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
|
| 46947061 | 17197 | 1 | None | - | 1 | Human | 8.0 | pEC50 | = | 8 | Functional | Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay |
ChEMBL | 283 | 2 | 1 | 3 | 4.2 | Cc1ccc([C@](C)(O)c2nc3ccccc3s2)c(C)c1 | 10.1016/j.bmcl.2010.07.077 | |
| CHEMBL1256368 | 17197 | 1 | None | - | 1 | Human | 8.0 | pEC50 | = | 8 | Functional | Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay |
ChEMBL | 283 | 2 | 1 | 3 | 4.2 | Cc1ccc([C@](C)(O)c2nc3ccccc3s2)c(C)c1 | 10.1016/j.bmcl.2010.07.077 | |
| 137638922 | 156747 | 0 | None | - | 1 | Human | 7.0 | pEC50 | = | 7 | Functional | Agonist activity at human CaSR expressed in HEK293 cells assessed as increase in intracellular calcium mobilization by fluo-4AM dye based FLIPR assayAgonist activity at human CaSR expressed in HEK293 cells assessed as increase in intracellular calcium mobilization by fluo-4AM dye based FLIPR assay |
ChEMBL | 488 | 11 | 4 | 5 | 4.1 | C[C@@H](N[C@H]1CCN(c2ccc(C(=O)N[C@H](CCCCN)C(=O)O)cc2)C1)c1cccc2ccccc12 | 10.1016/j.bmcl.2017.09.008 | |
| CHEMBL4070562 | 156747 | 0 | None | - | 1 | Human | 7.0 | pEC50 | = | 7 | Functional | Agonist activity at human CaSR expressed in HEK293 cells assessed as increase in intracellular calcium mobilization by fluo-4AM dye based FLIPR assayAgonist activity at human CaSR expressed in HEK293 cells assessed as increase in intracellular calcium mobilization by fluo-4AM dye based FLIPR assay |
ChEMBL | 488 | 11 | 4 | 5 | 4.1 | C[C@@H](N[C@H]1CCN(c2ccc(C(=O)N[C@H](CCCCN)C(=O)O)cc2)C1)c1cccc2ccccc12 | 10.1016/j.bmcl.2017.09.008 | |
| 52946350 | 17191 | 0 | None | - | 1 | Human | 7.0 | pEC50 | = | 7 | Functional | Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay |
ChEMBL | 323 | 2 | 1 | 3 | 4.9 | CC(O)(c1ccc(Cl)c(Cl)c1)c1nc2ccccc2s1 | 10.1016/j.bmcl.2010.07.077 | |
| CHEMBL1256303 | 17191 | 0 | None | - | 1 | Human | 7.0 | pEC50 | = | 7 | Functional | Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay |
ChEMBL | 323 | 2 | 1 | 3 | 4.9 | CC(O)(c1ccc(Cl)c(Cl)c1)c1nc2ccccc2s1 | 10.1016/j.bmcl.2010.07.077 | |
| 52946370 | 17204 | 0 | None | - | 1 | Human | 7.0 | pEC50 | = | 7 | Functional | Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay |
ChEMBL | 323 | 2 | 1 | 3 | 4.9 | CC(O)(c1nc2ccccc2s1)c1ccc(Cl)cc1Cl | 10.1016/j.bmcl.2010.07.077 | |
| CHEMBL1256404 | 17204 | 0 | None | - | 1 | Human | 7.0 | pEC50 | = | 7 | Functional | Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay |
ChEMBL | 323 | 2 | 1 | 3 | 4.9 | CC(O)(c1nc2ccccc2s1)c1ccc(Cl)cc1Cl | 10.1016/j.bmcl.2010.07.077 | |
| 73353386 | 89619 | 0 | None | - | 1 | Human | 7.0 | pEC50 | = | 7 | Functional | Positive allosteric modulation of human CaSR expressed in CHO cells assessed as increase in intracellular calcium level after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR expressed in CHO cells assessed as increase in intracellular calcium level after 5 hrs by luciferase reporter gene assay |
ChEMBL | 544 | 10 | 2 | 6 | 5.4 | O=C(O)c1ccc2nc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)sc2c1 | 10.1016/j.bmcl.2013.01.077 | |
| CHEMBL2375383 | 89619 | 0 | None | - | 1 | Human | 7.0 | pEC50 | = | 7 | Functional | Positive allosteric modulation of human CaSR expressed in CHO cells assessed as increase in intracellular calcium level after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR expressed in CHO cells assessed as increase in intracellular calcium level after 5 hrs by luciferase reporter gene assay |
ChEMBL | 544 | 10 | 2 | 6 | 5.4 | O=C(O)c1ccc2nc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)sc2c1 | 10.1016/j.bmcl.2013.01.077 | |
| 719 | 784 | 5 | None | 1 | 3 | Rat | 6.0 | pEC50 | = | 6 | Functional | Ability to stimulate [3H]inositol phosphates accumulation in CHO cells expressing rat Calcium sensing receptor (CaSR) at 2 mM [Ca2+]Ability to stimulate [3H]inositol phosphates accumulation in CHO cells expressing rat Calcium sensing receptor (CaSR) at 2 mM [Ca2+] |
ChEMBL | 300 | 4 | 2 | 1 | 5.2 | C[C@H](c1cccc2c1cccc2)NCc1cc2c([nH]1)cccc2 | 10.1016/j.bmcl.2004.03.056 | |
| 9882793 | 784 | 5 | None | 1 | 3 | Rat | 6.0 | pEC50 | = | 6 | Functional | Ability to stimulate [3H]inositol phosphates accumulation in CHO cells expressing rat Calcium sensing receptor (CaSR) at 2 mM [Ca2+]Ability to stimulate [3H]inositol phosphates accumulation in CHO cells expressing rat Calcium sensing receptor (CaSR) at 2 mM [Ca2+] |
ChEMBL | 300 | 4 | 2 | 1 | 5.2 | C[C@H](c1cccc2c1cccc2)NCc1cc2c([nH]1)cccc2 | 10.1016/j.bmcl.2004.03.056 | |
