 pKi = 5.5 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 328 6 2 4 2.9 O=C(NN1CCC(c2ccccc2)CC1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL15813 51343 0 None -30 2 Guinea pig 5.5 pKi = 5.5 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 328 6 2 4 2.9 O=C(NN1CCC(c2ccccc2)CC1)OCCCc1c[nH]cn1 10.1021/jm9507688
155536080 172114 0 None -21 10 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-Pyrilamine from human recombinant histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Pyrilamine from human recombinant histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 219 2 1 2 2.9 CC[C@H]1c2cc(OC)ccc2CC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
CHEMBL4472703 172114 0 None -21 10 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-Pyrilamine from human recombinant histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Pyrilamine from human recombinant histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 219 2 1 2 2.9 CC[C@H]1c2cc(OC)ccc2CC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
11723317 102894 0 None -100 3 Guinea pig 5.5 pKi = 5.5 Binding
Displacement of [3H]mepyramine bound to membranes of CHO cells expressing guinea pig H1 receptorsDisplacement of [3H]mepyramine bound to membranes of CHO cells expressing guinea pig H1 receptors
ChEMBL 316 9 3 2 2.8 S=C(NCCCCCc1c[nH]cn1)NCCc1ccccc1 10.1021/jm00012a025
CHEMBL305929 102894 0 None -100 3 Guinea pig 5.5 pKi = 5.5 Binding
Displacement of [3H]mepyramine bound to membranes of CHO cells expressing guinea pig H1 receptorsDisplacement of [3H]mepyramine bound to membranes of CHO cells expressing guinea pig H1 receptors
ChEMBL 316 9 3 2 2.8 S=C(NCCCCCc1c[nH]cn1)NCCc1ccccc1 10.1021/jm00012a025
10015196 103620 0 None -158 3 Guinea pig 5.5 pKi = 5.5 Binding
Displacement of [3H]mepyramine bound to membranes of CHO cells expressing guinea pig H1 receptorsDisplacement of [3H]mepyramine bound to membranes of CHO cells expressing guinea pig H1 receptors
ChEMBL 254 8 3 2 2.4 CCC/N=C(\S)NCCCCCc1c[nH]cn1 10.1021/jm00012a025
CHEMBL308717 103620 0 None -158 3 Guinea pig 5.5 pKi = 5.5 Binding
Displacement of [3H]mepyramine bound to membranes of CHO cells expressing guinea pig H1 receptorsDisplacement of [3H]mepyramine bound to membranes of CHO cells expressing guinea pig H1 receptors
ChEMBL 254 8 3 2 2.4 CCC/N=C(\S)NCCCCCc1c[nH]cn1 10.1021/jm00012a025
10803416 54615 0 None -1023 2 Guinea pig 4.5 pKi = 4.5 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 290 6 2 5 2.5 O=C(Nc1ccccc1[N+](=O)[O-])OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL16109 54615 0 None -1023 2 Guinea pig 4.5 pKi = 4.5 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 290 6 2 5 2.5 O=C(Nc1ccccc1[N+](=O)[O-])OCCCc1c[nH]cn1 10.1021/jm9507688
1204 1932 119 None -501 24 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor N7.45Q mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor N7.45Q mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1038/nchembio714
1247 1932 119 None -501 24 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor N7.45Q mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor N7.45Q mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1038/nchembio714
1375 1932 119 None -501 24 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor N7.45Q mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor N7.45Q mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1038/nchembio714
774 1932 119 None -501 24 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor N7.45Q mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor N7.45Q mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1038/nchembio714
CHEMBL90 1932 119 None -501 24 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor N7.45Q mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor N7.45Q mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1038/nchembio714
DB05381 1932 119 None -501 24 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor N7.45Q mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor N7.45Q mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1038/nchembio714
90654502 110311 0 None -741 2 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 319 9 2 4 1.9 C[C@H](NCc1ccc(OCCCN2CCCCC2)cc1)C(N)=O 10.1016/j.ejmech.2014.03.014
CHEMBL3238446 110311 0 None -741 2 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 319 9 2 4 1.9 C[C@H](NCc1ccc(OCCCN2CCCCC2)cc1)C(N)=O 10.1016/j.ejmech.2014.03.014
53317594 57751 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 318 6 0 4 3.4 C[C@H](C1=C(CCN(C)CC#N)Cc2ccccc21)c1cnccn1 10.1016/j.bmcl.2010.12.053
CHEMBL1669409 57751 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 318 6 0 4 3.4 C[C@H](C1=C(CCN(C)CC#N)Cc2ccccc21)c1cnccn1 10.1016/j.bmcl.2010.12.053
155544150 173334 0 None 8 2 Guinea pig 7.5 pKi = 7.5 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysisDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysis
ChEMBL 316 5 0 3 2.8 CC1CCN(CCCOc2ccc3c(c2)C(=O)N(C)CC3)CC1 10.1016/j.bmcl.2019.04.015
CHEMBL4526723 173334 0 None 8 2 Guinea pig 7.5 pKi = 7.5 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysisDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysis
ChEMBL 316 5 0 3 2.8 CC1CCN(CCCOc2ccc3c(c2)C(=O)N(C)CC3)CC1 10.1016/j.bmcl.2019.04.015
72152555 162730 5 None 1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 345 7 1 5 3.1 Clc1cncc(NCCCCN2CCN(c3ccccc3)CC2)n1 10.1021/acs.jmedchem.8b00718
CHEMBL4171171 162730 5 None 1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 345 7 1 5 3.1 Clc1cncc(NCCCCN2CCN(c3ccccc3)CC2)n1 10.1021/acs.jmedchem.8b00718
44326320 112819 0 None 2 3 Human 7.5 pKi = 7.5 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 295 2 0 3 4.0 CN(C)CC1C[C@H]2c3ccccc3Oc3ccccc3[C@H]2O1 10.1016/j.bmcl.2004.03.069
CHEMBL330713 112819 0 None 2 3 Human 7.5 pKi = 7.5 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 295 2 0 3 4.0 CN(C)CC1C[C@H]2c3ccccc3Oc3ccccc3[C@H]2O1 10.1016/j.bmcl.2004.03.069
1853 3551 38 None - 1 Rat 6.5 pKi = 6.5 Binding
Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.
ChEMBL 352 0 0 2 4.3 Clc1ccc2c(c1)CCc1c(C2=C2CCN(CC2)C(=O)C)nccc1 10.1016/S0960-894X(00)80290-5
60680 3551 38 None - 1 Rat 6.5 pKi = 6.5 Binding
Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.
ChEMBL 352 0 0 2 4.3 Clc1ccc2c(c1)CCc1c(C2=C2CCN(CC2)C(=O)C)nccc1 10.1016/S0960-894X(00)80290-5
CHEMBL10971 3551 38 None - 1 Rat 6.5 pKi = 6.5 Binding
Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.
ChEMBL 352 0 0 2 4.3 Clc1ccc2c(c1)CCc1c(C2=C2CCN(CC2)C(=O)C)nccc1 10.1016/S0960-894X(00)80290-5
1853 3551 38 None - 1 Rat 6.5 pKi = 6.5 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 352 0 0 2 4.3 Clc1ccc2c(c1)CCc1c(C2=C2CCN(CC2)C(=O)C)nccc1 10.1016/s0960-894x(98)00626-x
60680 3551 38 None - 1 Rat 6.5 pKi = 6.5 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 352 0 0 2 4.3 Clc1ccc2c(c1)CCc1c(C2=C2CCN(CC2)C(=O)C)nccc1 10.1016/s0960-894x(98)00626-x
CHEMBL10971 3551 38 None - 1 Rat 6.5 pKi = 6.5 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 352 0 0 2 4.3 Clc1ccc2c(c1)CCc1c(C2=C2CCN(CC2)C(=O)C)nccc1 10.1016/s0960-894x(98)00626-x
1853 3551 38 None - 1 Rat 6.5 pKi = 6.5 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 352 0 0 2 4.3 Clc1ccc2c(c1)CCc1c(C2=C2CCN(CC2)C(=O)C)nccc1 10.1021/jm00105a069
60680 3551 38 None - 1 Rat 6.5 pKi = 6.5 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 352 0 0 2 4.3 Clc1ccc2c(c1)CCc1c(C2=C2CCN(CC2)C(=O)C)nccc1 10.1021/jm00105a069
CHEMBL10971 3551 38 None - 1 Rat 6.5 pKi = 6.5 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 352 0 0 2 4.3 Clc1ccc2c(c1)CCc1c(C2=C2CCN(CC2)C(=O)C)nccc1 10.1021/jm00105a069
45485498 197671 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation counting
ChEMBL 231 5 0 1 3.8 Cc1ccc(CCCCN2CCCCC2)cc1 10.1016/j.bmcl.2009.07.047
CHEMBL571073 197671 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation counting
ChEMBL 231 5 0 1 3.8 Cc1ccc(CCCCN2CCCCC2)cc1 10.1016/j.bmcl.2009.07.047
46884062 8359 0 None - 1 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 296 5 1 3 4.2 CNCCc1sc2ccccc2c1[C@@H](C)c1ccccn1 10.1016/j.bmcl.2010.01.134
CHEMBL1093044 8359 0 None - 1 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 296 5 1 3 4.2 CNCCc1sc2ccccc2c1[C@@H](C)c1ccccn1 10.1016/j.bmcl.2010.01.134
95339542 162030 1 None -1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 286 4 0 3 4.3 CC(C)c1nc(CN2CC[C@H](c3ccccc3)C2)cs1 10.1021/acs.jmedchem.8b00718
CHEMBL4159893 162030 1 None -1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 286 4 0 3 4.3 CC(C)c1nc(CN2CC[C@H](c3ccccc3)C2)cs1 10.1021/acs.jmedchem.8b00718
1353 1911 93 None -489 83 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
3559 1911 93 None -489 83 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
86 1911 93 None -489 83 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
CHEMBL54 1911 93 None -489 83 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
DB00502 1911 93 None -489 83 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
44335571 5272 0 None -128 4 Human 5.5 pKi = 5.5 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 322 6 0 4 3.3 N#Cc1ccc(-c2ccc(OCCCN3CCOCC3)cc2)cc1 10.1016/s0960-894x(02)00648-0
CHEMBL106483 5272 0 None -128 4 Human 5.5 pKi = 5.5 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 322 6 0 4 3.3 N#Cc1ccc(-c2ccc(OCCCN3CCOCC3)cc2)cc1 10.1016/s0960-894x(02)00648-0
40011786 69028 3 None -32 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 282 2 0 4 2.7 c1ccc2c(N3CCN(C4CCCC4)CC3)ncnc2c1 10.1021/jm2011589
CHEMBL1923530 69028 3 None -32 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 282 2 0 4 2.7 c1ccc2c(N3CCN(C4CCCC4)CC3)ncnc2c1 10.1021/jm2011589
25491778 162665 1 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 378 6 0 5 5.1 CO[C@@H]1CCCN(Cc2nc(-c3cccc(Oc4ccccc4)c3)oc2C)C1 10.1021/acs.jmedchem.8b00718
CHEMBL4170001 162665 1 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 378 6 0 5 5.1 CO[C@@H]1CCCN(Cc2nc(-c3cccc(Oc4ccccc4)c3)oc2C)C1 10.1021/acs.jmedchem.8b00718
11023546 78478 0 None 2 4 Rat 7.5 pKi = 7.5 Binding
Half-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenateHalf-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenate
ChEMBL 317 1 0 4 3.1 CN1CCN([C@H]2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
CHEMBL2111783 78478 0 None 2 4 Rat 7.5 pKi = 7.5 Binding
Half-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenateHalf-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenate
ChEMBL 317 1 0 4 3.1 CN1CCN([C@H]2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
2389 3331 118 None -46 67 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm049632c
5073 3331 118 None -46 67 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm049632c
96 3331 118 None -46 67 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm049632c
CHEMBL85 3331 118 None -46 67 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm049632c
DB00734 3331 118 None -46 67 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm049632c
44401194 71295 0 None -4 7 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 313 2 0 3 4.1 CN(C)C[C@@H]1CC2c3ccccc3Oc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL195706 71295 0 None -4 7 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 313 2 0 3 4.1 CN(C)C[C@@H]1CC2c3ccccc3Oc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
56835171 69740 0 None -204 9 Mouse 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from mouse H1RDisplacement of [3H]histamine from mouse H1R
ChEMBL 295 2 2 6 1.9 Nc1nc(N2CCNCC2)c2ccc(-c3ccco3)cc2n1 10.1016/j.bmcl.2011.10.104
CHEMBL1935574 69740 0 None -204 9 Mouse 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from mouse H1RDisplacement of [3H]histamine from mouse H1R
ChEMBL 295 2 2 6 1.9 Nc1nc(N2CCNCC2)c2ccc(-c3ccco3)cc2n1 10.1016/j.bmcl.2011.10.104
44304412 201648 0 None -223 3 Human 5.5 pKi = 5.5 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 517 13 1 6 4.9 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](NC(=O)OC(C)(C)C)C(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
CHEMBL60598 201648 0 None -223 3 Human 5.5 pKi = 5.5 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 517 13 1 6 4.9 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](NC(=O)OC(C)(C)C)C(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
44304753 203195 0 None -363 3 Human 5.5 pKi = 5.5 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 466 13 1 6 3.3 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](N)Cc3ccncc3)CC2)cc1 10.1016/s0960-894x(02)00310-4
CHEMBL64321 203195 0 None -363 3 Human 5.5 pKi = 5.5 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 466 13 1 6 3.3 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](N)Cc3ccncc3)CC2)cc1 10.1016/s0960-894x(02)00310-4
112936267 137295 1 None 2 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 373 6 1 5 3.6 CN1CCN(c2cc(-c3ccccc3)nc(NCCc3ccccc3)n2)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3752383 137295 1 None 2 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 373 6 1 5 3.6 CN1CCN(c2cc(-c3ccccc3)nc(NCCc3ccccc3)n2)CC1 10.1016/j.bmcl.2015.12.035
132060776 162402 0 None -1 16 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-Pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 419 4 0 4 4.4 O=C(OCc1ccccc1)N1CCc2ccc(N3CCN(C4CCCC4)CC3)cc2C1 10.1016/j.ejmech.2018.02.024
CHEMBL4165863 162402 0 None -1 16 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-Pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 419 4 0 4 4.4 O=C(OCc1ccccc1)N1CCc2ccc(N3CCN(C4CCCC4)CC3)cc2C1 10.1016/j.ejmech.2018.02.024
168296769 192332 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 758 20 7 9 0.8 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5206578 192332 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 758 20 7 9 0.8 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
44304256 168019 0 None -123 3 Human 5.5 pKi = 5.5 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 360 12 0 4 4.2 CCCCCC(=O)c1ccc(OCCCN2CCN(CCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL432144 168019 0 None -123 3 Human 5.5 pKi = 5.5 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 360 12 0 4 4.2 CCCCCC(=O)c1ccc(OCCCN2CCN(CCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
127035836 137518 0 None 5 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 399 4 1 5 3.9 Cc1ccc(CNc2nc3c(c(N4CCN(C)CC4)n2)CCc2ccccc2-3)cc1 10.1016/j.bmcl.2015.12.035
CHEMBL3754176 137518 0 None 5 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 399 4 1 5 3.9 Cc1ccc(CNc2nc3c(c(N4CCN(C)CC4)n2)CCc2ccccc2-3)cc1 10.1016/j.bmcl.2015.12.035
71525678 89725 0 None -3548 6 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]histamine from human histamine H1 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H1 receptor expressed in HEK cells
ChEMBL 258 3 2 6 0.6 CCc1cnc2c(N3CC(NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
CHEMBL2376800 89725 0 None -3548 6 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]histamine from human histamine H1 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H1 receptor expressed in HEK cells
ChEMBL 258 3 2 6 0.6 CCc1cnc2c(N3CC(NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
129103322 167373 0 None -53 6 Guinea pig 6.5 pKi = 6.5 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by liquid scintillation countingDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by liquid scintillation counting
ChEMBL 463 6 1 5 4.5 O=C1CCc2cc(C(O)CCCN3CCC(c4noc5cc(F)ccc45)CC3)cc3c2N1CC3 10.1021/acs.jmedchem.8b01096
CHEMBL4294799 167373 0 None -53 6 Guinea pig 6.5 pKi = 6.5 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by liquid scintillation countingDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by liquid scintillation counting
ChEMBL 463 6 1 5 4.5 O=C1CCc2cc(C(O)CCCN3CCC(c4noc5cc(F)ccc45)CC3)cc3c2N1CC3 10.1021/acs.jmedchem.8b01096
168296769 192332 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 758 20 7 9 0.8 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5206578 192332 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 758 20 7 9 0.8 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
2812 4779 101 None -28 34 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 4779 101 None -28 34 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
44335384 4638 0 None -489 4 Human 5.5 pKi = 5.5 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 334 6 0 3 4.9 CC1CCCCN1CCCOc1ccc(-c2ccc(C#N)cc2)cc1 10.1016/s0960-894x(02)00648-0
CHEMBL102984 4638 0 None -489 4 Human 5.5 pKi = 5.5 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 334 6 0 3 4.9 CC1CCCCN1CCCOc1ccc(-c2ccc(C#N)cc2)cc1 10.1016/s0960-894x(02)00648-0
44304277 100947 0 None -457 3 Human 4.5 pKi = 4.5 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 401 10 1 5 2.4 CN[C@@H](C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1)C(C)C 10.1016/s0960-894x(02)00310-4
CHEMBL294087 100947 0 None -457 3 Human 4.5 pKi = 4.5 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 401 10 1 5 2.4 CN[C@@H](C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1)C(C)C 10.1016/s0960-894x(02)00310-4
46884638 7724 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 293 5 0 3 3.3 Cc1cnc(CC2=C(CCN(C)C)Cc3ccccc32)cn1 10.1016/j.bmcl.2010.02.055
CHEMBL1088899 7724 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 293 5 0 3 3.3 Cc1cnc(CC2=C(CCN(C)C)Cc3ccccc32)cn1 10.1016/j.bmcl.2010.02.055
155566038 175742 0 None 26 2 Guinea pig 7.5 pKi = 7.5 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysisDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysis
ChEMBL 318 5 1 4 1.5 CN1CCc2ccc(OCCCN3CCC(O)CC3)cc2C1=O 10.1016/j.bmcl.2019.04.015
CHEMBL4583183 175742 0 None 26 2 Guinea pig 7.5 pKi = 7.5 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysisDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysis
ChEMBL 318 5 1 4 1.5 CN1CCc2ccc(OCCCN3CCC(O)CC3)cc2C1=O 10.1016/j.bmcl.2019.04.015
51111982 162578 6 None 1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 344 5 0 4 3.2 N#Cc1c(CN2CCN(CCc3ccccc3)CC2)cn2ccccc12 10.1021/acs.jmedchem.8b00718
CHEMBL4168691 162578 6 None 1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 344 5 0 4 3.2 N#Cc1c(CN2CCN(CCc3ccccc3)CC2)cn2ccccc12 10.1021/acs.jmedchem.8b00718
11623845 8323 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 316 5 0 4 4.6 CC(c1nccs1)c1c(CCN(C)C)sc2ccccc12 10.1016/j.bmcl.2010.01.134
CHEMBL1092767 8323 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 316 5 0 4 4.6 CC(c1nccs1)c1c(CCN(C)C)sc2ccccc12 10.1016/j.bmcl.2010.01.134
1605 2342 117 None -2 4 Rat 6.5 pKi = 6.5 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1021/jm00105a069
3957 2342 117 None -2 4 Rat 6.5 pKi = 6.5 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1021/jm00105a069
7216 2342 117 None -2 4 Rat 6.5 pKi = 6.5 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1021/jm00105a069
CHEMBL998 2342 117 None -2 4 Rat 6.5 pKi = 6.5 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1021/jm00105a069
DB00455 2342 117 None -2 4 Rat 6.5 pKi = 6.5 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1021/jm00105a069
CHEMBL5274312 193809 0 None -3 5 Human 5.5 pKi = 5.5 Binding
Binding affinity to histamine H1 receptor (unknown origin)Binding affinity to histamine H1 receptor (unknown origin)
ChEMBL 383 4 0 3 5.0 CC[Si](C#Cc1cccc2c1OC(C(F)(F)F)C([N+](=O)[O-])=C2)(CC)CC 10.1016/j.bmcl.2022.128981
44335351 5067 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Binding affinity at human cortical Histamine 1 receptorBinding affinity at human cortical Histamine 1 receptor
ChEMBL 402 7 0 4 4.6 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(Cl)cc3)cc2)CC1 10.1016/s0960-894x(02)00648-0
CHEMBL105385 5067 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Binding affinity at human cortical Histamine 1 receptorBinding affinity at human cortical Histamine 1 receptor
ChEMBL 402 7 0 4 4.6 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(Cl)cc3)cc2)CC1 10.1016/s0960-894x(02)00648-0
44304021 102795 0 None -9 3 Human 6.5 pKi = 6.5 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 374 8 0 5 3.4 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)C=C(C)C)cc2)CC1 10.1016/s0960-894x(02)00309-8
CHEMBL305313 102795 0 None -9 3 Human 6.5 pKi = 6.5 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 374 8 0 5 3.4 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)C=C(C)C)cc2)CC1 10.1016/s0960-894x(02)00309-8
10069595 203128 0 None -112 3 Human 6.5 pKi = 6.5 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 400 11 0 4 4.2 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)C3CCC3)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL64100 203128 0 None -112 3 Human 6.5 pKi = 6.5 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 400 11 0 4 4.2 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)C3CCC3)CC2)cc1 10.1016/s0960-894x(02)00309-8
44335350 5080 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 398 8 0 5 3.9 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(OC)cc3)cc2)CC1 10.1016/s0960-894x(02)00648-0
CHEMBL105483 5080 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 398 8 0 5 3.9 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(OC)cc3)cc2)CC1 10.1016/s0960-894x(02)00648-0
44335336 4558 0 None -27 4 Human 5.5 pKi = 5.5 Binding
Binding affinity at human cortical Histamine 1 receptorBinding affinity at human cortical Histamine 1 receptor
ChEMBL 335 6 1 4 3.4 N#Cc1ccc(-c2ccc(OCCCN3CCC(N)CC3)cc2)cc1 10.1016/s0960-894x(02)00648-0
CHEMBL102452 4558 0 None -27 4 Human 5.5 pKi = 5.5 Binding
Binding affinity at human cortical Histamine 1 receptorBinding affinity at human cortical Histamine 1 receptor
ChEMBL 335 6 1 4 3.4 N#Cc1ccc(-c2ccc(OCCCN3CCC(N)CC3)cc2)cc1 10.1016/s0960-894x(02)00648-0
25109291 191386 10 None -83176 8 Human 5.5 pKi = 5.5 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 327 1 2 6 1.7 Nc1nc2c(c(N3CCNCC3)n1)CCC1=C2[C@@H]2CCCC[C@@H]2O1 10.1021/jm8007618
CHEMBL519240 191386 10 None -83176 8 Human 5.5 pKi = 5.5 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 327 1 2 6 1.7 Nc1nc2c(c(N3CCNCC3)n1)CCC1=C2[C@@H]2CCCC[C@@H]2O1 10.1021/jm8007618
168273640 192805 0 None -100 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 568 15 8 10 -0.1 N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5176229 192805 0 None -100 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 568 15 8 10 -0.1 N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221444 192805 0 None -100 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 568 15 8 10 -0.1 N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
44304012 202832 0 None -18620 3 Human 4.5 pKi = 4.5 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 389 11 1 5 2.7 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](C)N)CC2)cc1 10.1016/s0960-894x(02)00310-4
CHEMBL62421 202832 0 None -18620 3 Human 4.5 pKi = 4.5 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 389 11 1 5 2.7 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](C)N)CC2)cc1 10.1016/s0960-894x(02)00310-4
44289035 100514 0 None -186 7 Human 6.5 pKi = 6.5 Binding
Selectivity screen against human Histamine H1 receptorSelectivity screen against human Histamine H1 receptor
ChEMBL 524 7 1 4 4.4 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1C 10.1016/s0960-894x(99)00696-4
CHEMBL291166 100514 0 None -186 7 Human 6.5 pKi = 6.5 Binding
Selectivity screen against human Histamine H1 receptorSelectivity screen against human Histamine H1 receptor
ChEMBL 524 7 1 4 4.4 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1C 10.1016/s0960-894x(99)00696-4
50985821 176218 31 None -2 3 Human 5.5 pKi = 5.5 Binding
Binding affinity to H1 receptor (unknown origin) by radioligand displacement assayBinding affinity to H1 receptor (unknown origin) by radioligand displacement assay
ChEMBL 474 5 2 5 6.2 N=c1c2c(-c3ccccc3)c(-c3ccccc3)n(Cc3ccccc3)c2ncn1[C@H]1CC[C@H](O)CC1 10.1021/acs.jmedchem.2c00204
CHEMBL4594433 176218 31 None -2 3 Human 5.5 pKi = 5.5 Binding
Binding affinity to H1 receptor (unknown origin) by radioligand displacement assayBinding affinity to H1 receptor (unknown origin) by radioligand displacement assay
ChEMBL 474 5 2 5 6.2 N=c1c2c(-c3ccccc3)c(-c3ccccc3)n(Cc3ccccc3)c2ncn1[C@H]1CC[C@H](O)CC1 10.1021/acs.jmedchem.2c00204
44343572 10286 0 None - 1 Rat 5.4 pKi = 5.4 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 383 3 0 3 3.9 CCCC(=O)N1CCN(C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/s0960-894x(98)00626-x
CHEMBL116144 10286 0 None - 1 Rat 5.4 pKi = 5.4 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 383 3 0 3 3.9 CCCC(=O)N1CCN(C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/s0960-894x(98)00626-x
71457970 78470 0 None - 1 Rat 5.4 pKi = 5.4 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 355 1 0 3 3.1 CC(=O)N1CCN([C@@H]2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/s0960-894x(98)00626-x
CHEMBL2111767 78470 0 None - 1 Rat 5.4 pKi = 5.4 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 355 1 0 3 3.1 CC(=O)N1CCN([C@@H]2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/s0960-894x(98)00626-x
19918406 111359 0 None - 1 Rat 5.4 pKi = 5.4 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 367 1 0 3 3.2 O=C1CCC2CN(C3c4ccc(Cl)cc4CCc4cccnc43)CCN12 10.1016/s0960-894x(98)00626-x
CHEMBL326978 111359 0 None - 1 Rat 5.4 pKi = 5.4 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 367 1 0 3 3.2 O=C1CCC2CN(C3c4ccc(Cl)cc4CCc4cccnc43)CCN12 10.1016/s0960-894x(98)00626-x
11848625 5792 0 None -38 6 Human 5.4 pKi = 5.4 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 451 8 1 7 4.9 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OC2CCOCC2)c1 10.1016/j.bmcl.2009.09.024
CHEMBL1078745 5792 0 None -38 6 Human 5.4 pKi = 5.4 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 451 8 1 7 4.9 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OC2CCOCC2)c1 10.1016/j.bmcl.2009.09.024
44334407 109085 0 None -1202 3 Human 5.4 pKi = 5.4 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 462 10 1 5 3.8 O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3cccc(Cl)c3)C2)cc1)C1CC1 10.1016/s0960-894x(02)00685-6
CHEMBL321320 109085 0 None -1202 3 Human 5.4 pKi = 5.4 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 462 10 1 5 3.8 O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3cccc(Cl)c3)C2)cc1)C1CC1 10.1016/s0960-894x(02)00685-6
56835171 69740 0 None -223 9 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]histamine from rat H1RDisplacement of [3H]histamine from rat H1R
ChEMBL 295 2 2 6 1.9 Nc1nc(N2CCNCC2)c2ccc(-c3ccco3)cc2n1 10.1016/j.bmcl.2011.10.104
CHEMBL1935574 69740 0 None -223 9 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]histamine from rat H1RDisplacement of [3H]histamine from rat H1R
ChEMBL 295 2 2 6 1.9 Nc1nc(N2CCNCC2)c2ccc(-c3ccco3)cc2n1 10.1016/j.bmcl.2011.10.104
127052465 140731 0 None -97 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 340 5 0 3 3.6 O=C1c2ccccc2C(=O)N1CCCCN1CCC2CCCCC2C1 10.1016/j.bmc.2016.05.053
CHEMBL3817911 140731 0 None -97 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 340 5 0 3 3.6 O=C1c2ccccc2C(=O)N1CCCCN1CCC2CCCCC2C1 10.1016/j.bmc.2016.05.053
127052465 140731 0 None -97 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 340 5 0 3 3.6 O=C1c2ccccc2C(=O)N1CCCCN1CCC2CCCCC2C1 10.1016/j.bmc.2016.05.053
CHEMBL3817911 140731 0 None -97 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 340 5 0 3 3.6 O=C1c2ccccc2C(=O)N1CCCCN1CCC2CCCCC2C1 10.1016/j.bmc.2016.05.053
162662563 182046 0 None -61 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cell membranes co-expressing RGS4 measured after 60 mins by scintillation counting analysisDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cell membranes co-expressing RGS4 measured after 60 mins by scintillation counting analysis
ChEMBL 391 7 0 4 4.5 Fc1ccc(-c2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)cc1 10.1016/j.ejmech.2020.113041
CHEMBL4781093 182046 0 None -61 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cell membranes co-expressing RGS4 measured after 60 mins by scintillation counting analysisDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cell membranes co-expressing RGS4 measured after 60 mins by scintillation counting analysis
ChEMBL 391 7 0 4 4.5 Fc1ccc(-c2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)cc1 10.1016/j.ejmech.2020.113041
1605 2342 117 None -2 4 Human 7.4 pKi = 7.4 Binding
Binding affinity for H1 histamine receptor expressed in CHO cellsBinding affinity for H1 histamine receptor expressed in CHO cells
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1021/jm049495j
3957 2342 117 None -2 4 Human 7.4 pKi = 7.4 Binding
Binding affinity for H1 histamine receptor expressed in CHO cellsBinding affinity for H1 histamine receptor expressed in CHO cells
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1021/jm049495j
7216 2342 117 None -2 4 Human 7.4 pKi = 7.4 Binding
Binding affinity for H1 histamine receptor expressed in CHO cellsBinding affinity for H1 histamine receptor expressed in CHO cells
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1021/jm049495j
CHEMBL998 2342 117 None -2 4 Human 7.4 pKi = 7.4 Binding
Binding affinity for H1 histamine receptor expressed in CHO cellsBinding affinity for H1 histamine receptor expressed in CHO cells
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1021/jm049495j
DB00455 2342 117 None -2 4 Human 7.4 pKi = 7.4 Binding
Binding affinity for H1 histamine receptor expressed in CHO cellsBinding affinity for H1 histamine receptor expressed in CHO cells
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1021/jm049495j
10660 14416 58 None 2 12 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 469 6 1 7 3.0 CN(C)CCOC(c1ccccc1)c1ccccc1.Cn1c(=O)c2[nH]c(Cl)nc2n(C)c1=O nan
CHEMBL1200406 14416 58 None 2 12 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 469 6 1 7 3.0 CN(C)CCOC(c1ccccc1)c1ccccc1.Cn1c(=O)c2[nH]c(Cl)nc2n(C)c1=O nan
44343938 113063 0 None - 1 Rat 5.4 pKi = 5.4 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 320 1 0 2 3.0 CC(=O)N1CCN(C2c3ccccc3CCc3ccccc32)CC1 10.1016/s0960-894x(98)00626-x
CHEMBL331159 113063 0 None - 1 Rat 5.4 pKi = 5.4 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 320 1 0 2 3.0 CC(=O)N1CCN(C2c3ccccc3CCc3ccccc32)CC1 10.1016/s0960-894x(98)00626-x
44334035 110045 0 None -741 3 Human 4.4 pKi = 4.4 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 476 10 1 7 4.1 O=C(N[C@H]1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)C1)c1csc(-c2cccnc2)n1 10.1016/s0960-894x(02)00685-6
CHEMBL323517 110045 0 None -741 3 Human 4.4 pKi = 4.4 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 476 10 1 7 4.1 O=C(N[C@H]1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)C1)c1csc(-c2cccnc2)n1 10.1016/s0960-894x(02)00685-6
2771 195017 74 None -2 27 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 nan
CHEMBL1200781 195017 74 None -2 27 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 nan
CHEMBL549 195017 74 None -2 27 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 nan
168277300 190180 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 754 19 5 7 3.5 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O)C(C)C 10.1021/acs.jmedchem.2c00125
CHEMBL5174142 190180 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 754 19 5 7 3.5 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O)C(C)C 10.1021/acs.jmedchem.2c00125
10268636 5283 0 None -436 4 Human 5.4 pKi = 5.4 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 335 7 1 4 3.3 CN[C@@H]1CCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)C1 10.1016/s0960-894x(02)00648-0
CHEMBL106545 5283 0 None -436 4 Human 5.4 pKi = 5.4 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 335 7 1 4 3.3 CN[C@@H]1CCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)C1 10.1016/s0960-894x(02)00648-0
44335222 163456 0 None -1 3 Human 5.4 pKi = 5.4 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 369 7 0 5 3.3 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccncc3)cc2)CC1 10.1016/s0960-894x(02)00648-0
CHEMBL419912 163456 0 None -1 3 Human 5.4 pKi = 5.4 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 369 7 0 5 3.3 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccncc3)cc2)CC1 10.1016/s0960-894x(02)00648-0
168294166 193014 0 None -1 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 360 6 4 4 3.3 CCCCCNC(=O)/N=C(\N)Nc1ccc(-c2sc(N)nc2C)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5209081 193014 0 None -1 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 360 6 4 4 3.3 CCCCCNC(=O)/N=C(\N)Nc1ccc(-c2sc(N)nc2C)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222775 193014 0 None -1 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 360 6 4 4 3.3 CCCCCNC(=O)/N=C(\N)Nc1ccc(-c2sc(N)nc2C)cc1 10.1021/acs.jmedchem.1c00692
44304329 203227 0 None -1230 3 Human 4.4 pKi = 4.4 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 385 8 1 5 1.9 O=C(c1ccc(OCCCN2CCN(C(=O)[C@H]3CCCN3)CC2)cc1)C1CC1 10.1016/s0960-894x(02)00310-4
CHEMBL64461 203227 0 None -1230 3 Human 4.4 pKi = 4.4 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 385 8 1 5 1.9 O=C(c1ccc(OCCCN2CCN(C(=O)[C@H]3CCCN3)CC2)cc1)C1CC1 10.1016/s0960-894x(02)00310-4
168277300 190180 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 754 19 5 7 3.5 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O)C(C)C 10.1021/acs.jmedchem.2c00125
CHEMBL5174142 190180 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 754 19 5 7 3.5 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O)C(C)C 10.1021/acs.jmedchem.2c00125
71450550 83807 0 None -7 16 Human 5.4 pKi = 5.4 Binding
Binding affinity to Histamine H1 receptorBinding affinity to Histamine H1 receptor
ChEMBL 309 4 1 3 2.0 COc1ccccc1CCN1C2C3C4CC5C6C4C2C6C1(O)C53 10.1016/j.bmcl.2012.08.046
CHEMBL2205836 83807 0 None -7 16 Human 5.4 pKi = 5.4 Binding
Binding affinity to Histamine H1 receptorBinding affinity to Histamine H1 receptor
ChEMBL 309 4 1 3 2.0 COc1ccccc1CCN1C2C3C4CC5C6C4C2C6C1(O)C53 10.1016/j.bmcl.2012.08.046
44455426 155149 0 None -5 12 Human 6.4 pKi = 6.4 Binding
Inhibition of human cloned histamine H1 receptor by competitive binding experimentInhibition of human cloned histamine H1 receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL402143 155149 0 None -5 12 Human 6.4 pKi = 6.4 Binding
Inhibition of human cloned histamine H1 receptor by competitive binding experimentInhibition of human cloned histamine H1 receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
9894665 103813 1 None -114 8 Guinea pig 7.4 pKi = 7.4 Binding
Binding affinity towards histamine H1 receptor was determined in guinea pig brain using [3H]pyrilamine as radioligandBinding affinity towards histamine H1 receptor was determined in guinea pig brain using [3H]pyrilamine as radioligand
ChEMBL 585 10 2 8 3.3 CC(C)Oc1ccccc1N1CCN(C[C@@H](O)CNC(=O)c2ccc3c(c2)C(=O)N(c2ccc(N(C)C)cc2)C3=O)CC1 10.1021/jm9905918
CHEMBL309106 103813 1 None -114 8 Guinea pig 7.4 pKi = 7.4 Binding
Binding affinity towards histamine H1 receptor was determined in guinea pig brain using [3H]pyrilamine as radioligandBinding affinity towards histamine H1 receptor was determined in guinea pig brain using [3H]pyrilamine as radioligand
ChEMBL 585 10 2 8 3.3 CC(C)Oc1ccccc1N1CCN(C[C@@H](O)CNC(=O)c2ccc3c(c2)C(=O)N(c2ccc(N(C)C)cc2)C3=O)CC1 10.1021/jm9905918
46884119 8150 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 328 5 0 3 4.7 CC(c1cccc(F)n1)c1c(CCN(C)C)sc2ccccc12 10.1016/j.bmcl.2010.01.134
CHEMBL1091793 8150 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 328 5 0 3 4.7 CC(c1cccc(F)n1)c1c(CCN(C)C)sc2ccccc12 10.1016/j.bmcl.2010.01.134
57334404 90512 0 None -3 5 Guinea pig 7.4 pKi = 7.4 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysisDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysis
ChEMBL 512 8 0 6 6.8 O=c1cc(-c2ccccc2)c2ccc(OCCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc2o1 10.1021/jm400408r
CHEMBL2387265 90512 0 None -3 5 Guinea pig 7.4 pKi = 7.4 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysisDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysis
ChEMBL 512 8 0 6 6.8 O=c1cc(-c2ccccc2)c2ccc(OCCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc2o1 10.1021/jm400408r
2389 3331 118 None -52 67 Guinea pig 7.4 pKi = 7.4 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates after 60 mins by liquid scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates after 60 mins by liquid scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2015.09.045
5073 3331 118 None -52 67 Guinea pig 7.4 pKi = 7.4 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates after 60 mins by liquid scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates after 60 mins by liquid scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2015.09.045
96 3331 118 None -52 67 Guinea pig 7.4 pKi = 7.4 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates after 60 mins by liquid scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates after 60 mins by liquid scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2015.09.045
CHEMBL85 3331 118 None -52 67 Guinea pig 7.4 pKi = 7.4 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates after 60 mins by liquid scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates after 60 mins by liquid scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2015.09.045
DB00734 3331 118 None -52 67 Guinea pig 7.4 pKi = 7.4 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates after 60 mins by liquid scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates after 60 mins by liquid scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2015.09.045
44335368 5050 0 None 2 3 Human 6.4 pKi = 6.4 Binding
Binding affinity at human cortical Histamine 1 receptorBinding affinity at human cortical Histamine 1 receptor
ChEMBL 393 7 0 5 3.8 CCOC(=O)N1CCN(CCCOc2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/s0960-894x(02)00648-0
CHEMBL105268 5050 0 None 2 3 Human 6.4 pKi = 6.4 Binding
Binding affinity at human cortical Histamine 1 receptorBinding affinity at human cortical Histamine 1 receptor
ChEMBL 393 7 0 5 3.8 CCOC(=O)N1CCN(CCCOc2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/s0960-894x(02)00648-0
44304282 203113 0 None -1 3 Human 6.4 pKi = 6.4 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 410 8 0 5 3.8 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3cccc(C)c3)cc2)CC1 10.1016/s0960-894x(02)00309-8
CHEMBL64021 203113 0 None -1 3 Human 6.4 pKi = 6.4 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 410 8 0 5 3.8 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3cccc(C)c3)cc2)CC1 10.1016/s0960-894x(02)00309-8
11808247 18075 0 None -4 9 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL126667 18075 0 None -4 9 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819366 18075 0 None -4 9 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
127052294 140302 0 None -15 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 incubated for 60 mins by liquid scintillation counting method
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3806079 140302 0 None -15 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 incubated for 60 mins by liquid scintillation counting method
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
164610892 185198 0 None -53 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 394 8 4 4 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CC1CCCCC1 10.1016/j.ejmech.2021.113190
CHEMBL4857560 185198 0 None -53 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 394 8 4 4 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CC1CCCCC1 10.1016/j.ejmech.2021.113190
11808247 18075 0 None -4 9 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL126667 18075 0 None -4 9 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819366 18075 0 None -4 9 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
71452382 83794 0 None -120 10 Human 5.4 pKi = 5.4 Binding
Binding affinity to Histamine H1 receptorBinding affinity to Histamine H1 receptor
ChEMBL 309 4 1 3 2.0 COc1ccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1 10.1016/j.bmcl.2012.08.046
CHEMBL2205812 83794 0 None -120 10 Human 5.4 pKi = 5.4 Binding
Binding affinity to Histamine H1 receptorBinding affinity to Histamine H1 receptor
ChEMBL 309 4 1 3 2.0 COc1ccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1 10.1016/j.bmcl.2012.08.046
1353 1911 93 None -602 83 Rat 6.4 pKi = 6.4 Binding
Half-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenateHalf-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenate
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm010982y
3559 1911 93 None -602 83 Rat 6.4 pKi = 6.4 Binding
Half-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenateHalf-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenate
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm010982y
86 1911 93 None -602 83 Rat 6.4 pKi = 6.4 Binding
Half-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenateHalf-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenate
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm010982y
CHEMBL54 1911 93 None -602 83 Rat 6.4 pKi = 6.4 Binding
Half-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenateHalf-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenate
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm010982y
DB00502 1911 93 None -602 83 Rat 6.4 pKi = 6.4 Binding
Half-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenateHalf-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenate
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm010982y
1353 1911 93 None -602 83 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamineIn vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamine
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0309811
3559 1911 93 None -602 83 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamineIn vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamine
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0309811
86 1911 93 None -602 83 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamineIn vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamine
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0309811
CHEMBL54 1911 93 None -602 83 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamineIn vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamine
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0309811
DB00502 1911 93 None -602 83 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamineIn vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamine
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0309811
46882224 6348 0 None -354 5 Human 4.4 pKi = 4.4 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 543 10 1 9 4.7 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)CC)ccc4o3)CC2)cc(OC2CCOCC2)c1 10.1016/j.bmcl.2009.09.024
CHEMBL1082036 6348 0 None -354 5 Human 4.4 pKi = 4.4 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 543 10 1 9 4.7 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)CC)ccc4o3)CC2)cc(OC2CCOCC2)c1 10.1016/j.bmcl.2009.09.024
20293994 199815 8 None 1 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cellsDisplacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cells
ChEMBL 239 6 1 1 3.8 CNCCCC(c1ccccc1)c1ccccc1 10.1016/j.bmc.2009.08.016
CHEMBL594138 199815 8 None 1 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cellsDisplacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cells
ChEMBL 239 6 1 1 3.8 CNCCCC(c1ccccc1)c1ccccc1 10.1016/j.bmc.2009.08.016
11393516 5172 0 None -467 4 Human 5.4 pKi = 5.4 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 335 6 1 4 3.3 N#Cc1ccc(-c2ccc(OCCCN3CCCNCC3)cc2)cc1 10.1016/s0960-894x(02)00648-0
CHEMBL105967 5172 0 None -467 4 Human 5.4 pKi = 5.4 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 335 6 1 4 3.3 N#Cc1ccc(-c2ccc(OCCCN3CCCNCC3)cc2)cc1 10.1016/s0960-894x(02)00648-0
69355600 78685 0 None -954 4 Human 5.4 pKi = 5.4 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 336 6 1 4 3.5 C[C@@]1(O)CCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)C1 10.1016/s0960-894x(02)00648-0
CHEMBL2112461 78685 0 None -954 4 Human 5.4 pKi = 5.4 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 336 6 1 4 3.5 C[C@@]1(O)CCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)C1 10.1016/s0960-894x(02)00648-0
168278543 192851 0 None -2 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 358 4 4 4 1.6 N/C(=N\C(=O)NCc1ccccc1)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
CHEMBL5184846 192851 0 None -2 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 358 4 4 4 1.6 N/C(=N\C(=O)NCc1ccccc1)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
CHEMBL5221764 192851 0 None -2 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 358 4 4 4 1.6 N/C(=N\C(=O)NCc1ccccc1)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
168284289 192906 0 None -3 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 428 8 4 4 3.1 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
CHEMBL5194860 192906 0 None -3 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 428 8 4 4 3.1 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
CHEMBL5222123 192906 0 None -3 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 428 8 4 4 3.1 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
44301729 200942 0 None -1 2 Rat 7.4 pKi = 7.4 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
ChEMBL 382 11 2 3 5.0 Clc1ccc(C(CCNCCCCCc2c[nH]cn2)c2ccccn2)cc1 10.1016/s0960-894x(03)00357-3
CHEMBL60175 200942 0 None -1 2 Rat 7.4 pKi = 7.4 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
ChEMBL 382 11 2 3 5.0 Clc1ccc(C(CCNCCCCCc2c[nH]cn2)c2ccccn2)cc1 10.1016/s0960-894x(03)00357-3
141485892 170978 0 None 4 2 Guinea pig 7.4 pKi = 7.4 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysisDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysis
ChEMBL 288 5 0 3 2.2 CN1CCc2ccc(OCCCN3CCCC3)cc2C1=O 10.1016/j.bmcl.2019.04.015
CHEMBL4456092 170978 0 None 4 2 Guinea pig 7.4 pKi = 7.4 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysisDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysis
ChEMBL 288 5 0 3 2.2 CN1CCc2ccc(OCCCN3CCCC3)cc2C1=O 10.1016/j.bmcl.2019.04.015
44622872 197716 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation counting
ChEMBL 413 8 1 2 6.0 Cc1ccc(CCCCN2CCC(C(O)(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2009.07.047
CHEMBL571389 197716 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation counting
ChEMBL 413 8 1 2 6.0 Cc1ccc(CCCCN2CCC(C(O)(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2009.07.047
66615619 81271 0 None -79 2 Human 7.4 pKi = 7.4 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 522 8 1 4 5.7 Cc1c(Cl)ccc(OC2CCN(CC3CCN([C@@H](Cc4ccc(F)cc4)C(=O)O)CC3)CC2)c1Cl 10.1016/j.bmcl.2012.08.103
CHEMBL2158783 81271 0 None -79 2 Human 7.4 pKi = 7.4 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 522 8 1 4 5.7 Cc1c(Cl)ccc(OC2CCN(CC3CCN([C@@H](Cc4ccc(F)cc4)C(=O)O)CC3)CC2)c1Cl 10.1016/j.bmcl.2012.08.103
71462103 81302 1 None 2 2 Human 7.4 pKi = 7.4 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 492 8 1 5 5.2 O=C(O)COc1ccc(N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.103
CHEMBL2158830 81302 1 None 2 2 Human 7.4 pKi = 7.4 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 492 8 1 5 5.2 O=C(O)COc1ccc(N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.103
59296099 84090 0 None -50 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 494 7 3 5 3.7 Cc1c(Cl)ccc(OC2CCN(C[C@H](O)CNC(=O)c3c[nH]nc3C(F)(F)F)CC2)c1Cl 10.1016/j.bmcl.2012.09.112
CHEMBL2207660 84090 0 None -50 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 494 7 3 5 3.7 Cc1c(Cl)ccc(OC2CCN(C[C@H](O)CNC(=O)c3c[nH]nc3C(F)(F)F)CC2)c1Cl 10.1016/j.bmcl.2012.09.112
2337 3256 77 None -1 62 Guinea pig 7.4 pKi = 7.4 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm070516u
50 3256 77 None -1 62 Guinea pig 7.4 pKi = 7.4 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm070516u
5002 3256 77 None -1 62 Guinea pig 7.4 pKi = 7.4 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm070516u
CHEMBL716 3256 77 None -1 62 Guinea pig 7.4 pKi = 7.4 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm070516u
DB01224 3256 77 None -1 62 Guinea pig 7.4 pKi = 7.4 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm070516u
71449859 82248 0 None 10 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 600 10 1 8 5.1 O=C(O)CCCCn1nnc(-c2ccc(C(=O)N3CCC(N4CCC(Oc5ccc(Cl)c(Cl)c5)CC4)CC3)cc2)n1 10.1016/j.bmcl.2012.08.124
CHEMBL2171029 82248 0 None 10 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 600 10 1 8 5.1 O=C(O)CCCCn1nnc(-c2ccc(C(=O)N3CCC(N4CCC(Oc5ccc(Cl)c(Cl)c5)CC4)CC3)cc2)n1 10.1016/j.bmcl.2012.08.124
17963347 82264 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 579 5 1 5 5.4 O=C(NS(=O)(=O)c1cccc(C(F)(F)F)c1)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
CHEMBL2171045 82264 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 579 5 1 5 5.4 O=C(NS(=O)(=O)c1cccc(C(F)(F)F)c1)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
11702578 8148 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 324 5 0 3 4.9 Cc1ccnc(C(C)c2c(CCN(C)C)sc3ccccc23)c1 10.1016/j.bmcl.2010.01.134
CHEMBL1091791 8148 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 324 5 0 3 4.9 Cc1ccnc(C(C)c2c(CCN(C)C)sc3ccccc23)c1 10.1016/j.bmcl.2010.01.134
25212275 174421 0 None -9332 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 682 13 0 8 7.4 O=C(OCCN1CCN(CCCN2c3ccccc3Sc3ccc(C(F)(F)F)cc32)CC1)c1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
CHEMBL455288 174421 0 None -9332 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 682 13 0 8 7.4 O=C(OCCN1CCN(CCCN2c3ccccc3Sc3ccc(C(F)(F)F)cc32)CC1)c1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
10436842 100256 0 None -501 7 Human 6.4 pKi = 6.4 Binding
Selectivity screen against human Histamine H1 receptorSelectivity screen against human Histamine H1 receptor
ChEMBL 524 7 1 4 4.6 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1C 10.1016/s0960-894x(99)00696-4
CHEMBL288772 100256 0 None -501 7 Human 6.4 pKi = 6.4 Binding
Selectivity screen against human Histamine H1 receptorSelectivity screen against human Histamine H1 receptor
ChEMBL 524 7 1 4 4.6 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1C 10.1016/s0960-894x(99)00696-4
44304247 202809 0 None -38 3 Human 6.4 pKi = 6.4 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 412 11 0 5 4.3 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccco3)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL62312 202809 0 None -38 3 Human 6.4 pKi = 6.4 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 412 11 0 5 4.3 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccco3)CC2)cc1 10.1016/s0960-894x(02)00309-8
71451390 81266 0 None -7 2 Human 6.4 pKi = 6.4 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 474 8 1 4 4.7 O=C(O)[C@H](Cc1ccc(F)cc1)N1CCC(CN2CCC(Oc3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158778 81266 0 None -7 2 Human 6.4 pKi = 6.4 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 474 8 1 4 4.7 O=C(O)[C@H](Cc1ccc(F)cc1)N1CCC(CN2CCC(Oc3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2012.08.103
1353 1911 93 None -213 83 Guinea pig 6.4 pKi = 6.4 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm070516u
3559 1911 93 None -213 83 Guinea pig 6.4 pKi = 6.4 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm070516u
86 1911 93 None -213 83 Guinea pig 6.4 pKi = 6.4 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm070516u
CHEMBL54 1911 93 None -213 83 Guinea pig 6.4 pKi = 6.4 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm070516u
DB00502 1911 93 None -213 83 Guinea pig 6.4 pKi = 6.4 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm070516u
44304291 202852 0 None -891 3 Human 5.4 pKi = 5.4 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 388 11 0 4 4.0 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)C(C)C)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL62527 202852 0 None -891 3 Human 5.4 pKi = 5.4 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 388 11 0 4 4.0 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)C(C)C)CC2)cc1 10.1016/s0960-894x(02)00309-8
44335238 5089 0 None -1862 4 Human 5.4 pKi = 5.4 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 348 6 0 3 5.3 CC1CCCC(C)N1CCCOc1ccc(-c2ccc(C#N)cc2)cc1 10.1016/s0960-894x(02)00648-0
CHEMBL105515 5089 0 None -1862 4 Human 5.4 pKi = 5.4 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 348 6 0 3 5.3 CC1CCCC(C)N1CCCOc1ccc(-c2ccc(C#N)cc2)cc1 10.1016/s0960-894x(02)00648-0
168294182 193048 0 None -57 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 314 6 4 2 1.7 C[C@@H](NC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5208722 193048 0 None -57 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 314 6 4 2 1.7 C[C@@H](NC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222960 193048 0 None -57 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 314 6 4 2 1.7 C[C@@H](NC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/acs.jmedchem.1c00692
10017820 204195 0 None -199 3 Guinea pig 5.4 pKi = 5.4 Binding
Displacement of [3H]mepyramine bound to membranes of CHO cells expressing guinea pig H1 receptorsDisplacement of [3H]mepyramine bound to membranes of CHO cells expressing guinea pig H1 receptors
ChEMBL 302 8 3 2 2.8 S=C(NCCCCCc1c[nH]cn1)NCc1ccccc1 10.1021/jm00012a025
CHEMBL70811 204195 0 None -199 3 Guinea pig 5.4 pKi = 5.4 Binding
Displacement of [3H]mepyramine bound to membranes of CHO cells expressing guinea pig H1 receptorsDisplacement of [3H]mepyramine bound to membranes of CHO cells expressing guinea pig H1 receptors
ChEMBL 302 8 3 2 2.8 S=C(NCCCCCc1c[nH]cn1)NCc1ccccc1 10.1021/jm00012a025
18878 144203 90 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 177 2 1 2 1.8 c1ccc(OC2CCNCC2)cc1 10.1021/acs.jmedchem.6b00981
CHEMBL3904359 144203 90 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 177 2 1 2 1.8 c1ccc(OC2CCNCC2)cc1 10.1021/acs.jmedchem.6b00981
10686633 56532 0 None -1621 2 Guinea pig 4.4 pKi = 4.4 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 313 5 2 3 3.6 O=C(Nc1ccccc1C(F)(F)F)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL16373 56532 0 None -1621 2 Guinea pig 4.4 pKi = 4.4 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 313 5 2 3 3.6 O=C(Nc1ccccc1C(F)(F)F)OCCCc1c[nH]cn1 10.1021/jm9507688
10682710 57493 1 None -3801 2 Guinea pig 4.4 pKi = 4.4 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 259 6 2 3 2.3 O=C(NCc1ccccc1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL16592 57493 1 None -3801 2 Guinea pig 4.4 pKi = 4.4 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 259 6 2 3 2.3 O=C(NCc1ccccc1)OCCCc1c[nH]cn1 10.1021/jm9507688
10474353 58777 0 None -4168 2 Guinea pig 4.4 pKi = 4.4 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 371 5 2 3 3.2 O=C(Nc1ccc(I)cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL16874 58777 0 None -4168 2 Guinea pig 4.4 pKi = 4.4 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 371 5 2 3 3.2 O=C(Nc1ccc(I)cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
1204 1932 119 None -501 24 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor S3.36C mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor S3.36C mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1038/nchembio714
1247 1932 119 None -501 24 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor S3.36C mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor S3.36C mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1038/nchembio714
1375 1932 119 None -501 24 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor S3.36C mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor S3.36C mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1038/nchembio714
774 1932 119 None -501 24 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor S3.36C mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor S3.36C mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1038/nchembio714
CHEMBL90 1932 119 None -501 24 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor S3.36C mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor S3.36C mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1038/nchembio714
DB05381 1932 119 None -501 24 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor S3.36C mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor S3.36C mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1038/nchembio714
2775690 93011 53 None -15 6 Human 6.4 pKi = 6.4 Binding
Binding affinity to histamine H1 receptor (unknown origin)Binding affinity to histamine H1 receptor (unknown origin)
ChEMBL 295 1 1 3 3.0 Cc1ccc2nc(C(F)(F)F)cc(N3CCNCC3)c2c1 10.1021/ml400312j
CHEMBL2441619 93011 53 None -15 6 Human 6.4 pKi = 6.4 Binding
Binding affinity to histamine H1 receptor (unknown origin)Binding affinity to histamine H1 receptor (unknown origin)
ChEMBL 295 1 1 3 3.0 Cc1ccc2nc(C(F)(F)F)cc(N3CCNCC3)c2c1 10.1021/ml400312j
11265950 195913 0 None -6 3 Human 8.4 pKi = 8.4 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 279 5 0 3 3.0 CN(C)CCC1=C(Cc2cnccn2)c2ccccc2C1 10.1016/j.bmcl.2010.02.055
CHEMBL559251 195913 0 None -6 3 Human 8.4 pKi = 8.4 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 279 5 0 3 3.0 CN(C)CCC1=C(Cc2cnccn2)c2ccccc2C1 10.1016/j.bmcl.2010.02.055
11265950 195913 0 None -6 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 279 5 0 3 3.0 CN(C)CCC1=C(Cc2cnccn2)c2ccccc2C1 10.1016/j.bmcl.2010.12.053
CHEMBL559251 195913 0 None -6 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 279 5 0 3 3.0 CN(C)CCC1=C(Cc2cnccn2)c2ccccc2C1 10.1016/j.bmcl.2010.12.053
11265950 195913 0 None -6 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation counting
ChEMBL 279 5 0 3 3.0 CN(C)CCC1=C(Cc2cnccn2)c2ccccc2C1 10.1021/jm900933k
CHEMBL559251 195913 0 None -6 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation counting
ChEMBL 279 5 0 3 3.0 CN(C)CCC1=C(Cc2cnccn2)c2ccccc2C1 10.1021/jm900933k
11580427 196610 11 None 1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation counting
ChEMBL 310 5 0 3 4.6 C[C@@H](c1ccccn1)c1c(CCN(C)C)sc2ccccc12 10.1021/jm900933k
CHEMBL564144 196610 11 None 1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation counting
ChEMBL 310 5 0 3 4.6 C[C@@H](c1ccccn1)c1c(CCN(C)C)sc2ccccc12 10.1021/jm900933k
11465618 102398 23 None -14 19 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]pyrilamine from recombinant human H1 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]pyrilamine from recombinant human H1 receptor measured after 60 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
CHEMBL3039528 102398 23 None -14 19 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]pyrilamine from recombinant human H1 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]pyrilamine from recombinant human H1 receptor measured after 60 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
CHEMBL5191141 102398 23 None -14 19 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]pyrilamine from recombinant human H1 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]pyrilamine from recombinant human H1 receptor measured after 60 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
44312705 103098 0 None - 1 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cellsIn vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 454 7 2 5 4.1 NC(=O)N(O)Cc1ccc(CN2CCN([C@H](c3ccccc3)c3ccc(Cl)cc3)CC2)o1 10.1016/j.bmcl.2004.02.005
CHEMBL307609 103098 0 None - 1 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cellsIn vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 454 7 2 5 4.1 NC(=O)N(O)Cc1ccc(CN2CCN([C@H](c3ccccc3)c3ccc(Cl)cc3)CC2)o1 10.1016/j.bmcl.2004.02.005
11580427 196610 11 None 1 2 Human 8.4 pKi = 8.4 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 310 5 0 3 4.6 C[C@@H](c1ccccn1)c1c(CCN(C)C)sc2ccccc12 10.1016/j.bmcl.2010.07.117
CHEMBL564144 196610 11 None 1 2 Human 8.4 pKi = 8.4 Binding
Inhibition of histamine H1 receptorInhibition of histamine H1 receptor
ChEMBL 310 5 0 3 4.6 C[C@@H](c1ccccn1)c1c(CCN(C)C)sc2ccccc12 10.1016/j.bmcl.2010.07.117
46884699 8305 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 307 5 0 3 3.9 Cc1ccc2c(c1)CC(CCN(C)C)=C2[C@@H](C)c1cnccn1 10.1016/j.bmcl.2010.02.055
CHEMBL1092663 8305 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 307 5 0 3 3.9 Cc1ccc2c(c1)CC(CCN(C)C)=C2[C@@H](C)c1cnccn1 10.1016/j.bmcl.2010.02.055
14127191 11297 0 None - 1 Guinea pig 8.4 pKi = 8.4 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 323 4 1 3 3.7 CN(C)CC/C=C1\c2ccccc2COc2ccc(C(=O)O)cc21 10.1021/jm00089a020
CHEMBL1179239 11297 0 None - 1 Guinea pig 8.4 pKi = 8.4 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 323 4 1 3 3.7 CN(C)CC/C=C1\c2ccccc2COc2ccc(C(=O)O)cc21 10.1021/jm00089a020
CHEMBL65822 11297 0 None - 1 Guinea pig 8.4 pKi = 8.4 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 323 4 1 3 3.7 CN(C)CC/C=C1\c2ccccc2COc2ccc(C(=O)O)cc21 10.1021/jm00089a020
15749428 100876 0 None - 1 Guinea pig 8.4 pKi = 8.4 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 351 6 1 3 4.0 CN(C)CC/C=C1\c2ccccc2COc2ccc(CCC(=O)O)cc21 10.1021/jm00089a020
CHEMBL293652 100876 0 None - 1 Guinea pig 8.4 pKi = 8.4 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 351 6 1 3 4.0 CN(C)CC/C=C1\c2ccccc2COc2ccc(CCC(=O)O)cc21 10.1021/jm00089a020
9805944 56227 37 None -6 9 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptorDisplacement of [3H]pyrilamine from human histamine H1 receptor
ChEMBL 462 7 2 3 4.7 CNC(=O)C(CCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm800510m
CHEMBL1627 56227 37 None -6 9 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptorDisplacement of [3H]pyrilamine from human histamine H1 receptor
ChEMBL 462 7 2 3 4.7 CNC(=O)C(CCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm800510m
2726 919 68 None -2 72 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2008.09.012
621 919 68 None -2 72 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2008.09.012
83 919 68 None -2 72 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2008.09.012
CHEMBL71 919 68 None -2 72 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2008.09.012
DB00477 919 68 None -2 72 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2008.09.012
44326336 111413 0 None 5 3 Human 8.4 pKi = 8.4 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 311 2 0 3 4.3 CN(C)CC1C[C@@H]2c3ccccc3Sc3ccccc3[C@H]2O1 10.1016/j.bmcl.2004.03.069
CHEMBL327306 111413 0 None 5 3 Human 8.4 pKi = 8.4 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 311 2 0 3 4.3 CN(C)CC1C[C@@H]2c3ccccc3Sc3ccccc3[C@H]2O1 10.1016/j.bmcl.2004.03.069
53320189 57755 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 291 5 0 3 3.1 c1ccc2c(c1)CC(CCN1CCC1)=C2Cc1cnccn1 10.1016/j.bmcl.2010.12.053
CHEMBL1669412 57755 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 291 5 0 3 3.1 c1ccc2c(c1)CC(CCN1CCC1)=C2Cc1cnccn1 10.1016/j.bmcl.2010.12.053
9949441 114461 0 None 2 5 Rat 8.4 pKi = 8.4 Binding
Half-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenateHalf-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenate
ChEMBL 331 2 0 4 3.5 CCN1CCN(C2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
CHEMBL333455 114461 0 None 2 5 Rat 8.4 pKi = 8.4 Binding
Half-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenateHalf-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenate
ChEMBL 331 2 0 4 3.5 CCN1CCN(C2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
135398745 2914 112 None -1 65 Rat 8.4 pKi = 8.4 Binding
In vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamineIn vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamine
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm0309811
47 2914 112 None -1 65 Rat 8.4 pKi = 8.4 Binding
In vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamineIn vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamine
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm0309811
CHEMBL715 2914 112 None -1 65 Rat 8.4 pKi = 8.4 Binding
In vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamineIn vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamine
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm0309811
DB00334 2914 112 None -1 65 Rat 8.4 pKi = 8.4 Binding
In vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamineIn vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamine
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm0309811
44401243 168494 0 None -1 9 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 329 2 0 3 4.6 CN(C)C[C@H]1CC2c3ccccc3Oc3ccc(Cl)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL435301 168494 0 None -1 9 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 329 2 0 3 4.6 CN(C)C[C@H]1CC2c3ccccc3Oc3ccc(Cl)cc3[C@H]2O1 10.1021/jm049632c
46830289 8360 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 299 5 0 4 3.8 C[C@H](c1c(CCN(C)C)sc2ccccc12)n1cccn1 10.1016/j.bmcl.2010.01.134
CHEMBL1093058 8360 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 299 5 0 4 3.8 C[C@H](c1c(CCN(C)C)sc2ccccc12)n1cccn1 10.1016/j.bmcl.2010.01.134
6726 1280 51 None 3 13 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
7151 1280 51 None 3 13 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
749 1280 51 None 3 13 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
CHEMBL648 1280 51 None 3 13 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
DB01176 1280 51 None 3 13 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
1210 918 51 None -20 21 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/j.bmcl.2013.12.024
1213 918 51 None -20 21 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/j.bmcl.2013.12.024
2725 918 51 None -20 21 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/j.bmcl.2013.12.024
33036 918 51 None -20 21 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/j.bmcl.2013.12.024
4411 918 51 None -20 21 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/j.bmcl.2013.12.024
616 918 51 None -20 21 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/j.bmcl.2013.12.024
6976 918 51 None -20 21 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/j.bmcl.2013.12.024
716121 918 51 None -20 21 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/j.bmcl.2013.12.024
CHEMBL1201353 918 51 None -20 21 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/j.bmcl.2013.12.024
CHEMBL1554789 918 51 None -20 21 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/j.bmcl.2013.12.024
CHEMBL505 918 51 None -20 21 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/j.bmcl.2013.12.024
DB01114 918 51 None -20 21 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/j.bmcl.2013.12.024
DB13679 918 51 None -20 21 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/j.bmcl.2013.12.024
1227 2489 43 None -2 12 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmcl.2011.09.001
2331 2489 43 None -2 12 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmcl.2011.09.001
3957 2489 43 None -2 12 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmcl.2011.09.001
4992 2489 43 None -2 12 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmcl.2011.09.001
CHEMBL511 2489 43 None -2 12 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmcl.2011.09.001
DB06691 2489 43 None -2 12 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
ChEMBL 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 10.1016/j.bmcl.2011.09.001
49782794 17916 0 None -16 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cellsDisplacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 409 4 1 4 4.0 CC(C)C(=O)NCc1ccc2c(c1)[C@H](N1CCN(C)CC1)Cc1ccccc1S2 10.1021/jm100652h
CHEMBL1259189 17916 0 None -16 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cellsDisplacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 409 4 1 4 4.0 CC(C)C(=O)NCc1ccc2c(c1)[C@H](N1CCN(C)CC1)Cc1ccccc1S2 10.1021/jm100652h
45272889 195900 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 422 6 1 5 4.2 Fc1ccc(Cn2c(N3CCC(NCC4CCOCC4)CC3)nc3ccccc32)cc1 10.1016/j.bmcl.2009.05.086
CHEMBL559060 195900 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 422 6 1 5 4.2 Fc1ccc(Cn2c(N3CCC(NCC4CCOCC4)CC3)nc3ccccc32)cc1 10.1016/j.bmcl.2009.05.086
2337 3256 77 None 1 62 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
50 3256 77 None 1 62 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
5002 3256 77 None 1 62 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
CHEMBL716 3256 77 None 1 62 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
DB01224 3256 77 None 1 62 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
25056048 102613 0 None - 1 Guinea pig 8.3 pKi = 8.3 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 351 6 1 3 4.0 CN(C)CCC/C=C1/c2ccccc2COc2ccc(CC(=O)O)cc21 10.1021/jm00089a020
CHEMBL304185 102613 0 None - 1 Guinea pig 8.3 pKi = 8.3 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 351 6 1 3 4.0 CN(C)CCC/C=C1/c2ccccc2COc2ccc(CC(=O)O)cc21 10.1021/jm00089a020
46884201 8145 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 316 5 0 4 4.6 C[C@@H](c1cscn1)c1c(CCN(C)C)sc2ccccc12 10.1016/j.bmcl.2010.01.134
CHEMBL1091782 8145 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 316 5 0 4 4.6 C[C@@H](c1cscn1)c1c(CCN(C)C)sc2ccccc12 10.1016/j.bmcl.2010.01.134
11023546 78478 0 None 2 4 Rat 8.3 pKi = 8.3 Binding
Half-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenateHalf-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenate
ChEMBL 317 1 0 4 3.1 CN1CCN([C@H]2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
CHEMBL2111783 78478 0 None 2 4 Rat 8.3 pKi = 8.3 Binding
Half-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenateHalf-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenate
ChEMBL 317 1 0 4 3.1 CN1CCN([C@H]2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
1212 1662 50 None -41 65 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 1662 50 None -41 65 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 1662 50 None -41 65 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 1662 50 None -41 65 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 1662 50 None -41 65 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
49836299 18744 0 None 10 5 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]pyrilamine from histamine H1 receptor in Sprague-Dawley rat cortical membrane by liquid scintillation countingDisplacement of [3H]pyrilamine from histamine H1 receptor in Sprague-Dawley rat cortical membrane by liquid scintillation counting
ChEMBL 375 2 1 2 4.4 O=C(O)C1CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)CC1 10.1021/jm100856p
CHEMBL1277770 18744 0 None 10 5 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]pyrilamine from histamine H1 receptor in Sprague-Dawley rat cortical membrane by liquid scintillation countingDisplacement of [3H]pyrilamine from histamine H1 receptor in Sprague-Dawley rat cortical membrane by liquid scintillation counting
ChEMBL 375 2 1 2 4.4 O=C(O)C1CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)CC1 10.1021/jm100856p
46889258 7541 0 None 316 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation counting
ChEMBL 302 6 0 5 2.2 CCOCCn1c(N2CC[C@H](N(C)C)C2)nc2ccccc21 10.1016/j.bmcl.2010.03.027
CHEMBL1087493 7541 0 None 316 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation counting
ChEMBL 302 6 0 5 2.2 CCOCCn1c(N2CC[C@H](N(C)C)C2)nc2ccccc21 10.1016/j.bmcl.2010.03.027
51039226 57768 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 370 7 0 4 4.5 C[C@H](C1=C(CCN(C)Cc2ccncc2)Cc2ccccc21)c1cnccn1 10.1016/j.bmcl.2010.12.053
CHEMBL1669425 57768 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 370 7 0 4 4.5 C[C@H](C1=C(CCN(C)Cc2ccncc2)Cc2ccccc21)c1cnccn1 10.1016/j.bmcl.2010.12.053
44267118 9698 0 None - 1 Rat 7.4 pKi = 7.4 Binding
Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.
ChEMBL 396 1 1 3 4.3 CC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3cc(C(C)O)cnc32)CC1 10.1016/S0960-894X(00)80290-5
CHEMBL11313 9698 0 None - 1 Rat 7.4 pKi = 7.4 Binding
Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.
ChEMBL 396 1 1 3 4.3 CC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3cc(C(C)O)cnc32)CC1 10.1016/S0960-894X(00)80290-5
17867054 48941 0 None -1 4 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]- pyrilamine from rat brain membrane Histamine H1 receptorDisplacement of [3H]- pyrilamine from rat brain membrane Histamine H1 receptor
ChEMBL 435 5 0 5 4.3 Cn1c(=O)sc2cc(CCN3CCN(Cc4ccc(Cl)c(Cl)c4)CC3)ccc21 10.1016/s0960-894x(02)00123-3
CHEMBL15601 48941 0 None -1 4 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]- pyrilamine from rat brain membrane Histamine H1 receptorDisplacement of [3H]- pyrilamine from rat brain membrane Histamine H1 receptor
ChEMBL 435 5 0 5 4.3 Cn1c(=O)sc2cc(CCN3CCN(Cc4ccc(Cl)c(Cl)c4)CC3)ccc21 10.1016/s0960-894x(02)00123-3
137646281 157806 0 None -91 17 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-pyrilamine from recombinant human H1 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-pyrilamine from recombinant human H1 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 423 8 0 7 3.8 COc1ccccc1N1CCN(CCCSc2nnc(-c3ccccc3)n2C)CC1 10.1021/acs.jmedchem.9b00412
CHEMBL4083252 157806 0 None -91 17 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-pyrilamine from recombinant human H1 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-pyrilamine from recombinant human H1 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 423 8 0 7 3.8 COc1ccccc1N1CCN(CCCSc2nnc(-c3ccccc3)n2C)CC1 10.1021/acs.jmedchem.9b00412
72152557 163072 5 None -1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 331 6 1 5 2.8 Clc1cncc(NCCCN2CCN(c3ccccc3)CC2)n1 10.1021/acs.jmedchem.8b00718
CHEMBL4176490 163072 5 None -1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 331 6 1 5 2.8 Clc1cncc(NCCCN2CCN(c3ccccc3)CC2)n1 10.1021/acs.jmedchem.8b00718
1212 1662 50 None -41 65 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1016/j.bmcl.2008.09.012
204 1662 50 None -41 65 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1016/j.bmcl.2008.09.012
3372 1662 50 None -41 65 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1016/j.bmcl.2008.09.012
CHEMBL726 1662 50 None -41 65 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1016/j.bmcl.2008.09.012
DB00623 1662 50 None -41 65 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1016/j.bmcl.2008.09.012
25212276 190066 0 None -112 6 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 508 11 0 3 7.4 CN(CCCC12CCC(c3ccccc31)c1ccccc12)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
CHEMBL517244 190066 0 None -112 6 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 508 11 0 3 7.4 CN(CCCC12CCC(c3ccccc31)c1ccccc12)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
2600 3779 74 None 1 13 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation counting
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1016/j.bmcl.2009.07.047
2608 3779 74 None 1 13 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation counting
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1016/j.bmcl.2009.07.047
5405 3779 74 None 1 13 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation counting
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1016/j.bmcl.2009.07.047
CHEMBL17157 3779 74 None 1 13 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation counting
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1016/j.bmcl.2009.07.047
DB00342 3779 74 None 1 13 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation counting
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1016/j.bmcl.2009.07.047
44308991 163497 0 None -8 2 Guinea pig 7.4 pKi = 7.4 Binding
Evaluated for the percent binding affinity against H1 receptor by an H1 histamine-mediated bronchospasmEvaluated for the percent binding affinity against H1 receptor by an H1 histamine-mediated bronchospasm
ChEMBL 435 12 1 5 3.8 O=S(=O)(c1ccc(Cl)cc1)N(CCCCc1c[nH]cn1)CCCCn1ccnc1 10.1016/s0960-894x(98)00379-5
CHEMBL420181 163497 0 None -8 2 Guinea pig 7.4 pKi = 7.4 Binding
Evaluated for the percent binding affinity against H1 receptor by an H1 histamine-mediated bronchospasmEvaluated for the percent binding affinity against H1 receptor by an H1 histamine-mediated bronchospasm
ChEMBL 435 12 1 5 3.8 O=S(=O)(c1ccc(Cl)cc1)N(CCCCc1c[nH]cn1)CCCCn1ccnc1 10.1016/s0960-894x(98)00379-5
168296738 192269 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 714 18 6 8 1.2 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5205682 192269 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 714 18 6 8 1.2 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
168296738 192269 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 714 18 6 8 1.2 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5205682 192269 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 714 18 6 8 1.2 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
9818650 203525 0 None -1621 4 Human 5.4 pKi = 5.4 Binding
Compound was tested for its binding affinity towards human H1 receptorCompound was tested for its binding affinity towards human H1 receptor
ChEMBL 323 5 1 3 4.4 c1ccc2c(NCCCN3CCCC3)c3c(nc2c1)CCCCC3 10.1016/s0960-894x(03)00356-1
CHEMBL66388 203525 0 None -1621 4 Human 5.4 pKi = 5.4 Binding
Compound was tested for its binding affinity towards human H1 receptorCompound was tested for its binding affinity towards human H1 receptor
ChEMBL 323 5 1 3 4.4 c1ccc2c(NCCCN3CCCC3)c3c(nc2c1)CCCCC3 10.1016/s0960-894x(03)00356-1
162664702 182210 0 None -29 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cell membranes co-expressing RGS4 measured after 60 mins by scintillation counting analysisDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cell membranes co-expressing RGS4 measured after 60 mins by scintillation counting analysis
ChEMBL 407 7 0 4 5.0 Clc1ccc(-c2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)cc1 10.1016/j.ejmech.2020.113041
CHEMBL4783066 182210 0 None -29 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cell membranes co-expressing RGS4 measured after 60 mins by scintillation counting analysisDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cell membranes co-expressing RGS4 measured after 60 mins by scintillation counting analysis
ChEMBL 407 7 0 4 5.0 Clc1ccc(-c2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)cc1 10.1016/j.ejmech.2020.113041
53326712 57748 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 307 7 0 3 3.8 CCCN(C)CCC1=C(Cc2cnccn2)c2ccccc2C1 10.1016/j.bmcl.2010.12.053
CHEMBL1669406 57748 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 307 7 0 3 3.8 CCCN(C)CCC1=C(Cc2cnccn2)c2ccccc2C1 10.1016/j.bmcl.2010.12.053
10480204 116527 0 None - 1 Guinea pig 7.4 pKi = 7.4 Binding
Inhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptorInhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptor
ChEMBL 478 6 1 5 5.1 O=C(O)c1ccc2c(c1)C(SCCN1CCN(c3ccc(F)cc3)CC1)c1ccccc1CO2 10.1021/jm00055a013
CHEMBL336204 116527 0 None - 1 Guinea pig 7.4 pKi = 7.4 Binding
Inhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptorInhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptor
ChEMBL 478 6 1 5 5.1 O=C(O)c1ccc2c(c1)C(SCCN1CCN(c3ccc(F)cc3)CC1)c1ccccc1CO2 10.1021/jm00055a013
2389 3331 118 None -52 67 Guinea pig 7.4 pKi = 7.4 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellumDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C4MD00578C
5073 3331 118 None -52 67 Guinea pig 7.4 pKi = 7.4 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellumDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C4MD00578C
96 3331 118 None -52 67 Guinea pig 7.4 pKi = 7.4 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellumDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C4MD00578C
CHEMBL85 3331 118 None -52 67 Guinea pig 7.4 pKi = 7.4 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellumDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C4MD00578C
DB00734 3331 118 None -52 67 Guinea pig 7.4 pKi = 7.4 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellumDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C4MD00578C
1605 2342 117 None -2 4 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human histamine H1 receptor expressed in CHO-K1 cellsBinding affinity towards human histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1016/j.bmcl.2004.08.060
3957 2342 117 None -2 4 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human histamine H1 receptor expressed in CHO-K1 cellsBinding affinity towards human histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1016/j.bmcl.2004.08.060
7216 2342 117 None -2 4 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human histamine H1 receptor expressed in CHO-K1 cellsBinding affinity towards human histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1016/j.bmcl.2004.08.060
CHEMBL998 2342 117 None -2 4 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human histamine H1 receptor expressed in CHO-K1 cellsBinding affinity towards human histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1016/j.bmcl.2004.08.060
DB00455 2342 117 None -2 4 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human histamine H1 receptor expressed in CHO-K1 cellsBinding affinity towards human histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1016/j.bmcl.2004.08.060
13091358 70455 0 None -1023 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-Pyrilamine from human histamine H1 receptor by liquid scintillation counterDisplacement of [3H]-Pyrilamine from human histamine H1 receptor by liquid scintillation counter
ChEMBL 389 6 1 3 4.8 OC1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2CCCOc1ccc(F)cc1 10.1016/j.bmc.2012.01.022
CHEMBL1946122 70455 0 None -1023 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-Pyrilamine from human histamine H1 receptor by liquid scintillation counterDisplacement of [3H]-Pyrilamine from human histamine H1 receptor by liquid scintillation counter
ChEMBL 389 6 1 3 4.8 OC1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2CCCOc1ccc(F)cc1 10.1016/j.bmc.2012.01.022
13091356 113538 0 None -1023 8 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation countingDisplacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation counting
ChEMBL 389 6 1 3 4.8 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCOc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
CHEMBL3321789 113538 0 None -1023 8 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation countingDisplacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation counting
ChEMBL 389 6 1 3 4.8 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCOc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
44304376 202970 0 None -7 3 Human 6.4 pKi = 6.4 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 423 11 0 5 4.1 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccccn3)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL63036 202970 0 None -7 3 Human 6.4 pKi = 6.4 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 423 11 0 5 4.1 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccccn3)CC2)cc1 10.1016/s0960-894x(02)00309-8
10455457 203403 0 None -707 3 Human 5.4 pKi = 5.4 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 431 10 0 5 3.3 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)N3CCOCC3)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL65518 203403 0 None -707 3 Human 5.4 pKi = 5.4 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 431 10 0 5 3.3 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)N3CCOCC3)CC2)cc1 10.1016/s0960-894x(02)00309-8
112936352 137494 1 None 17 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 389 6 1 6 3.5 COc1ccc(CNc2cc(-c3ccccc3)nc(N3CCN(C)CC3)n2)cc1 10.1016/j.bmcl.2015.12.035
CHEMBL3754008 137494 1 None 17 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 389 6 1 6 3.5 COc1ccc(CNc2cc(-c3ccccc3)nc(N3CCN(C)CC3)n2)cc1 10.1016/j.bmcl.2015.12.035
873049 69029 8 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 269 3 0 5 2.2 c1ccc2c(c1)n(CCN1CCCCC1)c1ncnn21 10.1021/jm2011589
CHEMBL1923531 69029 8 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 269 3 0 5 2.2 c1ccc2c(c1)n(CCN1CCCCC1)c1ncnn21 10.1021/jm2011589
73353884 92322 0 None -3 8 Human 5.4 pKi = 5.4 Binding
Inhibition of histamine H1 receptor (unknown origin) by PDSP assayInhibition of histamine H1 receptor (unknown origin) by PDSP assay
ChEMBL 295 3 1 3 2.7 c1cc2c(cc1CN[C@H]1C3C4CC5C6C4CC3C6C51)OCO2 10.1016/j.bmc.2013.07.045
CHEMBL2429890 92322 0 None -3 8 Human 5.4 pKi = 5.4 Binding
Inhibition of histamine H1 receptor (unknown origin) by PDSP assayInhibition of histamine H1 receptor (unknown origin) by PDSP assay
ChEMBL 295 3 1 3 2.7 c1cc2c(cc1CN[C@H]1C3C4CC5C6C4CC3C6C51)OCO2 10.1016/j.bmc.2013.07.045
213 3853 55 None -8 44 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
2717 3853 55 None -8 44 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
5533 3853 55 None -8 44 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
CHEMBL621 3853 55 None -8 44 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
DB00656 3853 55 None -8 44 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
9864676 127808 0 None -2 5 Rat 7.4 pKi = 7.4 Binding
Inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat cortexInhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat cortex
ChEMBL 380 6 0 3 4.5 O=C(CCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
CHEMBL366388 127808 0 None -2 5 Rat 7.4 pKi = 7.4 Binding
Inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat cortexInhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat cortex
ChEMBL 380 6 0 3 4.5 O=C(CCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
44401105 69576 0 None -4 9 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 373 2 0 3 4.7 CN(C)C[C@H]1CC2c3ccccc3Oc3ccc(Br)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL193435 69576 0 None -4 9 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 373 2 0 3 4.7 CN(C)C[C@H]1CC2c3ccccc3Oc3ccc(Br)cc3[C@H]2O1 10.1021/jm049632c
10000169 22222 0 None - 1 Guinea pig 7.4 pKi = 7.4 Binding
Inhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptorInhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptor
ChEMBL 385 5 1 5 3.4 O=C(O)c1ccc2c(c1)C(SCCN1CCOCC1)c1ccccc1CO2 10.1021/jm00055a013
CHEMBL132306 22222 0 None - 1 Guinea pig 7.4 pKi = 7.4 Binding
Inhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptorInhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptor
ChEMBL 385 5 1 5 3.4 O=C(O)c1ccc2c(c1)C(SCCN1CCOCC1)c1ccccc1CO2 10.1021/jm00055a013
129103161 167070 0 None -588 13 Guinea pig 6.4 pKi = 6.4 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by liquid scintillation countingDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by liquid scintillation counting
ChEMBL 461 6 0 5 4.6 O=C(CCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1021/acs.jmedchem.8b01096
CHEMBL4289498 167070 0 None -588 13 Guinea pig 6.4 pKi = 6.4 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by liquid scintillation countingDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by liquid scintillation counting
ChEMBL 461 6 0 5 4.6 O=C(CCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1021/acs.jmedchem.8b01096
162657344 180932 0 None -489 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cell membranes co-expressing RGS4 measured after 60 mins by scintillation counting analysisDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cell membranes co-expressing RGS4 measured after 60 mins by scintillation counting analysis
ChEMBL 388 8 1 5 4.4 c1ccc(Nc2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)cc1 10.1016/j.ejmech.2020.113041
CHEMBL4758080 180932 0 None -489 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cell membranes co-expressing RGS4 measured after 60 mins by scintillation counting analysisDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cell membranes co-expressing RGS4 measured after 60 mins by scintillation counting analysis
ChEMBL 388 8 1 5 4.4 c1ccc(Nc2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)cc1 10.1016/j.ejmech.2020.113041
162666847 182457 0 None -239 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cell membranes co-expressing RGS4 measured after 60 mins by scintillation counting analysisDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cell membranes co-expressing RGS4 measured after 60 mins by scintillation counting analysis
ChEMBL 387 8 0 4 4.3 c1ccc(Cc2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)cc1 10.1016/j.ejmech.2020.113041
CHEMBL4786308 182457 0 None -239 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cell membranes co-expressing RGS4 measured after 60 mins by scintillation counting analysisDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cell membranes co-expressing RGS4 measured after 60 mins by scintillation counting analysis
ChEMBL 387 8 0 4 4.3 c1ccc(Cc2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)cc1 10.1016/j.ejmech.2020.113041
95232163 163089 1 None -2 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 338 7 1 5 1.5 O[C@@H](COC[C@@H]1CCCO1)CN1CCN(c2ccccc2F)CC1 10.1021/acs.jmedchem.8b00718
CHEMBL4176800 163089 1 None -2 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 338 7 1 5 1.5 O[C@@H](COC[C@@H]1CCCO1)CN1CCN(c2ccccc2F)CC1 10.1021/acs.jmedchem.8b00718
44304304 170063 0 None -67 3 Human 6.4 pKi = 6.4 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 423 9 0 6 3.5 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)/C=C/c3cccnc3)cc2)CC1 10.1016/s0960-894x(02)00309-8
CHEMBL444307 170063 0 None -67 3 Human 6.4 pKi = 6.4 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 423 9 0 6 3.5 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)/C=C/c3cccnc3)cc2)CC1 10.1016/s0960-894x(02)00309-8
44335558 110070 0 None -43 4 Human 6.4 pKi = 6.4 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 334 6 0 3 4.7 CC1CCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)CC1 10.1016/s0960-894x(02)00648-0
CHEMBL323562 110070 0 None -43 4 Human 6.4 pKi = 6.4 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 334 6 0 3 4.7 CC1CCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)CC1 10.1016/s0960-894x(02)00648-0
3300652 69022 35 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 263 1 2 5 2.3 NC1=NC(c2ccccc2)n2c(nc3ccccc32)N1 10.1021/jm2011589
CHEMBL1923523 69022 35 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 263 1 2 5 2.3 NC1=NC(c2ccccc2)n2c(nc3ccccc32)N1 10.1021/jm2011589
44304032 201487 0 None -95 3 Human 5.4 pKi = 5.4 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 413 11 0 6 3.7 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cnco3)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL60509 201487 0 None -95 3 Human 5.4 pKi = 5.4 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 413 11 0 6 3.7 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cnco3)CC2)cc1 10.1016/s0960-894x(02)00309-8
129103315 167122 0 None -5 6 Guinea pig 7.4 pKi = 7.4 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by liquid scintillation countingDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by liquid scintillation counting
ChEMBL 477 7 1 5 4.9 O=C1CCc2cc(C(O)CCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc3c2N1CC3 10.1021/acs.jmedchem.8b01096
CHEMBL4290311 167122 0 None -5 6 Guinea pig 7.4 pKi = 7.4 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by liquid scintillation countingDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by liquid scintillation counting
ChEMBL 477 7 1 5 4.9 O=C1CCc2cc(C(O)CCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc3c2N1CC3 10.1021/acs.jmedchem.8b01096
127041705 136676 0 None -1 5 Guinea pig 7.4 pKi = 7.4 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellumDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum
ChEMBL 525 5 0 5 5.3 O=S(=O)(c1ccc(C(F)(F)F)cc1)N1CCC(CN2CCC(c3noc4cc(F)ccc34)CC2)CC1 10.1039/C4MD00578C
CHEMBL3740256 136676 0 None -1 5 Guinea pig 7.4 pKi = 7.4 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellumDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum
ChEMBL 525 5 0 5 5.3 O=S(=O)(c1ccc(C(F)(F)F)cc1)N1CCC(CN2CCC(c3noc4cc(F)ccc34)CC2)CC1 10.1039/C4MD00578C
44267139 9371 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.
