Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
46947061 23969 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 23969 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 163526 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 163526 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 23963 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 23963 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 23976 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 23976 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 96394 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 96394 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 7571 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 7571 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 7571 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 155235 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 155235 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 158450 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 158450 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 96395 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 96395 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 96623 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 96623 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 144339 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 144339 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 144339 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 144339 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 23021 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 23021 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 174393 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 174393 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 174393 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 156592 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 156592 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 158861 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 158861 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 144223 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 144223 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 144223 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 144223 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 205224 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 205224 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 162617 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 162617 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 163271 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 163271 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 174519 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 174519 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 174519 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 161005 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 161005 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 22972 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
CHEMBL1224190 22972 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
137629864 167969 0 None - 1 Human 6.9 pEC50 = 6.9 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 445 8 2 3 4.2 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCC[N+](C)(C)C)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
CHEMBL4062970 167969 0 None - 1 Human 6.9 pEC50 = 6.9 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 445 8 2 3 4.2 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCC[N+](C)(C)C)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
CHEMBL4117685 167969 0 None - 1 Human 6.9 pEC50 = 6.9 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 445 8 2 3 4.2 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCC[N+](C)(C)C)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
9835971 20157 2 None - 1 Rat 5.9 pEC50 = 5.9 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 CC(NCc1cc2ccccc2[nH]1)c1cccc2ccccc12 10.1016/j.bmcl.2004.03.056
CHEMBL1192611 20157 2 None - 1 Rat 5.9 pEC50 = 5.9 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 CC(NCc1cc2ccccc2[nH]1)c1cccc2ccccc12 10.1016/j.bmcl.2004.03.056
CHEMBL543875 20157 2 None - 1 Rat 5.9 pEC50 = 5.9 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 CC(NCc1cc2ccccc2[nH]1)c1cccc2ccccc12 10.1016/j.bmcl.2004.03.056
10408861 23006 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calciumPositive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calcium
ChEMBL 403 6 1 2 6.4 COc1ccc(CN[C@H](C)c2cccc(F)c2)cc1-c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2010.07.060
CHEMBL1224342 23006 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calciumPositive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calcium
ChEMBL 403 6 1 2 6.4 COc1ccc(CN[C@H](C)c2cccc(F)c2)cc1-c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2010.07.060
53379291 155618 0 None - 1 Human 4.9 pEC50 = 4.9 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 303 6 4 6 -0.5 N[C@@H](CCC(=O)Nc1cccc(S(=O)(=O)O)n1)C(=O)O nan
CHEMBL3941122 155618 0 None - 1 Human 4.9 pEC50 = 4.9 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 303 6 4 6 -0.5 N[C@@H](CCC(=O)Nc1cccc(S(=O)(=O)O)n1)C(=O)O nan
57385341 144193 0 None - 1 Rat 6.9 pEC50 = 6.9 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 318 4 2 1 5.3 CC(NCc1cc2ccccc2[nH]1)c1ccc(F)c2ccccc12 10.1016/j.bmc.2015.12.019
CHEMBL3753320 144193 0 None - 1 Rat 6.9 pEC50 = 6.9 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 318 4 2 1 5.3 CC(NCc1cc2ccccc2[nH]1)c1ccc(F)c2ccccc12 10.1016/j.bmc.2015.12.019
719 7571 5 None 1 3 Rat 6.9 pEC50 = 6.9 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 300 4 2 1 5.2 C[C@H](c1cccc2c1cccc2)NCc1cc2c([nH]1)cccc2 10.1016/j.bmc.2015.12.019
9882793 7571 5 None 1 3 Rat 6.9 pEC50 = 6.9 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 300 4 2 1 5.2 C[C@H](c1cccc2c1cccc2)NCc1cc2c([nH]1)cccc2 10.1016/j.bmc.2015.12.019
CHEMBL1801356 7571 5 None 1 3 Rat 6.9 pEC50 = 6.9 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 300 4 2 1 5.2 C[C@H](c1cccc2c1cccc2)NCc1cc2c([nH]1)cccc2 10.1016/j.bmc.2015.12.019
57385341 144193 0 None - 1 Rat 6.9 pEC50 = 6.9 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 318 4 2 1 5.3 CC(NCc1cc2ccccc2[nH]1)c1ccc(F)c2ccccc12 10.1016/j.bmc.2015.12.019
CHEMBL3753320 144193 0 None - 1 Rat 6.9 pEC50 = 6.9 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 318 4 2 1 5.3 CC(NCc1cc2ccccc2[nH]1)c1ccc(F)c2ccccc12 10.1016/j.bmc.2015.12.019
719 7571 5 None 1 3 Rat 6.9 pEC50 = 6.9 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 300 4 2 1 5.2 C[C@H](c1cccc2c1cccc2)NCc1cc2c([nH]1)cccc2 10.1016/j.bmc.2015.12.019
9882793 7571 5 None 1 3 Rat 6.9 pEC50 = 6.9 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 300 4 2 1 5.2 C[C@H](c1cccc2c1cccc2)NCc1cc2c([nH]1)cccc2 10.1016/j.bmc.2015.12.019
CHEMBL1801356 7571 5 None 1 3 Rat 6.9 pEC50 = 6.9 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 300 4 2 1 5.2 C[C@H](c1cccc2c1cccc2)NCc1cc2c([nH]1)cccc2 10.1016/j.bmc.2015.12.019
127026335 144242 0 None - 1 Rat 6.9 pEC50 = 6.9 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 376 5 2 1 6.8 C[C@@H](NCc1cc2c(-c3ccccc3)cccc2[nH]1)c1cccc2ccccc12 10.1016/j.bmc.2015.12.019
CHEMBL3753729 144242 0 None - 1 Rat 6.9 pEC50 = 6.9 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 376 5 2 1 6.8 C[C@@H](NCc1cc2c(-c3ccccc3)cccc2[nH]1)c1cccc2ccccc12 10.1016/j.bmc.2015.12.019
127026335 144242 0 None - 1 Rat 6.9 pEC50 = 6.9 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 376 5 2 1 6.8 C[C@@H](NCc1cc2c(-c3ccccc3)cccc2[nH]1)c1cccc2ccccc12 10.1016/j.bmc.2015.12.019
