Ligand source activities (1 row/activity)
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | 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
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
| 46947061 | 17204 | None | 0 | Human | Functional | pEC50 | = | 8 | 8.0 | - | 1 | 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 | 17204 | None | 0 | Human | Functional | pEC50 | = | 8 | 8.0 | - | 1 | 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 | 156839 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | 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 | 156839 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | 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 | 17198 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | 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 | 17198 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | 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 | 17211 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | 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 | 17211 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | 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 | 89653 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | 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 | 89653 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | 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 | None | 4 | Rat | Functional | pEC50 | = | 6 | 6.0 | 1 | 3 | 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 | None | 4 | Rat | Functional | pEC50 | = | 6 | 6.0 | 1 | 3 | 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 | None | 4 | Rat | Functional | pEC50 | = | 6 | 6.0 | 1 | 3 | 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 | 148544 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | 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 | 148544 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | 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 | 151760 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | 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 | 151760 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | 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 | 89654 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | 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 | 89654 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | 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 | 89882 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | 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 | 89882 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | 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 | 137648 | None | 0 | Rat | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | 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 | 137648 | None | 0 | Rat | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | 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 | 137648 | None | 0 | Rat | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | 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 | 137648 | None | 0 | Rat | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | 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 | ||
| 66549010 | 197450 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | Agonist activity at human CaSR expresssed in HEK293 cells in presence of glucose by Fluo4NW dye based FLIPR assayAgonist activity at human CaSR expresssed in HEK293 cells in presence of glucose by Fluo4NW dye based FLIPR assay |
ChEMBL | 452 | 7 | 2 | 4 | 5.7 | C[C@@H](NCC1CN(c2cccc(CC(=O)O)c2)c2ccccc2O1)c1cccc2ccccc12 | 10.1021/acs.jmedchem.3c00698 | ||
| CHEMBL5406632 | 197450 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | Agonist activity at human CaSR expresssed in HEK293 cells in presence of glucose by Fluo4NW dye based FLIPR assayAgonist activity at human CaSR expresssed in HEK293 cells in presence of glucose by Fluo4NW dye based FLIPR assay |
ChEMBL | 452 | 7 | 2 | 4 | 5.7 | C[C@@H](NCC1CN(c2cccc(CC(=O)O)c2)c2ccccc2O1)c1cccc2ccccc12 | 10.1021/acs.jmedchem.3c00698 | ||
| CHEMBL5499353 | 197450 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | Agonist activity at human CaSR expresssed in HEK293 cells in presence of glucose by Fluo4NW dye based FLIPR assayAgonist activity at human CaSR expresssed in HEK293 cells in presence of glucose by Fluo4NW dye based FLIPR assay |
ChEMBL | 452 | 7 | 2 | 4 | 5.7 | C[C@@H](NCC1CN(c2cccc(CC(=O)O)c2)c2ccccc2O1)c1cccc2ccccc12 | 10.1021/acs.jmedchem.3c00698 | ||
| 49866114 | 16256 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | 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 | 16256 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | 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 | 167714 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | 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 | 167714 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | 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 | 167714 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | 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 | 149901 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | 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 | 149901 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | 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 | 152171 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | 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 | 152171 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | 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 | 137532 | None | 0 | Rat | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | 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 | 137532 | None | 0 | Rat | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | 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 | 137532 | None | 0 | Rat | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | 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 | 137532 | None | 0 | Rat | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | 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 | ||
| 66551524 | 195105 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | Agonist activity at human CaSR expresssed in HEK293 cells in presence of glucose by Fluo4NW dye based FLIPR assayAgonist activity at human CaSR expresssed in HEK293 cells in presence of glucose by Fluo4NW dye based FLIPR assay |
ChEMBL | 394 | 5 | 1 | 3 | 6.1 | C[C@@H](NCC1CN(c2ccccc2)c2ccccc2O1)c1cccc2ccccc12 | 10.1021/acs.jmedchem.3c00698 | ||
| CHEMBL5396763 | 195105 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | Agonist activity at human CaSR expresssed in HEK293 cells in presence of glucose by Fluo4NW dye based FLIPR assayAgonist activity at human CaSR expresssed in HEK293 cells in presence of glucose by Fluo4NW dye based FLIPR assay |
ChEMBL | 394 | 5 | 1 | 3 | 6.1 | C[C@@H](NCC1CN(c2ccccc2)c2ccccc2O1)c1cccc2ccccc12 | 10.1021/acs.jmedchem.3c00698 | ||