| CHEMBL1801356 | 784 | 5 | None | 1 | 3 | Rat | 6.0 | pEC50 | = | 6 | Functional | Ability to stimulate [3H]inositol phosphates accumulation in CHO cells expressing rat Calcium sensing receptor (CaSR) at 2 mM [Ca2+]Ability to stimulate [3H]inositol phosphates accumulation in CHO cells expressing rat Calcium sensing receptor (CaSR) at 2 mM [Ca2+] |
ChEMBL | 300 | 4 | 2 | 1 | 5.2 | C[C@H](c1cccc2c1cccc2)NCc1cc2c([nH]1)cccc2 | 10.1016/j.bmcl.2004.03.056 | |
| 53377661 | 148456 | 0 | None | - | 1 | Human | 6.0 | pEC50 | = | 6 | Functional | Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 ul/well of a compound dissolved in a 0.1% BSA-containing assay buffer to measure 3-minute change in the fluorescence intensity.Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 ul/well of a compound dissolved in a 0.1% BSA-containing assay buffer to measure 3-minute change in the fluorescence intensity. |
ChEMBL | 283 | 5 | 6 | 5 | -0.4 | N[C@@H](CNC(=O)Nc1cccc(C(=O)O)c1O)C(=O)O | nan | |
| CHEMBL3937957 | 148456 | 0 | None | - | 1 | Human | 6.0 | pEC50 | = | 6 | Functional | Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 ul/well of a compound dissolved in a 0.1% BSA-containing assay buffer to measure 3-minute change in the fluorescence intensity.Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 ul/well of a compound dissolved in a 0.1% BSA-containing assay buffer to measure 3-minute change in the fluorescence intensity. |
ChEMBL | 283 | 5 | 6 | 5 | -0.4 | N[C@@H](CNC(=O)Nc1cccc(C(=O)O)c1O)C(=O)O | nan | |
| 71542724 | 151671 | 0 | None | - | 1 | Human | 6.0 | pEC50 | = | 6 | Functional | Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 ul/well of a compound dissolved in a 0.1% BSA-containing assay buffer to measure 3-minute change in the fluorescence intensity.Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 ul/well of a compound dissolved in a 0.1% BSA-containing assay buffer to measure 3-minute change in the fluorescence intensity. |
ChEMBL | 333 | 6 | 5 | 6 | -0.5 | COc1ccc(S(=O)(=O)O)cc1NC(=O)NC[C@H](N)C(=O)O | nan | |
| CHEMBL3964061 | 151671 | 0 | None | - | 1 | Human | 6.0 | pEC50 | = | 6 | Functional | Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 ul/well of a compound dissolved in a 0.1% BSA-containing assay buffer to measure 3-minute change in the fluorescence intensity.Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 ul/well of a compound dissolved in a 0.1% BSA-containing assay buffer to measure 3-minute change in the fluorescence intensity. |
ChEMBL | 333 | 6 | 5 | 6 | -0.5 | COc1ccc(S(=O)(=O)O)cc1NC(=O)NC[C@H](N)C(=O)O | nan | |
| 73356416 | 89620 | 0 | None | - | 1 | Human | 6.0 | pEC50 | = | 6 | Functional | Positive allosteric modulation of human CaSR expressed in CHO cells assessed as increase in intracellular calcium level after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR expressed in CHO cells assessed as increase in intracellular calcium level after 5 hrs by luciferase reporter gene assay |
ChEMBL | 544 | 11 | 1 | 6 | 6.1 | CCOc1ccc2nc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)sc2c1 | 10.1016/j.bmcl.2013.01.077 | |
| CHEMBL2375385 | 89620 | 0 | None | - | 1 | Human | 6.0 | pEC50 | = | 6 | Functional | Positive allosteric modulation of human CaSR expressed in CHO cells assessed as increase in intracellular calcium level after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR expressed in CHO cells assessed as increase in intracellular calcium level after 5 hrs by luciferase reporter gene assay |
ChEMBL | 544 | 11 | 1 | 6 | 6.1 | CCOc1ccc2nc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)sc2c1 | 10.1016/j.bmcl.2013.01.077 | |
| 16735430 | 89848 | 0 | None | - | 1 | Human | 6.0 | pEC50 | = | 6 | Functional | Positive allosteric modulation of human CaSR expressed in CHO cells assessed as increase in intracellular calcium level after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR expressed in CHO cells assessed as increase in intracellular calcium level after 5 hrs by luciferase reporter gene assay |
ChEMBL | 444 | 9 | 1 | 4 | 4.5 | O=C(Nc1cccnc1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 | 10.1016/j.bmcl.2013.01.077 | |
| CHEMBL2377726 | 89848 | 0 | None | - | 1 | Human | 6.0 | pEC50 | = | 6 | Functional | Positive allosteric modulation of human CaSR expressed in CHO cells assessed as increase in intracellular calcium level after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR expressed in CHO cells assessed as increase in intracellular calcium level after 5 hrs by luciferase reporter gene assay |
ChEMBL | 444 | 9 | 1 | 4 | 4.5 | O=C(Nc1cccnc1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 | 10.1016/j.bmcl.2013.01.077 | |