CHEMBL3753729 144242 0 None - 1 Rat 6.9 pEC50 = 6.9 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 376 5 2 1 6.8 C[C@@H](NCc1cc2c(-c3ccccc3)cccc2[nH]1)c1cccc2ccccc12 10.1016/j.bmc.2015.12.019
49866002 22993 0 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 347 7 1 3 5.2 COc1cccc([C@@H](C)NCc2cccc(-c3ccccc3OC)c2)c1 10.1016/j.bmcl.2010.07.060
CHEMBL1224262 22993 0 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 347 7 1 3 5.2 COc1cccc([C@@H](C)NCc2cccc(-c3ccccc3OC)c2)c1 10.1016/j.bmcl.2010.07.060
44542629 204616 0 None - 1 Human 6.8 pEC50 = 6.8 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 377 5 1 3 5.4 C[C@@H](N[C@H](C)c1ccn(-c2ccc(C(F)(F)F)cc2)n1)c1cccc(F)c1 10.1021/jm9012278
CHEMBL572363 204616 0 None - 1 Human 6.8 pEC50 = 6.8 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 377 5 1 3 5.4 C[C@@H](N[C@H](C)c1ccn(-c2ccc(C(F)(F)F)cc2)n1)c1cccc(F)c1 10.1021/jm9012278
137661671 166116 0 None - 1 Human 7.8 pEC50 = 7.8 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 534 14 6 7 2.6 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCCCCNC(CO)(CO)CO)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
CHEMBL4100132 166116 0 None - 1 Human 7.8 pEC50 = 7.8 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 534 14 6 7 2.6 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCCCCNC(CO)(CO)CO)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
58938055 96634 0 None - 1 Human 6.8 pEC50 = 6.8 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 497 9 1 5 5.0 Cn1c(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)nc2ccccc21 10.1016/j.bmcl.2013.01.077
CHEMBL2377737 96634 0 None - 1 Human 6.8 pEC50 = 6.8 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 497 9 1 5 5.0 Cn1c(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)nc2ccccc21 10.1016/j.bmcl.2013.01.077
53374571 157826 0 None - 1 Human 4.8 pEC50 = 4.8 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 281 5 5 4 0.2 Cc1ccc(NC(=O)NC[C@H](N)C(=O)O)cc1C(=O)O nan
CHEMBL3958734 157826 0 None - 1 Human 4.8 pEC50 = 4.8 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 281 5 5 4 0.2 Cc1ccc(NC(=O)NC[C@H](N)C(=O)O)cc1C(=O)O nan
58973485 164306 0 None -26 2 Human 6.8 pEC50 = 6.8 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 360 5 2 3 4.5 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)O)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
CHEMBL4079960 164306 0 None -26 2 Human 6.8 pEC50 = 6.8 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 360 5 2 3 4.5 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)O)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
CHEMBL4126482 164306 0 None -26 2 Human 6.8 pEC50 = 6.8 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 360 5 2 3 4.5 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)O)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
52947599 23968 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
ChEMBL 287 2 1 3 4.0 Cc1cc(C(C)(O)c2nc3ccccc3s2)ccc1F 10.1016/j.bmcl.2010.07.077
CHEMBL1256366 23968 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
ChEMBL 287 2 1 3 4.0 Cc1cc(C(C)(O)c2nc3ccccc3s2)ccc1F 10.1016/j.bmcl.2010.07.077
44542931 204446 2 None - 1 Human 5.8 pEC50 = 5.8 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 277 5 1 3 3.7 C[C@@H](NCc1ccn(-c2ccccc2)n1)c1ccccc1 10.1021/jm9012278
CHEMBL571048 204446 2 None - 1 Human 5.8 pEC50 = 5.8 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 277 5 1 3 3.7 C[C@@H](NCc1ccn(-c2ccccc2)n1)c1ccccc1 10.1021/jm9012278
137638744 163478 0 None - 1 Human 5.8 pEC50 = 5.8 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 481 8 3 6 3.0 C[C@@H](N[C@H]1CCN(c2ccc(S(=O)(=O)NC(=O)CC(=O)O)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
