Ligand source activities (1 row/activity)
Ligands (move mouse cursor over ligand name to see structure) | Receptor | Assay information | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| #Vendors | Reference ligand
| Fold selectivity | # Tested GPCRs | Species
| p-value (-log) | Activity Type
| Activity Relation
| Activity Value
| AssayType
| Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
|
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Assay information
| Chemical information
| ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| #Vendors | Reference ligand
| Fold selectivity | # Tested GPCRs | Species
| p-value (-log) | Activity Type
| Activity Relation
| Activity Value
| AssayType
| Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
|
91826086 | 114936 | 47 | None | - | 1 | Human | 10.2 | pEC50 | = | 10.2 | Functional | Agonist activity at human GPR39 expressed in HEK293 cells by cAMP assayAgonist activity at human GPR39 expressed in HEK293 cells by cAMP assay |
ChEMBL | 418 | 7 | 3 | 7 | 3.2 | CNc1nc(NCc2ccc(NS(C)(=O)=O)cc2Cl)cc(-c2ccccn2)n1 | 10.1021/ml500240d | |
CHEMBL3342358 | 114936 | 47 | None | - | 1 | Human | 10.2 | pEC50 | = | 10.2 | Functional | Agonist activity at human GPR39 expressed in HEK293 cells by cAMP assayAgonist activity at human GPR39 expressed in HEK293 cells by cAMP assay |
ChEMBL | 418 | 7 | 3 | 7 | 3.2 | CNc1nc(NCc2ccc(NS(C)(=O)=O)cc2Cl)cc(-c2ccccn2)n1 | 10.1021/ml500240d | |
118716417 | 114954 | 0 | None | 10 | 2 | Human | 9.7 | pEC50 | = | 9.7 | Functional | Agonist activity at human GPR39 expressed in HEK293 cells by cAMP assayAgonist activity at human GPR39 expressed in HEK293 cells by cAMP assay |
ChEMBL | 384 | 7 | 3 | 7 | 2.6 | CNc1nc(NCc2ccc(NS(C)(=O)=O)cc2)cc(-c2ccccn2)n1 | 10.1021/ml500240d | |
CHEMBL3342376 | 114954 | 0 | None | 10 | 2 | Human | 9.7 | pEC50 | = | 9.7 | Functional | Agonist activity at human GPR39 expressed in HEK293 cells by cAMP assayAgonist activity at human GPR39 expressed in HEK293 cells by cAMP assay |
ChEMBL | 384 | 7 | 3 | 7 | 2.6 | CNc1nc(NCc2ccc(NS(C)(=O)=O)cc2)cc(-c2ccccn2)n1 | 10.1021/ml500240d | |
118716420 | 114957 | 0 | None | - | 1 | Human | 9.5 | pEC50 | = | 9.5 | Functional | Agonist activity at human GPR39 expressed in HEK293 cells by cAMP assayAgonist activity at human GPR39 expressed in HEK293 cells by cAMP assay |
ChEMBL | 366 | 6 | 3 | 6 | 3.3 | CNc1nc(NCc2ccc(NC(C)=O)cc2F)cc(-c2ccccn2)n1 | 10.1021/ml500240d | |
CHEMBL3342379 | 114957 | 0 | None | - | 1 | Human | 9.5 | pEC50 | = | 9.5 | Functional | Agonist activity at human GPR39 expressed in HEK293 cells by cAMP assayAgonist activity at human GPR39 expressed in HEK293 cells by cAMP assay |
ChEMBL | 366 | 6 | 3 | 6 | 3.3 | CNc1nc(NCc2ccc(NC(C)=O)cc2F)cc(-c2ccccn2)n1 | 10.1021/ml500240d | |
7803 | 993 | 0 | None | 1 | 2 | Mouse | 9.3 | pEC50 | = | 9.3 | Functional | Agonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 359 | 5 | 2 | 5 | 4.5 | CNc1nc(NCc2ccc(cc2Cl)Cl)cc(n1)c1ccccn1 | 10.1021/ml500240d | |
86277841 | 993 | 0 | None | 1 | 2 | Mouse | 9.3 | pEC50 | = | 9.3 | Functional | Agonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 359 | 5 | 2 | 5 | 4.5 | CNc1nc(NCc2ccc(cc2Cl)Cl)cc(n1)c1ccccn1 | 10.1021/ml500240d | |