| 127026651 | 137561 | 0 | None | - | 1 | Rat | 7.0 | pEC50 | = | 7.0 | Functional | Agonist activity at rat brain CaSR expressed in CHO cells assessed as inositol phosphate production in presence of 3 mM extracellular Ca2+ by IP-one assayAgonist activity at rat brain CaSR expressed in CHO cells assessed as inositol phosphate production in presence of 3 mM extracellular Ca2+ by IP-one assay |
ChEMBL | 316 | 4 | 3 | 2 | 4.9 | C[C@@H](NCc1cc2c(O)cccc2[nH]1)c1cccc2ccccc12 | 10.1016/j.bmc.2015.12.019 | |
| CHEMBL3754639 | 137561 | 0 | None | - | 1 | Rat | 7.0 | pEC50 | = | 7.0 | Functional | Agonist activity at rat brain CaSR expressed in CHO cells assessed as inositol phosphate production in presence of 3 mM extracellular Ca2+ by IP-one assayAgonist activity at rat brain CaSR expressed in CHO cells assessed as inositol phosphate production in presence of 3 mM extracellular Ca2+ by IP-one assay |
ChEMBL | 316 | 4 | 3 | 2 | 4.9 | C[C@@H](NCc1cc2c(O)cccc2[nH]1)c1cccc2ccccc12 | 10.1016/j.bmc.2015.12.019 | |
| 127026651 | 137561 | 0 | None | - | 1 | Rat | 7.0 | pEC50 | = | 7.0 | Functional | Agonist activity at rat brain CaSR expressed in CHO cells assessed as inositol phosphate production in presence of 3 mM extracellular Ca2+ by IP-one assayAgonist activity at rat brain CaSR expressed in CHO cells assessed as inositol phosphate production in presence of 3 mM extracellular Ca2+ by IP-one assay |
ChEMBL | 316 | 4 | 3 | 2 | 4.9 | C[C@@H](NCc1cc2c(O)cccc2[nH]1)c1cccc2ccccc12 | 10.1016/j.bmc.2015.12.019 | |
| CHEMBL3754639 | 137561 | 0 | None | - | 1 | Rat | 7.0 | pEC50 | = | 7.0 | Functional | Agonist activity at rat brain CaSR expressed in CHO cells assessed as inositol phosphate production in presence of 3 mM extracellular Ca2+ by IP-one assayAgonist activity at rat brain CaSR expressed in CHO cells assessed as inositol phosphate production in presence of 3 mM extracellular Ca2+ by IP-one assay |
ChEMBL | 316 | 4 | 3 | 2 | 4.9 | C[C@@H](NCc1cc2c(O)cccc2[nH]1)c1cccc2ccccc12 | 10.1016/j.bmc.2015.12.019 | |
| 49866114 | 16249 | 0 | None | - | 1 | Human | 7.0 | pEC50 | = | 7.0 | Functional | Positive allosteric modulation of calcium sensing receptor by FLIPR assay in presence of extracellular calciumPositive allosteric modulation of calcium sensing receptor by FLIPR assay in presence of extracellular calcium |
ChEMBL | 439 | 6 | 1 | 2 | 7.1 | C[C@@H](NCc1ccc(OC(F)(F)F)c(-c2ccc(C(F)(F)F)cc2)c1)c1ccccc1 | 10.1016/j.bmcl.2010.07.060 | |
| CHEMBL1224426 | 16249 | 0 | None | - | 1 | Human | 7.0 | pEC50 | = | 7.0 | Functional | Positive allosteric modulation of calcium sensing receptor by FLIPR assay in presence of extracellular calciumPositive allosteric modulation of calcium sensing receptor by FLIPR assay in presence of extracellular calcium |
ChEMBL | 439 | 6 | 1 | 2 | 7.1 | C[C@@H](NCc1ccc(OC(F)(F)F)c(-c2ccc(C(F)(F)F)cc2)c1)c1ccccc1 | 10.1016/j.bmcl.2010.07.060 | |
| 145946881 | 167614 | 0 | None | - | 1 | Human | 6.0 | pEC50 | = | 6.0 | Functional | Agonist activity at human CaSR expressed in CHO cells assessed as increase in intracellular calcium mobilization after 1 hr by Fura-2 dye-based fluorescence assayAgonist activity at human CaSR expressed in CHO cells assessed as increase in intracellular calcium mobilization after 1 hr by Fura-2 dye-based fluorescence assay |
ChEMBL | 374 | 5 | 2 | 3 | 4.9 | C[C@@H](N[C@H]1CCCN(c2ccc(C(=O)O)cc2)C1)c1cccc2ccccc12 | 10.1016/j.bmcl.2018.04.055 | |
| CHEMBL4130141 | 167614 | 0 | None | - | 1 | Human | 6.0 | pEC50 | = | 6.0 | Functional | Agonist activity at human CaSR expressed in CHO cells assessed as increase in intracellular calcium mobilization after 1 hr by Fura-2 dye-based fluorescence assayAgonist activity at human CaSR expressed in CHO cells assessed as increase in intracellular calcium mobilization after 1 hr by Fura-2 dye-based fluorescence assay |
ChEMBL | 374 | 5 | 2 | 3 | 4.9 | C[C@@H](N[C@H]1CCCN(c2ccc(C(=O)O)cc2)C1)c1cccc2ccccc12 | 10.1016/j.bmcl.2018.04.055 | |
| CHEMBL4301203 | 167614 | 0 | None | - | 1 | Human | 6.0 | pEC50 | = | 6.0 | Functional | Agonist activity at human CaSR expressed in CHO cells assessed as increase in intracellular calcium mobilization after 1 hr by Fura-2 dye-based fluorescence assayAgonist activity at human CaSR expressed in CHO cells assessed as increase in intracellular calcium mobilization after 1 hr by Fura-2 dye-based fluorescence assay |
ChEMBL | 374 | 5 | 2 | 3 | 4.9 | C[C@@H](N[C@H]1CCCN(c2ccc(C(=O)O)cc2)C1)c1cccc2ccccc12 | 10.1016/j.bmcl.2018.04.055 | |