CHEMBL4069946 163478 0 None - 1 Human 5.8 pEC50 = 5.8 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 481 8 3 6 3.0 C[C@@H](N[C@H]1CCN(c2ccc(S(=O)(=O)NC(=O)CC(=O)O)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
10453544 23007 0 None - 1 Human 6.8 pEC50 = 6.8 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 399 6 1 2 6.5 COc1ccc(CNC(C)c2cccc(C)c2)cc1-c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2010.07.060
CHEMBL1224343 23007 0 None - 1 Human 6.8 pEC50 = 6.8 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 399 6 1 2 6.5 COc1ccc(CNC(C)c2cccc(C)c2)cc1-c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2010.07.060
68245625 153648 0 None - 1 Human 5.8 pEC50 = 5.8 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 267 5 5 4 -0.1 N[C@@H](CNC(=O)Nc1cccc(C(=O)O)c1)C(=O)O nan
CHEMBL3925295 153648 0 None - 1 Human 5.8 pEC50 = 5.8 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 267 5 5 4 -0.1 N[C@@H](CNC(=O)Nc1cccc(C(=O)O)c1)C(=O)O nan
145948146 174520 0 None -36 2 Human 7.8 pEC50 = 7.8 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 384 5 2 5 3.9 C[C@@H](N[C@H]1CCN(c2ccc(-c3nn[nH]n3)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4126450 174520 0 None -36 2 Human 7.8 pEC50 = 7.8 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 384 5 2 5 3.9 C[C@@H](N[C@H]1CCN(c2ccc(-c3nn[nH]n3)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4302858 174520 0 None -36 2 Human 7.8 pEC50 = 7.8 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 384 5 2 5 3.9 C[C@@H](N[C@H]1CCN(c2ccc(-c3nn[nH]n3)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
46934584 23019 0 None - 1 Human 7.8 pEC50 = 7.8 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 399 6 1 2 6.8 COc1ccc([C@@H](C)N[C@H](C)c2ccccc2)cc1-c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2010.07.060
CHEMBL1224424 23019 0 None - 1 Human 7.8 pEC50 = 7.8 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 399 6 1 2 6.8 COc1ccc([C@@H](C)N[C@H](C)c2ccccc2)cc1-c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2010.07.060
49865952 22974 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calciumPositive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calcium
ChEMBL 351 6 1 2 5.9 COc1cccc([C@@H](C)NCc2cccc(-c3ccccc3Cl)c2)c1 10.1016/j.bmcl.2010.07.060
CHEMBL1224192 22974 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calciumPositive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calcium
ChEMBL 351 6 1 2 5.9 COc1cccc([C@@H](C)NCc2cccc(-c3ccccc3Cl)c2)c1 10.1016/j.bmcl.2010.07.060
49866112 23018 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calciumPositive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calcium
ChEMBL 403 6 1 2 6.4 COc1ccc(CN[C@H](C)c2ccc(F)cc2)cc1-c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2010.07.060
CHEMBL1224423 23018 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calciumPositive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calcium
ChEMBL 403 6 1 2 6.4 COc1ccc(CN[C@H](C)c2ccc(F)cc2)cc1-c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2010.07.060
58938052 96630 0 None - 1 Human 5.8 pEC50 = 5.8 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 462 9 1 5 4.7 Cc1noc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1C 10.1016/j.bmcl.2013.01.077
CHEMBL2377733 96630 0 None - 1 Human 5.8 pEC50 = 5.8 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 462 9 1 5 4.7 Cc1noc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1C 10.1016/j.bmcl.2013.01.077
88905973 149204 0 None - 1 Human 7.8 pEC50 = 7.8 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 303 5 5 5 -0.5 N[C@@H](CNC(=O)Nc1cccc(S(=O)(=O)O)c1)C(=O)O nan
CHEMBL3889990 149204 0 None - 1 Human 7.8 pEC50 = 7.8 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 303 5 5 5 -0.5 N[C@@H](CNC(=O)Nc1cccc(S(=O)(=O)O)c1)C(=O)O nan
156419 7725 74 None 11 15 Human 6.8 pEC50 = 6.8 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 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2018.04.055