CHEMBL3342370 | 993 | 0 | None | 1 | 2 | Mouse | 9.3 | pEC50 | = | 9.3 | Functional | Agonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 359 | 5 | 2 | 5 | 4.5 | CNc1nc(NCc2ccc(cc2Cl)Cl)cc(n1)c1ccccn1 | 10.1021/ml500240d | |
118716418 | 114955 | 0 | None | 1 | 2 | Human | 9.3 | pEC50 | = | 9.3 | Functional | Agonist activity at human GPR39 expressed in HEK293 cells by cAMP assayAgonist activity at human GPR39 expressed in HEK293 cells by cAMP assay |
ChEMBL | 348 | 6 | 3 | 6 | 3.2 | CNc1nc(NCc2ccc(NC(C)=O)cc2)cc(-c2ccccn2)n1 | 10.1021/ml500240d | |
CHEMBL3342377 | 114955 | 0 | None | 1 | 2 | Human | 9.3 | pEC50 | = | 9.3 | Functional | Agonist activity at human GPR39 expressed in HEK293 cells by cAMP assayAgonist activity at human GPR39 expressed in HEK293 cells by cAMP assay |
ChEMBL | 348 | 6 | 3 | 6 | 3.2 | CNc1nc(NCc2ccc(NC(C)=O)cc2)cc(-c2ccccn2)n1 | 10.1021/ml500240d | |
91826086 | 114936 | 47 | None | - | 1 | Human | 9.1 | pEC50 | = | 9.1 | Functional | Agonist activity at human GPR39 by IP1 assayAgonist activity at human GPR39 by IP1 assay |
ChEMBL | 418 | 7 | 3 | 7 | 3.2 | CNc1nc(NCc2ccc(NS(C)(=O)=O)cc2Cl)cc(-c2ccccn2)n1 | 10.1021/ml500240d | |
CHEMBL3342358 | 114936 | 47 | None | - | 1 | Human | 9.1 | pEC50 | = | 9.1 | Functional | Agonist activity at human GPR39 by IP1 assayAgonist activity at human GPR39 by IP1 assay |
ChEMBL | 418 | 7 | 3 | 7 | 3.2 | CNc1nc(NCc2ccc(NS(C)(=O)=O)cc2Cl)cc(-c2ccccn2)n1 | 10.1021/ml500240d | |
7803 | 993 | 0 | None | -1 | 2 | Human | 9.1 | pEC50 | = | 9.1 | Functional | Agonist activity at human GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at human GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 359 | 5 | 2 | 5 | 4.5 | CNc1nc(NCc2ccc(cc2Cl)Cl)cc(n1)c1ccccn1 | 10.1021/ml500240d | |
86277841 | 993 | 0 | None | -1 | 2 | Human | 9.1 | pEC50 | = | 9.1 | Functional | Agonist activity at human GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at human GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 359 | 5 | 2 | 5 | 4.5 | CNc1nc(NCc2ccc(cc2Cl)Cl)cc(n1)c1ccccn1 | 10.1021/ml500240d | |
CHEMBL3342370 | 993 | 0 | None | -1 | 2 | Human | 9.1 | pEC50 | = | 9.1 | Functional | Agonist activity at human GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at human GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 359 | 5 | 2 | 5 | 4.5 | CNc1nc(NCc2ccc(cc2Cl)Cl)cc(n1)c1ccccn1 | 10.1021/ml500240d | |
91826086 | 114936 | 47 | None | - | 1 | Human | 9.1 | pEC50 | = | 9.1 | Functional | Agonist activity at human GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at human GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 418 | 7 | 3 | 7 | 3.2 | CNc1nc(NCc2ccc(NS(C)(=O)=O)cc2Cl)cc(-c2ccccn2)n1 | 10.1021/ml500240d | |
CHEMBL3342358 | 114936 | 47 | None | - | 1 | Human | 9.1 | pEC50 | = | 9.1 | Functional | Agonist activity at human GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at human GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 418 | 7 | 3 | 7 | 3.2 | CNc1nc(NCc2ccc(NS(C)(=O)=O)cc2Cl)cc(-c2ccccn2)n1 | 10.1021/ml500240d | |