ChEMBL 382 1 0 3 4.3 COc1cnc2c(c1)CCc1cc(Cl)ccc1C2=C1CCN(C(C)=O)CC1 10.1016/S0960-894X(00)80290-5
CHEMBL11136 9371 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.
ChEMBL 382 1 0 3 4.3 COc1cnc2c(c1)CCc1cc(Cl)ccc1C2=C1CCN(C(C)=O)CC1 10.1016/S0960-894X(00)80290-5
44568347 191651 0 None -20 15 Human 6.4 pKi = 6.4 Binding
Antagonist activity at histamine H1 receptor (unknown origin) by PDSP assayAntagonist activity at histamine H1 receptor (unknown origin) by PDSP assay
ChEMBL 356 6 0 4 5.2 CCN(CC)CCCOC(=O)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
CHEMBL519609 191651 0 None -20 15 Human 6.4 pKi = 6.4 Binding
Antagonist activity at histamine H1 receptor (unknown origin) by PDSP assayAntagonist activity at histamine H1 receptor (unknown origin) by PDSP assay
ChEMBL 356 6 0 4 5.2 CCN(CC)CCCOC(=O)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
162655547 180796 0 None 20 5 Human 6.4 pKi = 6.4 Binding
Binding affinity to H1 receptor (unknown origin)Binding affinity to H1 receptor (unknown origin)
ChEMBL 306 4 0 2 3.8 CN(C)CCCN1C(=O)c2ccccc2/C=C\c2ccccc21 10.1016/j.bmcl.2020.127493
CHEMBL4756446 180796 0 None 20 5 Human 6.4 pKi = 6.4 Binding
Binding affinity to H1 receptor (unknown origin)Binding affinity to H1 receptor (unknown origin)
ChEMBL 306 4 0 2 3.8 CN(C)CCCN1C(=O)c2ccccc2/C=C\c2ccccc21 10.1016/j.bmcl.2020.127493
44334503 4995 0 None -281 3 Human 4.4 pKi = 4.4 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 349 9 3 6 0.2 CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@@H](N)CO)C2)cc1 10.1016/s0960-894x(02)00685-6
CHEMBL104994 4995 0 None -281 3 Human 4.4 pKi = 4.4 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 349 9 3 6 0.2 CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@@H](N)CO)C2)cc1 10.1016/s0960-894x(02)00685-6
44335407 171844 0 None -1 3 Human 6.4 pKi = 6.4 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 452 8 0 5 4.8 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(OC(F)(F)F)cc3)cc2)CC1 10.1016/s0960-894x(02)00648-0
CHEMBL446885 171844 0 None -1 3 Human 6.4 pKi = 6.4 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 452 8 0 5 4.8 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(OC(F)(F)F)cc3)cc2)CC1 10.1016/s0960-894x(02)00648-0
168280835 190722 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 818 20 6 8 3.8 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5182490 190722 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 818 20 6 8 3.8 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
168293792 192177 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 834 21 7 9 2.8 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5204037 192177 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 834 21 7 9 2.8 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
44304293 202962 0 None -15 3 Human 5.4 pKi = 5.4 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 491 10 1 6 4.0 N[C@H](Cc1cc2ccccc2s1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL63002 202962 0 None -15 3 Human 5.4 pKi = 5.4 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 491 10 1 6 4.0 N[C@H](Cc1cc2ccccc2s1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
168280835 190722 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 818 20 6 8 3.8 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5182490 190722 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 818 20 6 8 3.8 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
168293792 192177 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 834 21 7 9 2.8 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5204037 192177 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 834 21 7 9 2.8 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
44582678 181574 0 None -3 10 Human 6.4 pKi = 6.4 Binding
Inhibition of human cloned histamine H1 receptor by competitive binding experimentInhibition of human cloned histamine H1 receptor by competitive binding experiment
ChEMBL 401 9 1 4 4.3 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL476839 181574 0 None -3 10 Human 6.4 pKi = 6.4 Binding
Inhibition of human cloned histamine H1 receptor by competitive binding experimentInhibition of human cloned histamine H1 receptor by competitive binding experiment
ChEMBL 401 9 1 4 4.3 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
71937057 119575 3 None -1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 341 6 2 4 2.0 Cc1cccc(N2CCN(CCCNC(=O)c3cn[nH]c3C)CC2)c1 10.1021/acs.jmedchem.8b00718
CHEMBL3461530 119575 3 None -1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 341 6 2 4 2.0 Cc1cccc(N2CCN(CCCNC(=O)c3cn[nH]c3C)CC2)c1 10.1021/acs.jmedchem.8b00718
1353 1911 93 None -489 83 Human 6.4 pKi = 6.4 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.06.030
3559 1911 93 None -489 83 Human 6.4 pKi = 6.4 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.06.030
86 1911 93 None -489 83 Human 6.4 pKi = 6.4 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.06.030
CHEMBL54 1911 93 None -489 83 Human 6.4 pKi = 6.4 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.06.030
DB00502 1911 93 None -489 83 Human 6.4 pKi = 6.4 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.06.030
1353 1911 93 None -489 83 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation countingDisplacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.07.018
3559 1911 93 None -489 83 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation countingDisplacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.07.018
86 1911 93 None -489 83 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation countingDisplacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.07.018
CHEMBL54 1911 93 None -489 83 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation countingDisplacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.07.018
DB00502 1911 93 None -489 83 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation countingDisplacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.07.018
1353 1911 93 None -489 83 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]pyrilamine from human H1 receptor by liquid scintillation countingDisplacement of [3H]pyrilamine from human H1 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2011.12.019
3559 1911 93 None -489 83 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]pyrilamine from human H1 receptor by liquid scintillation countingDisplacement of [3H]pyrilamine from human H1 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2011.12.019
86 1911 93 None -489 83 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]pyrilamine from human H1 receptor by liquid scintillation countingDisplacement of [3H]pyrilamine from human H1 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2011.12.019
CHEMBL54 1911 93 None -489 83 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]pyrilamine from human H1 receptor by liquid scintillation countingDisplacement of [3H]pyrilamine from human H1 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2011.12.019
DB00502 1911 93 None -489 83 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]pyrilamine from human H1 receptor by liquid scintillation countingDisplacement of [3H]pyrilamine from human H1 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2011.12.019
44334781 5406 0 None -1513 3 Human 5.4 pKi = 5.4 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 458 11 1 6 3.1 COc1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1 10.1016/s0960-894x(02)00685-6
CHEMBL107162 5406 0 None -1513 3 Human 5.4 pKi = 5.4 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 458 11 1 6 3.1 COc1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1 10.1016/s0960-894x(02)00685-6
20659961 116095 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting method
ChEMBL 434 2 0 2 6.2 O=C(CC1CCCCC1)N1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/jm501086v
CHEMBL3357045 116095 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting method
ChEMBL 434 2 0 2 6.2 O=C(CC1CCCCC1)N1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/jm501086v
71449142 79518 0 None -7 3 Human 6.4 pKi = 6.4 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 442 9 0 6 4.2 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3ccc(SC)cc3)cc2)CC1 10.1016/s0960-894x(02)00309-8
CHEMBL2113738 79518 0 None -7 3 Human 6.4 pKi = 6.4 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 442 9 0 6 4.2 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3ccc(SC)cc3)cc2)CC1 10.1016/s0960-894x(02)00309-8
44335430 5297 0 None -1 3 Human 6.4 pKi = 6.4 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 374 7 0 5 4.0 CCOC(=O)N1CCN(CCCOc2ccc(-c3cccs3)cc2)CC1 10.1016/s0960-894x(02)00648-0
CHEMBL106602 5297 0 None -1 3 Human 6.4 pKi = 6.4 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 374 7 0 5 4.0 CCOC(=O)N1CCN(CCCOc2ccc(-c3cccs3)cc2)CC1 10.1016/s0960-894x(02)00648-0
9880208 4924 0 None -537 4 Human 5.4 pKi = 5.4 Binding
Binding affinity at human cortical Histamine 1 receptorBinding affinity at human cortical Histamine 1 receptor
ChEMBL 322 6 1 4 3.1 N#Cc1ccc(-c2ccc(OCCCN3CC[C@@H](O)C3)cc2)cc1 10.1016/s0960-894x(02)00648-0
CHEMBL104669 4924 0 None -537 4 Human 5.4 pKi = 5.4 Binding
Binding affinity at human cortical Histamine 1 receptorBinding affinity at human cortical Histamine 1 receptor
ChEMBL 322 6 1 4 3.1 N#Cc1ccc(-c2ccc(OCCCN3CC[C@@H](O)C3)cc2)cc1 10.1016/s0960-894x(02)00648-0
164622153 185568 0 None -95 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 394 6 4 4 3.0 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(Cl)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4863347 185568 0 None -95 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 394 6 4 4 3.0 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(Cl)cc1 10.1016/j.ejmech.2021.113190
164610824 185110 0 None -30 4 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 452 8 4 4 3.6 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NCC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4856200 185110 0 None -30 4 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 452 8 4 4 3.6 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NCC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
44334025 4547 0 None -1202 3 Human 5.4 pKi = 5.4 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 462 10 1 5 3.8 O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccccc3Cl)C2)cc1)C1CC1 10.1016/s0960-894x(02)00685-6
CHEMBL102384 4547 0 None -1202 3 Human 5.4 pKi = 5.4 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 462 10 1 5 3.8 O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccccc3Cl)C2)cc1)C1CC1 10.1016/s0960-894x(02)00685-6
44304223 200389 0 None -48 3 Human 6.3 pKi = 6.3 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 374 12 0 4 4.5 CCCCCC(=O)c1ccc(OCCCN2CCN(CC(C)C)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL59798 200389 0 None -48 3 Human 6.3 pKi = 6.3 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 374 12 0 4 4.5 CCCCCC(=O)c1ccc(OCCCN2CCN(CC(C)C)CC2)cc1 10.1016/s0960-894x(02)00309-8
57390225 67882 0 None -53 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
ChEMBL 469 9 2 5 4.1 COc1ccc(CN(CCN[C@H]2CCN(C(=O)c3cc4ccccc4[nH]3)C2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
CHEMBL1910384 67882 0 None -53 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
ChEMBL 469 9 2 5 4.1 COc1ccc(CN(CCN[C@H]2CCN(C(=O)c3cc4ccccc4[nH]3)C2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
44304049 102138 0 None -165 3 Human 5.3 pKi = 5.3 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 421 9 1 5 2.9 N[C@@H](C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1)c1ccccc1 10.1016/s0960-894x(02)00310-4
CHEMBL302468 102138 0 None -165 3 Human 5.3 pKi = 5.3 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 421 9 1 5 2.9 N[C@@H](C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1)c1ccccc1 10.1016/s0960-894x(02)00310-4
17156312 69030 14 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 215 4 1 2 3.4 CC(C)NCc1ccc(-c2ccccc2)o1 10.1021/jm2011589
CHEMBL1923532 69030 14 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 215 4 1 2 3.4 CC(C)NCc1ccc(-c2ccccc2)o1 10.1021/jm2011589
44304003 203134 0 None -1584 3 Human 4.3 pKi = 4.3 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 384 9 1 6 1.4 N#CC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL64124 203134 0 None -1584 3 Human 4.3 pKi = 4.3 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 384 9 1 6 1.4 N#CC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
164609493 184436 0 None -2630 6 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 350 6 4 5 1.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccco1 10.1016/j.ejmech.2021.113190
CHEMBL4846380 184436 0 None -2630 6 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 350 6 4 5 1.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccco1 10.1016/j.ejmech.2021.113190
162676676 183589 0 None -223 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cell membranes co-expressing RGS4 measured after 60 mins by scintillation counting analysisDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cell membranes co-expressing RGS4 measured after 60 mins by scintillation counting analysis
ChEMBL 389 8 0 5 4.5 c1ccc(Oc2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)cc1 10.1016/j.ejmech.2020.113041
CHEMBL4800672 183589 0 None -223 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cell membranes co-expressing RGS4 measured after 60 mins by scintillation counting analysisDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cell membranes co-expressing RGS4 measured after 60 mins by scintillation counting analysis
ChEMBL 389 8 0 5 4.5 c1ccc(Oc2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)cc1 10.1016/j.ejmech.2020.113041
60165681 75356 0 None -1 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]Pyrilamine from human H1 histamine receptor by liquid scintillation assayDisplacement of [3H]Pyrilamine from human H1 histamine receptor by liquid scintillation assay
ChEMBL 413 7 0 5 5.1 O=C(CCCCN1CCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL2037528 75356 0 None -1 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]Pyrilamine from human H1 histamine receptor by liquid scintillation assayDisplacement of [3H]Pyrilamine from human H1 histamine receptor by liquid scintillation assay
ChEMBL 413 7 0 5 5.1 O=C(CCCCN1CCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
2389 3331 118 None -52 67 Guinea pig 7.3 pKi = 7.3 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by liquid scintillation countingDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by liquid scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/acs.jmedchem.8b01096
5073 3331 118 None -52 67 Guinea pig 7.3 pKi = 7.3 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by liquid scintillation countingDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by liquid scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/acs.jmedchem.8b01096
96 3331 118 None -52 67 Guinea pig 7.3 pKi = 7.3 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by liquid scintillation countingDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by liquid scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/acs.jmedchem.8b01096
CHEMBL85 3331 118 None -52 67 Guinea pig 7.3 pKi = 7.3 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by liquid scintillation countingDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by liquid scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/acs.jmedchem.8b01096
DB00734 3331 118 None -52 67 Guinea pig 7.3 pKi = 7.3 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by liquid scintillation countingDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by liquid scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/acs.jmedchem.8b01096
44324737 207238 0 None -158 5 Human 6.3 pKi = 6.3 Binding
Inhibition of [3H]pyrilamine binding to Histamine H1 receptorInhibition of [3H]pyrilamine binding to Histamine H1 receptor
ChEMBL 473 6 0 7 3.8 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(Cc4ccc5ccccc5c4)CC3)[C@@H]1CO2 10.1021/jm049619s
CHEMBL92860 207238 0 None -158 5 Human 6.3 pKi = 6.3 Binding
Inhibition of [3H]pyrilamine binding to Histamine H1 receptorInhibition of [3H]pyrilamine binding to Histamine H1 receptor
ChEMBL 473 6 0 7 3.8 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(Cc4ccc5ccccc5c4)CC3)[C@@H]1CO2 10.1021/jm049619s
53326725 57758 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 327 5 0 3 3.4 FC1(F)CN(CCC2=C(Cc3cnccn3)c3ccccc3C2)C1 10.1016/j.bmcl.2010.12.053
CHEMBL1669415 57758 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 327 5 0 3 3.4 FC1(F)CN(CCC2=C(Cc3cnccn3)c3ccccc3C2)C1 10.1016/j.bmcl.2010.12.053
118721934 116096 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting method
ChEMBL 423 3 1 3 4.6 CC(C)C[C@@H](N)C(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/jm501086v
CHEMBL3357049 116096 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting method
ChEMBL 423 3 1 3 4.6 CC(C)C[C@@H](N)C(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/jm501086v
44304320 163274 0 None -1862 3 Human 5.3 pKi = 5.3 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 373 9 1 5 1.9 CC[C@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL418666 163274 0 None -1862 3 Human 5.3 pKi = 5.3 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 373 9 1 5 1.9 CC[C@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
44304449 200499 0 None -323 3 Human 5.3 pKi = 5.3 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 531 14 1 6 5.3 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](CC(C)C)NC(=O)OC(C)(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
CHEMBL59870 200499 0 None -323 3 Human 5.3 pKi = 5.3 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 531 14 1 6 5.3 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](CC(C)C)NC(=O)OC(C)(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
44304348 100602 0 None -11748 3 Human 4.3 pKi = 4.3 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 387 10 1 5 2.3 CCC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL291821 100602 0 None -11748 3 Human 4.3 pKi = 4.3 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 387 10 1 5 2.3 CCC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
44304056 102724 1 None -5370 3 Human 4.3 pKi = 4.3 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 401 10 1 5 2.6 CC(C)N[C@H](C)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL304888 102724 1 None -5370 3 Human 4.3 pKi = 4.3 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 401 10 1 5 2.6 CC(C)N[C@H](C)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
44304462 202882 0 None -6606 3 Human 4.3 pKi = 4.3 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 405 12 2 6 1.7 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](N)CO)CC2)cc1 10.1016/s0960-894x(02)00310-4
CHEMBL62660 202882 0 None -6606 3 Human 4.3 pKi = 4.3 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 405 12 2 6 1.7 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](N)CO)CC2)cc1 10.1016/s0960-894x(02)00310-4
44304316 203133 0 None -389 3 Human 4.3 pKi = 4.3 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 485 8 0 6 3.6 CC(C)(C)OC(=O)N1CCC[C@@H]1C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL64120 203133 0 None -389 3 Human 4.3 pKi = 4.3 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 485 8 0 6 3.6 CC(C)(C)OC(=O)N1CCC[C@@H]1C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
1278 2150 84 None -1778 8 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.09.001
1279 2150 84 None -1778 8 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.09.001
4908365 2150 84 None -1778 8 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.09.001
CHEMBL129198 2150 84 None -1778 8 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.09.001
164610289 185133 0 None -77 4 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 438 7 4 4 3.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4856602 185133 0 None -77 4 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 438 7 4 4 3.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
2865 4143 73 None -58 53 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmc.2008.06.030
59 4143 73 None -58 53 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmc.2008.06.030
60854 4143 73 None -58 53 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmc.2008.06.030
CHEMBL708 4143 73 None -58 53 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmc.2008.06.030
DB00246 4143 73 None -58 53 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmc.2008.06.030
10411944 22228 0 None - 1 Guinea pig 7.3 pKi = 7.3 Binding
Inhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptorInhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptor
ChEMBL 460 6 1 5 4.9 O=C(O)c1ccc2c(c1)C(SCCN1CCN(c3ccccc3)CC1)c1ccccc1CO2 10.1021/jm00055a013
CHEMBL132311 22228 0 None - 1 Guinea pig 7.3 pKi = 7.3 Binding
Inhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptorInhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptor
ChEMBL 460 6 1 5 4.9 O=C(O)c1ccc2c(c1)C(SCCN1CCN(c3ccccc3)CC1)c1ccccc1CO2 10.1021/jm00055a013
44326124 106955 0 None 1 3 Human 7.3 pKi = 7.3 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 427 3 0 3 6.6 c1ccc(C2CCN(CC3C[C@@H]4c5ccccc5Sc5ccccc5[C@H]4O3)CC2)cc1 10.1016/j.bmcl.2004.03.069
CHEMBL314968 106955 0 None 1 3 Human 7.3 pKi = 7.3 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 427 3 0 3 6.6 c1ccc(C2CCN(CC3C[C@@H]4c5ccccc5Sc5ccccc5[C@H]4O3)CC2)cc1 10.1016/j.bmcl.2004.03.069
73213195 104459 0 None -1 12 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)
ChEMBL 288 0 0 2 3.6 CN1CCc2c(c3cccc4c3n2Cc2ccccc2C4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104092 104459 0 None -1 12 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)
ChEMBL 288 0 0 2 3.6 CN1CCc2c(c3cccc4c3n2Cc2ccccc2C4)C1 10.1016/j.bmcl.2013.12.024
44326219 207158 0 None -8 3 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 444 3 0 3 5.7 Clc1cccc(N2CCN(CC3C[C@@H]4c5ccccc5Cc5ccccc5[C@H]4O3)CC2)c1 10.1016/j.bmcl.2004.03.069
CHEMBL92333 207158 0 None -8 3 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 444 3 0 3 5.7 Clc1cccc(N2CCN(CC3C[C@@H]4c5ccccc5Cc5ccccc5[C@H]4O3)CC2)c1 10.1016/j.bmcl.2004.03.069
73355415 92533 0 None -23 13 Human 5.3 pKi = 5.3 Binding
Inhibition of histamine H1 receptor (unknown origin) by PDSP assayInhibition of histamine H1 receptor (unknown origin) by PDSP assay
ChEMBL 277 3 1 1 2.1 C1C2C3CC4C2C2C1C3[C@H](NCC13C5C6C7C5C1C7C63)C42 10.1016/j.bmc.2013.07.045
CHEMBL2432039 92533 0 None -23 13 Human 5.3 pKi = 5.3 Binding
Inhibition of histamine H1 receptor (unknown origin) by PDSP assayInhibition of histamine H1 receptor (unknown origin) by PDSP assay
ChEMBL 277 3 1 1 2.1 C1C2C3CC4C2C2C1C3[C@H](NCC13C5C6C7C5C1C7C63)C42 10.1016/j.bmc.2013.07.045
44304269 100544 0 None -75 3 Human 6.3 pKi = 6.3 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 423 11 0 5 4.1 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccncc3)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL291394 100544 0 None -75 3 Human 6.3 pKi = 6.3 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 423 11 0 5 4.1 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccncc3)CC2)cc1 10.1016/s0960-894x(02)00309-8
53325600 57763 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 376 7 0 5 4.6 C[C@H](C1=C(CCN(C)Cc2nccs2)Cc2ccccc21)c1cnccn1 10.1016/j.bmcl.2010.12.053
CHEMBL1669420 57763 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 376 7 0 5 4.6 C[C@H](C1=C(CCN(C)Cc2nccs2)Cc2ccccc21)c1cnccn1 10.1016/j.bmcl.2010.12.053
14554129 10535 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 366 1 0 2 4.7 CCC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/jm00105a069
CHEMBL116935 10535 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 366 1 0 2 4.7 CCC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/jm00105a069
46929648 16759 0 None 3 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 355 5 2 3 4.3 FC(F)(F)c1ccc(SC[C@@H](c2c[nH]cn2)C2CCNCC2)cc1 10.1021/jm100643t
CHEMBL1243395 16759 0 None 3 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 355 5 2 3 4.3 FC(F)(F)c1ccc(SC[C@@H](c2c[nH]cn2)C2CCNCC2)cc1 10.1021/jm100643t
73213195 104459 0 None -1 12 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)
ChEMBL 288 0 0 2 3.6 CN1CCc2c(c3cccc4c3n2Cc2ccccc2C4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104092 104459 0 None -1 12 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)
ChEMBL 288 0 0 2 3.6 CN1CCc2c(c3cccc4c3n2Cc2ccccc2C4)C1 10.1016/j.bmcl.2013.12.024
44521012 199979 0 None 1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cellsDisplacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cells
ChEMBL 237 3 1 1 3.3 CNCCC1c2ccccc2Cc2ccccc21 10.1016/j.bmc.2009.08.016
CHEMBL595158 199979 0 None 1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cellsDisplacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cells
ChEMBL 237 3 1 1 3.3 CNCCC1c2ccccc2Cc2ccccc21 10.1016/j.bmc.2009.08.016
133 2496 52 None -102 42 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
1723 2496 52 None -102 42 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
28693 2496 52 None -102 42 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
CHEMBL19215 2496 52 None -102 42 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
DB13520 2496 52 None -102 42 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
132060743 162236 0 None -1 13 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-Pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 351 3 0 4 3.1 CN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)C3)CC1 10.1016/j.ejmech.2018.02.024
CHEMBL4163428 162236 0 None -1 13 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-Pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 351 3 0 4 3.1 CN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)C3)CC1 10.1016/j.ejmech.2018.02.024
164620704 186083 0 None -33 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 416 8 4 4 3.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)c1ccc(C(C)C)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4871482 186083 0 None -33 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 416 8 4 4 3.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)c1ccc(C(C)C)cc1 10.1016/j.ejmech.2021.113190
44343626 114149 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 341 1 0 3 2.7 CN1CCN(C2c3ccc(Cl)cc3CCc3cccnc32)CC1=O 10.1016/s0960-894x(98)00626-x
CHEMBL332936 114149 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 341 1 0 3 2.7 CN1CCN(C2c3ccc(Cl)cc3CCc3cccnc32)CC1=O 10.1016/s0960-894x(98)00626-x
53321512 57757 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 309 5 0 3 3.1 FC1CN(CCC2=C(Cc3cnccn3)c3ccccc3C2)C1 10.1016/j.bmcl.2010.12.053
CHEMBL1669414 57757 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 309 5 0 3 3.1 FC1CN(CCC2=C(Cc3cnccn3)c3ccccc3C2)C1 10.1016/j.bmcl.2010.12.053
71459761 84080 0 None -81 7 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis
ChEMBL 540 7 0 5 6.1 COc1ccccc1N1CCN(Cc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207642 84080 0 None -81 7 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis
ChEMBL 540 7 0 5 6.1 COc1ccccc1N1CCN(Cc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
10326069 39296 1 None -27 9 Human 6.3 pKi = 6.3 Binding
Binding affinity for recombinant human Histamine H1 receptor using [3H]pyrilamine as radioligand.Binding affinity for recombinant human Histamine H1 receptor using [3H]pyrilamine as radioligand.
ChEMBL 589 10 3 8 3.3 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980506g
CHEMBL147077 39296 1 None -27 9 Human 6.3 pKi = 6.3 Binding
Binding affinity for recombinant human Histamine H1 receptor using [3H]pyrilamine as radioligand.Binding affinity for recombinant human Histamine H1 receptor using [3H]pyrilamine as radioligand.
ChEMBL 589 10 3 8 3.3 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980506g
25055258 12056 0 None - 1 Guinea pig 8.3 pKi = 8.3 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 349 4 1 3 4.2 O=C(O)c1ccc2c(c1)/C(=C\CCN1CCCC1)c1ccccc1CO2 10.1021/jm00089a020
CHEMBL1183550 12056 0 None - 1 Guinea pig 8.3 pKi = 8.3 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 349 4 1 3 4.2 O=C(O)c1ccc2c(c1)/C(=C\CCN1CCCC1)c1ccccc1CO2 10.1021/jm00089a020
CHEMBL304223 12056 0 None - 1 Guinea pig 8.3 pKi = 8.3 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 349 4 1 3 4.2 O=C(O)c1ccc2c(c1)/C(=C\CCN1CCCC1)c1ccccc1CO2 10.1021/jm00089a020
135398737 958 93 None -4 89 Rat 8.3 pKi = 8.3 Binding
Compound was tested for the binding affinity against rat cortical H1 receptor by radioligand [3H]-pyrilamine binding assay.Compound was tested for the binding affinity against rat cortical H1 receptor by radioligand [3H]-pyrilamine binding assay.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9601720
38 958 93 None -4 89 Rat 8.3 pKi = 8.3 Binding
Compound was tested for the binding affinity against rat cortical H1 receptor by radioligand [3H]-pyrilamine binding assay.Compound was tested for the binding affinity against rat cortical H1 receptor by radioligand [3H]-pyrilamine binding assay.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9601720
722 958 93 None -4 89 Rat 8.3 pKi = 8.3 Binding
Compound was tested for the binding affinity against rat cortical H1 receptor by radioligand [3H]-pyrilamine binding assay.Compound was tested for the binding affinity against rat cortical H1 receptor by radioligand [3H]-pyrilamine binding assay.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9601720
CHEMBL42 958 93 None -4 89 Rat 8.3 pKi = 8.3 Binding
Compound was tested for the binding affinity against rat cortical H1 receptor by radioligand [3H]-pyrilamine binding assay.Compound was tested for the binding affinity against rat cortical H1 receptor by radioligand [3H]-pyrilamine binding assay.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9601720
DB00363 958 93 None -4 89 Rat 8.3 pKi = 8.3 Binding
Compound was tested for the binding affinity against rat cortical H1 receptor by radioligand [3H]-pyrilamine binding assay.Compound was tested for the binding affinity against rat cortical H1 receptor by radioligand [3H]-pyrilamine binding assay.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9601720
49782998 17917 0 None -31 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cellsDisplacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 409 4 1 4 4.0 CC(C)C(=O)NCc1ccc2c(c1)[C@@H](N1CCN(C)CC1)Cc1ccccc1S2 10.1021/jm100652h
CHEMBL1259190 17917 0 None -31 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cellsDisplacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 409 4 1 4 4.0 CC(C)C(=O)NCc1ccc2c(c1)[C@@H](N1CCN(C)CC1)Cc1ccccc1S2 10.1021/jm100652h
46884120 8056 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 340 6 0 4 4.6 COc1cccnc1[C@H](C)c1c(CCN(C)C)sc2ccccc12 10.1016/j.bmcl.2010.01.134
CHEMBL1091069 8056 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 340 6 0 4 4.6 COc1cccnc1[C@H](C)c1c(CCN(C)C)sc2ccccc12 10.1016/j.bmcl.2010.01.134
44389293 128805 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for human Histamine H1 receptor in CHO K1 cellsBinding affinity for human Histamine H1 receptor in CHO K1 cells
ChEMBL 577 11 1 6 5.7 COC(=O)N(O)CCC#Cc1ccc(OCCCCN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2004.12.023
CHEMBL366925 128805 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for human Histamine H1 receptor in CHO K1 cellsBinding affinity for human Histamine H1 receptor in CHO K1 cells
ChEMBL 577 11 1 6 5.7 COC(=O)N(O)CCC#Cc1ccc(OCCCCN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2004.12.023
CHEMBL5272464 194625 0 None 11 3 Human 8.3 pKi = 8.3 Binding
Antagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysisAntagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysis
ChEMBL 480 10 1 5 4.4 CCCNC(=O)CCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
CHEMBL5315453 194625 0 None 11 3 Human 8.3 pKi = 8.3 Binding
Antagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysisAntagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysis
ChEMBL 480 10 1 5 4.4 CCCNC(=O)CCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1021/acsmedchemlett.7b00112
69260946 81294 1 None 19 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 462 6 1 4 5.5 O=C(O)c1cccc(N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.103
CHEMBL2158823 81294 1 None 19 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 462 6 1 4 5.5 O=C(O)c1cccc(N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.103
69274365 81297 1 None 7 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 476 7 1 4 5.4 O=C(O)Cc1cccc(N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.103
CHEMBL2158826 81297 1 None 7 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 476 7 1 4 5.4 O=C(O)Cc1cccc(N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.103
71449585 81300 0 None 7 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 492 8 1 5 5.2 O=C(O)COc1cccc(N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.103
CHEMBL2158829 81300 0 None 7 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 492 8 1 5 5.2 O=C(O)COc1cccc(N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.103
59295969 84017 0 None -1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 608 10 4 7 2.9 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c(=O)c2cc(S(=O)(=O)NC3CC3)ccc12 10.1016/j.bmcl.2012.09.112
CHEMBL2207285 84017 0 None -1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 608 10 4 7 2.9 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c(=O)c2cc(S(=O)(=O)NC3CC3)ccc12 10.1016/j.bmcl.2012.09.112
71454296 84095 0 None -1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 521 7 2 6 3.3 Cn1cc(C(=O)NC[C@@H](O)CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)c(C(F)(F)F)cc1=O 10.1016/j.bmcl.2012.09.112
CHEMBL2207665 84095 0 None -1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 521 7 2 6 3.3 Cn1cc(C(=O)NC[C@@H](O)CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)c(C(F)(F)F)cc1=O 10.1016/j.bmcl.2012.09.112
155521446 170583 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 402 2 0 4 4.7 Clc1ccc2c(c1)CCc1cccnc1C2=C1CCN(Cc2ccncn2)CC1 10.1021/acs.jmedchem.9b00447
CHEMBL4450560 170583 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 402 2 0 4 4.7 Clc1ccc2c(c1)CCc1cccnc1C2=C1CCN(Cc2ccncn2)CC1 10.1021/acs.jmedchem.9b00447
10069660 206908 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 401 2 0 3 5.3 Clc1ccc2c(c1)CCc1cccnc1C2=C1CCN(Cc2cccnc2)CC1 10.1021/acs.jmedchem.9b00447
CHEMBL90893 206908 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 401 2 0 3 5.3 Clc1ccc2c(c1)CCc1cccnc1C2=C1CCN(Cc2cccnc2)CC1 10.1021/acs.jmedchem.9b00447
28125512 203423 25 None - 1 Guinea pig 8.3 pKi = 8.3 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 337 5 1 3 3.6 CN(C)CC/C=C1\c2ccccc2COc2ccc(CC(=O)O)cc21 10.1021/jm00089a020
5284599 203423 25 None - 1 Guinea pig 8.3 pKi = 8.3 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 337 5 1 3 3.6 CN(C)CC/C=C1\c2ccccc2COc2ccc(CC(=O)O)cc21 10.1021/jm00089a020
CHEMBL65699 203423 25 None - 1 Guinea pig 8.3 pKi = 8.3 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 337 5 1 3 3.6 CN(C)CC/C=C1\c2ccccc2COc2ccc(CC(=O)O)cc21 10.1021/jm00089a020
46884202 8202 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 316 5 0 4 4.6 C[C@@H](c1cncs1)c1c(CCN(C)C)sc2ccccc12 10.1016/j.bmcl.2010.01.134
CHEMBL1092118 8202 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 316 5 0 4 4.6 C[C@@H](c1cncs1)c1c(CCN(C)C)sc2ccccc12 10.1016/j.bmcl.2010.01.134
2865 4143 73 None -58 53 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human histamine H1 receptorBinding affinity towards human histamine H1 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm030480f
59 4143 73 None -58 53 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human histamine H1 receptorBinding affinity towards human histamine H1 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm030480f
60854 4143 73 None -58 53 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human histamine H1 receptorBinding affinity towards human histamine H1 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm030480f
CHEMBL708 4143 73 None -58 53 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human histamine H1 receptorBinding affinity towards human histamine H1 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm030480f
DB00246 4143 73 None -58 53 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human histamine H1 receptorBinding affinity towards human histamine H1 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm030480f
49836528 18658 0 None 5 5 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]pyrilamine from histamine H1 receptor in Sprague-Dawley rat cortical membrane by liquid scintillation countingDisplacement of [3H]pyrilamine from histamine H1 receptor in Sprague-Dawley rat cortical membrane by liquid scintillation counting
ChEMBL 373 2 1 2 4.0 O=C(O)[C@]12C[C@H]1CN(C1CC[C@]3(Cc4ccccc4Cc4ccccc43)C1)C2 10.1021/jm100856p
CHEMBL1276947 18658 0 None 5 5 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]pyrilamine from histamine H1 receptor in Sprague-Dawley rat cortical membrane by liquid scintillation countingDisplacement of [3H]pyrilamine from histamine H1 receptor in Sprague-Dawley rat cortical membrane by liquid scintillation counting
ChEMBL 373 2 1 2 4.0 O=C(O)[C@]12C[C@H]1CN(C1CC[C@]3(Cc4ccccc4Cc4ccccc43)C1)C2 10.1021/jm100856p
57393730 67884 0 None -1 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
ChEMBL 579 8 2 6 5.0 O=C(c1cc2ccccc2[nH]1)N1CCN(CCN2CCC(Nc3nc4ccccc4n3Cc3ccc(F)cc3)CC2)CC1 10.1016/j.bmcl.2011.09.001
CHEMBL1910386 67884 0 None -1 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
ChEMBL 579 8 2 6 5.0 O=C(c1cc2ccccc2[nH]1)N1CCN(CCN2CCC(Nc3nc4ccccc4n3Cc3ccc(F)cc3)CC2)CC1 10.1016/j.bmcl.2011.09.001
1210 918 51 None -9 21 Rat 8.3 pKi = 8.3 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/s0960-894x(98)00626-x
1213 918 51 None -9 21 Rat 8.3 pKi = 8.3 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/s0960-894x(98)00626-x
2725 918 51 None -9 21 Rat 8.3 pKi = 8.3 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/s0960-894x(98)00626-x
33036 918 51 None -9 21 Rat 8.3 pKi = 8.3 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/s0960-894x(98)00626-x
4411 918 51 None -9 21 Rat 8.3 pKi = 8.3 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/s0960-894x(98)00626-x
616 918 51 None -9 21 Rat 8.3 pKi = 8.3 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/s0960-894x(98)00626-x
6976 918 51 None -9 21 Rat 8.3 pKi = 8.3 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/s0960-894x(98)00626-x
716121 918 51 None -9 21 Rat 8.3 pKi = 8.3 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/s0960-894x(98)00626-x
CHEMBL1201353 918 51 None -9 21 Rat 8.3 pKi = 8.3 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/s0960-894x(98)00626-x
CHEMBL1554789 918 51 None -9 21 Rat 8.3 pKi = 8.3 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/s0960-894x(98)00626-x
CHEMBL505 918 51 None -9 21 Rat 8.3 pKi = 8.3 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/s0960-894x(98)00626-x
DB01114 918 51 None -9 21 Rat 8.3 pKi = 8.3 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/s0960-894x(98)00626-x
DB13679 918 51 None -9 21 Rat 8.3 pKi = 8.3 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1016/s0960-894x(98)00626-x
1210 918 51 None -9 21 Rat 8.3 pKi = 8.3 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm00105a069
1213 918 51 None -9 21 Rat 8.3 pKi = 8.3 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm00105a069
2725 918 51 None -9 21 Rat 8.3 pKi = 8.3 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm00105a069
33036 918 51 None -9 21 Rat 8.3 pKi = 8.3 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm00105a069
4411 918 51 None -9 21 Rat 8.3 pKi = 8.3 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm00105a069
616 918 51 None -9 21 Rat 8.3 pKi = 8.3 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm00105a069
6976 918 51 None -9 21 Rat 8.3 pKi = 8.3 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm00105a069
716121 918 51 None -9 21 Rat 8.3 pKi = 8.3 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm00105a069
CHEMBL1201353 918 51 None -9 21 Rat 8.3 pKi = 8.3 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm00105a069
CHEMBL1554789 918 51 None -9 21 Rat 8.3 pKi = 8.3 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm00105a069
CHEMBL505 918 51 None -9 21 Rat 8.3 pKi = 8.3 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm00105a069
DB01114 918 51 None -9 21 Rat 8.3 pKi = 8.3 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm00105a069
DB13679 918 51 None -9 21 Rat 8.3 pKi = 8.3 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm00105a069
135398745 2914 112 None 1 65 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human H1 receptorBinding affinity towards human H1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm0002432
47 2914 112 None 1 65 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human H1 receptorBinding affinity towards human H1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm0002432
CHEMBL715 2914 112 None 1 65 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human H1 receptorBinding affinity towards human H1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm0002432
DB00334 2914 112 None 1 65 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human H1 receptorBinding affinity towards human H1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm0002432
49836633 18659 0 None 1 5 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]pyrilamine from histamine H1 receptor in Sprague-Dawley rat cortical membrane by liquid scintillation countingDisplacement of [3H]pyrilamine from histamine H1 receptor in Sprague-Dawley rat cortical membrane by liquid scintillation counting
ChEMBL 347 2 1 2 3.6 O=C(O)C1CN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
CHEMBL1276948 18659 0 None 1 5 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]pyrilamine from histamine H1 receptor in Sprague-Dawley rat cortical membrane by liquid scintillation countingDisplacement of [3H]pyrilamine from histamine H1 receptor in Sprague-Dawley rat cortical membrane by liquid scintillation counting
ChEMBL 347 2 1 2 3.6 O=C(O)C1CN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
15749431 100995 0 None - 1 Guinea pig 8.2 pKi = 8.2 Binding
The compound was tested in vitro for binding affinity against histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMThe compound was tested in vitro for binding affinity against histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 337 5 1 3 4.1 CN(C)CCC/C=C1/c2ccccc2COc2ccc(C(=O)O)cc21 10.1021/jm00089a020
CHEMBL294345 100995 0 None - 1 Guinea pig 8.2 pKi = 8.2 Binding
The compound was tested in vitro for binding affinity against histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMThe compound was tested in vitro for binding affinity against histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 337 5 1 3 4.1 CN(C)CCC/C=C1/c2ccccc2COc2ccc(C(=O)O)cc21 10.1021/jm00089a020
1971 2866 38 None -1 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
2404 2866 38 None -1 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
4543 2866 38 None -1 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
CHEMBL445 2866 38 None -1 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
DB00540 2866 38 None -1 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
1222 881 0 None -1 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Histamine H1 receptor in CHO K1 cellsBinding affinity for human Histamine H1 receptor in CHO K1 cells
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1016/j.bmcl.2004.12.023
2678 881 0 None -1 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Histamine H1 receptor in CHO K1 cellsBinding affinity for human Histamine H1 receptor in CHO K1 cells
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1016/j.bmcl.2004.12.023
581 881 0 None -1 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Histamine H1 receptor in CHO K1 cellsBinding affinity for human Histamine H1 receptor in CHO K1 cells
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1016/j.bmcl.2004.12.023
CHEMBL1000 881 0 None -1 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Histamine H1 receptor in CHO K1 cellsBinding affinity for human Histamine H1 receptor in CHO K1 cells
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1016/j.bmcl.2004.12.023
DB00341 881 0 None -1 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Histamine H1 receptor in CHO K1 cellsBinding affinity for human Histamine H1 receptor in CHO K1 cells
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1016/j.bmcl.2004.12.023
11376787 63380 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Histamine H1 receptor in CHO K1 cellsBinding affinity for human Histamine H1 receptor in CHO K1 cells
ChEMBL 591 12 1 6 6.1 CCOC(=O)N(O)CCC#Cc1ccc(OCCCCN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2004.12.023
CHEMBL179590 63380 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Histamine H1 receptor in CHO K1 cellsBinding affinity for human Histamine H1 receptor in CHO K1 cells
ChEMBL 591 12 1 6 6.1 CCOC(=O)N(O)CCC#Cc1ccc(OCCCCN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2004.12.023
1214 2068 54 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for H1 histamine receptor expressed in CHO cellsBinding affinity for H1 histamine receptor expressed in CHO cells
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)[C@@H](c1ccc(cc1)Cl)c1ccccc1 10.1021/jm049495j
1549000 2068 54 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for H1 histamine receptor expressed in CHO cellsBinding affinity for H1 histamine receptor expressed in CHO cells
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)[C@@H](c1ccc(cc1)Cl)c1ccccc1 10.1021/jm049495j
1566 2068 54 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for H1 histamine receptor expressed in CHO cellsBinding affinity for H1 histamine receptor expressed in CHO cells
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)[C@@H](c1ccc(cc1)Cl)c1ccccc1 10.1021/jm049495j
28145931 2068 54 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for H1 histamine receptor expressed in CHO cellsBinding affinity for H1 histamine receptor expressed in CHO cells
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)[C@@H](c1ccc(cc1)Cl)c1ccccc1 10.1021/jm049495j
CHEMBL1201191 2068 54 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for H1 histamine receptor expressed in CHO cellsBinding affinity for H1 histamine receptor expressed in CHO cells
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)[C@@H](c1ccc(cc1)Cl)c1ccccc1 10.1021/jm049495j
DB06282 2068 54 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for H1 histamine receptor expressed in CHO cellsBinding affinity for H1 histamine receptor expressed in CHO cells
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)[C@@H](c1ccc(cc1)Cl)c1ccccc1 10.1021/jm049495j
2865 4143 73 None -58 53 Human 7.3 pKi = 7.3 Binding
Binding affinity to H1 histamine receptor (unknown origin)Binding affinity to H1 histamine receptor (unknown origin)
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmcl.2020.127681
59 4143 73 None -58 53 Human 7.3 pKi = 7.3 Binding
Binding affinity to H1 histamine receptor (unknown origin)Binding affinity to H1 histamine receptor (unknown origin)
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmcl.2020.127681
60854 4143 73 None -58 53 Human 7.3 pKi = 7.3 Binding
Binding affinity to H1 histamine receptor (unknown origin)Binding affinity to H1 histamine receptor (unknown origin)
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmcl.2020.127681
CHEMBL708 4143 73 None -58 53 Human 7.3 pKi = 7.3 Binding
Binding affinity to H1 histamine receptor (unknown origin)Binding affinity to H1 histamine receptor (unknown origin)
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmcl.2020.127681
DB00246 4143 73 None -58 53 Human 7.3 pKi = 7.3 Binding
Binding affinity to H1 histamine receptor (unknown origin)Binding affinity to H1 histamine receptor (unknown origin)
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmcl.2020.127681
12992629 122599 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human histamine H1 receptor expressed in CHO-K1 cellsBinding affinity towards human histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 584 8 2 5 6.1 NC(=O)N(O)CCC#Cc1ccc(OCCCCN2CCC(=C3c4ccc(Cl)cc4CCc4cccnc43)CC2)cc1 10.1016/j.bmcl.2004.08.060
CHEMBL360202 122599 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human histamine H1 receptor expressed in CHO-K1 cellsBinding affinity towards human histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 584 8 2 5 6.1 NC(=O)N(O)CCC#Cc1ccc(OCCCCN2CCC(=C3c4ccc(Cl)cc4CCc4cccnc43)CC2)cc1 10.1016/j.bmcl.2004.08.060
21509921 104458 0 None -4 24 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104091 104458 0 None -4 24 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
9870460 102859 0 None - 1 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cellsIn vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 496 7 2 5 3.8 NC(=O)N(O)CCC#C[C@@H]1CC[C@@H](CN2CCN([C@H](c3ccccc3)c3ccc(Cl)cc3)CC2)O1 10.1016/j.bmcl.2004.02.005
CHEMBL305662 102859 0 None - 1 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cellsIn vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 496 7 2 5 3.8 NC(=O)N(O)CCC#C[C@@H]1CC[C@@H](CN2CCN([C@H](c3ccccc3)c3ccc(Cl)cc3)CC2)O1 10.1016/j.bmcl.2004.02.005
71462100 81280 0 None -39 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 502 8 1 4 5.4 Cc1cc(OC2CCN(CC3CCN([C@@](C)(Cc4ccc(F)cc4)C(=O)O)CC3)CC2)ccc1Cl 10.1016/j.bmcl.2012.08.103
CHEMBL2158792 81280 0 None -39 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 502 8 1 4 5.4 Cc1cc(OC2CCN(CC3CCN([C@@](C)(Cc4ccc(F)cc4)C(=O)O)CC3)CC2)ccc1Cl 10.1016/j.bmcl.2012.08.103
10005242 81290 0 None -3 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 476 7 1 4 5.4 O=C(O)C(c1ccccc1)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158819 81290 0 None -3 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 476 7 1 4 5.4 O=C(O)C(c1ccccc1)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
69347980 81304 1 None 5 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 476 7 1 4 5.4 O=C(O)c1cccc(CN2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.103
CHEMBL2158832 81304 1 None 5 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 476 7 1 4 5.4 O=C(O)c1cccc(CN2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.103
71072040 81307 0 None -5 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 490 8 1 4 5.2 O=C(O)[C@H](Cc1ccccc1)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158835 81307 0 None -5 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 490 8 1 4 5.2 O=C(O)[C@H](Cc1ccccc1)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
71072044 81309 0 None -5 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 524 8 1 4 5.9 O=C(O)[C@H](Cc1ccccc1Cl)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158837 81309 0 None -5 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 524 8 1 4 5.9 O=C(O)[C@H](Cc1ccccc1Cl)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
71072050 81311 0 None -5 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 508 8 1 4 5.4 O=C(O)[C@H](Cc1ccccc1F)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158839 81311 0 None -5 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 508 8 1 4 5.4 O=C(O)[C@H](Cc1ccccc1F)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
71072118 81313 0 None -5 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 508 8 1 4 5.4 O=C(O)[C@H](Cc1ccc(F)cc1)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158841 81313 0 None -5 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 508 8 1 4 5.4 O=C(O)[C@H](Cc1ccc(F)cc1)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
59295946 84013 0 None -5 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 612 11 5 8 1.7 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c(=O)c2cc(S(=O)(=O)NCCO)ccc12 10.1016/j.bmcl.2012.09.112
CHEMBL2207281 84013 0 None -5 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 612 11 5 8 1.7 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c(=O)c2cc(S(=O)(=O)NCCO)ccc12 10.1016/j.bmcl.2012.09.112
59295974 84102 0 None -19 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 581 8 3 7 3.2 Cc1c(Cl)ccc(OC2CCN(C[C@H](O)CNC(=O)c3c[nH]c(=O)c4cc(S(C)(=O)=O)ccc34)CC2)c1Cl 10.1016/j.bmcl.2012.09.112
CHEMBL2207672 84102 0 None -19 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 581 8 3 7 3.2 Cc1c(Cl)ccc(OC2CCN(C[C@H](O)CNC(=O)c3c[nH]c(=O)c4cc(S(C)(=O)=O)ccc34)CC2)c1Cl 10.1016/j.bmcl.2012.09.112
21509921 104458 0 None -4 24 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104091 104458 0 None -4 24 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
1222 881 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor S3.36A mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor S3.36A mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/nchembio714
2678 881 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor S3.36A mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor S3.36A mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/nchembio714
581 881 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor S3.36A mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor S3.36A mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/nchembio714
CHEMBL1000 881 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor S3.36A mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor S3.36A mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/nchembio714
DB00341 881 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor S3.36A mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor S3.36A mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/nchembio714
1222 881 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]mepyramine from human wild-type histamine H1 receptor expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human wild-type histamine H1 receptor expressed in COS-7 cells by liquid scintillation counting
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/nchembio714
2678 881 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]mepyramine from human wild-type histamine H1 receptor expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human wild-type histamine H1 receptor expressed in COS-7 cells by liquid scintillation counting
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/nchembio714
581 881 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]mepyramine from human wild-type histamine H1 receptor expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human wild-type histamine H1 receptor expressed in COS-7 cells by liquid scintillation counting
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/nchembio714
CHEMBL1000 881 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]mepyramine from human wild-type histamine H1 receptor expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human wild-type histamine H1 receptor expressed in COS-7 cells by liquid scintillation counting
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/nchembio714
DB00341 881 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]mepyramine from human wild-type histamine H1 receptor expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human wild-type histamine H1 receptor expressed in COS-7 cells by liquid scintillation counting
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/nchembio714
2726 919 68 None -6 72 Guinea pig 7.3 pKi = 7.3 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
621 919 68 None -6 72 Guinea pig 7.3 pKi = 7.3 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
83 919 68 None -6 72 Guinea pig 7.3 pKi = 7.3 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
CHEMBL71 919 68 None -6 72 Guinea pig 7.3 pKi = 7.3 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
DB00477 919 68 None -6 72 Guinea pig 7.3 pKi = 7.3 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
17963208 82253 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 529 5 1 5 4.5 O=C(NS(=O)(=O)c1ccc(F)cc1)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
CHEMBL2171034 82253 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 529 5 1 5 4.5 O=C(NS(=O)(=O)c1ccc(F)cc1)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
17963334 82257 0 None -2 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 525 5 1 5 4.7 Cc1ccccc1S(=O)(=O)NC(=O)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
CHEMBL2171038 82257 0 None -2 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 525 5 1 5 4.7 Cc1ccccc1S(=O)(=O)NC(=O)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
71457010 82258 0 None -10 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 545 5 1 5 5.1 O=C(NS(=O)(=O)c1ccccc1Cl)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
CHEMBL2171039 82258 0 None -10 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 545 5 1 5 5.1 O=C(NS(=O)(=O)c1ccccc1Cl)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
10143016 82273 0 None 3 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 525 6 1 5 4.5 O=C(NS(=O)(=O)Cc1ccccc1)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
CHEMBL2171215 82273 0 None 3 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 525 6 1 5 4.5 O=C(NS(=O)(=O)Cc1ccccc1)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
10947658 28702 0 None -457 16 Human 6.3 pKi = 6.3 Binding
Binding affinity against Histamine H1 receptorBinding affinity against Histamine H1 receptor
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
CHEMBL137781 28702 0 None -457 16 Human 6.3 pKi = 6.3 Binding
Binding affinity against Histamine H1 receptorBinding affinity against Histamine H1 receptor
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
9826801 107937 0 None -2187 11 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cellsDisplacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 488 6 1 7 3.2 Cn1nnc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm100652h
CHEMBL319352 107937 0 None -2187 11 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cellsDisplacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 488 6 1 7 3.2 Cn1nnc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm100652h
10414153 21539 0 None - 1 Guinea pig 6.3 pKi = 6.3 Binding
Inhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptorInhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptor
ChEMBL 515 6 2 7 5.5 O=C(O)c1ccc2c(c1)C(SCCN1CCC(n3c(O)nc4ccccc43)CC1)c1ccccc1CO2 10.1021/jm00055a013
CHEMBL131648 21539 0 None - 1 Guinea pig 6.3 pKi = 6.3 Binding
Inhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptorInhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptor
ChEMBL 515 6 2 7 5.5 O=C(O)c1ccc2c(c1)C(SCCN1CCC(n3c(O)nc4ccccc43)CC1)c1ccccc1CO2 10.1021/jm00055a013
14885641 115088 0 None - 1 Rat 5.3 pKi = 5.3 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 317 0 0 1 4.2 CC(=O)N1CCC(=C2c3ccccc3CCc3ccccc32)CC1 10.1021/jm00105a069
CHEMBL334318 115088 0 None - 1 Rat 5.3 pKi = 5.3 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 317 0 0 1 4.2 CC(=O)N1CCC(=C2c3ccccc3CCc3ccccc32)CC1 10.1021/jm00105a069
46882182 5921 0 None -95 5 Human 5.3 pKi = 5.3 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 567 11 1 9 4.7 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)N(C)C)ccc4o3)CC2)cc(OCC)c1-n1cccc1 10.1016/j.bmcl.2009.09.024
CHEMBL1079686 5921 0 None -95 5 Human 5.3 pKi = 5.3 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 567 11 1 9 4.7 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)N(C)C)ccc4o3)CC2)cc(OCC)c1-n1cccc1 10.1016/j.bmcl.2009.09.024
168288633 191778 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 712 18 5 7 2.5 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5198008 191778 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 712 18 5 7 2.5 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
44304091 202951 0 None -63 3 Human 6.3 pKi = 6.3 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 432 14 0 5 5.2 CCCCCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL62949 202951 0 None -63 3 Human 6.3 pKi = 6.3 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 432 14 0 5 5.2 CCCCCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
44335463 4455 0 None -8 4 Human 6.3 pKi = 6.3 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 357 7 1 4 3.2 CCOC(=O)N1CCN(CCCOc2ccc(-c3cc[nH]c3)cc2)CC1 10.1016/s0960-894x(02)00648-0
CHEMBL101692 4455 0 None -8 4 Human 6.3 pKi = 6.3 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 357 7 1 4 3.2 CCOC(=O)N1CCN(CCCOc2ccc(-c3cc[nH]c3)cc2)CC1 10.1016/s0960-894x(02)00648-0
66615606 81273 0 None -398 2 Human 6.3 pKi = 6.3 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 513 8 1 5 4.9 Cc1c(OC2CCN(CC3CCN([C@@H](Cc4ccc(F)cc4)C(=O)O)CC3)CC2)ccc(C#N)c1Cl 10.1016/j.bmcl.2012.08.103
CHEMBL2158785 81273 0 None -398 2 Human 6.3 pKi = 6.3 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 513 8 1 5 4.9 Cc1c(OC2CCN(CC3CCN([C@@H](Cc4ccc(F)cc4)C(=O)O)CC3)CC2)ccc(C#N)c1Cl 10.1016/j.bmcl.2012.08.103
50878551 90745 61 None -21 18 Human 6.3 pKi = 6.3 Binding
Binding affinity to histamine H1 receptor (unknown origin) by competition binding assayBinding affinity to histamine H1 receptor (unknown origin) by competition binding assay
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL2391541 90745 61 None -21 18 Human 6.3 pKi = 6.3 Binding
Binding affinity to histamine H1 receptor (unknown origin) by competition binding assayBinding affinity to histamine H1 receptor (unknown origin) by competition binding assay
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2015.12.053
71459825 84200 0 None -3 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 433 8 2 5 3.9 N#Cc1ccc(OC[C@@H](O)CNC2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)cc1 10.1016/j.bmcl.2012.09.113
CHEMBL2208417 84200 0 None -3 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 433 8 2 5 3.9 N#Cc1ccc(OC[C@@H](O)CNC2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)cc1 10.1016/j.bmcl.2012.09.113
71452602 84219 0 None -1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 433 8 2 5 3.9 N#Cc1cccc(OC[C@@H](O)CNC2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)c1 10.1016/j.bmcl.2012.09.113
CHEMBL2208436 84219 0 None -1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 433 8 2 5 3.9 N#Cc1cccc(OC[C@@H](O)CNC2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)c1 10.1016/j.bmcl.2012.09.113
59296098 84098 0 None -15 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 446 7 3 6 2.0 N#Cc1ccc(OC2CCN(C[C@H](O)CNC(=O)c3c[nH]c(=O)c4ccccc34)CC2)cc1 10.1016/j.bmcl.2012.09.112
CHEMBL2207668 84098 0 None -15 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 446 7 3 6 2.0 N#Cc1ccc(OC2CCN(C[C@H](O)CNC(=O)c3c[nH]c(=O)c4ccccc34)CC2)cc1 10.1016/j.bmcl.2012.09.112
168288633 191778 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 712 18 5 7 2.5 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5198008 191778 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 712 18 5 7 2.5 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
18672441 95395 0 None -691 4 Human 5.3 pKi = 5.3 Binding
Binding affinity at human cortical Histamine 1 receptorBinding affinity at human cortical Histamine 1 receptor
ChEMBL 306 6 0 3 4.1 N#Cc1ccc(-c2ccc(OCCCN3CCCC3)cc2)cc1 10.1016/s0960-894x(02)00648-0
CHEMBL25688 95395 0 None -691 4 Human 5.3 pKi = 5.3 Binding
Binding affinity at human cortical Histamine 1 receptorBinding affinity at human cortical Histamine 1 receptor
ChEMBL 306 6 0 3 4.1 N#Cc1ccc(-c2ccc(OCCCN3CCCC3)cc2)cc1 10.1016/s0960-894x(02)00648-0
168290815 192973 0 None -10232 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 327 9 4 5 1.2 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5200771 192973 0 None -10232 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 327 9 4 5 1.2 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222529 192973 0 None -10232 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 327 9 4 5 1.2 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
10802229 56556 0 None -794 2 Guinea pig 4.3 pKi = 4.3 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 273 6 2 3 2.8 C[C@@H](NC(=O)OCCCc1c[nH]cn1)c1ccccc1 10.1021/jm9507688
CHEMBL16401 56556 0 None -794 2 Guinea pig 4.3 pKi = 4.3 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 273 6 2 3 2.8 C[C@@H](NC(=O)OCCCc1c[nH]cn1)c1ccccc1 10.1021/jm9507688
10729448 56564 0 None -1584 2 Guinea pig 4.3 pKi = 4.3 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 251 6 2 3 2.3 O=C(NCC1CCCC1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL16407 56564 0 None -1584 2 Guinea pig 4.3 pKi = 4.3 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 251 6 2 3 2.3 O=C(NCC1CCCC1)OCCCc1c[nH]cn1 10.1021/jm9507688
10588560 96574 0 None -2089 2 Guinea pig 4.3 pKi = 4.3 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 277 6 2 3 2.4 O=C(NCc1ccc(F)cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL263070 96574 0 None -2089 2 Guinea pig 4.3 pKi = 4.3 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 277 6 2 3 2.4 O=C(NCc1ccc(F)cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
10852027 98688 0 None -3890 2 Guinea pig 4.3 pKi = 4.3 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 304 7 2 5 2.2 O=C(NCc1cccc([N+](=O)[O-])c1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL277537 98688 0 None -3890 2 Guinea pig 4.3 pKi = 4.3 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 304 7 2 5 2.2 O=C(NCc1cccc([N+](=O)[O-])c1)OCCCc1c[nH]cn1 10.1021/jm9507688
57345618 70459 0 None -7 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-Pyrilamine from human histamine H1 receptor by liquid scintillation counterDisplacement of [3H]-Pyrilamine from human histamine H1 receptor by liquid scintillation counter
ChEMBL 362 6 0 3 4.5 Fc1ccc(OCCCN2CCCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2012.01.022
CHEMBL1946126 70459 0 None -7 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-Pyrilamine from human histamine H1 receptor by liquid scintillation counterDisplacement of [3H]-Pyrilamine from human histamine H1 receptor by liquid scintillation counter
ChEMBL 362 6 0 3 4.5 Fc1ccc(OCCCN2CCCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2012.01.022
44582675 189701 0 None -8 15 Human 6.3 pKi = 6.3 Binding
Inhibition of human cloned histamine H1 receptor by competitive binding experimentInhibition of human cloned histamine H1 receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1[C@H](O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL515472 189701 0 None -8 15 Human 6.3 pKi = 6.3 Binding
Inhibition of human cloned histamine H1 receptor by competitive binding experimentInhibition of human cloned histamine H1 receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1[C@H](O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
14554127 113325 0 None 3 2 Rat 7.3 pKi = 7.3 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 380 2 0 2 5.1 CCCC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/jm00105a069
CHEMBL331603 113325 0 None 3 2 Rat 7.3 pKi = 7.3 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 380 2 0 2 5.1 CCCC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/jm00105a069
2865 4143 73 None -58 53 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human H1 receptorBinding affinity towards human H1 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm0002432
59 4143 73 None -58 53 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human H1 receptorBinding affinity towards human H1 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm0002432
60854 4143 73 None -58 53 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human H1 receptorBinding affinity towards human H1 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm0002432
CHEMBL708 4143 73 None -58 53 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human H1 receptorBinding affinity towards human H1 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm0002432
DB00246 4143 73 None -58 53 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human H1 receptorBinding affinity towards human H1 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm0002432
73346042 91834 5 None -5128 17 Human 6.3 pKi = 6.3 Binding
Binding affinity to histamine H1 receptor (unknown origin)Binding affinity to histamine H1 receptor (unknown origin)
ChEMBL 405 9 0 8 0.9 Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3OCCF)CC2)c1=O 10.1016/j.bmc.2013.05.050
CHEMBL2413153 91834 5 None -5128 17 Human 6.3 pKi = 6.3 Binding
Binding affinity to histamine H1 receptor (unknown origin)Binding affinity to histamine H1 receptor (unknown origin)
ChEMBL 405 9 0 8 0.9 Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3OCCF)CC2)c1=O 10.1016/j.bmc.2013.05.050
168269172 190002 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 684 17 5 7 1.8 C[C@H](NC(=O)CNC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5171289 190002 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 684 17 5 7 1.8 C[C@H](NC(=O)CNC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
168286426 192926 0 None -58 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 403 10 4 5 2.3 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5198795 192926 0 None -58 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 403 10 4 5 2.3 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222241 192926 0 None -58 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 403 10 4 5 2.3 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
164618508 185932 0 None -165 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 374 6 4 4 2.7 Cc1ccc(C(C)NC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4869194 185932 0 None -165 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 374 6 4 4 2.7 Cc1ccc(C(C)NC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1 10.1016/j.ejmech.2021.113190
168269172 190002 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 684 17 5 7 1.8 C[C@H](NC(=O)CNC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5171289 190002 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 684 17 5 7 1.8 C[C@H](NC(=O)CNC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
83632 5180 7 None 1 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cellsDisplacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cells
ChEMBL 225 4 0 1 3.4 CN(C)CC(c1ccccc1)c1ccccc1 10.1016/j.bmc.2009.08.016
CHEMBL10602 5180 7 None 1 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cellsDisplacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cells
ChEMBL 225 4 0 1 3.4 CN(C)CC(c1ccccc1)c1ccccc1 10.1016/j.bmc.2009.08.016
60165413 75360 0 None -15 7 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]Pyrilamine from human H1 histamine receptor by liquid scintillation assayDisplacement of [3H]Pyrilamine from human H1 histamine receptor by liquid scintillation assay
ChEMBL 378 7 0 4 5.5 O=C(CCCCN1CCC(c2ccccc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL2037531 75360 0 None -15 7 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]Pyrilamine from human H1 histamine receptor by liquid scintillation assayDisplacement of [3H]Pyrilamine from human H1 histamine receptor by liquid scintillation assay
ChEMBL 378 7 0 4 5.5 O=C(CCCCN1CCC(c2ccccc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
11848677 148352 0 None -1 5 Human 6.3 pKi = 6.3 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 460 8 2 8 3.0 CCOc1cc(CN2CCC(Nc3nc4cc(S(N)(=O)=O)ccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
CHEMBL393718 148352 0 None -1 5 Human 6.3 pKi = 6.3 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 460 8 2 8 3.0 CCOc1cc(CN2CCC(Nc3nc4cc(S(N)(=O)=O)ccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
10341609 200270 0 None -117 3 Human 6.3 pKi = 6.3 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 412 11 1 5 3.4 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3c[nH]cn3)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL59715 200270 0 None -117 3 Human 6.3 pKi = 6.3 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 412 11 1 5 3.4 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3c[nH]cn3)CC2)cc1 10.1016/s0960-894x(02)00309-8
168274129 192809 0 None -16 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 370 12 5 6 1.0 NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5176780 192809 0 None -16 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 370 12 5 6 1.0 NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221468 192809 0 None -16 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 370 12 5 6 1.0 NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168294770 193020 0 None -2 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 436 6 4 4 4.3 Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5208327 193020 0 None -2 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 436 6 4 4 4.3 Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222806 193020 0 None -2 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 436 6 4 4 4.3 Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)cc1 10.1021/acs.jmedchem.1c00692
168295803 193045 0 None -3 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 338 6 4 4 1.6 CCCCCNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
CHEMBL5207206 193045 0 None -3 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 338 6 4 4 1.6 CCCCCNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
CHEMBL5222937 193045 0 None -3 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 338 6 4 4 1.6 CCCCCNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
112936262 137276 1 None -3 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 389 6 1 6 3.5 COc1ccc(CNc2nc(-c3ccccc3)cc(N3CCN(C)CC3)n2)cc1 10.1016/j.bmcl.2015.12.035
CHEMBL3752195 137276 1 None -3 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 389 6 1 6 3.5 COc1ccc(CNc2nc(-c3ccccc3)cc(N3CCN(C)CC3)n2)cc1 10.1016/j.bmcl.2015.12.035
164620139 185788 0 None -60 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 436 8 4 4 3.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4866734 185788 0 None -60 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 436 8 4 4 3.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
164608941 184383 0 None -123 4 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 390 7 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4845733 184383 0 None -123 4 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 390 7 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
3168 9262 92 None -87 21 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
CHEMBL1108 9262 92 None -87 21 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
17590280 69023 6 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 264 4 1 2 3.5 Cc1cccc2c(CCN)cn(Cc3ccccc3)c12 10.1021/jm2011589
CHEMBL1923524 69023 6 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 264 4 1 2 3.5 Cc1cccc2c(CCN)cn(Cc3ccccc3)c12 10.1021/jm2011589
168295528 193031 0 None -2951 20 Human 5.3 pKi = 5.3 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5206565 193031 0 None -2951 20 Human 5.3 pKi = 5.3 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222872 193031 0 None -2951 20 Human 5.3 pKi = 5.3 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
4440801 168284 9 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 298 3 1 6 1.5 OCCN1CCN(c2ncnc3c2oc2ccccc23)CC1 10.1021/jm2011589
CHEMBL434001 168284 9 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 298 3 1 6 1.5 OCCN1CCN(c2ncnc3c2oc2ccccc23)CC1 10.1021/jm2011589
12016525 202915 0 None -2630 3 Human 4.3 pKi = 4.3 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 359 8 1 5 1.5 C[C@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL62804 202915 0 None -2630 3 Human 4.3 pKi = 4.3 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 359 8 1 5 1.5 C[C@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
164611143 184716 0 None -234 4 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 414 6 4 4 2.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)C(F)(F)F 10.1016/j.ejmech.2021.113190
CHEMBL4850448 184716 0 None -234 4 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 414 6 4 4 2.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)C(F)(F)F 10.1016/j.ejmech.2021.113190
9830741 207856 1 None -275 6 Human 7.3 pKi = 7.3 Binding
Binding affinity towards Histamine H1 receptor in human brain tissue preparation, using [3H]rauwolscine as radioligand.Binding affinity towards Histamine H1 receptor in human brain tissue preparation, using [3H]rauwolscine as radioligand.
ChEMBL 475 6 1 4 5.0 C[C@@H]1OC(=O)N(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@H]1c1ccc(F)c(F)c1 10.1021/jm000085e
CHEMBL96467 207856 1 None -275 6 Human 7.3 pKi = 7.3 Binding
Binding affinity towards Histamine H1 receptor in human brain tissue preparation, using [3H]rauwolscine as radioligand.Binding affinity towards Histamine H1 receptor in human brain tissue preparation, using [3H]rauwolscine as radioligand.