3308 7725 74 None 11 15 Human 6.8 pEC50 = 6.8 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 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2018.04.055
647 7725 74 None 11 15 Human 6.8 pEC50 = 6.8 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 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2018.04.055
CHEMBL1201284 7725 74 None 11 15 Human 6.8 pEC50 = 6.8 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 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2018.04.055
DB01012 7725 74 None 11 15 Human 6.8 pEC50 = 6.8 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 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2018.04.055
89449922 155914 0 None - 1 Human 6.8 pEC50 = 6.8 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 390 6 4 8 1.4 Cc1nnc([C@@H](N)CCC(=O)Nc2cc(Cl)cc(S(=O)(=O)O)c2O)o1 nan
CHEMBL3943365 155914 0 None - 1 Human 6.8 pEC50 = 6.8 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 390 6 4 8 1.4 Cc1nnc([C@@H](N)CCC(=O)Nc2cc(Cl)cc(S(=O)(=O)O)c2O)o1 nan
68245626 156316 0 None - 1 Human 5.8 pEC50 = 5.8 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 312 6 5 6 -0.2 N[C@@H](CNC(=O)Nc1cc(C(=O)O)cc([N+](=O)[O-])c1)C(=O)O nan
CHEMBL3946636 156316 0 None - 1 Human 5.8 pEC50 = 5.8 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 312 6 5 6 -0.2 N[C@@H](CNC(=O)Nc1cc(C(=O)O)cc([N+](=O)[O-])c1)C(=O)O nan
71542722 157435 0 None - 1 Human 5.8 pEC50 = 5.8 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 380 7 4 6 1.0 CN(C)[C@@H](CCC(=O)Nc1cc(Cl)cc(S(=O)(=O)O)c1O)C(=O)O nan
CHEMBL3955623 157435 0 None - 1 Human 5.8 pEC50 = 5.8 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 380 7 4 6 1.0 CN(C)[C@@H](CCC(=O)Nc1cc(Cl)cc(S(=O)(=O)O)c1O)C(=O)O nan
137638587 163748 0 None - 1 Human 7.7 pEC50 = 7.7 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 395 5 2 4 3.4 C[C@@H](N[C@H]1CCN(c2ccc(S(N)(=O)=O)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
CHEMBL4072950 163748 0 None - 1 Human 7.7 pEC50 = 7.7 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 395 5 2 4 3.4 C[C@@H](N[C@H]1CCN(c2ccc(S(N)(=O)=O)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
156419 7725 74 None 11 15 Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2010.07.077
3308 7725 74 None 11 15 Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2010.07.077
647 7725 74 None 11 15 Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2010.07.077
CHEMBL1201284 7725 74 None 11 15 Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2010.07.077
DB01012 7725 74 None 11 15 Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2010.07.077
67406779 174499 0 None -134 2 Human 6.7 pEC50 = 6.7 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 414 5 1 3 6.1 C[C@@H](N[C@@H]1CCCN(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4128542 174499 0 None -134 2 Human 6.7 pEC50 = 6.7 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 414 5 1 3 6.1 C[C@@H](N[C@@H]1CCCN(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4302632 174499 0 None -134 2 Human 6.7 pEC50 = 6.7 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 414 5 1 3 6.1 C[C@@H](N[C@@H]1CCCN(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
44543376 205589 0 None - 1 Human 5.7 pEC50 = 5.7 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 399 7 2 5 4.6 COc1cc([C@@H](C)N[C@H](C)c2cccc(Cl)c2)nn1-c1ccc(C(=O)O)cc1 10.1021/jm9012278
CHEMBL583469 205589 0 None - 1 Human 5.7 pEC50 = 5.7 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 399 7 2 5 4.6 COc1cc([C@@H](C)N[C@H](C)c2cccc(Cl)c2)nn1-c1ccc(C(=O)O)cc1 10.1021/jm9012278
158797 10543 24 None - 1 Human 6.7 pEC50 = 6.7 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 303 7 1 2 4.6 COc1cccc(c1)[C@H](NCCCc1ccccc1Cl)C 10.1021/jm9012278