118716420 | 114957 | 0 | None | - | 1 | Human | 9.0 | pEC50 | = | 9 | Functional | Agonist activity at human GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at human GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 366 | 6 | 3 | 6 | 3.3 | CNc1nc(NCc2ccc(NC(C)=O)cc2F)cc(-c2ccccn2)n1 | 10.1021/ml500240d | |
CHEMBL3342379 | 114957 | 0 | None | - | 1 | Human | 9.0 | pEC50 | = | 9 | Functional | Agonist activity at human GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at human GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 366 | 6 | 3 | 6 | 3.3 | CNc1nc(NCc2ccc(NC(C)=O)cc2F)cc(-c2ccccn2)n1 | 10.1021/ml500240d | |
137639471 | 156896 | 0 | None | - | 1 | Human | 9.0 | pEC50 | = | 9 | Functional | Agonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assayAgonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assay |
ChEMBL | 393 | 4 | 2 | 7 | 2.6 | Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCc1ccc(F)cc1)CC(=O)N2 | 10.1021/acs.jmedchem.6b00648 | |
CHEMBL4072160 | 156896 | 0 | None | - | 1 | Human | 9.0 | pEC50 | = | 9 | Functional | Agonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assayAgonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assay |
ChEMBL | 393 | 4 | 2 | 7 | 2.6 | Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCc1ccc(F)cc1)CC(=O)N2 | 10.1021/acs.jmedchem.6b00648 | |
118716413 | 114949 | 0 | None | 60 | 2 | Mouse | 9.0 | pEC50 | = | 9 | Functional | Agonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 393 | 6 | 2 | 5 | 4.8 | FC(F)(F)CNc1nc(NCc2ccc(Cl)cc2)cc(-c2ccccn2)n1 | 10.1021/ml500240d | |
CHEMBL3342371 | 114949 | 0 | None | 60 | 2 | Mouse | 9.0 | pEC50 | = | 9 | Functional | Agonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 393 | 6 | 2 | 5 | 4.8 | FC(F)(F)CNc1nc(NCc2ccc(Cl)cc2)cc(-c2ccccn2)n1 | 10.1021/ml500240d | |
137661197 | 159334 | 1 | None | -3 | 2 | Human | 8.8 | pEC50 | = | 8.8 | Functional | Agonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assayAgonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assay |
ChEMBL | 451 | 4 | 2 | 9 | 2.5 | Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCc1cc(F)cc3c1OCOC3)CC(=O)N2 | 10.1021/acs.jmedchem.6b00648 | |
CHEMBL4100119 | 159334 | 1 | None | -3 | 2 | Human | 8.8 | pEC50 | = | 8.8 | Functional | Agonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assayAgonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assay |
ChEMBL | 451 | 4 | 2 | 9 | 2.5 | Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCc1cc(F)cc3c1OCOC3)CC(=O)N2 | 10.1021/acs.jmedchem.6b00648 | |
137633277 | 156581 | 0 | None | - | 1 | Human | 8.0 | pEC50 | = | 8 | Functional | Agonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assayAgonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assay |
ChEMBL | 388 | 3 | 3 | 7 | 1.9 | Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(C(=O)Nc1ccccc1)CC(=O)N2 | 10.1021/acs.jmedchem.6b00648 | |
CHEMBL4068635 | 156581 | 0 | None | - | 1 | Human | 8.0 | pEC50 | = | 8 | Functional | Agonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assayAgonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assay |
ChEMBL | 388 | 3 | 3 | 7 | 1.9 | Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(C(=O)Nc1ccccc1)CC(=O)N2 | 10.1021/acs.jmedchem.6b00648 | |