ChEMBL 475 6 1 4 5.0 C[C@@H]1OC(=O)N(C(=O)NCCCN2CCC(c3ccc(F)cc3)CC2)[C@H]1c1ccc(F)c(F)c1 10.1021/jm000085e
122196373 124287 0 None -2 5 Guinea pig 7.3 pKi = 7.3 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates after 60 mins by liquid scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates after 60 mins by liquid scintillation counting
ChEMBL 471 7 0 6 6.4 Fc1ccc2c(C3CCN(CCCOc4ccc(-c5nc6ccccc6o5)cc4)CC3)noc2c1 10.1016/j.bmcl.2015.09.045
CHEMBL3634813 124287 0 None -2 5 Guinea pig 7.3 pKi = 7.3 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates after 60 mins by liquid scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates after 60 mins by liquid scintillation counting
ChEMBL 471 7 0 6 6.4 Fc1ccc2c(C3CCN(CCCOc4ccc(-c5nc6ccccc6o5)cc4)CC3)noc2c1 10.1016/j.bmcl.2015.09.045
46929554 16754 0 None -31 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 349 5 1 3 4.7 FC(F)(F)c1ccc(SCC(c2ccncc2)c2c[nH]cn2)cc1 10.1021/jm100643t
CHEMBL1243367 16754 0 None -31 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 349 5 1 3 4.7 FC(F)(F)c1ccc(SCC(c2ccncc2)c2c[nH]cn2)cc1 10.1021/jm100643t
1854 3552 7 None - 1 Rat 5.3 pKi = 5.3 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 355 1 0 3 3.1 Clc1ccc2c(c1)CCc1c(C2N2CCN(CC2)C(=O)C)nccc1 10.1016/s0960-894x(98)00626-x
9950564 3552 7 None - 1 Rat 5.3 pKi = 5.3 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 355 1 0 3 3.1 Clc1ccc2c(c1)CCc1c(C2N2CCN(CC2)C(=O)C)nccc1 10.1016/s0960-894x(98)00626-x
CHEMBL326821 3552 7 None - 1 Rat 5.3 pKi = 5.3 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 355 1 0 3 3.1 Clc1ccc2c(c1)CCc1c(C2N2CCN(CC2)C(=O)C)nccc1 10.1016/s0960-894x(98)00626-x
141485889 171198 0 None - 1 Guinea pig 6.3 pKi = 6.3 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysisDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysis
ChEMBL 290 7 0 3 2.4 CCN(CC)CCCOc1ccc2c(c1)C(=O)N(C)CC2 10.1016/j.bmcl.2019.04.015
CHEMBL4459304 171198 0 None - 1 Guinea pig 6.3 pKi = 6.3 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysisDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysis
ChEMBL 290 7 0 3 2.4 CCN(CC)CCCOc1ccc2c(c1)C(=O)N(C)CC2 10.1016/j.bmcl.2019.04.015
9906447 195577 2 None -7585 13 Human 5.3 pKi = 5.3 Binding
Binding affinity to human recombinant H1 receptorBinding affinity to human recombinant H1 receptor
ChEMBL 351 5 0 3 4.8 C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc(F)cc3)ccc2o1 10.1021/jm201690h
CHEMBL2031738 195577 2 None -7585 13 Human 5.3 pKi = 5.3 Binding
Binding affinity to human recombinant H1 receptorBinding affinity to human recombinant H1 receptor
ChEMBL 351 5 0 3 4.8 C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc(F)cc3)ccc2o1 10.1021/jm201690h
CHEMBL555146 195577 2 None -7585 13 Human 5.3 pKi = 5.3 Binding
Binding affinity to human recombinant H1 receptorBinding affinity to human recombinant H1 receptor
ChEMBL 351 5 0 3 4.8 C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc(F)cc3)ccc2o1 10.1021/jm201690h
25147772 173409 9 None -6 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 373 4 1 6 3.7 CN1CCN(c2nc(NCc3cccs3)c3cc(Cl)ccc3n2)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL452847 173409 9 None -6 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 373 4 1 6 3.7 CN1CCN(c2nc(NCc3cccs3)c3cc(Cl)ccc3n2)CC1 10.1016/j.bmcl.2015.12.035
168274690 190538 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 770 20 6 8 2.3 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5179725 190538 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 770 20 6 8 2.3 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
71681209 90272 0 None -138 5 Guinea pig 6.3 pKi = 6.3 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysisDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysis
ChEMBL 464 7 0 6 5.7 Cc1c(C)c2ccc(OCCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc2oc1=O 10.1021/jm400408r
CHEMBL2385102 90272 0 None -138 5 Guinea pig 6.3 pKi = 6.3 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysisDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysis
ChEMBL 464 7 0 6 5.7 Cc1c(C)c2ccc(OCCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc2oc1=O 10.1021/jm400408r
44304327 200882 0 None -1380 3 Human 5.3 pKi = 5.3 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 535 11 1 6 4.3 CC(C)(C)OC(=O)N[C@H](Cc1ccccc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL60143 200882 0 None -1380 3 Human 5.3 pKi = 5.3 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 535 11 1 6 4.3 CC(C)(C)OC(=O)N[C@H](Cc1ccccc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
168268716 192762 0 None -1 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 372 3 4 4 3.5 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NC2CCCCC2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5170276 192762 0 None -1 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 372 3 4 4 3.5 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NC2CCCCC2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5221176 192762 0 None -1 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 372 3 4 4 3.5 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NC2CCCCC2)cc1 10.1021/acs.jmedchem.1c00692
168274690 190538 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 770 20 6 8 2.3 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5179725 190538 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 770 20 6 8 2.3 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
10051425 204666 0 None - 1 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cellsIn vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 494 7 2 5 4.0 NC(=O)N(O)CCC#Cc1ccc(CN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)o1 10.1016/j.bmcl.2004.02.005
CHEMBL73706 204666 0 None - 1 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cellsIn vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 494 7 2 5 4.0 NC(=O)N(O)CCC#Cc1ccc(CN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)o1 10.1016/j.bmcl.2004.02.005
44334782 5425 0 None -1318 3 Human 5.3 pKi = 5.3 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 442 10 1 5 3.4 Cc1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1 10.1016/s0960-894x(02)00685-6
CHEMBL107293 5425 0 None -1318 3 Human 5.3 pKi = 5.3 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 442 10 1 5 3.4 Cc1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1 10.1016/s0960-894x(02)00685-6
71457844 84076 0 None -2884 7 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis
ChEMBL 429 6 0 4 5.1 COc1ccccc1N1CCN(Cc2cc(CN3CCCCC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207638 84076 0 None -2884 7 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis
ChEMBL 429 6 0 4 5.1 COc1ccccc1N1CCN(Cc2cc(CN3CCCCC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
73349359 92543 0 None -8 8 Human 5.3 pKi = 5.3 Binding
Inhibition of histamine H1 receptor (unknown origin) by PDSP assayInhibition of histamine H1 receptor (unknown origin) by PDSP assay
ChEMBL 341 6 1 4 2.9 COc1cc(CN[C@H]2C3C4CC5C6C4CC3C6C52)cc(OC)c1OC 10.1016/j.bmc.2013.07.045
CHEMBL2432051 92543 0 None -8 8 Human 5.3 pKi = 5.3 Binding
Inhibition of histamine H1 receptor (unknown origin) by PDSP assayInhibition of histamine H1 receptor (unknown origin) by PDSP assay
ChEMBL 341 6 1 4 2.9 COc1cc(CN[C@H]2C3C4CC5C6C4CC3C6C52)cc(OC)c1OC 10.1016/j.bmc.2013.07.045
44591012 175580 0 None -114 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 522 10 0 3 6.6 CN(CCC=C1c2ccccc2CCc2ccccc21)C(=O)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
CHEMBL457957 175580 0 None -114 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 522 10 0 3 6.6 CN(CCC=C1c2ccccc2CCc2ccccc21)C(=O)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
44304439 102798 0 None -5 3 Human 7.3 pKi = 7.3 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 436 12 0 4 4.6 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)Cc3ccccc3)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL305338 102798 0 None -5 3 Human 7.3 pKi = 7.3 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 436 12 0 4 4.6 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)Cc3ccccc3)CC2)cc1 10.1016/s0960-894x(02)00309-8
44304245 203328 0 None -13 3 Human 7.3 pKi = 7.3 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 425 11 0 5 4.0 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cccn3C)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL64884 203328 0 None -13 3 Human 7.3 pKi = 7.3 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 425 11 0 5 4.0 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cccn3C)CC2)cc1 10.1016/s0960-894x(02)00309-8
44334281 4759 0 None -181 3 Human 4.3 pKi = 4.3 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 433 9 2 6 2.8 CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@@H](C)NC(=O)OC(C)(C)C)C2)cc1 10.1016/s0960-894x(02)00685-6
CHEMBL103828 4759 0 None -181 3 Human 4.3 pKi = 4.3 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 433 9 2 6 2.8 CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@@H](C)NC(=O)OC(C)(C)C)C2)cc1 10.1016/s0960-894x(02)00685-6
168281024 190915 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 741 19 6 8 1.1 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5185247 190915 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 741 19 6 8 1.1 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
44304459 172600 0 None -151 3 Human 6.3 pKi = 6.3 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 418 13 0 5 4.8 CCCCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL449040 172600 0 None -151 3 Human 6.3 pKi = 6.3 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 418 13 0 5 4.8 CCCCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
44304283 203173 0 None -42 3 Human 6.3 pKi = 6.3 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 452 8 0 5 4.8 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3ccc(C(C)(C)C)cc3)cc2)CC1 10.1016/s0960-894x(02)00309-8
CHEMBL64247 203173 0 None -42 3 Human 6.3 pKi = 6.3 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 452 8 0 5 4.8 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3ccc(C(C)(C)C)cc3)cc2)CC1 10.1016/s0960-894x(02)00309-8
10472082 5141 0 None -831 4 Human 6.3 pKi = 6.3 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 334 6 0 3 4.9 C[C@@H]1CC[C@@H](C)N1CCCOc1ccc(-c2ccc(C#N)cc2)cc1 10.1016/s0960-894x(02)00648-0
CHEMBL105762 5141 0 None -831 4 Human 6.3 pKi = 6.3 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 334 6 0 3 4.9 C[C@@H]1CC[C@@H](C)N1CCCOc1ccc(-c2ccc(C#N)cc2)cc1 10.1016/s0960-894x(02)00648-0
168281024 190915 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 741 19 6 8 1.1 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5185247 190915 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 741 19 6 8 1.1 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
9923186 107542 0 None -288 4 Human 5.3 pKi = 5.3 Binding
Binding affinity at human cortical Histamine 1 receptorBinding affinity at human cortical Histamine 1 receptor
ChEMBL 322 6 1 4 3.1 N#Cc1ccc(-c2ccc(OCCCN3CC[C@H](O)C3)cc2)cc1 10.1016/s0960-894x(02)00648-0
CHEMBL318801 107542 0 None -288 4 Human 5.3 pKi = 5.3 Binding
Binding affinity at human cortical Histamine 1 receptorBinding affinity at human cortical Histamine 1 receptor
ChEMBL 322 6 1 4 3.1 N#Cc1ccc(-c2ccc(OCCCN3CC[C@H](O)C3)cc2)cc1 10.1016/s0960-894x(02)00648-0
168273745 192808 0 None -114 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 332 6 4 4 1.5 N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5178472 192808 0 None -114 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 332 6 4 4 1.5 N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221451 192808 0 None -114 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 332 6 4 4 1.5 N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
2435 3590 83 None -95 48 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human histamine H1 receptorBinding affinity towards human histamine H1 receptor
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm030480f
60149 3590 83 None -95 48 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human histamine H1 receptorBinding affinity towards human histamine H1 receptor
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm030480f
98 3590 83 None -95 48 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human histamine H1 receptorBinding affinity towards human histamine H1 receptor
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm030480f
CHEMBL12713 3590 83 None -95 48 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human histamine H1 receptorBinding affinity towards human histamine H1 receptor
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm030480f
DB06144 3590 83 None -95 48 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human histamine H1 receptorBinding affinity towards human histamine H1 receptor
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm030480f
44304399 203193 0 None -28 3 Human 6.2 pKi = 6.2 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 418 13 0 5 4.8 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCCCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL64317 203193 0 None -28 3 Human 6.2 pKi = 6.2 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 418 13 0 5 4.8 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCCCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
44335456 4553 0 None -18 4 Human 6.2 pKi = 6.2 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 336 6 1 4 3.5 N#Cc1ccc(-c2ccc(OCCCN3CCC(O)CC3)cc2)cc1 10.1016/s0960-894x(02)00648-0
CHEMBL102416 4553 0 None -18 4 Human 6.2 pKi = 6.2 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 336 6 1 4 3.5 N#Cc1ccc(-c2ccc(OCCCN3CCC(O)CC3)cc2)cc1 10.1016/s0960-894x(02)00648-0
127036978 137281 0 None -1 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 415 5 1 6 3.6 COc1ccc(CNc2nc3c(c(N4CCN(C)CC4)n2)CCc2ccccc2-3)cc1 10.1016/j.bmcl.2015.12.035
CHEMBL3752225 137281 0 None -1 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 415 5 1 6 3.6 COc1ccc(CNc2nc3c(c(N4CCN(C)CC4)n2)CCc2ccccc2-3)cc1 10.1016/j.bmcl.2015.12.035
2600 3779 74 None 1 13 Human 7.2 pKi = 7.2 Binding
Binding affinity towards histamine H1 receptorBinding affinity towards histamine H1 receptor
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1021/jm0205651
2608 3779 74 None 1 13 Human 7.2 pKi = 7.2 Binding
Binding affinity towards histamine H1 receptorBinding affinity towards histamine H1 receptor
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1021/jm0205651
5405 3779 74 None 1 13 Human 7.2 pKi = 7.2 Binding
Binding affinity towards histamine H1 receptorBinding affinity towards histamine H1 receptor
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1021/jm0205651
CHEMBL17157 3779 74 None 1 13 Human 7.2 pKi = 7.2 Binding
Binding affinity towards histamine H1 receptorBinding affinity towards histamine H1 receptor
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1021/jm0205651
DB00342 3779 74 None 1 13 Human 7.2 pKi = 7.2 Binding
Binding affinity towards histamine H1 receptorBinding affinity towards histamine H1 receptor
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1021/jm0205651
10474964 130471 0 None -181 7 Rat 7.2 pKi = 7.2 Binding
Inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat cortexInhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat cortex
ChEMBL 381 5 1 3 3.3 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
CHEMBL368061 130471 0 None -181 7 Rat 7.2 pKi = 7.2 Binding
Inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat cortexInhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat cortex
ChEMBL 381 5 1 3 3.3 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
CHEMBL5206021 130471 0 None -181 7 Rat 7.2 pKi = 7.2 Binding
Inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat cortexInhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat cortex
ChEMBL 381 5 1 3 3.3 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
9827677 168422 0 None -288 7 Human 7.2 pKi = 7.2 Binding
Selectivity screen against human Histamine H1 receptorSelectivity screen against human Histamine H1 receptor
ChEMBL 510 7 2 4 4.2 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1 10.1016/s0960-894x(99)00696-4
CHEMBL43491 168422 0 None -288 7 Human 7.2 pKi = 7.2 Binding
Selectivity screen against human Histamine H1 receptorSelectivity screen against human Histamine H1 receptor
ChEMBL 510 7 2 4 4.2 CC1=C(C(=O)NCCCN2CCC(c3ccc(F)cc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1 10.1016/s0960-894x(99)00696-4
71212556 143562 0 None -7 6 Human 7.2 pKi = 7.2 Binding
Scintillation Proximity Assay: [3H]-Pyrilamine binding experiments are carried out in SPA (scintillation proximity assay) 96-well format. Membranes used in this assay are prepared from HEK-293 cells stably expressing recombinant H1 receptor (human). The incubation is initiated by the addition of a mixture of WGA PVT SPA beads (1 mg/well, Perkin Elmer (MA, USA) RPNQ0001) and 3 μg membranes to assay buffer (67 mM Tris; pH 7.6) containing 3.5 nM [3H]-Pyrilamine and varying concentrations of the test compound (10 point concentration response curves). Non-specific binding is determined in the presence of 10 μM Triprolidine. Samples are incubated for 4 hr. at room temperature (22° C.) and then read in a Microbeta Trilux.Scintillation Proximity Assay: [3H]-Pyrilamine binding experiments are carried out in SPA (scintillation proximity assay) 96-well format. Membranes used in this assay are prepared from HEK-293 cells stably expressing recombinant H1 receptor (human). The incubation is initiated by the addition of a mixture of WGA PVT SPA beads (1 mg/well, Perkin Elmer (MA, USA) RPNQ0001) and 3 μg membranes to assay buffer (67 mM Tris; pH 7.6) containing 3.5 nM [3H]-Pyrilamine and varying concentrations of the test compound (10 point concentration response curves). Non-specific binding is determined in the presence of 10 μM Triprolidine. Samples are incubated for 4 hr. at room temperature (22° C.) and then read in a Microbeta Trilux.
ChEMBL 433 3 1 6 4.6 Cc1ccc2c(c1)Oc1sc(Cl)cc1C(N1CCN(CC(C)(C)C(=O)O)CC1)=N2 nan
CHEMBL3899169 143562 0 None -7 6 Human 7.2 pKi = 7.2 Binding
Scintillation Proximity Assay: [3H]-Pyrilamine binding experiments are carried out in SPA (scintillation proximity assay) 96-well format. Membranes used in this assay are prepared from HEK-293 cells stably expressing recombinant H1 receptor (human). The incubation is initiated by the addition of a mixture of WGA PVT SPA beads (1 mg/well, Perkin Elmer (MA, USA) RPNQ0001) and 3 μg membranes to assay buffer (67 mM Tris; pH 7.6) containing 3.5 nM [3H]-Pyrilamine and varying concentrations of the test compound (10 point concentration response curves). Non-specific binding is determined in the presence of 10 μM Triprolidine. Samples are incubated for 4 hr. at room temperature (22° C.) and then read in a Microbeta Trilux.Scintillation Proximity Assay: [3H]-Pyrilamine binding experiments are carried out in SPA (scintillation proximity assay) 96-well format. Membranes used in this assay are prepared from HEK-293 cells stably expressing recombinant H1 receptor (human). The incubation is initiated by the addition of a mixture of WGA PVT SPA beads (1 mg/well, Perkin Elmer (MA, USA) RPNQ0001) and 3 μg membranes to assay buffer (67 mM Tris; pH 7.6) containing 3.5 nM [3H]-Pyrilamine and varying concentrations of the test compound (10 point concentration response curves). Non-specific binding is determined in the presence of 10 μM Triprolidine. Samples are incubated for 4 hr. at room temperature (22° C.) and then read in a Microbeta Trilux.
ChEMBL 433 3 1 6 4.6 Cc1ccc2c(c1)Oc1sc(Cl)cc1C(N1CCN(CC(C)(C)C(=O)O)CC1)=N2 nan
51002362 82622 0 None 3 6 Human 6.2 pKi = 6.2 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 448 5 1 7 3.8 COc1ccc(S(=O)(=O)n2cc(C)c3cc(Cl)cnc32)cc1NC1CCN(C)CC1 10.1021/jm300955x
CHEMBL2179222 82622 0 None 3 6 Human 6.2 pKi = 6.2 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 448 5 1 7 3.8 COc1ccc(S(=O)(=O)n2cc(C)c3cc(Cl)cnc32)cc1NC1CCN(C)CC1 10.1021/jm300955x
164618283 184544 0 None -158 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 390 7 4 5 2.4 COc1ccc(C(C)NC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4848026 184544 0 None -158 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 390 7 4 5 2.4 COc1ccc(C(C)NC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1 10.1016/j.ejmech.2021.113190
164614645 185132 0 None -57 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 402 8 4 4 3.0 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(c1ccccc1)C(C)C 10.1016/j.ejmech.2021.113190
CHEMBL4856572 185132 0 None -57 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 402 8 4 4 3.0 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(c1ccccc1)C(C)C 10.1016/j.ejmech.2021.113190
11530223 8149 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 340 6 0 4 4.6 COc1cccc(C(C)c2c(CCN(C)C)sc3ccccc23)n1 10.1016/j.bmcl.2010.01.134
CHEMBL1091792 8149 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 340 6 0 4 4.6 COc1cccc(C(C)c2c(CCN(C)C)sc3ccccc23)n1 10.1016/j.bmcl.2010.01.134
45273828 195834 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 374 4 0 4 4.9 Fc1ccc(Cn2c(N3CCC(n4cccc4)CC3)nc3ccccc32)cc1 10.1016/j.bmcl.2009.05.086
CHEMBL558339 195834 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 374 4 0 4 4.9 Fc1ccc(Cn2c(N3CCC(n4cccc4)CC3)nc3ccccc32)cc1 10.1016/j.bmcl.2009.05.086
10343536 4962 0 None -3715 3 Human 5.2 pKi = 5.2 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 446 10 1 5 3.2 O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3cccc(F)c3)C2)cc1)C1CC1 10.1016/s0960-894x(02)00685-6
CHEMBL104809 4962 0 None -3715 3 Human 5.2 pKi = 5.2 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 446 10 1 5 3.2 O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3cccc(F)c3)C2)cc1)C1CC1 10.1016/s0960-894x(02)00685-6
132060746 163070 0 None -3 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-Pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 405 4 0 4 4.4 O=C(OCc1ccccc1)N1Cc2ccc(N3CCN(C4CCCC4)CC3)cc2C1 10.1016/j.ejmech.2018.02.024
CHEMBL4176474 163070 0 None -3 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-Pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 405 4 0 4 4.4 O=C(OCc1ccccc1)N1Cc2ccc(N3CCN(C4CCCC4)CC3)cc2C1 10.1016/j.ejmech.2018.02.024
91864602 140738 0 None -169 8 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 313 5 0 2 4.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818047 140738 0 None -169 8 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 313 5 0 2 4.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.05.053
44301676 199197 0 None 8 2 Rat 8.2 pKi = 8.2 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
ChEMBL 396 11 1 3 5.3 CN(CCCCCc1c[nH]cn1)CCC(c1ccc(Cl)cc1)c1ccccn1 10.1016/s0960-894x(03)00357-3
CHEMBL58973 199197 0 None 8 2 Rat 8.2 pKi = 8.2 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
ChEMBL 396 11 1 3 5.3 CN(CCCCCc1c[nH]cn1)CCC(c1ccc(Cl)cc1)c1ccccn1 10.1016/s0960-894x(03)00357-3
44326357 111609 0 None 2 3 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 308 2 0 3 3.9 CN(C)CC1C[C@@H]2c3ccccc3N(C)c3ccccc3[C@H]2O1 10.1016/j.bmcl.2004.03.069
CHEMBL328356 111609 0 None 2 3 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 308 2 0 3 3.9 CN(C)CC1C[C@@H]2c3ccccc3N(C)c3ccccc3[C@H]2O1 10.1016/j.bmcl.2004.03.069
5074 3332 80 None -10 30 Guinea pig 8.2 pKi = 8.2 Binding
Binding constant against histamine H1 receptor (in vitro)Binding constant against histamine H1 receptor (in vitro)
ChEMBL 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 10.1021/jm00112a025
97 3332 80 None -10 30 Guinea pig 8.2 pKi = 8.2 Binding
Binding constant against histamine H1 receptor (in vitro)Binding constant against histamine H1 receptor (in vitro)
ChEMBL 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 10.1021/jm00112a025
CHEMBL267777 3332 80 None -10 30 Guinea pig 8.2 pKi = 8.2 Binding
Binding constant against histamine H1 receptor (in vitro)Binding constant against histamine H1 receptor (in vitro)
ChEMBL 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 10.1021/jm00112a025
DB12693 3332 80 None -10 30 Guinea pig 8.2 pKi = 8.2 Binding
Binding constant against histamine H1 receptor (in vitro)Binding constant against histamine H1 receptor (in vitro)
ChEMBL 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 10.1021/jm00112a025
44521013 199793 0 None 13 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cellsDisplacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cells
ChEMBL 251 3 0 1 3.7 CN(C)CCC1c2ccccc2Cc2ccccc21 10.1016/j.bmc.2009.08.016
CHEMBL593988 199793 0 None 13 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cellsDisplacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cells
ChEMBL 251 3 0 1 3.7 CN(C)CCC1c2ccccc2Cc2ccccc21 10.1016/j.bmc.2009.08.016
23722970 69020 21 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 267 4 1 2 3.4 c1ccc(Cc2ccccc2OC2CCNCC2)cc1 10.1021/jm2011589
CHEMBL1923521 69020 21 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 267 4 1 2 3.4 c1ccc(Cc2ccccc2OC2CCNCC2)cc1 10.1021/jm2011589
CHEMBL3977546 69020 21 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 267 4 1 2 3.4 c1ccc(Cc2ccccc2OC2CCNCC2)cc1 10.1021/jm2011589
135515431 4247 34 None 3 3 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity of compound against histamine H1 neuronal receptorIn vitro binding affinity of compound against histamine H1 neuronal receptor
ChEMBL 328 1 2 6 2.6 CN1CCN(C2=Nc3ccccc3Nc3sc(CO)cc32)CC1 10.1016/S0960-894X(96)00567-7
CHEMBL100454 4247 34 None 3 3 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity of compound against histamine H1 neuronal receptorIn vitro binding affinity of compound against histamine H1 neuronal receptor
ChEMBL 328 1 2 6 2.6 CN1CCN(C2=Nc3ccccc3Nc3sc(CO)cc32)CC1 10.1016/S0960-894X(96)00567-7
15749430 102513 0 None - 1 Guinea pig 8.2 pKi = 8.2 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 337 5 1 3 4.1 CN(C)CCC/C=C1\c2ccccc2COc2ccc(C(=O)O)cc21 10.1021/jm00089a020
CHEMBL304042 102513 0 None - 1 Guinea pig 8.2 pKi = 8.2 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 337 5 1 3 4.1 CN(C)CCC/C=C1\c2ccccc2COc2ccc(C(=O)O)cc21 10.1021/jm00089a020
69262172 81293 1 None -3 2 Human 8.2 pKi = 8.2 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 462 6 1 4 5.5 O=C(O)c1ccccc1N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158822 81293 1 None -3 2 Human 8.2 pKi = 8.2 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 462 6 1 4 5.5 O=C(O)c1ccccc1N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
59296010 84214 0 None -3 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 490 7 3 6 2.9 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1n[nH]c(=O)c2ccccc12 10.1016/j.bmcl.2012.09.113
CHEMBL2208431 84214 0 None -3 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 490 7 3 6 2.9 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1n[nH]c(=O)c2ccccc12 10.1016/j.bmcl.2012.09.113
59295958 84012 0 None -1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 507 7 3 5 3.6 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c(=O)c2ccc(F)cc12 10.1016/j.bmcl.2012.09.112
CHEMBL2207280 84012 0 None -1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 507 7 3 5 3.6 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c(=O)c2ccc(F)cc12 10.1016/j.bmcl.2012.09.112
23722970 69020 21 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 267 4 1 2 3.4 c1ccc(Cc2ccccc2OC2CCNCC2)cc1 10.1021/jm2011589
CHEMBL1923521 69020 21 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 267 4 1 2 3.4 c1ccc(Cc2ccccc2OC2CCNCC2)cc1 10.1021/jm2011589
CHEMBL3977546 69020 21 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 267 4 1 2 3.4 c1ccc(Cc2ccccc2OC2CCNCC2)cc1 10.1021/jm2011589
134132469 154561 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 301 4 1 2 4.1 Clc1ccc(Cc2ccccc2OC2CCNCC2)cc1 10.1021/acs.jmedchem.6b00981
CHEMBL3910939 154561 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 301 4 1 2 4.1 Clc1ccc(Cc2ccccc2OC2CCNCC2)cc1 10.1021/acs.jmedchem.6b00981
CHEMBL3991161 154561 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 301 4 1 2 4.1 Clc1ccc(Cc2ccccc2OC2CCNCC2)cc1 10.1021/acs.jmedchem.6b00981
134155595 154595 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 267 6 0 2 3.4 c1ccc(Cc2ccccc2OCCN2CCC2)cc1 10.1021/acs.jmedchem.6b00981
CHEMBL3962094 154595 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 267 6 0 2 3.4 c1ccc(Cc2ccccc2OCCN2CCC2)cc1 10.1021/acs.jmedchem.6b00981
CHEMBL3991444 154595 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 267 6 0 2 3.4 c1ccc(Cc2ccccc2OCCN2CCC2)cc1 10.1021/acs.jmedchem.6b00981
135398745 2914 112 None -2 65 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
47 2914 112 None -2 65 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
CHEMBL715 2914 112 None -2 65 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
DB00334 2914 112 None -2 65 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
11291 98796 25 None 4 2 Guinea pig 8.2 pKi = 8.2 Binding
Inhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 minInhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 min
ChEMBL 261 1 0 1 3.9 CN1CCC2=C(C1)C(c1ccccc1)c1ccccc12 10.1021/jm00017a019
CHEMBL278398 98796 25 None 4 2 Guinea pig 8.2 pKi = 8.2 Binding
Inhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 minInhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 min
ChEMBL 261 1 0 1 3.9 CN1CCC2=C(C1)C(c1ccccc1)c1ccccc12 10.1021/jm00017a019
5255691 11014 1 None - 1 Rat 8.2 pKi = 8.2 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 313 1 1 3 2.8 Clc1ccc2c(c1)CCc1cccnc1C2N1CCNCC1 10.1016/s0960-894x(98)00626-x
CHEMBL117406 11014 1 None - 1 Rat 8.2 pKi = 8.2 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 313 1 1 3 2.8 Clc1ccc2c(c1)CCc1cccnc1C2N1CCNCC1 10.1016/s0960-894x(98)00626-x
44343920 12790 0 None - 1 Rat 8.2 pKi = 8.2 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 327 1 0 3 3.2 CN1CCN(C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/s0960-894x(98)00626-x
CHEMBL118807 12790 0 None - 1 Rat 8.2 pKi = 8.2 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 327 1 0 3 3.2 CN1CCN(C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/s0960-894x(98)00626-x
155554396 174617 0 None 158 2 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysisDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysis
ChEMBL 304 5 0 4 1.4 CN1CCc2ccc(OCCCN3CCOCC3)cc2C1=O 10.1016/j.bmcl.2019.04.015
CHEMBL4557586 174617 0 None 158 2 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysisDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysis
ChEMBL 304 5 0 4 1.4 CN1CCc2ccc(OCCCN3CCOCC3)cc2C1=O 10.1016/j.bmcl.2019.04.015
45270339 195398 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 406 4 0 4 4.2 O=C1CCCCN1C1CCN(c2nc3ccccc3n2Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2009.05.086
CHEMBL552026 195398 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 406 4 0 4 4.2 O=C1CCCCN1C1CCN(c2nc3ccccc3n2Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2009.05.086
11393666 192986 0 None -16 19 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]pyrilamine from recombinant human H1 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]pyrilamine from recombinant human H1 receptor measured after 60 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
CHEMBL5201983 192986 0 None -16 19 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]pyrilamine from recombinant human H1 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]pyrilamine from recombinant human H1 receptor measured after 60 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
CHEMBL5222597 192986 0 None -16 19 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]pyrilamine from recombinant human H1 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]pyrilamine from recombinant human H1 receptor measured after 60 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
53322838 57762 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 375 7 0 4 5.2 C[C@H](C1=C(CCN(C)Cc2cccs2)Cc2ccccc21)c1cnccn1 10.1016/j.bmcl.2010.12.053
CHEMBL1669419 57762 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 375 7 0 4 5.2 C[C@H](C1=C(CCN(C)Cc2cccs2)Cc2ccccc21)c1cnccn1 10.1016/j.bmcl.2010.12.053
135398737 958 93 None -2 89 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2014.01.012
38 958 93 None -2 89 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2014.01.012
722 958 93 None -2 89 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2014.01.012
CHEMBL42 958 93 None -2 89 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2014.01.012
DB00363 958 93 None -2 89 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2014.01.012
45272895 195657 18 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 389 4 0 5 4.6 Cc1cnn(C2CCN(c3nc4ccccc4n3Cc3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2009.05.086
CHEMBL556450 195657 18 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 389 4 0 5 4.6 Cc1cnn(C2CCN(c3nc4ccccc4n3Cc3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2009.05.086
45272895 195657 18 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation counting
ChEMBL 389 4 0 5 4.6 Cc1cnn(C2CCN(c3nc4ccccc4n3Cc3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.03.027
CHEMBL556450 195657 18 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation counting
ChEMBL 389 4 0 5 4.6 Cc1cnn(C2CCN(c3nc4ccccc4n3Cc3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.03.027
9980189 115227 0 None - 1 Guinea pig 8.2 pKi = 8.2 Binding
Inhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptorInhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptor
ChEMBL 431 5 1 4 5.2 O=C(O)c1ccc2c(c1)C(SCCN1CCc3ccccc3C1)c1ccccc1CO2 10.1021/jm00055a013
CHEMBL334678 115227 0 None - 1 Guinea pig 8.2 pKi = 8.2 Binding
Inhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptorInhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptor
ChEMBL 431 5 1 4 5.2 O=C(O)c1ccc2c(c1)C(SCCN1CCc3ccccc3C1)c1ccccc1CO2 10.1021/jm00055a013
44304402 201212 0 None -3 3 Human 7.2 pKi = 7.2 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 415 12 0 6 4.5 CCCCCC(=O)c1ccc(OCCCN2CCN(Cc3nccs3)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL60360 201212 0 None -3 3 Human 7.2 pKi = 7.2 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 415 12 0 6 4.5 CCCCCC(=O)c1ccc(OCCCN2CCN(Cc3nccs3)CC2)cc1 10.1016/s0960-894x(02)00309-8
23562970 100913 0 None -10 2 Rat 6.2 pKi = 6.2 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
ChEMBL 340 8 2 3 3.8 Clc1ccc(C(CCNCCc2c[nH]cn2)c2ccccn2)cc1 10.1016/s0960-894x(03)00357-3
CHEMBL293895 100913 0 None -10 2 Rat 6.2 pKi = 6.2 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
ChEMBL 340 8 2 3 3.8 Clc1ccc(C(CCNCCc2c[nH]cn2)c2ccccn2)cc1 10.1016/s0960-894x(03)00357-3
1204 1932 119 None -501 24 Human 5.2 pKi = 5.2 Binding
Binding affinity to histamine H1 receptor (unknown origin)Binding affinity to histamine H1 receptor (unknown origin)
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
1247 1932 119 None -501 24 Human 5.2 pKi = 5.2 Binding
Binding affinity to histamine H1 receptor (unknown origin)Binding affinity to histamine H1 receptor (unknown origin)
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
1375 1932 119 None -501 24 Human 5.2 pKi = 5.2 Binding
Binding affinity to histamine H1 receptor (unknown origin)Binding affinity to histamine H1 receptor (unknown origin)
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
774 1932 119 None -501 24 Human 5.2 pKi = 5.2 Binding
Binding affinity to histamine H1 receptor (unknown origin)Binding affinity to histamine H1 receptor (unknown origin)
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
CHEMBL90 1932 119 None -501 24 Human 5.2 pKi = 5.2 Binding
Binding affinity to histamine H1 receptor (unknown origin)Binding affinity to histamine H1 receptor (unknown origin)
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
DB05381 1932 119 None -501 24 Human 5.2 pKi = 5.2 Binding
Binding affinity to histamine H1 receptor (unknown origin)Binding affinity to histamine H1 receptor (unknown origin)
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
10339767 53188 0 None -602 3 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]- pyrilamine from rat brain membrane Histamine H1 receptorDisplacement of [3H]- pyrilamine from rat brain membrane Histamine H1 receptor
ChEMBL 380 6 0 4 4.8 Cn1c(=O)sc2cc(CCCCN3CCC(c4ccccc4)CC3)ccc21 10.1016/s0960-894x(02)00123-3
CHEMBL15986 53188 0 None -602 3 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]- pyrilamine from rat brain membrane Histamine H1 receptorDisplacement of [3H]- pyrilamine from rat brain membrane Histamine H1 receptor
ChEMBL 380 6 0 4 4.8 Cn1c(=O)sc2cc(CCCCN3CCC(c4ccccc4)CC3)ccc21 10.1016/s0960-894x(02)00123-3
44333987 108549 0 None -66 3 Human 4.2 pKi = 4.2 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 433 9 2 6 2.8 CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@H](C)NC(=O)OC(C)(C)C)C2)cc1 10.1016/s0960-894x(02)00685-6
CHEMBL320174 108549 0 None -66 3 Human 4.2 pKi = 4.2 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 433 9 2 6 2.8 CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@H](C)NC(=O)OC(C)(C)C)C2)cc1 10.1016/s0960-894x(02)00685-6
44304088 202387 0 None -23 3 Human 6.2 pKi = 6.2 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 402 8 0 5 4.0 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)C3CCCCC3)cc2)CC1 10.1016/s0960-894x(02)00309-8
CHEMBL61070 202387 0 None -23 3 Human 6.2 pKi = 6.2 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 402 8 0 5 4.0 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)C3CCCCC3)cc2)CC1 10.1016/s0960-894x(02)00309-8
91864602 140738 0 None -169 8 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 313 5 0 2 4.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818047 140738 0 None -169 8 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 313 5 0 2 4.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.05.053
57400700 67878 0 None -83 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
ChEMBL 470 8 1 6 3.4 COc1ccc(CN(CCN2CCN(C(=O)c3nc4ccccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
CHEMBL1910380 67878 0 None -83 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
ChEMBL 470 8 1 6 3.4 COc1ccc(CN(CCN2CCN(C(=O)c3nc4ccccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
18539962 102131 0 None -223 3 Human 5.2 pKi = 5.2 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 318 10 1 4 3.1 CCCCCC(=O)c1ccc(OCCCN2CCNCC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL302445 102131 0 None -223 3 Human 5.2 pKi = 5.2 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 318 10 1 4 3.1 CCCCCC(=O)c1ccc(OCCCN2CCNCC2)cc1 10.1016/s0960-894x(02)00309-8
168283321 192895 0 None -2 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 364 7 4 4 2.3 Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1 10.1021/acs.jmedchem.1c00692
CHEMBL5183015 192895 0 None -2 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 364 7 4 4 2.3 Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1 10.1021/acs.jmedchem.1c00692
CHEMBL5222057 192895 0 None -2 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 364 7 4 4 2.3 Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1 10.1021/acs.jmedchem.1c00692
127052293 140238 3 None -131 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 incubated for 60 mins by liquid scintillation counting method
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805361 140238 3 None -131 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 incubated for 60 mins by liquid scintillation counting method
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
242 470 124 None -22 51 Human 7.2 pKi = 7.2 Binding
Binding affinity to H1 histamine receptor (unknown origin)Binding affinity to H1 histamine receptor (unknown origin)
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2020.127681
34 470 124 None -22 51 Human 7.2 pKi = 7.2 Binding
Binding affinity to H1 histamine receptor (unknown origin)Binding affinity to H1 histamine receptor (unknown origin)
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2020.127681
60795 470 124 None -22 51 Human 7.2 pKi = 7.2 Binding
Binding affinity to H1 histamine receptor (unknown origin)Binding affinity to H1 histamine receptor (unknown origin)
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2020.127681
CHEMBL1112 470 124 None -22 51 Human 7.2 pKi = 7.2 Binding
Binding affinity to H1 histamine receptor (unknown origin)Binding affinity to H1 histamine receptor (unknown origin)
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2020.127681
DB01238 470 124 None -22 51 Human 7.2 pKi = 7.2 Binding
Binding affinity to H1 histamine receptor (unknown origin)Binding affinity to H1 histamine receptor (unknown origin)
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2020.127681
57399432 70465 0 None -2 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-Pyrilamine from human histamine H1 receptor by liquid scintillation counterDisplacement of [3H]-Pyrilamine from human histamine H1 receptor by liquid scintillation counter
ChEMBL 399 6 0 4 5.5 Clc1ccc(N2CCCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2012.01.022
CHEMBL1946254 70465 0 None -2 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-Pyrilamine from human histamine H1 receptor by liquid scintillation counterDisplacement of [3H]-Pyrilamine from human histamine H1 receptor by liquid scintillation counter
ChEMBL 399 6 0 4 5.5 Clc1ccc(N2CCCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2012.01.022
45485462 197686 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation counting
ChEMBL 419 8 1 2 6.6 CC1CCC(CCCCN2CCC(C(O)(c3ccccc3)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2009.07.047
CHEMBL571174 197686 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation counting
ChEMBL 419 8 1 2 6.6 CC1CCC(CCCCN2CCC(C(O)(c3ccccc3)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2009.07.047
29136870 69021 7 None 46 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 301 2 0 7 0.7 CN1CCN(c2nc(N3CCCC3)c3cnn(C)c3n2)CC1 10.1021/jm2011589
CHEMBL1923522 69021 7 None 46 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 301 2 0 7 0.7 CN1CCN(c2nc(N3CCCC3)c3cnn(C)c3n2)CC1 10.1021/jm2011589
289 242 12 None -56 14 Human 6.2 pKi = 6.2 Binding
Binding affinity to human histamine H1 receptor by radioligand displacement assayBinding affinity to human histamine H1 receptor by radioligand displacement assay
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm100697g
9948320 242 12 None -56 14 Human 6.2 pKi = 6.2 Binding
Binding affinity to human histamine H1 receptor by radioligand displacement assayBinding affinity to human histamine H1 receptor by radioligand displacement assay
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm100697g
CHEMBL1242950 242 12 None -56 14 Human 6.2 pKi = 6.2 Binding
Binding affinity to human histamine H1 receptor by radioligand displacement assayBinding affinity to human histamine H1 receptor by radioligand displacement assay
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm100697g
44288877 168599 0 None -87 5 Human 6.2 pKi = 6.2 Binding
Selectivity screen against human Histamine H1 receptorSelectivity screen against human Histamine H1 receptor
ChEMBL 549 7 1 5 4.3 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1C 10.1016/s0960-894x(99)00696-4
CHEMBL43594 168599 0 None -87 5 Human 6.2 pKi = 6.2 Binding
Selectivity screen against human Histamine H1 receptorSelectivity screen against human Histamine H1 receptor
ChEMBL 549 7 1 5 4.3 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1C 10.1016/s0960-894x(99)00696-4
44304031 100672 0 None -85 3 Human 6.2 pKi = 6.2 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 452 10 0 6 4.1 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)/C=C/c3ccc(OC)cc3)cc2)CC1 10.1016/s0960-894x(02)00309-8
CHEMBL292275 100672 0 None -85 3 Human 6.2 pKi = 6.2 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 452 10 0 6 4.1 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)/C=C/c3ccc(OC)cc3)cc2)CC1 10.1016/s0960-894x(02)00309-8
164611342 185088 0 None -134 6 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 346 6 4 4 1.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4856005 185088 0 None -134 6 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 346 6 4 4 1.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccccc1 10.1016/j.ejmech.2021.113190
3041343 109799 5 None -10 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 377 6 1 3 3.4 O=C1NC(c2ccccc2)(c2ccccc2)C(=O)N1CCCN1CCCCC1 10.1016/j.ejmech.2014.03.014
CHEMBL3233067 109799 5 None -10 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysis
ChEMBL 377 6 1 3 3.4 O=C1NC(c2ccccc2)(c2ccccc2)C(=O)N1CCCN1CCCCC1 10.1016/j.ejmech.2014.03.014
132060770 162639 0 None 5 10 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-Pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 451 7 0 6 3.5 CCOC(=O)CCN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)CC3)CC1 10.1016/j.ejmech.2018.02.024
CHEMBL4169689 162639 0 None 5 10 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-Pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 451 7 0 6 3.5 CCOC(=O)CCN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)CC3)CC1 10.1016/j.ejmech.2018.02.024
29136870 69021 7 None 46 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 301 2 0 7 0.7 CN1CCN(c2nc(N3CCCC3)c3cnn(C)c3n2)CC1 10.1021/jm2011589
CHEMBL1923522 69021 7 None 46 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 301 2 0 7 0.7 CN1CCN(c2nc(N3CCCC3)c3cnn(C)c3n2)CC1 10.1021/jm2011589
3069135 70164 3 None -8 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]pyrilamine from human H1 receptor by liquid scintillation countingDisplacement of [3H]pyrilamine from human H1 receptor by liquid scintillation counting
ChEMBL 314 6 0 3 3.4 Fc1ccc(OCCCN2CCN(c3ccccc3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940412 70164 3 None -8 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]pyrilamine from human H1 receptor by liquid scintillation countingDisplacement of [3H]pyrilamine from human H1 receptor by liquid scintillation counting
ChEMBL 314 6 0 3 3.4 Fc1ccc(OCCCN2CCN(c3ccccc3)CC2)cc1 10.1016/j.bmc.2011.12.019
44334042 163489 0 None -562 3 Human 5.2 pKi = 5.2 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 453 10 1 6 3.0 N#Cc1ccccc1S(=O)(=O)N[C@H]1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)C1 10.1016/s0960-894x(02)00685-6
CHEMBL420108 163489 0 None -562 3 Human 5.2 pKi = 5.2 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 453 10 1 6 3.0 N#Cc1ccccc1S(=O)(=O)N[C@H]1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)C1 10.1016/s0960-894x(02)00685-6
11848624 89146 0 None -15 6 Human 6.2 pKi = 6.2 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 381 7 1 6 4.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC 10.1021/jm701143p
CHEMBL236587 89146 0 None -15 6 Human 6.2 pKi = 6.2 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 381 7 1 6 4.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC 10.1021/jm701143p
11848624 89146 0 None -15 6 Human 6.2 pKi = 6.2 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 381 7 1 6 4.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
CHEMBL236587 89146 0 None -15 6 Human 6.2 pKi = 6.2 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 381 7 1 6 4.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
46884637 7723 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 293 5 0 3 3.3 Cc1nccnc1CC1=C(CCN(C)C)Cc2ccccc21 10.1016/j.bmcl.2010.02.055
CHEMBL1088898 7723 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 293 5 0 3 3.3 Cc1nccnc1CC1=C(CCN(C)C)Cc2ccccc21 10.1016/j.bmcl.2010.02.055
44288917 100255 0 None -34 4 Human 7.2 pKi = 7.2 Binding
Selectivity screen against human Histamine H1 receptorSelectivity screen against human Histamine H1 receptor
ChEMBL 510 7 2 4 4.0 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1 10.1016/s0960-894x(99)00696-4
CHEMBL288768 100255 0 None -34 4 Human 7.2 pKi = 7.2 Binding
Selectivity screen against human Histamine H1 receptorSelectivity screen against human Histamine H1 receptor
ChEMBL 510 7 2 4 4.0 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1 10.1016/s0960-894x(99)00696-4
71072104 81263 0 None -15 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 520 9 1 5 5.3 COc1ccccc1C[C@@H](C(=O)O)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158775 81263 0 None -15 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 520 9 1 5 5.3 COc1ccccc1C[C@@H](C(=O)O)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
71460416 81264 0 None -2 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 520 9 1 5 5.3 COc1ccc(C[C@@H](C(=O)O)N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.103
CHEMBL2158776 81264 0 None -2 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 520 9 1 5 5.3 COc1ccc(C[C@@H](C(=O)O)N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.103
66615617 81276 0 None -31 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 504 8 1 4 5.6 Cc1c(OC2CCN(CC3CCN([C@@H](Cc4ccccc4)C(=O)O)CC3)CC2)ccc(Cl)c1Cl 10.1016/j.bmcl.2012.08.103
CHEMBL2158788 81276 0 None -31 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 504 8 1 4 5.6 Cc1c(OC2CCN(CC3CCN([C@@H](Cc4ccccc4)C(=O)O)CC3)CC2)ccc(Cl)c1Cl 10.1016/j.bmcl.2012.08.103
10151756 81286 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 462 6 1 4 5.1 O=C(O)C(c1ccccc1)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158815 81286 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 462 6 1 4 5.1 O=C(O)C(c1ccccc1)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
68846936 81287 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 476 7 1 4 5.4 O=C(O)C(c1ccccc1)N1CCCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.08.103
CHEMBL2158816 81287 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 476 7 1 4 5.4 O=C(O)C(c1ccccc1)N1CCCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.08.103
69260851 81295 1 None 2 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 462 6 1 4 5.5 O=C(O)c1ccc(N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.103
CHEMBL2158824 81295 1 None 2 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 462 6 1 4 5.5 O=C(O)c1ccc(N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.103
69347719 81303 1 None -3 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 476 7 1 4 5.4 O=C(O)c1ccccc1CN1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158831 81303 1 None -3 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 476 7 1 4 5.4 O=C(O)c1ccccc1CN1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
59296039 84210 0 None -15 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 467 8 3 6 3.2 COc1cc(C(=O)NC[C@@H](O)CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)ccc1N 10.1016/j.bmcl.2012.09.113
CHEMBL2208427 84210 0 None -15 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 467 8 3 6 3.2 COc1cc(C(=O)NC[C@@H](O)CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)ccc1N 10.1016/j.bmcl.2012.09.113
59296024 84009 0 None -9 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 547 8 3 7 2.5 Cc1cc(Cl)ccc1OC1CCN(C[C@H](O)CNC(=O)c2c[nH]c(=O)c3ccc(S(C)(=O)=O)cc23)CC1 10.1016/j.bmcl.2012.09.112
CHEMBL2207277 84009 0 None -9 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 547 8 3 7 2.5 Cc1cc(Cl)ccc1OC1CCN(C[C@H](O)CNC(=O)c2c[nH]c(=O)c3ccc(S(C)(=O)=O)cc23)CC1 10.1016/j.bmcl.2012.09.112
59295928 84015 0 None -63 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 581 8 3 7 3.2 Cc1c(Cl)ccc(OC2CCN(C[C@H](O)CNC(=O)c3c[nH]c(=O)c4ccc(S(C)(=O)=O)cc34)CC2)c1Cl 10.1016/j.bmcl.2012.09.112
CHEMBL2207283 84015 0 None -63 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 581 8 3 7 3.2 Cc1c(Cl)ccc(OC2CCN(C[C@H](O)CNC(=O)c3c[nH]c(=O)c4ccc(S(C)(=O)=O)cc34)CC2)c1Cl 10.1016/j.bmcl.2012.09.112
43229249 140817 1 None -16 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 279 5 0 2 3.7 O=C(CCCN1CCc2ccccc2C1)c1ccccc1 10.1016/j.bmc.2016.05.053
CHEMBL3818989 140817 1 None -16 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 279 5 0 2 3.7 O=C(CCCN1CCc2ccccc2C1)c1ccccc1 10.1016/j.bmc.2016.05.053
1222 881 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor N7.45Q mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor N7.45Q mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/nchembio714
2678 881 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor N7.45Q mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor N7.45Q mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/nchembio714
581 881 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor N7.45Q mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor N7.45Q mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/nchembio714
CHEMBL1000 881 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor N7.45Q mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor N7.45Q mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/nchembio714
DB00341 881 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor N7.45Q mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor N7.45Q mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/nchembio714
1222 881 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor N7.45S mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor N7.45S mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/nchembio714
2678 881 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor N7.45S mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor N7.45S mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/nchembio714
581 881 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor N7.45S mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor N7.45S mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/nchembio714
CHEMBL1000 881 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor N7.45S mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor N7.45S mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/nchembio714
DB00341 881 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor N7.45S mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor N7.45S mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/nchembio714
134145497 149163 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 309 6 0 2 4.5 c1ccc(Cc2ccccc2OCCN2CCCCCC2)cc1 10.1021/acs.jmedchem.6b00981
CHEMBL3943575 149163 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 309 6 0 2 4.5 c1ccc(Cc2ccccc2OCCN2CCCCCC2)cc1 10.1021/acs.jmedchem.6b00981
129103318 167314 0 None -870 14 Human 6.2 pKi = 6.2 Binding
Binding affinity to H1 receptor (unknown origin)Binding affinity to H1 receptor (unknown origin)
ChEMBL 475 7 0 5 5.0 O=C(CCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1016/j.ejmech.2020.112709
CHEMBL4293999 167314 0 None -870 14 Human 6.2 pKi = 6.2 Binding
Binding affinity to H1 receptor (unknown origin)Binding affinity to H1 receptor (unknown origin)
ChEMBL 475 7 0 5 5.0 O=C(CCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1016/j.ejmech.2020.112709
129103318 167314 0 None -870 14 Guinea pig 6.2 pKi = 6.2 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by liquid scintillation countingDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by liquid scintillation counting
ChEMBL 475 7 0 5 5.0 O=C(CCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1021/acs.jmedchem.8b01096
CHEMBL4293999 167314 0 None -870 14 Guinea pig 6.2 pKi = 6.2 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by liquid scintillation countingDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by liquid scintillation counting
ChEMBL 475 7 0 5 5.0 O=C(CCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1021/acs.jmedchem.8b01096
10263017 207462 2 None 1 3 Guinea pig 6.2 pKi = 6.2 Binding
Binding affinity against H1 receptor of guinea pig by the displacement of [3H]mepyramine, bound to membranes of CHO cellsBinding affinity against H1 receptor of guinea pig by the displacement of [3H]mepyramine, bound to membranes of CHO cells
ChEMBL 223 10 2 2 3.0 NCCCCCCCCCCc1c[nH]cn1 10.1021/jm00002a008
CHEMBL94249 207462 2 None 1 3 Guinea pig 6.2 pKi = 6.2 Binding
Binding affinity against H1 receptor of guinea pig by the displacement of [3H]mepyramine, bound to membranes of CHO cellsBinding affinity against H1 receptor of guinea pig by the displacement of [3H]mepyramine, bound to membranes of CHO cells
ChEMBL 223 10 2 2 3.0 NCCCCCCCCCCc1c[nH]cn1 10.1021/jm00002a008
127036982 137467 0 None 3 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 525 6 1 6 5.9 COc1ccc(CNc2nc(N3CCN(C)CC3)nc3c2CCc2ccccc2-3)cc1-c1ccc(Cl)cc1 10.1016/j.bmcl.2015.12.035
CHEMBL3753784 137467 0 None 3 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 525 6 1 6 5.9 COc1ccc(CNc2nc(N3CCN(C)CC3)nc3c2CCc2ccccc2-3)cc1-c1ccc(Cl)cc1 10.1016/j.bmcl.2015.12.035
550981 69031 12 None -2 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 280 5 2 3 2.9 OC(CNC1CC1)Cn1c2ccccc2c2ccccc21 10.1021/jm2011589
CHEMBL1923533 69031 12 None -2 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 280 5 2 3 2.9 OC(CNC1CC1)Cn1c2ccccc2c2ccccc21 10.1021/jm2011589
10805119 54602 0 None -3235 2 Guinea pig 4.2 pKi = 4.2 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 313 5 2 3 3.6 O=C(Nc1cccc(C(F)(F)F)c1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL16108 54602 0 None -3235 2 Guinea pig 4.2 pKi = 4.2 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 313 5 2 3 3.6 O=C(Nc1cccc(C(F)(F)F)c1)OCCCc1c[nH]cn1 10.1021/jm9507688
10062176 55835 0 None -15488 2 Guinea pig 4.2 pKi = 4.2 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 279 5 2 3 3.2 O=C(Nc1ccc(Cl)cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL16231 55835 0 None -15488 2 Guinea pig 4.2 pKi = 4.2 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 279 5 2 3 3.2 O=C(Nc1ccc(Cl)cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
10612308 98211 0 None -6309 2 Guinea pig 4.2 pKi = 4.2 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 273 7 2 3 2.3 O=C(NCCc1ccccc1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL274262 98211 0 None -6309 2 Guinea pig 4.2 pKi = 4.2 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 273 7 2 3 2.3 O=C(NCCc1ccccc1)OCCCc1c[nH]cn1 10.1021/jm9507688
164612760 184718 0 None -54 4 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 390 7 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4850490 184718 0 None -54 4 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 390 7 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
13091273 182438 0 None -275 6 Human 6.2 pKi = 6.2 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 367 6 1 3 4.3 O=C(CCCN1C2CCC1CC(O)(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL478617 182438 0 None -275 6 Human 6.2 pKi = 6.2 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 367 6 1 3 4.3 O=C(CCCN1C2CCC1CC(O)(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL553327 182438 0 None -275 6 Human 6.2 pKi = 6.2 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 367 6 1 3 4.3 O=C(CCCN1C2CCC1CC(O)(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
119812 199730 65 None 23 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cellsDisplacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cells
ChEMBL 225 5 1 1 3.4 CNCCC(c1ccccc1)c1ccccc1 10.1016/j.bmc.2009.08.016
CHEMBL593494 199730 65 None 23 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cellsDisplacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cells
ChEMBL 225 5 1 1 3.4 CNCCC(c1ccccc1)c1ccccc1 10.1016/j.bmc.2009.08.016
9932698 17909 0 None -354 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cellsDisplacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 435 6 2 4 3.4 NCc1ccc2c(c1)c(C1CCN(CCN3CCNC3=O)CC1)cn2-c1ccc(F)cc1 10.1021/jm100652h
CHEMBL1259172 17909 0 None -354 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cellsDisplacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 435 6 2 4 3.4 NCc1ccc2c(c1)c(C1CCN(CCN3CCNC3=O)CC1)cn2-c1ccc(F)cc1 10.1021/jm100652h
52946023 17914 0 None -95 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cellsDisplacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 477 7 2 4 3.6 CC(=O)NCc1ccc2c(c1)c(C1CCN(CCN3CCNC3=O)CC1)cn2-c1ccc(F)cc1 10.1021/jm100652h
CHEMBL1259187 17914 0 None -95 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cellsDisplacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 477 7 2 4 3.6 CC(=O)NCc1ccc2c(c1)c(C1CCN(CCN3CCNC3=O)CC1)cn2-c1ccc(F)cc1 10.1021/jm100652h
45485529 197718 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation counting
ChEMBL 385 6 1 2 5.2 Cc1ccc(CCN2CCC(C(O)(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2009.07.047
CHEMBL571391 197718 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation counting
ChEMBL 385 6 1 2 5.2 Cc1ccc(CCN2CCC(C(O)(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2009.07.047
49841845 69739 0 None -1288 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]histamine from human H1 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H1 receptor expressed in HEK cell membranes
ChEMBL 309 2 1 6 2.2 CN1CCN(c2nc(N)nc3cc(-c4ccco4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL1935573 69739 0 None -1288 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]histamine from human H1 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H1 receptor expressed in HEK cell membranes
ChEMBL 309 2 1 6 2.2 CN1CCN(c2nc(N)nc3cc(-c4ccco4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
168294767 193019 0 None -3235 20 Human 5.2 pKi = 5.2 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5207281 193019 0 None -3235 20 Human 5.2 pKi = 5.2 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222802 193019 0 None -3235 20 Human 5.2 pKi = 5.2 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
71454294 84077 0 None -1412 7 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis
ChEMBL 431 6 0 5 4.0 COc1ccccc1N1CCN(Cc2cc(CN3CCOCC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207639 84077 0 None -1412 7 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis
ChEMBL 431 6 0 5 4.0 COc1ccccc1N1CCN(Cc2cc(CN3CCOCC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
6918107 78146 16 None -7 5 Rat 5.2 pKi = 5.2 Binding
The binding affinity was measured on histamine H1 receptor using [3H]- mepyramine as radioligand.The binding affinity was measured on histamine H1 receptor using [3H]- mepyramine as radioligand.
ChEMBL 319 2 0 4 3.5 Cc1nccn1C[C@H]1CCc2c(c3cccc4c3n2CCC4)C1=O 10.1021/jm00075a026
CHEMBL2103778 78146 16 None -7 5 Rat 5.2 pKi = 5.2 Binding
The binding affinity was measured on histamine H1 receptor using [3H]- mepyramine as radioligand.The binding affinity was measured on histamine H1 receptor using [3H]- mepyramine as radioligand.
ChEMBL 319 2 0 4 3.5 Cc1nccn1C[C@H]1CCc2c(c3cccc4c3n2CCC4)C1=O 10.1021/jm00075a026
127052293 140238 3 None -131 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 incubated for 60 mins by liquid scintillation counting method
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805361 140238 3 None -131 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 incubated for 60 mins by liquid scintillation counting method
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
15723 18539 111 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation counting
ChEMBL 267 3 2 2 2.9 OC(c1ccccc1)(c1ccccc1)C1CCNCC1 10.1016/j.bmcl.2009.07.047
CHEMBL127508 18539 111 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation counting
ChEMBL 267 3 2 2 2.9 OC(c1ccccc1)(c1ccccc1)C1CCNCC1 10.1016/j.bmcl.2009.07.047
44312568 204773 0 None - 1 Human 6.2 pKi = 6.2 Binding
In vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cellsIn vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 498 7 2 5 3.4 NC(=O)N(O)CCC#C[C@@H]1CC[C@@H](CN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)O1 10.1016/j.bmcl.2004.02.005
CHEMBL74779 204773 0 None - 1 Human 6.2 pKi = 6.2 Binding
In vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cellsIn vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 498 7 2 5 3.4 NC(=O)N(O)CCC#C[C@@H]1CC[C@@H](CN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)O1 10.1016/j.bmcl.2004.02.005
44304243 203199 0 None -48 3 Human 6.2 pKi = 6.2 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 374 13 0 4 4.6 CCCCCC(=O)c1ccc(OCCCN2CCN(CCCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL64334 203199 0 None -48 3 Human 6.2 pKi = 6.2 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 374 13 0 4 4.6 CCCCCC(=O)c1ccc(OCCCN2CCN(CCCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
10003483 4644 0 None -2454 3 Human 5.2 pKi = 5.2 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 442 10 1 5 3.4 Cc1cccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)c1 10.1016/s0960-894x(02)00685-6
CHEMBL103027 4644 0 None -2454 3 Human 5.2 pKi = 5.2 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 442 10 1 5 3.4 Cc1cccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)c1 10.1016/s0960-894x(02)00685-6
168294161 193006 0 None -3 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 360 6 4 4 3.3 CCCCCNC(=O)/N=C(\N)Nc1cccc(-c2sc(N)nc2C)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5204739 193006 0 None -3 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 360 6 4 4 3.3 CCCCCNC(=O)/N=C(\N)Nc1cccc(-c2sc(N)nc2C)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5222742 193006 0 None -3 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 360 6 4 4 3.3 CCCCCNC(=O)/N=C(\N)Nc1cccc(-c2sc(N)nc2C)c1 10.1021/acs.jmedchem.1c00692
57390694 70466 0 None -3 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-Pyrilamine from human histamine H1 receptor by liquid scintillation counterDisplacement of [3H]-Pyrilamine from human histamine H1 receptor by liquid scintillation counter
ChEMBL 385 5 0 4 5.1 Clc1ccc(N2CCCN(CCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2012.01.022
CHEMBL1946255 70466 0 None -3 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-Pyrilamine from human histamine H1 receptor by liquid scintillation counterDisplacement of [3H]-Pyrilamine from human histamine H1 receptor by liquid scintillation counter
ChEMBL 385 5 0 4 5.1 Clc1ccc(N2CCCN(CCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2012.01.022
44582705 186996 0 None -4 13 Human 6.2 pKi = 6.2 Binding
Inhibition of human cloned histamine H1 receptor by competitive binding experimentInhibition of human cloned histamine H1 receptor by competitive binding experiment
ChEMBL 399 9 0 4 4.5 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL490632 186996 0 None -4 13 Human 6.2 pKi = 6.2 Binding
Inhibition of human cloned histamine H1 receptor by competitive binding experimentInhibition of human cloned histamine H1 receptor by competitive binding experiment
ChEMBL 399 9 0 4 4.5 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
3050372 70166 7 None -15 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]pyrilamine from human H1 receptor by liquid scintillation countingDisplacement of [3H]pyrilamine from human H1 receptor by liquid scintillation counting
ChEMBL 296 6 0 3 3.3 c1ccc(OCCCN2CCN(c3ccccc3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940414 70166 7 None -15 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]pyrilamine from human H1 receptor by liquid scintillation countingDisplacement of [3H]pyrilamine from human H1 receptor by liquid scintillation counting
ChEMBL 296 6 0 3 3.3 c1ccc(OCCCN2CCN(c3ccccc3)CC2)cc1 10.1016/j.bmc.2011.12.019
127036186 137414 0 None -21 19 Human 6.2 pKi = 6.2 Binding
Binding affinity to histamine H1 receptor (unknown origin) by competition binding assayBinding affinity to histamine H1 receptor (unknown origin) by competition binding assay
ChEMBL 254 7 1 1 3.7 C=CCN(CC=C)CCc1c[nH]c2ccc(C)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3753318 137414 0 None -21 19 Human 6.2 pKi = 6.2 Binding
Binding affinity to histamine H1 receptor (unknown origin) by competition binding assayBinding affinity to histamine H1 receptor (unknown origin) by competition binding assay
ChEMBL 254 7 1 1 3.7 C=CCN(CC=C)CCc1c[nH]c2ccc(C)cc12 10.1016/j.bmcl.2015.12.053
44304494 202992 0 None -5495 3 Human 5.2 pKi = 5.2 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 489 12 1 6 4.3 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](C)NC(=O)OC(C)(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
CHEMBL63125 202992 0 None -5495 3 Human 5.2 pKi = 5.2 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 489 12 1 6 4.3 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](C)NC(=O)OC(C)(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
127049856 140245 0 None -23 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 incubated for 60 mins by liquid scintillation counting method
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805431 140245 0 None -23 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 incubated for 60 mins by liquid scintillation counting method
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
43229249 140817 1 None -16 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 279 5 0 2 3.7 O=C(CCCN1CCc2ccccc2C1)c1ccccc1 10.1016/j.bmc.2016.05.053
CHEMBL3818989 140817 1 None -16 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 279 5 0 2 3.7 O=C(CCCN1CCc2ccccc2C1)c1ccccc1 10.1016/j.bmc.2016.05.053
71457264 82621 0 None -2 6 Human 6.2 pKi = 6.2 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 447 5 1 6 4.4 COc1ccc(S(=O)(=O)n2cc(C)c3cc(Cl)ccc32)cc1NC1CCN(C)CC1 10.1021/jm300955x
CHEMBL2179217 82621 0 None -2 6 Human 6.2 pKi = 6.2 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 447 5 1 6 4.4 COc1ccc(S(=O)(=O)n2cc(C)c3cc(Cl)ccc32)cc1NC1CCN(C)CC1 10.1021/jm300955x
122065 189549 3 None -1380 8 Guinea pig 6.2 pKi = 6.2 Binding
Compound is evaluated for binding affinity towards Histamine H1 receptor using [3H]pyrilamine in guinea pig lungCompound is evaluated for binding affinity towards Histamine H1 receptor using [3H]pyrilamine in guinea pig lung
ChEMBL 380 5 1 6 1.5 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3ccccc3c2=O)CC1 10.1021/jm970159v
CHEMBL51433 189549 3 None -1380 8 Guinea pig 6.2 pKi = 6.2 Binding
Compound is evaluated for binding affinity towards Histamine H1 receptor using [3H]pyrilamine in guinea pig lungCompound is evaluated for binding affinity towards Histamine H1 receptor using [3H]pyrilamine in guinea pig lung
ChEMBL 380 5 1 6 1.5 COc1ccccc1N1CCN(CCn2c(=O)[nH]c3ccccc3c2=O)CC1 10.1021/jm970159v
44591098 176762 0 None -199 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 508 9 0 3 6.6 CN(CCC=C1c2ccccc2CCc2ccccc21)C(=O)c1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
CHEMBL460402 176762 0 None -199 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 508 9 0 3 6.6 CN(CCC=C1c2ccccc2CCc2ccccc21)C(=O)c1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
162651034 180305 0 None -301 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cell membranes co-expressing RGS4 measured after 60 mins by scintillation counting analysisDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cell membranes co-expressing RGS4 measured after 60 mins by scintillation counting analysis
ChEMBL 435 8 0 5 4.6 O=C(c1ccc(Cl)cc1)c1ccc(OCCCN2CCN(c3ccncc3)CC2)cc1 10.1016/j.ejmech.2020.113041
CHEMBL4750996 180305 0 None -301 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cell membranes co-expressing RGS4 measured after 60 mins by scintillation counting analysisDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cell membranes co-expressing RGS4 measured after 60 mins by scintillation counting analysis
ChEMBL 435 8 0 5 4.6 O=C(c1ccc(Cl)cc1)c1ccc(OCCCN2CCN(c3ccncc3)CC2)cc1 10.1016/j.ejmech.2020.113041
11681378 8269 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 324 5 0 3 4.9 Cc1ccc(C(C)c2c(CCN(C)C)sc3ccccc23)cn1 10.1016/j.bmcl.2010.01.134
CHEMBL1092496 8269 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 324 5 0 3 4.9 Cc1ccc(C(C)c2c(CCN(C)C)sc3ccccc23)cn1 10.1016/j.bmcl.2010.01.134
56944383 112119 0 None -125 12 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]pyrilamine from human recombinant H1 receptor expressed in HEK293 cellsDisplacement of [3H]pyrilamine from human recombinant H1 receptor expressed in HEK293 cells
ChEMBL 487 8 1 6 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
CHEMBL3290012 112119 0 None -125 12 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]pyrilamine from human recombinant H1 receptor expressed in HEK293 cellsDisplacement of [3H]pyrilamine from human recombinant H1 receptor expressed in HEK293 cells
ChEMBL 487 8 1 6 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
10104 3566 12 None -2 6 Human 7.2 pKi = 7.2 Binding
Compound was evaluated for binding affinity towards cloned human histamine H1 receptors stably expressed in CHO-K1 cells using [3H]mepyramineCompound was evaluated for binding affinity towards cloned human histamine H1 receptors stably expressed in CHO-K1 cells using [3H]mepyramine
ChEMBL 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 10.1021/jm020895l
6604866 3566 12 None -2 6 Human 7.2 pKi = 7.2 Binding
Compound was evaluated for binding affinity towards cloned human histamine H1 receptors stably expressed in CHO-K1 cells using [3H]mepyramineCompound was evaluated for binding affinity towards cloned human histamine H1 receptors stably expressed in CHO-K1 cells using [3H]mepyramine
ChEMBL 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 10.1021/jm020895l
CHEMBL1493369 3566 12 None -2 6 Human 7.2 pKi = 7.2 Binding
Compound was evaluated for binding affinity towards cloned human histamine H1 receptors stably expressed in CHO-K1 cells using [3H]mepyramineCompound was evaluated for binding affinity towards cloned human histamine H1 receptors stably expressed in CHO-K1 cells using [3H]mepyramine
ChEMBL 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 10.1021/jm020895l
168286548 191389 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 792 20 6 8 2.8 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5192441 191389 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 792 20 6 8 2.8 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
1258 196 12 None -34673 5 Human 4.2 pKi = 4.2 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 359 8 1 5 1.5 C[C@H](C(=O)N1CCN(CC1)CCCOc1ccc(cc1)C(=O)C1CC1)N 10.1016/s0960-894x(02)00310-4
9906860 196 12 None -34673 5 Human 4.2 pKi = 4.2 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 359 8 1 5 1.5 C[C@H](C(=O)N1CCN(CC1)CCCOc1ccc(cc1)C(=O)C1CC1)N 10.1016/s0960-894x(02)00310-4
CHEMBL302196 196 12 None -34673 5 Human 4.2 pKi = 4.2 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 359 8 1 5 1.5 C[C@H](C(=O)N1CCN(CC1)CCCOc1ccc(cc1)C(=O)C1CC1)N 10.1016/s0960-894x(02)00310-4
168286548 191389 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 792 20 6 8 2.8 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5192441 191389 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 792 20 6 8 2.8 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
21527771 70156 1 None -275 10 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation countingDisplacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation counting
ChEMBL 363 6 1 3 4.2 OC1(c2ccc(Cl)cc2)CCN(CCCOc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
CHEMBL1940404 70156 1 None -275 10 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation countingDisplacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation counting
ChEMBL 363 6 1 3 4.2 OC1(c2ccc(Cl)cc2)CCN(CCCOc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
56966475 105462 0 None -3467 4 Guinea pig 6.2 pKi = 6.2 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation counting
ChEMBL 448 8 0 6 4.3 COc1ccccc1N1CCN(CCCCOc2ccc3c4c(c(=O)oc3c2)CCC4)CC1 10.1016/j.ejmech.2014.01.012
CHEMBL3120682 105462 0 None -3467 4 Guinea pig 6.2 pKi = 6.2 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation counting
ChEMBL 448 8 0 6 4.3 COc1ccccc1N1CCN(CCCCOc2ccc3c4c(c(=O)oc3c2)CCC4)CC1 10.1016/j.ejmech.2014.01.012
10177985 100656 0 None -1 4 Rat 8.2 pKi = 8.2 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
ChEMBL 382 10 1 3 4.9 CN(CCCCc1c[nH]cn1)CCC(c1ccc(Cl)cc1)c1ccccn1 10.1016/s0960-894x(03)00357-3
CHEMBL292195 100656 0 None -1 4 Rat 8.2 pKi = 8.2 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
ChEMBL 382 10 1 3 4.9 CN(CCCCc1c[nH]cn1)CCC(c1ccc(Cl)cc1)c1ccccn1 10.1016/s0960-894x(03)00357-3
135398745 2914 112 None 1 65 Human 8.2 pKi = 8.2 Binding
Binding affinity to H1 histamine receptor (unknown origin)Binding affinity to H1 histamine receptor (unknown origin)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2020.127681
47 2914 112 None 1 65 Human 8.2 pKi = 8.2 Binding
Binding affinity to H1 histamine receptor (unknown origin)Binding affinity to H1 histamine receptor (unknown origin)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2020.127681
CHEMBL715 2914 112 None 1 65 Human 8.2 pKi = 8.2 Binding
Binding affinity to H1 histamine receptor (unknown origin)Binding affinity to H1 histamine receptor (unknown origin)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2020.127681
DB00334 2914 112 None 1 65 Human 8.2 pKi = 8.2 Binding
Binding affinity to H1 histamine receptor (unknown origin)Binding affinity to H1 histamine receptor (unknown origin)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2020.127681
1210 918 51 None -20 21 Human 8.2 pKi = 8.2 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm1013874
1213 918 51 None -20 21 Human 8.2 pKi = 8.2 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm1013874
2725 918 51 None -20 21 Human 8.2 pKi = 8.2 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm1013874
33036 918 51 None -20 21 Human 8.2 pKi = 8.2 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm1013874
4411 918 51 None -20 21 Human 8.2 pKi = 8.2 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm1013874
616 918 51 None -20 21 Human 8.2 pKi = 8.2 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm1013874
6976 918 51 None -20 21 Human 8.2 pKi = 8.2 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm1013874
716121 918 51 None -20 21 Human 8.2 pKi = 8.2 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm1013874
CHEMBL1201353 918 51 None -20 21 Human 8.2 pKi = 8.2 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm1013874
CHEMBL1554789 918 51 None -20 21 Human 8.2 pKi = 8.2 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm1013874
CHEMBL505 918 51 None -20 21 Human 8.2 pKi = 8.2 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm1013874
DB01114 918 51 None -20 21 Human 8.2 pKi = 8.2 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm1013874
DB13679 918 51 None -20 21 Human 8.2 pKi = 8.2 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1021/jm1013874
10177985 100656 0 None 1 4 Human 8.2 pKi = 8.2 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 382 10 1 3 4.9 CN(CCCCc1c[nH]cn1)CCC(c1ccc(Cl)cc1)c1ccccn1 10.1021/jm100064d
CHEMBL292195 100656 0 None 1 4 Human 8.2 pKi = 8.2 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 382 10 1 3 4.9 CN(CCCCc1c[nH]cn1)CCC(c1ccc(Cl)cc1)c1ccccn1 10.1021/jm100064d
15288693 52858 0 None 4 3 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]- pyrilamine from rat brain membrane Histamine H1 receptorDisplacement of [3H]- pyrilamine from rat brain membrane Histamine H1 receptor
ChEMBL 367 5 0 5 3.0 Cn1c(=O)sc2cc(CCN3CCN(Cc4ccccc4)CC3)ccc21 10.1016/s0960-894x(02)00123-3
CHEMBL15955 52858 0 None 4 3 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]- pyrilamine from rat brain membrane Histamine H1 receptorDisplacement of [3H]- pyrilamine from rat brain membrane Histamine H1 receptor
ChEMBL 367 5 0 5 3.0 Cn1c(=O)sc2cc(CCN3CCN(Cc4ccccc4)CC3)ccc21 10.1016/s0960-894x(02)00123-3
135398745 2914 112 None 1 65 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity of compound against histamine H1 neuronal receptorIn vitro binding affinity of compound against histamine H1 neuronal receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/S0960-894X(96)00567-7
47 2914 112 None 1 65 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity of compound against histamine H1 neuronal receptorIn vitro binding affinity of compound against histamine H1 neuronal receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/S0960-894X(96)00567-7
CHEMBL715 2914 112 None 1 65 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity of compound against histamine H1 neuronal receptorIn vitro binding affinity of compound against histamine H1 neuronal receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/S0960-894X(96)00567-7
DB00334 2914 112 None 1 65 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity of compound against histamine H1 neuronal receptorIn vitro binding affinity of compound against histamine H1 neuronal receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/S0960-894X(96)00567-7
10177985 100656 0 None 1 4 Human 8.2 pKi = 8.2 Binding
Inhibition constant against histamine H1 receptorInhibition constant against histamine H1 receptor
ChEMBL 382 10 1 3 4.9 CN(CCCCc1c[nH]cn1)CCC(c1ccc(Cl)cc1)c1ccccn1 10.1021/jm058225d
CHEMBL292195 100656 0 None 1 4 Human 8.2 pKi = 8.2 Binding
Inhibition constant against histamine H1 receptorInhibition constant against histamine H1 receptor
ChEMBL 382 10 1 3 4.9 CN(CCCCc1c[nH]cn1)CCC(c1ccc(Cl)cc1)c1ccccn1 10.1021/jm058225d
57402472 67879 0 None -1 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
ChEMBL 526 11 1 6 4.0 COc1ccc(CN(CCN(C)CCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
CHEMBL1910381 67879 0 None -1 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
ChEMBL 526 11 1 6 4.0 COc1ccc(CN(CCN(C)CCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
45271166 196416 1 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 401 5 0 6 4.4 COc1ccc(Cn2c(N3CCC(n4cc(C)cn4)CC3)nc3ccccc32)cc1 10.1016/j.bmcl.2009.05.086
CHEMBL562894 196416 1 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 401 5 0 6 4.4 COc1ccc(Cn2c(N3CCC(n4cc(C)cn4)CC3)nc3ccccc32)cc1 10.1016/j.bmcl.2009.05.086
9819674 12934 0 None 1 5 Rat 8.2 pKi = 8.2 Binding
Half-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenateHalf-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenate
ChEMBL 347 3 1 5 2.4 OCCN1CCN(C2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
CHEMBL118919 12934 0 None 1 5 Rat 8.2 pKi = 8.2 Binding
Half-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenateHalf-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenate
ChEMBL 347 3 1 5 2.4 OCCN1CCN(C2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
53320177 57747 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 293 6 0 3 3.4 CCN(C)CCC1=C(Cc2cnccn2)c2ccccc2C1 10.1016/j.bmcl.2010.12.053
CHEMBL1669405 57747 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 293 6 0 3 3.4 CCN(C)CCC1=C(Cc2cnccn2)c2ccccc2C1 10.1016/j.bmcl.2010.12.053
10969390 59677 0 None 4 6 Human 8.1 pKi = 8.1 Binding
Compound was evaluated for binding affinity towards cloned human histamine H1 receptors stably expressed in CHO-K1 cells using [3H]mepyramineCompound was evaluated for binding affinity towards cloned human histamine H1 receptors stably expressed in CHO-K1 cells using [3H]mepyramine
ChEMBL 324 7 0 2 4.5 CC(C1=C(CCN(C)CCF)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL172233 59677 0 None 4 6 Human 8.1 pKi = 8.1 Binding
Compound was evaluated for binding affinity towards cloned human histamine H1 receptors stably expressed in CHO-K1 cells using [3H]mepyramineCompound was evaluated for binding affinity towards cloned human histamine H1 receptors stably expressed in CHO-K1 cells using [3H]mepyramine
ChEMBL 324 7 0 2 4.5 CC(C1=C(CCN(C)CCF)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
44401041 70487 0 None -1 7 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 313 2 0 3 4.1 CN(C)C[C@H]1CC2c3ccccc3Oc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL194659 70487 0 None -1 7 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
ChEMBL 313 2 0 3 4.1 CN(C)C[C@H]1CC2c3ccccc3Oc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
10070478 13466 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 415 2 0 3 5.6 Cc1ccc(CN2CCC(=C3c4ccc(Cl)cc4CCc4cccnc43)CC2)cn1 10.1021/acs.jmedchem.9b00447
CHEMBL1193187 13466 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 415 2 0 3 5.6 Cc1ccc(CN2CCC(=C3c4ccc(Cl)cc4CCc4cccnc43)CC2)cn1 10.1021/acs.jmedchem.9b00447
44389301 64311 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Histamine H1 receptor in CHO K1 cellsBinding affinity for human Histamine H1 receptor in CHO K1 cells
ChEMBL 619 13 1 6 6.8 CC(C)COC(=O)N(O)CCC#Cc1ccc(OCCCCN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2004.12.023
CHEMBL181085 64311 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Histamine H1 receptor in CHO K1 cellsBinding affinity for human Histamine H1 receptor in CHO K1 cells
ChEMBL 619 13 1 6 6.8 CC(C)COC(=O)N(O)CCC#Cc1ccc(OCCCCN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2004.12.023
44305842 203399 0 None - 1 Guinea pig 8.1 pKi = 8.1 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 381 4 1 4 4.1 O=C(O)c1ccc2c(c1)/C(=C\CCN1CCSCC1)c1ccccc1CO2 10.1021/jm00089a020
CHEMBL65492 203399 0 None - 1 Guinea pig 8.1 pKi = 8.1 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
ChEMBL 381 4 1 4 4.1 O=C(O)c1ccc2c(c1)/C(=C\CCN1CCSCC1)c1ccccc1CO2 10.1021/jm00089a020
46884640 7913 0 None 2187 2 Human 8.1 pKi = 8.1 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 279 5 0 3 3.0 CN(C)CCC1=C(Cc2cccnn2)c2ccccc2C1 10.1016/j.bmcl.2010.02.055
CHEMBL1090197 7913 0 None 2187 2 Human 8.1 pKi = 8.1 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 279 5 0 3 3.0 CN(C)CCC1=C(Cc2cccnn2)c2ccccc2C1 10.1016/j.bmcl.2010.02.055
11846300 80266 3 None 2 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm800876b
CHEMBL213912 80266 3 None 2 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm800876b
11846300 80266 3 None 2 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]mepyramine from human histamine H1 receptorDisplacement of [3H]mepyramine from human histamine H1 receptor
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm051008s
CHEMBL213912 80266 3 None 2 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]mepyramine from human histamine H1 receptorDisplacement of [3H]mepyramine from human histamine H1 receptor
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm051008s
59295931 84212 0 None -5 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 462 7 3 5 3.5 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1n[nH]c2ccccc12 10.1016/j.bmcl.2012.09.113
CHEMBL2208429 84212 0 None -5 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 462 7 3 5 3.5 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1n[nH]c2ccccc12 10.1016/j.bmcl.2012.09.113
59295935 84010 0 None -3 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 507 7 3 5 3.6 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c(=O)c2cc(F)ccc12 10.1016/j.bmcl.2012.09.112
CHEMBL2207278 84010 0 None -3 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 507 7 3 5 3.6 O=C(NC[C@@H](O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)c1c[nH]c(=O)c2cc(F)ccc12 10.1016/j.bmcl.2012.09.112
10408773 165299 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 401 2 0 3 5.3 Clc1ccc2c(c1)CCc1cccnc1C2=C1CCN(Cc2ccncc2)CC1 10.1021/acs.jmedchem.9b00447
CHEMBL423316 165299 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 401 2 0 3 5.3 Clc1ccc2c(c1)CCc1cccnc1C2=C1CCN(Cc2ccncc2)CC1 10.1021/acs.jmedchem.9b00447
155527187 171152 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 414 2 0 2 6.2 Cc1cccc(CN2CCC(=C3c4ccc(Cl)cc4CCc4cccnc43)CC2)c1 10.1021/acs.jmedchem.9b00447
CHEMBL4458676 171152 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 414 2 0 2 6.2 Cc1cccc(CN2CCC(=C3c4ccc(Cl)cc4CCc4cccnc43)CC2)c1 10.1021/acs.jmedchem.9b00447
134156988 154519 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 281 7 0 2 3.8 c1ccc(Cc2ccccc2OCCCN2CCC2)cc1 10.1021/acs.jmedchem.6b00981
CHEMBL3984221 154519 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 281 7 0 2 3.8 c1ccc(Cc2ccccc2OCCCN2CCC2)cc1 10.1021/acs.jmedchem.6b00981
CHEMBL3990754 154519 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysisDisplacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis
ChEMBL 281 7 0 2 3.8 c1ccc(Cc2ccccc2OCCCN2CCC2)cc1 10.1021/acs.jmedchem.6b00981
135398737 958 93 None -2 89 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
38 958 93 None -2 89 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
722 958 93 None -2 89 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
CHEMBL42 958 93 None -2 89 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
DB00363 958 93 None -2 89 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
2389 3331 118 None -52 67 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm070516u
5073 3331 118 None -52 67 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm070516u
96 3331 118 None -52 67 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm070516u
CHEMBL85 3331 118 None -52 67 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm070516u
DB00734 3331 118 None -52 67 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellumDisplacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm070516u
22397436 82237 0 None 6 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 510 5 0 5 4.5 CS(=O)(=O)c1cccc(C(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.124
CHEMBL2171019 82237 0 None 6 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 510 5 0 5 4.5 CS(=O)(=O)c1cccc(C(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.124
17963183 82262 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 545 5 1 5 5.1 O=C(NS(=O)(=O)c1cccc(Cl)c1)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
CHEMBL2171043 82262 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 545 5 1 5 5.1 O=C(NS(=O)(=O)c1cccc(Cl)c1)N1CCC(N2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.124
44267108 98345 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.