| 89346565 | 149813 | 0 | None | - | 1 | Human | 6.0 | pEC50 | = | 6.0 | Functional | Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 ul/well of a compound dissolved in a 0.1% BSA-containing assay buffer to measure 3-minute change in the fluorescence intensity.Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 ul/well of a compound dissolved in a 0.1% BSA-containing assay buffer to measure 3-minute change in the fluorescence intensity. |
ChEMBL | 363 | 6 | 4 | 7 | 1.5 | N#CCC[C@H](N)COC(=O)Nc1cc(Cl)cc(S(=O)(=O)O)c1O | nan | |
| CHEMBL3948703 | 149813 | 0 | None | - | 1 | Human | 6.0 | pEC50 | = | 6.0 | Functional | Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 ul/well of a compound dissolved in a 0.1% BSA-containing assay buffer to measure 3-minute change in the fluorescence intensity.Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 ul/well of a compound dissolved in a 0.1% BSA-containing assay buffer to measure 3-minute change in the fluorescence intensity. |
ChEMBL | 363 | 6 | 4 | 7 | 1.5 | N#CCC[C@H](N)COC(=O)Nc1cc(Cl)cc(S(=O)(=O)O)c1O | nan | |
| 71542726 | 152082 | 0 | None | - | 1 | Human | 6.0 | pEC50 | = | 6.0 | Functional | Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 ul/well of a compound dissolved in a 0.1% BSA-containing assay buffer to measure 3-minute change in the fluorescence intensity.Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 ul/well of a compound dissolved in a 0.1% BSA-containing assay buffer to measure 3-minute change in the fluorescence intensity. |
ChEMBL | 331 | 5 | 5 | 5 | 0.1 | Cc1cc(C)c(S(=O)(=O)O)cc1NC(=O)NC[C@H](N)C(=O)O | nan | |
| CHEMBL3967566 | 152082 | 0 | None | - | 1 | Human | 6.0 | pEC50 | = | 6.0 | Functional | Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 ul/well of a compound dissolved in a 0.1% BSA-containing assay buffer to measure 3-minute change in the fluorescence intensity.Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 ul/well of a compound dissolved in a 0.1% BSA-containing assay buffer to measure 3-minute change in the fluorescence intensity. |
ChEMBL | 331 | 5 | 5 | 5 | 0.1 | Cc1cc(C)c(S(=O)(=O)O)cc1NC(=O)NC[C@H](N)C(=O)O | nan | |
| 127028250 | 137445 | 0 | None | - | 1 | Rat | 7.0 | pEC50 | = | 7.0 | Functional | Agonist activity at rat brain CaSR expressed in CHO cells assessed as inositol phosphate production in presence of 3 mM extracellular Ca2+ by IP-one assayAgonist activity at rat brain CaSR expressed in CHO cells assessed as inositol phosphate production in presence of 3 mM extracellular Ca2+ by IP-one assay |
ChEMBL | 316 | 4 | 3 | 2 | 4.9 | C[C@@H](NCc1cc2cc(O)ccc2[nH]1)c1cccc2ccccc12 | 10.1016/j.bmc.2015.12.019 | |
| CHEMBL3753595 | 137445 | 0 | None | - | 1 | Rat | 7.0 | pEC50 | = | 7.0 | Functional | Agonist activity at rat brain CaSR expressed in CHO cells assessed as inositol phosphate production in presence of 3 mM extracellular Ca2+ by IP-one assayAgonist activity at rat brain CaSR expressed in CHO cells assessed as inositol phosphate production in presence of 3 mM extracellular Ca2+ by IP-one assay |
ChEMBL | 316 | 4 | 3 | 2 | 4.9 | C[C@@H](NCc1cc2cc(O)ccc2[nH]1)c1cccc2ccccc12 | 10.1016/j.bmc.2015.12.019 | |
| 127028250 | 137445 | 0 | None | - | 1 | Rat | 7.0 | pEC50 | = | 7.0 | Functional | Agonist activity at rat brain CaSR expressed in CHO cells assessed as inositol phosphate production in presence of 3 mM extracellular Ca2+ by IP-one assayAgonist activity at rat brain CaSR expressed in CHO cells assessed as inositol phosphate production in presence of 3 mM extracellular Ca2+ by IP-one assay |
ChEMBL | 316 | 4 | 3 | 2 | 4.9 | C[C@@H](NCc1cc2cc(O)ccc2[nH]1)c1cccc2ccccc12 | 10.1016/j.bmc.2015.12.019 | |
| CHEMBL3753595 | 137445 | 0 | None | - | 1 | Rat | 7.0 | pEC50 | = | 7.0 | Functional | Agonist activity at rat brain CaSR expressed in CHO cells assessed as inositol phosphate production in presence of 3 mM extracellular Ca2+ by IP-one assayAgonist activity at rat brain CaSR expressed in CHO cells assessed as inositol phosphate production in presence of 3 mM extracellular Ca2+ by IP-one assay |
ChEMBL | 316 | 4 | 3 | 2 | 4.9 | C[C@@H](NCc1cc2cc(O)ccc2[nH]1)c1cccc2ccccc12 | 10.1016/j.bmc.2015.12.019 | |
| 44542482 | 198445 | 0 | None | - | 1 | Human | 5.9 | pEC50 | = | 5.9 | Functional | Activity at human CaSR expressed in HEK293 cells assessed as calcium release by FLIPR assayActivity at human CaSR expressed in HEK293 cells assessed as calcium release by FLIPR assay |
ChEMBL | 373 | 6 | 1 | 3 | 5.7 | CC[C@@H](N[C@H](C)c1ccccc1)c1ccn(-c2ccc(C(F)(F)F)cc2)n1 | 10.1021/jm9012278 | |