137644326 | 158098 | 0 | None | - | 1 | Human | 8.0 | pEC50 | = | 8 | Functional | Agonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assayAgonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assay |
ChEMBL | 393 | 5 | 2 | 9 | 1.5 | Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCCn1nccc1C)CC(=O)N2 | 10.1021/acs.jmedchem.6b00648 | |
CHEMBL4086570 | 158098 | 0 | None | - | 1 | Human | 8.0 | pEC50 | = | 8 | Functional | Agonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assayAgonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assay |
ChEMBL | 393 | 5 | 2 | 9 | 1.5 | Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCCn1nccc1C)CC(=O)N2 | 10.1021/acs.jmedchem.6b00648 | |
118716409 | 114944 | 0 | None | 1 | 2 | Mouse | 8.0 | pEC50 | = | 8 | Functional | Agonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 297 | 5 | 2 | 5 | 3.6 | CNc1nc(NCC2CCCCC2)cc(-c2ccccn2)n1 | 10.1021/ml500240d | |
CHEMBL3342366 | 114944 | 0 | None | 1 | 2 | Mouse | 8.0 | pEC50 | = | 8 | Functional | Agonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 297 | 5 | 2 | 5 | 3.6 | CNc1nc(NCC2CCCCC2)cc(-c2ccccn2)n1 | 10.1021/ml500240d | |
118716404 | 114939 | 0 | None | -4 | 2 | Mouse | 5.0 | pEC50 | = | 5 | Functional | Agonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 299 | 8 | 2 | 6 | 2.4 | COCCNc1nc(NCC2CC2)cc(-c2ccccn2)n1 | 10.1021/ml500240d | |
CHEMBL3342361 | 114939 | 0 | None | -4 | 2 | Mouse | 5.0 | pEC50 | = | 5 | Functional | Agonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 299 | 8 | 2 | 6 | 2.4 | COCCNc1nc(NCC2CC2)cc(-c2ccccn2)n1 | 10.1021/ml500240d | |
118716406 | 114941 | 0 | None | 2 | 2 | Mouse | 5.0 | pEC50 | = | 5 | Functional | Agonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 226 | 4 | 1 | 4 | 2.4 | c1ccc(-c2cc(NCC3CC3)ncn2)nc1 | 10.1021/ml500240d | |
CHEMBL3342363 | 114941 | 0 | None | 2 | 2 | Mouse | 5.0 | pEC50 | = | 5 | Functional | Agonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 226 | 4 | 1 | 4 | 2.4 | c1ccc(-c2cc(NCC3CC3)ncn2)nc1 | 10.1021/ml500240d | |
118716401 | 114830 | 0 | None | -3 | 2 | Human | 8.0 | pEC50 | = | 8.0 | Functional | Agonist activity at human GPR39 by IP1 assayAgonist activity at human GPR39 by IP1 assay |
ChEMBL | 510 | 10 | 3 | 7 | 4.4 | O=S(=O)(NC[C@H]1CC[C@H](CNc2cc(-c3ccccn3)nc(NC3CC3)n2)CC1)c1cccc(F)c1 | 10.1021/ml500240d | |
CHEMBL3341764 | 114830 | 0 | None | -3 | 2 | Human | 8.0 | pEC50 | = | 8.0 | Functional | Agonist activity at human GPR39 by IP1 assayAgonist activity at human GPR39 by IP1 assay |
ChEMBL | 510 | 10 | 3 | 7 | 4.4 | O=S(=O)(NC[C@H]1CC[C@H](CNc2cc(-c3ccccn3)nc(NC3CC3)n2)CC1)c1cccc(F)c1 | 10.1021/ml500240d | |
118716409 | 114944 | 0 | None | -1 | 2 | Human | 8.0 | pEC50 | = | 8.0 | Functional | Agonist activity at human GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at human GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 297 | 5 | 2 | 5 | 3.6 | CNc1nc(NCC2CCCCC2)cc(-c2ccccn2)n1 | 10.1021/ml500240d | |
CHEMBL3342366 | 114944 | 0 | None | -1 | 2 | Human | 8.0 | pEC50 | = | 8.0 | Functional | Agonist activity at human GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at human GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 297 | 5 | 2 | 5 | 3.6 | CNc1nc(NCC2CCCCC2)cc(-c2ccccn2)n1 | 10.1021/ml500240d | |