ChEMBL 366 0 0 2 4.6 CC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3cc(C)cnc32)CC1 10.1016/S0960-894X(00)80290-5
CHEMBL275109 98345 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.
ChEMBL 366 0 0 2 4.6 CC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3cc(C)cnc32)CC1 10.1016/S0960-894X(00)80290-5
120445 202064 4 None 16 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cellsDisplacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cells
ChEMBL 253 6 0 1 4.2 CN(C)CCCC(c1ccccc1)c1ccccc1 10.1016/j.bmc.2009.08.016
CHEMBL608689 202064 4 None 16 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cellsDisplacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cells
ChEMBL 253 6 0 1 4.2 CN(C)CCCC(c1ccccc1)c1ccccc1 10.1016/j.bmc.2009.08.016
9998826 120477 0 None -69 5 Rat 7.2 pKi = 7.2 Binding
Inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat cortexInhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat cortex
ChEMBL 363 5 1 3 3.1 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccccc1 10.1021/jm950759z
CHEMBL354210 120477 0 None -69 5 Rat 7.2 pKi = 7.2 Binding
Inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat cortexInhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat cortex
ChEMBL 363 5 1 3 3.1 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccccc1 10.1021/jm950759z
44266960 97156 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.
ChEMBL 380 1 0 3 4.1 CC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3cc(C=O)cnc32)CC1 10.1016/S0960-894X(00)80290-5
CHEMBL268022 97156 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane.
ChEMBL 380 1 0 3 4.1 CC(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3cc(C=O)cnc32)CC1 10.1016/S0960-894X(00)80290-5
69082816 74937 0 None -4168 3 Human 5.2 pKi = 5.2 Binding
Binding affinity to H1 receptorBinding affinity to H1 receptor
ChEMBL 431 5 0 3 4.1 C[C@H]1CCCN1C(=O)c1ccc(-c2ccc3c(c2)CCN(CCN2CCCC2)C3=O)cc1 10.1021/jm300011d
CHEMBL2031877 74937 0 None -4168 3 Human 5.2 pKi = 5.2 Binding
Binding affinity to H1 receptorBinding affinity to H1 receptor
ChEMBL 431 5 0 3 4.1 C[C@H]1CCCN1C(=O)c1ccc(-c2ccc3c(c2)CCN(CCN2CCCC2)C3=O)cc1 10.1021/jm300011d
145986752 167276 0 None -16 17 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Pyrilamine from human H1 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 562 10 1 5 7.3 COc1ccc(N(CCCCN2CCC(O)(c3ccc(Cl)c(C(F)(F)F)c3)CC2)c2ccc(OC)cc2)cc1 10.1016/j.bmcl.2018.10.036
CHEMBL4293307 167276 0 None -16 17 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Pyrilamine from human H1 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 562 10 1 5 7.3 COc1ccc(N(CCCCN2CCC(O)(c3ccc(Cl)c(C(F)(F)F)c3)CC2)c2ccc(OC)cc2)cc1 10.1016/j.bmcl.2018.10.036
56963799 74895 0 None -17782 10 Human 5.2 pKi = 5.2 Binding
Binding affinity to human recombinant H1 receptorBinding affinity to human recombinant H1 receptor
ChEMBL 378 6 0 5 4.6 C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc([N+](=O)[O-])cc3)ccc2o1 10.1021/jm201690h
CHEMBL2031737 74895 0 None -17782 10 Human 5.2 pKi = 5.2 Binding
Binding affinity to human recombinant H1 receptorBinding affinity to human recombinant H1 receptor
ChEMBL 378 6 0 5 4.6 C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc([N+](=O)[O-])cc3)ccc2o1 10.1021/jm201690h
141485893 175738 0 None - 1 Guinea pig 6.2 pKi = 6.2 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysisDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysis
ChEMBL 317 5 0 4 1.3 CN1CCN(CCCOc2ccc3c(c2)C(=O)N(C)CC3)CC1 10.1016/j.bmcl.2019.04.015
CHEMBL4583068 175738 0 None - 1 Guinea pig 6.2 pKi = 6.2 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysisDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysis
ChEMBL 317 5 0 4 1.3 CN1CCN(CCCOc2ccc3c(c2)C(=O)N(C)CC3)CC1 10.1016/j.bmcl.2019.04.015
45833388 69024 7 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 274 4 0 7 1.3 CN(C)CCSc1nc2ccccc2c2nnnn12 10.1021/jm2011589
CHEMBL1923525 69024 7 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 274 4 0 7 1.3 CN(C)CCSc1nc2ccccc2c2nnnn12 10.1021/jm2011589
2537688 69025 3 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 264 3 1 6 0.8 OCCN1CCN(c2ncnc3sccc23)CC1 10.1021/jm2011589
CHEMBL1923526 69025 3 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 264 3 1 6 0.8 OCCN1CCN(c2ncnc3sccc23)CC1 10.1021/jm2011589
168294776 193026 0 None -11 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 366 7 3 4 2.6 Cc1nnc(CCCN/C(N)=N/C(=O)NCC(C)C2CCCCC2)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5209479 193026 0 None -11 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 366 7 3 4 2.6 Cc1nnc(CCCN/C(N)=N/C(=O)NCC(C)C2CCCCC2)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222831 193026 0 None -11 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 366 7 3 4 2.6 Cc1nnc(CCCN/C(N)=N/C(=O)NCC(C)C2CCCCC2)s1 10.1021/acs.jmedchem.1c00692
164609017 184425 0 None -125 6 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 416 10 4 4 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCCc1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4846201 184425 0 None -125 6 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 416 10 4 4 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCCc1ccccc1 10.1016/j.ejmech.2021.113190
44304211 102197 0 None -6918 3 Human 4.2 pKi = 4.2 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 373 9 1 5 1.9 CC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL302829 102197 0 None -6918 3 Human 4.2 pKi = 4.2 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 373 9 1 5 1.9 CC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
129103313 166753 0 None -70 6 Guinea pig 6.2 pKi = 6.2 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by liquid scintillation countingDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by liquid scintillation counting
ChEMBL 447 6 0 4 5.0 O=C1CCc2cc(CCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc3c2N1CC3 10.1021/acs.jmedchem.8b01096
CHEMBL4283548 166753 0 None -70 6 Guinea pig 6.2 pKi = 6.2 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by liquid scintillation countingDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by liquid scintillation counting
ChEMBL 447 6 0 4 5.0 O=C1CCc2cc(CCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc3c2N1CC3 10.1021/acs.jmedchem.8b01096
145980875 166707 0 None -5 11 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Pyrilamine from human H1 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 443 7 1 2 6.2 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCCc2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL4282702 166707 0 None -5 11 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Pyrilamine from human H1 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 443 7 1 2 6.2 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCCc2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
145992489 166977 0 None -2 12 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Pyrilamine from human H1 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 535 7 1 2 7.8 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC=C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL4287623 166977 0 None -2 12 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Pyrilamine from human H1 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 535 7 1 2 7.8 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC=C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
95104704 162138 1 None 2 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 344 6 1 4 3.1 CCOc1ccc([C@H](O)CN2CCN(c3ccccc3F)CC2)cc1 10.1021/acs.jmedchem.8b00718
CHEMBL4161676 162138 1 None 2 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]pyrilamine from human HRH1 expressed in HEK cell membranes after 90 mins by scintillation counting method
ChEMBL 344 6 1 4 3.1 CCOc1ccc([C@H](O)CN2CCN(c3ccccc3F)CC2)cc1 10.1021/acs.jmedchem.8b00718
14885628 119434 0 None - 1 Rat 6.1 pKi = 6.1 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 336 0 0 2 3.8 CC(=O)N1CCC(=C2c3ccc(F)cc3CCc3cccnc32)CC1 10.1021/jm00105a069
CHEMBL344942 119434 0 None - 1 Rat 6.1 pKi = 6.1 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 336 0 0 2 3.8 CC(=O)N1CCC(=C2c3ccc(F)cc3CCc3cccnc32)CC1 10.1021/jm00105a069
25216680 74944 0 None -7244 3 Human 5.1 pKi = 5.1 Binding
Binding affinity to H1 receptorBinding affinity to H1 receptor
ChEMBL 405 6 1 3 3.6 CCNC(=O)c1ccc(-c2ccc3c(c2)CCN(CCN2CCC[C@H]2C)C3=O)cc1 10.1021/jm300011d
CHEMBL2031884 74944 0 None -7244 3 Human 5.1 pKi = 5.1 Binding
Binding affinity to H1 receptorBinding affinity to H1 receptor
ChEMBL 405 6 1 3 3.6 CCNC(=O)c1ccc(-c2ccc3c(c2)CCN(CCN2CCC[C@H]2C)C3=O)cc1 10.1021/jm300011d
44304378 163272 0 None -35 3 Human 6.1 pKi = 6.1 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 423 11 0 5 4.1 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cccnc3)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL418658 163272 0 None -35 3 Human 6.1 pKi = 6.1 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 423 11 0 5 4.1 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cccnc3)CC2)cc1 10.1016/s0960-894x(02)00309-8
56852956 112043 1 None -186 9 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor by PDSP assayDisplacement of [3H]pyrilamine from human histamine H1 receptor by PDSP assay
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289656 112043 1 None -186 9 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor by PDSP assayDisplacement of [3H]pyrilamine from human histamine H1 receptor by PDSP assay
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
168277996 192846 0 None -60 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 380 4 4 4 3.3 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCc2ccccc2)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5173373 192846 0 None -60 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 380 4 4 4 3.3 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCc2ccccc2)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5221736 192846 0 None -60 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 380 4 4 4 3.3 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCc2ccccc2)c1 10.1021/acs.jmedchem.1c00692
46216771 202165 0 None -3 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]Pyrilamine from human cloned histamine H1 receptorDisplacement of [3H]Pyrilamine from human cloned histamine H1 receptor
ChEMBL 327 6 1 1 4.9 c1ccc(CCCNCC2c3ccccc3Cc3ccccc32)cc1 10.1016/j.bmcl.2009.12.064
CHEMBL609328 202165 0 None -3 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]Pyrilamine from human cloned histamine H1 receptorDisplacement of [3H]Pyrilamine from human cloned histamine H1 receptor
ChEMBL 327 6 1 1 4.9 c1ccc(CCCNCC2c3ccccc3Cc3ccccc32)cc1 10.1016/j.bmcl.2009.12.064
1353 1911 93 None -489 83 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human histamine H1 receptorBinding affinity towards human histamine H1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm030480f
3559 1911 93 None -489 83 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human histamine H1 receptorBinding affinity towards human histamine H1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm030480f
86 1911 93 None -489 83 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human histamine H1 receptorBinding affinity towards human histamine H1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm030480f
CHEMBL54 1911 93 None -489 83 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human histamine H1 receptorBinding affinity towards human histamine H1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm030480f
DB00502 1911 93 None -489 83 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human histamine H1 receptorBinding affinity towards human histamine H1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm030480f
56852956 112043 1 None -186 9 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor by PDSP assayDisplacement of [3H]pyrilamine from human histamine H1 receptor by PDSP assay
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289656 112043 1 None -186 9 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor by PDSP assayDisplacement of [3H]pyrilamine from human histamine H1 receptor by PDSP assay
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
49841719 69737 0 None -1513 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human H1 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H1 receptor expressed in HEK cell membranes
ChEMBL 309 2 1 6 2.2 CN1CCN(c2nc(N)nc3cc(-c4ccoc4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL1935571 69737 0 None -1513 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human H1 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H1 receptor expressed in HEK cell membranes
ChEMBL 309 2 1 6 2.2 CN1CCN(c2nc(N)nc3cc(-c4ccoc4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
127051015 140874 0 None -27 9 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 283 5 0 1 4.2 Fc1ccc(CCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818128 140874 0 None -27 9 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 283 5 0 1 4.2 Fc1ccc(CCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819731 140874 0 None -27 9 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 283 5 0 1 4.2 Fc1ccc(CCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
16655023 107441 2 None -60 7 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]pyrilamine from human cloned histamine H1 receptorDisplacement of [3H]pyrilamine from human cloned histamine H1 receptor
ChEMBL 481 7 0 7 3.7 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4ccc(F)cc4)CC3)[C@@H]1CO2 10.1016/j.bmc.2007.03.053
CHEMBL318235 107441 2 None -60 7 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]pyrilamine from human cloned histamine H1 receptorDisplacement of [3H]pyrilamine from human cloned histamine H1 receptor
ChEMBL 481 7 0 7 3.7 COc1cc2c(cc1OC)C1=NO[C@@H](CN3CCN(C/C(C)=C/c4ccc(F)cc4)CC3)[C@@H]1CO2 10.1016/j.bmc.2007.03.053
44304287 202898 0 None -4 3 Human 7.1 pKi = 7.1 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 428 11 0 5 4.7 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cccs3)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL62726 202898 0 None -4 3 Human 7.1 pKi = 7.1 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 428 11 0 5 4.7 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cccs3)CC2)cc1 10.1016/s0960-894x(02)00309-8
132356 14677 1 None - 1 Guinea pig 6.1 pKi = 6.1 Binding
Inhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptorInhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptor
ChEMBL 473 7 1 4 6.1 O=C(O)c1ccc2c(c1)C(SCCN1CCC(Cc3ccccc3)CC1)c1ccccc1CO2 10.1021/jm00055a013
CHEMBL1205688 14677 1 None - 1 Guinea pig 6.1 pKi = 6.1 Binding
Inhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptorInhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptor
ChEMBL 473 7 1 4 6.1 O=C(O)c1ccc2c(c1)C(SCCN1CCC(Cc3ccccc3)CC1)c1ccccc1CO2 10.1021/jm00055a013
CHEMBL133778 14677 1 None - 1 Guinea pig 6.1 pKi = 6.1 Binding
Inhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptorInhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptor
ChEMBL 473 7 1 4 6.1 O=C(O)c1ccc2c(c1)C(SCCN1CCC(Cc3ccccc3)CC1)c1ccccc1CO2 10.1021/jm00055a013
44333988 4535 0 None -199 3 Human 5.1 pKi = 5.1 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 367 8 1 5 2.6 CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)c3cccnc3)C2)cc1 10.1016/s0960-894x(02)00685-6
CHEMBL102331 4535 0 None -199 3 Human 5.1 pKi = 5.1 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 367 8 1 5 2.6 CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)c3cccnc3)C2)cc1 10.1016/s0960-894x(02)00685-6
44304037 102693 0 None -204 3 Human 6.1 pKi = 6.1 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 362 9 0 5 3.2 CCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL304714 102693 0 None -204 3 Human 6.1 pKi = 6.1 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 362 9 0 5 3.2 CCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
127051015 140874 0 None -27 9 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 283 5 0 1 4.2 Fc1ccc(CCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818128 140874 0 None -27 9 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 283 5 0 1 4.2 Fc1ccc(CCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819731 140874 0 None -27 9 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 283 5 0 1 4.2 Fc1ccc(CCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
24759623 96349 20 None -18 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in NIH3T3 cellsDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in NIH3T3 cells
ChEMBL 318 3 0 4 3.0 CN1CCN(c2nc3ccccc3nc2Cc2ccccc2)CC1 10.1021/jm7014217
CHEMBL261551 96349 20 None -18 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in NIH3T3 cellsDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in NIH3T3 cells
ChEMBL 318 3 0 4 3.0 CN1CCN(c2nc3ccccc3nc2Cc2ccccc2)CC1 10.1021/jm7014217
168294449 193018 0 None -74 6 Human 5.1 pKi = 5.1 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 367 7 4 5 1.9 CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1 10.1021/acs.jmedchem.1c00692
CHEMBL5204599 193018 0 None -74 6 Human 5.1 pKi = 5.1 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 367 7 4 5 1.9 CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1 10.1021/acs.jmedchem.1c00692
CHEMBL5222793 193018 0 None -74 6 Human 5.1 pKi = 5.1 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 367 7 4 5 1.9 CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1 10.1021/acs.jmedchem.1c00692
162646011 179735 0 None -109 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cell membranes co-expressing RGS4 measured after 60 mins by scintillation counting analysisDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cell membranes co-expressing RGS4 measured after 60 mins by scintillation counting analysis
ChEMBL 347 6 0 4 3.8 c1ccc2cc(OCCCN3CCN(c4ccncc4)CC3)ccc2c1 10.1016/j.ejmech.2020.113041
CHEMBL4744110 179735 0 None -109 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cell membranes co-expressing RGS4 measured after 60 mins by scintillation counting analysisDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cell membranes co-expressing RGS4 measured after 60 mins by scintillation counting analysis
ChEMBL 347 6 0 4 3.8 c1ccc2cc(OCCCN3CCN(c4ccncc4)CC3)ccc2c1 10.1016/j.ejmech.2020.113041
151221 202395 11 None 21 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cellsDisplacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cells
ChEMBL 239 5 0 1 3.8 CN(C)CCC(c1ccccc1)c1ccccc1 10.1016/j.bmc.2009.08.016
CHEMBL610739 202395 11 None 21 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cellsDisplacement of [3H]chlorphniramine from human histamine H1 receptor expressed in cells
ChEMBL 239 5 0 1 3.8 CN(C)CCC(c1ccccc1)c1ccccc1 10.1016/j.bmc.2009.08.016
11659397 195282 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation counting
ChEMBL 297 5 0 4 3.4 CN(C)CCc1sc2ccccc2c1Cc1cnccn1 10.1021/jm900933k
CHEMBL551340 195282 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation counting
ChEMBL 297 5 0 4 3.4 CN(C)CCc1sc2ccccc2c1Cc1cnccn1 10.1021/jm900933k
45267774 196207 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 416 5 0 6 4.1 CN(c1ncccn1)C1CCN(c2nc3ccccc3n2Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2009.05.086
CHEMBL561489 196207 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assayDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay
ChEMBL 416 5 0 6 4.1 CN(c1ncccn1)C1CCN(c2nc3ccccc3n2Cc2ccc(F)cc2)CC1 10.1016/j.bmcl.2009.05.086
44334556 107267 0 None -128 3 Human 4.1 pKi = 4.1 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 449 10 3 7 1.7 CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@H](CO)NC(=O)OC(C)(C)C)C2)cc1 10.1016/s0960-894x(02)00685-6
CHEMBL316968 107267 0 None -128 3 Human 4.1 pKi = 4.1 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 449 10 3 7 1.7 CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@H](CO)NC(=O)OC(C)(C)C)C2)cc1 10.1016/s0960-894x(02)00685-6
44335172 5097 0 None -3 3 Human 6.1 pKi = 6.1 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 374 7 0 5 4.0 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccsc3)cc2)CC1 10.1016/s0960-894x(02)00648-0
CHEMBL105567 5097 0 None -3 3 Human 6.1 pKi = 6.1 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 374 7 0 5 4.0 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccsc3)cc2)CC1 10.1016/s0960-894x(02)00648-0
168286141 192924 0 None -3 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 450 8 4 4 4.8 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5192993 192924 0 None -3 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 450 8 4 4 4.8 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222231 192924 0 None -3 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 450 8 4 4 4.8 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
29298 203450 1 None -794 4 Human 5.1 pKi = 5.1 Binding
Compound was tested for its binding affinity towards human H1 receptorCompound was tested for its binding affinity towards human H1 receptor
ChEMBL 297 5 1 3 3.9 CN(C)CCCNc1c2c(nc3ccccc13)CCCCC2 10.1016/s0960-894x(03)00356-1
CHEMBL65849 203450 1 None -794 4 Human 5.1 pKi = 5.1 Binding
Compound was tested for its binding affinity towards human H1 receptorCompound was tested for its binding affinity towards human H1 receptor
ChEMBL 297 5 1 3 3.9 CN(C)CCCNc1c2c(nc3ccccc13)CCCCC2 10.1016/s0960-894x(03)00356-1
57390224 67877 0 None -38 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
ChEMBL 503 8 1 5 4.7 COc1ccc(CN(CCN2CCN(C(=O)c3cc4cc(Cl)ccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
CHEMBL1910379 67877 0 None -38 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingDisplacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
ChEMBL 503 8 1 5 4.7 COc1ccc(CN(CCN2CCN(C(=O)c3cc4cc(Cl)ccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
44335483 5293 0 None -257 4 Human 5.1 pKi = 5.1 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 336 6 1 4 3.5 N#Cc1ccc(-c2ccc(OCCCN3CCCC(O)C3)cc2)cc1 10.1016/s0960-894x(02)00648-0
CHEMBL106596 5293 0 None -257 4 Human 5.1 pKi = 5.1 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 336 6 1 4 3.5 N#Cc1ccc(-c2ccc(OCCCN3CCCC(O)C3)cc2)cc1 10.1016/s0960-894x(02)00648-0
164614549 184943 0 None -549 6 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 340 9 4 4 2.2 CCCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
CHEMBL4853668 184943 0 None -549 6 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 340 9 4 4 2.2 CCCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
164626153 186378 0 None -3801 6 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 378 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1cccc(F)c1 10.1016/j.ejmech.2021.113190
CHEMBL4875600 186378 0 None -3801 6 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 378 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1cccc(F)c1 10.1016/j.ejmech.2021.113190
164611807 184984 0 None -229 4 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 376 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)N[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4854278 184984 0 None -229 4 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 376 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)N[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
1353 1911 93 None -489 83 Human 6.1 pKi = 6.1 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
3559 1911 93 None -489 83 Human 6.1 pKi = 6.1 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
86 1911 93 None -489 83 Human 6.1 pKi = 6.1 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
CHEMBL54 1911 93 None -489 83 Human 6.1 pKi = 6.1 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
DB00502 1911 93 None -489 83 Human 6.1 pKi = 6.1 Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
44207909 16699 3 None -2 9 Human 6.1 pKi = 6.1 Binding
Binding affinity to human histamine H1 receptor by radioligand displacement assayBinding affinity to human histamine H1 receptor by radioligand displacement assay
ChEMBL 407 7 1 4 2.6 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm100697g
CHEMBL1242923 16699 3 None -2 9 Human 6.1 pKi = 6.1 Binding
Binding affinity to human histamine H1 receptor by radioligand displacement assayBinding affinity to human histamine H1 receptor by radioligand displacement assay
ChEMBL 407 7 1 4 2.6 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm100697g
10403711 96333 33 None -4168 9 Human 5.1 pKi = 5.1 Binding
Inhibition of histamine H1 receptor (unknown origin)Inhibition of histamine H1 receptor (unknown origin)
ChEMBL 320 3 4 9 -1.7 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=O)NC2CC2)[C@@H](O)[C@H]1O 10.1021/acs.jmedchem.8b01662
CHEMBL261482 96333 33 None -4168 9 Human 5.1 pKi = 5.1 Binding
Inhibition of histamine H1 receptor (unknown origin)Inhibition of histamine H1 receptor (unknown origin)
ChEMBL 320 3 4 9 -1.7 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=O)NC2CC2)[C@@H](O)[C@H]1O 10.1021/acs.jmedchem.8b01662
44591099 176190 0 None -295 6 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 494 10 0 3 7.0 CN(CCC=C1c2ccccc2CCc2ccccc21)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
CHEMBL459350 176190 0 None -295 6 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
ChEMBL 494 10 0 3 7.0 CN(CCC=C1c2ccccc2CCc2ccccc21)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
44304259 100615 0 None -2 3 Human 7.1 pKi = 7.1 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 462 11 0 5 5.4 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3sccc3Cl)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL291882 100615 0 None -2 3 Human 7.1 pKi = 7.1 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 462 11 0 5 5.4 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3sccc3Cl)CC2)cc1 10.1016/s0960-894x(02)00309-8
71072113 81262 0 None -3 2 Human 7.1 pKi = 7.1 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 504 8 1 4 5.6 Cc1ccc(C[C@@H](C(=O)O)N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.103
CHEMBL2158774 81262 0 None -3 2 Human 7.1 pKi = 7.1 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 504 8 1 4 5.6 Cc1ccc(C[C@@H](C(=O)O)N2CCC(CN3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2012.08.103
66615678 81268 0 None -19 2 Human 7.1 pKi = 7.1 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 488 8 1 4 5.0 Cc1cc(Cl)ccc1OC1CCN(CC2CCN([C@@H](Cc3ccc(F)cc3)C(=O)O)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158780 81268 0 None -19 2 Human 7.1 pKi = 7.1 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 488 8 1 4 5.0 Cc1cc(Cl)ccc1OC1CCN(CC2CCN([C@@H](Cc3ccc(F)cc3)C(=O)O)CC2)CC1 10.1016/j.bmcl.2012.08.103
66615702 81275 0 None -100 2 Human 7.1 pKi = 7.1 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 522 8 1 4 5.8 C[C@](Cc1ccc(F)cc1)(C(=O)O)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158787 81275 0 None -100 2 Human 7.1 pKi = 7.1 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 522 8 1 4 5.8 C[C@](Cc1ccc(F)cc1)(C(=O)O)N1CCC(CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2012.08.103
71456722 81281 0 None -39 2 Human 7.1 pKi = 7.1 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 486 8 1 4 4.9 Cc1cc(F)ccc1OC1CCN(CC2CCN([C@@](C)(Cc3ccc(F)cc3)C(=O)O)CC2)CC1 10.1016/j.bmcl.2012.08.103
CHEMBL2158793 81281 0 None -39 2 Human 7.1 pKi = 7.1 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 486 8 1 4 4.9 Cc1cc(F)ccc1OC1CCN(CC2CCN([C@@](C)(Cc3ccc(F)cc3)C(=O)O)CC2)CC1 10.1016/j.bmcl.2012.08.103
127026052 137553 0 None -4 19 Human 7.1 pKi = 7.1 Binding
Binding affinity to histamine H1 receptor (unknown origin) by competition binding assayBinding affinity to histamine H1 receptor (unknown origin) by competition binding assay
ChEMBL 258 7 1 1 3.5 C=CCN(CC=C)CCc1c[nH]c2ccc(F)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3754496 137553 0 None -4 19 Human 7.1 pKi = 7.1 Binding
Binding affinity to histamine H1 receptor (unknown origin) by competition binding assayBinding affinity to histamine H1 receptor (unknown origin) by competition binding assay
ChEMBL 258 7 1 1 3.5 C=CCN(CC=C)CCc1c[nH]c2ccc(F)cc12 10.1016/j.bmcl.2015.12.053
59296073 84205 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 483 8 2 6 3.0 N#Cc1cccc(S(=O)(=O)NC[C@@H](O)CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)c1 10.1016/j.bmcl.2012.09.113
CHEMBL2208422 84205 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in recombinant CHOK1 cells after 1 hr
ChEMBL 483 8 2 6 3.0 N#Cc1cccc(S(=O)(=O)NC[C@@H](O)CN2CCC(Oc3ccc(Cl)c(Cl)c3)CC2)c1 10.1016/j.bmcl.2012.09.113
59296077 84008 0 None -5 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 547 8 3 7 2.5 Cc1cc(Cl)ccc1OC1CCN(C[C@H](O)CNC(=O)c2c[nH]c(=O)c3cc(S(C)(=O)=O)ccc23)CC1 10.1016/j.bmcl.2012.09.112
CHEMBL2207276 84008 0 None -5 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hrDisplacement of [3H]-pyrilamine from human recombinant H1 histamine receptor expressed in CHOK1 cells after 1 hr
ChEMBL 547 8 3 7 2.5 Cc1cc(Cl)ccc1OC1CCN(C[C@H](O)CNC(=O)c2c[nH]c(=O)c3cc(S(C)(=O)=O)ccc23)CC1 10.1016/j.bmcl.2012.09.112
1222 881 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor N7.45C mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor N7.45C mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/nchembio714
2678 881 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor N7.45C mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor N7.45C mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/nchembio714
581 881 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor N7.45C mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor N7.45C mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/nchembio714
CHEMBL1000 881 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor N7.45C mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor N7.45C mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/nchembio714
DB00341 881 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor N7.45C mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor N7.45C mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/nchembio714
71449858 82246 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 582 9 1 6 4.8 O=C(O)CCCS(=O)(=O)c1cccc(C(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.124
CHEMBL2171027 82246 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cellsDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells
ChEMBL 582 9 1 6 4.8 O=C(O)CCCS(=O)(=O)c1cccc(C(=O)N2CCC(N3CCC(Oc4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2012.08.124
11515125 8144 0 None - 1 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 310 5 0 3 4.6 C[C@@H](c1cccnc1)c1c(CCN(C)C)sc2ccccc12 10.1016/j.bmcl.2010.01.134
CHEMBL1091778 8144 0 None - 1 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 310 5 0 3 4.6 C[C@@H](c1cccnc1)c1c(CCN(C)C)sc2ccccc12 10.1016/j.bmcl.2010.01.134
127049855 140228 0 None -13 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 incubated for 60 mins by liquid scintillation counting method
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805220 140228 0 None -13 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 incubated for 60 mins by liquid scintillation counting method
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
168282610 190916 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 802 20 5 7 4.1 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5185281 190916 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 802 20 5 7 4.1 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
2199935 119215 13 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 215 5 1 2 2.8 CNCCCOc1cccc2ccccc12 10.1021/jm2011589
CHEMBL343324 119215 13 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 215 5 1 2 2.8 CNCCCOc1cccc2ccccc12 10.1021/jm2011589
168282610 190916 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 802 20 5 7 4.1 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5185281 190916 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 802 20 5 7 4.1 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
10517956 56255 0 None -66 2 Guinea pig 5.1 pKi = 5.1 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 295 5 2 3 3.7 O=C(Nc1ccc2ccccc2c1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL16274 56255 0 None -66 2 Guinea pig 5.1 pKi = 5.1 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 295 5 2 3 3.7 O=C(Nc1ccc2ccccc2c1)OCCCc1c[nH]cn1 10.1021/jm9507688
10833949 57191 0 None -645 2 Guinea pig 5.1 pKi = 5.1 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 385 6 2 3 2.9 O=C(NCc1ccc(I)cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL16496 57191 0 None -645 2 Guinea pig 5.1 pKi = 5.1 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 385 6 2 3 2.9 O=C(NCc1ccc(I)cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
168290235 192968 0 None -12882 20 Human 5.1 pKi = 5.1 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5201074 192968 0 None -12882 20 Human 5.1 pKi = 5.1 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222491 192968 0 None -12882 20 Human 5.1 pKi = 5.1 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
10085839 204502 0 None -251 3 Guinea pig 5.1 pKi = 5.1 Binding
Displacement of [3H]mepyramine bound to membranes of CHO cells expressing guinea pig H1 receptorsDisplacement of [3H]mepyramine bound to membranes of CHO cells expressing guinea pig H1 receptors
ChEMBL 294 7 3 2 2.9 S=C(NCCCCCc1c[nH]cn1)NC1CCCCC1 10.1021/jm00012a025
CHEMBL72571 204502 0 None -251 3 Guinea pig 5.1 pKi = 5.1 Binding
Displacement of [3H]mepyramine bound to membranes of CHO cells expressing guinea pig H1 receptorsDisplacement of [3H]mepyramine bound to membranes of CHO cells expressing guinea pig H1 receptors
ChEMBL 294 7 3 2 2.9 S=C(NCCCCCc1c[nH]cn1)NC1CCCCC1 10.1021/jm00012a025
164617783 184590 0 None -123 6 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 388 8 4 4 2.8 CCC(CNC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4848815 184590 0 None -123 6 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 388 8 4 4 2.8 CCC(CNC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1 10.1016/j.ejmech.2021.113190
10541297 57549 0 None -3090 2 Guinea pig 4.1 pKi = 4.1 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 287 8 2 3 2.7 O=C(NCCCc1ccccc1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL16639 57549 0 None -3090 2 Guinea pig 4.1 pKi = 4.1 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 287 8 2 3 2.7 O=C(NCCCc1ccccc1)OCCCc1c[nH]cn1 10.1021/jm9507688
10611565 98320 0 None -3235 2 Guinea pig 4.1 pKi = 4.1 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 263 5 2 3 2.7 O=C(Nc1ccc(F)cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL274989 98320 0 None -3235 2 Guinea pig 4.1 pKi = 4.1 Binding
Binding affinity against H1 receptor of Guinea pig ileumBinding affinity against H1 receptor of Guinea pig ileum
ChEMBL 263 5 2 3 2.7 O=C(Nc1ccc(F)cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
1204 1932 119 None -501 24 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor S3.36T mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor S3.36T mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1038/nchembio714
1247 1932 119 None -501 24 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor S3.36T mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor S3.36T mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1038/nchembio714
1375 1932 119 None -501 24 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor S3.36T mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor S3.36T mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1038/nchembio714
774 1932 119 None -501 24 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor S3.36T mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor S3.36T mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1038/nchembio714
CHEMBL90 1932 119 None -501 24 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor S3.36T mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor S3.36T mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1038/nchembio714
DB05381 1932 119 None -501 24 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor S3.36T mutant expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor S3.36T mutant expressed in COS-7 cells by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1038/nchembio714
1204 1932 119 None -501 24 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]mepyramine from human wild-type histamine H1 receptor expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human wild-type histamine H1 receptor expressed in COS-7 cells by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1038/nchembio714
1247 1932 119 None -501 24 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]mepyramine from human wild-type histamine H1 receptor expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human wild-type histamine H1 receptor expressed in COS-7 cells by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1038/nchembio714
1375 1932 119 None -501 24 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]mepyramine from human wild-type histamine H1 receptor expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human wild-type histamine H1 receptor expressed in COS-7 cells by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1038/nchembio714
774 1932 119 None -501 24 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]mepyramine from human wild-type histamine H1 receptor expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human wild-type histamine H1 receptor expressed in COS-7 cells by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1038/nchembio714
CHEMBL90 1932 119 None -501 24 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]mepyramine from human wild-type histamine H1 receptor expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human wild-type histamine H1 receptor expressed in COS-7 cells by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1038/nchembio714
DB05381 1932 119 None -501 24 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]mepyramine from human wild-type histamine H1 receptor expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human wild-type histamine H1 receptor expressed in COS-7 cells by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1038/nchembio714
16093484 98060 6 None -3 6 Human 8.1 pKi = 8.1 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 229 0 2 3 2.6 CC1NC(N)=Nc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2007.10.080
CHEMBL273170 98060 6 None -3 6 Human 8.1 pKi = 8.1 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 229 0 2 3 2.6 CC1NC(N)=Nc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2007.10.080
137645406 157902 0 None 4 13 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-pyrilamine from recombinant human H1 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-pyrilamine from recombinant human H1 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 491 8 0 7 5.4 COc1ccccc1N1CCC2(CCN(CCCSc3nnc(-c4ccccc4)n3C)CC2)CC1 10.1021/acs.jmedchem.9b00412
CHEMBL4084262 157902 0 None 4 13 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-pyrilamine from recombinant human H1 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-pyrilamine from recombinant human H1 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 491 8 0 7 5.4 COc1ccccc1N1CCC2(CCN(CCCSc3nnc(-c4ccccc4)n3C)CC2)CC1 10.1021/acs.jmedchem.9b00412
46884153 8267 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 344 5 0 3 5.2 C[C@@H](c1ncccc1Cl)c1c(CCN(C)C)sc2ccccc12 10.1016/j.bmcl.2010.01.134
CHEMBL1092494 8267 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 344 5 0 3 5.2 C[C@@H](c1ncccc1Cl)c1c(CCN(C)C)sc2ccccc12 10.1016/j.bmcl.2010.01.134
53326726 57761 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 359 7 0 4 4.7 C[C@H](C1=C(CCN(C)Cc2ccco2)Cc2ccccc21)c1cnccn1 10.1016/j.bmcl.2010.12.053
CHEMBL1669418 57761 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 359 7 0 4 4.7 C[C@H](C1=C(CCN(C)Cc2ccco2)Cc2ccccc21)c1cnccn1 10.1016/j.bmcl.2010.12.053
135398737 958 93 None -2 89 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellumDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C4MD00578C
38 958 93 None -2 89 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellumDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C4MD00578C
722 958 93 None -2 89 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellumDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C4MD00578C
CHEMBL42 958 93 None -2 89 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellumDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C4MD00578C
DB00363 958 93 None -2 89 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellumDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C4MD00578C
11846300 80266 3 None 2 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL213912 80266 3 None 2 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1016/j.bmcl.2015.12.035
46889257 7528 0 None 301 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation counting
ChEMBL 350 5 0 5 3.2 COc1ccc(Cn2c(N3CC[C@@H](N(C)C)C3)nc3ccccc32)cc1 10.1016/j.bmcl.2010.03.027
CHEMBL1087367 7528 0 None 301 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation counting
ChEMBL 350 5 0 5 3.2 COc1ccc(Cn2c(N3CC[C@@H](N(C)C)C3)nc3ccccc32)cc1 10.1016/j.bmcl.2010.03.027
11140 2519 49 None -9 3 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: The pharmacological profile of metopimazine, metopimazine acid (MPZA), domperidone, and metoclopramide were assessed by radioligand binding and by a functional antagonist assay. For the radioligand binding assay, cell membranes of dopamine D2 receptor expressing cells were incubated with [3H]spiperone and competing drugs in buffer. The assay was terminated by rapid filtration, and the bound radioactive signal was determined by liquid scintillation counting.Radioligand Binding Assay: The pharmacological profile of metopimazine, metopimazine acid (MPZA), domperidone, and metoclopramide were assessed by radioligand binding and by a functional antagonist assay. For the radioligand binding assay, cell membranes of dopamine D2 receptor expressing cells were incubated with [3H]spiperone and competing drugs in buffer. The assay was terminated by rapid filtration, and the bound radioactive signal was determined by liquid scintillation counting.
ChEMBL 445 6 1 6 3.3 NC(=O)C1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)S(=O)(=O)C nan
1784 2519 49 None -9 3 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: The pharmacological profile of metopimazine, metopimazine acid (MPZA), domperidone, and metoclopramide were assessed by radioligand binding and by a functional antagonist assay. For the radioligand binding assay, cell membranes of dopamine D2 receptor expressing cells were incubated with [3H]spiperone and competing drugs in buffer. The assay was terminated by rapid filtration, and the bound radioactive signal was determined by liquid scintillation counting.Radioligand Binding Assay: The pharmacological profile of metopimazine, metopimazine acid (MPZA), domperidone, and metoclopramide were assessed by radioligand binding and by a functional antagonist assay. For the radioligand binding assay, cell membranes of dopamine D2 receptor expressing cells were incubated with [3H]spiperone and competing drugs in buffer. The assay was terminated by rapid filtration, and the bound radioactive signal was determined by liquid scintillation counting.
ChEMBL 445 6 1 6 3.3 NC(=O)C1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)S(=O)(=O)C nan
26388 2519 49 None -9 3 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: The pharmacological profile of metopimazine, metopimazine acid (MPZA), domperidone, and metoclopramide were assessed by radioligand binding and by a functional antagonist assay. For the radioligand binding assay, cell membranes of dopamine D2 receptor expressing cells were incubated with [3H]spiperone and competing drugs in buffer. The assay was terminated by rapid filtration, and the bound radioactive signal was determined by liquid scintillation counting.Radioligand Binding Assay: The pharmacological profile of metopimazine, metopimazine acid (MPZA), domperidone, and metoclopramide were assessed by radioligand binding and by a functional antagonist assay. For the radioligand binding assay, cell membranes of dopamine D2 receptor expressing cells were incubated with [3H]spiperone and competing drugs in buffer. The assay was terminated by rapid filtration, and the bound radioactive signal was determined by liquid scintillation counting.
ChEMBL 445 6 1 6 3.3 NC(=O)C1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)S(=O)(=O)C nan
CHEMBL398615 2519 49 None -9 3 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: The pharmacological profile of metopimazine, metopimazine acid (MPZA), domperidone, and metoclopramide were assessed by radioligand binding and by a functional antagonist assay. For the radioligand binding assay, cell membranes of dopamine D2 receptor expressing cells were incubated with [3H]spiperone and competing drugs in buffer. The assay was terminated by rapid filtration, and the bound radioactive signal was determined by liquid scintillation counting.Radioligand Binding Assay: The pharmacological profile of metopimazine, metopimazine acid (MPZA), domperidone, and metoclopramide were assessed by radioligand binding and by a functional antagonist assay. For the radioligand binding assay, cell membranes of dopamine D2 receptor expressing cells were incubated with [3H]spiperone and competing drugs in buffer. The assay was terminated by rapid filtration, and the bound radioactive signal was determined by liquid scintillation counting.
ChEMBL 445 6 1 6 3.3 NC(=O)C1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)S(=O)(=O)C nan
DB13591 2519 49 None -9 3 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: The pharmacological profile of metopimazine, metopimazine acid (MPZA), domperidone, and metoclopramide were assessed by radioligand binding and by a functional antagonist assay. For the radioligand binding assay, cell membranes of dopamine D2 receptor expressing cells were incubated with [3H]spiperone and competing drugs in buffer. The assay was terminated by rapid filtration, and the bound radioactive signal was determined by liquid scintillation counting.Radioligand Binding Assay: The pharmacological profile of metopimazine, metopimazine acid (MPZA), domperidone, and metoclopramide were assessed by radioligand binding and by a functional antagonist assay. For the radioligand binding assay, cell membranes of dopamine D2 receptor expressing cells were incubated with [3H]spiperone and competing drugs in buffer. The assay was terminated by rapid filtration, and the bound radioactive signal was determined by liquid scintillation counting.
ChEMBL 445 6 1 6 3.3 NC(=O)C1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)S(=O)(=O)C nan
100 3805 58 None -7 55 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
2637 3805 58 None -7 55 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
5452 3805 58 None -7 55 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
CHEMBL479 3805 58 None -7 55 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
DB00679 3805 58 None -7 55 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
1547484 940 74 None -1 20 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
654 940 74 None -1 20 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
9072 940 74 None -1 20 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
CHEMBL43064 940 74 None -1 20 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
DB00568 940 74 None -1 20 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
2337 3256 77 None 1 62 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
50 3256 77 None 1 62 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
5002 3256 77 None 1 62 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
CHEMBL716 3256 77 None 1 62 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
DB01224 3256 77 None 1 62 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
49836295 18766 0 None 2 4 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]pyrilamine from histamine H1 receptor in Sprague-Dawley rat cortical membrane by liquid scintillation countingDisplacement of [3H]pyrilamine from histamine H1 receptor in Sprague-Dawley rat cortical membrane by liquid scintillation counting
ChEMBL 373 2 1 2 4.3 O=C(O)C1=CCCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
CHEMBL1277935 18766 0 None 2 4 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]pyrilamine from histamine H1 receptor in Sprague-Dawley rat cortical membrane by liquid scintillation countingDisplacement of [3H]pyrilamine from histamine H1 receptor in Sprague-Dawley rat cortical membrane by liquid scintillation counting
ChEMBL 373 2 1 2 4.3 O=C(O)C1=CCCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1 10.1021/jm100856p
51039225 57765 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 359 7 1 4 3.8 C[C@H](C1=C(CCN(C)Cc2ncc[nH]2)Cc2ccccc21)c1cnccn1 10.1016/j.bmcl.2010.12.053
CHEMBL1669422 57765 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 359 7 1 4 3.8 C[C@H](C1=C(CCN(C)Cc2ncc[nH]2)Cc2ccccc21)c1cnccn1 10.1016/j.bmcl.2010.12.053
46884669 8222 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 309 6 0 4 3.0 COc1ccc2c(c1)CC(CCN(C)C)=C2Cc1cnccn1 10.1016/j.bmcl.2010.02.055
CHEMBL1092258 8222 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity at histamine H1 receptorBinding affinity at histamine H1 receptor
ChEMBL 309 6 0 4 3.0 COc1ccc2c(c1)CC(CCN(C)C)=C2Cc1cnccn1 10.1016/j.bmcl.2010.02.055
9979272 207058 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 415 2 0 3 5.6 Cc1ncccc1CN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/acs.jmedchem.9b00447
CHEMBL91729 207058 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting methodDisplacement of [3H]mepyramine from N-terminal HA-tagged H1R (unknown origin) expressed in HEK293T cells measured after 4 hrs by microbeta scintillation counting method
ChEMBL 415 2 0 3 5.6 Cc1ncccc1CN1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/acs.jmedchem.9b00447
57394285 70458 0 None -24 7 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-Pyrilamine from human histamine H1 receptor by liquid scintillation counterDisplacement of [3H]-Pyrilamine from human histamine H1 receptor by liquid scintillation counter
ChEMBL 378 6 0 3 5.2 Fc1ccc(SCCCN2CCCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2012.01.022
CHEMBL1946125 70458 0 None -24 7 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-Pyrilamine from human histamine H1 receptor by liquid scintillation counterDisplacement of [3H]-Pyrilamine from human histamine H1 receptor by liquid scintillation counter
ChEMBL 378 6 0 3 5.2 Fc1ccc(SCCCN2CCCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2012.01.022
44334252 4548 0 None -257 3 Human 4.1 pKi = 4.1 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 449 10 3 7 1.7 CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@@H](CO)NC(=O)OC(C)(C)C)C2)cc1 10.1016/s0960-894x(02)00685-6
CHEMBL102390 4548 0 None -257 3 Human 4.1 pKi = 4.1 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 449 10 3 7 1.7 CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@@H](CO)NC(=O)OC(C)(C)C)C2)cc1 10.1016/s0960-894x(02)00685-6
14554123 118982 0 None - 1 Rat 7.1 pKi = 7.1 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 394 0 0 2 5.3 CC(C)(C)C(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/jm00105a069
CHEMBL342455 118982 0 None - 1 Rat 7.1 pKi = 7.1 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 394 0 0 2 5.3 CC(C)(C)C(=O)N1CCC(=C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1021/jm00105a069
44335412 107459 0 None 1 3 Human 7.1 pKi = 7.1 Binding
Binding affinity at human cortical Histamine 1 receptorBinding affinity at human cortical Histamine 1 receptor
ChEMBL 413 8 0 6 3.8 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc([N+](=O)[O-])cc3)cc2)CC1 10.1016/s0960-894x(02)00648-0
CHEMBL318320 107459 0 None 1 3 Human 7.1 pKi = 7.1 Binding
Binding affinity at human cortical Histamine 1 receptorBinding affinity at human cortical Histamine 1 receptor
ChEMBL 413 8 0 6 3.8 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc([N+](=O)[O-])cc3)cc2)CC1 10.1016/s0960-894x(02)00648-0
162655663 180807 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to H1 receptor (unknown origin)Binding affinity to H1 receptor (unknown origin)
ChEMBL 308 4 0 2 3.4 CN(C)CCCN1C(=O)c2ccccc2CCc2ccccc21 10.1016/j.bmcl.2020.127493
CHEMBL4756695 180807 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to H1 receptor (unknown origin)Binding affinity to H1 receptor (unknown origin)
ChEMBL 308 4 0 2 3.4 CN(C)CCCN1C(=O)c2ccccc2CCc2ccccc21 10.1016/j.bmcl.2020.127493
44304284 163279 0 None -20 3 Human 6.1 pKi = 6.1 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 426 9 0 6 3.5 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3ccc(OC)cc3)cc2)CC1 10.1016/s0960-894x(02)00309-8
CHEMBL418691 163279 0 None -20 3 Human 6.1 pKi = 6.1 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 426 9 0 6 3.5 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3ccc(OC)cc3)cc2)CC1 10.1016/s0960-894x(02)00309-8
44304445 202988 0 None -72 3 Human 5.1 pKi = 5.1 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 531 14 1 6 5.3 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](CC(C)C)NC(=O)OC(C)(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
CHEMBL63112 202988 0 None -72 3 Human 5.1 pKi = 5.1 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 531 14 1 6 5.3 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](CC(C)C)NC(=O)OC(C)(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
44304752 203212 0 None -3890 3 Human 5.1 pKi = 5.1 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 459 9 1 6 3.1 C[C@@H](NC(=O)OC(C)(C)C)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL64406 203212 0 None -3890 3 Human 5.1 pKi = 5.1 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 459 9 1 6 3.1 C[C@@H](NC(=O)OC(C)(C)C)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
127036981 137450 0 None 1 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 399 5 1 5 3.6 CN1CCN(c2nc(NCCc3ccccc3)c3c(n2)-c2ccccc2CC3)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3753621 137450 0 None 1 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 399 5 1 5 3.6 CN1CCN(c2nc(NCCc3ccccc3)c3c(n2)-c2ccccc2CC3)CC1 10.1016/j.bmcl.2015.12.035
2421311 69032 3 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 302 5 1 5 3.4 NCCSc1nc(C2CCCCC2)n(-c2ccccc2)n1 10.1021/jm2011589
CHEMBL1923534 69032 3 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 302 5 1 5 3.4 NCCSc1nc(C2CCCCC2)n(-c2ccccc2)n1 10.1021/jm2011589
145988693 167166 0 None -32 17 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Pyrilamine from human H1 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 524 7 1 3 7.1 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL4291048 167166 0 None -32 17 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Pyrilamine from human H1 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 524 7 1 3 7.1 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
162662985 181979 0 None -1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-pyrilamine from human H1 histamine receptor expressed in human HEK293 cellsDisplacement of [3H]-pyrilamine from human H1 histamine receptor expressed in human HEK293 cells
ChEMBL 414 5 1 3 5.3 C[C@H]1CN(CC[C@H]2CC[C@H](NC(=O)c3ccco3)CC2)CCc2ccc(Cl)cc21 10.1016/j.bmcl.2020.127681
CHEMBL4780335 181979 0 None -1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-pyrilamine from human H1 histamine receptor expressed in human HEK293 cellsDisplacement of [3H]-pyrilamine from human H1 histamine receptor expressed in human HEK293 cells
ChEMBL 414 5 1 3 5.3 C[C@H]1CN(CC[C@H]2CC[C@H](NC(=O)c3ccco3)CC2)CCc2ccc(Cl)cc21 10.1016/j.bmcl.2020.127681
24740862 148008 0 None -4 5 Human 6.1 pKi = 6.1 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 369 6 1 5 4.4 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1F 10.1016/j.bmcl.2009.09.024
CHEMBL393436 148008 0 None -4 5 Human 6.1 pKi = 6.1 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 369 6 1 5 4.4 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1F 10.1016/j.bmcl.2009.09.024
127052467 140851 0 None -23 7 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 1 1 4.5 c1ccc2c(c1)CCN(CCCCc1c[nH]c3ccccc13)C2 10.1016/j.bmc.2016.05.053
CHEMBL3819494 140851 0 None -23 7 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 1 1 4.5 c1ccc2c(c1)CCN(CCCCc1c[nH]c3ccccc13)C2 10.1016/j.bmc.2016.05.053
168290238 191975 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 769 20 6 8 1.7 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5201159 191975 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 769 20 6 8 1.7 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
168290238 191975 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 769 20 6 8 1.7 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5201159 191975 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 769 20 6 8 1.7 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
127052635 140207 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 incubated for 60 mins by liquid scintillation counting method
ChEMBL 288 5 3 3 2.0 CC(C)CN/C(=N/C#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805003 140207 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 incubated for 60 mins by liquid scintillation counting method
ChEMBL 288 5 3 3 2.0 CC(C)CN/C(=N/C#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
127052467 140851 0 None -23 7 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 1 1 4.5 c1ccc2c(c1)CCN(CCCCc1c[nH]c3ccccc13)C2 10.1016/j.bmc.2016.05.053
CHEMBL3819494 140851 0 None -23 7 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 1 1 4.5 c1ccc2c(c1)CCN(CCCCc1c[nH]c3ccccc13)C2 10.1016/j.bmc.2016.05.053
11948707 166167 0 None -2041 13 Human 6.1 pKi = 6.1 Binding
Binding affinity to histamine H1 receptor by radioligand binding assayBinding affinity to histamine H1 receptor by radioligand binding assay
ChEMBL 373 7 0 8 0.6 COc1cccc(N2CCN(CCCCn3ncc(=O)n(C)c3=O)CC2)c1 10.1016/j.bmcl.2006.01.052
CHEMBL426317 166167 0 None -2041 13 Human 6.1 pKi = 6.1 Binding
Binding affinity to histamine H1 receptor by radioligand binding assayBinding affinity to histamine H1 receptor by radioligand binding assay
ChEMBL 373 7 0 8 0.6 COc1cccc(N2CCN(CCCCn3ncc(=O)n(C)c3=O)CC2)c1 10.1016/j.bmcl.2006.01.052
44361141 32801 0 None - 1 Rat 6.1 pKi = 6.1 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 340 3 0 2 4.1 CC(=O)N(C)CC/C=C1/c2ccc(Cl)cc2CCc2cccnc21 10.1021/jm00105a069
CHEMBL141432 32801 0 None - 1 Rat 6.1 pKi = 6.1 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
ChEMBL 340 3 0 2 4.1 CC(=O)N(C)CC/C=C1/c2ccc(Cl)cc2CCc2cccnc21 10.1021/jm00105a069
155559236 174852 0 None - 1 Guinea pig 6.1 pKi = 6.1 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysisDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysis
ChEMBL 318 6 0 4 1.8 CN1CCc2ccc(OCCCCN3CCOCC3)cc2C1=O 10.1016/j.bmcl.2019.04.015
CHEMBL4563108 174852 0 None - 1 Guinea pig 6.1 pKi = 6.1 Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysisDisplacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by Cheng and Prusoff equation analysis by scintillation counting analysis
ChEMBL 318 6 0 4 1.8 CN1CCc2ccc(OCCCCN3CCOCC3)cc2C1=O 10.1016/j.bmcl.2019.04.015
27620 140818 13 None -38 8 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 297 5 0 2 3.8 O=C(CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818994 140818 13 None -38 8 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]Pyrilamine from human H1 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 297 5 0 2 3.8 O=C(CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
132060763 162861 0 None -3 8 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-Pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 405 5 0 4 4.1 C=C(C)CN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)CC3)CC1 10.1016/j.ejmech.2018.02.024
CHEMBL4173095 162861 0 None -3 8 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-Pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 405 5 0 4 4.1 C=C(C)CN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)CC3)CC1 10.1016/j.ejmech.2018.02.024
135409492 169170 50 None 1 3 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity of compound against histamine H1 neuronal receptorIn vitro binding affinity of compound against histamine H1 neuronal receptor
ChEMBL 328 0 1 5 3.5 Cc1cc2c(s1)Nc1ccccc1N=C2N1CC[N+](C)([O-])CC1 10.1016/S0960-894X(96)00567-7
CHEMBL440512 169170 50 None 1 3 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity of compound against histamine H1 neuronal receptorIn vitro binding affinity of compound against histamine H1 neuronal receptor
ChEMBL 328 0 1 5 3.5 Cc1cc2c(s1)Nc1ccccc1N=C2N1CC[N+](C)([O-])CC1 10.1016/S0960-894X(96)00567-7
44304307 203233 0 None -134 3 Human 6.1 pKi = 6.1 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 388 12 0 4 4.2 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)CCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL64479 203233 0 None -134 3 Human 6.1 pKi = 6.1 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 388 12 0 4 4.2 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)CCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
164610648 184838 0 None -87 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 374 7 4 4 2.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4852212 184838 0 None -87 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 374 7 4 4 2.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
164609729 185098 0 None -1412 6 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 360 6 4 4 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4856059 185098 0 None -1412 6 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 360 6 4 4 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
25218401 74945 0 None -43651 3 Human 5.1 pKi = 5.1 Binding
Binding affinity to H1 receptorBinding affinity to H1 receptor
ChEMBL 431 5 0 3 4.1 C[C@@H]1CCCN1CCN1CCc2cc(-c3ccc(C(=O)N4CCCC4)cc3)ccc2C1=O 10.1021/jm300011d
CHEMBL2031885 74945 0 None -43651 3 Human 5.1 pKi = 5.1 Binding
Binding affinity to H1 receptorBinding affinity to H1 receptor
ChEMBL 431 5 0 3 4.1 C[C@@H]1CCCN1CCN1CCc2cc(-c3ccc(C(=O)N4CCCC4)cc3)ccc2C1=O 10.1021/jm300011d
127048828 140320 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 incubated for 60 mins by liquid scintillation counting method
ChEMBL 288 5 3 3 2.0 CC(C)CN/C(=N/C#N)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3806255 140320 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 incubated for 60 mins by liquid scintillation counting method
ChEMBL 288 5 3 3 2.0 CC(C)CN/C(=N/C#N)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
13091268 78224 0 None -9549 14 Human 5.1 pKi = 5.1 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL210578 78224 0 None -9549 14 Human 5.1 pKi = 5.1 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
13091268 78224 0 None -9549 14 Human 5.1 pKi = 5.1 Binding
Binding affinity to human cloned histamine H1 receptor by radioligand binding assayBinding affinity to human cloned histamine H1 receptor by radioligand binding assay
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2006.03.057
CHEMBL210578 78224 0 None -9549 14 Human 5.1 pKi = 5.1 Binding
Binding affinity to human cloned histamine H1 receptor by radioligand binding assayBinding affinity to human cloned histamine H1 receptor by radioligand binding assay
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2006.03.057
13091268 78224 0 None -9549 14 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation countingDisplacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation counting
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
CHEMBL210578 78224 0 None -9549 14 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation countingDisplacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation counting
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
2389 3331 118 None -46 67 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human H1 receptorBinding affinity towards human H1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm0002432
5073 3331 118 None -46 67 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human H1 receptorBinding affinity towards human H1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm0002432
96 3331 118 None -46 67 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human H1 receptorBinding affinity towards human H1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm0002432
CHEMBL85 3331 118 None -46 67 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human H1 receptorBinding affinity towards human H1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm0002432
DB00734 3331 118 None -46 67 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human H1 receptorBinding affinity towards human H1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm0002432
71459604 83793 0 None -15 14 Human 5.1 pKi = 5.1 Binding
Binding affinity to Histamine H1 receptorBinding affinity to Histamine H1 receptor
ChEMBL 309 4 1 3 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1 10.1016/j.bmcl.2012.08.046
CHEMBL2205811 83793 0 None -15 14 Human 5.1 pKi = 5.1 Binding
Binding affinity to Histamine H1 receptorBinding affinity to Histamine H1 receptor
ChEMBL 309 4 1 3 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1 10.1016/j.bmcl.2012.08.046
168288775 191446 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 785 21 7 9 0.7 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5193095 191446 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 785 21 7 9 0.7 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
168288775 191446 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 785 21 7 9 0.7 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5193095 191446 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 785 21 7 9 0.7 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
9851785 51911 0 None -371 3 Human 6.1 pKi = 6.1 Binding
Binding affinity towards histamine H1 receptor of human colon cells was determinedBinding affinity towards histamine H1 receptor of human colon cells was determined
ChEMBL 606 12 1 8 4.4 C[C@@H](NC(=O)c1ccc(N(C)C)cc1)C(=O)N1CCN(CCCOc2ccc(-c3noc(CC4CCCC4)n3)c(F)c2)CC1 10.1016/j.bmcl.2003.11.038
CHEMBL158595 51911 0 None -371 3 Human 6.1 pKi = 6.1 Binding
Binding affinity towards histamine H1 receptor of human colon cells was determinedBinding affinity towards histamine H1 receptor of human colon cells was determined
ChEMBL 606 12 1 8 4.4 C[C@@H](NC(=O)c1ccc(N(C)C)cc1)C(=O)N1CCN(CCCOc2ccc(-c3noc(CC4CCCC4)n3)c(F)c2)CC1 10.1016/j.bmcl.2003.11.038
44334038 4462 0 None -3162 3 Human 5.1 pKi = 5.1 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 453 10 1 6 3.0 N#Cc1cccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)c1 10.1016/s0960-894x(02)00685-6
CHEMBL101748 4462 0 None -3162 3 Human 5.1 pKi = 5.1 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 453 10 1 6 3.0 N#Cc1cccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)c1 10.1016/s0960-894x(02)00685-6
127036980 137346 0 None 16 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 385 4 1 5 3.6 CN1CCN(c2nc(NCc3ccccc3)c3c(n2)-c2ccccc2CC3)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3752885 137346 0 None 16 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 385 4 1 5 3.6 CN1CCN(c2nc(NCc3ccccc3)c3c(n2)-c2ccccc2CC3)CC1 10.1016/j.bmcl.2015.12.035
44335405 5103 0 None -75 4 Human 5.1 pKi = 5.1 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 321 6 1 4 2.9 N#Cc1ccc(-c2ccc(OCCCN3CCNCC3)cc2)cc1 10.1016/s0960-894x(02)00648-0
CHEMBL105594 5103 0 None -75 4 Human 5.1 pKi = 5.1 Binding
Binding affinity of human cortical histamine H1 receptorBinding affinity of human cortical histamine H1 receptor
ChEMBL 321 6 1 4 2.9 N#Cc1ccc(-c2ccc(OCCCN3CCNCC3)cc2)cc1 10.1016/s0960-894x(02)00648-0
168283097 192893 0 None -66 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 311 9 4 5 0.8 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)o1 10.1021/acs.jmedchem.1c00692
CHEMBL5186770 192893 0 None -66 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 311 9 4 5 0.8 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)o1 10.1021/acs.jmedchem.1c00692
CHEMBL5222043 192893 0 None -66 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 311 9 4 5 0.8 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)o1 10.1021/acs.jmedchem.1c00692
168284480 192910 0 None -66 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 330 6 4 4 1.3 Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCc1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5197548 192910 0 None -66 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 330 6 4 4 1.3 Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCc1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222137 192910 0 None -66 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 330 6 4 4 1.3 Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCc1ccccc1 10.1021/acs.jmedchem.1c00692
44395530 67073 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human histamine H1 receptor expressed in CHO-K1 cellsBinding affinity towards human histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 546 10 2 5 5.0 NC(=O)N(O)CCC#Cc1ccc(OCCCN2CCN([C@H](c3ccccc3)c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmcl.2004.08.060
CHEMBL187264 67073 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human histamine H1 receptor expressed in CHO-K1 cellsBinding affinity towards human histamine H1 receptor expressed in CHO-K1 cells
ChEMBL 546 10 2 5 5.0 NC(=O)N(O)CCC#Cc1ccc(OCCCN2CCN([C@H](c3ccccc3)c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmcl.2004.08.060
10027435 47495 0 None 11 4 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]- pyrilamine from rat brain membrane Histamine H1 receptorDisplacement of [3H]- pyrilamine from rat brain membrane Histamine H1 receptor
ChEMBL 463 7 0 5 5.0 Cn1c(=O)sc2cc(CCCCN3CCN(Cc4ccc(Cl)c(Cl)c4)CC3)ccc21 10.1016/s0960-894x(02)00123-3
CHEMBL15456 47495 0 None 11 4 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]- pyrilamine from rat brain membrane Histamine H1 receptorDisplacement of [3H]- pyrilamine from rat brain membrane Histamine H1 receptor
ChEMBL 463 7 0 5 5.0 Cn1c(=O)sc2cc(CCCCN3CCN(Cc4ccc(Cl)c(Cl)c4)CC3)ccc21 10.1016/s0960-894x(02)00123-3
21474204 54774 0 None 3 4 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]- pyrilamine from rat brain membrane Histamine H1 receptorDisplacement of [3H]- pyrilamine from rat brain membrane Histamine H1 receptor
ChEMBL 394 7 0 4 4.9 Cn1c(=O)sc2cc(CCCCN3CCC(Cc4ccccc4)CC3)ccc21 10.1016/s0960-894x(02)00123-3
CHEMBL16123 54774 0 None 3 4 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]- pyrilamine from rat brain membrane Histamine H1 receptorDisplacement of [3H]- pyrilamine from rat brain membrane Histamine H1 receptor
ChEMBL 394 7 0 4 4.9 Cn1c(=O)sc2cc(CCCCN3CCC(Cc4ccccc4)CC3)ccc21 10.1016/s0960-894x(02)00123-3
10382839 116552 0 None - 1 Guinea pig 8.1 pKi = 8.1 Binding
Inhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptorInhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptor
ChEMBL 343 5 1 4 3.7 CN(C)CCSC1c2ccccc2COc2ccc(C(=O)O)cc21 10.1021/jm00055a013
CHEMBL336317 116552 0 None - 1 Guinea pig 8.1 pKi = 8.1 Binding
Inhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptorInhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptor
ChEMBL 343 5 1 4 3.7 CN(C)CCSC1c2ccccc2COc2ccc(C(=O)O)cc21 10.1021/jm00055a013
CHEMBL538750 116552 0 None - 1 Guinea pig 8.1 pKi = 8.1 Binding
Inhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptorInhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptor
ChEMBL 343 5 1 4 3.7 CN(C)CCSC1c2ccccc2COc2ccc(C(=O)O)cc21 10.1021/jm00055a013
44326422 112393 0 None 1 3 Human 8.0 pKi = 8.0 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 279 2 1 2 3.4 CNCC1C[C@@H]2c3ccccc3Cc3ccccc3[C@H]2O1 10.1016/j.bmcl.2004.03.069
CHEMBL329685 112393 0 None 1 3 Human 8.0 pKi = 8.0 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 279 2 1 2 3.4 CNCC1C[C@@H]2c3ccccc3Cc3ccccc3[C@H]2O1 10.1016/j.bmcl.2004.03.069
11500781 8203 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 324 5 0 3 4.9 Cc1cccnc1[C@H](C)c1c(CCN(C)C)sc2ccccc12 10.1016/j.bmcl.2010.01.134
CHEMBL1092126 8203 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation counting
ChEMBL 324 5 0 3 4.9 Cc1cccnc1[C@H](C)c1c(CCN(C)C)sc2ccccc12 10.1016/j.bmcl.2010.01.134
10851717 78477 1 None 11 5 Rat 8.0 pKi = 8.0 Binding
Half-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenateHalf-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenate
ChEMBL 299 1 0 4 2.9 CN1CCN([C@@H]2Cn3cccc3Sc3ccccc32)CC1 10.1021/jm010982y
CHEMBL2111782 78477 1 None 11 5 Rat 8.0 pKi = 8.0 Binding
Half-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenateHalf-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenate
ChEMBL 299 1 0 4 2.9 CN1CCN([C@@H]2Cn3cccc3Sc3ccccc32)CC1 10.1021/jm010982y
44389292 63811 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity for human Histamine H1 receptor in CHO K1 cellsBinding affinity for human Histamine H1 receptor in CHO K1 cells
ChEMBL 605 12 1 6 6.5 CC(C)OC(=O)N(O)CCC#Cc1ccc(OCCCCN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2004.12.023
CHEMBL180233 63811 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity for human Histamine H1 receptor in CHO K1 cellsBinding affinity for human Histamine H1 receptor in CHO K1 cells
ChEMBL 605 12 1 6 6.5 CC(C)OC(=O)N(O)CCC#Cc1ccc(OCCCCN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2004.12.023
44326358 207302 0 None 3 3 Human 8.0 pKi = 8.0 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 309 2 0 3 3.8 CN(C)CC1C[C@@H]2c3ccccc3OCc3ccccc3[C@H]2O1 10.1016/j.bmcl.2004.03.069
CHEMBL93321 207302 0 None 3 3 Human 8.0 pKi = 8.0 Binding
Ability to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cellsAbility to displace [3H]pyrilamine from human cloned histamine H1 receptor expressed in CHO cells
ChEMBL 309 2 0 3 3.8 CN(C)CC1C[C@@H]2c3ccccc3OCc3ccccc3[C@H]2O1 10.1016/j.bmcl.2004.03.069
2398 954 62 None -1 29 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
2801 954 62 None -1 29 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
701 954 62 None -1 29 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
CHEMBL415 954 62 None -1 29 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
DB01242 954 62 None -1 29 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
132356 14677 1 None - 1 Guinea pig 8.0 pKi = 8 Binding
Inhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptorInhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptor
ChEMBL 473 7 1 4 6.1 O=C(O)c1ccc2c(c1)C(SCCN1CCC(Cc3ccccc3)CC1)c1ccccc1CO2 10.1021/jm00055a013
CHEMBL1205688 14677 1 None - 1 Guinea pig 8.0 pKi = 8 Binding
Inhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptorInhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptor
ChEMBL 473 7 1 4 6.1 O=C(O)c1ccc2c(c1)C(SCCN1CCC(Cc3ccccc3)CC1)c1ccccc1CO2 10.1021/jm00055a013
CHEMBL133778 14677 1 None - 1 Guinea pig 8.0 pKi = 8 Binding
Inhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptorInhibition of the specific binding of [3H]pyrilamine to guinea pig cerebellum histamine H1 receptor
ChEMBL 473 7 1 4 6.1 O=C(O)c1ccc2c(c1)C(SCCN1CCC(Cc3ccccc3)CC1)c1ccccc1CO2 10.1021/jm00055a013
44334521 107836 0 None -85 3 Human 4.1 pKi = 4.1 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 262 6 1 4 1.7 CC(=O)c1ccc(OCCCN2CC[C@H](N)C2)cc1 10.1016/s0960-894x(02)00685-6
CHEMBL319231 107836 0 None -85 3 Human 4.1 pKi = 4.1 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 262 6 1 4 1.7 CC(=O)c1ccc(OCCCN2CC[C@H](N)C2)cc1 10.1016/s0960-894x(02)00685-6
53321511 57754 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 375 7 0 3 4.9 C[C@H](C1=C(CCN(C)CCC(F)(F)F)Cc2ccccc21)c1cnccn1 10.1016/j.bmcl.2010.12.053
CHEMBL1669411 57754 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to histamine H1 receptorBinding affinity to histamine H1 receptor
ChEMBL 375 7 0 3 4.9 C[C@H](C1=C(CCN(C)CCC(F)(F)F)Cc2ccccc21)c1cnccn1 10.1016/j.bmcl.2010.12.053
44288847 165309 0 None -64 5 Human 7.0 pKi = 7.0 Binding
Selectivity screen against human Histamine H1 receptorSelectivity screen against human Histamine H1 receptor
ChEMBL 535 7 2 5 3.9 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1 10.1016/s0960-894x(99)00696-4
CHEMBL42335 165309 0 None -64 5 Human 7.0 pKi = 7.0 Binding
Selectivity screen against human Histamine H1 receptorSelectivity screen against human Histamine H1 receptor
ChEMBL 535 7 2 5 3.9 CC1=C(C(=O)NCCCN2CCC(C#N)(c3ccc(F)cc3C#N)CC2)[C@@H](c2ccc(F)c(F)c2)CC(=O)N1 10.1016/s0960-894x(99)00696-4
44334430 4454 0 None -3019 3 Human 5.0 pKi = 5.0 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 428 10 1 5 3.1 O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccccc3)C2)cc1)C1CC1 10.1016/s0960-894x(02)00685-6
CHEMBL101691 4454 0 None -3019 3 Human 5.0 pKi = 5.0 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 428 10 1 5 3.1 O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccccc3)C2)cc1)C1CC1 10.1016/s0960-894x(02)00685-6
44334234 109679 0 None -9120 3 Human 4.0 pKi = 4.0 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 432 10 1 7 1.8 Cn1cnc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)c1 10.1016/s0960-894x(02)00685-6
CHEMBL322678 109679 0 None -9120 3 Human 4.0 pKi = 4.0 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 432 10 1 7 1.8 Cn1cnc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)c1 10.1016/s0960-894x(02)00685-6
10065083 32103 1 None -141 10 Human 6.0 pKi = 6.0 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 328 6 0 5 2.4 O=C(CCCN1CCN(c2ncccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL140872 32103 1 None -141 10 Human 6.0 pKi = 6.0 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 328 6 0 5 2.4 O=C(CCCN1CCN(c2ncccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
10065083 32103 1 None -141 10 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]pyrilamine from human H1 receptor by liquid scintillation countingDisplacement of [3H]pyrilamine from human H1 receptor by liquid scintillation counting
ChEMBL 328 6 0 5 2.4 O=C(CCCN1CCN(c2ncccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2011.12.019
CHEMBL140872 32103 1 None -141 10 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]pyrilamine from human H1 receptor by liquid scintillation countingDisplacement of [3H]pyrilamine from human H1 receptor by liquid scintillation counting
ChEMBL 328 6 0 5 2.4 O=C(CCCN1CCN(c2ncccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2011.12.019
168273267 190499 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 698 17 5 7 2.2 C[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5179303 190499 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 698 17 5 7 2.2 C[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
168273267 190499 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 698 17 5 7 2.2 C[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5179303 190499 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 698 17 5 7 2.2 C[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
25128822 187481 0 None -1698 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 295 1 1 5 1.6 CN1CCN(c2nc(N)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL494093 187481 0 None -1698 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 295 1 1 5 1.6 CN1CCN(c2nc(N)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
10201714 198714 0 None -39 2 Rat 6.0 pKi = 6.0 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
ChEMBL 411 10 3 3 4.3 O=C(NCCCCc1c[nH]cn1)NCCC(c1ccc(Cl)cc1)c1ccccn1 10.1016/s0960-894x(03)00357-3
CHEMBL58239 198714 0 None -39 2 Rat 6.0 pKi = 6.0 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
ChEMBL 411 10 3 3 4.3 O=C(NCCCCc1c[nH]cn1)NCCC(c1ccc(Cl)cc1)c1ccccn1 10.1016/s0960-894x(03)00357-3
44334395 4961 0 None -2630 3 Human 5.0 pKi = 5.0 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 446 10 1 5 3.2 O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccc(F)cc3)C2)cc1)C1CC1 10.1016/s0960-894x(02)00685-6
CHEMBL104808 4961 0 None -2630 3 Human 5.0 pKi = 5.0 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 446 10 1 5 3.2 O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccc(F)cc3)C2)cc1)C1CC1 10.1016/s0960-894x(02)00685-6
46882133 5808 0 None -5 7 Human 6.0 pKi = 6.0 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 478 9 2 7 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(NC(=O)C5CCC5)ccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
CHEMBL1078896 5808 0 None -5 7 Human 6.0 pKi = 6.0 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 478 9 2 7 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(NC(=O)C5CCC5)ccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
168294661 192402 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 764 19 6 8 2.2 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5207888 192402 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 764 19 6 8 2.2 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
44304079 202626 0 None -128 3 Human 6.0 pKi = 6.0 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 376 9 0 5 3.5 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)CC(C)C)cc2)CC1 10.1016/s0960-894x(02)00309-8
CHEMBL61231 202626 0 None -128 3 Human 6.0 pKi = 6.0 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 376 9 0 5 3.5 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)CC(C)C)cc2)CC1 10.1016/s0960-894x(02)00309-8
44304035 203309 0 None -13 3 Human 6.0 pKi = 6.0 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 410 9 0 5 3.7 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)Cc3ccccc3)cc2)CC1 10.1016/s0960-894x(02)00309-8
CHEMBL64799 203309 0 None -13 3 Human 6.0 pKi = 6.0 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 410 9 0 5 3.7 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)Cc3ccccc3)cc2)CC1 10.1016/s0960-894x(02)00309-8
168294661 192402 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 764 19 6 8 2.2 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5207888 192402 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 764 19 6 8 2.2 C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
44304312 162787 0 None -316 3 Human 5.0 pKi = 5.0 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 453 10 1 5 2.9 N[C@H](Cc1ccc(F)cc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL417215 162787 0 None -316 3 Human 5.0 pKi = 5.0 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 453 10 1 5 2.9 N[C@H](Cc1ccc(F)cc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
44304349 202801 0 None -173 3 Human 5.0 pKi = 5.0 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 566 14 1 7 4.9 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](Cc3ccncc3)NC(=O)OC(C)(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
CHEMBL62266 202801 0 None -173 3 Human 5.0 pKi = 5.0 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 566 14 1 7 4.9 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](Cc3ccncc3)NC(=O)OC(C)(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
127036979 137488 0 None -1 2 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 399 5 1 5 3.6 CN1CCN(c2nc(NCCc3ccccc3)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3753962 137488 0 None -1 2 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]mepyramine from human histamine 1 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 399 5 1 5 3.6 CN1CCN(c2nc(NCCc3ccccc3)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
127052292 140266 0 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 incubated for 60 mins by liquid scintillation counting method
ChEMBL 350 7 3 3 2.9 N#C/N=C(/NCCCc1ccccc1)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805663 140266 0 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 incubated for 60 mins by liquid scintillation counting method
ChEMBL 350 7 3 3 2.9 N#C/N=C(/NCCCc1ccccc1)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
50878551 90745 61 None -21 18 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
CHEMBL2391541 90745 61 None -21 18 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
44334396 4916 0 None -3467 3 Human 5.0 pKi = 5.0 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 446 10 1 5 3.2 O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccccc3F)C2)cc1)C1CC1 10.1016/s0960-894x(02)00685-6
CHEMBL104618 4916 0 None -3467 3 Human 5.0 pKi = 5.0 Binding
Binding affinity to the human Histamine H1 receptorBinding affinity to the human Histamine H1 receptor
ChEMBL 446 10 1 5 3.2 O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccccc3F)C2)cc1)C1CC1 10.1016/s0960-894x(02)00685-6
44582676 189779 0 None -7 17 Human 6.0 pKi = 6.0 Binding
Inhibition of human cloned histamine H1 receptor by competitive binding experimentInhibition of human cloned histamine H1 receptor by competitive binding experiment
ChEMBL 403 9 0 4 4.3 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL516088 189779 0 None -7 17 Human 6.0 pKi = 6.0 Binding
Inhibition of human cloned histamine H1 receptor by competitive binding experimentInhibition of human cloned histamine H1 receptor by competitive binding experiment
ChEMBL 403 9 0 4 4.3 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
168274424 190131 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 834 21 7 9 2.8 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5173453 190131 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 834 21 7 9 2.8 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
168297312 192526 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 785 21 7 9 0.7 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5209546 192526 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 785 21 7 9 0.7 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
168274424 190131 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 834 21 7 9 2.8 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5173453 190131 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 834 21 7 9 2.8 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
168297312 192526 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 785 21 7 9 0.7 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
CHEMBL5209546 192526 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assayDisplacement of fluorophore-labeled mepyramine from Nluc-tagged human H1R expressed in HEK293T cells incubated for 2 hrs by NanoBRET competition binding assay
ChEMBL 785 21 7 9 0.7 CC(C)[C@H](NC(=O)CCN1CCC(Oc2ccccc2Cc2ccccc2)CC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.2c00125
168278471 192848 0 None -229 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 312 8 4 4 1.5 CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5183205 192848 0 None -229 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 312 8 4 4 1.5 CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221757 192848 0 None -229 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysisDisplacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis
ChEMBL 312 8 4 4 1.5 CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
164622886 185942 0 None -93 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 374 7 4 4 2.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4869389 185942 0 None -93 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 374 7 4 4 2.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
44304332 201344 0 None -20417 3 Human 4.0 pKi = 4.0 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 399 9 1 5 2.3 O=C(c1ccc(OCCCN2CCN(C(=O)C[C@H]3CCCN3)CC2)cc1)C1CC1 10.1016/s0960-894x(02)00310-4
CHEMBL60435 201344 0 None -20417 3 Human 4.0 pKi = 4.0 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 399 9 1 5 2.3 O=C(c1ccc(OCCCN2CCN(C(=O)C[C@H]3CCCN3)CC2)cc1)C1CC1 10.1016/s0960-894x(02)00310-4
44304719 202722 0 None -20892 3 Human 4.0 pKi = 4.0 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 425 10 2 6 1.5 N[C@H](Cc1c[nH]cn1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL61792 202722 0 None -20892 3 Human 4.0 pKi = 4.0 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 425 10 2 6 1.5 N[C@H](Cc1c[nH]cn1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
135559170 102060 0 None -1479 7 Guinea pig 6.0 pKi = 6.0 Binding
Compound is evaluated for binding affinity towards Histamine H1 receptor using [3H]pyrilamine in guinea pig lungCompound is evaluated for binding affinity towards Histamine H1 receptor using [3H]pyrilamine in guinea pig lung
ChEMBL 391 4 1 5 2.5 COc1ccccc1N1CCN(CC2CN3C(=O)Nc4ccccc4C3=N2)CC1 10.1021/jm970159v
CHEMBL302021 102060 0 None -1479 7 Guinea pig 6.0 pKi = 6.0 Binding
Compound is evaluated for binding affinity towards Histamine H1 receptor using [3H]pyrilamine in guinea pig lungCompound is evaluated for binding affinity towards Histamine H1 receptor using [3H]pyrilamine in guinea pig lung
ChEMBL 391 4 1 5 2.5 COc1ccccc1N1CCN(CC2CN3C(=O)Nc4ccccc4C3=N2)CC1 10.1021/jm970159v
25218143 74933 0 None -5011 3 Human 5.0 pKi = 5.0 Binding
Binding affinity to H1 receptorBinding affinity to H1 receptor
ChEMBL 431 6 1 3 4.1 O=C(NC1CCCC1)c1ccc(-c2ccc3c(c2)CCN(CCN2CCCC2)C3=O)cc1 10.1021/jm300011d
CHEMBL2031873 74933 0 None -5011 3 Human 5.0 pKi = 5.0 Binding
Binding affinity to H1 receptorBinding affinity to H1 receptor
ChEMBL 431 6 1 3 4.1 O=C(NC1CCCC1)c1ccc(-c2ccc3c(c2)CCN(CCN2CCCC2)C3=O)cc1 10.1021/jm300011d
46216789 200328 0 None -2 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]Pyrilamine from human cloned histamine H1 receptorDisplacement of [3H]Pyrilamine from human cloned histamine H1 receptor
ChEMBL 341 7 1 1 5.3 c1ccc(CCCCNCC2c3ccccc3Cc3ccccc32)cc1 10.1016/j.bmcl.2009.12.064
CHEMBL597528 200328 0 None -2 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]Pyrilamine from human cloned histamine H1 receptorDisplacement of [3H]Pyrilamine from human cloned histamine H1 receptor
ChEMBL 341 7 1 1 5.3 c1ccc(CCCCNCC2c3ccccc3Cc3ccccc32)cc1 10.1016/j.bmcl.2009.12.064
44304270 201248 0 None -6 3 Human 7.0 pKi = 7.0 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 442 11 0 5 5.0 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccc(C)s3)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL60383 201248 0 None -6 3 Human 7.0 pKi = 7.0 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 442 11 0 5 5.0 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccc(C)s3)CC2)cc1 10.1016/s0960-894x(02)00309-8
25147771 174238 0 None -3 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in NIH3T3 cellsDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in NIH3T3 cells
ChEMBL 357 4 1 6 3.2 CN1CCN(c2nc(NCc3ccoc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL454890 174238 0 None -3 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]mepyramine from human histamine H1 receptor expressed in NIH3T3 cellsDisplacement of [3H]mepyramine from human histamine H1 receptor expressed in NIH3T3 cells
ChEMBL 357 4 1 6 3.2 CN1CCN(c2nc(NCc3ccoc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
44343936 11059 0 None - 1 Rat 6.0 pKi = 6.0 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 369 1 0 3 3.5 CC(=O)N1CCCN(C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/s0960-894x(98)00626-x
CHEMBL117745 11059 0 None - 1 Rat 6.0 pKi = 6.0 Binding
Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranesBinding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes
ChEMBL 369 1 0 3 3.5 CC(=O)N1CCCN(C2c3ccc(Cl)cc3CCc3cccnc32)CC1 10.1016/s0960-894x(98)00626-x
44350664 118149 0 None -9 6 Human 6.0 pKi = 6.0 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 351 6 0 2 5.2 O=C(CCCN1C2CCC1CC(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL340816 118149 0 None -9 6 Human 6.0 pKi = 6.0 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 351 6 0 2 5.2 O=C(CCCN1C2CCC1CC(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL553417 118149 0 None -9 6 Human 6.0 pKi = 6.0 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
ChEMBL 351 6 0 2 5.2 O=C(CCCN1C2CCC1CC(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
13091359 113539 0 None -1380 10 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation countingDisplacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
CHEMBL3321790 113539 0 None -1380 10 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation countingDisplacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
44304036 96782 0 None -17 3 Human 6.0 pKi = 6.0 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 360 8 0 5 3.0 C=C(C)C(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL264761 96782 0 None -17 3 Human 6.0 pKi = 6.0 Binding
Binding affinity for the human Histamine H1 ReceptorBinding affinity for the human Histamine H1 Receptor
ChEMBL 360 8 0 5 3.0 C=C(C)C(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
1278 2150 84 None -1778 8 Human 6.0 pKi = 6.0 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm8007618
1279 2150 84 None -1778 8 Human 6.0 pKi = 6.0 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm8007618
4908365 2150 84 None -1778 8 Human 6.0 pKi = 6.0 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm8007618
CHEMBL129198 2150 84 None -1778 8 Human 6.0 pKi = 6.0 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm8007618
44304743 100609 0 None -57 3 Human 5.0 pKi = 5.0 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 431 13 1 5 3.7 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](N)CC(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
CHEMBL291847 100609 0 None -57 3 Human 5.0 pKi = 5.0 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 431 13 1 5 3.7 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](N)CC(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
44304064 102810 0 None -323 3 Human 5.0 pKi = 5.0 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 451 10 2 6 2.5 N[C@H](Cc1ccc(O)cc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL305371 102810 0 None -323 3 Human 5.0 pKi = 5.0 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 451 10 2 6 2.5 N[C@H](Cc1ccc(O)cc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
44304313 201585 0 None -426 3 Human 5.0 pKi = 5.0 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 441 10 1 6 2.8 N[C@H](Cc1ccsc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL60559 201585 0 None -426 3 Human 5.0 pKi = 5.0 Binding
Binding affinity towards Histamine H1 receptor of human membranes.Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL 441 10 1 6 2.8 N[C@H](Cc1ccsc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
11525848 114591 31 None - 1 Human 7.0 pKi = 7.0 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000729a HRH1Selectivity interaction (GPCR panel (PDSP screen)) EUB0000729a HRH1
ChEMBL 479 9 3 7 3.3 COc1cccc(CNC(=O)c2nc3scc(COCc4ccc(C(=O)O)cc4)c3c(=O)[nH]2)c1 10.6019/CHEMBL5212743
CHEMBL3337894 114591 31 None - 1 Human 7.0 pKi = 7.0 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000729a HRH1Selectivity interaction (GPCR panel (PDSP screen)) EUB0000729a HRH1
ChEMBL 479 9 3 7 3.3 COc1cccc(CNC(=O)c2nc3scc(COCc4ccc(C(=O)O)cc4)c3c(=O)[nH]2)c1 10.6019/CHEMBL5212743
130442572 171908 0 None -208 24 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4469848 171908 0 None -208 24 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-pyrilamine from human histamine H1 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
1164 1630 26 None - 12 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
Drug Central 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
1626 1630 26 None - 12 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
Drug Central 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
3345 1630 26 None - 12 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
Drug Central 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
CHEMBL596 1630 26 None - 12 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
Drug Central 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
DB00813 1630 26 None - 12 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
Drug Central 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
2031 120433 31 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
Drug Central 311 8 0 3 3.7 CCN(CC)CCOC(=O)C(c1ccccc1)c1ccccc1 None
CHEMBL353846 120433 31 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
Drug Central 311 8 0 3 3.7 CCN(CC)CCOC(=O)C(c1ccccc1)c1ccccc1 None
2142 3096 58 None -7585 36 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 3096 58 None -7585 36 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 3096 58 None -7585 36 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 3096 58 None -7585 36 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 3096 58 None -7585 36 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 3096 58 None -7585 36 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4919 206234 23 None - 8 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
Drug Central 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 None
CHEMBL86715 206234 23 None - 8 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
Drug Central 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 None
2284 3182 33 None -10 29 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
4926 3182 33 None -10 29 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
7281 3182 33 None -10 29 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
CHEMBL564 3182 33 None -10 29 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
DB00420 3182 33 None -10 29 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
1613 2348 53 None - 44 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligandBinding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligand
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2348 53 None - 44 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligandBinding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligand
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2348 53 None - 44 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligandBinding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligand
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2348 53 None - 44 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligandBinding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligand
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2348 53 None - 44 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligandBinding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligand
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3689 102771 55 None - 0 Human 8.2 pIC50 = 8.2 Binding
Compound was tested for the binding affinity against histamine H1 receptor by using [3H]mepyramine as radioligandCompound was tested for the binding affinity against histamine H1 receptor by using [3H]mepyramine as radioligand
Drug Central 325 5 2 3 3.8 CC(C(O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 None
CHEMBL1372983 102771 55 None - 0 Human 8.2 pIC50 = 8.2 Binding
Compound was tested for the binding affinity against histamine H1 receptor by using [3H]mepyramine as radioligandCompound was tested for the binding affinity against histamine H1 receptor by using [3H]mepyramine as radioligand
Drug Central 325 5 2 3 3.8 CC(C(O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 None
CHEMBL305187 102771 55 None - 0 Human 8.2 pIC50 = 8.2 Binding
Compound was tested for the binding affinity against histamine H1 receptor by using [3H]mepyramine as radioligandCompound was tested for the binding affinity against histamine H1 receptor by using [3H]mepyramine as radioligand
Drug Central 325 5 2 3 3.8 CC(C(O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 None
4601 206747 35 None - 16 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
Drug Central 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
CHEMBL1201023 206747 35 None - 16 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
Drug Central 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
CHEMBL900 206747 35 None - 16 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
Drug Central 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
2865 4143 73 None -1047 53 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [3H]mepyramine from H1R in rat brainDisplacement of [3H]mepyramine from H1R in rat brain
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4143 73 None -1047 53 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [3H]mepyramine from H1R in rat brainDisplacement of [3H]mepyramine from H1R in rat brain
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4143 73 None -1047 53 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [3H]mepyramine from H1R in rat brainDisplacement of [3H]mepyramine from H1R in rat brain
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4143 73 None -1047 53 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [3H]mepyramine from H1R in rat brainDisplacement of [3H]mepyramine from H1R in rat brain
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4143 73 None -1047 53 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [3H]mepyramine from H1R in rat brainDisplacement of [3H]mepyramine from H1R in rat brain
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
100 3805 58 None -23 55 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity against Histamine H1 receptor was measured using radioligand ([3H]pyrilamine) binding assayBinding affinity against Histamine H1 receptor was measured using radioligand ([3H]pyrilamine) binding assay
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3805 58 None -23 55 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity against Histamine H1 receptor was measured using radioligand ([3H]pyrilamine) binding assayBinding affinity against Histamine H1 receptor was measured using radioligand ([3H]pyrilamine) binding assay
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3805 58 None -23 55 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity against Histamine H1 receptor was measured using radioligand ([3H]pyrilamine) binding assayBinding affinity against Histamine H1 receptor was measured using radioligand ([3H]pyrilamine) binding assay
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3805 58 None -23 55 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity against Histamine H1 receptor was measured using radioligand ([3H]pyrilamine) binding assayBinding affinity against Histamine H1 receptor was measured using radioligand ([3H]pyrilamine) binding assay
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3805 58 None -23 55 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity against Histamine H1 receptor was measured using radioligand ([3H]pyrilamine) binding assayBinding affinity against Histamine H1 receptor was measured using radioligand ([3H]pyrilamine) binding assay
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2389 3331 118 None -346 67 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [3H]mepyramine from H1R in rat brainDisplacement of [3H]mepyramine from H1R in rat brain
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 118 None -346 67 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [3H]mepyramine from H1R in rat brainDisplacement of [3H]mepyramine from H1R in rat brain
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 118 None -346 67 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [3H]mepyramine from H1R in rat brainDisplacement of [3H]mepyramine from H1R in rat brain
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 118 None -346 67 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [3H]mepyramine from H1R in rat brainDisplacement of [3H]mepyramine from H1R in rat brain
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 118 None -346 67 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [3H]mepyramine from H1R in rat brainDisplacement of [3H]mepyramine from H1R in rat brain
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
3191 102858 97 None - 25 Guinea pig 8.1 pIC50 = 8.1 Binding
Compound is evaluated for in vitro receptor binding affinity against H1 receptorCompound is evaluated for in vitro receptor binding affinity against H1 receptor
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
CHEMBL305660 102858 97 None - 25 Guinea pig 8.1 pIC50 = 8.1 Binding
Compound is evaluated for in vitro receptor binding affinity against H1 receptorCompound is evaluated for in vitro receptor binding affinity against H1 receptor
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
2337 3256 77 None -1 62 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]mepyramine from H1R in rat brainDisplacement of [3H]mepyramine from H1R in rat brain
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 77 None -1 62 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]mepyramine from H1R in rat brainDisplacement of [3H]mepyramine from H1R in rat brain
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 77 None -1 62 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]mepyramine from H1R in rat brainDisplacement of [3H]mepyramine from H1R in rat brain
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 77 None -1 62 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]mepyramine from H1R in rat brainDisplacement of [3H]mepyramine from H1R in rat brain
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 77 None -1 62 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]mepyramine from H1R in rat brainDisplacement of [3H]mepyramine from H1R in rat brain
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
1385580 29276 76 None - 5 Guinea pig 8.1 pIC50 = 8.1 Binding
Inhibitory activity against Tritiated [3H]- mepyramine binding to Histamine H1 receptor in guinea pig cerebral cortexInhibitory activity against Tritiated [3H]- mepyramine binding to Histamine H1 receptor in guinea pig cerebral cortex
Drug Central 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 None
4615 29276 76 None - 5 Guinea pig 8.1 pIC50 = 8.1 Binding
Inhibitory activity against Tritiated [3H]- mepyramine binding to Histamine H1 receptor in guinea pig cerebral cortexInhibitory activity against Tritiated [3H]- mepyramine binding to Histamine H1 receptor in guinea pig cerebral cortex
Drug Central 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 None
CHEMBL13828 29276 76 None - 5 Guinea pig 8.1 pIC50 = 8.1 Binding
Inhibitory activity against Tritiated [3H]- mepyramine binding to Histamine H1 receptor in guinea pig cerebral cortexInhibitory activity against Tritiated [3H]- mepyramine binding to Histamine H1 receptor in guinea pig cerebral cortex
Drug Central 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 None
1210 918 51 None 9 21 Guinea pig 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
1213 918 51 None 9 21 Guinea pig 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
2725 918 51 None 9 21 Guinea pig 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
33036 918 51 None 9 21 Guinea pig 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
4411 918 51 None 9 21 Guinea pig 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
616 918 51 None 9 21 Guinea pig 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
6976 918 51 None 9 21 Guinea pig 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
716121 918 51 None 9 21 Guinea pig 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1201353 918 51 None 9 21 Guinea pig 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1554789 918 51 None 9 21 Guinea pig 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL505 918 51 None 9 21 Guinea pig 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
DB01114 918 51 None 9 21 Guinea pig 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
DB13679 918 51 None 9 21 Guinea pig 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortexInhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
1227 2489 43 None -5 12 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
Drug Central 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
2331 2489 43 None -5 12 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
Drug Central 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
3957 2489 43 None -5 12 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
Drug Central 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
4992 2489 43 None -5 12 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
Drug Central 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
CHEMBL511 2489 43 None -5 12 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
Drug Central 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
DB06691 2489 43 None -5 12 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
Drug Central 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
11976 920 59 None - 24 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
667467 920 59 None - 24 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
CHEMBL908 920 59 None - 24 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
DB01239 920 59 None - 24 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation countingDisplacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
1027 1576 73 None -6 2 Human 7.6 pIC50 = 7.6 Binding
Antagonism of 5 nM [<sup>3</sup>H]mepyramine binding in an intact cell assay using U373 MG astrocytoma cells.Antagonism of 5 nM [<sup>3</sup>H]mepyramine binding in an intact cell assay using U373 MG astrocytoma cells.