| CHEMBL577306 | 198445 | 0 | None | - | 1 | Human | 5.9 | pEC50 | = | 5.9 | Functional | Activity at human CaSR expressed in HEK293 cells assessed as calcium release by FLIPR assayActivity at human CaSR expressed in HEK293 cells assessed as calcium release by FLIPR assay |
ChEMBL | 373 | 6 | 1 | 3 | 5.7 | CC[C@@H](N[C@H](C)c1ccccc1)c1ccn(-c2ccc(C(F)(F)F)cc2)n1 | 10.1021/jm9012278 | |
| 137635178 | 155838 | 0 | None | - | 1 | Human | 7.9 | pEC50 | = | 7.9 | Functional | Agonist activity at human CaSR expressed in HEK293 cells assessed as increase in intracellular calcium mobilization by fluo-4AM dye based FLIPR assayAgonist activity at human CaSR expressed in HEK293 cells assessed as increase in intracellular calcium mobilization by fluo-4AM dye based FLIPR assay |
ChEMBL | 402 | 7 | 3 | 4 | 3.5 | C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCCN)cc2)C1)c1cccc2ccccc12 | 10.1016/j.bmcl.2017.09.008 | |
| CHEMBL4060025 | 155838 | 0 | None | - | 1 | Human | 7.9 | pEC50 | = | 7.9 | Functional | Agonist activity at human CaSR expressed in HEK293 cells assessed as increase in intracellular calcium mobilization by fluo-4AM dye based FLIPR assayAgonist activity at human CaSR expressed in HEK293 cells assessed as increase in intracellular calcium mobilization by fluo-4AM dye based FLIPR assay |
ChEMBL | 402 | 7 | 3 | 4 | 3.5 | C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCCN)cc2)C1)c1cccc2ccccc12 | 10.1016/j.bmcl.2017.09.008 | |
| 11706057 | 156492 | 1 | None | - | 1 | Human | 7.9 | pEC50 | = | 7.9 | Functional | Agonist activity at human CaSR expressed in HEK293 cells assessed as increase in intracellular calcium mobilization by fluo-4AM dye based FLIPR assayAgonist activity at human CaSR expressed in HEK293 cells assessed as increase in intracellular calcium mobilization by fluo-4AM dye based FLIPR assay |
ChEMBL | 466 | 9 | 2 | 5 | 3.6 | C[C@@H](N[C@H]1CCN(c2ccc(S(=O)(=O)NCCN(C)C)cc2)C1)c1cccc2ccccc12 | 10.1016/j.bmcl.2017.09.008 | |
| CHEMBL4067601 | 156492 | 1 | None | - | 1 | Human | 7.9 | pEC50 | = | 7.9 | Functional | Agonist activity at human CaSR expressed in HEK293 cells assessed as increase in intracellular calcium mobilization by fluo-4AM dye based FLIPR assayAgonist activity at human CaSR expressed in HEK293 cells assessed as increase in intracellular calcium mobilization by fluo-4AM dye based FLIPR assay |
ChEMBL | 466 | 9 | 2 | 5 | 3.6 | C[C@@H](N[C@H]1CCN(c2ccc(S(=O)(=O)NCCN(C)C)cc2)C1)c1cccc2ccccc12 | 10.1016/j.bmcl.2017.09.008 | |
| 11682773 | 167740 | 0 | None | -15 | 2 | Human | 6.9 | pEC50 | = | 6.9 | Functional | Agonist activity at human CaSR expressed in CHO cells assessed as increase in intracellular calcium mobilization after 1 hr by Fura-2 dye-based fluorescence assayAgonist activity at human CaSR expressed in CHO cells assessed as increase in intracellular calcium mobilization after 1 hr by Fura-2 dye-based fluorescence assay |
ChEMBL | 400 | 5 | 1 | 3 | 5.7 | C[C@@H](N[C@H]1CCN(c2ccc(OC(F)(F)F)cc2)C1)c1cccc2ccccc12 | 10.1016/j.bmcl.2018.04.055 | |
| CHEMBL4129011 | 167740 | 0 | None | -15 | 2 | Human | 6.9 | pEC50 | = | 6.9 | Functional | Agonist activity at human CaSR expressed in CHO cells assessed as increase in intracellular calcium mobilization after 1 hr by Fura-2 dye-based fluorescence assayAgonist activity at human CaSR expressed in CHO cells assessed as increase in intracellular calcium mobilization after 1 hr by Fura-2 dye-based fluorescence assay |
ChEMBL | 400 | 5 | 1 | 3 | 5.7 | C[C@@H](N[C@H]1CCN(c2ccc(OC(F)(F)F)cc2)C1)c1cccc2ccccc12 | 10.1016/j.bmcl.2018.04.055 | |
| CHEMBL4302857 | 167740 | 0 | None | -15 | 2 | Human | 6.9 | pEC50 | = | 6.9 | Functional | Agonist activity at human CaSR expressed in CHO cells assessed as increase in intracellular calcium mobilization after 1 hr by Fura-2 dye-based fluorescence assayAgonist activity at human CaSR expressed in CHO cells assessed as increase in intracellular calcium mobilization after 1 hr by Fura-2 dye-based fluorescence assay |
ChEMBL | 400 | 5 | 1 | 3 | 5.7 | C[C@@H](N[C@H]1CCN(c2ccc(OC(F)(F)F)cc2)C1)c1cccc2ccccc12 | 10.1016/j.bmcl.2018.04.055 | |
| 71542641 | 154226 | 0 | None | - | 1 | Human | 5.9 | pEC50 | = | 5.9 | Functional | Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 ul/well of a compound dissolved in a 0.1% BSA-containing assay buffer to measure 3-minute change in the fluorescence intensity.Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 ul/well of a compound dissolved in a 0.1% BSA-containing assay buffer to measure 3-minute change in the fluorescence intensity. |
ChEMBL | 489 | 9 | 5 | 6 | 2.4 | N[C@@H](CCC(=O)Nc1cc(Cl)cc(S(=O)(=O)O)c1O)C(=O)NCCc1cccc(Cl)c1 | nan | |