5407221 | 155904 | 13 | None | - | 1 | Human | 6.0 | pEC50 | = | 6.0 | Functional | Agonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assayAgonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assay |
ChEMBL | 319 | 3 | 3 | 4 | 3.3 | C/C(=N\NC(=O)c1cc2ccccc2cc1O)c1ccc(N)cc1 | 10.1021/acs.jmedchem.6b00648 | |
CHEMBL4060705 | 155904 | 13 | None | - | 1 | Human | 6.0 | pEC50 | = | 6.0 | Functional | Agonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assayAgonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation in presence of 10 uM Zn2+ measured after 75 mins by scintillation proximity assay |
ChEMBL | 319 | 3 | 3 | 4 | 3.3 | C/C(=N\NC(=O)c1cc2ccccc2cc1O)c1ccc(N)cc1 | 10.1021/acs.jmedchem.6b00648 | |
137645445 | 157537 | 0 | None | - | 1 | Human | 7.0 | pEC50 | = | 7.0 | Functional | Agonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation measured after 75 mins by scintillation proximity assayAgonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation measured after 75 mins by scintillation proximity assay |
ChEMBL | 341 | 4 | 2 | 7 | 1.9 | Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCC(C)C)CC(=O)N2 | 10.1021/acs.jmedchem.6b00648 | |
CHEMBL4080106 | 157537 | 0 | None | - | 1 | Human | 7.0 | pEC50 | = | 7.0 | Functional | Agonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation measured after 75 mins by scintillation proximity assayAgonist activity at human GPR39 expressed in HEK293 cells co-expressing Galphaq assessed as myo-[2-3H]inositol phosphate accumulation measured after 75 mins by scintillation proximity assay |
ChEMBL | 341 | 4 | 2 | 7 | 1.9 | Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCC(C)C)CC(=O)N2 | 10.1021/acs.jmedchem.6b00648 | |
118716402 | 114937 | 0 | None | 1 | 2 | Mouse | 6.9 | pEC50 | = | 6.9 | Functional | Agonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 255 | 5 | 2 | 5 | 2.4 | CNc1nc(NCC2CC2)cc(-c2ccccn2)n1 | 10.1021/ml500240d | |
CHEMBL3342359 | 114937 | 0 | None | 1 | 2 | Mouse | 6.9 | pEC50 | = | 6.9 | Functional | Agonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at mouse GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 255 | 5 | 2 | 5 | 2.4 | CNc1nc(NCC2CC2)cc(-c2ccccn2)n1 | 10.1021/ml500240d | |
118716412 | 114947 | 0 | None | 2 | 2 | Human | 5.9 | pEC50 | = | 5.9 | Functional | Agonist activity at human GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at human GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 362 | 6 | 2 | 6 | 3.2 | CNc1nc(NCc2ccc(N(C)C(C)=O)cc2)cc(-c2ccccn2)n1 | 10.1021/ml500240d | |
CHEMBL3342369 | 114947 | 0 | None | 2 | 2 | Human | 5.9 | pEC50 | = | 5.9 | Functional | Agonist activity at human GPR39 expressed in HEK293 cells by IP1 assayAgonist activity at human GPR39 expressed in HEK293 cells by IP1 assay |
ChEMBL | 362 | 6 | 2 | 6 | 3.2 | CNc1nc(NCc2ccc(N(C)C(C)=O)cc2)cc(-c2ccccn2)n1 | 10.1021/ml500240d | |
137661197 | 159334 | 1 | None | -3 | 2 | Human | 7.9 | pEC50 | = | 7.9 | Functional | Agonist activity at GPR39 (unknown origin) expressed in COS7 cells co-expressing Galphas assessed as increase in intracellular cAMP level in presence of 3 uM Zn2+ measured after 30 mins by chemiluminescence assayAgonist activity at GPR39 (unknown origin) expressed in COS7 cells co-expressing Galphas assessed as increase in intracellular cAMP level in presence of 3 uM Zn2+ measured after 30 mins by chemiluminescence assay |