Guide to Pharmacology 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 18446005
3241 1576 73 None -6 2 Human 7.6 pIC50 = 7.6 Binding
Antagonism of 5 nM [<sup>3</sup>H]mepyramine binding in an intact cell assay using U373 MG astrocytoma cells.Antagonism of 5 nM [<sup>3</sup>H]mepyramine binding in an intact cell assay using U373 MG astrocytoma cells.
Guide to Pharmacology 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 18446005
7176 1576 73 None -6 2 Human 7.6 pIC50 = 7.6 Binding
Antagonism of 5 nM [<sup>3</sup>H]mepyramine binding in an intact cell assay using U373 MG astrocytoma cells.Antagonism of 5 nM [<sup>3</sup>H]mepyramine binding in an intact cell assay using U373 MG astrocytoma cells.
Guide to Pharmacology 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 18446005
CHEMBL1106 1576 73 None -6 2 Human 7.6 pIC50 = 7.6 Binding
Antagonism of 5 nM [<sup>3</sup>H]mepyramine binding in an intact cell assay using U373 MG astrocytoma cells.Antagonism of 5 nM [<sup>3</sup>H]mepyramine binding in an intact cell assay using U373 MG astrocytoma cells.
Guide to Pharmacology 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 18446005
DB00751 1576 73 None -6 2 Human 7.6 pIC50 = 7.6 Binding
Antagonism of 5 nM [<sup>3</sup>H]mepyramine binding in an intact cell assay using U373 MG astrocytoma cells.Antagonism of 5 nM [<sup>3</sup>H]mepyramine binding in an intact cell assay using U373 MG astrocytoma cells.
Guide to Pharmacology 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 18446005
10102 2546 88 None - 1 Guinea pig 7.3 pIC50 = 7.3 Binding
Inhibition of [3H]pyrilamine binding to histamine H1 receptors in guinea pig cerebellar membranes and sections.Inhibition of [3H]pyrilamine binding to histamine H1 receptors in guinea pig cerebellar membranes and sections.
Guide to Pharmacology 432 5 1 6 3.4 Fc1ccc(cc1)Cn1c(nc2c1cccc2)N1CCC(CC1)N(c1nccc(=O)[nH]1)C 7612054
1824 2546 88 None - 1 Guinea pig 7.3 pIC50 = 7.3 Binding
Inhibition of [3H]pyrilamine binding to histamine H1 receptors in guinea pig cerebellar membranes and sections.Inhibition of [3H]pyrilamine binding to histamine H1 receptors in guinea pig cerebellar membranes and sections.
Guide to Pharmacology 432 5 1 6 3.4 Fc1ccc(cc1)Cn1c(nc2c1cccc2)N1CCC(CC1)N(c1nccc(=O)[nH]1)C 7612054
65906 2546 88 None - 1 Guinea pig 7.3 pIC50 = 7.3 Binding
Inhibition of [3H]pyrilamine binding to histamine H1 receptors in guinea pig cerebellar membranes and sections.Inhibition of [3H]pyrilamine binding to histamine H1 receptors in guinea pig cerebellar membranes and sections.
Guide to Pharmacology 432 5 1 6 3.4 Fc1ccc(cc1)Cn1c(nc2c1cccc2)N1CCC(CC1)N(c1nccc(=O)[nH]1)C 7612054
CHEMBL94454 2546 88 None - 1 Guinea pig 7.3 pIC50 = 7.3 Binding
Inhibition of [3H]pyrilamine binding to histamine H1 receptors in guinea pig cerebellar membranes and sections.Inhibition of [3H]pyrilamine binding to histamine H1 receptors in guinea pig cerebellar membranes and sections.
Guide to Pharmacology 432 5 1 6 3.4 Fc1ccc(cc1)Cn1c(nc2c1cccc2)N1CCC(CC1)N(c1nccc(=O)[nH]1)C 7612054
DB12523 2546 88 None - 1 Guinea pig 7.3 pIC50 = 7.3 Binding
Inhibition of [3H]pyrilamine binding to histamine H1 receptors in guinea pig cerebellar membranes and sections.Inhibition of [3H]pyrilamine binding to histamine H1 receptors in guinea pig cerebellar membranes and sections.
Guide to Pharmacology 432 5 1 6 3.4 Fc1ccc(cc1)Cn1c(nc2c1cccc2)N1CCC(CC1)N(c1nccc(=O)[nH]1)C 7612054
2200 20203 61 None 26 2 Guinea pig 8.2 pKd = 8.2 Binding
Antagonist activity at H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced ileum contraction measured after 15 minsAntagonist activity at H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced ileum contraction measured after 15 mins
Drug Central 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 None
CHEMBL1256819 20203 61 None 26 2 Guinea pig 8.2 pKd = 8.2 Binding
Antagonist activity at H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced ileum contraction measured after 15 minsAntagonist activity at H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced ileum contraction measured after 15 mins
Drug Central 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 None
CHEMBL1305 20203 61 None 26 2 Guinea pig 8.2 pKd = 8.2 Binding
Antagonist activity at H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced ileum contraction measured after 15 minsAntagonist activity at H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced ileum contraction measured after 15 mins
Drug Central 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 None
1605 2342 117 None 1 4 Guinea pig 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 None
3957 2342 117 None 1 4 Guinea pig 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 None
7216 2342 117 None 1 4 Guinea pig 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 None
CHEMBL998 2342 117 None 1 4 Guinea pig 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 None
DB00455 2342 117 None 1 4 Guinea pig 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 None
2600 3779 74 None -3 13 Guinea pig 8.1 pKd = 8.1 Binding
Dissociation constant was determined against H1 receptor of guinea pig lung membranes using radioligand binding assays.Dissociation constant was determined against H1 receptor of guinea pig lung membranes using radioligand binding assays.
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
2608 3779 74 None -3 13 Guinea pig 8.1 pKd = 8.1 Binding
Dissociation constant was determined against H1 receptor of guinea pig lung membranes using radioligand binding assays.Dissociation constant was determined against H1 receptor of guinea pig lung membranes using radioligand binding assays.
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
5405 3779 74 None -3 13 Guinea pig 8.1 pKd = 8.1 Binding
Dissociation constant was determined against H1 receptor of guinea pig lung membranes using radioligand binding assays.Dissociation constant was determined against H1 receptor of guinea pig lung membranes using radioligand binding assays.
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
CHEMBL17157 3779 74 None -3 13 Guinea pig 8.1 pKd = 8.1 Binding
Dissociation constant was determined against H1 receptor of guinea pig lung membranes using radioligand binding assays.Dissociation constant was determined against H1 receptor of guinea pig lung membranes using radioligand binding assays.
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
DB00342 3779 74 None -3 13 Guinea pig 8.1 pKd = 8.1 Binding
Dissociation constant was determined against H1 receptor of guinea pig lung membranes using radioligand binding assays.Dissociation constant was determined against H1 receptor of guinea pig lung membranes using radioligand binding assays.
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
1971 2866 38 None -1 30 Human 8.1 pKd = 8.1 Binding
NoneNone
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
2404 2866 38 None -1 30 Human 8.1 pKd = 8.1 Binding
NoneNone
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
4543 2866 38 None -1 30 Human 8.1 pKd = 8.1 Binding
NoneNone
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
CHEMBL445 2866 38 None -1 30 Human 8.1 pKd = 8.1 Binding
NoneNone
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
DB00540 2866 38 None -1 30 Human 8.1 pKd = 8.1 Binding
NoneNone
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
11291 98796 25 None 4 2 Guinea pig 8.1 pKd = 8.1 Binding
Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum
Drug Central 261 1 0 1 3.9 CN1CCC2=C(C1)C(c1ccccc1)c1ccccc12 None
CHEMBL278398 98796 25 None 4 2 Guinea pig 8.1 pKd = 8.1 Binding
Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum
Drug Central 261 1 0 1 3.9 CN1CCC2=C(C1)C(c1ccccc1)c1ccccc12 None
277 1301 62 None 2 50 Guinea pig 8.1 pKd = 8.1 Binding
Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1301 62 None 2 50 Guinea pig 8.1 pKd = 8.1 Binding
Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1301 62 None 2 50 Guinea pig 8.1 pKd = 8.1 Binding
Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1301 62 None 2 50 Guinea pig 8.1 pKd = 8.1 Binding
Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1301 62 None 2 50 Guinea pig 8.1 pKd = 8.1 Binding
Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
1227 2489 43 None 2 12 Guinea pig 8.0 pKd = 8.0 Binding
Antagonist activity at histamine H1 receptor in Cavia porcellus (guinea pig) ileum assessed as inhibition of electrically-induced contractionAntagonist activity at histamine H1 receptor in Cavia porcellus (guinea pig) ileum assessed as inhibition of electrically-induced contraction
Drug Central 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
2331 2489 43 None 2 12 Guinea pig 8.0 pKd = 8.0 Binding
Antagonist activity at histamine H1 receptor in Cavia porcellus (guinea pig) ileum assessed as inhibition of electrically-induced contractionAntagonist activity at histamine H1 receptor in Cavia porcellus (guinea pig) ileum assessed as inhibition of electrically-induced contraction
Drug Central 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
3957 2489 43 None 2 12 Guinea pig 8.0 pKd = 8.0 Binding
Antagonist activity at histamine H1 receptor in Cavia porcellus (guinea pig) ileum assessed as inhibition of electrically-induced contractionAntagonist activity at histamine H1 receptor in Cavia porcellus (guinea pig) ileum assessed as inhibition of electrically-induced contraction
Drug Central 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
4992 2489 43 None 2 12 Guinea pig 8.0 pKd = 8.0 Binding
Antagonist activity at histamine H1 receptor in Cavia porcellus (guinea pig) ileum assessed as inhibition of electrically-induced contractionAntagonist activity at histamine H1 receptor in Cavia porcellus (guinea pig) ileum assessed as inhibition of electrically-induced contraction
Drug Central 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
CHEMBL511 2489 43 None 2 12 Guinea pig 8.0 pKd = 8.0 Binding
Antagonist activity at histamine H1 receptor in Cavia porcellus (guinea pig) ileum assessed as inhibition of electrically-induced contractionAntagonist activity at histamine H1 receptor in Cavia porcellus (guinea pig) ileum assessed as inhibition of electrically-induced contraction
Drug Central 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
DB06691 2489 43 None 2 12 Guinea pig 8.0 pKd = 8.0 Binding
Antagonist activity at histamine H1 receptor in Cavia porcellus (guinea pig) ileum assessed as inhibition of electrically-induced contractionAntagonist activity at histamine H1 receptor in Cavia porcellus (guinea pig) ileum assessed as inhibition of electrically-induced contraction
Drug Central 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
1228 3866 34 None 5 4 Guinea pig 8.0 pKd = 8 Binding
Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum
Drug Central 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
2763 3866 34 None 5 4 Guinea pig 8.0 pKd = 8 Binding
Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum
Drug Central 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
5282443 3866 34 None 5 4 Guinea pig 8.0 pKd = 8 Binding
Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum
Drug Central 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
CHEMBL855 3866 34 None 5 4 Guinea pig 8.0 pKd = 8 Binding
Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum
Drug Central 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
DB00427 3866 34 None 5 4 Guinea pig 8.0 pKd = 8 Binding
Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum
Drug Central 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
2762 3863 31 None -9 2 Human 8.0 pKd = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 14667234
5587 3863 31 None -9 2 Human 8.0 pKd = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 14667234
7318 3863 31 None -9 2 Human 8.0 pKd = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 14667234
CHEMBL1241 3863 31 None -9 2 Human 8.0 pKd = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 14667234
DB00792 3863 31 None -9 2 Human 8.0 pKd = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C 14667234
1225 1471 26 None -1 22 Human 9.0 pKd = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C 15093820
3958 1471 26 None -1 22 Human 9.0 pKd = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C 15093820
667477 1471 26 None -1 22 Human 9.0 pKd = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C 15093820
CHEMBL860 1471 26 None -1 22 Human 9.0 pKd = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C 15093820
DB01142 1471 26 None -1 22 Human 9.0 pKd = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C 15093820
None 216151 0 3H-Histamine 8912 2 Guinea pig 10.5 pKi = 10.5 Binding
NoneNone
PDSP KiDatabase 139 3 2 2 0.6 CC(CC1=CN=CN1)NC None
None 216152 0 3H-Histamine 60255 2 Guinea pig 10.5 pKi = 10.5 Binding
NoneNone
PDSP KiDatabase 139 2 2 2 0.9 CC(C1=CN=CN1)C(C)N None
277 1301 62 3H-MEPYRAMINE -2 50 Human 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1301 62 3H-MEPYRAMINE -2 50 Human 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1301 62 3H-MEPYRAMINE -2 50 Human 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1301 62 3H-MEPYRAMINE -2 50 Human 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1301 62 3H-MEPYRAMINE -2 50 Human 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
1225 1471 26 3H-trans-H2-PAT,(-) -1 22 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
3958 1471 26 3H-trans-H2-PAT,(-) -1 22 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667477 1471 26 3H-trans-H2-PAT,(-) -1 22 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
CHEMBL860 1471 26 3H-trans-H2-PAT,(-) -1 22 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
DB01142 1471 26 3H-trans-H2-PAT,(-) -1 22 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
135398745 2914 112 3H-PYRILAMINE 1 65 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 3H-PYRILAMINE 1 65 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 3H-PYRILAMINE 1 65 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 3H-PYRILAMINE 1 65 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
277 1301 62 3H-MEPYRAMINE 2 50 Guinea pig 10.0 pKi = 10 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1301 62 3H-MEPYRAMINE 2 50 Guinea pig 10.0 pKi = 10 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1301 62 3H-MEPYRAMINE 2 50 Guinea pig 10.0 pKi = 10 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1301 62 3H-MEPYRAMINE 2 50 Guinea pig 10.0 pKi = 10 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1301 62 3H-MEPYRAMINE 2 50 Guinea pig 10.0 pKi = 10 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
1225 1471 26 3H-trans-H2-PAT,(-) 1 22 Guinea pig 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
1225 1471 26 3H-MEPYRAMINE -1 22 Human 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
3958 1471 26 3H-trans-H2-PAT,(-) 1 22 Guinea pig 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
3958 1471 26 3H-MEPYRAMINE -1 22 Human 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667477 1471 26 3H-trans-H2-PAT,(-) 1 22 Guinea pig 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667477 1471 26 3H-MEPYRAMINE -1 22 Human 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
CHEMBL860 1471 26 3H-trans-H2-PAT,(-) 1 22 Guinea pig 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
CHEMBL860 1471 26 3H-MEPYRAMINE -1 22 Human 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
DB01142 1471 26 3H-trans-H2-PAT,(-) 1 22 Guinea pig 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
DB01142 1471 26 3H-MEPYRAMINE -1 22 Human 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
46780481 107531 20 3H-PYRILAMINE -13 53 Human 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107531 20 3H-PYRILAMINE -13 53 Human 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107531 20 3H-PYRILAMINE -13 53 Human 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107531 20 3H-PYRILAMINE -13 53 Human 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
180 401 56 3H-PYRILAMINE 1 40 Guinea pig 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 401 56 3H-PYRILAMINE 1 40 Guinea pig 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 401 56 3H-PYRILAMINE 1 40 Guinea pig 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 401 56 3H-PYRILAMINE 1 40 Guinea pig 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 401 56 3H-PYRILAMINE 1 40 Guinea pig 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
1225 1471 26 3H-PYRILAMINE -1 22 Human 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
3958 1471 26 3H-PYRILAMINE -1 22 Human 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667477 1471 26 3H-PYRILAMINE -1 22 Human 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
CHEMBL860 1471 26 3H-PYRILAMINE -1 22 Human 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
DB01142 1471 26 3H-PYRILAMINE -1 22 Human 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
2726 919 68 3H-PYRILAMINE -2 72 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 68 3H-PYRILAMINE -2 72 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 68 3H-PYRILAMINE -2 72 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 68 3H-PYRILAMINE -2 72 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 68 3H-PYRILAMINE -2 72 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
135398737 958 93 3H-PYRILAMINE 2 89 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-PYRILAMINE 2 89 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-PYRILAMINE 2 89 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-PYRILAMINE 2 89 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-PYRILAMINE 2 89 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2286 3183 51 3H-MEPYRAMINE -2 30 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
4927 3183 51 3H-MEPYRAMINE -2 30 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
7282 3183 51 3H-MEPYRAMINE -2 30 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
CHEMBL643 3183 51 3H-MEPYRAMINE -2 30 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
DB01069 3183 51 3H-MEPYRAMINE -2 30 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
1225 1471 26 3H-MEPYRAMINE 1 22 Guinea pig 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
3958 1471 26 3H-MEPYRAMINE 1 22 Guinea pig 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667477 1471 26 3H-MEPYRAMINE 1 22 Guinea pig 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
CHEMBL860 1471 26 3H-MEPYRAMINE 1 22 Guinea pig 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
DB01142 1471 26 3H-MEPYRAMINE 1 22 Guinea pig 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
135 2532 43 3H-MEPYRAMINE -1 58 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 43 3H-MEPYRAMINE -1 58 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 43 3H-MEPYRAMINE -1 58 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 43 3H-MEPYRAMINE -1 58 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 43 3H-MEPYRAMINE -1 58 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1228 3866 34 3H-MEPYRAMINE 5 4 Guinea pig 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
2763 3866 34 3H-MEPYRAMINE 5 4 Guinea pig 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
5282443 3866 34 3H-MEPYRAMINE 5 4 Guinea pig 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
CHEMBL855 3866 34 3H-MEPYRAMINE 5 4 Guinea pig 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
DB00427 3866 34 3H-MEPYRAMINE 5 4 Guinea pig 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
16667681 216153 0 3H-MEPYRAMINE 4 3 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 390 7 1 5 3.5 CN(C)CCCC1=CC=CC=N1.C1=CC(=CC=C1OC(=O)C=CC(=O)O)Cl None
1225 1471 26 3H-MEPYRAMINE -1 22 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
3958 1471 26 3H-MEPYRAMINE -1 22 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667477 1471 26 3H-MEPYRAMINE -1 22 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
CHEMBL860 1471 26 3H-MEPYRAMINE -1 22 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
DB01142 1471 26 3H-MEPYRAMINE -1 22 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
1816 2540 102 3H-MEPYRAMINE 3 18 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
4205 2540 102 3H-MEPYRAMINE 3 18 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
7241 2540 102 3H-MEPYRAMINE 3 18 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
CHEMBL654 2540 102 3H-MEPYRAMINE 3 18 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
DB00370 2540 102 3H-MEPYRAMINE 3 18 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
135398745 2914 112 3H-pirilamine -1 65 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 3H-pirilamine -1 65 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 3H-pirilamine -1 65 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 3H-pirilamine -1 65 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135 2532 43 3H-doxepin -1 58 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 43 3H-doxepin -1 58 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 43 3H-doxepin -1 58 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 43 3H-doxepin -1 58 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 43 3H-doxepin -1 58 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1225 1471 26 3H-MEPYRAMINE -1 22 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
3958 1471 26 3H-MEPYRAMINE -1 22 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667477 1471 26 3H-MEPYRAMINE -1 22 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
CHEMBL860 1471 26 3H-MEPYRAMINE -1 22 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
DB01142 1471 26 3H-MEPYRAMINE -1 22 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
135 2532 43 3H-PYRILAMINE -1 58 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 43 3H-PYRILAMINE -1 58 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 43 3H-PYRILAMINE -1 58 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 43 3H-PYRILAMINE -1 58 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 43 3H-PYRILAMINE -1 58 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1210 918 51 3H-PYRILAMINE 9 21 Guinea pig 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
1213 918 51 3H-PYRILAMINE 9 21 Guinea pig 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
2725 918 51 3H-PYRILAMINE 9 21 Guinea pig 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
33036 918 51 3H-PYRILAMINE 9 21 Guinea pig 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
4411 918 51 3H-PYRILAMINE 9 21 Guinea pig 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
616 918 51 3H-PYRILAMINE 9 21 Guinea pig 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
6976 918 51 3H-PYRILAMINE 9 21 Guinea pig 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
716121 918 51 3H-PYRILAMINE 9 21 Guinea pig 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1201353 918 51 3H-PYRILAMINE 9 21 Guinea pig 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1554789 918 51 3H-PYRILAMINE 9 21 Guinea pig 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL505 918 51 3H-PYRILAMINE 9 21 Guinea pig 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
DB01114 918 51 3H-PYRILAMINE 9 21 Guinea pig 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
DB13679 918 51 3H-PYRILAMINE 9 21 Guinea pig 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
1228 3866 34 3H-MEPYRAMINE -5 4 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
2763 3866 34 3H-MEPYRAMINE -5 4 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
5282443 3866 34 3H-MEPYRAMINE -5 4 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
CHEMBL855 3866 34 3H-MEPYRAMINE -5 4 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
DB00427 3866 34 3H-MEPYRAMINE -5 4 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
1225 1471 26 3H-doxepin -1 22 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
3958 1471 26 3H-doxepin -1 22 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667477 1471 26 3H-doxepin -1 22 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
CHEMBL860 1471 26 3H-doxepin -1 22 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
DB01142 1471 26 3H-doxepin -1 22 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
180 401 56 3H-MEPYRAMINE -1 40 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 401 56 3H-MEPYRAMINE -1 40 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 401 56 3H-MEPYRAMINE -1 40 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 401 56 3H-MEPYRAMINE -1 40 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 401 56 3H-MEPYRAMINE -1 40 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
1210 918 51 3H-MEPYRAMINE 9 21 Guinea pig 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
1213 918 51 3H-MEPYRAMINE 9 21 Guinea pig 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
2725 918 51 3H-MEPYRAMINE 9 21 Guinea pig 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
33036 918 51 3H-MEPYRAMINE 9 21 Guinea pig 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
4411 918 51 3H-MEPYRAMINE 9 21 Guinea pig 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
616 918 51 3H-MEPYRAMINE 9 21 Guinea pig 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
6976 918 51 3H-MEPYRAMINE 9 21 Guinea pig 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
716121 918 51 3H-MEPYRAMINE 9 21 Guinea pig 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1201353 918 51 3H-MEPYRAMINE 9 21 Guinea pig 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1554789 918 51 3H-MEPYRAMINE 9 21 Guinea pig 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL505 918 51 3H-MEPYRAMINE 9 21 Guinea pig 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
DB01114 918 51 3H-MEPYRAMINE 9 21 Guinea pig 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
DB13679 918 51 3H-MEPYRAMINE 9 21 Guinea pig 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
1225 1471 26 3H-MEPYRAMINE 1 22 Guinea pig 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
3958 1471 26 3H-MEPYRAMINE 1 22 Guinea pig 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667477 1471 26 3H-MEPYRAMINE 1 22 Guinea pig 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
CHEMBL860 1471 26 3H-MEPYRAMINE 1 22 Guinea pig 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
DB01142 1471 26 3H-MEPYRAMINE 1 22 Guinea pig 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
1227 2489 43 3H-MEPYRAMINE 2 12 Guinea pig 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
2331 2489 43 3H-MEPYRAMINE 2 12 Guinea pig 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
3957 2489 43 3H-MEPYRAMINE 2 12 Guinea pig 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
4992 2489 43 3H-MEPYRAMINE 2 12 Guinea pig 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
CHEMBL511 2489 43 3H-MEPYRAMINE 2 12 Guinea pig 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
DB06691 2489 43 3H-MEPYRAMINE 2 12 Guinea pig 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
1816 2540 102 3H-PYRILAMINE -3 18 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
1816 2540 102 3H-MEPYRAMINE 3 18 Rat 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
4205 2540 102 3H-PYRILAMINE -3 18 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
4205 2540 102 3H-MEPYRAMINE 3 18 Rat 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
7241 2540 102 3H-PYRILAMINE -3 18 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
7241 2540 102 3H-MEPYRAMINE 3 18 Rat 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
CHEMBL654 2540 102 3H-PYRILAMINE -3 18 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
CHEMBL654 2540 102 3H-MEPYRAMINE 3 18 Rat 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
DB00370 2540 102 3H-PYRILAMINE -3 18 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
DB00370 2540 102 3H-MEPYRAMINE 3 18 Rat 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
None 216141 0 3H-Histamine -4 6 Guinea pig 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 125 2 2 2 0.3 CC(CC1=CN=CN1)N None
1227 2489 43 3H-MEPYRAMINE -2 12 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
2331 2489 43 3H-MEPYRAMINE -2 12 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
3957 2489 43 3H-MEPYRAMINE -2 12 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
4992 2489 43 3H-MEPYRAMINE -2 12 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
CHEMBL511 2489 43 3H-MEPYRAMINE -2 12 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
DB06691 2489 43 3H-MEPYRAMINE -2 12 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
1227 2489 43 3H-MEPYRAMINE 2 12 Guinea pig 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
2331 2489 43 3H-MEPYRAMINE 2 12 Guinea pig 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
3957 2489 43 3H-MEPYRAMINE 2 12 Guinea pig 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
4992 2489 43 3H-MEPYRAMINE 2 12 Guinea pig 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
CHEMBL511 2489 43 3H-MEPYRAMINE 2 12 Guinea pig 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
DB06691 2489 43 3H-MEPYRAMINE 2 12 Guinea pig 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
72287 61061 38 3H-doxepin 6 2 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 328 5 0 4 4.5 COc1ccc2c(c1)N(C[C@H](C)CN(C)C)c1ccccc1S2 None
CHEMBL1764 61061 38 3H-doxepin 6 2 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 328 5 0 4 4.5 COc1ccc2c(c1)N(C[C@H](C)CN(C)C)c1ccccc1S2 None
1228 3866 34 3H-MEPYRAMINE 5 4 Guinea pig 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
2763 3866 34 3H-MEPYRAMINE 5 4 Guinea pig 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
5282443 3866 34 3H-MEPYRAMINE 5 4 Guinea pig 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
CHEMBL855 3866 34 3H-MEPYRAMINE 5 4 Guinea pig 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
DB00427 3866 34 3H-MEPYRAMINE 5 4 Guinea pig 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
103 4153 61 3H-PYRILAMINE -1 53 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4153 61 3H-PYRILAMINE -1 53 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4153 61 3H-PYRILAMINE -1 53 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4153 61 3H-PYRILAMINE -1 53 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4153 61 3H-PYRILAMINE -1 53 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
1816 2540 102 3H-MEPYRAMINE 3 18 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
4205 2540 102 3H-MEPYRAMINE 3 18 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
7241 2540 102 3H-MEPYRAMINE 3 18 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
CHEMBL654 2540 102 3H-MEPYRAMINE 3 18 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
DB00370 2540 102 3H-MEPYRAMINE 3 18 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
135398745 2914 112 3H-PYRILAMINE 1 65 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 3H-PYRILAMINE 1 65 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 3H-PYRILAMINE 1 65 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 3H-PYRILAMINE 1 65 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
180 401 56 3H-doxepin -1 40 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 401 56 3H-doxepin -1 40 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 401 56 3H-doxepin -1 40 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 401 56 3H-doxepin -1 40 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 401 56 3H-doxepin -1 40 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
1228 3866 34 3H-trans-H2-PAT,(-) 5 4 Guinea pig 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
1228 3866 34 3H-MEPYRAMINE -5 4 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
2763 3866 34 3H-trans-H2-PAT,(-) 5 4 Guinea pig 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
2763 3866 34 3H-MEPYRAMINE -5 4 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
5282443 3866 34 3H-trans-H2-PAT,(-) 5 4 Guinea pig 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
5282443 3866 34 3H-MEPYRAMINE -5 4 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
CHEMBL855 3866 34 3H-trans-H2-PAT,(-) 5 4 Guinea pig 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
CHEMBL855 3866 34 3H-MEPYRAMINE -5 4 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
DB00427 3866 34 3H-trans-H2-PAT,(-) 5 4 Guinea pig 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
DB00427 3866 34 3H-MEPYRAMINE -5 4 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
90475904 216022 0 3H-trans-H2-PAT,(-) 6 6 Guinea pig 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(C)CCC(C1=CC=C(C=C1)Cl)C2=CC=CC=N2 None
1225 1471 26 3H-MEPYRAMINE -2 22 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
3958 1471 26 3H-MEPYRAMINE -2 22 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667477 1471 26 3H-MEPYRAMINE -2 22 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
CHEMBL860 1471 26 3H-MEPYRAMINE -2 22 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
DB01142 1471 26 3H-MEPYRAMINE -2 22 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
3246155 215962 0 3H-MEPYRAMINE -3 16 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 307 4 0 2 4.4 CN1C2CCC1CC(C2)OC(C3=CC=CC=C3)C4=CC=CC=C4 None
1227 2489 43 3H-trans-H2-PAT,(-) 2 12 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
1227 2489 43 3H-MEPYRAMINE -2 12 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
2331 2489 43 3H-trans-H2-PAT,(-) 2 12 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
2331 2489 43 3H-MEPYRAMINE -2 12 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
3957 2489 43 3H-trans-H2-PAT,(-) 2 12 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
3957 2489 43 3H-MEPYRAMINE -2 12 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
4992 2489 43 3H-trans-H2-PAT,(-) 2 12 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
4992 2489 43 3H-MEPYRAMINE -2 12 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
CHEMBL511 2489 43 3H-trans-H2-PAT,(-) 2 12 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
CHEMBL511 2489 43 3H-MEPYRAMINE -2 12 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
DB06691 2489 43 3H-trans-H2-PAT,(-) 2 12 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
DB06691 2489 43 3H-MEPYRAMINE -2 12 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
4011 82408 49 3H-doxepin 6 24 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
CHEMBL21731 82408 49 3H-doxepin 6 24 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
2247 505 81 3H-PYRILAMINE 3 42 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
2247 505 81 3H-PYRILAMINE -4 42 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
249 505 81 3H-PYRILAMINE 3 42 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
249 505 81 3H-PYRILAMINE -4 42 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
2603 505 81 3H-PYRILAMINE 3 42 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
2603 505 81 3H-PYRILAMINE -4 42 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
CHEMBL296419 505 81 3H-PYRILAMINE 3 42 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
CHEMBL296419 505 81 3H-PYRILAMINE -4 42 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
DB00637 505 81 3H-PYRILAMINE 3 42 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
DB00637 505 81 3H-PYRILAMINE -4 42 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
565544 109743 11 3H-Histamine 354 2 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 125 2 2 2 0.5 CC(CN)c1cnc[nH]1 None
CHEMBL322988 109743 11 3H-Histamine 354 2 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 125 2 2 2 0.5 CC(CN)c1cnc[nH]1 None
5281878 1660 35 3H-MEPYRAMINE -1 17 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 1660 35 3H-MEPYRAMINE -1 17 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 1660 35 3H-MEPYRAMINE -1 17 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 1660 35 3H-MEPYRAMINE -1 17 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 1660 35 3H-MEPYRAMINE -1 17 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 1660 35 3H-MEPYRAMINE -1 17 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 1660 35 3H-MEPYRAMINE -1 17 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
46780481 107531 20 3H-PYRILAMINE -5 53 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107531 20 3H-PYRILAMINE -5 53 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107531 20 3H-PYRILAMINE -5 53 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107531 20 3H-PYRILAMINE -5 53 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
1228 3866 34 3H-MEPYRAMINE 5 4 Guinea pig 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
2763 3866 34 3H-MEPYRAMINE 5 4 Guinea pig 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
5282443 3866 34 3H-MEPYRAMINE 5 4 Guinea pig 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
CHEMBL855 3866 34 3H-MEPYRAMINE 5 4 Guinea pig 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
DB00427 3866 34 3H-MEPYRAMINE 5 4 Guinea pig 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
180 401 56 3H-PYRILAMINE -1 40 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 401 56 3H-PYRILAMINE -1 40 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 401 56 3H-PYRILAMINE -1 40 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 401 56 3H-PYRILAMINE -1 40 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 401 56 3H-PYRILAMINE -1 40 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
1400 1957 70 3H-MEPYRAMINE 2 3 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
3658 1957 70 3H-MEPYRAMINE 2 3 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
7199 1957 70 3H-MEPYRAMINE 2 3 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
91513 1957 70 3H-MEPYRAMINE 2 3 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
CHEMBL896 1957 70 3H-MEPYRAMINE 2 3 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
DB00557 1957 70 3H-MEPYRAMINE 2 3 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
1227 2489 43 3H-MEPYRAMINE -2 12 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
2331 2489 43 3H-MEPYRAMINE -2 12 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
3957 2489 43 3H-MEPYRAMINE -2 12 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
4992 2489 43 3H-MEPYRAMINE -2 12 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
CHEMBL511 2489 43 3H-MEPYRAMINE -2 12 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
DB06691 2489 43 3H-MEPYRAMINE -2 12 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
135 2532 43 3H-MEPYRAMINE 1 58 Rat 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 43 3H-MEPYRAMINE 1 58 Rat 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 43 3H-MEPYRAMINE 1 58 Rat 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 43 3H-MEPYRAMINE 1 58 Rat 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 43 3H-MEPYRAMINE 1 58 Rat 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1228 3866 34 3H-MEPYRAMINE -5 4 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
2763 3866 34 3H-MEPYRAMINE -5 4 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
5282443 3866 34 3H-MEPYRAMINE -5 4 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
CHEMBL855 3866 34 3H-MEPYRAMINE -5 4 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
DB00427 3866 34 3H-MEPYRAMINE -5 4 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
1227 2489 43 3H-trans-H2-PAT,(-) -2 12 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
2331 2489 43 3H-trans-H2-PAT,(-) -2 12 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
3957 2489 43 3H-trans-H2-PAT,(-) -2 12 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
4992 2489 43 3H-trans-H2-PAT,(-) -2 12 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
CHEMBL511 2489 43 3H-trans-H2-PAT,(-) -2 12 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
DB06691 2489 43 3H-trans-H2-PAT,(-) -2 12 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
180 401 56 3H-MEPYRAMINE -1 40 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 401 56 3H-MEPYRAMINE -1 40 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 401 56 3H-MEPYRAMINE -1 40 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 401 56 3H-MEPYRAMINE -1 40 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 401 56 3H-MEPYRAMINE -1 40 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
135398737 958 93 3H-PYRILAMINE 2 89 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-PYRILAMINE 2 89 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-PYRILAMINE 2 89 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-PYRILAMINE 2 89 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-PYRILAMINE 2 89 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
3246155 215962 0 3H-doxepin -3 16 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 307 4 0 2 4.4 CN1C2CCC1CC(C2)OC(C3=CC=CC=C3)C4=CC=CC=C4 None
1228 3866 34 3H-trans-H2-PAT,(-) -5 4 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
2763 3866 34 3H-trans-H2-PAT,(-) -5 4 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
5282443 3866 34 3H-trans-H2-PAT,(-) -5 4 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
CHEMBL855 3866 34 3H-trans-H2-PAT,(-) -5 4 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
DB00427 3866 34 3H-trans-H2-PAT,(-) -5 4 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
180 401 56 UNDEFINED -1 40 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 401 56 UNDEFINED -1 40 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 401 56 UNDEFINED -1 40 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 401 56 UNDEFINED -1 40 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 401 56 UNDEFINED -1 40 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
1228 3866 34 3H-MEPYRAMINE 5 4 Guinea pig 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
2763 3866 34 3H-MEPYRAMINE 5 4 Guinea pig 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
5282443 3866 34 3H-MEPYRAMINE 5 4 Guinea pig 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
CHEMBL855 3866 34 3H-MEPYRAMINE 5 4 Guinea pig 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
DB00427 3866 34 3H-MEPYRAMINE 5 4 Guinea pig 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
16667681 216153 0 3H-MEPYRAMINE 4 3 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 390 7 1 5 3.5 CN(C)CCCC1=CC=CC=N1.C1=CC(=CC=C1OC(=O)C=CC(=O)O)Cl None
1227 2489 43 3H-MEPYRAMINE -2 12 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
2331 2489 43 3H-MEPYRAMINE -2 12 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
3957 2489 43 3H-MEPYRAMINE -2 12 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
4992 2489 43 3H-MEPYRAMINE -2 12 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
CHEMBL511 2489 43 3H-MEPYRAMINE -2 12 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
DB06691 2489 43 3H-MEPYRAMINE -2 12 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
135398737 958 93 3H-PYRILAMINE 2 89 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 958 93 3H-doxepin 2 89 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-PYRILAMINE 2 89 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-doxepin 2 89 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-PYRILAMINE 2 89 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-doxepin 2 89 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-PYRILAMINE 2 89 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-doxepin 2 89 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-PYRILAMINE 2 89 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-doxepin 2 89 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398745 2914 112 3H-PYRILAMINE 1 65 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 3H-PYRILAMINE 1 65 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 3H-PYRILAMINE 1 65 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 3H-PYRILAMINE 1 65 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398737 958 93 3H-MEPYRAMINE -2 89 Guinea pig 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-MEPYRAMINE -2 89 Guinea pig 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-MEPYRAMINE -2 89 Guinea pig 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-MEPYRAMINE -2 89 Guinea pig 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-MEPYRAMINE -2 89 Guinea pig 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1227 2489 43 3H-MEPYRAMINE 2 12 Guinea pig 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
2331 2489 43 3H-MEPYRAMINE 2 12 Guinea pig 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
3957 2489 43 3H-MEPYRAMINE 2 12 Guinea pig 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
4992 2489 43 3H-MEPYRAMINE 2 12 Guinea pig 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
CHEMBL511 2489 43 3H-MEPYRAMINE 2 12 Guinea pig 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
DB06691 2489 43 3H-MEPYRAMINE 2 12 Guinea pig 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
2749 344 40 3H-MEPYRAMINE -1 2 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 298 4 0 3 4.5 CN(CC(CN1c2ccccc2Sc2c1cccc2)C)C None
5574 344 40 3H-MEPYRAMINE -1 2 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 298 4 0 3 4.5 CN(CC(CN1c2ccccc2Sc2c1cccc2)C)C None
7237 344 40 3H-MEPYRAMINE -1 2 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 298 4 0 3 4.5 CN(CC(CN1c2ccccc2Sc2c1cccc2)C)C None
CHEMBL829 344 40 3H-MEPYRAMINE -1 2 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 298 4 0 3 4.5 CN(CC(CN1c2ccccc2Sc2c1cccc2)C)C None
DB01246 344 40 3H-MEPYRAMINE -1 2 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 298 4 0 3 4.5 CN(CC(CN1c2ccccc2Sc2c1cccc2)C)C None
3246155 215962 0 3H-MEPYRAMINE -5 16 Guinea pig 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 307 4 0 2 4.4 CN1C2CCC1CC(C2)OC(C3=CC=CC=C3)C4=CC=CC=C4 None
5584 203211 44 3H-doxepin - 1 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 294 4 0 2 4.1 CC(CN(C)C)CN1c2ccccc2CCc2ccccc21 None
CHEMBL644 203211 44 3H-doxepin - 1 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 294 4 0 2 4.1 CC(CN(C)C)CN1c2ccccc2CCc2ccccc21 None
None 216175 0 3H-MEPYRAMINE - 1 Rat 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 296 3 0 3 4.4 C1CCN(C1)CCN2C3=CC=CC=C3SC4=CC=CC=C42 None
1228 3866 34 3H-MEPYRAMINE -5 4 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
2763 3866 34 3H-MEPYRAMINE -5 4 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
5282443 3866 34 3H-MEPYRAMINE -5 4 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
CHEMBL855 3866 34 3H-MEPYRAMINE -5 4 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
DB00427 3866 34 3H-MEPYRAMINE -5 4 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
135398737 958 93 3H-trans-H2-PAT,(-) 2 89 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-trans-H2-PAT,(-) 2 89 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-trans-H2-PAT,(-) 2 89 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-trans-H2-PAT,(-) 2 89 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-trans-H2-PAT,(-) 2 89 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
180 401 56 3H-MEPYRAMINE 1 40 Guinea pig 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 401 56 3H-MEPYRAMINE 1 40 Guinea pig 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 401 56 3H-MEPYRAMINE 1 40 Guinea pig 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 401 56 3H-MEPYRAMINE 1 40 Guinea pig 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 401 56 3H-MEPYRAMINE 1 40 Guinea pig 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
1816 2540 102 3H-PYRILAMINE -3 18 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
4205 2540 102 3H-PYRILAMINE -3 18 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
7241 2540 102 3H-PYRILAMINE -3 18 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
CHEMBL654 2540 102 3H-PYRILAMINE -3 18 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
DB00370 2540 102 3H-PYRILAMINE -3 18 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
135398737 958 93 3H-MEPYRAMINE 2 89 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-MEPYRAMINE 2 89 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-MEPYRAMINE 2 89 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-MEPYRAMINE 2 89 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-MEPYRAMINE 2 89 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
4011 82408 49 UNDEFINED 6 24 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
CHEMBL21731 82408 49 UNDEFINED 6 24 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
135 2532 43 3H-PYRILAMINE -1 58 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 43 3H-PYRILAMINE -1 58 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 43 3H-PYRILAMINE -1 58 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 43 3H-PYRILAMINE -1 58 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 43 3H-PYRILAMINE -1 58 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
135 2532 43 3H-MEPYRAMINE 1 58 Rat 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 43 3H-MEPYRAMINE 1 58 Rat 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 43 3H-MEPYRAMINE 1 58 Rat 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 43 3H-MEPYRAMINE 1 58 Rat 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 43 3H-MEPYRAMINE 1 58 Rat 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1524 2181 96 3H-MEPYRAMINE -2 52 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2181 96 3H-MEPYRAMINE -2 52 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2181 96 3H-MEPYRAMINE -2 52 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2181 96 3H-MEPYRAMINE -2 52 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2181 96 3H-MEPYRAMINE -2 52 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2181 96 3H-MEPYRAMINE -2 52 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
135398737 958 93 3H-PYRILAMINE 2 89 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 958 93 UNDEFINED 2 89 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-PYRILAMINE 2 89 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 UNDEFINED 2 89 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-PYRILAMINE 2 89 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 UNDEFINED 2 89 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-PYRILAMINE 2 89 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 UNDEFINED 2 89 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-PYRILAMINE 2 89 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 UNDEFINED 2 89 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1712 2492 43 3H-doxepin 1 22 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
4078 2492 43 3H-doxepin 1 22 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
7227 2492 43 3H-doxepin 1 22 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
CHEMBL1088 2492 43 3H-doxepin 1 22 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
DB00933 2492 43 3H-doxepin 1 22 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
1712 2492 43 UNDEFINED 1 22 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
4078 2492 43 UNDEFINED 1 22 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
7227 2492 43 UNDEFINED 1 22 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
CHEMBL1088 2492 43 UNDEFINED 1 22 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
DB00933 2492 43 UNDEFINED 1 22 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
135398737 958 93 3H-PYRILAMINE 2 89 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-PYRILAMINE 2 89 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-PYRILAMINE 2 89 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-PYRILAMINE 2 89 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-PYRILAMINE 2 89 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 958 93 3H-MEPYRAMINE 2 89 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-MEPYRAMINE 2 89 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-MEPYRAMINE 2 89 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-MEPYRAMINE 2 89 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-MEPYRAMINE 2 89 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
90475904 216022 0 3H-MEPYRAMINE 6 6 Guinea pig 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(C)CCC(C1=CC=C(C=C1)Cl)C2=CC=CC=N2 None
1222 881 0 3H-MEPYRAMINE -1 2 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
2678 881 0 3H-MEPYRAMINE -1 2 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
581 881 0 3H-MEPYRAMINE -1 2 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
CHEMBL1000 881 0 3H-MEPYRAMINE -1 2 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
DB00341 881 0 3H-MEPYRAMINE -1 2 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
1170 1633 75 3H-MEPYRAMINE - 1 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C None
3348 1633 75 3H-MEPYRAMINE - 1 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C None
4819 1633 75 3H-MEPYRAMINE - 1 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C None
74685737 1633 75 3H-MEPYRAMINE - 1 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C None
CHEMBL914 1633 75 3H-MEPYRAMINE - 1 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C None
DB00950 1633 75 3H-MEPYRAMINE - 1 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C None
1971 2866 38 3H-MEPYRAMINE -1 30 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
2404 2866 38 3H-MEPYRAMINE -1 30 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
4543 2866 38 3H-MEPYRAMINE -1 30 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
CHEMBL445 2866 38 3H-MEPYRAMINE -1 30 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
DB00540 2866 38 3H-MEPYRAMINE -1 30 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
115237 55585 119 3H-PYRILAMINE -42 54 Guinea pig 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55585 119 3H-PYRILAMINE -42 54 Guinea pig 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
None 216919 0 UNDEFINED - 1 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 311 4 1 4 2.7 C1COC2=C1C=CC=C2OC(C3CNCCO3)C4=CC=CC=C4 None
None 216920 0 UNDEFINED - 1 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 305 4 1 3 3.1 C1COC(CN1)C(C2=CC=CC=C2)OC3=C(C(=CC=C3)F)F None
None 216921 0 UNDEFINED - 1 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 301 4 1 3 3.2 CC1=C(C=CC(=C1)F)OC(C2CNCCO2)C3=CC=CC=C3 None
None 216922 0 UNDEFINED - 1 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 3.6 C1COC(CN1)C(C2=CC=CC=C2)OC3=C(C=C(C=C3)F)Cl None
None 216923 0 UNDEFINED - 1 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 317 5 1 4 2.9 COC1=C(C=CC(=C1)F)OC(C2CNCCO2)C3=CC=CC=C3 None
277 1301 62 None -2 50 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1301 62 None -2 50 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1301 62 None -2 50 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1301 62 None -2 50 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1301 62 None -2 50 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
3246155 215962 0 3H-MEPYRAMINE -46 16 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 307 4 0 2 4.4 CN1C2CCC1CC(C2)OC(C3=CC=CC=C3)C4=CC=CC=C4 None
1204 1932 119 3H-Histamine -46 24 Guinea pig 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1932 119 3H-Histamine -46 24 Guinea pig 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1932 119 3H-Histamine -46 24 Guinea pig 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1932 119 3H-Histamine -46 24 Guinea pig 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1932 119 3H-Histamine -46 24 Guinea pig 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1932 119 3H-Histamine -46 24 Guinea pig 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
21722 17992 31 3H-MEPYRAMINE -1 6 Rat 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 None
CHEMBL126224 17992 31 3H-MEPYRAMINE -1 6 Rat 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 None
1353 1911 93 3H-MEPYRAMINE -602 83 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 3H-MEPYRAMINE -602 83 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 3H-MEPYRAMINE -602 83 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 3H-MEPYRAMINE -602 83 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 3H-MEPYRAMINE -602 83 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
46222048 8984 0 UNDEFINED -4365 13 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 260 4 1 2 4.0 CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1 None
CHEMBL1098230 8984 0 UNDEFINED -4365 13 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 260 4 1 2 4.0 CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1 None
18922713 98498 0 3H-PYRILAMINE -12882 9 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 298 6 1 2 4.0 CCCN(CCC)C1Cc2c[nH]c3ccc(C(C)=O)c(c23)C1 None
CHEMBL276031 98498 0 3H-PYRILAMINE -12882 9 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 298 6 1 2 4.0 CCCN(CCC)C1Cc2c[nH]c3ccc(C(C)=O)c(c23)C1 None
54841 203127 52 3H-PYRILAMINE -2 27 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 255 6 1 2 3.7 CNCC[C@@H](Oc1ccccc1C)c1ccccc1 None
CHEMBL641 203127 52 3H-PYRILAMINE -2 27 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 255 6 1 2 3.7 CNCC[C@@H](Oc1ccccc1C)c1ccccc1 None
3947 206395 53 3H-MEPYRAMINE -147 16 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 None
CHEMBL87708 206395 53 3H-MEPYRAMINE -147 16 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 None
12057539 208041 42 3H-MEPYRAMINE -676 20 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 208041 42 3H-MEPYRAMINE -676 20 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 208041 42 3H-MEPYRAMINE -676 20 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
179 400 115 3H-PYRILAMINE -4365 49 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
179 400 115 3H-PYRILAMINE -4365 49 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 400 115 3H-PYRILAMINE -4365 49 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 400 115 3H-PYRILAMINE -4365 49 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 400 115 3H-PYRILAMINE -4365 49 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 400 115 3H-PYRILAMINE -4365 49 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 400 115 3H-PYRILAMINE -4365 49 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 400 115 3H-PYRILAMINE -4365 49 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 400 115 3H-PYRILAMINE -4365 49 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 400 115 3H-PYRILAMINE -4365 49 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2247 505 81 3H-Histamine -4 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
249 505 81 3H-Histamine -4 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
2603 505 81 3H-Histamine -4 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
CHEMBL296419 505 81 3H-Histamine -4 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
DB00637 505 81 3H-Histamine -4 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
1001 620 95 3H-Histamine -3 2 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 121 2 1 1 1.2 NCCc1ccccc1 None
2144 620 95 3H-Histamine -3 2 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 121 2 1 1 1.2 NCCc1ccccc1 None
CHEMBL610 620 95 3H-Histamine -3 2 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 121 2 1 1 1.2 NCCc1ccccc1 None
DB04325 620 95 3H-Histamine -3 2 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 121 2 1 1 1.2 NCCc1ccccc1 None
31101 729 40 3H-PYRILAMINE -14454 36 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 729 40 3H-PYRILAMINE -14454 36 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 729 40 3H-PYRILAMINE -14454 36 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 729 40 3H-PYRILAMINE -14454 36 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 729 40 3H-PYRILAMINE -14454 36 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
2554 796 119 3H-doxepin 1 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 236 0 1 1 3.4 NC(=O)N1c2ccccc2C=Cc2c1cccc2 None
489 796 119 3H-doxepin 1 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 236 0 1 1 3.4 NC(=O)N1c2ccccc2C=Cc2c1cccc2 None
5339 796 119 3H-doxepin 1 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 236 0 1 1 3.4 NC(=O)N1c2ccccc2C=Cc2c1cccc2 None
CHEMBL108 796 119 3H-doxepin 1 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 236 0 1 1 3.4 NC(=O)N1c2ccccc2C=Cc2c1cccc2 None
DB00564 796 119 3H-doxepin 1 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 236 0 1 1 3.4 NC(=O)N1c2ccccc2C=Cc2c1cccc2 None
1222 881 0 3H-Histamine -1 2 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
2678 881 0 3H-Histamine -1 2 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
581 881 0 3H-Histamine -1 2 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
CHEMBL1000 881 0 3H-Histamine -1 2 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
DB00341 881 0 3H-Histamine -1 2 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
1210 918 51 3H-Histamine -20 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
1213 918 51 3H-Histamine -20 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
2725 918 51 3H-Histamine -20 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
33036 918 51 3H-Histamine -20 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
4411 918 51 3H-Histamine -20 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
616 918 51 3H-Histamine -20 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
6976 918 51 3H-Histamine -20 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
716121 918 51 3H-Histamine -20 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1201353 918 51 3H-Histamine -20 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1554789 918 51 3H-Histamine -20 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL505 918 51 3H-Histamine -20 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
DB01114 918 51 3H-Histamine -20 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
DB13679 918 51 3H-Histamine -20 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
1231 937 116 3H-doxepin -81 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
2756 937 116 3H-doxepin -81 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
645 937 116 3H-doxepin -81 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
CHEMBL30 937 116 3H-doxepin -81 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
DB00501 937 116 3H-doxepin -81 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
1248 1424 28 3H-MEPYRAMINE -208 6 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 161 4 2 3 0.6 CN(CCCSC(=N)N)C None
3077 1424 28 3H-MEPYRAMINE -208 6 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 161 4 2 3 0.6 CN(CCCSC(=N)N)C None
90045 1424 28 3H-MEPYRAMINE -208 6 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 161 4 2 3 0.6 CN(CCCSC(=N)N)C None
CHEMBL12344 1424 28 3H-MEPYRAMINE -208 6 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 161 4 2 3 0.6 CN(CCCSC(=N)N)C None
1224 1432 83 3H-Histamine -2 13 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
3100 1432 83 3H-Histamine -2 13 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
8980 1432 83 3H-Histamine -2 13 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
916 1432 83 3H-Histamine -2 13 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
CHEMBL657 1432 83 3H-Histamine -2 13 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
DB01075 1432 83 3H-Histamine -2 13 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
1170 1633 75 3H-Histamine - 1 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C None
3348 1633 75 3H-Histamine - 1 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C None
4819 1633 75 3H-Histamine - 1 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C None
74685737 1633 75 3H-Histamine - 1 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C None
CHEMBL914 1633 75 3H-Histamine - 1 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C None
DB00950 1633 75 3H-Histamine - 1 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C None
1209 1658 75 3H-PYRILAMINE -144 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
203 1658 75 3H-PYRILAMINE -144 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
3386 1658 75 3H-PYRILAMINE -144 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL41 1658 75 3H-PYRILAMINE -144 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
DB00472 1658 75 3H-PYRILAMINE -144 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
119376 1841 48 3H-MEPYRAMINE -43651 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
247 1841 48 3H-MEPYRAMINE -43651 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
CHEMBL33884 1841 48 3H-MEPYRAMINE -43651 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
1204 1932 119 3H-MEPYRAMINE -46 24 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1204 1932 119 3H-MEPYRAMINE -501 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1204 1932 119 3H-doxepin -501 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1204 1932 119 3H-trans-H2-PAT,(-) -501 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1204 1932 119 3H-MEPYRAMINE -309 24 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1932 119 3H-MEPYRAMINE -46 24 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1932 119 3H-MEPYRAMINE -501 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1932 119 3H-doxepin -501 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1932 119 3H-trans-H2-PAT,(-) -501 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1932 119 3H-MEPYRAMINE -309 24 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1932 119 3H-MEPYRAMINE -46 24 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1932 119 3H-MEPYRAMINE -501 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1932 119 3H-doxepin -501 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1932 119 3H-trans-H2-PAT,(-) -501 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1932 119 3H-MEPYRAMINE -309 24 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1932 119 3H-MEPYRAMINE -46 24 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1932 119 3H-MEPYRAMINE -501 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1932 119 3H-doxepin -501 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1932 119 3H-trans-H2-PAT,(-) -501 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1932 119 3H-MEPYRAMINE -309 24 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1932 119 3H-MEPYRAMINE -46 24 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1932 119 3H-MEPYRAMINE -501 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1932 119 3H-doxepin -501 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1932 119 3H-trans-H2-PAT,(-) -501 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1932 119 3H-MEPYRAMINE -309 24 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1932 119 3H-MEPYRAMINE -46 24 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1932 119 3H-MEPYRAMINE -501 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1932 119 3H-doxepin -501 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1932 119 3H-trans-H2-PAT,(-) -501 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1932 119 3H-MEPYRAMINE -309 24 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1400 1957 70 3H-Histamine 2 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
3658 1957 70 3H-Histamine 2 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
7199 1957 70 3H-Histamine 2 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
91513 1957 70 3H-Histamine 2 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
CHEMBL896 1957 70 3H-Histamine 2 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
DB00557 1957 70 3H-Histamine 2 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
1427 2013 54 3H-Histamine -5 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
357 2013 54 3H-Histamine -5 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
3696 2013 54 3H-Histamine -5 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
CHEMBL11 2013 54 3H-Histamine -5 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
DB00458 2013 54 3H-Histamine -5 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
1530 2182 50 3H-Histamine -5 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
3827 2182 50 3H-Histamine -5 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
7206 2182 50 3H-Histamine -5 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
CHEMBL534 2182 50 3H-Histamine -5 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
DB00920 2182 50 3H-Histamine -5 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
18971832 2418 0 3H-PYRILAMINE -1621 13 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 3 2 2 4.0 CN(C1CCc2c(C1)c1cc(ccc1[nH]2)NC(=O)c1ccc(cc1)F)C None
21 2418 0 3H-PYRILAMINE -1621 13 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 3 2 2 4.0 CN(C1CCc2c(C1)c1cc(ccc1[nH]2)NC(=O)c1ccc(cc1)F)C None
CHEMBL3186179 2418 0 3H-PYRILAMINE -1621 13 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 3 2 2 4.0 CN(C1CCc2c(C1)c1cc(ccc1[nH]2)NC(=O)c1ccc(cc1)F)C None
1227 2489 43 3H-Histamine -2 12 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
2331 2489 43 3H-Histamine -2 12 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
3957 2489 43 3H-Histamine -2 12 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
4992 2489 43 3H-Histamine -2 12 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
CHEMBL511 2489 43 3H-Histamine -2 12 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
DB06691 2489 43 3H-Histamine -2 12 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
134 2514 24 3H-PYRILAMINE -933 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
134 2514 24 3H-MEPYRAMINE -15488 67 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 24 3H-PYRILAMINE -933 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 24 3H-MEPYRAMINE -15488 67 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 24 3H-PYRILAMINE -933 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 24 3H-MEPYRAMINE -15488 67 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 24 3H-PYRILAMINE -933 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 24 3H-MEPYRAMINE -15488 67 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 24 3H-PYRILAMINE -933 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 24 3H-MEPYRAMINE -15488 67 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1233 2515 0 3H-MEPYRAMINE -19 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 244 5 3 3 1.0 CNC(=S)NCCSCc1nc[nH]c1C None
1548992 2515 0 3H-MEPYRAMINE -19 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 244 5 3 3 1.0 CNC(=S)NCCSCc1nc[nH]c1C None
CHEMBL275446 2515 0 3H-MEPYRAMINE -19 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 244 5 3 3 1.0 CNC(=S)NCCSCc1nc[nH]c1C None
DB08805 2515 0 3H-MEPYRAMINE -19 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 244 5 3 3 1.0 CNC(=S)NCCSCc1nc[nH]c1C None
1782 2518 84 3H-MEPYRAMINE -676 22 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
241 2518 84 3H-MEPYRAMINE -676 22 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
4168 2518 84 3H-MEPYRAMINE -676 22 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
CHEMBL86 2518 84 3H-MEPYRAMINE -676 22 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
DB01233 2518 84 3H-MEPYRAMINE -676 22 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
135 2532 43 3H-Histamine -1 58 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 43 3H-Histamine -1 58 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 43 3H-Histamine -1 58 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 43 3H-Histamine -1 58 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 43 3H-Histamine -1 58 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1830 2590 44 3H-doxepin -125 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
1830 2590 44 UNDEFINED -125 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 2590 44 3H-doxepin -125 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 2590 44 UNDEFINED -125 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 2590 44 3H-doxepin -125 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 2590 44 UNDEFINED -125 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 2590 44 3H-doxepin -125 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 2590 44 UNDEFINED -125 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 2590 44 3H-doxepin -125 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 2590 44 UNDEFINED -125 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
1890 2759 49 3H-PYRILAMINE -44 16 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
4449 2759 49 3H-PYRILAMINE -44 16 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
7247 2759 49 3H-PYRILAMINE -44 16 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
CHEMBL623 2759 49 3H-PYRILAMINE -44 16 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
DB01149 2759 49 3H-PYRILAMINE -44 16 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
15897 2862 0 3H-PYRILAMINE -354 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2862 0 3H-PYRILAMINE -354 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2862 0 3H-PYRILAMINE -354 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
208 2863 0 3H-PYRILAMINE -109 13 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 4.2 NCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
4541 2863 0 3H-PYRILAMINE -109 13 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 4.2 NCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL1494 2863 0 3H-PYRILAMINE -109 13 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 4.2 NCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
2142 3096 58 3H-MEPYRAMINE -7585 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 3096 58 3H-MEPYRAMINE -7585 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 3096 58 3H-MEPYRAMINE -7585 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 3096 58 3H-MEPYRAMINE -7585 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 3096 58 3H-MEPYRAMINE -7585 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 3096 58 3H-MEPYRAMINE -7585 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
2202 3132 96 3H-PYRILAMINE -316 21 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
4850 3132 96 3H-PYRILAMINE -316 21 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
49 3132 96 3H-PYRILAMINE -316 21 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
CHEMBL1371770 3132 96 3H-PYRILAMINE -316 21 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
DB12478 3132 96 3H-PYRILAMINE -316 21 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
119570 3159 96 3H-PYRILAMINE -7585 40 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
119570 3159 96 3H-PYRILAMINE -162 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 3159 96 3H-PYRILAMINE -7585 40 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 3159 96 3H-PYRILAMINE -162 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 3159 96 3H-PYRILAMINE -7585 40 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 3159 96 3H-PYRILAMINE -162 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 3159 96 3H-PYRILAMINE -7585 40 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 3159 96 3H-PYRILAMINE -162 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 3159 96 3H-PYRILAMINE -7585 40 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 3159 96 3H-PYRILAMINE -162 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2286 3183 51 3H-Histamine -2 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
4927 3183 51 3H-Histamine -2 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
7282 3183 51 3H-Histamine -2 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
CHEMBL643 3183 51 3H-Histamine -2 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
DB01069 3183 51 3H-Histamine -2 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
243 3202 91 3H-PYRILAMINE -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3052762 3202 91 3H-PYRILAMINE -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3502 3202 91 3H-PYRILAMINE -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
CHEMBL117287 3202 91 3H-PYRILAMINE -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
DB06480 3202 91 3H-PYRILAMINE -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
1234 3291 68 3H-MEPYRAMINE -162 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C None
1234 3291 68 3H-doxepin -162 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C None
3001055 3291 68 3H-MEPYRAMINE -162 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C None
3001055 3291 68 3H-doxepin -162 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C None
CHEMBL512 3291 68 3H-MEPYRAMINE -162 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C None
CHEMBL512 3291 68 3H-doxepin -162 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C None
DB00863 3291 68 3H-MEPYRAMINE -162 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C None
DB00863 3291 68 3H-doxepin -162 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C None
128563 3464 33 3H-PYRILAMINE -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
1666 3464 33 3H-PYRILAMINE -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
CHEMBL445332 3464 33 3H-PYRILAMINE -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
DB12327 3464 33 3H-PYRILAMINE -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
221 3491 71 UNDEFINED -478 14 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
3277600 3491 71 UNDEFINED -478 14 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
CHEMBL323356 3491 71 UNDEFINED -478 14 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
189 3492 39 3H-MEPYRAMINE -4168 17 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 None
5163 3492 39 3H-MEPYRAMINE -4168 17 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 None
CHEMBL297784 3492 39 3H-MEPYRAMINE -4168 17 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 None
6917970 3691 61 3H-PYRILAMINE -2290 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
8370 3691 61 3H-PYRILAMINE -2290 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
CHEMBL487387 3691 61 3H-PYRILAMINE -2290 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
1577 3703 110 3H-MEPYRAMINE -549 21 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2537 3703 110 3H-MEPYRAMINE -549 21 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5355 3703 110 3H-MEPYRAMINE -549 21 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5501 3703 110 3H-MEPYRAMINE -549 21 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
643497 3703 110 3H-MEPYRAMINE -549 21 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
688272 3703 110 3H-MEPYRAMINE -549 21 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
958 3703 110 3H-MEPYRAMINE -549 21 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
960 3703 110 3H-MEPYRAMINE -549 21 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL196677 3703 110 3H-MEPYRAMINE -549 21 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL26 3703 110 3H-MEPYRAMINE -549 21 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL267044 3703 110 3H-MEPYRAMINE -549 21 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB00391 3703 110 3H-MEPYRAMINE -549 21 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB16021 3703 110 3H-MEPYRAMINE -549 21 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
1267 3804 49 3H-MEPYRAMINE -4168 26 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
1267 3804 49 3H-MEPYRAMINE -4168 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
3035905 3804 49 3H-MEPYRAMINE -4168 26 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
3035905 3804 49 3H-MEPYRAMINE -4168 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
CHEMBL260374 3804 49 3H-MEPYRAMINE -4168 26 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
CHEMBL260374 3804 49 3H-MEPYRAMINE -4168 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
1235 3823 36 3H-doxepin -316 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N None
3959 3823 36 3H-doxepin -316 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N None
50287 3823 36 3H-doxepin -316 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N None
CHEMBL269646 3823 36 3H-doxepin -316 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N None
2762 3863 31 3H-Histamine -9 2 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C None
5587 3863 31 3H-Histamine -9 2 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C None
7318 3863 31 3H-Histamine -9 2 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C None
CHEMBL1241 3863 31 3H-Histamine -9 2 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C None
DB00792 3863 31 3H-Histamine -9 2 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C None
1228 3866 34 3H-Histamine -5 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
2763 3866 34 3H-Histamine -5 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
5282443 3866 34 3H-Histamine -5 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
CHEMBL855 3866 34 3H-Histamine -5 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
DB00427 3866 34 3H-Histamine -5 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
46882224 6348 0 UNDEFINED -354 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 543 10 1 9 4.7 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)CC)ccc4o3)CC2)cc(OC2CCOCC2)c1 None
CHEMBL1082036 6348 0 UNDEFINED -354 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 543 10 1 9 4.7 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)CC)ccc4o3)CC2)cc(OC2CCOCC2)c1 None
2662 11384 131 3H-PYRILAMINE -41 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 None
CHEMBL118 11384 131 3H-PYRILAMINE -41 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 None
3032915 15495 24 3H-MEPYRAMINE -169 6 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 None
CHEMBL12160 15495 24 3H-MEPYRAMINE -169 6 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 None
3380 22790 34 3H-MEPYRAMINE - 1 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 313 2 0 4 2.5 CN1C(=O)CN=C(c2ccccc2F)c2cc([N+](=O)[O-])ccc21 None
CHEMBL13280 22790 34 3H-MEPYRAMINE - 1 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 313 2 0 4 2.5 CN1C(=O)CN=C(c2ccccc2F)c2cc([N+](=O)[O-])ccc21 None
10297 27112 30 3H-PYRILAMINE -38 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
CHEMBL136560 27112 30 3H-PYRILAMINE -38 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
156391 46800 99 3H-PYRILAMINE -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
CHEMBL1200806 46800 99 3H-PYRILAMINE -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
CHEMBL154 46800 99 3H-PYRILAMINE -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
10624 70300 19 3H-PYRILAMINE -776 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
10624 70300 19 3H-MEPYRAMINE -776 33 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
138543650 70300 19 3H-PYRILAMINE -776 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
138543650 70300 19 3H-MEPYRAMINE -776 33 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
CHEMBL194378 70300 19 3H-PYRILAMINE -776 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
CHEMBL194378 70300 19 3H-MEPYRAMINE -776 33 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
54477 84653 36 3H-MEPYRAMINE -70 23 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
54477 84653 36 3H-PYRILAMINE -70 23 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
CHEMBL22242 84653 36 3H-MEPYRAMINE -70 23 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
CHEMBL22242 84653 36 3H-PYRILAMINE -70 23 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
2244 94233 100 3H-PYRILAMINE -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 180 2 1 3 1.3 CC(=O)Oc1ccccc1C(=O)O None
CHEMBL25 94233 100 3H-PYRILAMINE -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 180 2 1 3 1.3 CC(=O)Oc1ccccc1C(=O)O None
4528 98126 80 3H-Histamine -7 10 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 238 1 1 2 2.8 CN1Cc2c(N)cccc2C(c2ccccc2)C1 None
CHEMBL273575 98126 80 3H-Histamine -7 10 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 238 1 1 2 2.8 CN1Cc2c(N)cccc2C(c2ccccc2)C1 None
104870 98880 47 3H-PYRILAMINE -549 21 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
5374 98880 47 3H-PYRILAMINE -549 21 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
CHEMBL279085 98880 47 3H-PYRILAMINE -549 21 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
3663 99967 83 3H-PYRILAMINE -288 29 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 504 0 6 8 5.1 Cc1cc(O)c2c(=O)c3c(O)cc(O)c4c5c(O)cc(O)c6c(=O)c7c(O)cc(C)c8c1c2c(c34)c(c78)c65 None
CHEMBL286494 99967 83 3H-PYRILAMINE -288 29 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 504 0 6 8 5.1 Cc1cc(O)c2c(=O)c3c(O)cc(O)c4c5c(O)cc(O)c6c(=O)c7c(O)cc(C)c8c1c2c(c34)c(c78)c65 None
37632 111592 28 3H-PYRILAMINE -1 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 3 0 5 3.3 CN(C)Cc1nnc2n1-c1ccc(Cl)cc1C(c1ccccc1)=NC2 None
CHEMBL328250 111592 28 3H-PYRILAMINE -1 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 3 0 5 3.3 CN(C)Cc1nnc2n1-c1ccc(Cl)cc1C(c1ccccc1)=NC2 None
3452843 119525 15 3H-PYRILAMINE -1 10 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 516 6 2 4 5.5 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)c3ccccc3C)C2=O)c1 None
CHEMBL345686 119525 15 3H-PYRILAMINE -1 10 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 516 6 2 4 5.5 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)c3ccccc3C)C2=O)c1 None
44208932 140707 7 UNDEFINED -89125 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 475 5 1 3 6.8 Cc1ccc(Cn2nc(C(=O)NC3C4(C)CCC(C4)C3(C)C)cc2-c2ccc(Cl)c(C)c2)cc1 None
CHEMBL381689 140707 7 UNDEFINED -89125 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 475 5 1 3 6.8 Cc1ccc(Cn2nc(C(=O)NC3C4(C)CCC(C4)C3(C)C)cc2-c2ccc(Cl)c(C)c2)cc1 None
4737 172454 27 3H-doxepin - 1 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 226 4 2 3 1.2 CCCC(C)C1(CC)C(=O)NC(=O)NC1=O None
CHEMBL448 172454 27 3H-doxepin - 1 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 226 4 2 3 1.2 CCCC(C)C1(CC)C(=O)NC(=O)NC1=O None
4595 176715 106 3H-MEPYRAMINE -186 15 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 293 2 0 4 3.1 Cc1nccn1CC1CCc2c(c3ccccc3n2C)C1=O None
CHEMBL46 176715 106 3H-MEPYRAMINE -186 15 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 293 2 0 4 3.1 Cc1nccn1CC1CCc2c(c3ccccc3n2C)C1=O None
43815 186920 64 3H-PYRILAMINE -1995 25 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
43815 186920 64 3H-PYRILAMINE -1995 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
43815 186920 64 3H-MEPYRAMINE -1995 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
CHEMBL1708 186920 64 3H-PYRILAMINE -1995 25 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
CHEMBL1708 186920 64 3H-PYRILAMINE -1995 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
CHEMBL1708 186920 64 3H-MEPYRAMINE -1995 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
CHEMBL490 186920 64 3H-PYRILAMINE -1995 25 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
CHEMBL490 186920 64 3H-PYRILAMINE -1995 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
CHEMBL490 186920 64 3H-MEPYRAMINE -1995 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
5280343 188275 124 3H-PYRILAMINE -147 32 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL1520590 188275 124 3H-PYRILAMINE -147 32 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL50 188275 124 3H-PYRILAMINE -147 32 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
12016890 190776 6 3H-PYRILAMINE -16982 11 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 318 4 1 3 2.6 NC(=O)c1ccc(F)c2c1CC(N(C1CCC1)C1CCC1)CO2 None
CHEMBL5183389 190776 6 3H-PYRILAMINE -16982 11 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 318 4 1 3 2.6 NC(=O)c1ccc(F)c2c1CC(N(C1CCC1)C1CCC1)CO2 None
3672 192533 136 3H-PYRILAMINE -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 206 4 1 1 3.1 CC(C)Cc1ccc(C(C)C(=O)O)cc1 None
CHEMBL521 192533 136 3H-PYRILAMINE -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 206 4 1 1 3.1 CC(C)Cc1ccc(C(C)C(=O)O)cc1 None
54676228 193615 112 3H-PYRILAMINE -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 2 2 5 1.6 CN1C(C(=O)Nc2ccccn2)=C(O)c2ccccc2S1(=O)=O None
CHEMBL527 193615 112 3H-PYRILAMINE -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 2 2 5 1.6 CN1C(C(=O)Nc2ccccn2)=C(O)c2ccccc2S1(=O)=O None
4495 196535 92 3H-PYRILAMINE -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 None
CHEMBL56367 196535 92 3H-PYRILAMINE -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 None
54677470 200551 115 3H-PYRILAMINE -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
CHEMBL1256873 200551 115 3H-PYRILAMINE -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
CHEMBL599 200551 115 3H-PYRILAMINE -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
162265 202274 22 3H-PYRILAMINE -239 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4786 202274 22 3H-PYRILAMINE -239 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
CHEMBL61006 202274 22 3H-PYRILAMINE -239 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
5281600 203025 92 3H-PYRILAMINE -275 33 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
CHEMBL63354 203025 92 3H-PYRILAMINE -275 33 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
5656 203066 87 3H-PYRILAMINE -79 40 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
5656 203066 87 3H-PYRILAMINE -79 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
5656 203066 87 3H-MEPYRAMINE -79 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
CHEMBL637 203066 87 3H-PYRILAMINE -79 40 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
CHEMBL637 203066 87 3H-PYRILAMINE -79 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
CHEMBL637 203066 87 3H-MEPYRAMINE -79 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
1238 203174 24 3H-Histamine -38 16 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL64249 203174 24 3H-Histamine -38 16 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
1973 203483 15 3H-PYRILAMINE -3 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL1394464 203483 15 3H-PYRILAMINE -3 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL66089 203483 15 3H-PYRILAMINE -3 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
2118 203485 36 3H-doxepin -24 2 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 308 1 0 4 3.6 Cc1nnc2n1-c1ccc(Cl)cc1C(c1ccccc1)=NC2 None
CHEMBL661 203485 36 3H-doxepin -24 2 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 308 1 0 4 3.6 Cc1nnc2n1-c1ccc(Cl)cc1C(c1ccccc1)=NC2 None
3291 204000 77 3H-doxepin - 1 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 141 1 1 2 0.4 CCC1(C)CC(=O)NC1=O None
CHEMBL696 204000 77 3H-doxepin - 1 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 141 1 1 2 0.4 CCC1(C)CC(=O)NC1=O None
2995 204405 53 3H-Histamine -14 23 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 204405 53 3H-Histamine -14 23 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 204405 53 3H-Histamine -14 23 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
3821 204718 17 3H-PYRILAMINE -1 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 237 2 1 2 2.9 CNC1(c2ccccc2Cl)CCCCC1=O None
CHEMBL742 204718 17 3H-PYRILAMINE -1 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 237 2 1 2 2.9 CNC1(c2ccccc2Cl)CCCCC1=O None
4054 205501 72 3H-PYRILAMINE -1 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL1699 205501 72 3H-PYRILAMINE -1 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL807 205501 72 3H-PYRILAMINE -1 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
68617 205527 62 3H-PYRILAMINE -1023 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
68617 205527 62 3H-MEPYRAMINE -1445 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL1709 205527 62 3H-PYRILAMINE -1023 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL1709 205527 62 3H-MEPYRAMINE -1445 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL809 205527 62 3H-PYRILAMINE -1023 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL809 205527 62 3H-MEPYRAMINE -1445 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
5324346 205582 59 3H-PYRILAMINE -1 10 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 318 9 1 4 3.2 COCCCC/C(=N\OCCN)c1ccc(C(F)(F)F)cc1 None
5324346 205582 59 3H-MEPYRAMINE -1 10 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 318 9 1 4 3.2 COCCCC/C(=N\OCCN)c1ccc(C(F)(F)F)cc1 None
CHEMBL1409 205582 59 3H-PYRILAMINE -1 10 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 318 9 1 4 3.2 COCCCC/C(=N\OCCN)c1ccc(C(F)(F)F)cc1 None
CHEMBL1409 205582 59 3H-MEPYRAMINE -1 10 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 318 9 1 4 3.2 COCCCC/C(=N\OCCN)c1ccc(C(F)(F)F)cc1 None
CHEMBL814 205582 59 3H-PYRILAMINE -1 10 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 318 9 1 4 3.2 COCCCC/C(=N\OCCN)c1ccc(C(F)(F)F)cc1 None
CHEMBL814 205582 59 3H-MEPYRAMINE -1 10 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 318 9 1 4 3.2 COCCCC/C(=N\OCCN)c1ccc(C(F)(F)F)cc1 None
119607 206203 113 3H-PYRILAMINE -97 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 1 4 3.0 Cc1onc(-c2ccccc2)c1-c1ccc(S(N)(=O)=O)cc1 None
CHEMBL865 206203 113 3H-PYRILAMINE -97 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 1 4 3.0 Cc1onc(-c2ccccc2)c1-c1ccc(S(N)(=O)=O)cc1 None
3337 206367 27 3H-PYRILAMINE -1513 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 206367 27 3H-PYRILAMINE -1513 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 206367 27 3H-PYRILAMINE -1513 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 206367 27 3H-PYRILAMINE -1513 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 206367 27 3H-PYRILAMINE -1513 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
444 206666 53 3H-PYRILAMINE -2089 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 239 3 1 2 3.3 CC(NC(C)(C)C)C(=O)c1cccc(Cl)c1 None
CHEMBL894 206666 53 3H-PYRILAMINE -2089 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 239 3 1 2 3.3 CC(NC(C)(C)C)C(=O)c1cccc(Cl)c1 None
16231 207509 57 3H-MEPYRAMINE -7 17 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 229 1 5 6 -1.1 N=C(N)NC(=O)c1nc(Cl)c(N)nc1N None