| CHEMBL3986052 | 154226 | 0 | None | - | 1 | Human | 5.9 | pEC50 | = | 5.9 | Functional | Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 ul/well of a compound dissolved in a 0.1% BSA-containing assay buffer to measure 3-minute change in the fluorescence intensity.Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 ul/well of a compound dissolved in a 0.1% BSA-containing assay buffer to measure 3-minute change in the fluorescence intensity. |
ChEMBL | 489 | 9 | 5 | 6 | 2.4 | N[C@@H](CCC(=O)Nc1cc(Cl)cc(S(=O)(=O)O)c1O)C(=O)NCCc1cccc(Cl)c1 | nan | |
| 7145229 | 16200 | 4 | None | - | 1 | Human | 5.9 | pEC50 | = | 5.9 | Functional | Positive allosteric modulation of calcium sensing receptor by FLIPR assay in presence of extracellular calciumPositive allosteric modulation of calcium sensing receptor by FLIPR assay in presence of extracellular calcium |
ChEMBL | 241 | 5 | 1 | 2 | 3.5 | COc1cccc([C@@H](C)NCc2ccccc2)c1 | 10.1016/j.bmcl.2010.07.060 | |
Showing 1 to 50 of 1,235 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
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
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 |
| 72725441 | 104074 | 0 | None | - | 0 | Human | 8.0 | pEC50 | = | 8 | Binding | Activation of human CaSRActivation of human CaSR |
ChEMBL | 675 | 11 | 2 | 7 | 5.8 | NS(=O)(=O)c1ccc(-c2nc(NC(=O)N(CCC(c3ccc(F)cc3)c3ccc(F)cc3)CCN3CCOCC3)sc2Cl)cc1 | 10.1016/j.bmcl.2013.10.050 | ||
| CHEMBL3093427 | 104074 | 0 | None | - | 0 | Human | 8.0 | pEC50 | = | 8 | Binding | Activation of human CaSRActivation of human CaSR |
ChEMBL | 675 | 11 | 2 | 7 | 5.8 | NS(=O)(=O)c1ccc(-c2nc(NC(=O)N(CCC(c3ccc(F)cc3)c3ccc(F)cc3)CCN3CCOCC3)sc2Cl)cc1 | 10.1016/j.bmcl.2013.10.050 | ||
| 16738376 | 88138 | 0 | None | - | 0 | Human | 7.0 | pEC50 | = | 7 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 501 | 10 | 1 | 5 | 4.9 | COC(=O)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1 | 10.1016/j.bmcl.2013.01.078 | ||
| CHEMBL2346786 | 88138 | 0 | None | - | 0 | Human | 7.0 | pEC50 | = | 7 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 501 | 10 | 1 | 5 | 4.9 | COC(=O)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1 | 10.1016/j.bmcl.2013.01.078 | ||
| 69029375 | 88450 | 0 | None | - | 0 | Human | 7.0 | pEC50 | = | 7 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 528 | 11 | 1 | 5 | 5.2 | COC(=O)c1cccc(NC(=O)N(CCCN2CCN(C)CC2)CCC(c2ccccc2)c2ccccc2)c1 | 10.1016/j.bmcl.2013.01.078 | ||
| CHEMBL2349577 | 88450 | 0 | None | - | 0 | Human | 7.0 | pEC50 | = | 7 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 528 | 11 | 1 | 5 | 5.2 | COC(=O)c1cccc(NC(=O)N(CCCN2CCN(C)CC2)CCC(c2ccccc2)c2ccccc2)c1 | 10.1016/j.bmcl.2013.01.078 | ||
| 71719613 | 88447 | 0 | None | - | 0 | Human | 6.0 | pEC50 | = | 6 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 526 | 11 | 3 | 7 | 4.3 | O=C(Nc1cccc(Nc2nnn[nH]2)c1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 | 10.1016/j.bmcl.2013.01.078 | ||
| CHEMBL2349574 | 88447 | 0 | None | - | 0 | Human | 6.0 | pEC50 | = | 6 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 526 | 11 | 3 | 7 | 4.3 | O=C(Nc1cccc(Nc2nnn[nH]2)c1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 | 10.1016/j.bmcl.2013.01.078 | ||
| 58938083 | 88455 | 0 | None | - | 0 | Human | 6.0 | pEC50 | = | 6 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 571 | 11 | 1 | 5 | 6.7 | CC(OC(=O)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1)C(C)(C)C | 10.1016/j.bmcl.2013.01.078 | ||
| CHEMBL2349582 | 88455 | 0 | None | - | 0 | Human | 6.0 | pEC50 | = | 6 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 571 | 11 | 1 | 5 | 6.7 | CC(OC(=O)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1)C(C)(C)C | 10.1016/j.bmcl.2013.01.078 | ||
| 16737653 | 88466 | 0 | None | - | 0 | Human | 6.0 | pEC50 | = | 6 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 521 | 10 | 1 | 5 | 4.5 | CS(=O)(=O)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1 | 10.1016/j.bmcl.2013.01.078 | ||
| CHEMBL2349593 | 88466 | 0 | None | - | 0 | Human | 6.0 | pEC50 | = | 6 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 521 | 10 | 1 | 5 | 4.5 | CS(=O)(=O)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1 | 10.1016/j.bmcl.2013.01.078 | ||
| 3336 | 95001 | 30 | None | - | 1 | Human | 6.0 | pEC50 | = | 6 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 315 | 7 | 1 | 1 | 5.6 | CC(NCCC(c1ccccc1)c1ccccc1)c1ccccc1 | 10.1016/j.bmcl.2013.01.078 | ||
| CHEMBL1405922 | 95001 | 30 | None | - | 1 | Human | 6.0 | pEC50 | = | 6 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 315 | 7 | 1 | 1 | 5.6 | CC(NCCC(c1ccccc1)c1ccccc1)c1ccccc1 | 10.1016/j.bmcl.2013.01.078 | ||