ChEMBL | 451 | 4 | 2 | 9 | 2.5 | Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCc1cc(F)cc3c1OCOC3)CC(=O)N2 | 10.1021/acs.jmedchem.6b00648 | |
CHEMBL4100119 | 159334 | 1 | None | -3 | 2 | Human | 7.9 | pEC50 | = | 7.9 | Functional | Agonist activity at GPR39 (unknown origin) expressed in COS7 cells co-expressing Galphas assessed as increase in intracellular cAMP level in presence of 3 uM Zn2+ measured after 30 mins by chemiluminescence assayAgonist activity at GPR39 (unknown origin) expressed in COS7 cells co-expressing Galphas assessed as increase in intracellular cAMP level in presence of 3 uM Zn2+ measured after 30 mins by chemiluminescence assay |
ChEMBL | 451 | 4 | 2 | 9 | 2.5 | Cc1nn(-c2ncnc3nc[nH]c23)c2c1C(OCc1cc(F)cc3c1OCOC3)CC(=O)N2 | 10.1021/acs.jmedchem.6b00648 |
Showing 1 to 50 of 300 entries
Ligands (move mouse cursor over ligand name to see structure) | Receptor | Assay information | Chemical information | |||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Similar- ity
| Common name
| GPCRdb ID | #Vendors
| Reference ligand | Fold selectivity | # Tested GPCRs
| Species | p-value (-log)
| Activity Type
| Activity Relation
| Activity Value
| Assay Type
| Assay Description
| Source | Mol weight | Rot Bonds | H don | H acc | LogP
| Smiles
| DOI |
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Assay information
| Chemical information
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Sel. page | Similar- ity
| Common name
| GPCRdb ID | #Vendors
| Reference ligand | Fold selectivity | # Tested GPCRs
| Species | p-value (-log)
| Activity Type
| Activity Relation
| Activity Value
| Assay Type
| Assay Description
| Source | Mol weight | Rot Bonds | H don | H acc | LogP
| Smiles
| DOI |
168269293 | 189973 | 0 | None | - | 0 | Human | 6.9 | pEC50 | = | 6.9 | Binding | Positive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ fluxPositive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ flux |
ChEMBL | 355 | 3 | 0 | 5 | 4.1 | Cc1cc(N2CCC(c3ccccc3)C2)n2ncc(-c3ccccn3)c2n1 | 10.1016/j.bmcl.2022.128607 | ||
CHEMBL5170821 | 189973 | 0 | None | - | 0 | Human | 6.9 | pEC50 | = | 6.9 | Binding | Positive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ fluxPositive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ flux |
ChEMBL | 355 | 3 | 0 | 5 | 4.1 | Cc1cc(N2CCC(c3ccccc3)C2)n2ncc(-c3ccccn3)c2n1 | 10.1016/j.bmcl.2022.128607 | ||
76313672 | 103917 | 0 | None | - | 0 | Human | 6.7 | pEC50 | = | 6.7 | Binding | Agonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assayAgonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assay |
ChEMBL | 423 | 7 | 2 | 4 | 3.6 | CCc1nc(CN2C[C@@H](C(=O)NCc3ccccc3Cl)[C@H](c3cccnc3)C2)c[nH]1 | 10.1021/ml400275z | ||
CHEMBL3092410 | 103917 | 0 | None | - | 0 | Human | 6.7 | pEC50 | = | 6.7 | Binding | Agonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assayAgonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assay |
ChEMBL | 423 | 7 | 2 | 4 | 3.6 | CCc1nc(CN2C[C@@H](C(=O)NCc3ccccc3Cl)[C@H](c3cccnc3)C2)c[nH]1 | 10.1021/ml400275z | ||