CHEMBL945 207509 57 3H-MEPYRAMINE -7 17 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 229 1 5 6 -1.1 N=C(N)NC(=O)c1nc(Cl)c(N)nc1N None
165193 215945 0 3H-doxepin -42657 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
62882 215945 0 3H-doxepin -42657 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
66366 215945 0 3H-doxepin -42657 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
11954224 215953 0 3H-PYRILAMINE -141253 58 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
None 215958 0 3H-MEPYRAMINE -63095 19 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 421 9 1 6 4.3 COC1=C(C(=CC=C1)OC)OCCNCC2C(OC3=CC=CC=C3O2)C4=CC=CC=C4 None
25058166 215960 0 3H-PYRILAMINE -5011 27 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 215960 0 3H-PYRILAMINE -5011 27 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
44134711 215991 0 3H-MEPYRAMINE -112201 14 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 340 6 2 4 2.8 CCC1=CC(=C(C(=C1O)C(=O)NCC2CCCN2CC)OC)Cl None
None 215993 0 3H-PYRILAMINE -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 2 0 4 3.6 CC1=NC=CN1CC2CCC3=C(C2=O)C4=CC=CC=C4N3C.Cl None
104911 216019 0 3H-PYRILAMINE -41686 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 530 7 0 5 5.1 COC1=CC=CC=C1N2CCN(CC2)CCN(C3=CC=CC=N3)C(=O)C4CCCCC4.Cl.Cl.Cl None
104911 216019 0 3H-PYRILAMINE -41686 37 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 530 7 0 5 5.1 COC1=CC=CC=C1N2CCN(CC2)CCN(C3=CC=CC=N3)C(=O)C4CCCCC4.Cl.Cl.Cl None
131632304 216037 0 3H-MEPYRAMINE -70794 12 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 4 1 5 0.9 CN1C2CC(CC1C3C2O3)OC(=O)C(CO)C4=CC=CC=C4 None
119380 216129 0 3H-PYRILAMINE -1 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 166 1 0 3 1.8 CC1=NOC(=C1)C2CCCN2C None
None 216154 0 3H-doxepin - 1 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 2 1 4 2.4 C1C(=O)NC2=C(C=C(C=C2)[N+](=O)[O-])C(=N1)C3=CC=CC=C3 None
None 216155 0 3H-doxepin 1 2 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 1 0 7 2.6 CN1CCC2=CC3=C(C=C2C1C4C5=C(C6=C(C=C5)OCO6)C(=O)O4)OCO3 None
25137849 216179 0 3H-PYRILAMINE -4 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
71290 216179 0 3H-PYRILAMINE -4 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
None 216249 0 3H-MEPYRAMINE -501 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 468 12 0 9 -0.1 C1COCCN1CCCN2CN(CN(C2)CCCN3CCOCC3)CCCN4CCOCC4 None
None 216250 0 3H-MEPYRAMINE -1258 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 434 6 4 8 2.2 CC(C)O.COC1=C(C=CC(=C1)CC2COC(=O)C2(CC3=CC(=C(C=C3)O)OC)O)O None
None 216251 0 3H-MEPYRAMINE -3981 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 234 2 1 3 2.0 CC(=O)NC1=C(C(=C(C=C1F)F)F)[N+](=O)[O-] None
None 216252 0 3H-MEPYRAMINE -4677 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 0 1 2 4.0 CC12CCC(CC1CCC3C2CCC4(C3CCC4=O)C)(C#C)O None
None 216253 0 3H-MEPYRAMINE -6025 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 5 1 3 4.5 CCCC1=CC2=C(C=C1NC(=O)C3C(C3(C)C)C=C(C)C)OCO2 None
None 216311 0 3H-PYRILAMINE -1 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 240 7 4 6 -0.8 C(C(C(=O)O)N)SSCC(C(=O)O)N None
None 216311 0 3H-PYRILAMINE -1 33 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 240 7 4 6 -0.8 C(C(C(=O)O)N)SSCC(C(=O)O)N None
None 216312 0 3H-PYRILAMINE -1 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 4 2 3 0.2 CSCCC(C(=O)O)N None
None 216312 0 3H-PYRILAMINE -1 33 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 4 2 3 0.2 CSCCC(C(=O)O)N None
None 216313 0 3H-PYRILAMINE -1 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 135 3 3 3 -0.3 C(CS)C(C(=O)O)N None
None 216313 0 3H-PYRILAMINE -1 33 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 135 3 3 3 -0.3 C(CS)C(C(=O)O)N None
None 216314 0 3H-PYRILAMINE -1 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 121 2 3 3 -0.7 C(C(C(=O)O)N)S None
None 216314 0 3H-PYRILAMINE -1 33 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 121 2 3 3 -0.7 C(C(C(=O)O)N)S None
None 216315 0 3H-PYRILAMINE -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 117 0 1 3 -0.0 C1CSC(=O)C1N None
None 216316 0 3H-PYRILAMINE -1 39 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 3 3 3 -1.4 C(C(C(=O)O)N)S(=O)O None
None 216316 0 3H-PYRILAMINE -1 39 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 3 3 3 -1.4 C(C(C(=O)O)N)S(=O)O None
None 216317 0 3H-PYRILAMINE -1 38 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 3 3 4 -1.7 C(C(C(=O)O)N)S(=O)(=O)O None
None 216317 0 3H-PYRILAMINE -1 38 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 3 3 4 -1.7 C(C(C(=O)O)N)S(=O)(=O)O None
None 216318 0 3H-PYRILAMINE -1 30 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 183 4 3 4 -1.3 C(CS(=O)(=O)O)C(C(=O)O)N None
None 216325 0 3H-PYRILAMINE -13 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 2 1 2 1.2 CC(C(=O)C1=CC=CC=C1)N None
1576 216326 0 3H-PYRILAMINE -16 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 163 3 1 2 1.5 CC(C(=O)C1=CC=CC=C1)NC None
None 216327 0 3H-PYRILAMINE -16 28 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 536 11 1 4 9.0 CC(C)C(=O)C12C(=O)C(=C(C(C1=O)(CC(C2(C)CCC=C(C)C)CC=C(C)C)CC=C(C)C)O)CC=C(C)C None
4978 216328 0 3H-PYRILAMINE -16 28 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 520 1 7 9 4.3 CC1=CC(=C2C3=C1C4=C5C(=C(C=C4CO)O)C(=O)C6=C(C=C(C7=C6C5=C3C8=C7C(=CC(=C8C2=O)O)O)O)O)O None
None 216329 0 3H-PYRILAMINE -3 28 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 464 4 8 12 -0.6 C1=CC(=C(C=C1C2=C(C(=C3C(=CC(=O)C=C3O2)O)O)OC4C(C(C(C(O4)CO)O)O)O)O)O None
None 216330 0 3H-PYRILAMINE -281 28 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 610 6 10 16 -1.7 CC1C(C(C(C(O1)OCC2C(C(C(C(O2)OC3=C(OC4=CC(=CC(=C4C3=O)O)O)C5=CC(=C(C=C5)O)O)O)O)O)O)O)O None
None 216331 0 3H-PYRILAMINE -1 28 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 448 3 7 11 0.4 CC1C(C(C(C(O1)OC2=C(OC3=CC(=O)C=C(C3=C2O)O)C4=CC(=C(C=C4)O)O)O)O)O None
None 216388 0 3H-PYRILAMINE 1 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 313 5 1 3 3.5 CN(C)CC(C1=CC=C(C=C1)OC)C2(CCCCC2)O.Cl None
135269 216389 0 3H-PYRILAMINE -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 222 5 1 3 2.5 CCCCC(=O)OC1=CC=CC=C1C(=O)O None
5018304 216391 0 3H-PYRILAMINE -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 317 4 1 3 0.0 C1=CC=C(C(=C1)CC(=O)[O-])NC2=C(C=CC=C2Cl)Cl.[Na+] None
84003 216392 0 3H-PYRILAMINE -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 376 6 5 7 -0.0 C1CN2C(=CC=C2C(=O)C3=CC=CC=C3)C1C(=O)O.C(C(CO)(CO)N)O None
119828 216394 0 3H-PYRILAMINE -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 5 1 5 3.5 CCC(=O)NS(=O)(=O)C1=CC=C(C=C1)C2=C(ON=C2C3=CC=CC=C3)C None
None 216395 0 3H-PYRILAMINE -7 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 517 8 2 5 5.2 CC1=C(C2=C(N1C(=O)C3=CC=C(C=C3)Cl)C=CC(=C2)OC)CC(=O)NCCC4=CC=C(C=C4)NC(=O)C None
None 216450 0 UNDEFINED -660 28 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
None 216450 0 Functional -660 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
None 216489 0 3H-PYRILAMINE -4570 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 347 6 0 3 5.0 CC(=O)N(CC1=CC=CC=C1OC)C2=CC=CC=C2OC3=CC=CC=C3 None
None 216493 0 3H-PYRILAMINE -10471285 17 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 372 2 1 3 4.4 CC(C)(C)C1=CC=C(C=C1)NC(=O)N2CCN(CC2)C3=C(C=CC=N3)Cl None
None 216494 0 3H-Strychnine -1 13 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 399 7 4 5 1.8 CN(C)CC(C1=CC=C(C=C1)O)C2(CCCCC2)O.C(CC(=O)O)C(=O)O.O None
1233 2515 0 3H-MEPYRAMINE -19 3 Rat 4.0 pKi = 4 Binding
NoneNone
PDSP KiDatabase 244 5 3 3 1.0 CNC(=S)NCCSCc1nc[nH]c1C None
1548992 2515 0 3H-MEPYRAMINE -19 3 Rat 4.0 pKi = 4 Binding
NoneNone
PDSP KiDatabase 244 5 3 3 1.0 CNC(=S)NCCSCc1nc[nH]c1C None
CHEMBL275446 2515 0 3H-MEPYRAMINE -19 3 Rat 4.0 pKi = 4 Binding
NoneNone
PDSP KiDatabase 244 5 3 3 1.0 CNC(=S)NCCSCc1nc[nH]c1C None
DB08805 2515 0 3H-MEPYRAMINE -19 3 Rat 4.0 pKi = 4 Binding
NoneNone
PDSP KiDatabase 244 5 3 3 1.0 CNC(=S)NCCSCc1nc[nH]c1C None
3036864 202754 19 3H-MEPYRAMINE -416 28 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 202754 19 3H-MEPYRAMINE -416 28 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 202754 19 3H-MEPYRAMINE -416 28 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 202754 19 3H-MEPYRAMINE -416 28 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
46882664 5717 0 UNDEFINED -2 5 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 494 8 2 8 3.6 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)c(S(N)(=O)=O)cc4o3)CC2)ccc1OC None
CHEMBL1078240 5717 0 UNDEFINED -2 5 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 494 8 2 8 3.6 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)c(S(N)(=O)=O)cc4o3)CC2)ccc1OC None
11545813 181194 0 UNDEFINED -24 7 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 400 6 0 3 5.2 O=C(CCCN1C2CCC1CN(c1ccc(Cl)cc1)CC2)c1ccc(F)cc1 None
CHEMBL476109 181194 0 UNDEFINED -24 7 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 400 6 0 3 5.2 O=C(CCCN1C2CCC1CN(c1ccc(Cl)cc1)CC2)c1ccc(F)cc1 None
21830793 91835 10 3H-8-OH-DPAT -6760 45 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
CHEMBL2413154 91835 10 3H-8-OH-DPAT -6760 45 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
2 3261 23 3H-PYRILAMINE -218 29 Guinea pig 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
54562 3261 23 3H-PYRILAMINE -218 29 Guinea pig 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
CHEMBL240773 3261 23 3H-PYRILAMINE -218 29 Guinea pig 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
None 216342 0 3H-PYRILAMINE -194 19 Guinea pig 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 246 2 1 4 1.6 CCCN1CCCC2C1CC3=CN=C(N=C3C2)N None
1427 2013 54 3H-MEPYRAMINE -5 27 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
357 2013 54 3H-MEPYRAMINE -5 27 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
3696 2013 54 3H-MEPYRAMINE -5 27 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
CHEMBL11 2013 54 3H-MEPYRAMINE -5 27 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
DB00458 2013 54 3H-MEPYRAMINE -5 27 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
2337 3256 77 3H-PYRILAMINE 1 62 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2337 3256 77 3H-PYRILAMINE -1 62 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 77 3H-PYRILAMINE 1 62 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 77 3H-PYRILAMINE -1 62 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 77 3H-PYRILAMINE 1 62 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 77 3H-PYRILAMINE -1 62 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 77 3H-PYRILAMINE 1 62 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 77 3H-PYRILAMINE -1 62 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 77 3H-PYRILAMINE 1 62 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 77 3H-PYRILAMINE -1 62 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
1224 1432 83 3H-trans-H2-PAT,(-) -2 13 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
3100 1432 83 3H-trans-H2-PAT,(-) -2 13 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
8980 1432 83 3H-trans-H2-PAT,(-) -2 13 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
916 1432 83 3H-trans-H2-PAT,(-) -2 13 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
CHEMBL657 1432 83 3H-trans-H2-PAT,(-) -2 13 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
DB01075 1432 83 3H-trans-H2-PAT,(-) -2 13 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
1209 1658 75 3H-doxepin -144 32 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
203 1658 75 3H-doxepin -144 32 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
3386 1658 75 3H-doxepin -144 32 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL41 1658 75 3H-doxepin -144 32 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
DB00472 1658 75 3H-doxepin -144 32 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
213 3853 55 3H-PYRILAMINE -8 44 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 3853 55 3H-PYRILAMINE -8 44 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 3853 55 3H-PYRILAMINE -8 44 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 3853 55 3H-PYRILAMINE -8 44 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 3853 55 3H-PYRILAMINE -8 44 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
1353 1911 93 3H-PYRILAMINE -489 83 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 3H-PYRILAMINE -489 83 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 3H-PYRILAMINE -489 83 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 3H-PYRILAMINE -489 83 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 3H-PYRILAMINE -489 83 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1222 1664 49 3H-PYRILAMINE -17 33 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3396 1664 49 3H-PYRILAMINE -17 33 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
85 1664 49 3H-PYRILAMINE -17 33 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL46516 1664 49 3H-PYRILAMINE -17 33 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
DB04842 1664 49 3H-PYRILAMINE -17 33 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
11954259 215979 0 3H-PYRILAMINE -19 43 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
3294 2006 111 3H-PYRILAMINE -14 45 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 2006 111 3H-PYRILAMINE -14 45 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 2006 111 3H-PYRILAMINE -14 45 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 2006 111 3H-PYRILAMINE -14 45 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 2006 111 3H-PYRILAMINE -14 45 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
1222 881 0 3H-MEPYRAMINE 1 2 Guinea pig 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
2678 881 0 3H-MEPYRAMINE 1 2 Guinea pig 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
581 881 0 3H-MEPYRAMINE 1 2 Guinea pig 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
CHEMBL1000 881 0 3H-MEPYRAMINE 1 2 Guinea pig 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
DB00341 881 0 3H-MEPYRAMINE 1 2 Guinea pig 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
100 3805 58 3H-MEPYRAMINE -23 55 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3805 58 3H-MEPYRAMINE -23 55 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3805 58 3H-MEPYRAMINE -23 55 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3805 58 3H-MEPYRAMINE -23 55 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3805 58 3H-MEPYRAMINE -23 55 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
21722 17992 31 3H-doxepin 1 6 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 None
CHEMBL126224 17992 31 3H-doxepin 1 6 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 None
2995 204405 53 3H-doxepin -14 23 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 204405 53 3H-doxepin -14 23 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 204405 53 3H-doxepin -14 23 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
16667681 216153 0 3H-doxepin 4 3 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 390 7 1 5 3.5 CN(C)CCCC1=CC=CC=N1.C1=CC(=CC=C1OC(=O)C=CC(=O)O)Cl None
45485525 197799 0 UNDEFINED - 1 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 337 7 1 2 4.8 Cc1ccc(CCCCN2CCC(C(O)c3ccccc3)CC2)cc1 None
CHEMBL572034 197799 0 UNDEFINED - 1 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 337 7 1 2 4.8 Cc1ccc(CCCCN2CCC(C(O)c3ccccc3)CC2)cc1 None
2995 204405 53 3H-PYRILAMINE -42 23 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 204405 53 3H-PYRILAMINE -42 23 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 204405 53 3H-PYRILAMINE -42 23 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
12057539 208041 42 3H-MEPYRAMINE -676 20 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 208041 42 3H-MEPYRAMINE -676 20 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 208041 42 3H-MEPYRAMINE -676 20 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
1204 1932 119 3H-MEPYRAMINE -501 24 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1932 119 3H-MEPYRAMINE -501 24 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1932 119 3H-MEPYRAMINE -501 24 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1932 119 3H-MEPYRAMINE -501 24 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1932 119 3H-MEPYRAMINE -501 24 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1932 119 3H-MEPYRAMINE -501 24 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1204 1932 119 3H-MEPYRAMINE -501 24 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1932 119 3H-MEPYRAMINE -501 24 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1932 119 3H-MEPYRAMINE -501 24 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1932 119 3H-MEPYRAMINE -501 24 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1932 119 3H-MEPYRAMINE -501 24 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1932 119 3H-MEPYRAMINE -501 24 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
219050 3373 25 3H-PYRILAMINE -794 21 Guinea pig 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 None
52 3373 25 3H-PYRILAMINE -794 21 Guinea pig 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 None
CHEMBL431367 3373 25 3H-PYRILAMINE -794 21 Guinea pig 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 None
2444 14478 26 3H-MEPYRAMINE -1 2 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 333 6 0 2 4.1 CN(C)CCOC(c1ccccc1)c1ccc(Br)cc1 None
CHEMBL1201245 14478 26 3H-MEPYRAMINE -1 2 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 333 6 0 2 4.1 CN(C)CCOC(c1ccccc1)c1ccc(Br)cc1 None
1224 1432 83 3H-MEPYRAMINE -2 13 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
3100 1432 83 3H-MEPYRAMINE -2 13 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
8980 1432 83 3H-MEPYRAMINE -2 13 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
916 1432 83 3H-MEPYRAMINE -2 13 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
CHEMBL657 1432 83 3H-MEPYRAMINE -2 13 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
DB01075 1432 83 3H-MEPYRAMINE -2 13 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
1224 1432 83 3H-MEPYRAMINE 1 13 Guinea pig 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
3100 1432 83 3H-MEPYRAMINE 1 13 Guinea pig 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
8980 1432 83 3H-MEPYRAMINE 1 13 Guinea pig 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
916 1432 83 3H-MEPYRAMINE 1 13 Guinea pig 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
CHEMBL657 1432 83 3H-MEPYRAMINE 1 13 Guinea pig 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
DB01075 1432 83 3H-MEPYRAMINE 1 13 Guinea pig 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
2435 3590 83 3H-PYRILAMINE -95 48 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3590 83 3H-PYRILAMINE -95 48 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3590 83 3H-PYRILAMINE -95 48 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3590 83 3H-PYRILAMINE -95 48 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3590 83 3H-PYRILAMINE -95 48 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
2865 4143 73 3H-PYRILAMINE -58 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4143 73 3H-PYRILAMINE -58 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4143 73 3H-PYRILAMINE -58 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4143 73 3H-PYRILAMINE -58 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4143 73 3H-PYRILAMINE -58 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
37459 746 13 3H-MEPYRAMINE -3019 25 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
62 746 13 3H-MEPYRAMINE -3019 25 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
CHEMBL8514 746 13 3H-MEPYRAMINE -3019 25 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
1621 2429 17 3H-MEPYRAMINE -4570 45 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2429 17 3H-MEPYRAMINE -4570 45 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2429 17 3H-MEPYRAMINE -4570 45 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2429 17 3H-MEPYRAMINE -4570 45 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2429 17 3H-MEPYRAMINE -4570 45 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
46882180 5841 0 UNDEFINED -5 6 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 482 7 2 7 3.7 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)c(S(N)(=O)=O)cc4o3)CC2)ccc1F None
CHEMBL1079180 5841 0 UNDEFINED -5 6 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 482 7 2 7 3.7 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)c(S(N)(=O)=O)cc4o3)CC2)ccc1F None
None 216341 0 3H-PYRILAMINE -1819 19 Guinea pig 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 451 8 2 4 3.2 CCNC(=O)N(CCCN(C)C)C(=O)C1CC2C(CC3=CNC4=CC=CC2=C34)N(C1)CC=C None
135398737 958 93 3H-pirilamine -4 89 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-pirilamine -4 89 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-pirilamine -4 89 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-pirilamine -4 89 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-pirilamine -4 89 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
100 3805 58 3H-PYRILAMINE -7 55 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3805 58 3H-PYRILAMINE -7 55 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3805 58 3H-PYRILAMINE -7 55 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3805 58 3H-PYRILAMINE -7 55 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3805 58 3H-PYRILAMINE -7 55 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
1224 1432 83 UNDEFINED -2 13 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
3100 1432 83 UNDEFINED -2 13 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
8980 1432 83 UNDEFINED -2 13 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
916 1432 83 UNDEFINED -2 13 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
CHEMBL657 1432 83 UNDEFINED -2 13 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
DB01075 1432 83 UNDEFINED -2 13 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
9906978 42711 2 UNDEFINED -28 12 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 None
CHEMBL150161 42711 2 UNDEFINED -28 12 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 None
37459 746 13 3H-MEPYRAMINE -1174 25 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
62 746 13 3H-MEPYRAMINE -1174 25 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
CHEMBL8514 746 13 3H-MEPYRAMINE -1174 25 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
1224 1432 83 3H-MEPYRAMINE -2 13 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
3100 1432 83 3H-MEPYRAMINE -2 13 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
8980 1432 83 3H-MEPYRAMINE -2 13 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
916 1432 83 3H-MEPYRAMINE -2 13 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
CHEMBL657 1432 83 3H-MEPYRAMINE -2 13 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
DB01075 1432 83 3H-MEPYRAMINE -2 13 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
2389 3331 118 3H-PYRILAMINE -46 67 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 118 3H-PYRILAMINE -46 67 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 118 3H-PYRILAMINE -46 67 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 118 3H-PYRILAMINE -46 67 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 118 3H-PYRILAMINE -46 67 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2865 4143 73 3H-PYRILAMINE -58 53 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4143 73 3H-PYRILAMINE -58 53 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4143 73 3H-PYRILAMINE -58 53 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4143 73 3H-PYRILAMINE -58 53 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4143 73 3H-PYRILAMINE -58 53 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
90475904 216022 0 3H-doxepin -7 6 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(C)CCC(C1=CC=C(C=C1)Cl)C2=CC=CC=N2 None
1971 2866 38 3H-MEPYRAMINE -1 30 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
2404 2866 38 3H-MEPYRAMINE -1 30 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
4543 2866 38 3H-MEPYRAMINE -1 30 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
CHEMBL445 2866 38 3H-MEPYRAMINE -1 30 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
DB00540 2866 38 3H-MEPYRAMINE -1 30 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
1204 1932 119 3H-Histamine -501 24 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1932 119 3H-Histamine -501 24 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1932 119 3H-Histamine -501 24 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1932 119 3H-Histamine -501 24 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1932 119 3H-Histamine -501 24 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1932 119 3H-Histamine -501 24 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
11957566 184 25 3H-MEPYRAMINE -812 9 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC None
1219 184 25 3H-MEPYRAMINE -812 9 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC None
3296 184 25 3H-MEPYRAMINE -812 9 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC None
950 184 25 3H-MEPYRAMINE -812 9 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC None
CHEMBL285755 184 25 3H-MEPYRAMINE -812 9 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC None
2142 3096 58 3H-MEPYRAMINE -263 36 Human 4.8 pKi = 4.8 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 3096 58 3H-MEPYRAMINE -263 36 Human 4.8 pKi = 4.8 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 3096 58 3H-MEPYRAMINE -263 36 Human 4.8 pKi = 4.8 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 3096 58 3H-MEPYRAMINE -263 36 Human 4.8 pKi = 4.8 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 3096 58 3H-MEPYRAMINE -263 36 Human 4.8 pKi = 4.8 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 3096 58 3H-MEPYRAMINE -263 36 Human 4.8 pKi = 4.8 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
1621 2429 17 3H-PYRILAMINE -4570 45 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2429 17 3H-PYRILAMINE -4570 45 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2429 17 3H-PYRILAMINE -4570 45 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2429 17 3H-PYRILAMINE -4570 45 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2429 17 3H-PYRILAMINE -4570 45 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
1209 1658 75 3H-PYRILAMINE -223 32 Guinea pig 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
203 1658 75 3H-PYRILAMINE -223 32 Guinea pig 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
3386 1658 75 3H-PYRILAMINE -223 32 Guinea pig 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL41 1658 75 3H-PYRILAMINE -223 32 Guinea pig 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
DB00472 1658 75 3H-PYRILAMINE -223 32 Guinea pig 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
2389 3331 118 3H-PYRILAMINE -346 67 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 118 3H-PYRILAMINE -346 67 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 118 3H-PYRILAMINE -346 67 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 118 3H-PYRILAMINE -346 67 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 118 3H-PYRILAMINE -346 67 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
45485535 197621 0 UNDEFINED - 1 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 399 7 1 2 5.6 Cc1ccc(CCCN2CCC(C(O)(c3ccccc3)c3ccccc3)CC2)cc1 None
CHEMBL570695 197621 0 UNDEFINED - 1 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 399 7 1 2 5.6 Cc1ccc(CCCN2CCC(C(O)(c3ccccc3)c3ccccc3)CC2)cc1 None
44395741 181581 0 UNDEFINED -10 10 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
CHEMBL476935 181581 0 UNDEFINED -10 10 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
CHEMBL558392 181581 0 UNDEFINED -10 10 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
1001 620 95 3H-MEPYRAMINE -3 2 Human 3.8 pKi = 3.8 Binding
NoneNone
PDSP KiDatabase 121 2 1 1 1.2 NCCc1ccccc1 None
2144 620 95 3H-MEPYRAMINE -3 2 Human 3.8 pKi = 3.8 Binding
NoneNone
PDSP KiDatabase 121 2 1 1 1.2 NCCc1ccccc1 None
CHEMBL610 620 95 3H-MEPYRAMINE -3 2 Human 3.8 pKi = 3.8 Binding
NoneNone
PDSP KiDatabase 121 2 1 1 1.2 NCCc1ccccc1 None
DB04325 620 95 3H-MEPYRAMINE -3 2 Human 3.8 pKi = 3.8 Binding
NoneNone
PDSP KiDatabase 121 2 1 1 1.2 NCCc1ccccc1 None
1427 2013 54 3H-MEPYRAMINE -1 27 Guinea pig 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
1427 2013 54 3H-doxepin -5 27 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
357 2013 54 3H-MEPYRAMINE -1 27 Guinea pig 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
357 2013 54 3H-doxepin -5 27 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
3696 2013 54 3H-MEPYRAMINE -1 27 Guinea pig 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
3696 2013 54 3H-doxepin -5 27 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
CHEMBL11 2013 54 3H-MEPYRAMINE -1 27 Guinea pig 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
CHEMBL11 2013 54 3H-doxepin -5 27 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
DB00458 2013 54 3H-MEPYRAMINE -1 27 Guinea pig 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
DB00458 2013 54 3H-doxepin -5 27 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
100 3805 58 3H-doxepin -7 55 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3805 58 3H-doxepin -7 55 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3805 58 3H-doxepin -7 55 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3805 58 3H-doxepin -7 55 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3805 58 3H-doxepin -7 55 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
44622869 197717 0 UNDEFINED - 1 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 371 5 1 2 5.1 Cc1ccc(CN2CCC(C(O)(c3ccccc3)c3ccccc3)CC2)cc1 None
CHEMBL571390 197717 0 UNDEFINED - 1 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 371 5 1 2 5.1 Cc1ccc(CN2CCC(C(O)(c3ccccc3)c3ccccc3)CC2)cc1 None
100 3805 58 UNDEFINED -7 55 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3805 58 UNDEFINED -7 55 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3805 58 UNDEFINED -7 55 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3805 58 UNDEFINED -7 55 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3805 58 UNDEFINED -7 55 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2389 3331 118 3H-PYRILAMINE -346 67 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 118 3H-PYRILAMINE -346 67 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 118 3H-PYRILAMINE -346 67 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 118 3H-PYRILAMINE -346 67 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 118 3H-PYRILAMINE -346 67 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
12057539 208041 42 3H-doxepin -676 20 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 208041 42 3H-doxepin -676 20 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 208041 42 3H-doxepin -676 20 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
186 1807 52 3H-PYRILAMINE -269 17 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
71781 1807 52 3H-PYRILAMINE -269 17 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
CHEMBL18972 1807 52 3H-PYRILAMINE -269 17 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
2105 3054 37 3H-PYRILAMINE -2754 33 Guinea pig 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 3054 37 3H-PYRILAMINE -2754 33 Guinea pig 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 3054 37 3H-PYRILAMINE -2754 33 Guinea pig 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 3054 37 3H-PYRILAMINE -2754 33 Guinea pig 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 3054 37 3H-PYRILAMINE -2754 33 Guinea pig 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
135398737 958 93 UNDEFINED -4 89 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 UNDEFINED -4 89 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 UNDEFINED -4 89 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 UNDEFINED -4 89 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 UNDEFINED -4 89 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1224 1432 83 3H-MEPYRAMINE -1 13 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
3100 1432 83 3H-MEPYRAMINE -1 13 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
8980 1432 83 3H-MEPYRAMINE -1 13 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
916 1432 83 3H-MEPYRAMINE -1 13 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
CHEMBL657 1432 83 3H-MEPYRAMINE -1 13 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
DB01075 1432 83 3H-MEPYRAMINE -1 13 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
1353 1911 93 3H-doxepin -489 83 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 3H-doxepin -489 83 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 3H-doxepin -489 83 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 3H-doxepin -489 83 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 3H-doxepin -489 83 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
None 216254 0 3H-MEPYRAMINE -1412 19 Guinea pig 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 416 9 3 4 2.8 C1=CC(=CC=C1CCNC(N)SCCCC2=CN=CN2)I None
None 215992 0 3H-PYRILAMINE -1 11 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 522 10 0 3 6.2 C1CN(CCN1CCCC2=CC=CC=C2)CCOC(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F.Cl.Cl None
2389 3331 118 3H-PYRILAMINE -46 67 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 118 3H-PYRILAMINE -46 67 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 118 3H-PYRILAMINE -46 67 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 118 3H-PYRILAMINE -46 67 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 118 3H-PYRILAMINE -46 67 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2274 3173 58 UNDEFINED -3 31 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 3173 58 UNDEFINED -3 31 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 3173 58 UNDEFINED -3 31 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 3173 58 UNDEFINED -3 31 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 3173 58 UNDEFINED -3 31 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
1353 1911 93 3H-PYRILAMINE -213 83 Guinea pig 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 1911 93 3H-PYRILAMINE -489 83 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 3H-PYRILAMINE -213 83 Guinea pig 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 3H-PYRILAMINE -489 83 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 3H-PYRILAMINE -213 83 Guinea pig 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 3H-PYRILAMINE -489 83 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 3H-PYRILAMINE -213 83 Guinea pig 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 3H-PYRILAMINE -489 83 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 3H-PYRILAMINE -213 83 Guinea pig 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 3H-PYRILAMINE -489 83 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
12057539 208041 42 3H-MEPYRAMINE -3388 20 Guinea pig 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 208041 42 3H-MEPYRAMINE -3388 20 Guinea pig 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 208041 42 3H-MEPYRAMINE -3388 20 Guinea pig 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
214 3860 58 3H-MEPYRAMINE -218 30 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 3860 58 3H-MEPYRAMINE -218 30 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 3860 58 3H-MEPYRAMINE -218 30 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 3860 58 3H-MEPYRAMINE -218 30 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 3860 58 3H-MEPYRAMINE -218 30 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 3860 58 3H-MEPYRAMINE -218 30 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
11653679 181191 1 UNDEFINED -28 11 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 374 6 0 3 4.7 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
CHEMBL476108 181191 1 UNDEFINED -28 11 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 374 6 0 3 4.7 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
1353 1911 93 UNDEFINED -489 83 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 UNDEFINED -489 83 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 UNDEFINED -489 83 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 UNDEFINED -489 83 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 UNDEFINED -489 83 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1212 1662 50 3H-MEPYRAMINE -38 65 Guinea pig 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1662 50 3H-MEPYRAMINE -38 65 Guinea pig 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1662 50 3H-MEPYRAMINE -38 65 Guinea pig 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1662 50 3H-MEPYRAMINE -38 65 Guinea pig 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1662 50 3H-MEPYRAMINE -38 65 Guinea pig 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2274 3173 58 3H-doxepin -3 31 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 3173 58 3H-doxepin -3 31 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 3173 58 3H-doxepin -3 31 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 3173 58 3H-doxepin -3 31 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 3173 58 3H-doxepin -3 31 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2337 3256 77 3H-PYRILAMINE -1 62 Guinea pig 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2337 3256 77 3H-PYRILAMINE 1 62 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 77 3H-PYRILAMINE -1 62 Guinea pig 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 77 3H-PYRILAMINE 1 62 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 77 3H-PYRILAMINE -1 62 Guinea pig 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 77 3H-PYRILAMINE 1 62 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 77 3H-PYRILAMINE -1 62 Guinea pig 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 77 3H-PYRILAMINE 1 62 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 77 3H-PYRILAMINE -1 62 Guinea pig 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 77 3H-PYRILAMINE 1 62 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2389 3331 118 UNDEFINED -46 67 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 118 UNDEFINED -46 67 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 118 UNDEFINED -46 67 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 118 UNDEFINED -46 67 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 118 UNDEFINED -46 67 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
100 3805 58 3H-PYRILAMINE -7 55 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3805 58 3H-PYRILAMINE -7 55 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3805 58 3H-PYRILAMINE -7 55 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3805 58 3H-PYRILAMINE -7 55 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3805 58 3H-PYRILAMINE -7 55 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
1204 1932 119 Functional -501 24 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1932 119 Functional -501 24 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1932 119 Functional -501 24 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1932 119 Functional -501 24 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1932 119 Functional -501 24 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1932 119 Functional -501 24 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
None 217133 0 UNDEFINED -58 11 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 116 4 0 2 1.4 CCCCN(C)N=O None
1353 1911 93 3H-doxepin -489 83 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 3H-doxepin -489 83 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 3H-doxepin -489 83 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 3H-doxepin -489 83 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 3H-doxepin -489 83 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
2771 195017 74 3H-PYRILAMINE -2 27 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL1200781 195017 74 3H-PYRILAMINE -2 27 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL549 195017 74 3H-PYRILAMINE -2 27 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
2771 195017 74 3H-PYRILAMINE -9 27 Guinea pig 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL1200781 195017 74 3H-PYRILAMINE -9 27 Guinea pig 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL549 195017 74 3H-PYRILAMINE -9 27 Guinea pig 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
46882181 5681 0 UNDEFINED 1 5 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 536 10 2 8 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(NS(=O)(=O)c5ccccc5)ccc4o3)CC2)ccc1OC None
CHEMBL1077908 5681 0 UNDEFINED 1 5 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 536 10 2 8 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(NS(=O)(=O)c5ccccc5)ccc4o3)CC2)ccc1OC None
135398737 958 93 3H-Histamine 2 89 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-Histamine 2 89 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-Histamine 2 89 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-Histamine 2 89 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-Histamine 2 89 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 958 93 3H-PYRILAMINE 2 89 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-PYRILAMINE 2 89 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-PYRILAMINE 2 89 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-PYRILAMINE 2 89 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-PYRILAMINE 2 89 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1400 1957 70 3H-MEPYRAMINE 2 3 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
3658 1957 70 3H-MEPYRAMINE 2 3 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
7199 1957 70 3H-MEPYRAMINE 2 3 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
91513 1957 70 3H-MEPYRAMINE 2 3 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
CHEMBL896 1957 70 3H-MEPYRAMINE 2 3 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
DB00557 1957 70 3H-MEPYRAMINE 2 3 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
1427 2013 54 3H-PYRILAMINE -1 27 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
357 2013 54 3H-PYRILAMINE -1 27 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
3696 2013 54 3H-PYRILAMINE -1 27 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
CHEMBL11 2013 54 3H-PYRILAMINE -1 27 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
DB00458 2013 54 3H-PYRILAMINE -1 27 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
1227 2489 43 3H-MEPYRAMINE -2 12 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
2331 2489 43 3H-MEPYRAMINE -2 12 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
3957 2489 43 3H-MEPYRAMINE -2 12 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
4992 2489 43 3H-MEPYRAMINE -2 12 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
CHEMBL511 2489 43 3H-MEPYRAMINE -2 12 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
DB06691 2489 43 3H-MEPYRAMINE -2 12 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
135398745 2914 112 3H-PYRILAMINE 1 65 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 3H-PYRILAMINE 1 65 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 3H-PYRILAMINE 1 65 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 3H-PYRILAMINE 1 65 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
2284 3182 33 3H-doxepin 1 29 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
2284 3182 33 UNDEFINED 1 29 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
4926 3182 33 3H-doxepin 1 29 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
4926 3182 33 UNDEFINED 1 29 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
7281 3182 33 3H-doxepin 1 29 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
7281 3182 33 UNDEFINED 1 29 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
CHEMBL564 3182 33 3H-doxepin 1 29 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
CHEMBL564 3182 33 UNDEFINED 1 29 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
DB00420 3182 33 3H-doxepin 1 29 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
DB00420 3182 33 UNDEFINED 1 29 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
2600 3779 74 3H-MEPYRAMINE 1 13 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
2608 3779 74 3H-MEPYRAMINE 1 13 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
5405 3779 74 3H-MEPYRAMINE 1 13 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
CHEMBL17157 3779 74 3H-MEPYRAMINE 1 13 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
DB00342 3779 74 3H-MEPYRAMINE 1 13 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
46780481 107531 20 3H-PYRILAMINE -11 53 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107531 20 3H-PYRILAMINE -11 53 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107531 20 3H-PYRILAMINE -11 53 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107531 20 3H-PYRILAMINE -11 53 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
135398737 958 93 3H-trans-H2-PAT,(-) -2 89 Guinea pig 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-trans-H2-PAT,(-) -2 89 Guinea pig 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-trans-H2-PAT,(-) -2 89 Guinea pig 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-trans-H2-PAT,(-) -2 89 Guinea pig 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-trans-H2-PAT,(-) -2 89 Guinea pig 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 958 93 3H-PYRILAMINE -2 89 Guinea pig 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-PYRILAMINE -2 89 Guinea pig 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-PYRILAMINE -2 89 Guinea pig 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-PYRILAMINE -2 89 Guinea pig 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-PYRILAMINE -2 89 Guinea pig 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2337 3256 77 3H-PYRILAMINE 1 62 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 77 3H-PYRILAMINE 1 62 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 77 3H-PYRILAMINE 1 62 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 77 3H-PYRILAMINE 1 62 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 77 3H-PYRILAMINE 1 62 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2564 206184 51 3H-MEPYRAMINE 2 3 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 290 6 0 3 3.4 CN(C)CCOC(c1ccc(Cl)cc1)c1ccccn1 None
CHEMBL864 206184 51 3H-MEPYRAMINE 2 3 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 290 6 0 3 3.4 CN(C)CCOC(c1ccc(Cl)cc1)c1ccccn1 None
None 216176 0 3H-MEPYRAMINE - 1 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 296 2 0 3 4.2 CN1CCC(C1)CN2C3=CC=CC=C3SC4=CC=CC=C42 None
135398737 958 93 UNDEFINED 2 89 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 UNDEFINED 2 89 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 UNDEFINED 2 89 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 UNDEFINED 2 89 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 UNDEFINED 2 89 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2284 3182 33 3H-MEPYRAMINE -1 29 Guinea pig 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
4926 3182 33 3H-MEPYRAMINE -1 29 Guinea pig 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
7281 3182 33 3H-MEPYRAMINE -1 29 Guinea pig 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
CHEMBL564 3182 33 3H-MEPYRAMINE -1 29 Guinea pig 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
DB00420 3182 33 3H-MEPYRAMINE -1 29 Guinea pig 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
1227 2489 43 3H-PYRILAMINE -2 12 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
2331 2489 43 3H-PYRILAMINE -2 12 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
3957 2489 43 3H-PYRILAMINE -2 12 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
4992 2489 43 3H-PYRILAMINE -2 12 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
CHEMBL511 2489 43 3H-PYRILAMINE -2 12 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
DB06691 2489 43 3H-PYRILAMINE -2 12 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
1210 918 51 3H-MEPYRAMINE -20 21 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
1213 918 51 3H-MEPYRAMINE -20 21 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
2725 918 51 3H-MEPYRAMINE -20 21 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
33036 918 51 3H-MEPYRAMINE -20 21 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
4411 918 51 3H-MEPYRAMINE -20 21 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
616 918 51 3H-MEPYRAMINE -20 21 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
6976 918 51 3H-MEPYRAMINE -20 21 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
716121 918 51 3H-MEPYRAMINE -20 21 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1201353 918 51 3H-MEPYRAMINE -20 21 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1554789 918 51 3H-MEPYRAMINE -20 21 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL505 918 51 3H-MEPYRAMINE -20 21 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
DB01114 918 51 3H-MEPYRAMINE -20 21 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
DB13679 918 51 3H-MEPYRAMINE -20 21 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
16667681 216153 0 3H-MEPYRAMINE 4 3 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 390 7 1 5 3.5 CN(C)CCCC1=CC=CC=N1.C1=CC(=CC=C1OC(=O)C=CC(=O)O)Cl None
2286 3183 51 3H-MEPYRAMINE -2 30 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
4927 3183 51 3H-MEPYRAMINE -2 30 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
7282 3183 51 3H-MEPYRAMINE -2 30 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
CHEMBL643 3183 51 3H-MEPYRAMINE -2 30 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
DB01069 3183 51 3H-MEPYRAMINE -2 30 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
2389 3331 118 3H-PYRILAMINE -52 67 Guinea pig 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 118 3H-PYRILAMINE -52 67 Guinea pig 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 118 3H-PYRILAMINE -52 67 Guinea pig 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 118 3H-PYRILAMINE -52 67 Guinea pig 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 118 3H-PYRILAMINE -52 67 Guinea pig 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
90475904 216022 0 3H-trans-H2-PAT,(-) -7 6 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(C)CCC(C1=CC=C(C=C1)Cl)C2=CC=CC=N2 None
135398745 2914 112 3H-PYRILAMINE 1 65 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 3H-PYRILAMINE 1 65 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 3H-PYRILAMINE 1 65 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 3H-PYRILAMINE 1 65 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398737 958 93 UNDEFINED 2 89 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 UNDEFINED 2 89 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 UNDEFINED 2 89 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 UNDEFINED 2 89 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 UNDEFINED 2 89 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 958 93 3H-doxepin 2 89 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-doxepin 2 89 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-doxepin 2 89 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-doxepin 2 89 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-doxepin 2 89 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1613 2348 53 3H-PYRILAMINE -3 44 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2348 53 3H-PYRILAMINE -3 44 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2348 53 3H-PYRILAMINE -3 44 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2348 53 3H-PYRILAMINE -3 44 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2348 53 3H-PYRILAMINE -3 44 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
135398745 2914 112 UNDEFINED 1 65 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 UNDEFINED 1 65 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 UNDEFINED 1 65 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 UNDEFINED 1 65 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398737 958 93 3H-pirilamine -4 89 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-pirilamine -4 89 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-pirilamine -4 89 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-pirilamine -4 89 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-pirilamine -4 89 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2286 3183 51 3H-MEPYRAMINE -1 30 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
4927 3183 51 3H-MEPYRAMINE -1 30 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
7282 3183 51 3H-MEPYRAMINE -1 30 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
CHEMBL643 3183 51 3H-MEPYRAMINE -1 30 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
DB01069 3183 51 3H-MEPYRAMINE -1 30 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
100 3805 58 3H-MEPYRAMINE -23 55 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3805 58 3H-MEPYRAMINE -23 55 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3805 58 3H-MEPYRAMINE -23 55 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3805 58 3H-MEPYRAMINE -23 55 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3805 58 3H-MEPYRAMINE -23 55 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
1228 3866 34 3H-MEPYRAMINE -5 4 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
2763 3866 34 3H-MEPYRAMINE -5 4 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
5282443 3866 34 3H-MEPYRAMINE -5 4 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
CHEMBL855 3866 34 3H-MEPYRAMINE -5 4 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
DB00427 3866 34 3H-MEPYRAMINE -5 4 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
11291 98796 25 3H-MEPYRAMINE -4 2 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 261 1 0 1 3.9 CN1CCC2=C(C1)C(c1ccccc1)c1ccccc12 None
CHEMBL278398 98796 25 3H-MEPYRAMINE -4 2 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 261 1 0 1 3.9 CN1CCC2=C(C1)C(c1ccccc1)c1ccccc12 None
45485473 197335 0 UNDEFINED - 1 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 457 9 1 4 5.4 COC(=O)c1ccc(CCCCN2CCC(C(O)(c3ccccc3)c3ccccc3)CC2)cc1 None
CHEMBL568892 197335 0 UNDEFINED - 1 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 457 9 1 4 5.4 COC(=O)c1ccc(CCCCN2CCC(C(O)(c3ccccc3)c3ccccc3)CC2)cc1 None
1212 1662 50 UNDEFINED -41 65 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1662 50 UNDEFINED -41 65 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1662 50 UNDEFINED -41 65 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1662 50 UNDEFINED -41 65 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1662 50 UNDEFINED -41 65 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2995 204405 53 3H-MEPYRAMINE -14 23 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 204405 53 3H-MEPYRAMINE -14 23 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 204405 53 3H-MEPYRAMINE -14 23 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
1204 1932 119 3H-MEPYRAMINE -501 24 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1932 119 3H-MEPYRAMINE -501 24 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1932 119 3H-MEPYRAMINE -501 24 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1932 119 3H-MEPYRAMINE -501 24 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1932 119 3H-MEPYRAMINE -501 24 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1932 119 3H-MEPYRAMINE -501 24 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1599 2341 50 3H-MEPYRAMINE -2398 16 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
3955 2341 50 3H-MEPYRAMINE -2398 16 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
7215 2341 50 3H-MEPYRAMINE -2398 16 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
CHEMBL841 2341 50 3H-MEPYRAMINE -2398 16 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
DB00836 2341 50 3H-MEPYRAMINE -2398 16 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
12057539 208041 42 3H-MEPYRAMINE -3715 20 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 208041 42 3H-MEPYRAMINE -3715 20 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 208041 42 3H-MEPYRAMINE -3715 20 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
10456093 197509 0 UNDEFINED - 1 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 443 9 2 3 5.4 O=C(O)c1ccc(CCCCN2CCC(C(O)(c3ccccc3)c3ccccc3)CC2)cc1 None
CHEMBL570033 197509 0 UNDEFINED - 1 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 443 9 2 3 5.4 O=C(O)c1ccc(CCCCN2CCC(C(O)(c3ccccc3)c3ccccc3)CC2)cc1 None
44591134 176200 0 UNDEFINED -169 6 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 535 11 0 5 7.7 CN(CCCN1c2ccccc2Sc2ccc(Cl)cc21)Cc1ccc(OCCCN2CCCCC2)cc1 None
CHEMBL459373 176200 0 UNDEFINED -169 6 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 535 11 0 5 7.7 CN(CCCN1c2ccccc2Sc2ccc(Cl)cc21)Cc1ccc(OCCCN2CCCCC2)cc1 None
1204 1932 119 3H-MEPYRAMINE -501 24 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1932 119 3H-MEPYRAMINE -501 24 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1932 119 3H-MEPYRAMINE -501 24 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1932 119 3H-MEPYRAMINE -501 24 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1932 119 3H-MEPYRAMINE -501 24 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1932 119 3H-MEPYRAMINE -501 24 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1212 1662 50 3H-PYRILAMINE -41 65 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1212 1662 50 3H-doxepin -41 65 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1662 50 3H-PYRILAMINE -41 65 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1662 50 3H-doxepin -41 65 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1662 50 3H-PYRILAMINE -41 65 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1662 50 3H-doxepin -41 65 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1662 50 3H-PYRILAMINE -41 65 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1662 50 3H-doxepin -41 65 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1662 50 3H-PYRILAMINE -41 65 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1662 50 3H-doxepin -41 65 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2337 3256 77 UNDEFINED -1 62 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 77 UNDEFINED -1 62 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 77 UNDEFINED -1 62 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 77 UNDEFINED -1 62 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 77 UNDEFINED -1 62 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
37459 746 13 3H-MEPYRAMINE -1174 25 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
62 746 13 3H-MEPYRAMINE -1174 25 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
CHEMBL8514 746 13 3H-MEPYRAMINE -1174 25 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
16667681 216153 0 3H-trans-H2-PAT,(-) 4 3 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 390 7 1 5 3.5 CN(C)CCCC1=CC=CC=N1.C1=CC(=CC=C1OC(=O)C=CC(=O)O)Cl None
1830 2590 44 3H-PYRILAMINE -125 28 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 2590 44 3H-PYRILAMINE -125 28 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 2590 44 3H-PYRILAMINE -125 28 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 2590 44 3H-PYRILAMINE -125 28 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 2590 44 3H-PYRILAMINE -125 28 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
446220 133521 14 3H-PYRILAMINE -19 45 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
CHEMBL370805 133521 14 3H-PYRILAMINE -19 45 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
1615 167791 24 3H-PYRILAMINE -5 44 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
CHEMBL43048 167791 24 3H-PYRILAMINE -5 44 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
1353 1911 93 3H-MEPYRAMINE -489 83 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 3H-MEPYRAMINE -489 83 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 3H-MEPYRAMINE -489 83 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 3H-MEPYRAMINE -489 83 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 3H-MEPYRAMINE -489 83 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
2284 3182 33 3H-MEPYRAMINE -10 29 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
4926 3182 33 3H-MEPYRAMINE -10 29 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
7281 3182 33 3H-MEPYRAMINE -10 29 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
CHEMBL564 3182 33 3H-MEPYRAMINE -10 29 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
DB00420 3182 33 3H-MEPYRAMINE -10 29 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
100 3805 58 3H-MEPYRAMINE -7 55 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3805 58 3H-MEPYRAMINE -7 55 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3805 58 3H-MEPYRAMINE -7 55 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3805 58 3H-MEPYRAMINE -7 55 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3805 58 3H-MEPYRAMINE -7 55 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
213 3853 55 3H-PYRILAMINE -8 44 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 3853 55 3H-PYRILAMINE -8 44 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 3853 55 3H-PYRILAMINE -8 44 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 3853 55 3H-PYRILAMINE -8 44 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 3853 55 3H-PYRILAMINE -8 44 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
1204 1932 119 3H-MEPYRAMINE -501 24 Human 4.7 pKi = 4.7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1932 119 3H-MEPYRAMINE -501 24 Human 4.7 pKi = 4.7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1932 119 3H-MEPYRAMINE -501 24 Human 4.7 pKi = 4.7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1932 119 3H-MEPYRAMINE -501 24 Human 4.7 pKi = 4.7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1932 119 3H-MEPYRAMINE -501 24 Human 4.7 pKi = 4.7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1932 119 3H-MEPYRAMINE -501 24 Human 4.7 pKi = 4.7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
135398737 958 93 3H-PYRILAMINE -2 89 Guinea pig 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 958 93 3H-MEPYRAMINE -4 89 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-PYRILAMINE -2 89 Guinea pig 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-MEPYRAMINE -4 89 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-PYRILAMINE -2 89 Guinea pig 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-MEPYRAMINE -4 89 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-PYRILAMINE -2 89 Guinea pig 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-MEPYRAMINE -4 89 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-PYRILAMINE -2 89 Guinea pig 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-MEPYRAMINE -4 89 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
202 1508 77 3H-PYRILAMINE -1 30 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
60835 1508 77 3H-PYRILAMINE -1 30 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
972 1508 77 3H-PYRILAMINE -1 30 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
CHEMBL1175 1508 77 3H-PYRILAMINE -1 30 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
DB00476 1508 77 3H-PYRILAMINE -1 30 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
135398737 958 93 3H-PYRILAMINE -4 89 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-PYRILAMINE -4 89 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-PYRILAMINE -4 89 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-PYRILAMINE -4 89 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-PYRILAMINE -4 89 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2181 3128 46 3H-PYRILAMINE -269 35 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
4830 3128 46 3H-PYRILAMINE -269 35 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
92 3128 46 3H-PYRILAMINE -269 35 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
CHEMBL440294 3128 46 3H-PYRILAMINE -269 35 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
DB09286 3128 46 3H-PYRILAMINE -269 35 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
16362 3125 71 3H-PYRILAMINE -489 30 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 3125 71 3H-PYRILAMINE -489 30 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 3125 71 3H-PYRILAMINE -489 30 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 3125 71 3H-PYRILAMINE -489 30 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 3125 71 3H-PYRILAMINE -489 30 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
242 470 124 3H-PYRILAMINE -22 51 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 470 124 3H-PYRILAMINE -22 51 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 470 124 3H-PYRILAMINE -22 51 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 470 124 3H-PYRILAMINE -22 51 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 470 124 3H-PYRILAMINE -22 51 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
4034 55822 55 3H-MEPYRAMINE - 1 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 390 5 0 2 5.6 Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1 None
CHEMBL1623 55822 55 3H-MEPYRAMINE - 1 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 390 5 0 2 5.6 Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1 None
2995 204405 53 3H-MEPYRAMINE -12 23 Guinea pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
2995 204405 53 3H-MEPYRAMINE -42 23 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 204405 53 3H-MEPYRAMINE -12 23 Guinea pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 204405 53 3H-MEPYRAMINE -42 23 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 204405 53 3H-MEPYRAMINE -12 23 Guinea pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 204405 53 3H-MEPYRAMINE -42 23 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
1353 1911 93 3H-MEPYRAMINE -489 83 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 3H-MEPYRAMINE -489 83 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 3H-MEPYRAMINE -489 83 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 3H-MEPYRAMINE -489 83 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 3H-MEPYRAMINE -489 83 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1242 3613 27 3H-MEPYRAMINE -147 18 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
935 3613 27 3H-MEPYRAMINE -147 18 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
CHEMBL286080 3613 27 3H-MEPYRAMINE -147 18 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
9906978 42711 2 UNDEFINED -28 12 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 None
CHEMBL150161 42711 2 UNDEFINED -28 12 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 None
2726 919 68 3H-MEPYRAMINE -17 72 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 68 3H-MEPYRAMINE -17 72 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 68 3H-MEPYRAMINE -17 72 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 68 3H-MEPYRAMINE -17 72 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 68 3H-MEPYRAMINE -17 72 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1427 2013 54 3H-MEPYRAMINE -1 27 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
357 2013 54 3H-MEPYRAMINE -1 27 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
3696 2013 54 3H-MEPYRAMINE -1 27 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
CHEMBL11 2013 54 3H-MEPYRAMINE -1 27 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
DB00458 2013 54 3H-MEPYRAMINE -1 27 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
135398745 2914 112 3H-PYRILAMINE -1 65 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 3H-PYRILAMINE -1 65 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 3H-PYRILAMINE -1 65 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 3H-PYRILAMINE -1 65 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
None 216924 0 UNDEFINED - 1 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 333 5 1 4 3.5 COC1=C(C=CC(=C1)Cl)OC(C2CNCCO2)C3=CC=CC=C3 None
1353 1911 93 3H-PYRILAMINE -489 83 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 3H-PYRILAMINE -489 83 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 3H-PYRILAMINE -489 83 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 3H-PYRILAMINE -489 83 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 3H-PYRILAMINE -489 83 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
54477 84653 36 UNDEFINED -70 23 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
CHEMBL22242 84653 36 UNDEFINED -70 23 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
11848679 89244 0 UNDEFINED -204 6 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 489 9 3 9 2.9 CCOc1cc(CN2CCC(Nc3nc4cc(S(N)(=O)=O)ccc4o3)CC2)cc(OCC)c1N None
CHEMBL236788 89244 0 UNDEFINED -204 6 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 489 9 3 9 2.9 CCOc1cc(CN2CCC(Nc3nc4cc(S(N)(=O)=O)ccc4o3)CC2)cc(OCC)c1N None
24740863 89158 0 UNDEFINED -3 6 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 385 6 1 5 5.0 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1Cl None
CHEMBL236610 89158 0 UNDEFINED -3 6 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 385 6 1 5 5.0 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1Cl None
1170 1633 75 UNDEFINED - 1 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C None
3348 1633 75 UNDEFINED - 1 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C None
4819 1633 75 UNDEFINED - 1 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C None
74685737 1633 75 UNDEFINED - 1 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C None
CHEMBL914 1633 75 UNDEFINED - 1 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C None
DB00950 1633 75 UNDEFINED - 1 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C None
2389 3331 118 3H-PYRILAMINE -46 67 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 118 3H-PYRILAMINE -46 67 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 118 3H-PYRILAMINE -46 67 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 118 3H-PYRILAMINE -46 67 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 118 3H-PYRILAMINE -46 67 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
11954259 215979 0 3H-MEPYRAMINE -89 43 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
2470 3653 50 3H-MEPYRAMINE -81283 59 Guinea pig 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3653 50 3H-MEPYRAMINE -81283 59 Guinea pig 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3653 50 3H-MEPYRAMINE -81283 59 Guinea pig 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3653 50 3H-MEPYRAMINE -81283 59 Guinea pig 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3653 50 3H-MEPYRAMINE -81283 59 Guinea pig 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
4528 98126 80 3H-doxepin -1 10 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 238 1 1 2 2.8 CN1Cc2c(N)cccc2C(c2ccccc2)C1 None
CHEMBL273575 98126 80 3H-doxepin -1 10 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 238 1 1 2 2.8 CN1Cc2c(N)cccc2C(c2ccccc2)C1 None
1204 1932 119 3H-MEPYRAMINE -46 24 Guinea pig 4.6 pKi = 4.6 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1932 119 3H-MEPYRAMINE -46 24 Guinea pig 4.6 pKi = 4.6 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1932 119 3H-MEPYRAMINE -46 24 Guinea pig 4.6 pKi = 4.6 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1932 119 3H-MEPYRAMINE -46 24 Guinea pig 4.6 pKi = 4.6 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1932 119 3H-MEPYRAMINE -46 24 Guinea pig 4.6 pKi = 4.6 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1932 119 3H-MEPYRAMINE -46 24 Guinea pig 4.6 pKi = 4.6 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
2470 3653 50 3H-MEPYRAMINE -4570 59 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3653 50 3H-MEPYRAMINE -4570 59 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3653 50 3H-MEPYRAMINE -4570 59 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3653 50 3H-MEPYRAMINE -4570 59 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3653 50 3H-MEPYRAMINE -4570 59 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
1223 953 41 3H-MEPYRAMINE -14125 11 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N None
2790 953 41 3H-MEPYRAMINE -14125 11 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N None
CHEMBL14690 953 41 3H-MEPYRAMINE -14125 11 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N None
None 216100 0 3H-PYRILAMINE -3 3 Guinea pig 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 485 10 1 8 3.0 CC(C1=NN(C(=O)N1CCOC2=CC=CC=C2)CCCN3CCN(CC3)C4=CC=C(C=C4)Cl)O None
2771 195017 74 3H-PYRILAMINE -9 27 Guinea pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
2771 195017 74 3H-PYRILAMINE -2 27 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL1200781 195017 74 3H-PYRILAMINE -9 27 Guinea pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL1200781 195017 74 3H-PYRILAMINE -2 27 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL549 195017 74 3H-PYRILAMINE -9 27 Guinea pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL549 195017 74 3H-PYRILAMINE -2 27 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
242 470 124 3H-PYRILAMINE -22 51 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 470 124 3H-PYRILAMINE -22 51 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 470 124 3H-PYRILAMINE -22 51 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 470 124 3H-PYRILAMINE -22 51 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 470 124 3H-PYRILAMINE -22 51 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
213 3853 55 3H-PYRILAMINE -2 44 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 3853 55 3H-PYRILAMINE -2 44 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 3853 55 3H-PYRILAMINE -2 44 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 3853 55 3H-PYRILAMINE -2 44 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 3853 55 3H-PYRILAMINE -2 44 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
444 206666 53 3H-PYRILAMINE -6 18 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 239 3 1 2 3.3 CC(NC(C)(C)C)C(=O)c1cccc(Cl)c1 None
CHEMBL894 206666 53 3H-PYRILAMINE -6 18 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 239 3 1 2 3.3 CC(NC(C)(C)C)C(=O)c1cccc(Cl)c1 None
242 470 124 3H-PYRILAMINE -22 51 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 470 124 3H-PYRILAMINE -22 51 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 470 124 3H-PYRILAMINE -22 51 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 470 124 3H-PYRILAMINE -22 51 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 470 124 3H-PYRILAMINE -22 51 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
1353 1911 93 3H-PYRILAMINE -602 83 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 3H-PYRILAMINE -602 83 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 3H-PYRILAMINE -602 83 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 3H-PYRILAMINE -602 83 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 3H-PYRILAMINE -602 83 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
None 217161 0 UNDEFINED -190 6 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 532 10 0 4 8.0 CN(CCC=C1C2=CC=CC=C2SC3=C1C=C(C=C3)Cl)CC4=CC=C(C=C4)OCCCN5CCCCC5 None
2402 3370 62 3H-PYRILAMINE -194 24 Guinea pig 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
5095 3370 62 3H-PYRILAMINE -194 24 Guinea pig 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
7295 3370 62 3H-PYRILAMINE -194 24 Guinea pig 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
CHEMBL589 3370 62 3H-PYRILAMINE -194 24 Guinea pig 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
DB00268 3370 62 3H-PYRILAMINE -194 24 Guinea pig 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
1210 918 51 3H-MEPYRAMINE -20 21 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
1213 918 51 3H-MEPYRAMINE -20 21 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
2725 918 51 3H-MEPYRAMINE -20 21 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
33036 918 51 3H-MEPYRAMINE -20 21 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
4411 918 51 3H-MEPYRAMINE -20 21 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
616 918 51 3H-MEPYRAMINE -20 21 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
6976 918 51 3H-MEPYRAMINE -20 21 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
716121 918 51 3H-MEPYRAMINE -20 21 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1201353 918 51 3H-MEPYRAMINE -20 21 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1554789 918 51 3H-MEPYRAMINE -20 21 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL505 918 51 3H-MEPYRAMINE -20 21 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
DB01114 918 51 3H-MEPYRAMINE -20 21 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
DB13679 918 51 3H-MEPYRAMINE -20 21 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
2726 919 68 3H-doxepin -2 72 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 68 3H-doxepin -2 72 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 68 3H-doxepin -2 72 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 68 3H-doxepin -2 72 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 68 3H-doxepin -2 72 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1228 3866 34 3H-MEPYRAMINE -5 4 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
2763 3866 34 3H-MEPYRAMINE -5 4 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
5282443 3866 34 3H-MEPYRAMINE -5 4 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
CHEMBL855 3866 34 3H-MEPYRAMINE -5 4 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
DB00427 3866 34 3H-MEPYRAMINE -5 4 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
135398737 958 93 3H-PYRILAMINE 2 89 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-PYRILAMINE 2 89 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-PYRILAMINE 2 89 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-PYRILAMINE 2 89 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-PYRILAMINE 2 89 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
277 1301 62 3H-MEPYRAMINE -3 50 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1301 62 3H-MEPYRAMINE -3 50 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1301 62 3H-MEPYRAMINE -3 50 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1301 62 3H-MEPYRAMINE -3 50 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1301 62 3H-MEPYRAMINE -3 50 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
3103 41658 49 3H-MEPYRAMINE 1 4 Guinea pig 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 281 4 0 2 3.9 CN1CCC(OC(c2ccccc2)c2ccccc2)CC1 None
CHEMBL1492 41658 49 3H-MEPYRAMINE 1 4 Guinea pig 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 281 4 0 2 3.9 CN1CCC(OC(c2ccccc2)c2ccccc2)CC1 None
1222 881 0 3H-MEPYRAMINE -1 2 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
2678 881 0 3H-MEPYRAMINE -1 2 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
581 881 0 3H-MEPYRAMINE -1 2 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
CHEMBL1000 881 0 3H-MEPYRAMINE -1 2 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
DB00341 881 0 3H-MEPYRAMINE -1 2 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
2600 3779 74 3H-MEPYRAMINE 1 13 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
2608 3779 74 3H-MEPYRAMINE 1 13 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
5405 3779 74 3H-MEPYRAMINE 1 13 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
CHEMBL17157 3779 74 3H-MEPYRAMINE 1 13 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
DB00342 3779 74 3H-MEPYRAMINE 1 13 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
1227 2489 43 3H-MEPYRAMINE -3 12 Mouse 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
2331 2489 43 3H-MEPYRAMINE -3 12 Mouse 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
3957 2489 43 3H-MEPYRAMINE -3 12 Mouse 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
4992 2489 43 3H-MEPYRAMINE -3 12 Mouse 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
CHEMBL511 2489 43 3H-MEPYRAMINE -3 12 Mouse 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
DB06691 2489 43 3H-MEPYRAMINE -3 12 Mouse 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
2286 3183 51 3H-MEPYRAMINE -1 30 Guinea pig 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
4927 3183 51 3H-MEPYRAMINE -1 30 Guinea pig 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
7282 3183 51 3H-MEPYRAMINE -1 30 Guinea pig 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
CHEMBL643 3183 51 3H-MEPYRAMINE -1 30 Guinea pig 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
DB01069 3183 51 3H-MEPYRAMINE -1 30 Guinea pig 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
3103 41658 49 3H-MEPYRAMINE -1 4 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 281 4 0 2 3.9 CN1CCC(OC(c2ccccc2)c2ccccc2)CC1 None
CHEMBL1492 41658 49 3H-MEPYRAMINE -1 4 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 281 4 0 2 3.9 CN1CCC(OC(c2ccccc2)c2ccccc2)CC1 None
55482 216150 0 3H-MEPYRAMINE - 1 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 441 8 2 5 4.0 CC1=NC=C(C=C1)CC2=CN=C(NC2=O)NCCCCC3=NC=C(C=C3C)Br None
103 4153 61 3H-PYRILAMINE -1 53 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4153 61 3H-PYRILAMINE -1 53 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4153 61 3H-PYRILAMINE -1 53 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4153 61 3H-PYRILAMINE -1 53 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4153 61 3H-PYRILAMINE -1 53 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
135409468 2035 69 3H-PYRILAMINE -1 39 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
333 2035 69 3H-PYRILAMINE -1 39 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
CHEMBL845 2035 69 3H-PYRILAMINE -1 39 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
103 4153 61 3H-PYRILAMINE -2 53 Guinea pig 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4153 61 3H-PYRILAMINE -2 53 Guinea pig 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4153 61 3H-PYRILAMINE -2 53 Guinea pig 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4153 61 3H-PYRILAMINE -2 53 Guinea pig 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4153 61 3H-PYRILAMINE -2 53 Guinea pig 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
115237 55585 119 3H-PYRILAMINE -36 54 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55585 119 3H-PYRILAMINE -36 54 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
135398745 2914 112 3H-PYRILAMINE -2 65 Guinea pig 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 3H-PYRILAMINE -2 65 Guinea pig 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 3H-PYRILAMINE -2 65 Guinea pig 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 3H-PYRILAMINE -2 65 Guinea pig 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
1227 2489 43 3H-MEPYRAMINE -2 12 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
2331 2489 43 3H-MEPYRAMINE -2 12 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
3957 2489 43 3H-MEPYRAMINE -2 12 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
4992 2489 43 3H-MEPYRAMINE -2 12 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
CHEMBL511 2489 43 3H-MEPYRAMINE -2 12 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
DB06691 2489 43 3H-MEPYRAMINE -2 12 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
1228 3866 34 3H-MEPYRAMINE -5 4 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
2763 3866 34 3H-MEPYRAMINE -5 4 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
5282443 3866 34 3H-MEPYRAMINE -5 4 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
CHEMBL855 3866 34 3H-MEPYRAMINE -5 4 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
DB00427 3866 34 3H-MEPYRAMINE -5 4 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
11976 920 59 UNDEFINED -4 24 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
667467 920 59 UNDEFINED -4 24 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
CHEMBL908 920 59 UNDEFINED -4 24 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
DB01239 920 59 UNDEFINED -4 24 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
1227 2489 43 3H-MEPYRAMINE -2 12 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
2331 2489 43 3H-MEPYRAMINE -2 12 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
3957 2489 43 3H-MEPYRAMINE -2 12 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
4992 2489 43 3H-MEPYRAMINE -2 12 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
CHEMBL511 2489 43 3H-MEPYRAMINE -2 12 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
DB06691 2489 43 3H-MEPYRAMINE -2 12 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
1227 2489 43 3H-MEPYRAMINE -2 12 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
2331 2489 43 3H-MEPYRAMINE -2 12 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
3957 2489 43 3H-MEPYRAMINE -2 12 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
4992 2489 43 3H-MEPYRAMINE -2 12 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
CHEMBL511 2489 43 3H-MEPYRAMINE -2 12 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
DB06691 2489 43 3H-MEPYRAMINE -2 12 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
1890 2759 49 3H-PYRILAMINE -4 16 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
4449 2759 49 3H-PYRILAMINE -4 16 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
7247 2759 49 3H-PYRILAMINE -4 16 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
CHEMBL623 2759 49 3H-PYRILAMINE -4 16 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
DB01149 2759 49 3H-PYRILAMINE -4 16 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
1971 2866 38 3H-MEPYRAMINE -6 30 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
2404 2866 38 3H-MEPYRAMINE -6 30 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
4543 2866 38 3H-MEPYRAMINE -6 30 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
CHEMBL445 2866 38 3H-MEPYRAMINE -6 30 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
DB00540 2866 38 3H-MEPYRAMINE -6 30 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
2284 3182 33 3H-MEPYRAMINE -10 29 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
4926 3182 33 3H-MEPYRAMINE -10 29 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
7281 3182 33 3H-MEPYRAMINE -10 29 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
CHEMBL564 3182 33 3H-MEPYRAMINE -10 29 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
DB00420 3182 33 3H-MEPYRAMINE -10 29 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
90475904 216022 0 3H-doxepin -7 6 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(C)CCC(C1=CC=C(C=C1)Cl)C2=CC=CC=N2 None
134 2514 24 3H-MEPYRAMINE -2570 67 Guinea pig 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
134 2514 24 3H-MEPYRAMINE -933 67 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 24 3H-MEPYRAMINE -2570 67 Guinea pig 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 24 3H-MEPYRAMINE -933 67 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 24 3H-MEPYRAMINE -2570 67 Guinea pig 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 24 3H-MEPYRAMINE -933 67 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 24 3H-MEPYRAMINE -2570 67 Guinea pig 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 24 3H-MEPYRAMINE -933 67 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 24 3H-MEPYRAMINE -2570 67 Guinea pig 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 24 3H-MEPYRAMINE -933 67 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1353 1911 93 3H-PYRILAMINE -489 83 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 3H-PYRILAMINE -489 83 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 3H-PYRILAMINE -489 83 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 3H-PYRILAMINE -489 83 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 3H-PYRILAMINE -489 83 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
125564 666 97 3H-PYRILAMINE -5248 7 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 367 3 0 3 4.7 CCN1CCN(CC1)c1nc2CCCCCCc2c(c1)c1ccc(cc1)F None
388 666 97 3H-PYRILAMINE -5248 7 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 367 3 0 3 4.7 CCN1CCN(CC1)c1nc2CCCCCCc2c(c1)c1ccc(cc1)F None
7670 666 97 3H-PYRILAMINE -5248 7 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 367 3 0 3 4.7 CCN1CCN(CC1)c1nc2CCCCCCc2c(c1)c1ccc(cc1)F None
CHEMBL178803 666 97 3H-PYRILAMINE -5248 7 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 367 3 0 3 4.7 CCN1CCN(CC1)c1nc2CCCCCCc2c(c1)c1ccc(cc1)F None
DB09223 666 97 3H-PYRILAMINE -5248 7 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 367 3 0 3 4.7 CCN1CCN(CC1)c1nc2CCCCCCc2c(c1)c1ccc(cc1)F None
1427 2013 54 3H-Histamine -1 27 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
357 2013 54 3H-Histamine -1 27 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
3696 2013 54 3H-Histamine -1 27 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
CHEMBL11 2013 54 3H-Histamine -1 27 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
DB00458 2013 54 3H-Histamine -1 27 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
2995 204405 53 3H-PYRILAMINE -12 23 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
2995 204405 53 3H-PYRILAMINE -14 23 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 204405 53 3H-PYRILAMINE -12 23 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 204405 53 3H-PYRILAMINE -14 23 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 204405 53 3H-PYRILAMINE -12 23 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 204405 53 3H-PYRILAMINE -14 23 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
37459 746 13 3H-MEPYRAMINE -7244 25 Guinea pig 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
62 746 13 3H-MEPYRAMINE -7244 25 Guinea pig 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
CHEMBL8514 746 13 3H-MEPYRAMINE -7244 25 Guinea pig 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
40589 216144 0 3H-PYRILAMINE -5 8 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 377 7 0 6 2.5 CCC1=NN(C(=O)N1CC)CCCN2CCN(CC2)C3=CC(=CC=C3)Cl None
1204 1932 119 3H-MEPYRAMINE -46 24 Guinea pig 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1932 119 3H-MEPYRAMINE -46 24 Guinea pig 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1932 119 3H-MEPYRAMINE -46 24 Guinea pig 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1932 119 3H-MEPYRAMINE -46 24 Guinea pig 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1932 119 3H-MEPYRAMINE -46 24 Guinea pig 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1932 119 3H-MEPYRAMINE -46 24 Guinea pig 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
115237 55585 119 3H-PYRILAMINE -36 54 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55585 119 3H-PYRILAMINE -36 54 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
2435 3590 83 3H-PYRILAMINE -95 48 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3590 83 3H-PYRILAMINE -95 48 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3590 83 3H-PYRILAMINE -95 48 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3590 83 3H-PYRILAMINE -95 48 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3590 83 3H-PYRILAMINE -95 48 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
1209 1658 75 3H-MEPYRAMINE -602 32 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
203 1658 75 3H-MEPYRAMINE -602 32 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
3386 1658 75 3H-MEPYRAMINE -602 32 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL41 1658 75 3H-MEPYRAMINE -602 32 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
DB00472 1658 75 3H-MEPYRAMINE -602 32 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
108107 79944 38 3H-MEPYRAMINE -5 16 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 319 3 4 5 0.5 N/C(=N\C(=O)c1nc(Cl)c(N)nc1N)NCc1ccccc1 None
156592250 79944 38 3H-MEPYRAMINE -5 16 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 319 3 4 5 0.5 N/C(=N\C(=O)c1nc(Cl)c(N)nc1N)NCc1ccccc1 None
CHEMBL1256878 79944 38 3H-MEPYRAMINE -5 16 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 319 3 4 5 0.5 N/C(=N\C(=O)c1nc(Cl)c(N)nc1N)NCc1ccccc1 None
CHEMBL212579 79944 38 3H-MEPYRAMINE -5 16 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 319 3 4 5 0.5 N/C(=N\C(=O)c1nc(Cl)c(N)nc1N)NCc1ccccc1 None
45485498 197671 0 UNDEFINED - 1 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 231 5 0 1 3.8 Cc1ccc(CCCCN2CCCCC2)cc1 None
CHEMBL571073 197671 0 UNDEFINED - 1 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 231 5 0 1 3.8 Cc1ccc(CCCCN2CCCCC2)cc1 None
7153 98020 77 3H-PYRILAMINE -16 34 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 98020 77 3H-PYRILAMINE -16 34 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
2389 3331 118 3H-PYRILAMINE -46 67 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 118 3H-PYRILAMINE -46 67 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 118 3H-PYRILAMINE -46 67 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 118 3H-PYRILAMINE -46 67 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 118 3H-PYRILAMINE -46 67 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
1221 475 9 3H-MEPYRAMINE 2 3 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 380 9 3 3 3.0 NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)F None
65895 475 9 3H-MEPYRAMINE 2 3 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 380 9 3 3 3.0 NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)F None
CHEMBL293802 475 9 3H-MEPYRAMINE 2 3 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 380 9 3 3 3.0 NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)F None