| CHEMBL254832 | 95001 | 30 | None | - | 1 | Human | 6.0 | pEC50 | = | 6 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 315 | 7 | 1 | 1 | 5.6 | CC(NCCC(c1ccccc1)c1ccccc1)c1ccccc1 | 10.1016/j.bmcl.2013.01.078 | ||
| 71579790 | 88133 | 0 | None | - | 0 | Human | 5.0 | pEC50 | = | 5 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 501 | 10 | 1 | 5 | 4.5 | COC(=O)c1cccc(N(CCN2CCOCC2)C(=O)NCCC(c2ccccc2)c2ccccc2)c1 | 10.1016/j.bmcl.2013.01.078 | ||
| CHEMBL2346781 | 88133 | 0 | None | - | 0 | Human | 5.0 | pEC50 | = | 5 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 501 | 10 | 1 | 5 | 4.5 | COC(=O)c1cccc(N(CCN2CCOCC2)C(=O)NCCC(c2ccccc2)c2ccccc2)c1 | 10.1016/j.bmcl.2013.01.078 | ||
| 25175312 | 88137 | 0 | None | - | 0 | Human | 5.0 | pEC50 | = | 5 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 498 | 10 | 1 | 3 | 7.5 | COC(=O)c1cccc(NC(=O)N(CCC2CCCCC2)CCC(c2ccccc2)c2ccccc2)c1 | 10.1016/j.bmcl.2013.01.078 | ||
| CHEMBL2346785 | 88137 | 0 | None | - | 0 | Human | 5.0 | pEC50 | = | 5 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 498 | 10 | 1 | 3 | 7.5 | COC(=O)c1cccc(NC(=O)N(CCC2CCCCC2)CCC(c2ccccc2)c2ccccc2)c1 | 10.1016/j.bmcl.2013.01.078 | ||
| 72725153 | 104060 | 0 | None | - | 0 | Human | 6.0 | pEC50 | = | 6.0 | Binding | Activation of human CaSRActivation of human CaSR |
ChEMBL | 511 | 10 | 1 | 6 | 5.1 | O=C(Nc1nnc(-c2ccccc2)o1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 | 10.1016/j.bmcl.2013.10.050 | ||
| CHEMBL3093413 | 104060 | 0 | None | - | 0 | Human | 6.0 | pEC50 | = | 6.0 | Binding | Activation of human CaSRActivation of human CaSR |
ChEMBL | 511 | 10 | 1 | 6 | 5.1 | O=C(Nc1nnc(-c2ccccc2)o1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 | 10.1016/j.bmcl.2013.10.050 | ||
| 16737828 | 88463 | 0 | None | - | 0 | Human | 6.9 | pEC50 | = | 6.9 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 489 | 10 | 1 | 4 | 5.8 | CSc1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1 | 10.1016/j.bmcl.2013.01.078 | ||
| CHEMBL2349590 | 88463 | 0 | None | - | 0 | Human | 6.9 | pEC50 | = | 6.9 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 489 | 10 | 1 | 4 | 5.8 | CSc1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1 | 10.1016/j.bmcl.2013.01.078 | ||
| 69026659 | 88139 | 0 | None | - | 0 | Human | 6.8 | pEC50 | = | 6.8 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 515 | 11 | 1 | 5 | 5.3 | COC(=O)c1cccc(NC(=O)N(CCCN2CCOCC2)CCC(c2ccccc2)c2ccccc2)c1 | 10.1016/j.bmcl.2013.01.078 | ||
| CHEMBL2346787 | 88139 | 0 | None | - | 0 | Human | 6.8 | pEC50 | = | 6.8 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 515 | 11 | 1 | 5 | 5.3 | COC(=O)c1cccc(NC(=O)N(CCCN2CCOCC2)CCC(c2ccccc2)c2ccccc2)c1 | 10.1016/j.bmcl.2013.01.078 | ||
| 16736324 | 88446 | 0 | None | - | 0 | Human | 6.8 | pEC50 | = | 6.8 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 576 | 10 | 1 | 5 | 7.4 | O=C(Nc1cccc(-c2nc3ccccc3s2)c1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 | 10.1016/j.bmcl.2013.01.078 | ||
| CHEMBL2349573 | 88446 | 0 | None | - | 0 | Human | 6.8 | pEC50 | = | 6.8 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 576 | 10 | 1 | 5 | 7.4 | O=C(Nc1cccc(-c2nc3ccccc3s2)c1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 | 10.1016/j.bmcl.2013.01.078 | ||
| 16737152 | 88453 | 0 | None | - | 0 | Human | 6.8 | pEC50 | = | 6.8 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 529 | 11 | 1 | 5 | 5.6 | CC(C)OC(=O)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1 | 10.1016/j.bmcl.2013.01.078 | ||
| CHEMBL2349580 | 88453 | 0 | None | - | 0 | Human | 6.8 | pEC50 | = | 6.8 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 529 | 11 | 1 | 5 | 5.6 | CC(C)OC(=O)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1 | 10.1016/j.bmcl.2013.01.078 | ||
| 58938101 | 88457 | 0 | None | - | 0 | Human | 6.8 | pEC50 | = | 6.8 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 531 | 12 | 2 | 6 | 4.2 | O=C(OCCO)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1 | 10.1016/j.bmcl.2013.01.078 | ||
| CHEMBL2349584 | 88457 | 0 | None | - | 0 | Human | 6.8 | pEC50 | = | 6.8 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 531 | 12 | 2 | 6 | 4.2 | O=C(OCCO)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1 | 10.1016/j.bmcl.2013.01.078 | ||
| 16737168 | 88459 | 0 | None | - | 0 | Human | 6.8 | pEC50 | = | 6.8 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 499 | 11 | 1 | 4 | 5.7 | CCC(=O)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1 | 10.1016/j.bmcl.2013.01.078 | ||