168292047 | 191939 | 0 | None | - | 0 | Human | 7.6 | pEC50 | = | 7.6 | Binding | Positive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ fluxPositive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ flux |
ChEMBL | 278 | 4 | 1 | 5 | 3.4 | CNc1nc(Oc2ccccc2)cc(-c2ccccn2)n1 | 10.1016/j.bmcl.2022.128607 | ||
CHEMBL5200611 | 191939 | 0 | None | - | 0 | Human | 7.6 | pEC50 | = | 7.6 | Binding | Positive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ fluxPositive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ flux |
ChEMBL | 278 | 4 | 1 | 5 | 3.4 | CNc1nc(Oc2ccccc2)cc(-c2ccccn2)n1 | 10.1016/j.bmcl.2022.128607 | ||
168284637 | 191479 | 0 | None | - | 0 | Human | 6.6 | pEC50 | = | 6.6 | Binding | Positive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ fluxPositive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ flux |
ChEMBL | 331 | 4 | 3 | 4 | 2.6 | NC(Cc1cnc[nH]1)c1nc2ccc(-c3ccccc3)cc2c(=O)[nH]1 | 10.1016/j.bmcl.2022.128607 | ||
CHEMBL5193472 | 191479 | 0 | None | - | 0 | Human | 6.6 | pEC50 | = | 6.6 | Binding | Positive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ fluxPositive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ flux |
ChEMBL | 331 | 4 | 3 | 4 | 2.6 | NC(Cc1cnc[nH]1)c1nc2ccc(-c3ccccc3)cc2c(=O)[nH]1 | 10.1016/j.bmcl.2022.128607 | ||
168269293 | 189973 | 0 | None | - | 0 | Human | 6.6 | pEC50 | = | 6.6 | Binding | Positive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ fluxPositive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ flux |
ChEMBL | 355 | 3 | 0 | 5 | 4.1 | Cc1cc(N2CCC(c3ccccc3)C2)n2ncc(-c3ccccn3)c2n1 | 10.1016/j.bmcl.2022.128607 | ||
CHEMBL5170821 | 189973 | 0 | None | - | 0 | Human | 6.6 | pEC50 | = | 6.6 | Binding | Positive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ fluxPositive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ flux |
ChEMBL | 355 | 3 | 0 | 5 | 4.1 | Cc1cc(N2CCC(c3ccccc3)C2)n2ncc(-c3ccccn3)c2n1 | 10.1016/j.bmcl.2022.128607 | ||
76317176 | 103919 | 0 | None | - | 0 | Human | 5.5 | pEC50 | = | 5.5 | Binding | Agonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assayAgonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assay |
ChEMBL | 443 | 9 | 1 | 4 | 4.1 | COc1cccc([C@@H]2CCN(CCc3ccccc3)C[C@H]2C(=O)NCCc2ccccn2)c1 | 10.1021/ml400275z | ||
CHEMBL3092412 | 103919 | 0 | None | - | 0 | Human | 5.5 | pEC50 | = | 5.5 | Binding | Agonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assayAgonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assay |
ChEMBL | 443 | 9 | 1 | 4 | 4.1 | COc1cccc([C@@H]2CCN(CCc3ccccc3)C[C@H]2C(=O)NCCc2ccccn2)c1 | 10.1021/ml400275z | ||
76331797 | 103918 | 0 | None | - | 0 | Human | 6.5 | pEC50 | = | 6.5 | Binding | Agonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assayAgonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assay |
ChEMBL | 423 | 7 | 2 | 4 | 3.6 | CCc1nc(CN2C[C@H](c3cccnc3)[C@@H](C(=O)NCc3ccccc3Cl)C2)c[nH]1 | 10.1021/ml400275z | ||
CHEMBL3092411 | 103918 | 0 | None | - | 0 | Human | 6.5 | pEC50 | = | 6.5 | Binding | Agonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assayAgonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assay |