| 44542482 | 200901 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | 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 | 200901 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | 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 | 155928 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | 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 | 155928 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | 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 | 156583 | None | 1 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | 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 | 156583 | None | 1 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | 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 | 167842 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | -15 | 2 | 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 | ||
Showing 1 to 50 of 1,355 entries
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | 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
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
| 72725441 | 104129 | None | 0 | Human | Binding | pEC50 | = | 8 | 8.0 | - | 0 | 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 | 104129 | None | 0 | Human | Binding | pEC50 | = | 8 | 8.0 | - | 0 | 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 | 88172 | None | 0 | Human | Binding | pEC50 | = | 7 | 7.0 | - | 0 | 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 | 88172 | None | 0 | Human | Binding | pEC50 | = | 7 | 7.0 | - | 0 | 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 | 88484 | None | 0 | Human | Binding | pEC50 | = | 7 | 7.0 | - | 0 | 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 | 88484 | None | 0 | Human | Binding | pEC50 | = | 7 | 7.0 | - | 0 | 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 | 88481 | None | 0 | Human | Binding | pEC50 | = | 6 | 6.0 | - | 0 | 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 | 88481 | None | 0 | Human | Binding | pEC50 | = | 6 | 6.0 | - | 0 | 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 | 88489 | None | 0 | Human | Binding | pEC50 | = | 6 | 6.0 | - | 0 | 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 | 88489 | None | 0 | Human | Binding | pEC50 | = | 6 | 6.0 | - | 0 | 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 | 88500 | None | 0 | Human | Binding | pEC50 | = | 6 | 6.0 | - | 0 | 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 | 88500 | None | 0 | Human | Binding | pEC50 | = | 6 | 6.0 | - | 0 | 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 | 95054 | None | 22 | Human | Binding | pEC50 | = | 6 | 6.0 | - | 1 | 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 | 95054 | None | 22 | Human | Binding | pEC50 | = | 6 | 6.0 | - | 1 | 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 | 95054 | None | 22 | Human | Binding | pEC50 | = | 6 | 6.0 | - | 1 | 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 | 88167 | None | 0 | Human | Binding | pEC50 | = | 5 | 5.0 | - | 0 | 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 | 88167 | None | 0 | Human | Binding | pEC50 | = | 5 | 5.0 | - | 0 | 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 | 88171 | None | 0 | Human | Binding | pEC50 | = | 5 | 5.0 | - | 0 | 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 | 88171 | None | 0 | Human | Binding | pEC50 | = | 5 | 5.0 | - | 0 | 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 | 104115 | None | 0 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | 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 | 104115 | None | 0 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | 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 | 88497 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | 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 | 88497 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | 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 | 88173 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | 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 | 88173 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | 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 | 88480 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | 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 | 88480 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | 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 | 88487 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | 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 | 88487 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | 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 | 88491 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | 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 | 88491 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | 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 | 88493 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | 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 | 88493 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | 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 | 88510 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | 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 | 88510 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | 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 | 88512 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | 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 | 88512 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | 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 | 88168 | None | 0 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | 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 | 88168 | None | 0 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | 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 | 88151 | None | 0 | Human | Binding | pEC50 | = | 4.8 | 4.8 | - | 0 | 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 | 88151 | None | 0 | Human | Binding | pEC50 | = | 4.8 | 4.8 | - | 0 | 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 | 88160 | None | 0 | Human | Binding | pEC50 | = | 4.8 | 4.8 | - | 0 | 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 | 88160 | None | 0 | Human | Binding | pEC50 | = | 4.8 | 4.8 | - | 0 | 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 | 88164 | None | 0 | Human | Binding | pEC50 | = | 4.8 | 4.8 | - | 0 | 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 | 88164 | None | 0 | Human | Binding | pEC50 | = | 4.8 | 4.8 | - | 0 | 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 | 103875 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | 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 | 103875 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | 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 | 104113 | None | 0 | Human | Binding | pEC50 | = | 7.8 | 7.8 | - | 0 | 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 | 104113 | None | 0 | Human | Binding | pEC50 | = | 7.8 | 7.8 | - | 0 | 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 | 104121 | None | 0 | Human | Binding | pEC50 | = | 7.8 | 7.8 | - | 0 | 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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