| CHEMBL2349586 | 88459 | 0 | None | - | 0 | Human | 6.8 | pEC50 | = | 6.8 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 499 | 11 | 1 | 4 | 5.7 | CCC(=O)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1 | 10.1016/j.bmcl.2013.01.078 | ||
| 16735045 | 88476 | 0 | None | - | 0 | Human | 6.8 | pEC50 | = | 6.8 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 509 | 10 | 1 | 4 | 6.3 | O=C(Nc1cccc(-c2ccco2)c1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 | 10.1016/j.bmcl.2013.01.078 | ||
| CHEMBL2349602 | 88476 | 0 | None | - | 0 | Human | 6.8 | pEC50 | = | 6.8 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 509 | 10 | 1 | 4 | 6.3 | O=C(Nc1cccc(-c2ccco2)c1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 | 10.1016/j.bmcl.2013.01.078 | ||
| 16736322 | 88478 | 0 | None | - | 0 | Human | 6.8 | pEC50 | = | 6.8 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 524 | 10 | 1 | 5 | 6.0 | Cc1cc(-c2cccc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)c2)on1 | 10.1016/j.bmcl.2013.01.078 | ||
| CHEMBL2349604 | 88478 | 0 | None | - | 0 | Human | 6.8 | pEC50 | = | 6.8 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 524 | 10 | 1 | 5 | 6.0 | Cc1cc(-c2cccc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)c2)on1 | 10.1016/j.bmcl.2013.01.078 | ||
| 69025930 | 88134 | 0 | None | - | 0 | Human | 5.8 | pEC50 | = | 5.8 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 444 | 9 | 1 | 3 | 6.2 | COC(=O)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CC(C)C)c1 | 10.1016/j.bmcl.2013.01.078 | ||
| CHEMBL2346782 | 88134 | 0 | None | - | 0 | Human | 5.8 | pEC50 | = | 5.8 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 444 | 9 | 1 | 3 | 6.2 | COC(=O)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CC(C)C)c1 | 10.1016/j.bmcl.2013.01.078 | ||
| 23959728 | 88117 | 0 | None | - | 0 | Human | 4.8 | pEC50 | = | 4.8 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 360 | 7 | 2 | 2 | 5.0 | COc1ccc(NC(=O)NCCC(c2ccccc2)c2ccccc2)cc1 | 10.1016/j.bmcl.2013.01.078 | ||
| CHEMBL2346767 | 88117 | 0 | None | - | 0 | Human | 4.8 | pEC50 | = | 4.8 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 360 | 7 | 2 | 2 | 5.0 | COc1ccc(NC(=O)NCCC(c2ccccc2)c2ccccc2)cc1 | 10.1016/j.bmcl.2013.01.078 | ||
| 59729012 | 88126 | 0 | None | - | 0 | Human | 4.8 | pEC50 | = | 4.8 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 406 | 7 | 2 | 1 | 6.7 | O=C(NCCC(c1ccccc1)c1ccccc1)Nc1cccc(-c2ccccc2)c1 | 10.1016/j.bmcl.2013.01.078 | ||
| CHEMBL2346775 | 88126 | 0 | None | - | 0 | Human | 4.8 | pEC50 | = | 4.8 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 406 | 7 | 2 | 1 | 6.7 | O=C(NCCC(c1ccccc1)c1ccccc1)Nc1cccc(-c2ccccc2)c1 | 10.1016/j.bmcl.2013.01.078 | ||
| 59729055 | 88130 | 0 | None | - | 0 | Human | 4.8 | pEC50 | = | 4.8 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 374 | 8 | 2 | 2 | 4.7 | COc1ccc(CNC(=O)NCCC(c2ccccc2)c2ccccc2)cc1 | 10.1016/j.bmcl.2013.01.078 | ||
| CHEMBL2346779 | 88130 | 0 | None | - | 0 | Human | 4.8 | pEC50 | = | 4.8 | Binding | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay |
ChEMBL | 374 | 8 | 2 | 2 | 4.7 | COc1ccc(CNC(=O)NCCC(c2ccccc2)c2ccccc2)cc1 | 10.1016/j.bmcl.2013.01.078 | ||
| 72725272 | 103820 | 0 | None | - | 0 | Human | 6.8 | pEC50 | = | 6.8 | Binding | Activation of human CaSRActivation of human CaSR |
ChEMBL | 551 | 10 | 1 | 6 | 6.1 | N#Cc1sc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)nc1-c1ccccc1 | 10.1016/j.bmcl.2013.10.050 | ||
| CHEMBL3091483 | 103820 | 0 | None | - | 0 | Human | 6.8 | pEC50 | = | 6.8 | Binding | Activation of human CaSRActivation of human CaSR |
ChEMBL | 551 | 10 | 1 | 6 | 6.1 | N#Cc1sc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)nc1-c1ccccc1 | 10.1016/j.bmcl.2013.10.050 | ||
| 11955290 | 104058 | 0 | None | - | 0 | Human | 7.8 | pEC50 | = | 7.8 | Binding | Activation of human CaSRActivation of human CaSR |
ChEMBL | 619 | 12 | 2 | 7 | 5.6 | CS(=O)(=O)Nc1ccc(-c2csc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)n2)cc1 | 10.1016/j.bmcl.2013.10.050 | ||
| CHEMBL3093411 | 104058 | 0 | None | - | 0 | Human | 7.8 | pEC50 | = | 7.8 | Binding | Activation of human CaSRActivation of human CaSR |
ChEMBL | 619 | 12 | 2 | 7 | 5.6 | CS(=O)(=O)Nc1ccc(-c2csc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)n2)cc1 | 10.1016/j.bmcl.2013.10.050 | ||
| 72725335 | 104066 | 0 | None | - | 0 | Human | 7.8 | pEC50 | = | 7.8 | Binding | Activation of human CaSRActivation of human CaSR |
ChEMBL | 604 | 11 | 1 | 7 | 5.6 | CS(=O)(=O)c1sc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)nc1-c1ccccc1 | 10.1016/j.bmcl.2013.10.050 | ||
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