ChEMBL | 423 | 7 | 2 | 4 | 3.6 | CCc1nc(CN2C[C@H](c3cccnc3)[C@@H](C(=O)NCc3ccccc3Cl)C2)c[nH]1 | 10.1021/ml400275z | ||
168275606 | 190615 | 0 | None | - | 0 | Human | 5.4 | pEC50 | = | 5.4 | Binding | Positive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ fluxPositive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ flux |
ChEMBL | 362 | 6 | 1 | 5 | 2.5 | O=C(Cc1nn(CC2CCC2)c(=O)c2ccccc12)NCc1ccccn1 | 10.1016/j.bmcl.2022.128607 | ||
CHEMBL5180932 | 190615 | 0 | None | - | 0 | Human | 5.4 | pEC50 | = | 5.4 | Binding | Positive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ fluxPositive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ flux |
ChEMBL | 362 | 6 | 1 | 5 | 2.5 | O=C(Cc1nn(CC2CCC2)c(=O)c2ccccc12)NCc1ccccn1 | 10.1016/j.bmcl.2022.128607 | ||
124263402 | 191610 | 1 | None | - | 0 | Human | 6.3 | pEC50 | = | 6.3 | Binding | Positive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ fluxPositive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ flux |
ChEMBL | 283 | 4 | 2 | 5 | 3.3 | CNc1cc(-c2ccccn2)nc(NC2CCCCC2)n1 | 10.1016/j.bmcl.2022.128607 | ||
CHEMBL5195424 | 191610 | 1 | None | - | 0 | Human | 6.3 | pEC50 | = | 6.3 | Binding | Positive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ fluxPositive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ flux |
ChEMBL | 283 | 4 | 2 | 5 | 3.3 | CNc1cc(-c2ccccn2)nc(NC2CCCCC2)n1 | 10.1016/j.bmcl.2022.128607 | ||
73211886 | 1017 | 3 | None | - | 0 | Human | 7.3 | pEC50 | = | 7.3 | Binding | Agonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assayAgonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assay |
ChEMBL | 352 | 3 | 0 | 6 | 2.6 | N#Cc1ccc(nc1)N1CCN(CC1)Cc1cn2c(n1)ccc(c2)Cl | 10.1021/ml400275z | ||
7800 | 1017 | 3 | None | - | 0 | Human | 7.3 | pEC50 | = | 7.3 | Binding | Agonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assayAgonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assay |
ChEMBL | 352 | 3 | 0 | 6 | 2.6 | N#Cc1ccc(nc1)N1CCN(CC1)Cc1cn2c(n1)ccc(c2)Cl | 10.1021/ml400275z | ||
CHEMBL3092413 | 1017 | 3 | None | - | 0 | Human | 7.3 | pEC50 | = | 7.3 | Binding | Agonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assayAgonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced intracellular Ca+2 mobilization after 1 hr by Fluo-4 No staining-based FLIPR assay |
ChEMBL | 352 | 3 | 0 | 6 | 2.6 | N#Cc1ccc(nc1)N1CCN(CC1)Cc1cn2c(n1)ccc(c2)Cl | 10.1021/ml400275z | ||
168292856 | 192108 | 0 | None | - | 0 | Human | 6.2 | pEC50 | = | 6.2 | Binding | Positive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ fluxPositive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ flux |
ChEMBL | 389 | 7 | 2 | 6 | 2.9 | Cn1cc(-c2ccc3nc(C(N)CCOCc4ccccc4)[nH]c(=O)c3c2)cn1 | 10.1016/j.bmcl.2022.128607 | ||
CHEMBL5203229 | 192108 | 0 | None | - | 0 | Human | 6.2 | pEC50 | = | 6.2 | Binding | Positive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ fluxPositive allosteric activity at human GPR39 receptor expressed in CHO cells assessed as increase in zn2+ induced ca2+ flux |
ChEMBL | 389 | 7 | 2 | 6 | 2.9 | Cn1cc(-c2ccc3nc(C(N)CCOCc4ccccc4)[nH]c(=O)c3c2)cn1 | 10.1016/j.bmcl.2022.128607 |
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