1353 1911 93 3H-MEPYRAMINE -602 83 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 3H-MEPYRAMINE -602 83 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 3H-MEPYRAMINE -602 83 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 3H-MEPYRAMINE -602 83 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 3H-MEPYRAMINE -602 83 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
2142 3096 58 3H-MEPYRAMINE -1258 36 Guinea pig 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 3096 58 3H-MEPYRAMINE -1258 36 Guinea pig 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 3096 58 3H-MEPYRAMINE -1258 36 Guinea pig 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 3096 58 3H-MEPYRAMINE -1258 36 Guinea pig 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 3096 58 3H-MEPYRAMINE -1258 36 Guinea pig 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 3096 58 3H-MEPYRAMINE -1258 36 Guinea pig 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
134 2514 24 3H-MEPYRAMINE -15488 67 Rat 4.5 pKi = 4.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 24 3H-MEPYRAMINE -15488 67 Rat 4.5 pKi = 4.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 24 3H-MEPYRAMINE -15488 67 Rat 4.5 pKi = 4.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 24 3H-MEPYRAMINE -15488 67 Rat 4.5 pKi = 4.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 24 3H-MEPYRAMINE -15488 67 Rat 4.5 pKi = 4.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
2601 3780 33 3H-PYRILAMINE -389 21 Guinea pig 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
443951 3780 33 3H-PYRILAMINE -389 21 Guinea pig 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
56 3780 33 3H-PYRILAMINE -389 21 Guinea pig 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL73151 3780 33 3H-PYRILAMINE -389 21 Guinea pig 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
DB13399 3780 33 3H-PYRILAMINE -389 21 Guinea pig 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
100 3805 58 3H-MEPYRAMINE -16 55 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3805 58 3H-MEPYRAMINE -16 55 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3805 58 3H-MEPYRAMINE -16 55 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3805 58 3H-MEPYRAMINE -16 55 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3805 58 3H-MEPYRAMINE -16 55 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
1588 2325 27 3H-PYRILAMINE -100 44 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2325 27 3H-PYRILAMINE -100 44 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2325 27 3H-PYRILAMINE -100 44 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2325 27 3H-PYRILAMINE -100 44 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2325 27 3H-PYRILAMINE -100 44 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
2762 3863 31 3H-MEPYRAMINE 9 2 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C None
5587 3863 31 3H-MEPYRAMINE 9 2 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C None
7318 3863 31 3H-MEPYRAMINE 9 2 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C None
CHEMBL1241 3863 31 3H-MEPYRAMINE 9 2 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C None
DB00792 3863 31 3H-MEPYRAMINE 9 2 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 255 6 0 3 2.7 CN(CCN(c1ccccn1)Cc1ccccc1)C None
4528 98126 80 3H-PYRILAMINE -7 10 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 238 1 1 2 2.8 CN1Cc2c(N)cccc2C(c2ccccc2)C1 None
CHEMBL273575 98126 80 3H-PYRILAMINE -7 10 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 238 1 1 2 2.8 CN1Cc2c(N)cccc2C(c2ccccc2)C1 None
2771 195017 74 3H-MEPYRAMINE -6 27 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL1200781 195017 74 3H-MEPYRAMINE -6 27 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL549 195017 74 3H-MEPYRAMINE -6 27 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
1221 475 9 3H-MEPYRAMINE -12 3 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 380 9 3 3 3.0 NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)F None
65895 475 9 3H-MEPYRAMINE -12 3 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 380 9 3 3 3.0 NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)F None
CHEMBL293802 475 9 3H-MEPYRAMINE -12 3 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 380 9 3 3 3.0 NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)F None
2726 919 68 3H-MEPYRAMINE -17 72 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 68 3H-MEPYRAMINE -17 72 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 68 3H-MEPYRAMINE -17 72 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 68 3H-MEPYRAMINE -17 72 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 68 3H-MEPYRAMINE -17 72 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
135398737 958 93 3H-MEPYRAMINE -4 89 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-MEPYRAMINE -4 89 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-MEPYRAMINE -4 89 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-MEPYRAMINE -4 89 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-MEPYRAMINE -4 89 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
3947 206395 53 3H-PYRILAMINE -7 16 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 None
CHEMBL87708 206395 53 3H-PYRILAMINE -7 16 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 None
11848625 5792 0 UNDEFINED -38 6 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 451 8 1 7 4.9 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OC2CCOCC2)c1 None
CHEMBL1078745 5792 0 UNDEFINED -38 6 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 451 8 1 7 4.9 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OC2CCOCC2)c1 None
16667681 216153 0 3H-MEPYRAMINE 4 3 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 390 7 1 5 3.5 CN(C)CCCC1=CC=CC=N1.C1=CC(=CC=C1OC(=O)C=CC(=O)O)Cl None
1353 1911 93 3H-PYRILAMINE -602 83 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 3H-PYRILAMINE -602 83 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 3H-PYRILAMINE -602 83 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 3H-PYRILAMINE -602 83 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 3H-PYRILAMINE -602 83 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1427 2013 54 3H-PYRILAMINE -5 27 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
357 2013 54 3H-PYRILAMINE -5 27 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
3696 2013 54 3H-PYRILAMINE -5 27 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
CHEMBL11 2013 54 3H-PYRILAMINE -5 27 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
DB00458 2013 54 3H-PYRILAMINE -5 27 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
1890 2759 49 3H-PYRILAMINE -44 16 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
1890 2759 49 3H-MEPYRAMINE -57 16 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
4449 2759 49 3H-PYRILAMINE -44 16 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
4449 2759 49 3H-MEPYRAMINE -57 16 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
7247 2759 49 3H-PYRILAMINE -44 16 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
7247 2759 49 3H-MEPYRAMINE -57 16 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
CHEMBL623 2759 49 3H-PYRILAMINE -44 16 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
CHEMBL623 2759 49 3H-MEPYRAMINE -57 16 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
DB01149 2759 49 3H-PYRILAMINE -44 16 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
DB01149 2759 49 3H-MEPYRAMINE -57 16 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
1353 1911 93 3H-pirilamine -602 83 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 3H-pirilamine -602 83 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 3H-pirilamine -602 83 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 3H-pirilamine -602 83 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 3H-pirilamine -602 83 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
6852400 215937 0 UNDEFINED -977 22 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
73759726 215937 0 UNDEFINED -977 22 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
44622872 197716 0 UNDEFINED - 1 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 413 8 1 2 6.0 Cc1ccc(CCCCN2CCC(C(O)(c3ccccc3)c3ccccc3)CC2)cc1 None
CHEMBL571389 197716 0 UNDEFINED - 1 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 413 8 1 2 6.0 Cc1ccc(CCCCN2CCC(C(O)(c3ccccc3)c3ccccc3)CC2)cc1 None
25212275 174421 0 UNDEFINED -9332 6 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 682 13 0 8 7.4 O=C(OCCN1CCN(CCCN2c3ccccc3Sc3ccc(C(F)(F)F)cc32)CC1)c1ccc(OCCCN2CCCCC2)cc1 None
CHEMBL455288 174421 0 UNDEFINED -9332 6 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 682 13 0 8 7.4 O=C(OCCN1CCN(CCCN2c3ccccc3Sc3ccc(C(F)(F)F)cc32)CC1)c1ccc(OCCCN2CCCCC2)cc1 None
6852400 215937 0 3H-doxepin -977 22 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
73759726 215937 0 3H-doxepin -977 22 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
3025067 99382 64 3H-MEPYRAMINE -199 15 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 220 1 1 4 0.9 c1cc2c(c(N3CCNCC3)c1)OCCO2 None
65853 99382 64 3H-MEPYRAMINE -199 15 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 220 1 1 4 0.9 c1cc2c(c(N3CCNCC3)c1)OCCO2 None
CHEMBL282614 99382 64 3H-MEPYRAMINE -199 15 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 220 1 1 4 0.9 c1cc2c(c(N3CCNCC3)c1)OCCO2 None
1613 2348 53 3H-Histamine -3 44 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2348 53 3H-Histamine -3 44 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2348 53 3H-Histamine -3 44 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2348 53 3H-Histamine -3 44 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2348 53 3H-Histamine -3 44 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
135398737 958 93 3H-MEPYRAMINE -2 89 Guinea pig 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-MEPYRAMINE -2 89 Guinea pig 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-MEPYRAMINE -2 89 Guinea pig 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-MEPYRAMINE -2 89 Guinea pig 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-MEPYRAMINE -2 89 Guinea pig 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1227 2489 43 3H-doxepin -2 12 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
2331 2489 43 3H-doxepin -2 12 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
3957 2489 43 3H-doxepin -2 12 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
4992 2489 43 3H-doxepin -2 12 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
CHEMBL511 2489 43 3H-doxepin -2 12 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
DB06691 2489 43 3H-doxepin -2 12 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
2286 3183 51 3H-PYRILAMINE -1 30 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
4927 3183 51 3H-PYRILAMINE -1 30 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
7282 3183 51 3H-PYRILAMINE -1 30 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
CHEMBL643 3183 51 3H-PYRILAMINE -1 30 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
DB01069 3183 51 3H-PYRILAMINE -1 30 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
11954259 215979 0 3H-PYRILAMINE -19 43 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
20980871 216430 0 3H-MEPYRAMINE 4 8 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 295 3 0 2 4.7 CN(C)CCC=C1C2=CC=CC=C2CSC3=CC=CC=C31 None
135 2532 43 3H-MEPYRAMINE 1 58 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 43 3H-MEPYRAMINE 1 58 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 43 3H-MEPYRAMINE 1 58 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 43 3H-MEPYRAMINE 1 58 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 43 3H-MEPYRAMINE 1 58 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1204 1932 119 None -501 24 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]mepyramine from human wild-type histamine H1 receptor expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human wild-type histamine H1 receptor expressed in COS-7 cells by liquid scintillation counting
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1932 119 None -501 24 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]mepyramine from human wild-type histamine H1 receptor expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human wild-type histamine H1 receptor expressed in COS-7 cells by liquid scintillation counting
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1932 119 None -501 24 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]mepyramine from human wild-type histamine H1 receptor expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human wild-type histamine H1 receptor expressed in COS-7 cells by liquid scintillation counting
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1932 119 None -501 24 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]mepyramine from human wild-type histamine H1 receptor expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human wild-type histamine H1 receptor expressed in COS-7 cells by liquid scintillation counting
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1932 119 None -501 24 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]mepyramine from human wild-type histamine H1 receptor expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human wild-type histamine H1 receptor expressed in COS-7 cells by liquid scintillation counting
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1932 119 None -501 24 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]mepyramine from human wild-type histamine H1 receptor expressed in COS-7 cells by liquid scintillation countingDisplacement of [3H]mepyramine from human wild-type histamine H1 receptor expressed in COS-7 cells by liquid scintillation counting
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
180 401 56 3H-MEPYRAMINE -11 40 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 401 56 3H-MEPYRAMINE -11 40 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 401 56 3H-MEPYRAMINE -11 40 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 401 56 3H-MEPYRAMINE -11 40 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 401 56 3H-MEPYRAMINE -11 40 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2554 796 119 None 1 8 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 236 0 1 1 3.4 NC(=O)N1c2ccccc2C=Cc2c1cccc2 None
489 796 119 None 1 8 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 236 0 1 1 3.4 NC(=O)N1c2ccccc2C=Cc2c1cccc2 None
5339 796 119 None 1 8 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 236 0 1 1 3.4 NC(=O)N1c2ccccc2C=Cc2c1cccc2 None
CHEMBL108 796 119 None 1 8 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 236 0 1 1 3.4 NC(=O)N1c2ccccc2C=Cc2c1cccc2 None
DB00564 796 119 None 1 8 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 236 0 1 1 3.4 NC(=O)N1c2ccccc2C=Cc2c1cccc2 None
135 2532 43 3H-PYRILAMINE -1 58 Guinea pig 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 43 3H-PYRILAMINE -1 58 Guinea pig 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 43 3H-PYRILAMINE -1 58 Guinea pig 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 43 3H-PYRILAMINE -1 58 Guinea pig 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 43 3H-PYRILAMINE -1 58 Guinea pig 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
2284 3182 33 3H-MEPYRAMINE 1 29 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
4926 3182 33 3H-MEPYRAMINE 1 29 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
7281 3182 33 3H-MEPYRAMINE 1 29 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
CHEMBL564 3182 33 3H-MEPYRAMINE 1 29 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
DB00420 3182 33 3H-MEPYRAMINE 1 29 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
2726 919 68 UNDEFINED -2 72 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 68 UNDEFINED -2 72 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 68 UNDEFINED -2 72 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 68 UNDEFINED -2 72 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 68 UNDEFINED -2 72 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
135398745 2914 112 3H-pirilamine -1 65 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 3H-pirilamine -1 65 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 3H-pirilamine -1 65 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 3H-pirilamine -1 65 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
11954259 215979 0 3H-doxepin -19 43 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
2726 919 68 3H-MEPYRAMINE -6 72 Guinea pig 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 68 3H-MEPYRAMINE -6 72 Guinea pig 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 68 3H-MEPYRAMINE -6 72 Guinea pig 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 68 3H-MEPYRAMINE -6 72 Guinea pig 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 68 3H-MEPYRAMINE -6 72 Guinea pig 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1227 2489 43 3H-MEPYRAMINE -5 12 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
2331 2489 43 3H-MEPYRAMINE -5 12 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
3957 2489 43 3H-MEPYRAMINE -5 12 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
4992 2489 43 3H-MEPYRAMINE -5 12 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
CHEMBL511 2489 43 3H-MEPYRAMINE -5 12 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
DB06691 2489 43 3H-MEPYRAMINE -5 12 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
4098 32505 30 3H-MEPYRAMINE -1 11 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 None
CHEMBL1255739 32505 30 3H-MEPYRAMINE -1 11 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 None
CHEMBL1411979 32505 30 3H-MEPYRAMINE -1 11 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 None
2865 4143 73 3H-PYRILAMINE -58 53 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4143 73 3H-PYRILAMINE -58 53 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4143 73 3H-PYRILAMINE -58 53 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4143 73 3H-PYRILAMINE -58 53 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4143 73 3H-PYRILAMINE -58 53 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
2303 3187 68 None -363 26 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
4946 3187 68 None -363 26 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
564 3187 68 None -363 26 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
63 3187 68 None -363 26 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
91536 3187 68 None -363 26 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 3187 68 None -363 26 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 3187 68 None -363 26 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
DB00571 3187 68 None -363 26 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
1227 2489 43 3H-MEPYRAMINE -2 12 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
2331 2489 43 3H-MEPYRAMINE -2 12 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
3957 2489 43 3H-MEPYRAMINE -2 12 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
4992 2489 43 3H-MEPYRAMINE -2 12 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
CHEMBL511 2489 43 3H-MEPYRAMINE -2 12 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
DB06691 2489 43 3H-MEPYRAMINE -2 12 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
6834 205552 45 3H-MEPYRAMINE 1 2 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 318 5 0 2 3.9 CN(C)CCC(c1ccc(Br)cc1)c1ccccn1 None
CHEMBL811 205552 45 3H-MEPYRAMINE 1 2 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 318 5 0 2 3.9 CN(C)CCC(c1ccc(Br)cc1)c1ccccn1 None
3103 41658 49 3H-MEPYRAMINE -1 4 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 281 4 0 2 3.9 CN1CCC(OC(c2ccccc2)c2ccccc2)CC1 None
CHEMBL1492 41658 49 3H-MEPYRAMINE -1 4 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 281 4 0 2 3.9 CN1CCC(OC(c2ccccc2)c2ccccc2)CC1 None
90475904 216022 0 3H-MEPYRAMINE -7 6 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(C)CCC(C1=CC=C(C=C1)Cl)C2=CC=CC=N2 None
1613 2348 53 3H-doxepin -3 44 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2348 53 3H-doxepin -3 44 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2348 53 3H-doxepin -3 44 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2348 53 3H-doxepin -3 44 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2348 53 3H-doxepin -3 44 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
135398745 2914 112 3H-PYRILAMINE 1 65 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 3H-PYRILAMINE 1 65 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 3H-PYRILAMINE 1 65 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 3H-PYRILAMINE 1 65 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
2564 206184 51 3H-MEPYRAMINE -2 3 Guinea pig 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 290 6 0 3 3.4 CN(C)CCOC(c1ccc(Cl)cc1)c1ccccn1 None
CHEMBL864 206184 51 3H-MEPYRAMINE -2 3 Guinea pig 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 290 6 0 3 3.4 CN(C)CCOC(c1ccc(Cl)cc1)c1ccccn1 None
1212 1662 50 UNDEFINED -41 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1662 50 UNDEFINED -41 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1662 50 UNDEFINED -41 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1662 50 UNDEFINED -41 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1662 50 UNDEFINED -41 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2600 3779 74 UNDEFINED 1 13 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
2608 3779 74 UNDEFINED 1 13 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
5405 3779 74 UNDEFINED 1 13 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
CHEMBL17157 3779 74 UNDEFINED 1 13 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
DB00342 3779 74 UNDEFINED 1 13 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
25212276 190066 0 UNDEFINED -112 6 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 508 11 0 3 7.4 CN(CCCC12CCC(c3ccccc31)c1ccccc12)Cc1ccc(OCCCN2CCCCC2)cc1 None
CHEMBL517244 190066 0 UNDEFINED -112 6 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 508 11 0 3 7.4 CN(CCCC12CCC(c3ccccc31)c1ccccc12)Cc1ccc(OCCCN2CCCCC2)cc1 None
2142 3096 58 3H-doxepin -263 36 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 3096 58 3H-doxepin -263 36 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 3096 58 3H-doxepin -263 36 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 3096 58 3H-doxepin -263 36 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 3096 58 3H-doxepin -263 36 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 3096 58 3H-doxepin -263 36 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
1204 1932 119 3H-MEPYRAMINE -309 24 Rat 4.4 pKi = 4.4 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1932 119 3H-MEPYRAMINE -309 24 Rat 4.4 pKi = 4.4 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1932 119 3H-MEPYRAMINE -309 24 Rat 4.4 pKi = 4.4 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1932 119 3H-MEPYRAMINE -309 24 Rat 4.4 pKi = 4.4 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1932 119 3H-MEPYRAMINE -309 24 Rat 4.4 pKi = 4.4 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1932 119 3H-MEPYRAMINE -309 24 Rat 4.4 pKi = 4.4 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
2142 3096 58 3H-MEPYRAMINE -7585 36 Rat 4.4 pKi = 4.4 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 3096 58 3H-MEPYRAMINE -7585 36 Rat 4.4 pKi = 4.4 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 3096 58 3H-MEPYRAMINE -7585 36 Rat 4.4 pKi = 4.4 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 3096 58 3H-MEPYRAMINE -7585 36 Rat 4.4 pKi = 4.4 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 3096 58 3H-MEPYRAMINE -7585 36 Rat 4.4 pKi = 4.4 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 3096 58 3H-MEPYRAMINE -7585 36 Rat 4.4 pKi = 4.4 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
37459 746 13 3H-MEPYRAMINE -1174 25 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
62 746 13 3H-MEPYRAMINE -1174 25 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
CHEMBL8514 746 13 3H-MEPYRAMINE -1174 25 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
135398737 958 93 3H-MEPYRAMINE -4 89 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-MEPYRAMINE -4 89 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-MEPYRAMINE -4 89 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-MEPYRAMINE -4 89 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-MEPYRAMINE -4 89 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1353 1911 93 3H-PYRILAMINE -489 83 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 3H-PYRILAMINE -489 83 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 3H-PYRILAMINE -489 83 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 3H-PYRILAMINE -489 83 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 3H-PYRILAMINE -489 83 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3012003 216145 0 3H-PYRILAMINE -6 12 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 311 5 0 3 3.8 CN1CCC(C(C1)COC2=CC=C(C=C2)OC)C3=CC=CC=C3 None
2865 4143 73 3H-PYRILAMINE -58 53 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4143 73 3H-PYRILAMINE -58 53 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4143 73 3H-PYRILAMINE -58 53 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4143 73 3H-PYRILAMINE -58 53 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4143 73 3H-PYRILAMINE -58 53 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
3294 2006 111 3H-PYRILAMINE -630 45 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 2006 111 3H-PYRILAMINE -630 45 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 2006 111 3H-PYRILAMINE -630 45 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 2006 111 3H-PYRILAMINE -630 45 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 2006 111 3H-PYRILAMINE -630 45 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
1353 1911 93 3H-PYRILAMINE -489 83 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 3H-PYRILAMINE -489 83 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 3H-PYRILAMINE -489 83 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 3H-PYRILAMINE -489 83 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 3H-PYRILAMINE -489 83 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 1911 93 UNDEFINED -489 83 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 UNDEFINED -489 83 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 UNDEFINED -489 83 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 UNDEFINED -489 83 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 UNDEFINED -489 83 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
2435 3590 83 UNDEFINED -851 48 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3590 83 UNDEFINED -851 48 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3590 83 UNDEFINED -851 48 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3590 83 UNDEFINED -851 48 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3590 83 UNDEFINED -851 48 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
7153 98020 77 3H-PYRILAMINE -23 34 Guinea pig 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 98020 77 3H-PYRILAMINE -23 34 Guinea pig 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
2995 204405 53 3H-MEPYRAMINE -14 23 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 204405 53 3H-MEPYRAMINE -14 23 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 204405 53 3H-MEPYRAMINE -14 23 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
1971 2866 38 3H-MEPYRAMINE -9 30 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
2404 2866 38 3H-MEPYRAMINE -9 30 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
4543 2866 38 3H-MEPYRAMINE -9 30 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
CHEMBL445 2866 38 3H-MEPYRAMINE -9 30 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
DB00540 2866 38 3H-MEPYRAMINE -9 30 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
2865 4143 73 3H-PYRILAMINE -58 53 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4143 73 3H-PYRILAMINE -58 53 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4143 73 3H-PYRILAMINE -58 53 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4143 73 3H-PYRILAMINE -58 53 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4143 73 3H-PYRILAMINE -58 53 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
21722 17992 31 3H-MEPYRAMINE -5 6 Guinea pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 None
CHEMBL126224 17992 31 3H-MEPYRAMINE -5 6 Guinea pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 None
1204 1932 119 3H-MEPYRAMINE -46 24 Guinea pig 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1932 119 3H-MEPYRAMINE -46 24 Guinea pig 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1932 119 3H-MEPYRAMINE -46 24 Guinea pig 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1932 119 3H-MEPYRAMINE -46 24 Guinea pig 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1932 119 3H-MEPYRAMINE -46 24 Guinea pig 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1932 119 3H-MEPYRAMINE -46 24 Guinea pig 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1204 1932 119 3H-MEPYRAMINE -46 24 Guinea pig 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1932 119 3H-MEPYRAMINE -46 24 Guinea pig 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1932 119 3H-MEPYRAMINE -46 24 Guinea pig 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1932 119 3H-MEPYRAMINE -46 24 Guinea pig 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1932 119 3H-MEPYRAMINE -46 24 Guinea pig 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1932 119 3H-MEPYRAMINE -46 24 Guinea pig 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
2865 4143 73 UNDEFINED -58 53 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4143 73 UNDEFINED -58 53 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4143 73 UNDEFINED -58 53 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4143 73 UNDEFINED -58 53 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4143 73 UNDEFINED -58 53 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
2470 3653 50 UNDEFINED -4570 59 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3653 50 UNDEFINED -4570 59 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3653 50 UNDEFINED -4570 59 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3653 50 UNDEFINED -4570 59 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3653 50 UNDEFINED -4570 59 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
2470 3653 50 3H-doxepin -4570 59 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3653 50 3H-doxepin -4570 59 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3653 50 3H-doxepin -4570 59 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3653 50 3H-doxepin -4570 59 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3653 50 3H-doxepin -4570 59 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
1613 2348 53 UNDEFINED -3 44 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2348 53 UNDEFINED -3 44 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2348 53 UNDEFINED -3 44 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2348 53 UNDEFINED -3 44 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2348 53 UNDEFINED -3 44 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
1816 2540 102 3H-PYRILAMINE -10 18 Guinea pig 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
4205 2540 102 3H-PYRILAMINE -10 18 Guinea pig 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
7241 2540 102 3H-PYRILAMINE -10 18 Guinea pig 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
CHEMBL654 2540 102 3H-PYRILAMINE -10 18 Guinea pig 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
DB00370 2540 102 3H-PYRILAMINE -10 18 Guinea pig 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
2389 3331 118 3H-PYRILAMINE -46 67 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 118 3H-PYRILAMINE -46 67 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 118 3H-PYRILAMINE -46 67 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 118 3H-PYRILAMINE -46 67 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 118 3H-PYRILAMINE -46 67 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
1548955 88581 20 None 1 18 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 None
2800 88581 20 None 1 18 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 None
CHEMBL2355051 88581 20 None 1 18 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 None
2389 3331 118 3H-PYRILAMINE -46 67 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 118 3H-PYRILAMINE -46 67 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 118 3H-PYRILAMINE -46 67 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 118 3H-PYRILAMINE -46 67 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 118 3H-PYRILAMINE -46 67 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2865 4143 73 3H-PYRILAMINE -17 53 Guinea pig 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4143 73 3H-PYRILAMINE -17 53 Guinea pig 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4143 73 3H-PYRILAMINE -17 53 Guinea pig 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4143 73 3H-PYRILAMINE -17 53 Guinea pig 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4143 73 3H-PYRILAMINE -17 53 Guinea pig 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
2142 3096 58 None -263 36 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 3096 58 None -263 36 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 3096 58 None -263 36 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 3096 58 None -263 36 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 3096 58 None -263 36 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 3096 58 None -263 36 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
2812 4779 101 None -28 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
CHEMBL104 4779 101 None -28 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
40589 216144 0 None -5 8 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 377 7 0 6 2.5 CCC1=NN(C(=O)N1CC)CCCN2CCN(CC2)C3=CC(=CC=C3)Cl None
4528 98126 80 None -1 10 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 238 1 1 2 2.8 CN1Cc2c(N)cccc2C(c2ccccc2)C1 None
CHEMBL273575 98126 80 None -1 10 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 238 1 1 2 2.8 CN1Cc2c(N)cccc2C(c2ccccc2)C1 None
3114 189927 71 None - 1 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 339 8 1 3 3.4 CC(C)N(CCC(C(N)=O)(c1ccccc1)c1ccccn1)C(C)C None
CHEMBL517 189927 71 None - 1 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 339 8 1 3 3.4 CC(C)N(CCC(C(N)=O)(c1ccccc1)c1ccccn1)C(C)C None
2181 3128 46 None -269 35 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
4830 3128 46 None -269 35 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
92 3128 46 None -269 35 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
CHEMBL440294 3128 46 None -269 35 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
DB09286 3128 46 None -269 35 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
135398745 2914 112 UNDEFINED -1 65 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 UNDEFINED -1 65 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 UNDEFINED -1 65 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 UNDEFINED -1 65 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
1228 3866 34 3H-MEPYRAMINE -6 4 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
2763 3866 34 3H-MEPYRAMINE -6 4 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
5282443 3866 34 3H-MEPYRAMINE -6 4 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
CHEMBL855 3866 34 3H-MEPYRAMINE -6 4 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
DB00427 3866 34 3H-MEPYRAMINE -6 4 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
657255 199084 34 None -18 15 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 None
CHEMBL588119 199084 34 None -18 15 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 None
115237 55585 119 3H-PYRILAMINE -36 54 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55585 119 3H-PYRILAMINE -36 54 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
446220 133521 14 None -19 45 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
CHEMBL370805 133521 14 None -19 45 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
1830 2590 44 None -125 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 2590 44 None -125 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 2590 44 None -125 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 2590 44 None -125 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 2590 44 None -125 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
5281878 1660 35 3H-MEPYRAMINE -1 17 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 1660 35 3H-MEPYRAMINE -1 17 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 1660 35 3H-MEPYRAMINE -1 17 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 1660 35 3H-MEPYRAMINE -1 17 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 1660 35 3H-MEPYRAMINE -1 17 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 1660 35 3H-MEPYRAMINE -1 17 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 1660 35 3H-MEPYRAMINE -1 17 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
103 4153 61 3H-PYRILAMINE -1 53 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4153 61 3H-PYRILAMINE -1 53 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4153 61 3H-PYRILAMINE -1 53 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4153 61 3H-PYRILAMINE -1 53 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4153 61 3H-PYRILAMINE -1 53 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
4066 204626 78 3H-doxepin -1 7 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 None
CHEMBL73451 204626 78 3H-doxepin -1 7 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 None
1621 2429 17 None -301 45 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Histamine H1 receptorBinding affinity towards Histamine H1 receptor
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2429 17 None -301 45 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Histamine H1 receptorBinding affinity towards Histamine H1 receptor
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2429 17 None -301 45 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Histamine H1 receptorBinding affinity towards Histamine H1 receptor
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2429 17 None -301 45 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Histamine H1 receptorBinding affinity towards Histamine H1 receptor
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2429 17 None -301 45 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Histamine H1 receptorBinding affinity towards Histamine H1 receptor
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
11954259 215979 0 UNDEFINED -19 43 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
107782 14468 18 None 1 5 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O None
67151996 14468 18 None 1 5 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O None
CHEMBL1201207 14468 18 None 1 5 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O None
5048 3133 64 None -109 7 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysis
Drug Central 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 None
8924 3133 64 None -109 7 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysis
Drug Central 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 None
9948102 3133 64 None -109 7 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysis
Drug Central 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 None
CHEMBL462605 3133 64 None -109 7 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysis
Drug Central 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 None
DB11642 3133 64 None -109 7 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysisDisplacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysis
Drug Central 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 None
1209 1658 75 None -144 32 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
203 1658 75 None -144 32 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
3386 1658 75 None -144 32 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL41 1658 75 None -144 32 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
DB00472 1658 75 None -144 32 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
2181 3128 46 3H-PYRILAMINE -4168 35 Guinea pig 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
4830 3128 46 3H-PYRILAMINE -4168 35 Guinea pig 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
92 3128 46 3H-PYRILAMINE -4168 35 Guinea pig 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
CHEMBL440294 3128 46 3H-PYRILAMINE -4168 35 Guinea pig 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
DB09286 3128 46 3H-PYRILAMINE -4168 35 Guinea pig 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
46882182 5921 0 UNDEFINED -95 5 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 567 11 1 9 4.7 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)N(C)C)ccc4o3)CC2)cc(OCC)c1-n1cccc1 None
CHEMBL1079686 5921 0 UNDEFINED -95 5 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 567 11 1 9 4.7 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)N(C)C)ccc4o3)CC2)cc(OCC)c1-n1cccc1 None
53389 98447 23 3H-MEPYRAMINE 1 6 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 3.9 C[C@H]1CN(CCCn2c3ccccc3c3ccccc32)C[C@@H](C)N1 None
CHEMBL275707 98447 23 3H-MEPYRAMINE 1 6 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 3.9 C[C@H]1CN(CCCn2c3ccccc3c3ccccc32)C[C@@H](C)N1 None
68617 205527 62 3H-PYRILAMINE -1023 26 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL1709 205527 62 3H-PYRILAMINE -1023 26 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL809 205527 62 3H-PYRILAMINE -1023 26 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
None 216135 0 3H-KETANSERIN -5248 24 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 772 16 4 10 5.5 CN(C)CCONC(=CC=C1C=CC(=O)C=C1)C2=CC=CC=C2F.CN(C)CCONC(=CC=C1C=CC(=O)C=C1)C2=CC=CC=C2F.C(=CC(=O)O)C(=O)O None
191 403 98 3H-Histamine -56 29 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
201 403 98 3H-Histamine -56 29 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2170 403 98 3H-Histamine -56 29 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
CHEMBL1113 403 98 3H-Histamine -56 29 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
DB00543 403 98 3H-Histamine -56 29 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
1353 1911 93 3H-MEPYRAMINE -602 83 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 3H-MEPYRAMINE -602 83 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 3H-MEPYRAMINE -602 83 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 3H-MEPYRAMINE -602 83 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 3H-MEPYRAMINE -602 83 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
68617 205527 62 3H-PYRILAMINE -831 26 Guinea pig 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL1709 205527 62 3H-PYRILAMINE -831 26 Guinea pig 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL809 205527 62 3H-PYRILAMINE -831 26 Guinea pig 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
2865 4143 73 UNDEFINED -1047 53 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4143 73 UNDEFINED -1047 53 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4143 73 UNDEFINED -1047 53 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4143 73 UNDEFINED -1047 53 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4143 73 UNDEFINED -1047 53 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
5568 197500 29 3H-MEPYRAMINE -25 5 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 352 4 0 3 5.3 CN(C)CCCN1c2ccccc2Sc2ccc(C(F)(F)F)cc21 None
66069 197500 29 3H-MEPYRAMINE -25 5 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 352 4 0 3 5.3 CN(C)CCCN1c2ccccc2Sc2ccc(C(F)(F)F)cc21 None
CHEMBL1201102 197500 29 3H-MEPYRAMINE -25 5 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 352 4 0 3 5.3 CN(C)CCCN1c2ccccc2Sc2ccc(C(F)(F)F)cc21 None
CHEMBL570 197500 29 3H-MEPYRAMINE -25 5 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 352 4 0 3 5.3 CN(C)CCCN1c2ccccc2Sc2ccc(C(F)(F)F)cc21 None
11848677 148352 0 UNDEFINED -1 5 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 460 8 2 8 3.0 CCOc1cc(CN2CCC(Nc3nc4cc(S(N)(=O)=O)ccc4o3)CC2)ccc1OC None
CHEMBL393718 148352 0 UNDEFINED -1 5 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 460 8 2 8 3.0 CCOc1cc(CN2CCC(Nc3nc4cc(S(N)(=O)=O)ccc4o3)CC2)ccc1OC None
1222 1664 49 3H-PYRILAMINE -891 33 Guinea pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3396 1664 49 3H-PYRILAMINE -891 33 Guinea pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
85 1664 49 3H-PYRILAMINE -891 33 Guinea pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL46516 1664 49 3H-PYRILAMINE -891 33 Guinea pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
DB04842 1664 49 3H-PYRILAMINE -891 33 Guinea pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
1209 1658 75 3H-PYRILAMINE -144 32 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
203 1658 75 3H-PYRILAMINE -144 32 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
3386 1658 75 3H-PYRILAMINE -144 32 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL41 1658 75 3H-PYRILAMINE -144 32 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
DB00472 1658 75 3H-PYRILAMINE -144 32 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
54841 203127 52 3H-PYRILAMINE -2 27 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 255 6 1 2 3.7 CNCC[C@@H](Oc1ccccc1C)c1ccccc1 None
CHEMBL641 203127 52 3H-PYRILAMINE -2 27 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 255 6 1 2 3.7 CNCC[C@@H](Oc1ccccc1C)c1ccccc1 None
44591012 175580 0 UNDEFINED -114 6 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 522 10 0 3 6.6 CN(CCC=C1c2ccccc2CCc2ccccc21)C(=O)Cc1ccc(OCCCN2CCCCC2)cc1 None
CHEMBL457957 175580 0 UNDEFINED -114 6 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 522 10 0 3 6.6 CN(CCC=C1c2ccccc2CCc2ccccc21)C(=O)Cc1ccc(OCCCN2CCCCC2)cc1 None
1192 147 47 3H-MEPYRAMINE -91 17 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 311 2 3 5 0.5 NC(=NC(=O)c1nc(Cl)c(nc1N)N1CCCCCC1)N None
1794 147 47 3H-MEPYRAMINE -91 17 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 311 2 3 5 0.5 NC(=NC(=O)c1nc(Cl)c(nc1N)N1CCCCCC1)N None
CHEMBL501701 147 47 3H-MEPYRAMINE -91 17 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 311 2 3 5 0.5 NC(=NC(=O)c1nc(Cl)c(nc1N)N1CCCCCC1)N None
2435 3590 83 3H-PYRILAMINE -1122 48 Guinea pig 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3590 83 3H-PYRILAMINE -1122 48 Guinea pig 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3590 83 3H-PYRILAMINE -1122 48 Guinea pig 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3590 83 3H-PYRILAMINE -1122 48 Guinea pig 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3590 83 3H-PYRILAMINE -1122 48 Guinea pig 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
15387 45822 55 3H-PYRILAMINE -8 24 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
CHEMBL1531134 45822 55 3H-PYRILAMINE -8 24 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
12057539 208041 42 3H-MEPYRAMINE -676 20 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 208041 42 3H-MEPYRAMINE -676 20 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 208041 42 3H-MEPYRAMINE -676 20 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
33630 178957 99 None -13 28 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Pyrilamine from human H1 receptor expressed in HEK cells by radioligand binding assay
Drug Central 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
CHEMBL47050 178957 99 None -13 28 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Pyrilamine from human H1 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Pyrilamine from human H1 receptor expressed in HEK cells by radioligand binding assay
Drug Central 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
2726 919 68 3H-PYRILAMINE -2 72 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 68 3H-PYRILAMINE -2 72 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 68 3H-PYRILAMINE -2 72 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 68 3H-PYRILAMINE -2 72 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 68 3H-PYRILAMINE -2 72 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
135398737 958 93 3H-PYRILAMINE -4 89 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-PYRILAMINE -4 89 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-PYRILAMINE -4 89 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-PYRILAMINE -4 89 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-PYRILAMINE -4 89 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
11954259 215979 0 3H-doxepin -19 43 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
None 216149 0 3H-MEPYRAMINE - 1 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 411 6 0 1 0.8 CC1=CC=C(C=C1)C(C2=CC=CC=C2)OCC[N+](C)(C)C.[I-] None
6834 205552 45 3H-PYRILAMINE -1 2 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 318 5 0 2 3.9 CN(C)CCC(c1ccc(Br)cc1)c1ccccn1 None
CHEMBL811 205552 45 3H-PYRILAMINE -1 2 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 318 5 0 2 3.9 CN(C)CCC(c1ccc(Br)cc1)c1ccccn1 None
1224 1432 83 3H-MEPYRAMINE -2 13 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
3100 1432 83 3H-MEPYRAMINE -2 13 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
8980 1432 83 3H-MEPYRAMINE -2 13 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
916 1432 83 3H-MEPYRAMINE -2 13 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
CHEMBL657 1432 83 3H-MEPYRAMINE -2 13 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
DB01075 1432 83 3H-MEPYRAMINE -2 13 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
2448 99323 70 None -4 18 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 None
CHEMBL28218 99323 70 None -4 18 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 None
15723 18539 111 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation counting
Drug Central 267 3 2 2 2.9 OC(c1ccccc1)(c1ccccc1)C1CCNCC1 None
CHEMBL127508 18539 111 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation countingDisplacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation counting
Drug Central 267 3 2 2 2.9 OC(c1ccccc1)(c1ccccc1)C1CCNCC1 None
213 3853 55 None -8 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 3853 55 None -8 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 3853 55 None -8 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 3853 55 None -8 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 3853 55 None -8 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
4020 205150 39 None - 1 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 284 1 1 3 2.6 OC1(c2ccc(Cl)cc2)c2ccccc2C2=NCCN21 None
CHEMBL781 205150 39 None - 1 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 284 1 1 3 2.6 OC1(c2ccc(Cl)cc2)c2ccccc2C2=NCCN21 None
15387 45822 55 None -8 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
CHEMBL1531134 45822 55 None -8 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
3168 9262 92 None -87 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
CHEMBL1108 9262 92 None -87 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
1222 881 0 3H-MEPYRAMINE -1 2 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
2678 881 0 3H-MEPYRAMINE -1 2 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
581 881 0 3H-MEPYRAMINE -1 2 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
CHEMBL1000 881 0 3H-MEPYRAMINE -1 2 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
DB00341 881 0 3H-MEPYRAMINE -1 2 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
1971 2866 38 3H-PYRILAMINE -1 30 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
2404 2866 38 3H-PYRILAMINE -1 30 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
4543 2866 38 3H-PYRILAMINE -1 30 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
CHEMBL445 2866 38 3H-PYRILAMINE -1 30 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
DB00540 2866 38 3H-PYRILAMINE -1 30 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
1222 881 0 3H-MEPYRAMINE -1 2 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
2678 881 0 3H-MEPYRAMINE -1 2 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
581 881 0 3H-MEPYRAMINE -1 2 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
CHEMBL1000 881 0 3H-MEPYRAMINE -1 2 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
DB00341 881 0 3H-MEPYRAMINE -1 2 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
133 2496 52 None -102 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2496 52 None -102 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2496 52 None -102 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2496 52 None -102 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2496 52 None -102 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
2470 3653 50 None -4570 59 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3653 50 None -4570 59 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3653 50 None -4570 59 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3653 50 None -4570 59 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3653 50 None -4570 59 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
1353 1911 93 None -489 83 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 None -489 83 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 None -489 83 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 None -489 83 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 None -489 83 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned histamine H1 receptorBinding affinity to human cloned histamine H1 receptor
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 1911 93 None -213 83 Guinea pig 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 None -213 83 Guinea pig 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 None -213 83 Guinea pig 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 None -213 83 Guinea pig 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 None -213 83 Guinea pig 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
2710 84308 31 3H-MEPYRAMINE 1 3 Guinea pig 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 300 3 0 2 3.7 CN1CCN(C(c2ccccc2)c2ccc(Cl)cc2)CC1 None
CHEMBL22150 84308 31 3H-MEPYRAMINE 1 3 Guinea pig 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 300 3 0 2 3.7 CN1CCN(C(c2ccccc2)c2ccc(Cl)cc2)CC1 None
1353 1911 93 None -602 83 Rat 8.2 pKi = 8.2 Binding
Half-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenateHalf-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenate
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 None -602 83 Rat 8.2 pKi = 8.2 Binding
Half-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenateHalf-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenate
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 None -602 83 Rat 8.2 pKi = 8.2 Binding
Half-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenateHalf-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenate
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 None -602 83 Rat 8.2 pKi = 8.2 Binding
Half-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenateHalf-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenate
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 None -602 83 Rat 8.2 pKi = 8.2 Binding
Half-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenateHalf-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenate
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1890 2759 49 None -44 16 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
4449 2759 49 None -44 16 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
7247 2759 49 None -44 16 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
CHEMBL623 2759 49 None -44 16 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
DB01149 2759 49 None -44 16 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
3947 206395 53 None -7 16 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 None
CHEMBL87708 206395 53 None -7 16 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 None
1605 2342 117 None -2 4 Rat 8.2 pKi = 8.2 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
Drug Central 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 None
3957 2342 117 None -2 4 Rat 8.2 pKi = 8.2 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
Drug Central 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 None
7216 2342 117 None -2 4 Rat 8.2 pKi = 8.2 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
Drug Central 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 None
CHEMBL998 2342 117 None -2 4 Rat 8.2 pKi = 8.2 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
Drug Central 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 None
DB00455 2342 117 None -2 4 Rat 8.2 pKi = 8.2 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
Drug Central 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 None
2771 195017 74 None -2 27 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL1200781 195017 74 None -2 27 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL549 195017 74 None -2 27 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
2712 916 34 None -5 4 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl None
3370 916 34 None -5 4 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl None
594 916 34 None -5 4 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl None
CHEMBL451 916 34 None -5 4 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl None
DB00475 916 34 None -5 4 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 299 1 1 3 3.0 CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl None
2710 84308 31 3H-MEPYRAMINE -1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 300 3 0 2 3.7 CN1CCN(C(c2ccccc2)c2ccc(Cl)cc2)CC1 None
CHEMBL22150 84308 31 3H-MEPYRAMINE -1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 300 3 0 2 3.7 CN1CCN(C(c2ccccc2)c2ccc(Cl)cc2)CC1 None
2564 206184 51 3H-MEPYRAMINE -2 3 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 290 6 0 3 3.4 CN(C)CCOC(c1ccc(Cl)cc1)c1ccccn1 None
CHEMBL864 206184 51 3H-MEPYRAMINE -2 3 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 290 6 0 3 3.4 CN(C)CCOC(c1ccc(Cl)cc1)c1ccccn1 None
16362 3125 71 None -489 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 3125 71 None -489 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 3125 71 None -489 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 3125 71 None -489 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 3125 71 None -489 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
4806 4008 88 None -5 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
7351 4008 88 None -5 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
9966051 4008 88 None -5 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
CHEMBL2104993 4008 88 None -5 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
DB09068 4008 88 None -5 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human histamine H1 receptorBinding affinity to human histamine H1 receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
3151 1462 97 None -41 27 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
945 1462 97 None -41 27 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
965 1462 97 None -41 27 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
CHEMBL219916 1462 97 None -41 27 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
DB01184 1462 97 None -41 27 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
21722 17992 31 None 1 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 None
CHEMBL126224 17992 31 None 1 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 None
1605 2342 117 None -2 4 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 None
3957 2342 117 None -2 4 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 None
7216 2342 117 None -2 4 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 None
CHEMBL998 2342 117 None -2 4 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 None
DB00455 2342 117 None -2 4 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 None
4976 203579 29 3H-MEPYRAMINE -9 12 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 263 4 1 1 4.3 CNCCCC1c2ccccc2C=Cc2ccccc21 None
CHEMBL668 203579 29 3H-MEPYRAMINE -9 12 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 263 4 1 1 4.3 CNCCCC1c2ccccc2C=Cc2ccccc21 None
2995 204405 53 3H-PYRILAMINE -14 23 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 204405 53 3H-PYRILAMINE -14 23 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 204405 53 3H-PYRILAMINE -14 23 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
4020 205150 39 3H-MEPYRAMINE - 1 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 284 1 1 3 2.6 OC1(c2ccc(Cl)cc2)c2ccccc2C2=NCCN21 None
CHEMBL781 205150 39 3H-MEPYRAMINE - 1 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 284 1 1 3 2.6 OC1(c2ccc(Cl)cc2)c2ccccc2C2=NCCN21 None
2303 3187 68 3H-MEPYRAMINE -363 26 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
4946 3187 68 3H-MEPYRAMINE -363 26 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
564 3187 68 3H-MEPYRAMINE -363 26 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
63 3187 68 3H-MEPYRAMINE -363 26 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
91536 3187 68 3H-MEPYRAMINE -363 26 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 3187 68 3H-MEPYRAMINE -363 26 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 3187 68 3H-MEPYRAMINE -363 26 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
DB00571 3187 68 3H-MEPYRAMINE -363 26 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
45485462 197686 0 UNDEFINED - 1 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 419 8 1 2 6.6 CC1CCC(CCCCN2CCC(C(O)(c3ccccc3)c3ccccc3)CC2)CC1 None
CHEMBL571174 197686 0 UNDEFINED - 1 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 419 8 1 2 6.6 CC1CCC(CCCCN2CCC(C(O)(c3ccccc3)c3ccccc3)CC2)CC1 None
2200 20203 61 3H-MEPYRAMINE -26 2 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 None
CHEMBL1256819 20203 61 3H-MEPYRAMINE -26 2 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 None
CHEMBL1305 20203 61 3H-MEPYRAMINE -26 2 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 None
1224 1432 83 3H-doxepin -2 13 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
3100 1432 83 3H-doxepin -2 13 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
8980 1432 83 3H-doxepin -2 13 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
916 1432 83 3H-doxepin -2 13 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
CHEMBL657 1432 83 3H-doxepin -2 13 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
DB01075 1432 83 3H-doxepin -2 13 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
214 3860 58 3H-doxepin -43 30 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 3860 58 3H-doxepin -43 30 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 3860 58 3H-doxepin -43 30 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 3860 58 3H-doxepin -43 30 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 3860 58 3H-doxepin -43 30 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 3860 58 3H-doxepin -43 30 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
214 3860 58 UNDEFINED -43 30 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 3860 58 UNDEFINED -43 30 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 3860 58 UNDEFINED -43 30 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 3860 58 UNDEFINED -43 30 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 3860 58 UNDEFINED -43 30 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 3860 58 UNDEFINED -43 30 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
11848624 89146 0 UNDEFINED -15 6 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 381 7 1 6 4.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC None
CHEMBL236587 89146 0 UNDEFINED -15 6 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 381 7 1 6 4.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC None
214 3860 58 3H-PYRILAMINE -43 30 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 3860 58 3H-PYRILAMINE -43 30 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 3860 58 3H-PYRILAMINE -43 30 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 3860 58 3H-PYRILAMINE -43 30 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 3860 58 3H-PYRILAMINE -43 30 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 3860 58 3H-PYRILAMINE -43 30 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1204 1932 119 3H-MEPYRAMINE -501 24 Human 4.2 pKi = 4.2 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1932 119 3H-MEPYRAMINE -501 24 Human 4.2 pKi = 4.2 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1932 119 3H-MEPYRAMINE -501 24 Human 4.2 pKi = 4.2 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1932 119 3H-MEPYRAMINE -501 24 Human 4.2 pKi = 4.2 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1932 119 3H-MEPYRAMINE -501 24 Human 4.2 pKi = 4.2 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1932 119 3H-MEPYRAMINE -501 24 Human 4.2 pKi = 4.2 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
13091273 182438 0 UNDEFINED -275 6 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 367 6 1 3 4.3 O=C(CCCN1C2CCC1CC(O)(c1ccccc1)C2)c1ccc(F)cc1 None
CHEMBL478617 182438 0 UNDEFINED -275 6 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 367 6 1 3 4.3 O=C(CCCN1C2CCC1CC(O)(c1ccccc1)C2)c1ccc(F)cc1 None
CHEMBL553327 182438 0 UNDEFINED -275 6 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 367 6 1 3 4.3 O=C(CCCN1C2CCC1CC(O)(c1ccccc1)C2)c1ccc(F)cc1 None
45485529 197718 0 UNDEFINED - 1 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 385 6 1 2 5.2 Cc1ccc(CCN2CCC(C(O)(c3ccccc3)c3ccccc3)CC2)cc1 None
CHEMBL571391 197718 0 UNDEFINED - 1 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 385 6 1 2 5.2 Cc1ccc(CCN2CCC(C(O)(c3ccccc3)c3ccccc3)CC2)cc1 None
54841 203127 52 3H-Histamine -6 27 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 255 6 1 2 3.7 CNCC[C@@H](Oc1ccccc1C)c1ccccc1 None
CHEMBL641 203127 52 3H-Histamine -6 27 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 255 6 1 2 3.7 CNCC[C@@H](Oc1ccccc1C)c1ccccc1 None
68617 205527 62 3H-PYRILAMINE -831 26 Guinea pig 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL1709 205527 62 3H-PYRILAMINE -831 26 Guinea pig 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL809 205527 62 3H-PYRILAMINE -831 26 Guinea pig 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
15723 18539 111 UNDEFINED - 1 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 267 3 2 2 2.9 OC(c1ccccc1)(c1ccccc1)C1CCNCC1 None
CHEMBL127508 18539 111 UNDEFINED - 1 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 267 3 2 2 2.9 OC(c1ccccc1)(c1ccccc1)C1CCNCC1 None
185 4006 60 3H-PYRILAMINE -794 37 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
5311271 4006 60 3H-PYRILAMINE -794 37 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
CHEMBL74355 4006 60 3H-PYRILAMINE -794 37 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
DB16351 4006 60 3H-PYRILAMINE -794 37 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
2470 3653 50 3H-MEPYRAMINE -4570 59 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3653 50 3H-MEPYRAMINE -4570 59 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3653 50 3H-MEPYRAMINE -4570 59 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3653 50 3H-MEPYRAMINE -4570 59 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3653 50 3H-MEPYRAMINE -4570 59 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
1212 1662 50 3H-PYRILAMINE -41 65 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1212 1662 50 3H-MEPYRAMINE -134 65 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1662 50 3H-PYRILAMINE -41 65 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1662 50 3H-MEPYRAMINE -134 65 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1662 50 3H-PYRILAMINE -41 65 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1662 50 3H-MEPYRAMINE -134 65 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1662 50 3H-PYRILAMINE -41 65 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1662 50 3H-MEPYRAMINE -134 65 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1662 50 3H-PYRILAMINE -41 65 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1662 50 3H-MEPYRAMINE -134 65 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2470 3653 50 3H-MEPYRAMINE -20417 59 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3653 50 3H-MEPYRAMINE -20417 59 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3653 50 3H-MEPYRAMINE -20417 59 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3653 50 3H-MEPYRAMINE -20417 59 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3653 50 3H-MEPYRAMINE -20417 59 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
21722 17992 31 3H-MEPYRAMINE 1 6 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 None
CHEMBL126224 17992 31 3H-MEPYRAMINE 1 6 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 None
44591098 176762 0 UNDEFINED -199 6 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 508 9 0 3 6.6 CN(CCC=C1c2ccccc2CCc2ccccc21)C(=O)c1ccc(OCCCN2CCCCC2)cc1 None
CHEMBL460402 176762 0 UNDEFINED -199 6 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 508 9 0 3 6.6 CN(CCC=C1c2ccccc2CCc2ccccc21)C(=O)c1ccc(OCCCN2CCCCC2)cc1 None
16362 3125 71 3H-PYRILAMINE -489 30 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 3125 71 3H-PYRILAMINE -489 30 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 3125 71 3H-PYRILAMINE -489 30 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 3125 71 3H-PYRILAMINE -489 30 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 3125 71 3H-PYRILAMINE -489 30 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
242 470 124 None -23 51 Guinea pig 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 470 124 None -23 51 Guinea pig 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 470 124 None -23 51 Guinea pig 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 470 124 None -23 51 Guinea pig 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 470 124 None -23 51 Guinea pig 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
1613 2348 53 3H-PYRILAMINE -3 44 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2348 53 3H-PYRILAMINE -3 44 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2348 53 3H-PYRILAMINE -3 44 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2348 53 3H-PYRILAMINE -3 44 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2348 53 3H-PYRILAMINE -3 44 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
135398745 2914 112 UNDEFINED 1 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745 2914 112 3H-PYRILAMINE -1 65 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 UNDEFINED 1 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 3H-PYRILAMINE -1 65 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 UNDEFINED 1 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 3H-PYRILAMINE -1 65 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 UNDEFINED 1 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 3H-PYRILAMINE -1 65 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
22530 56130 58 None -1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 2 0 2 3.7 CN1CCc2c(c3ccccc3n2Cc2ccccc2)C1 None
CHEMBL1600878 56130 58 None -1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 2 0 2 3.7 CN1CCc2c(c3ccccc3n2Cc2ccccc2)C1 None
CHEMBL1625607 56130 58 None -1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 2 0 2 3.7 CN1CCc2c(c3ccccc3n2Cc2ccccc2)C1 None
2995 204405 53 None -14 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 204405 53 None -14 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 204405 53 None -14 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
11579 635 0 None - 1 Human 8.1 pKi = 8.1 Binding
inhibition of [3H]-pyrilamine binding to human recombinant histamine H1-receptorsinhibition of [3H]-pyrilamine binding to human recombinant histamine H1-receptors
Drug Central 463 10 1 5 4.9 CCOCCn1c(nc2c1cccc2)C1CCN(CC1)CCc1ccc(cc1)C(C(=O)O)(C)C None
185460 635 0 None - 1 Human 8.1 pKi = 8.1 Binding
inhibition of [3H]-pyrilamine binding to human recombinant histamine H1-receptorsinhibition of [3H]-pyrilamine binding to human recombinant histamine H1-receptors
Drug Central 463 10 1 5 4.9 CCOCCn1c(nc2c1cccc2)C1CCN(CC1)CCc1ccc(cc1)C(C(=O)O)(C)C None
CHEMBL1742423 635 0 None - 1 Human 8.1 pKi = 8.1 Binding
inhibition of [3H]-pyrilamine binding to human recombinant histamine H1-receptorsinhibition of [3H]-pyrilamine binding to human recombinant histamine H1-receptors
Drug Central 463 10 1 5 4.9 CCOCCn1c(nc2c1cccc2)C1CCN(CC1)CCc1ccc(cc1)C(C(=O)O)(C)C None
DB11591 635 0 None - 1 Human 8.1 pKi = 8.1 Binding
inhibition of [3H]-pyrilamine binding to human recombinant histamine H1-receptorsinhibition of [3H]-pyrilamine binding to human recombinant histamine H1-receptors
Drug Central 463 10 1 5 4.9 CCOCCn1c(nc2c1cccc2)C1CCN(CC1)CCc1ccc(cc1)C(C(=O)O)(C)C None
214 3860 58 None -43 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 3860 58 None -43 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 3860 58 None -43 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 3860 58 None -43 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 3860 58 None -43 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 3860 58 None -43 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
242 470 124 None -22 51 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 470 124 None -22 51 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 470 124 None -22 51 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 470 124 None -22 51 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 470 124 None -22 51 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
49831411 217746 0 None -1 15 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 659 19 0 6 8.7 CCCCCCCCCCCC(=O)OCN1C(=O)CCC2=CC=C(OCCCCN3CCN(CC3)C3=C(Cl)C(Cl)=CC=C3)C=C12 None
4976 203579 29 None -1 12 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 263 4 1 1 4.3 CNCCCC1c2ccccc2C=Cc2ccccc21 None
CHEMBL668 203579 29 None -1 12 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 263 4 1 1 4.3 CNCCCC1c2ccccc2C=Cc2ccccc21 None
146159772 2311 33 None 2 3 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 420 4 1 3 4.9 N#C[C@@]1(CC[C@@H](CC1)N1CC[C@]([C@@H](C1)C)(C(=O)O)c1ccccc1)c1ccc(cc1)F None
1564 2311 33 None 2 3 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 420 4 1 3 4.9 N#C[C@@]1(CC[C@@H](CC1)N1CC[C@]([C@@H](C1)C)(C(=O)O)c1ccccc1)c1ccc(cc1)F None
1586 2311 33 None 2 3 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 420 4 1 3 4.9 N#C[C@@]1(CC[C@@H](CC1)N1CC[C@]([C@@H](C1)C)(C(=O)O)c1ccccc1)c1ccc(cc1)F None
54385 2311 33 None 2 3 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 420 4 1 3 4.9 N#C[C@@]1(CC[C@@H](CC1)N1CC[C@]([C@@H](C1)C)(C(=O)O)c1ccccc1)c1ccc(cc1)F None
CHEMBL1615438 2311 33 None 2 3 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 420 4 1 3 4.9 N#C[C@@]1(CC[C@@H](CC1)N1CC[C@]([C@@H](C1)C)(C(=O)O)c1ccccc1)c1ccc(cc1)F None
DB01106 2311 33 None 2 3 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 420 4 1 3 4.9 N#C[C@@]1(CC[C@@H](CC1)N1CC[C@]([C@@H](C1)C)(C(=O)O)c1ccccc1)c1ccc(cc1)F None
2726 919 68 None -6 72 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 68 None -6 72 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 68 None -6 72 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 68 None -6 72 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 68 None -6 72 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1212 1662 50 3H-PYRILAMINE -41 65 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1662 50 3H-PYRILAMINE -41 65 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1662 50 3H-PYRILAMINE -41 65 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1662 50 3H-PYRILAMINE -41 65 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1662 50 3H-PYRILAMINE -41 65 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2865 4143 73 None -58 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4143 73 None -58 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4143 73 None -58 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4143 73 None -58 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4143 73 None -58 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
2337 3256 77 None -1 62 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 77 None -1 62 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 77 None -1 62 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 77 None -1 62 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 77 None -1 62 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2389 3331 118 None -46 67 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 118 None -46 67 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 118 None -46 67 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 118 None -46 67 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 118 None -46 67 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2337 3256 77 3H-PYRILAMINE 1 62 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 77 3H-PYRILAMINE 1 62 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 77 3H-PYRILAMINE 1 62 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 77 3H-PYRILAMINE 1 62 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 77 3H-PYRILAMINE 1 62 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5440 28724 37 None -1 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 None
CHEMBL1378 28724 37 None -1 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 None
11154555 800 62 None -56 12 Human 8.1 pKi = 8.1 Binding
CHO-1 cells, [3H]Pyrilamine (1.5nM)CHO-1 cells, [3H]Pyrilamine (1.5nM)
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
5037 800 62 None -56 12 Human 8.1 pKi = 8.1 Binding
CHO-1 cells, [3H]Pyrilamine (1.5nM)CHO-1 cells, [3H]Pyrilamine (1.5nM)
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
7671 800 62 None -56 12 Human 8.1 pKi = 8.1 Binding
CHO-1 cells, [3H]Pyrilamine (1.5nM)CHO-1 cells, [3H]Pyrilamine (1.5nM)
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL2028019 800 62 None -56 12 Human 8.1 pKi = 8.1 Binding
CHO-1 cells, [3H]Pyrilamine (1.5nM)CHO-1 cells, [3H]Pyrilamine (1.5nM)
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL3085826 800 62 None -56 12 Human 8.1 pKi = 8.1 Binding
CHO-1 cells, [3H]Pyrilamine (1.5nM)CHO-1 cells, [3H]Pyrilamine (1.5nM)
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB06016 800 62 None -56 12 Human 8.1 pKi = 8.1 Binding
CHO-1 cells, [3H]Pyrilamine (1.5nM)CHO-1 cells, [3H]Pyrilamine (1.5nM)
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
2389 3331 118 None -52 67 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysisDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysis
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 118 None -52 67 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysisDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysis
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 118 None -52 67 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysisDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysis
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 118 None -52 67 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysisDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysis
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 118 None -52 67 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysisDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysis
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
3389 217711 0 None -1 26 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 549 12 0 6 6.8 CCCCCCC(=O)OCCN1CCN(CCCN2C3=CC=CC=C3SC3=C2C=C(C=C3)C(F)(F)F)CC1 None
100 3805 58 None -7 55 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3805 58 None -7 55 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3805 58 None -7 55 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3805 58 None -7 55 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3805 58 None -7 55 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
1385580 29276 76 None -1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 None
4615 29276 76 None -1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 None
CHEMBL13828 29276 76 None -1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 None
1588 2325 27 None -35 44 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2325 27 None -35 44 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2325 27 None -35 44 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2325 27 None -35 44 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2325 27 None -35 44 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
11978813 721 79 None -9 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
5014 721 79 None -9 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
7672 721 79 None -9 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
CHEMBL2105760 721 79 None -9 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
DB09128 721 79 None -9 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
2274 3173 58 None -3 31 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 3173 58 None -3 31 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 3173 58 None -3 31 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 3173 58 None -3 31 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 3173 58 None -3 31 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
12488 1657 56 None -2 23 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
941361 1657 56 None -2 23 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
CHEMBL30008 1657 56 None -2 23 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
DB04841 1657 56 None -2 23 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
1212 1662 50 None -41 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1662 50 None -41 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1662 50 None -41 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1662 50 None -41 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1662 50 None -41 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
25271818 12967 58 None -1 2 Guinea pig 8.1 pKi = 8.1 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
Drug Central 337 5 1 3 3.6 CN(C)CC/C=C1/c2ccccc2COc2ccc(CC(=O)O)cc21 None
5281071 12967 58 None -1 2 Guinea pig 8.1 pKi = 8.1 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
Drug Central 337 5 1 3 3.6 CN(C)CC/C=C1/c2ccccc2COc2ccc(CC(=O)O)cc21 None
CHEMBL1189432 12967 58 None -1 2 Guinea pig 8.1 pKi = 8.1 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
Drug Central 337 5 1 3 3.6 CN(C)CC/C=C1/c2ccccc2COc2ccc(CC(=O)O)cc21 None
CHEMBL1719 12967 58 None -1 2 Guinea pig 8.1 pKi = 8.1 Binding
Binding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMBinding affinity for histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
Drug Central 337 5 1 3 3.6 CN(C)CC/C=C1/c2ccccc2COc2ccc(CC(=O)O)cc21 None
2865 4143 73 None -17 53 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4143 73 None -17 53 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4143 73 None -17 53 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4143 73 None -17 53 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4143 73 None -17 53 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
1224 1432 83 None -2 13 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
3100 1432 83 None -2 13 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
8980 1432 83 None -2 13 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
916 1432 83 None -2 13 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
CHEMBL657 1432 83 None -2 13 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
DB01075 1432 83 None -2 13 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
1222 1664 49 None -17 33 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3396 1664 49 None -17 33 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
85 1664 49 None -17 33 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL46516 1664 49 None -17 33 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
DB04842 1664 49 None -17 33 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
1222 881 0 None -1 2 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
2678 881 0 None -1 2 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
581 881 0 None -1 2 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
CHEMBL1000 881 0 None -1 2 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
DB00341 881 0 None -1 2 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
3294 2006 111 None -14 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 2006 111 None -14 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 2006 111 None -14 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 2006 111 None -14 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 2006 111 None -14 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
1214 2068 54 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)[C@@H](c1ccc(cc1)Cl)c1ccccc1 None
1549000 2068 54 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)[C@@H](c1ccc(cc1)Cl)c1ccccc1 None
1566 2068 54 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)[C@@H](c1ccc(cc1)Cl)c1ccccc1 None
28145931 2068 54 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)[C@@H](c1ccc(cc1)Cl)c1ccccc1 None
CHEMBL1201191 2068 54 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)[C@@H](c1ccc(cc1)Cl)c1ccccc1 None
DB06282 2068 54 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)[C@@H](c1ccc(cc1)Cl)c1ccccc1 None
191 403 98 None -56 29 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
201 403 98 None -56 29 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2170 403 98 None -56 29 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
CHEMBL1113 403 98 None -56 29 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
DB00543 403 98 None -56 29 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
4601 206747 35 None -1 16 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
CHEMBL1201023 206747 35 None -1 16 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
CHEMBL900 206747 35 None -1 16 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
1212 1662 50 3H-MEPYRAMINE -41 65 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1662 50 3H-MEPYRAMINE -41 65 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1662 50 3H-MEPYRAMINE -41 65 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1662 50 3H-MEPYRAMINE -41 65 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1662 50 3H-MEPYRAMINE -41 65 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
16667681 216153 0 3H-MEPYRAMINE -33 3 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 390 7 1 5 3.5 CN(C)CCCC1=CC=CC=N1.C1=CC(=CC=C1OC(=O)C=CC(=O)O)Cl None
1204 1932 119 3H-MEPYRAMINE -501 24 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1932 119 3H-MEPYRAMINE -501 24 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1932 119 3H-MEPYRAMINE -501 24 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1932 119 3H-MEPYRAMINE -501 24 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1932 119 3H-MEPYRAMINE -501 24 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1932 119 3H-MEPYRAMINE -501 24 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1353 1911 93 3H-PYRILAMINE -213 83 Guinea pig 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 1911 93 UNDEFINED -602 83 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 3H-PYRILAMINE -213 83 Guinea pig 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 UNDEFINED -602 83 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 3H-PYRILAMINE -213 83 Guinea pig 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 UNDEFINED -602 83 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 3H-PYRILAMINE -213 83 Guinea pig 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 UNDEFINED -602 83 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 3H-PYRILAMINE -213 83 Guinea pig 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 UNDEFINED -602 83 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
73333 5963 31 UNDEFINED -46 9 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 401 7 1 2 4.2 CCNC(=O)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
CHEMBL1079935 5963 31 UNDEFINED -46 9 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 401 7 1 2 4.2 CCNC(=O)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
2771 195017 74 3H-PYRILAMINE -6 27 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL1200781 195017 74 3H-PYRILAMINE -6 27 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL549 195017 74 3H-PYRILAMINE -6 27 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL146246 38278 0 3H-PYRILAMINE -2041 10 Bovine 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 401 5 1 5 2.2 NS(=O)(=O)c1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 None
44591099 176190 0 UNDEFINED -295 6 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 494 10 0 3 7.0 CN(CCC=C1c2ccccc2CCc2ccccc21)Cc1ccc(OCCCN2CCCCC2)cc1 None
CHEMBL459350 176190 0 UNDEFINED -295 6 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 494 10 0 3 7.0 CN(CCC=C1c2ccccc2CCc2ccccc21)Cc1ccc(OCCCN2CCCCC2)cc1 None
1353 1911 93 3H-PYRILAMINE -489 83 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 3H-PYRILAMINE -489 83 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 3H-PYRILAMINE -489 83 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 3H-PYRILAMINE -489 83 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 3H-PYRILAMINE -489 83 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1170 1633 75 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C None
3348 1633 75 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C None
4819 1633 75 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C None
74685737 1633 75 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C None
CHEMBL914 1633 75 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C None
DB00950 1633 75 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C None
3191 102858 97 None 2 25 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
CHEMBL305660 102858 97 None 2 25 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
4066 204626 78 None -1 7 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 None
CHEMBL73451 204626 78 None -1 7 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 None
209 3057 97 3H-PYRILAMINE -11 23 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
209 3057 97 3H-doxepin -11 23 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 3057 97 3H-PYRILAMINE -11 23 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 3057 97 3H-doxepin -11 23 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 3057 97 3H-PYRILAMINE -11 23 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 3057 97 3H-doxepin -11 23 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 3057 97 3H-PYRILAMINE -11 23 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 3057 97 3H-doxepin -11 23 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 3057 97 3H-PYRILAMINE -11 23 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 3057 97 3H-doxepin -11 23 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
90475904 216022 0 3H-MEPYRAMINE -6 6 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(C)CCC(C1=CC=C(C=C1)Cl)C2=CC=CC=N2 None
None 216174 0 3H-MEPYRAMINE 1258 2 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 408 7 2 4 3.9 CC(C1=CC=CC=N1)C2=C(CC3=CC=CC=C32)CCN(C)C.C(=CC(=O)O)C(=O)O None
2398 954 62 None -1 29 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
2801 954 62 None -1 29 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
701 954 62 None -1 29 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
CHEMBL415 954 62 None -1 29 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
DB01242 954 62 None -1 29 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
1547484 940 74 None -1 20 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
654 940 74 None -1 20 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
9072 940 74 None -1 20 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
CHEMBL43064 940 74 None -1 20 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
DB00568 940 74 None -1 20 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
3103 41658 49 None -1 4 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 281 4 0 2 3.9 CN1CCC(OC(c2ccccc2)c2ccccc2)CC1 None
CHEMBL1492 41658 49 None -1 4 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 281 4 0 2 3.9 CN1CCC(OC(c2ccccc2)c2ccccc2)CC1 None
11140 2519 49 None -9 3 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: The pharmacological profile of metopimazine, metopimazine acid (MPZA), domperidone, and metoclopramide were assessed by radioligand binding and by a functional antagonist assay. For the radioligand binding assay, cell membranes of dopamine D2 receptor expressing cells were incubated with [3H]spiperone and competing drugs in buffer. The assay was terminated by rapid filtration, and the bound radioactive signal was determined by liquid scintillation counting.Radioligand Binding Assay: The pharmacological profile of metopimazine, metopimazine acid (MPZA), domperidone, and metoclopramide were assessed by radioligand binding and by a functional antagonist assay. For the radioligand binding assay, cell membranes of dopamine D2 receptor expressing cells were incubated with [3H]spiperone and competing drugs in buffer. The assay was terminated by rapid filtration, and the bound radioactive signal was determined by liquid scintillation counting.