718 10543 24 None - 1 Human 6.7 pEC50 = 6.7 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 303 7 1 2 4.6 COc1cccc(c1)[C@H](NCCCc1ccccc1Cl)C 10.1021/jm9012278
CHEMBL292376 10543 24 None - 1 Human 6.7 pEC50 = 6.7 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 303 7 1 2 4.6 COc1cccc(c1)[C@H](NCCCc1ccccc1Cl)C 10.1021/jm9012278
52948734 24426 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
ChEMBL 309 3 1 3 4.6 Cc1ccc(C(O)(c2nc3ccccc3s2)C2CC2)c(C)c1 10.1016/j.bmcl.2010.07.077
CHEMBL1258389 24426 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
ChEMBL 309 3 1 3 4.6 Cc1ccc(C(O)(c2nc3ccccc3s2)C2CC2)c(C)c1 10.1016/j.bmcl.2010.07.077
127036924 144190 0 None - 1 Rat 7.7 pEC50 = 7.7 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 345 5 2 3 5.1 C[C@@H](NCc1cc2cccc([N+](=O)[O-])c2[nH]1)c1cccc2ccccc12 10.1016/j.bmc.2015.12.019
CHEMBL3753306 144190 0 None - 1 Rat 7.7 pEC50 = 7.7 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 345 5 2 3 5.1 C[C@@H](NCc1cc2cccc([N+](=O)[O-])c2[nH]1)c1cccc2ccccc12 10.1016/j.bmc.2015.12.019
11955191 96632 0 None - 1 Human 7.7 pEC50 = 7.7 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 500 9 1 5 5.7 O=C(Nc1nc2ccccc2s1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.077
CHEMBL2377735 96632 0 None - 1 Human 7.7 pEC50 = 7.7 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 500 9 1 5 5.7 O=C(Nc1nc2ccccc2s1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.077
11955189 96637 0 None - 1 Human 7.7 pEC50 = 7.7 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 534 9 1 5 6.3 O=C(Nc1nc2c(Cl)cccc2s1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.077
CHEMBL2377740 96637 0 None - 1 Human 7.7 pEC50 = 7.7 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 534 9 1 5 6.3 O=C(Nc1nc2c(Cl)cccc2s1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.077
127036924 144190 0 None - 1 Rat 7.7 pEC50 = 7.7 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 345 5 2 3 5.1 C[C@@H](NCc1cc2cccc([N+](=O)[O-])c2[nH]1)c1cccc2ccccc12 10.1016/j.bmc.2015.12.019
CHEMBL3753306 144190 0 None - 1 Rat 7.7 pEC50 = 7.7 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 345 5 2 3 5.1 C[C@@H](NCc1cc2cccc([N+](=O)[O-])c2[nH]1)c1cccc2ccccc12 10.1016/j.bmc.2015.12.019
73350366 96396 0 None - 1 Human 6.7 pEC50 = 6.7 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 518 9 1 5 5.8 O=C(Nc1nc2ccc(F)cc2s1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.077
CHEMBL2375386 96396 0 None - 1 Human 6.7 pEC50 = 6.7 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 518 9 1 5 5.8 O=C(Nc1nc2ccc(F)cc2s1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.077
58938081 96627 0 None - 1 Human 6.7 pEC50 = 6.7 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 528 10 1 7 5.0 O=C(Nc1nccc(-c2nccs2)n1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.077
CHEMBL2377730 96627 0 None - 1 Human 6.7 pEC50 = 6.7 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 528 10 1 7 5.0 O=C(Nc1nccc(-c2nccs2)n1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.077
58938076 96629 0 None - 1 Human 6.7 pEC50 = 6.7 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 448 9 1 5 4.4 Cc1cc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)no1 10.1016/j.bmcl.2013.01.077
CHEMBL2377732 96629 0 None - 1 Human 6.7 pEC50 = 6.7 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 448 9 1 5 4.4 Cc1cc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)no1 10.1016/j.bmcl.2013.01.077
73345828 96647 0 None - 1 Human 6.7 pEC50 = 6.7 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 572 11 1 7 5.9 CCOC(=O)c1ccc2nc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)sc2c1 10.1016/j.bmcl.2013.01.077
CHEMBL2377750 96647 0 None - 1 Human 6.7 pEC50 = 6.7 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 572 11 1 7 5.9 CCOC(=O)c1ccc2nc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)sc2c1 10.1016/j.bmcl.2013.01.077