Drug Central 445 6 1 6 3.3 NC(=O)C1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)S(=O)(=O)C None
1784 2519 49 None -9 3 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: The pharmacological profile of metopimazine, metopimazine acid (MPZA), domperidone, and metoclopramide were assessed by radioligand binding and by a functional antagonist assay. For the radioligand binding assay, cell membranes of dopamine D2 receptor expressing cells were incubated with [3H]spiperone and competing drugs in buffer. The assay was terminated by rapid filtration, and the bound radioactive signal was determined by liquid scintillation counting.Radioligand Binding Assay: The pharmacological profile of metopimazine, metopimazine acid (MPZA), domperidone, and metoclopramide were assessed by radioligand binding and by a functional antagonist assay. For the radioligand binding assay, cell membranes of dopamine D2 receptor expressing cells were incubated with [3H]spiperone and competing drugs in buffer. The assay was terminated by rapid filtration, and the bound radioactive signal was determined by liquid scintillation counting.
Drug Central 445 6 1 6 3.3 NC(=O)C1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)S(=O)(=O)C None
26388 2519 49 None -9 3 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: The pharmacological profile of metopimazine, metopimazine acid (MPZA), domperidone, and metoclopramide were assessed by radioligand binding and by a functional antagonist assay. For the radioligand binding assay, cell membranes of dopamine D2 receptor expressing cells were incubated with [3H]spiperone and competing drugs in buffer. The assay was terminated by rapid filtration, and the bound radioactive signal was determined by liquid scintillation counting.Radioligand Binding Assay: The pharmacological profile of metopimazine, metopimazine acid (MPZA), domperidone, and metoclopramide were assessed by radioligand binding and by a functional antagonist assay. For the radioligand binding assay, cell membranes of dopamine D2 receptor expressing cells were incubated with [3H]spiperone and competing drugs in buffer. The assay was terminated by rapid filtration, and the bound radioactive signal was determined by liquid scintillation counting.
Drug Central 445 6 1 6 3.3 NC(=O)C1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)S(=O)(=O)C None
CHEMBL398615 2519 49 None -9 3 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: The pharmacological profile of metopimazine, metopimazine acid (MPZA), domperidone, and metoclopramide were assessed by radioligand binding and by a functional antagonist assay. For the radioligand binding assay, cell membranes of dopamine D2 receptor expressing cells were incubated with [3H]spiperone and competing drugs in buffer. The assay was terminated by rapid filtration, and the bound radioactive signal was determined by liquid scintillation counting.Radioligand Binding Assay: The pharmacological profile of metopimazine, metopimazine acid (MPZA), domperidone, and metoclopramide were assessed by radioligand binding and by a functional antagonist assay. For the radioligand binding assay, cell membranes of dopamine D2 receptor expressing cells were incubated with [3H]spiperone and competing drugs in buffer. The assay was terminated by rapid filtration, and the bound radioactive signal was determined by liquid scintillation counting.
Drug Central 445 6 1 6 3.3 NC(=O)C1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)S(=O)(=O)C None
DB13591 2519 49 None -9 3 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: The pharmacological profile of metopimazine, metopimazine acid (MPZA), domperidone, and metoclopramide were assessed by radioligand binding and by a functional antagonist assay. For the radioligand binding assay, cell membranes of dopamine D2 receptor expressing cells were incubated with [3H]spiperone and competing drugs in buffer. The assay was terminated by rapid filtration, and the bound radioactive signal was determined by liquid scintillation counting.Radioligand Binding Assay: The pharmacological profile of metopimazine, metopimazine acid (MPZA), domperidone, and metoclopramide were assessed by radioligand binding and by a functional antagonist assay. For the radioligand binding assay, cell membranes of dopamine D2 receptor expressing cells were incubated with [3H]spiperone and competing drugs in buffer. The assay was terminated by rapid filtration, and the bound radioactive signal was determined by liquid scintillation counting.
Drug Central 445 6 1 6 3.3 NC(=O)C1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)S(=O)(=O)C None
209 3057 97 None -11 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 3057 97 None -11 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 3057 97 None -11 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 3057 97 None -11 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 3057 97 None -11 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
1210 918 51 None -20 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
1213 918 51 None -20 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
2725 918 51 None -20 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
33036 918 51 None -20 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
4411 918 51 None -20 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
616 918 51 None -20 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
6976 918 51 None -20 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
716121 918 51 None -20 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1201353 918 51 None -20 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1554789 918 51 None -20 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL505 918 51 None -20 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
DB01114 918 51 None -20 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
DB13679 918 51 None -20 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
135398745 2914 112 None 1 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 None 1 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 None 1 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 None 1 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
2267 559 71 None 10 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 None
271 559 71 None 10 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 None
7121 559 71 None 10 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 None
CHEMBL639 559 71 None 10 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 None
DB00972 559 71 None 10 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 None
2726 919 68 None -2 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 68 None -2 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 68 None -2 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 68 None -2 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 68 None -2 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1613 2348 53 None -3 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2348 53 None -3 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2348 53 None -3 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2348 53 None -3 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2348 53 None -3 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
135398745 2914 112 None -2 65 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 None -2 65 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 None -2 65 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 None -2 65 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
6834 205552 45 None -1 2 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 5 0 2 3.9 CN(C)CCC(c1ccc(Br)cc1)c1ccccn1 None
CHEMBL811 205552 45 None -1 2 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 5 0 2 3.9 CN(C)CCC(c1ccc(Br)cc1)c1ccccn1 None
4066 204626 78 None -1 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 None
CHEMBL73451 204626 78 None -1 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 None
115237 55585 119 None -36 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55585 119 None -36 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
25271818 12967 58 None 1 2 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 337 5 1 3 3.6 CN(C)CC/C=C1/c2ccccc2COc2ccc(CC(=O)O)cc21 None
5281071 12967 58 None 1 2 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 337 5 1 3 3.6 CN(C)CC/C=C1/c2ccccc2COc2ccc(CC(=O)O)cc21 None
CHEMBL1189432 12967 58 None 1 2 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 337 5 1 3 3.6 CN(C)CC/C=C1/c2ccccc2COc2ccc(CC(=O)O)cc21 None
CHEMBL1719 12967 58 None 1 2 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 337 5 1 3 3.6 CN(C)CC/C=C1/c2ccccc2COc2ccc(CC(=O)O)cc21 None
180 401 56 3H-MEPYRAMINE -11 40 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 401 56 3H-MEPYRAMINE -11 40 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 401 56 3H-MEPYRAMINE -11 40 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 401 56 3H-MEPYRAMINE -11 40 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 401 56 3H-MEPYRAMINE -11 40 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
209 3057 97 UNDEFINED -11 23 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 3057 97 UNDEFINED -11 23 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 3057 97 UNDEFINED -11 23 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 3057 97 UNDEFINED -11 23 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 3057 97 UNDEFINED -11 23 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
6726 1280 51 None 3 13 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
7151 1280 51 None 3 13 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
749 1280 51 None 3 13 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
CHEMBL648 1280 51 None 3 13 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
DB01176 1280 51 None 3 13 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
212 3806 47 None -5 25 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
2639 3806 47 None -5 25 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
941651 3806 47 None -5 25 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
CHEMBL1201 3806 47 None -5 25 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
DB01623 3806 47 None -5 25 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
1971 2866 38 3H-doxepin -1 30 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
2404 2866 38 3H-doxepin -1 30 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
4543 2866 38 3H-doxepin -1 30 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
CHEMBL445 2866 38 3H-doxepin -1 30 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
DB00540 2866 38 3H-doxepin -1 30 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
19861 207523 50 None - 1 Rat 8.1 pKi = 8.1 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
Drug Central 290 0 0 2 3.7 CN1CCC(=C2c3ccccc3CCc3cccnc32)CC1 None
CHEMBL946 207523 50 None - 1 Rat 8.1 pKi = 8.1 Binding
Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligandBinding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand
Drug Central 290 0 0 2 3.7 CN1CCC(=C2c3ccccc3CCc3cccnc32)CC1 None
135398737 958 93 None -2 89 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysisDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysis
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 None -2 89 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysisDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysis
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 None -2 89 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysisDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysis
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 None -2 89 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysisDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysis
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 None -2 89 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysisDisplacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysis
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
11976 920 59 None -4 24 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
667467 920 59 None -4 24 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
CHEMBL908 920 59 None -4 24 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
DB01239 920 59 None -4 24 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsDisplacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
6075 150108 42 None 2 16 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 None
CHEMBL395110 150108 42 None 2 16 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 None
135398737 958 93 None -4 89 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamineIn vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamine
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 None -4 89 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamineIn vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamine
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 None -4 89 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamineIn vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamine
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 None -4 89 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamineIn vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamine
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 None -4 89 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamineIn vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamine
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
26987 949 33 None 16 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
6063 949 33 None 16 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
671 949 33 None 16 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
CHEMBL1626 949 33 None 16 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
DB00283 949 33 None 16 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
1210 918 51 None -9 21 Rat 8.1 pKi = 8.1 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
1213 918 51 None -9 21 Rat 8.1 pKi = 8.1 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
2725 918 51 None -9 21 Rat 8.1 pKi = 8.1 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
33036 918 51 None -9 21 Rat 8.1 pKi = 8.1 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
4411 918 51 None -9 21 Rat 8.1 pKi = 8.1 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
616 918 51 None -9 21 Rat 8.1 pKi = 8.1 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
6976 918 51 None -9 21 Rat 8.1 pKi = 8.1 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
716121 918 51 None -9 21 Rat 8.1 pKi = 8.1 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1201353 918 51 None -9 21 Rat 8.1 pKi = 8.1 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1554789 918 51 None -9 21 Rat 8.1 pKi = 8.1 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL505 918 51 None -9 21 Rat 8.1 pKi = 8.1 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
DB01114 918 51 None -9 21 Rat 8.1 pKi = 8.1 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
DB13679 918 51 None -9 21 Rat 8.1 pKi = 8.1 Binding
Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranesAbility to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
1400 1957 70 None 2 3 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
3658 1957 70 None 2 3 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
7199 1957 70 None 2 3 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
91513 1957 70 None 2 3 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
CHEMBL896 1957 70 None 2 3 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
DB00557 1957 70 None 2 3 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 None
2284 3182 33 None 1 29 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
4926 3182 33 None 1 29 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
7281 3182 33 None 1 29 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
CHEMBL564 3182 33 None 1 29 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
DB00420 3182 33 None 1 29 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
2600 3779 74 None 1 13 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
2608 3779 74 None 1 13 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
5405 3779 74 None 1 13 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
CHEMBL17157 3779 74 None 1 13 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
DB00342 3779 74 None 1 13 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
5284550 41721 15 None -1 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 None
CHEMBL1492500 41721 15 None -1 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 None
2337 3256 77 UNDEFINED 1 62 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 77 UNDEFINED 1 62 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 77 UNDEFINED 1 62 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 77 UNDEFINED 1 62 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 77 UNDEFINED 1 62 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2337 3256 77 3H-PYRILAMINE 1 62 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 77 3H-PYRILAMINE 1 62 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 77 3H-PYRILAMINE 1 62 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 77 3H-PYRILAMINE 1 62 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 77 3H-PYRILAMINE 1 62 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
4098 32505 30 None 1 11 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 None
CHEMBL1255739 32505 30 None 1 11 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 None
CHEMBL1411979 32505 30 None 1 11 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 None
1712 2492 43 None 1 22 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
4078 2492 43 None 1 22 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
7227 2492 43 None 1 22 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
CHEMBL1088 2492 43 None 1 22 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
DB00933 2492 43 None 1 22 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
1524 2181 96 None -2 52 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2181 96 None -2 52 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2181 96 None -2 52 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2181 96 None -2 52 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2181 96 None -2 52 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2181 96 None -2 52 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
4011 82408 49 None 6 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
CHEMBL21731 82408 49 None 6 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
1816 2540 102 None -3 18 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
4205 2540 102 None -3 18 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
7241 2540 102 None -3 18 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
CHEMBL654 2540 102 None -3 18 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
DB00370 2540 102 None -3 18 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
2895 203592 41 None -1 8 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 275 3 0 1 4.6 CN(C)CCC=C1c2ccccc2C=Cc2ccccc21 None
CHEMBL669 203592 41 None -1 8 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 275 3 0 1 4.6 CN(C)CCC=C1c2ccccc2C=Cc2ccccc21 None
10102 2546 88 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 432 5 1 6 3.4 Fc1ccc(cc1)Cn1c(nc2c1cccc2)N1CCC(CC1)N(c1nccc(=O)[nH]1)C None
1824 2546 88 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 432 5 1 6 3.4 Fc1ccc(cc1)Cn1c(nc2c1cccc2)N1CCC(CC1)N(c1nccc(=O)[nH]1)C None
65906 2546 88 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 432 5 1 6 3.4 Fc1ccc(cc1)Cn1c(nc2c1cccc2)N1CCC(CC1)N(c1nccc(=O)[nH]1)C None
CHEMBL94454 2546 88 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 432 5 1 6 3.4 Fc1ccc(cc1)Cn1c(nc2c1cccc2)N1CCC(CC1)N(c1nccc(=O)[nH]1)C None
DB12523 2546 88 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 432 5 1 6 3.4 Fc1ccc(cc1)Cn1c(nc2c1cccc2)N1CCC(CC1)N(c1nccc(=O)[nH]1)C None
5584 203211 44 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 294 4 0 2 4.1 CC(CN(C)C)CN1c2ccccc2CCc2ccccc21 None
CHEMBL644 203211 44 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 294 4 0 2 4.1 CC(CN(C)C)CN1c2ccccc2CCc2ccccc21 None
3219 199795 60 None - 1 Human 8.1 pKi = 8.1 Binding
Mechanism of ActionMechanism of Action
Drug Central 302 5 0 5 2.2 CCOCCn1c(N2CCCN(C)CC2)nc2ccccc21 None
CHEMBL594 199795 60 None - 1 Human 8.1 pKi = 8.1 Binding
Mechanism of ActionMechanism of Action
Drug Central 302 5 0 5 2.2 CCOCCn1c(N2CCCN(C)CC2)nc2ccccc21 None
2444 14478 26 None 1 2 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 333 6 0 2 4.1 CN(C)CCOC(c1ccccc1)c1ccc(Br)cc1 None
CHEMBL1201245 14478 26 None 1 2 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 333 6 0 2 4.1 CN(C)CCOC(c1ccccc1)c1ccc(Br)cc1 None
1027 1576 73 None -6 2 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 None
3241 1576 73 None -6 2 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 None
7176 1576 73 None -6 2 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 None
CHEMBL1106 1576 73 None -6 2 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 None
DB00751 1576 73 None -6 2 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 None
6761 67799 19 None -1 18 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL1909072 67799 19 None -1 18 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 None
1201549 597 24 None -1 20 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
333 597 24 None -1 20 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
7601 597 24 None -1 20 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
CHEMBL1201203 597 24 None -1 20 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
CHEMBL438151 597 24 None -1 20 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
DB00245 597 24 None -1 20 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
16667681 216153 0 3H-trans-H2-PAT,(-) -4 3 Guinea pig 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 390 7 1 5 3.5 CN(C)CCCC1=CC=CC=N1.C1=CC(=CC=C1OC(=O)C=CC(=O)O)Cl None
1353 1911 93 3H-MEPYRAMINE -213 83 Guinea pig 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 3H-MEPYRAMINE -213 83 Guinea pig 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 3H-MEPYRAMINE -213 83 Guinea pig 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 3H-MEPYRAMINE -213 83 Guinea pig 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 3H-MEPYRAMINE -213 83 Guinea pig 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
62857 216181 0 3H-PYRILAMINE -12 7 Guinea pig 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 345 6 1 2 4.9 CNCCC(C1=CC=CC=C1)OC2=CC=C(C=C2)C(F)(F)F.Cl None
24740862 148008 0 UNDEFINED -4 5 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 369 6 1 5 4.4 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1F None
CHEMBL393436 148008 0 UNDEFINED -4 5 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 369 6 1 5 4.4 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1F None
3033769 3281 61 3H-PYRILAMINE -2344 19 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
3033769 3281 61 3H-MEPYRAMINE -2344 19 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
3299 3281 61 3H-PYRILAMINE -2344 19 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
3299 3281 61 3H-MEPYRAMINE -2344 19 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
94 3281 61 3H-PYRILAMINE -2344 19 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
94 3281 61 3H-MEPYRAMINE -2344 19 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
CHEMBL8809 3281 61 3H-PYRILAMINE -2344 19 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
CHEMBL8809 3281 61 3H-MEPYRAMINE -2344 19 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
DB12518 3281 61 3H-PYRILAMINE -2344 19 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
DB12518 3281 61 3H-MEPYRAMINE -2344 19 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
13091268 78224 0 UNDEFINED -9549 14 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 None
CHEMBL210578 78224 0 UNDEFINED -9549 14 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 None
2389 3331 118 UNDEFINED -346 67 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 118 UNDEFINED -346 67 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 118 UNDEFINED -346 67 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 118 UNDEFINED -346 67 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 118 UNDEFINED -346 67 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2995 204405 53 3H-Histamine -42 23 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 204405 53 3H-Histamine -42 23 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 204405 53 3H-Histamine -42 23 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
46780481 107531 20 None -13 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107531 20 None -13 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107531 20 None -13 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107531 20 None -13 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
2726 919 68 3H-MEPYRAMINE -2 72 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
2726 919 68 3H-doxepin -2 72 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 68 3H-MEPYRAMINE -2 72 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 68 3H-doxepin -2 72 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 68 3H-MEPYRAMINE -2 72 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 68 3H-doxepin -2 72 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 68 3H-MEPYRAMINE -2 72 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 68 3H-doxepin -2 72 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 68 3H-MEPYRAMINE -2 72 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 68 3H-doxepin -2 72 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
2710 84308 31 3H-MEPYRAMINE -1 3 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 300 3 0 2 3.7 CN1CCN(C(c2ccccc2)c2ccc(Cl)cc2)CC1 None
CHEMBL22150 84308 31 3H-MEPYRAMINE -1 3 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 300 3 0 2 3.7 CN1CCN(C(c2ccccc2)c2ccc(Cl)cc2)CC1 None
135 2532 43 None -1 58 Guinea pig 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 43 None -1 58 Guinea pig 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 43 None -1 58 Guinea pig 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 43 None -1 58 Guinea pig 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 43 None -1 58 Guinea pig 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
2726 919 68 UNDEFINED -2 72 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 68 UNDEFINED -2 72 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 68 UNDEFINED -2 72 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 68 UNDEFINED -2 72 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 68 UNDEFINED -2 72 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1227 2489 43 None -2 12 Human 8.0 pKi = 8.0 Binding
GRAC: human H1 selective antagonistGRAC: human H1 selective antagonist
Drug Central 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
2331 2489 43 None -2 12 Human 8.0 pKi = 8.0 Binding
GRAC: human H1 selective antagonistGRAC: human H1 selective antagonist
Drug Central 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
3957 2489 43 None -2 12 Human 8.0 pKi = 8.0 Binding
GRAC: human H1 selective antagonistGRAC: human H1 selective antagonist
Drug Central 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
4992 2489 43 None -2 12 Human 8.0 pKi = 8.0 Binding
GRAC: human H1 selective antagonistGRAC: human H1 selective antagonist
Drug Central 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
CHEMBL511 2489 43 None -2 12 Human 8.0 pKi = 8.0 Binding
GRAC: human H1 selective antagonistGRAC: human H1 selective antagonist
Drug Central 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
DB06691 2489 43 None -2 12 Human 8.0 pKi = 8.0 Binding
GRAC: human H1 selective antagonistGRAC: human H1 selective antagonist
Drug Central 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C None
1228 3866 34 3H-MEPYRAMINE -10 4 Mouse 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
2763 3866 34 3H-MEPYRAMINE -10 4 Mouse 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
5282443 3866 34 3H-MEPYRAMINE -10 4 Mouse 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
CHEMBL855 3866 34 3H-MEPYRAMINE -10 4 Mouse 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
DB00427 3866 34 3H-MEPYRAMINE -10 4 Mouse 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
1210 918 51 None -20 21 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
1213 918 51 None -20 21 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
2725 918 51 None -20 21 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
33036 918 51 None -20 21 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
4411 918 51 None -20 21 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
616 918 51 None -20 21 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
6976 918 51 None -20 21 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
716121 918 51 None -20 21 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1201353 918 51 None -20 21 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1554789 918 51 None -20 21 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL505 918 51 None -20 21 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
DB01114 918 51 None -20 21 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
DB13679 918 51 None -20 21 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
21855 84246 42 None 7 6 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 292 5 0 2 4.1 CC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 None
CHEMBL22108 84246 42 None 7 6 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 292 5 0 2 4.1 CC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 None
135398737 958 93 None 2 89 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 None 2 89 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 None 2 89 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 None 2 89 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 None 2 89 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1224 1432 83 3H-MEPYRAMINE 1 13 Guinea pig 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
3100 1432 83 3H-MEPYRAMINE 1 13 Guinea pig 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
8980 1432 83 3H-MEPYRAMINE 1 13 Guinea pig 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
916 1432 83 3H-MEPYRAMINE 1 13 Guinea pig 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
CHEMBL657 1432 83 3H-MEPYRAMINE 1 13 Guinea pig 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
DB01075 1432 83 3H-MEPYRAMINE 1 13 Guinea pig 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
103 4153 61 None -1 53 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human H1 receptorBinding affinity towards human H1 receptor
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4153 61 None -1 53 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human H1 receptorBinding affinity towards human H1 receptor
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4153 61 None -1 53 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human H1 receptorBinding affinity towards human H1 receptor
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4153 61 None -1 53 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human H1 receptorBinding affinity towards human H1 receptor
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4153 61 None -1 53 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human H1 receptorBinding affinity towards human H1 receptor
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
135 2532 43 None -1 58 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 43 None -1 58 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 43 None -1 58 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 43 None -1 58 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 43 None -1 58 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
72287 61061 38 None 6 2 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 328 5 0 4 4.5 COc1ccc2c(c1)N(C[C@H](C)CN(C)C)c1ccccc1S2 None
CHEMBL1764 61061 38 None 6 2 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 328 5 0 4 4.5 COc1ccc2c(c1)N(C[C@H](C)CN(C)C)c1ccccc1S2 None
2435 3590 83 None -95 48 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cellsDisplacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cells
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3590 83 None -95 48 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cellsDisplacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cells
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3590 83 None -95 48 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cellsDisplacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cells
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3590 83 None -95 48 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cellsDisplacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cells
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3590 83 None -95 48 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cellsDisplacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cells
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
180 401 56 None -1 40 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 401 56 None -1 40 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 401 56 None -1 40 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 401 56 None -1 40 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 401 56 None -1 40 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
62865 1274 0 3H-PYRILAMINE -3 14 Guinea pig 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
746 1274 0 3H-PYRILAMINE -3 14 Guinea pig 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
84 1274 0 3H-PYRILAMINE -3 14 Guinea pig 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
CHEMBL2104153 1274 0 3H-PYRILAMINE -3 14 Guinea pig 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
DB09000 1274 0 3H-PYRILAMINE -3 14 Guinea pig 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
46780481 107531 20 3H-PYRILAMINE -13 53 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107531 20 3H-PYRILAMINE -13 53 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107531 20 3H-PYRILAMINE -13 53 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107531 20 3H-PYRILAMINE -13 53 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
None 215992 0 3H-MEPYRAMINE 1 11 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 522 10 0 3 6.2 C1CN(CCN1CCCC2=CC=CC=C2)CCOC(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F.Cl.Cl None
124087 1389 114 None 3 15 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
7157 1389 114 None 3 15 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
814 1389 114 None 3 15 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
CHEMBL1172 1389 114 None 3 15 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
DB00967 1389 114 None 3 15 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
1530 2182 50 None -5 21 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
3827 2182 50 None -5 21 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
7206 2182 50 None -5 21 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
CHEMBL534 2182 50 None -5 21 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
DB00920 2182 50 None -5 21 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
1530 2182 50 None 5 21 Guinea pig 8.0 pKi = 8.0 Binding
The compound was tested in vitro for binding affinity against histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMThe compound was tested in vitro for binding affinity against histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
3827 2182 50 None 5 21 Guinea pig 8.0 pKi = 8.0 Binding
The compound was tested in vitro for binding affinity against histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMThe compound was tested in vitro for binding affinity against histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
7206 2182 50 None 5 21 Guinea pig 8.0 pKi = 8.0 Binding
The compound was tested in vitro for binding affinity against histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMThe compound was tested in vitro for binding affinity against histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
CHEMBL534 2182 50 None 5 21 Guinea pig 8.0 pKi = 8.0 Binding
The compound was tested in vitro for binding affinity against histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMThe compound was tested in vitro for binding affinity against histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
DB00920 2182 50 None 5 21 Guinea pig 8.0 pKi = 8.0 Binding
The compound was tested in vitro for binding affinity against histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uMThe compound was tested in vitro for binding affinity against histamine H1 receptor from guinea pig cerebellum, using [3H]pyrilamine as radioligand at 0.1 uM
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
135398745 2914 112 None -1 65 Rat 8.0 pKi = 8.0 Binding
Half-maximal inhibition of [3H]7-OH-DPAT binding to Histamine H1 receptor in rat tissue homogenateHalf-maximal inhibition of [3H]7-OH-DPAT binding to Histamine H1 receptor in rat tissue homogenate
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 None -1 65 Rat 8.0 pKi = 8.0 Binding
Half-maximal inhibition of [3H]7-OH-DPAT binding to Histamine H1 receptor in rat tissue homogenateHalf-maximal inhibition of [3H]7-OH-DPAT binding to Histamine H1 receptor in rat tissue homogenate
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 None -1 65 Rat 8.0 pKi = 8.0 Binding
Half-maximal inhibition of [3H]7-OH-DPAT binding to Histamine H1 receptor in rat tissue homogenateHalf-maximal inhibition of [3H]7-OH-DPAT binding to Histamine H1 receptor in rat tissue homogenate
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 None -1 65 Rat 8.0 pKi = 8.0 Binding
Half-maximal inhibition of [3H]7-OH-DPAT binding to Histamine H1 receptor in rat tissue homogenateHalf-maximal inhibition of [3H]7-OH-DPAT binding to Histamine H1 receptor in rat tissue homogenate
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
1224 1432 83 3H-trans-H2-PAT,(-) 1 13 Guinea pig 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
1224 1432 83 3H-MEPYRAMINE -2 13 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
3100 1432 83 3H-trans-H2-PAT,(-) 1 13 Guinea pig 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
3100 1432 83 3H-MEPYRAMINE -2 13 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
8980 1432 83 3H-trans-H2-PAT,(-) 1 13 Guinea pig 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
8980 1432 83 3H-MEPYRAMINE -2 13 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
916 1432 83 3H-trans-H2-PAT,(-) 1 13 Guinea pig 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
916 1432 83 3H-MEPYRAMINE -2 13 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
CHEMBL657 1432 83 3H-trans-H2-PAT,(-) 1 13 Guinea pig 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
CHEMBL657 1432 83 3H-MEPYRAMINE -2 13 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
DB01075 1432 83 3H-trans-H2-PAT,(-) 1 13 Guinea pig 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
DB01075 1432 83 3H-MEPYRAMINE -2 13 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
2286 3183 51 None -2 30 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
4927 3183 51 None -2 30 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
7282 3183 51 None -2 30 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
CHEMBL643 3183 51 None -2 30 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
DB01069 3183 51 None -2 30 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
1238 203174 24 None -38 16 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cellsDisplacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cells
Drug Central 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL64249 203174 24 None -38 16 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cellsDisplacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cells
Drug Central 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
1225 1471 26 None -1 22 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
3958 1471 26 None -1 22 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667477 1471 26 None -1 22 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
CHEMBL860 1471 26 None -1 22 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
DB01142 1471 26 None -1 22 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
1228 3866 34 None -5 4 Human 8.0 pKi = 8 Binding
GRAC: human H1 selective antagonistGRAC: human H1 selective antagonist
Drug Central 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
2763 3866 34 None -5 4 Human 8.0 pKi = 8 Binding
GRAC: human H1 selective antagonistGRAC: human H1 selective antagonist
Drug Central 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
5282443 3866 34 None -5 4 Human 8.0 pKi = 8 Binding
GRAC: human H1 selective antagonistGRAC: human H1 selective antagonist
Drug Central 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
CHEMBL855 3866 34 None -5 4 Human 8.0 pKi = 8 Binding
GRAC: human H1 selective antagonistGRAC: human H1 selective antagonist
Drug Central 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
DB00427 3866 34 None -5 4 Human 8.0 pKi = 8 Binding
GRAC: human H1 selective antagonistGRAC: human H1 selective antagonist
Drug Central 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 None
134 2514 24 3H-MEPYRAMINE -933 67 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 24 3H-MEPYRAMINE -933 67 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 24 3H-MEPYRAMINE -933 67 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 24 3H-MEPYRAMINE -933 67 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 24 3H-MEPYRAMINE -933 67 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
114743 216101 0 3H-PYRILAMINE -5 8 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 291 1 1 1 4.9 C1CC(C2=CC=CC=C2C1C3=CC(=C(C=C3)Cl)Cl)N None
10065083 32103 1 UNDEFINED -141 10 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 328 6 0 5 2.4 O=C(CCCN1CCN(c2ncccn2)CC1)c1ccc(F)cc1 None
CHEMBL140872 32103 1 UNDEFINED -141 10 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 328 6 0 5 2.4 O=C(CCCN1CCN(c2ncccn2)CC1)c1ccc(F)cc1 None
46882133 5808 0 UNDEFINED -5 7 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 478 9 2 7 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(NC(=O)C5CCC5)ccc4o3)CC2)ccc1OC None
CHEMBL1078896 5808 0 UNDEFINED -5 7 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 478 9 2 7 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(NC(=O)C5CCC5)ccc4o3)CC2)ccc1OC None
1209 1658 75 3H-PYRILAMINE -223 32 Guinea pig 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
203 1658 75 3H-PYRILAMINE -223 32 Guinea pig 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
3386 1658 75 3H-PYRILAMINE -223 32 Guinea pig 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL41 1658 75 3H-PYRILAMINE -223 32 Guinea pig 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
DB00472 1658 75 3H-PYRILAMINE -223 32 Guinea pig 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
44350664 118149 0 UNDEFINED -9 6 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 351 6 0 2 5.2 O=C(CCCN1C2CCC1CC(c1ccccc1)C2)c1ccc(F)cc1 None
CHEMBL340816 118149 0 UNDEFINED -9 6 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 351 6 0 2 5.2 O=C(CCCN1C2CCC1CC(c1ccccc1)C2)c1ccc(F)cc1 None
CHEMBL553417 118149 0 UNDEFINED -9 6 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 351 6 0 2 5.2 O=C(CCCN1C2CCC1CC(c1ccccc1)C2)c1ccc(F)cc1 None
16667681 216153 0 3H-MEPYRAMINE -4 3 Guinea pig 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 390 7 1 5 3.5 CN(C)CCCC1=CC=CC=N1.C1=CC(=CC=C1OC(=O)C=CC(=O)O)Cl None
1204 1932 119 3H-trans-H2-PAT,(-) -46 24 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1932 119 3H-trans-H2-PAT,(-) -46 24 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1932 119 3H-trans-H2-PAT,(-) -46 24 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1932 119 3H-trans-H2-PAT,(-) -46 24 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1932 119 3H-trans-H2-PAT,(-) -46 24 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1932 119 3H-trans-H2-PAT,(-) -46 24 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
180 401 56 None -1 40 Human 9.3 pKi = 9.3 Binding
Antagonism of [<sup>3</sup>H]mepyramine bindingAntagonism of [<sup>3</sup>H]mepyramine binding
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 16782354
200 401 56 None -1 40 Human 9.3 pKi = 9.3 Binding
Antagonism of [<sup>3</sup>H]mepyramine bindingAntagonism of [<sup>3</sup>H]mepyramine binding
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 16782354
2160 401 56 None -1 40 Human 9.3 pKi = 9.3 Binding
Antagonism of [<sup>3</sup>H]mepyramine bindingAntagonism of [<sup>3</sup>H]mepyramine binding
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 16782354
CHEMBL629 401 56 None -1 40 Human 9.3 pKi = 9.3 Binding
Antagonism of [<sup>3</sup>H]mepyramine bindingAntagonism of [<sup>3</sup>H]mepyramine binding
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 16782354
DB00321 401 56 None -1 40 Human 9.3 pKi = 9.3 Binding
Antagonism of [<sup>3</sup>H]mepyramine bindingAntagonism of [<sup>3</sup>H]mepyramine binding
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 16782354
11753159 547 6 None -1 2 Human 7.5 pKi = 7.5 Binding
Assayed using the sodium salt of the compoundAssayed using the sodium salt of the compound
Guide to Pharmacology 525 5 1 5 4.7 Cc1ccc(cc1)S(=O)(=O)NC(=O)N1CCC(CC1)N1CCC(CC1)Oc1ccc(c(c1)Cl)Cl 23031591
7679 547 6 None -1 2 Human 7.5 pKi = 7.5 Binding
Assayed using the sodium salt of the compoundAssayed using the sodium salt of the compound
Guide to Pharmacology 525 5 1 5 4.7 Cc1ccc(cc1)S(=O)(=O)NC(=O)N1CCC(CC1)N1CCC(CC1)Oc1ccc(c(c1)Cl)Cl 23031591
CHEMBL2158814 547 6 None -1 2 Human 7.5 pKi = 7.5 Binding
Assayed using the sodium salt of the compoundAssayed using the sodium salt of the compound
Guide to Pharmacology 525 5 1 5 4.7 Cc1ccc(cc1)S(=O)(=O)NC(=O)N1CCC(CC1)N1CCC(CC1)Oc1ccc(c(c1)Cl)Cl 23031591
11579 635 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding to human recombinant histamine H<sub>1</sub> receptorsBinding to human recombinant histamine H<sub>1</sub> receptors
Guide to Pharmacology 463 10 1 5 4.9 CCOCCn1c(nc2c1cccc2)C1CCN(CC1)CCc1ccc(cc1)C(C(=O)O)(C)C 16274260
185460 635 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding to human recombinant histamine H<sub>1</sub> receptorsBinding to human recombinant histamine H<sub>1</sub> receptors
Guide to Pharmacology 463 10 1 5 4.9 CCOCCn1c(nc2c1cccc2)C1CCN(CC1)CCc1ccc(cc1)C(C(=O)O)(C)C 16274260
CHEMBL1742423 635 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding to human recombinant histamine H<sub>1</sub> receptorsBinding to human recombinant histamine H<sub>1</sub> receptors
Guide to Pharmacology 463 10 1 5 4.9 CCOCCn1c(nc2c1cccc2)C1CCN(CC1)CCc1ccc(cc1)C(C(=O)O)(C)C 16274260
DB11591 635 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding to human recombinant histamine H<sub>1</sub> receptorsBinding to human recombinant histamine H<sub>1</sub> receptors
Guide to Pharmacology 463 10 1 5 4.9 CCOCCn1c(nc2c1cccc2)C1CCN(CC1)CCc1ccc(cc1)C(C(=O)O)(C)C 16274260
2749 344 40 None 1 2 Bovine 9.1 pKi = 9.1 Binding
Inhibition of [<sup>3</sup>H]mepyramine binding to bovine brain membrane preparations <i>in vitro</i>.Inhibition of [<sup>3</sup>H]mepyramine binding to bovine brain membrane preparations <i>in vitro</i>.
Guide to Pharmacology 298 4 0 3 4.5 CN(CC(CN1c2ccccc2Sc2c1cccc2)C)C 2884340
5574 344 40 None 1 2 Bovine 9.1 pKi = 9.1 Binding
Inhibition of [<sup>3</sup>H]mepyramine binding to bovine brain membrane preparations <i>in vitro</i>.Inhibition of [<sup>3</sup>H]mepyramine binding to bovine brain membrane preparations <i>in vitro</i>.
Guide to Pharmacology 298 4 0 3 4.5 CN(CC(CN1c2ccccc2Sc2c1cccc2)C)C 2884340
7237 344 40 None 1 2 Bovine 9.1 pKi = 9.1 Binding
Inhibition of [<sup>3</sup>H]mepyramine binding to bovine brain membrane preparations <i>in vitro</i>.Inhibition of [<sup>3</sup>H]mepyramine binding to bovine brain membrane preparations <i>in vitro</i>.
Guide to Pharmacology 298 4 0 3 4.5 CN(CC(CN1c2ccccc2Sc2c1cccc2)C)C 2884340
CHEMBL829 344 40 None 1 2 Bovine 9.1 pKi = 9.1 Binding
Inhibition of [<sup>3</sup>H]mepyramine binding to bovine brain membrane preparations <i>in vitro</i>.Inhibition of [<sup>3</sup>H]mepyramine binding to bovine brain membrane preparations <i>in vitro</i>.
Guide to Pharmacology 298 4 0 3 4.5 CN(CC(CN1c2ccccc2Sc2c1cccc2)C)C 2884340
DB01246 344 40 None 1 2 Bovine 9.1 pKi = 9.1 Binding
Inhibition of [<sup>3</sup>H]mepyramine binding to bovine brain membrane preparations <i>in vitro</i>.Inhibition of [<sup>3</sup>H]mepyramine binding to bovine brain membrane preparations <i>in vitro</i>.
Guide to Pharmacology 298 4 0 3 4.5 CN(CC(CN1c2ccccc2Sc2c1cccc2)C)C 2884340
10102 2546 88 None - 1 Human 8.6 pKi = 8.6 Binding
Radioligand displacement membrane binding assay using CHO cells expressing the human H1 receptor and [3H]pyrilamine as tracer.Radioligand displacement membrane binding assay using CHO cells expressing the human H1 receptor and [3H]pyrilamine as tracer.
Guide to Pharmacology 432 5 1 6 3.4 Fc1ccc(cc1)Cn1c(nc2c1cccc2)N1CCC(CC1)N(c1nccc(=O)[nH]1)C 19553115
1824 2546 88 None - 1 Human 8.6 pKi = 8.6 Binding
Radioligand displacement membrane binding assay using CHO cells expressing the human H1 receptor and [3H]pyrilamine as tracer.Radioligand displacement membrane binding assay using CHO cells expressing the human H1 receptor and [3H]pyrilamine as tracer.
Guide to Pharmacology 432 5 1 6 3.4 Fc1ccc(cc1)Cn1c(nc2c1cccc2)N1CCC(CC1)N(c1nccc(=O)[nH]1)C 19553115
65906 2546 88 None - 1 Human 8.6 pKi = 8.6 Binding
Radioligand displacement membrane binding assay using CHO cells expressing the human H1 receptor and [3H]pyrilamine as tracer.Radioligand displacement membrane binding assay using CHO cells expressing the human H1 receptor and [3H]pyrilamine as tracer.
Guide to Pharmacology 432 5 1 6 3.4 Fc1ccc(cc1)Cn1c(nc2c1cccc2)N1CCC(CC1)N(c1nccc(=O)[nH]1)C 19553115
CHEMBL94454 2546 88 None - 1 Human 8.6 pKi = 8.6 Binding
Radioligand displacement membrane binding assay using CHO cells expressing the human H1 receptor and [3H]pyrilamine as tracer.Radioligand displacement membrane binding assay using CHO cells expressing the human H1 receptor and [3H]pyrilamine as tracer.
Guide to Pharmacology 432 5 1 6 3.4 Fc1ccc(cc1)Cn1c(nc2c1cccc2)N1CCC(CC1)N(c1nccc(=O)[nH]1)C 19553115
DB12523 2546 88 None - 1 Human 8.6 pKi = 8.6 Binding
Radioligand displacement membrane binding assay using CHO cells expressing the human H1 receptor and [3H]pyrilamine as tracer.Radioligand displacement membrane binding assay using CHO cells expressing the human H1 receptor and [3H]pyrilamine as tracer.
Guide to Pharmacology 432 5 1 6 3.4 Fc1ccc(cc1)Cn1c(nc2c1cccc2)N1CCC(CC1)N(c1nccc(=O)[nH]1)C 19553115
277 1301 62 None -2 50 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 7925364
2913 1301 62 None -2 50 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 7925364
765 1301 62 None -2 50 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 7925364
CHEMBL516 1301 62 None -2 50 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 7925364
DB00434 1301 62 None -2 50 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 7925364
26987 949 33 None 16 21 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
6063 949 33 None 16 21 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
671 949 33 None 16 21 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
CHEMBL1626 949 33 None 16 21 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
DB00283 949 33 None 16 21 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
10447834 1933 4 None -1862 5 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 15947036
4026 1933 4 None -1862 5 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 15947036
CHEMBL275507 1933 4 None -1862 5 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 15947036
5048 3133 64 None -109 7 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 26084539
8924 3133 64 None -109 7 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 26084539
9948102 3133 64 None -109 7 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 26084539
CHEMBL462605 3133 64 None -109 7 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 26084539
DB11642 3133 64 None -109 7 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 26084539
10403687 2511 3 None -331 5 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 12626648
1205 2511 3 None -331 5 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 12626648
CHEMBL275035 2511 3 None -331 5 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 12626648
1210 918 51 None -20 21 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 12065734
1213 918 51 None -20 21 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 12065734
2725 918 51 None -20 21 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 12065734
33036 918 51 None -20 21 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 12065734
4411 918 51 None -20 21 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 12065734
616 918 51 None -20 21 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 12065734
6976 918 51 None -20 21 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 12065734
716121 918 51 None -20 21 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 12065734
CHEMBL1201353 918 51 None -20 21 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 12065734
CHEMBL1554789 918 51 None -20 21 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 12065734
CHEMBL505 918 51 None -20 21 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 12065734
DB01114 918 51 None -20 21 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 12065734
DB13679 918 51 None -20 21 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 12065734
1215 2083 0 None - 1 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)[C@H](c1ccc(cc1)Cl)c1ccccc1 15206929
150716 2083 0 None - 1 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)[C@H](c1ccc(cc1)Cl)c1ccccc1 15206929
28145930 2083 0 None - 1 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)[C@H](c1ccc(cc1)Cl)c1ccccc1 15206929
CHEMBL1334217 2083 0 None - 1 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)[C@H](c1ccc(cc1)Cl)c1ccccc1 15206929
10104 3566 12 None -2 6 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 12593665
6604866 3566 12 None -2 6 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 12593665
CHEMBL1493369 3566 12 None -2 6 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 12593665
2600 3779 74 None 1 13 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 19660947
2608 3779 74 None 1 13 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 19660947
5405 3779 74 None 1 13 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 19660947
CHEMBL17157 3779 74 None 1 13 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 19660947
DB00342 3779 74 None 1 13 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 19660947
1605 2342 117 None -2 4 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 15771458
3957 2342 117 None -2 4 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 15771458
7216 2342 117 None -2 4 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 15771458
CHEMBL998 2342 117 None -2 4 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 15771458
DB00455 2342 117 None -2 4 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 15771458
1170 1633 75 None - 1 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 19660947
3348 1633 75 None - 1 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 19660947
4819 1633 75 None - 1 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 19660947
74685737 1633 75 None - 1 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 19660947
CHEMBL914 1633 75 None - 1 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 19660947
DB00950 1633 75 None - 1 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 501 10 3 4 5.5 OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C 19660947
1224 1432 83 None -2 13 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 12065734
3100 1432 83 None -2 13 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 12065734
8980 1432 83 None -2 13 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 12065734
916 1432 83 None -2 13 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 12065734
CHEMBL657 1432 83 None -2 13 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 12065734
DB01075 1432 83 None -2 13 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 12065734
1210 918 51 None -20 21 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 21381763
1213 918 51 None -20 21 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 21381763
2725 918 51 None -20 21 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 21381763
33036 918 51 None -20 21 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 21381763
4411 918 51 None -20 21 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 21381763
616 918 51 None -20 21 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 21381763
6976 918 51 None -20 21 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 21381763
716121 918 51 None -20 21 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 21381763
CHEMBL1201353 918 51 None -20 21 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 21381763
CHEMBL1554789 918 51 None -20 21 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 21381763
CHEMBL505 918 51 None -20 21 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 21381763
DB01114 918 51 None -20 21 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 21381763
DB13679 918 51 None -20 21 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 21381763
1222 881 0 None -1 2 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 7925364
2678 881 0 None -1 2 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 7925364
581 881 0 None -1 2 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 7925364
CHEMBL1000 881 0 None -1 2 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 7925364
DB00341 881 0 None -1 2 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 7925364
6726 1280 51 None 3 13 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
7151 1280 51 None 3 13 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
749 1280 51 None 3 13 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
CHEMBL648 1280 51 None 3 13 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
DB01176 1280 51 None 3 13 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
5282426 1466 0 None 4 6 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 3 0 2 4.7 CN(CC/C=C/1\c2ccccc2SCc2c1cccc2)C 10379421
7549 1466 0 None 4 6 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 3 0 2 4.7 CN(CC/C=C/1\c2ccccc2SCc2c1cccc2)C 10379421
CHEMBL108947 1466 0 None 4 6 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 3 0 2 4.7 CN(CC/C=C/1\c2ccccc2SCc2c1cccc2)C 10379421
11976 920 59 None -4 24 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 19091563
667467 920 59 None -4 24 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 19091563
CHEMBL908 920 59 None -4 24 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 19091563
DB01239 920 59 None -4 24 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 19091563
1210 918 51 None -20 21 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 12065734
1210 918 51 None -20 21 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 7925364
1213 918 51 None -20 21 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 12065734
1213 918 51 None -20 21 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 7925364
2725 918 51 None -20 21 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 12065734
2725 918 51 None -20 21 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 7925364
33036 918 51 None -20 21 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 12065734
33036 918 51 None -20 21 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 7925364
4411 918 51 None -20 21 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 12065734
4411 918 51 None -20 21 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 7925364
616 918 51 None -20 21 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 12065734
616 918 51 None -20 21 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 7925364
6976 918 51 None -20 21 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 12065734
6976 918 51 None -20 21 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 7925364
716121 918 51 None -20 21 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 12065734
716121 918 51 None -20 21 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 7925364
CHEMBL1201353 918 51 None -20 21 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 12065734
CHEMBL1201353 918 51 None -20 21 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 7925364
CHEMBL1554789 918 51 None -20 21 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 12065734
CHEMBL1554789 918 51 None -20 21 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 7925364
CHEMBL505 918 51 None -20 21 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 12065734
CHEMBL505 918 51 None -20 21 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 7925364
DB01114 918 51 None -20 21 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 12065734
DB01114 918 51 None -20 21 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 7925364
DB13679 918 51 None -20 21 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 12065734
DB13679 918 51 None -20 21 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 7925364
1214 2068 54 None - 1 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)[C@@H](c1ccc(cc1)Cl)c1ccccc1 15206929
1549000 2068 54 None - 1 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)[C@@H](c1ccc(cc1)Cl)c1ccccc1 15206929
1566 2068 54 None - 1 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)[C@@H](c1ccc(cc1)Cl)c1ccccc1 15206929
28145931 2068 54 None - 1 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)[C@@H](c1ccc(cc1)Cl)c1ccccc1 15206929
CHEMBL1201191 2068 54 None - 1 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)[C@@H](c1ccc(cc1)Cl)c1ccccc1 15206929
DB06282 2068 54 None - 1 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 388 8 1 4 3.1 OC(=O)COCCN1CCN(CC1)[C@@H](c1ccc(cc1)Cl)c1ccccc1 15206929
2247 505 81 None -4 42 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 12747773
249 505 81 None -4 42 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 12747773
2603 505 81 None -4 42 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 12747773
CHEMBL296419 505 81 None -4 42 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 12747773
DB00637 505 81 None -4 42 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 12747773
1530 2182 50 None -5 21 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 21470866
3827 2182 50 None -5 21 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 21470866
7206 2182 50 None -5 21 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 21470866
CHEMBL534 2182 50 None -5 21 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 21470866
DB00920 2182 50 None -5 21 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 21470866
1400 1957 70 None 2 3 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 11809864
3658 1957 70 None 2 3 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 11809864
7199 1957 70 None 2 3 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 11809864
91513 1957 70 None 2 3 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 11809864
CHEMBL896 1957 70 None 2 3 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 11809864
DB00557 1957 70 None 2 3 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 11809864
1228 3866 34 None -5 4 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 12065734
1228 3866 34 None -5 4 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 7925364
2763 3866 34 None -5 4 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 12065734
2763 3866 34 None -5 4 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 7925364
5282443 3866 34 None -5 4 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 12065734
5282443 3866 34 None -5 4 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 7925364
CHEMBL855 3866 34 None -5 4 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 12065734
CHEMBL855 3866 34 None -5 4 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 7925364
DB00427 3866 34 None -5 4 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 12065734
DB00427 3866 34 None -5 4 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 7925364
1227 2489 43 None -2 12 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 12065734
1227 2489 43 None -2 12 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 15206929
2331 2489 43 None -2 12 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 12065734
2331 2489 43 None -2 12 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 15206929
3957 2489 43 None -2 12 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 12065734
3957 2489 43 None -2 12 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 15206929
4992 2489 43 None -2 12 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 12065734
4992 2489 43 None -2 12 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 15206929
CHEMBL511 2489 43 None -2 12 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 12065734
CHEMBL511 2489 43 None -2 12 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 15206929
DB06691 2489 43 None -2 12 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 12065734
DB06691 2489 43 None -2 12 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 285 7 0 4 2.7 COc1ccc(cc1)CN(c1ccccn1)CCN(C)C 15206929
2267 559 71 None 10 7 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 21381763
271 559 71 None 10 7 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 21381763
7121 559 71 None 10 7 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 21381763
CHEMBL639 559 71 None 10 7 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 21381763
DB00972 559 71 None 10 7 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 21381763
124087 1389 114 None 3 15 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 15482930
7157 1389 114 None 3 15 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 15482930
814 1389 114 None 3 15 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 15482930
CHEMBL1172 1389 114 None 3 15 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 15482930
DB00967 1389 114 None 3 15 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 15482930
2286 3183 51 None -2 30 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 16782354
4927 3183 51 None -2 30 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 16782354
7282 3183 51 None -2 30 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 16782354
CHEMBL643 3183 51 None -2 30 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 16782354
DB01069 3183 51 None -2 30 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 16782354
10103 3416 72 None -25 3 Guinea pig 7.0 pKi = 7 Binding
[3H]-pyrilamine binding to guinea pig cerebellum membranes.[3H]-pyrilamine binding to guinea pig cerebellum membranes.
Guide to Pharmacology 415 2 0 3 5.6 Cc1cncc(c1)CN1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 8996188
133017 3416 72 None -25 3 Guinea pig 7.0 pKi = 7 Binding
[3H]-pyrilamine binding to guinea pig cerebellum membranes.[3H]-pyrilamine binding to guinea pig cerebellum membranes.
Guide to Pharmacology 415 2 0 3 5.6 Cc1cncc(c1)CN1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 8996188
2413 3416 72 None -25 3 Guinea pig 7.0 pKi = 7 Binding
[3H]-pyrilamine binding to guinea pig cerebellum membranes.[3H]-pyrilamine binding to guinea pig cerebellum membranes.
Guide to Pharmacology 415 2 0 3 5.6 Cc1cncc(c1)CN1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 8996188
CHEMBL91397 3416 72 None -25 3 Guinea pig 7.0 pKi = 7 Binding
[3H]-pyrilamine binding to guinea pig cerebellum membranes.[3H]-pyrilamine binding to guinea pig cerebellum membranes.
Guide to Pharmacology 415 2 0 3 5.6 Cc1cncc(c1)CN1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 8996188
DB11614 3416 72 None -25 3 Guinea pig 7.0 pKi = 7 Binding
[3H]-pyrilamine binding to guinea pig cerebellum membranes.[3H]-pyrilamine binding to guinea pig cerebellum membranes.
Guide to Pharmacology 415 2 0 3 5.6 Cc1cncc(c1)CN1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 8996188
1265 942 60 None -17782 8 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 26084539
6422124 942 60 None -17782 8 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 26084539
CHEMBL14638 942 60 None -17782 8 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 26084539
441082 1163 48 None -2137 8 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 1 0 2 4.8 CN([C@H]1CC[C@]2(C(=CC[C@@H]3[C@@H]2CC[C@]24[C@H]3CC[C@@H]4[C@@H](N(C2)C)C)C1)C)C 26084539
8981 1163 48 None -2137 8 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 1 0 2 4.8 CN([C@H]1CC[C@]2(C(=CC[C@@H]3[C@@H]2CC[C@]24[C@H]3CC[C@@H]4[C@@H](N(C2)C)C)C1)C)C 26084539
CHEMBL191703 1163 48 None -2137 8 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 1 0 2 4.8 CN([C@H]1CC[C@]2(C(=CC[C@@H]3[C@@H]2CC[C@]24[C@H]3CC[C@@H]4[C@@H](N(C2)C)C)C1)C)C 26084539
117072554 2023 0 None -1995 4 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 450 5 2 6 2.3 CN1CCN(CC1)C1=CC(=NC(N1)N)c1ccc2c(c1)CN(CC2)C(=O)CCC1CCCC1 26084539
8982 2023 0 None -1995 4 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 450 5 2 6 2.3 CN1CCN(CC1)C1=CC(=NC(N1)N)c1ccc2c(c1)CN(CC2)C(=O)CCC1CCCC1 26084539
11697697 2547 24 None -6309 6 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 431 6 0 5 4.6 Cc1nc2cccc(c2c(=O)n1c1ccc(cc1)OCCCN1CCCC1)C(F)(F)F 26084539
7346 2547 24 None -6309 6 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 431 6 0 5 4.6 Cc1nc2cccc(c2c(=O)n1c1ccc(cc1)OCCCN1CCCC1)C(F)(F)F 26084539
CHEMBL476323 2547 24 None -6309 6 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 431 6 0 5 4.6 Cc1nc2cccc(c2c(=O)n1c1ccc(cc1)OCCCN1CCCC1)C(F)(F)F 26084539
DB11910 2547 24 None -6309 6 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 431 6 0 5 4.6 Cc1nc2cccc(c2c(=O)n1c1ccc(cc1)OCCCN1CCCC1)C(F)(F)F 26084539
24994634 2142 31 None -194 7 Human 6.0 pKi > 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 26084539
8984 2142 31 None -194 7 Human 6.0 pKi > 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 26084539
CHEMBL3236549 2142 31 None -194 7 Human 6.0 pKi > 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 26084539
45257132 3682 10 None -83 4 Human 6.0 pKi > 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 26084539
8983 3682 10 None -83 4 Human 6.0 pKi > 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 26084539
CHEMBL595180 3682 10 None -83 4 Human 6.0 pKi > 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 26084539
3012003 216145 0 None -6 12 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 311 5 0 3 3.8 CN1CCC(C(C1)COC2=CC=C(C=C2)OC)C3=CC=CC=C3 None
134 2514 24 None -933 67 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 24 None -933 67 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 24 None -933 67 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 24 None -933 67 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 24 None -933 67 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
202 1508 77 None -1 30 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
60835 1508 77 None -1 30 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
972 1508 77 None -1 30 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
CHEMBL1175 1508 77 None -1 30 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
DB00476 1508 77 None -1 30 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
146570 43454 67 None -1 4 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 324 5 0 3 3.8 CN(C)CCC[C@@]1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL1508 43454 67 None -1 4 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 324 5 0 3 3.8 CN(C)CCC[C@@]1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
12057539 208041 42 None -676 20 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 208041 42 None -676 20 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 208041 42 None -676 20 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
5281878 1660 35 None -1 17 Human 8.0 pKi None 8.0 Binding
NoneNone
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 1660 35 None -1 17 Human 8.0 pKi None 8.0 Binding
NoneNone
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 1660 35 None -1 17 Human 8.0 pKi None 8.0 Binding
NoneNone
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 1660 35 None -1 17 Human 8.0 pKi None 8.0 Binding
NoneNone
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 1660 35 None -1 17 Human 8.0 pKi None 8.0 Binding
NoneNone
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 1660 35 None -1 17 Human 8.0 pKi None 8.0 Binding
NoneNone
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 1660 35 None -1 17 Human 8.0 pKi None 8.0 Binding
NoneNone
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1197 88 120 None - 1 Human 3.7 pKi None 3.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 122 2 1 2 0.6 NCCc1ccccn1 15206929
75919 88 120 None - 1 Human 3.7 pKi None 3.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 122 2 1 2 0.6 NCCc1ccccn1 15206929
CHEMBL32813 88 120 None - 1 Human 3.7 pKi None 3.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 122 2 1 2 0.6 NCCc1ccccn1 15206929
1200 3963 2 None -39 3 Human 4.4 pKi None 4.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 335 8 4 5 0.7 O=C(NC(=NCCCc1cnc[nH]1)N)CSCc1nc[nH]c1C 16394198
25149519 3963 2 None -39 3 Human 4.4 pKi None 4.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 335 8 4 5 0.7 O=C(NC(=NCCCc1cnc[nH]1)N)CSCc1nc[nH]c1C 16394198
CHEMBL513056 3963 2 None -39 3 Human 4.4 pKi None 4.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 335 8 4 5 0.7 O=C(NC(=NCCCc1cnc[nH]1)N)CSCc1nc[nH]c1C 16394198
1199 2976 0 None -316 3 Human 4.5 pKi None 4.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 8 3 4 2.5 NC(=NCCCc1[nH]cnc1)NC(=O)CC(c1ccccn1)c1ccc(cc1)F 16394198
25149244 2976 0 None -316 3 Human 4.5 pKi None 4.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 8 3 4 2.5 NC(=NCCCc1[nH]cnc1)NC(=O)CC(c1ccccn1)c1ccc(cc1)F 16394198
CHEMBL472273 2976 0 None -316 3 Human 4.5 pKi None 4.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 8 3 4 2.5 NC(=NCCCc1[nH]cnc1)NC(=O)CC(c1ccccn1)c1ccc(cc1)F 16394198
1198 3962 1 None - 1 Human 4.7 pKi None 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 8 4 4 2.0 O=C(CC(c1ccc(c(c1)F)F)c1ncc[nH]1)NC(=NCCCc1cnc[nH]1)N 16394198
25149704 3962 1 None - 1 Human 4.7 pKi None 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 8 4 4 2.0 O=C(CC(c1ccc(c(c1)F)F)c1ncc[nH]1)NC(=NCCCc1cnc[nH]1)N 16394198
CHEMBL470563 3962 1 None - 1 Human 4.7 pKi None 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 8 4 4 2.0 O=C(CC(c1ccc(c(c1)F)F)c1ncc[nH]1)NC(=NCCCc1cnc[nH]1)N 16394198
1201 3964 1 None -2 2 Human 4.7 pKi None 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 361 7 3 3 2.6 O=C(CC(c1ccccc1)c1ccccc1)NC(=NCCc1cnc[nH]1)N 16394198
25150700 3964 1 None -2 2 Human 4.7 pKi None 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 361 7 3 3 2.6 O=C(CC(c1ccccc1)c1ccccc1)NC(=NCCc1cnc[nH]1)N 16394198
CHEMBL499301 3964 1 None -2 2 Human 4.7 pKi None 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 361 7 3 3 2.6 O=C(CC(c1ccccc1)c1ccccc1)NC(=NCCc1cnc[nH]1)N 16394198
1226 2019 20 None -354 6 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 16394198
41376 2019 20 None -354 6 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 16394198
CHEMBL12608 2019 20 None -354 6 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 16394198
1202 3965 1 None - 1 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 411 8 3 3 3.3 O=C(CC(c1ccc(cc1)F)c1ccc(cc1)F)NC(=NCCCc1cnc[nH]1)N 16394198
25150704 3965 1 None - 1 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 411 8 3 3 3.3 O=C(CC(c1ccc(cc1)F)c1ccc(cc1)F)NC(=NCCCc1cnc[nH]1)N 16394198
CHEMBL513883 3965 1 None - 1 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 411 8 3 3 3.3 O=C(CC(c1ccc(cc1)F)c1ccc(cc1)F)NC(=NCCCc1cnc[nH]1)N 16394198
1204 1932 119 None -501 24 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 12065734
1204 1932 119 None -501 24 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 12626648
1204 1932 119 None -501 24 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15206929
1204 1932 119 None -501 24 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 16394198
1204 1932 119 None -501 24 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 7925364
1247 1932 119 None -501 24 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 12065734
1247 1932 119 None -501 24 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 12626648
1247 1932 119 None -501 24 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15206929
1247 1932 119 None -501 24 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 16394198
1247 1932 119 None -501 24 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 7925364
1375 1932 119 None -501 24 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 12065734
1375 1932 119 None -501 24 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 12626648
1375 1932 119 None -501 24 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15206929
1375 1932 119 None -501 24 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 16394198
1375 1932 119 None -501 24 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 7925364
774 1932 119 None -501 24 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 12065734
774 1932 119 None -501 24 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 12626648
774 1932 119 None -501 24 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15206929
774 1932 119 None -501 24 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 16394198
774 1932 119 None -501 24 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 7925364
CHEMBL90 1932 119 None -501 24 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 12065734
CHEMBL90 1932 119 None -501 24 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 12626648
CHEMBL90 1932 119 None -501 24 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15206929
CHEMBL90 1932 119 None -501 24 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 16394198
CHEMBL90 1932 119 None -501 24 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 7925364
DB05381 1932 119 None -501 24 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 12065734
DB05381 1932 119 None -501 24 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 12626648
DB05381 1932 119 None -501 24 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15206929
DB05381 1932 119 None -501 24 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 16394198
DB05381 1932 119 None -501 24 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 7925364
1193 44 0 None - 1 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 128 2 1 3 0.6 NCCc1nccs1 12626648
87653 44 0 None - 1 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 128 2 1 3 0.6 NCCc1nccs1 12626648
CHEMBL25414 44 0 None - 1 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 128 2 1 3 0.6 NCCc1nccs1 12626648
10389213 197 12 None -6025 3 Human 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 453 10 1 6 2.6 O=C([C@H](NC(=O)c1ccco1)C)N1CCN(CC1)CCCOc1ccc(cc1)C(=O)C1CC1 12606603
10389213 197 12 None -6025 3 Human 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 453 10 1 6 2.6 O=C([C@H](NC(=O)c1ccco1)C)N1CCN(CC1)CCCOc1ccc(cc1)C(=O)C1CC1 15294456
1216 197 12 None -6025 3 Human 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 453 10 1 6 2.6 O=C([C@H](NC(=O)c1ccco1)C)N1CCN(CC1)CCCOc1ccc(cc1)C(=O)C1CC1 12606603
1216 197 12 None -6025 3 Human 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 453 10 1 6 2.6 O=C([C@H](NC(=O)c1ccco1)C)N1CCN(CC1)CCCOc1ccc(cc1)C(=O)C1CC1 15294456
CHEMBL361355 197 12 None -6025 3 Human 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 453 10 1 6 2.6 O=C([C@H](NC(=O)c1ccco1)C)N1CCN(CC1)CCCOc1ccc(cc1)C(=O)C1CC1 12606603
CHEMBL361355 197 12 None -6025 3 Human 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 453 10 1 6 2.6 O=C([C@H](NC(=O)c1ccco1)C)N1CCN(CC1)CCCOc1ccc(cc1)C(=O)C1CC1 15294456
1217 199 0 None -6309 3 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 9 0 8 0.5 CO[C@H]([C@H]([C@H](C(OC(=O)C)[2H])OC(=O)C)OC)[C@@H](OC(=O)C)C 15294456
15608077 199 0 None -6309 3 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 9 0 8 0.5 CO[C@H]([C@H]([C@H](C(OC(=O)C)[2H])OC(=O)C)OC)[C@@H](OC(=O)C)C 15294456
1223 953 41 None -14125 11 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 12606603
2790 953 41 None -14125 11 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 12606603
CHEMBL14690 953 41 None -14125 11 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 12606603
2181 3128 46 None -269 35 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N 8935801
4830 3128 46 None -269 35 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N 8935801
92 3128 46 None -269 35 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N 8935801
CHEMBL440294 3128 46 None -269 35 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N 8935801
DB09286 3128 46 None -269 35 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N 8935801
1194 45 3 None -2089 4 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 265 3 2 2 2.3 NCCc1cnc([nH]1)c1cccc(c1)Br 12626648
23786499 45 3 None -2089 4 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 265 3 2 2 2.3 NCCc1cnc([nH]1)c1cccc(c1)Br 12626648
CHEMBL26116 45 3 None -2089 4 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 265 3 2 2 2.3 NCCc1cnc([nH]1)c1cccc(c1)Br 12626648
1195 46 5 None - 1 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 221 3 2 2 2.2 NCCc1cnc([nH]1)c1cccc(c1)Cl 12626648
14827778 46 5 None - 1 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 221 3 2 2 2.2 NCCc1cnc([nH]1)c1cccc(c1)Cl 12626648
CHEMBL287052 46 5 None - 1 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 221 3 2 2 2.2 NCCc1cnc([nH]1)c1cccc(c1)Cl 12626648
1830 2590 44 None -125 28 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 12629531
207 2590 44 None -125 28 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 12629531
23897 2590 44 None -125 28 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 12629531
CHEMBL460 2590 44 None -125 28 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 12629531
DB01618 2590 44 None -125 28 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 12629531
10245039 49 0 None - 1 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 3 2 2 2.2 NCCc1cnc([nH]1)c1cccc(c1)I 12626648
1196 49 0 None - 1 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 3 2 2 2.2 NCCc1cnc([nH]1)c1cccc(c1)I 12626648
CHEMBL287367 49 0 None - 1 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 3 2 2 2.2 NCCc1cnc([nH]1)c1cccc(c1)I 12626648
1218 229 52 None -891 4 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C 15608078
9818903 229 52 None -891 4 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C 15608078
CHEMBL351231 229 52 None -891 4 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C 15608078
1353 1911 93 None -489 83 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 12629531
1353 1911 93 None -489 83 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 8935801
3559 1911 93 None -489 83 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 12629531
3559 1911 93 None -489 83 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 8935801
86 1911 93 None -489 83 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 12629531
86 1911 93 None -489 83 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 8935801
CHEMBL54 1911 93 None -489 83 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 12629531
CHEMBL54 1911 93 None -489 83 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 8935801
DB00502 1911 93 None -489 83 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 12629531
DB00502 1911 93 None -489 83 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 8935801
16362 3125 71 None -489 30 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 12629531
2172 3125 71 None -489 30 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 12629531
90 3125 71 None -489 30 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 12629531
CHEMBL1423 3125 71 None -489 30 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 12629531
DB01100 3125 71 None -489 30 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 12629531
10042467 1426 1 None -173 3 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 333 8 1 2 4.3 CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C 12626648
1203 1426 1 None -173 3 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 333 8 1 2 4.3 CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C 12626648
CHEMBL11553 1426 1 None -173 3 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 333 8 1 2 4.3 CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C 12626648
1221 475 9 None -12 3 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 9 3 3 3.0 NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)F 12626648
1221 475 9 None -12 3 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 9 3 3 3.0 NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)F 16394198
65895 475 9 None -12 3 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 9 3 3 3.0 NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)F 12626648
65895 475 9 None -12 3 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 9 3 3 3.0 NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)F 16394198
CHEMBL293802 475 9 None -12 3 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 9 3 3 3.0 NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)F 12626648
CHEMBL293802 475 9 None -12 3 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 9 3 3 3.0 NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)F 16394198
1219 737 0 None -3 2 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 396 9 3 3 3.5 NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)Cl 12626648
14660352 737 0 None -3 2 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 396 9 3 3 3.5 NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)Cl 12626648
CHEMBL304239 737 0 None -3 2 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 396 9 3 3 3.5 NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)Cl 12626648
1208 1985 0 None - 1 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 251 2 0 1 3.7 CN([C@H]1Cc2ccccc2[C@H](C1)c1ccccc1)C 12065734
15657195 1985 0 None - 1 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 251 2 0 1 3.7 CN([C@H]1Cc2ccccc2[C@H](C1)c1ccccc1)C 12065734
2435 3590 83 None -95 48 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 12629531
2435 3590 83 None -95 48 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 8935801
60149 3590 83 None -95 48 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 12629531
60149 3590 83 None -95 48 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 8935801
98 3590 83 None -95 48 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 12629531
98 3590 83 None -95 48 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 8935801
CHEMBL12713 3590 83 None -95 48 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 12629531
CHEMBL12713 3590 83 None -95 48 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 8935801
DB06144 3590 83 None -95 48 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 12629531
DB06144 3590 83 None -95 48 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 8935801
214 3860 58 None -43 30 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 12629531
2740 3860 58 None -43 30 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 12629531
5566 3860 58 None -43 30 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 12629531
66064 3860 58 None -43 30 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 12629531
CHEMBL422 3860 58 None -43 30 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 12629531
DB00831 3860 58 None -43 30 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 12629531
10106214 2103 1 None -5 5 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 251 2 0 1 3.7 CN([C@@H]1Cc2ccccc2[C@H](C1)c1ccccc1)C 12065734
1207 2103 1 None -5 5 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 251 2 0 1 3.7 CN([C@@H]1Cc2ccccc2[C@H](C1)c1ccccc1)C 12065734
1209 2103 1 None -5 5 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 251 2 0 1 3.7 CN([C@@H]1Cc2ccccc2[C@H](C1)c1ccccc1)C 12065734
CHEMBL127307 2103 1 None -5 5 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 251 2 0 1 3.7 CN([C@@H]1Cc2ccccc2[C@H](C1)c1ccccc1)C 12065734
475100 189 0 None -31 6 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 4 1 7 2.6 OC1CCc2n(C1)c(=O)c(c(n2)C)CCN1CCC(CC1)c1noc2c1ccc(c2)F 8935801
67 189 0 None -31 6 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 4 1 7 2.6 OC1CCc2n(C1)c(=O)c(c(n2)C)CCN1CCC(CC1)c1noc2c1ccc(c2)F 8935801
CHEMBL3542429 189 0 None -31 6 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 4 1 7 2.6 OC1CCc2n(C1)c(=O)c(c(n2)C)CCN1CCC(CC1)c1noc2c1ccc(c2)F 8935801
242 470 124 None -22 51 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 12629531
34 470 124 None -22 51 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 12629531
60795 470 124 None -22 51 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 12629531
CHEMBL1112 470 124 None -22 51 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 12629531
DB01238 470 124 None -22 51 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 12629531
2865 4143 73 None -58 53 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 12629531
2865 4143 73 None -58 53 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 8935801
59 4143 73 None -58 53 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 12629531
59 4143 73 None -58 53 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 8935801
60854 4143 73 None -58 53 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 12629531
60854 4143 73 None -58 53 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 8935801
CHEMBL708 4143 73 None -58 53 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 12629531
CHEMBL708 4143 73 None -58 53 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 8935801
DB00246 4143 73 None -58 53 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 12629531
DB00246 4143 73 None -58 53 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 8935801
2389 3331 118 None -46 67 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 12629531
2389 3331 118 None -46 67 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 8935801
5073 3331 118 None -46 67 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 12629531
5073 3331 118 None -46 67 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 8935801
96 3331 118 None -46 67 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 12629531
96 3331 118 None -46 67 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 8935801
CHEMBL85 3331 118 None -46 67 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 12629531
CHEMBL85 3331 118 None -46 67 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 8935801
DB00734 3331 118 None -46 67 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 12629531
DB00734 3331 118 None -46 67 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 8935801
1212 1662 50 None -41 65 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 12629531
204 1662 50 None -41 65 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 12629531
3372 1662 50 None -41 65 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 12629531
CHEMBL726 1662 50 None -41 65 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 12629531
DB00623 1662 50 None -41 65 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 12629531
100 3805 58 None -7 55 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 12629531
2637 3805 58 None -7 55 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 12629531
5452 3805 58 None -7 55 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 12629531
CHEMBL479 3805 58 None -7 55 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 12629531
DB00679 3805 58 None -7 55 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 12629531
10037815 3141 0 None - 1 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 251 2 0 1 3.7 CN([C@@H]1Cc2ccccc2[C@@H](C1)c1ccccc1)C 12065734
1206 3141 0 None - 1 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 251 2 0 1 3.7 CN([C@@H]1Cc2ccccc2[C@@H](C1)c1ccccc1)C 12065734
CHEMBL340199 3141 0 None - 1 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 251 2 0 1 3.7 CN([C@@H]1Cc2ccccc2[C@@H](C1)c1ccccc1)C 12065734
1222 1664 49 None -17 33 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 8935801
3396 1664 49 None -17 33 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 8935801
85 1664 49 None -17 33 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 8935801
CHEMBL46516 1664 49 None -17 33 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 8935801
DB04842 1664 49 None -17 33 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 8935801
209 3057 97 None -11 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 12629531
2113 3057 97 None -11 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 12629531
4748 3057 97 None -11 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 12629531
CHEMBL567 3057 97 None -11 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 12629531
DB00850 3057 97 None -11 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 12629531
10037815 3141 0 None - 1 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 251 2 0 1 3.7 CN([C@@H]1Cc2ccccc2[C@@H](C1)c1ccccc1)C 12065734
1206 3141 0 None - 1 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 251 2 0 1 3.7 CN([C@@H]1Cc2ccccc2[C@@H](C1)c1ccccc1)C 12065734
CHEMBL340199 3141 0 None - 1 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 251 2 0 1 3.7 CN([C@@H]1Cc2ccccc2[C@@H](C1)c1ccccc1)C 12065734
2726 919 68 None -2 72 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 12629531
621 919 68 None -2 72 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 12629531
83 919 68 None -2 72 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 12629531
CHEMBL71 919 68 None -2 72 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 12629531
DB00477 919 68 None -2 72 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 12629531
1613 2348 53 None -3 44 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 12629531
205 2348 53 None -3 44 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 12629531
3964 2348 53 None -3 44 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 12629531
CHEMBL831 2348 53 None -3 44 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 12629531
DB00408 2348 53 None -3 44 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 12629531
2337 3256 77 None 1 62 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 12629531
2337 3256 77 None 1 62 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 8935801
50 3256 77 None 1 62 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 12629531
50 3256 77 None 1 62 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 8935801
5002 3256 77 None 1 62 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 12629531
5002 3256 77 None 1 62 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 8935801
CHEMBL716 3256 77 None 1 62 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 12629531
CHEMBL716 3256 77 None 1 62 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 8935801
DB01224 3256 77 None 1 62 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 12629531
DB01224 3256 77 None 1 62 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 8935801
212 3806 47 None -5 25 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 12629531
2639 3806 47 None -5 25 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 12629531
941651 3806 47 None -5 25 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 12629531
CHEMBL1201 3806 47 None -5 25 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 12629531
DB01623 3806 47 None -5 25 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 12629531
10106214 2103 1 None -5 5 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 251 2 0 1 3.7 CN([C@@H]1Cc2ccccc2[C@H](C1)c1ccccc1)C 12065734
1207 2103 1 None -5 5 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 251 2 0 1 3.7 CN([C@@H]1Cc2ccccc2[C@H](C1)c1ccccc1)C 12065734
1209 2103 1 None -5 5 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 251 2 0 1 3.7 CN([C@@H]1Cc2ccccc2[C@H](C1)c1ccccc1)C 12065734
CHEMBL127307 2103 1 None -5 5 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 251 2 0 1 3.7 CN([C@@H]1Cc2ccccc2[C@H](C1)c1ccccc1)C 12065734
10015055 2104 4 None 15 5 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 251 2 0 1 3.7 CN([C@H]1Cc2ccccc2[C@@H](C1)c1ccccc1)C 12065734
1212 2104 4 None 15 5 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 251 2 0 1 3.7 CN([C@H]1Cc2ccccc2[C@@H](C1)c1ccccc1)C 12065734
CHEMBL3402679 2104 4 None 15 5 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 251 2 0 1 3.7 CN([C@H]1Cc2ccccc2[C@@H](C1)c1ccccc1)C 12065734
135398745 2914 112 None 1 65 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 12629531
135398745 2914 112 None 1 65 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 8935801
47 2914 112 None 1 65 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 12629531
47 2914 112 None 1 65 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 8935801
CHEMBL715 2914 112 None 1 65 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 12629531
CHEMBL715 2914 112 None 1 65 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 8935801
DB00334 2914 112 None 1 65 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 12629531
DB00334 2914 112 None 1 65 Human 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 8935801
135398737 958 93 None 2 89 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 12065734
135398737 958 93 None 2 89 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 12629531
135398737 958 93 None 2 89 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8935801
38 958 93 None 2 89 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 12065734
38 958 93 None 2 89 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 12629531
38 958 93 None 2 89 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8935801
722 958 93 None 2 89 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 12065734
722 958 93 None 2 89 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 12629531
722 958 93 None 2 89 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8935801
CHEMBL42 958 93 None 2 89 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 12065734
CHEMBL42 958 93 None 2 89 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 12629531
CHEMBL42 958 93 None 2 89 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8935801
DB00363 958 93 None 2 89 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 12065734
DB00363 958 93 None 2 89 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 12629531
DB00363 958 93 None 2 89 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8935801
103 4153 61 None -1 53 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 8935801
2875 4153 61 None -1 53 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 8935801
5736 4153 61 None -1 53 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 8935801
CHEMBL285802 4153 61 None -1 53 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 8935801
DB09225 4153 61 None -1 53 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 8935801
1225 1471 26 None -1 22 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C 12065734
3958 1471 26 None -1 22 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C 12065734
667477 1471 26 None -1 22 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C 12065734
CHEMBL860 1471 26 None -1 22 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C 12065734
DB01142 1471 26 None -1 22 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C 12065734
163091 494 34 None -6 10 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 285 0 0 2 4.3 Clc1ccc2c(c1)[C@H]1CN(C[C@@H]1c1c(O2)cccc1)C 8935801
22 494 34 None -6 10 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 285 0 0 2 4.3 Clc1ccc2c(c1)[C@H]1CN(C[C@@H]1c1c(O2)cccc1)C 8935801
CHEMBL504548 494 34 None -6 10 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 285 0 0 2 4.3 Clc1ccc2c(c1)[C@H]1CN(C[C@@H]1c1c(O2)cccc1)C 8935801