73353387 96648 0 None - 1 Human 6.7 pEC50 = 6.7 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 614 13 2 7 5.0 CN(C)CCNC(=O)c1ccc2nc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)sc2c1 10.1016/j.bmcl.2013.01.077
CHEMBL2377751 96648 0 None - 1 Human 6.7 pEC50 = 6.7 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 614 13 2 7 5.0 CN(C)CCNC(=O)c1ccc2nc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)sc2c1 10.1016/j.bmcl.2013.01.077
46934584 23019 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calciumPositive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calcium
ChEMBL 399 6 1 2 6.8 COc1ccc([C@@H](C)N[C@H](C)c2ccccc2)cc1-c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2010.07.060
CHEMBL1224424 23019 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calciumPositive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calcium
ChEMBL 399 6 1 2 6.8 COc1ccc([C@@H](C)N[C@H](C)c2ccccc2)cc1-c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2010.07.060
71542725 153420 0 None - 1 Human 4.7 pEC50 = 4.7 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 376 6 7 7 -0.9 CC(=O)Nc1cc(S(=O)(=O)O)cc(NC(=O)NC[C@H](N)C(=O)O)c1O nan
CHEMBL3923504 153420 0 None - 1 Human 4.7 pEC50 = 4.7 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 376 6 7 7 -0.9 CC(=O)Nc1cc(S(=O)(=O)O)cc(NC(=O)NC[C@H](N)C(=O)O)c1O nan
49866001 22992 0 None - 1 Human 5.7 pEC50 = 5.7 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 331 6 1 2 5.5 COc1cccc([C@@H](C)NCc2cccc(-c3ccccc3C)c2)c1 10.1016/j.bmcl.2010.07.060
CHEMBL1224261 22992 0 None - 1 Human 5.7 pEC50 = 5.7 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 331 6 1 2 5.5 COc1cccc([C@@H](C)NCc2cccc(-c3ccccc3C)c2)c1 10.1016/j.bmcl.2010.07.060
44462802 204145 8 None - 1 Human 7.6 pEC50 = 7.6 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 433 6 1 4 5.7 COc1cc([C@@H](C)N[C@H](C)c2cccc(Cl)c2)nn1-c1ccc(Br)cc1 10.1021/jm9012278
CHEMBL569182 204145 8 None - 1 Human 7.6 pEC50 = 7.6 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 433 6 1 4 5.7 COc1cc([C@@H](C)N[C@H](C)c2cccc(Cl)c2)nn1-c1ccc(Br)cc1 10.1021/jm9012278
10341785 23004 0 None - 1 Human 7.6 pEC50 = 7.6 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 415 7 1 3 6.2 COc1cccc([C@@H](C)NCc2ccc(OC)c(-c3ccc(C(F)(F)F)cc3)c2)c1 10.1016/j.bmcl.2010.07.060
CHEMBL1224340 23004 0 None - 1 Human 7.6 pEC50 = 7.6 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 415 7 1 3 6.2 COc1cccc([C@@H](C)NCc2ccc(OC)c(-c3ccc(C(F)(F)F)cc3)c2)c1 10.1016/j.bmcl.2010.07.060
145947416 174427 0 None -1 2 Human 6.6 pEC50 = 6.6 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
CHEMBL4129371 174427 0 None -1 2 Human 6.6 pEC50 = 6.6 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
CHEMBL4301708 174427 0 None -1 2 Human 6.6 pEC50 = 6.6 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
68244249 154076 0 None - 1 Human 5.6 pEC50 = 5.6 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 301 5 5 4 0.6 N[C@@H](CNC(=O)Nc1cc(C(=O)O)ccc1Cl)C(=O)O nan
CHEMBL3928924 154076 0 None - 1 Human 5.6 pEC50 = 5.6 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 301 5 5 4 0.6 N[C@@H](CNC(=O)Nc1cc(C(=O)O)ccc1Cl)C(=O)O nan
53374667 158310 0 None - 1 Human 5.6 pEC50 = 5.6 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 491 8 5 8 0.8 N[C@@H](CCC(=O)Nc1cc(Cl)cc(S(=O)(=O)O)c1O)C(=O)NS(=O)(=O)c1ccccc1 nan
CHEMBL3962913 158310 0 None - 1 Human 5.6 pEC50 = 5.6 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 491 8 5 8 0.8 N[C@@H](CCC(=O)Nc1cc(Cl)cc(S(=O)(=O)O)c1O)C(=O)NS(=O)(=O)c1ccccc1 nan
44543086 205596 0 None - 1 Human 6.6 pEC50 = 6.6 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 359 5 1 3 5.3 C[C@@H](N[C@H](C)c1ccn(-c2ccc(C(F)(F)F)cc2)n1)c1ccccc1 10.1021/jm9012278
CHEMBL583522 205596 0 None - 1 Human 6.6 pEC50 = 6.6 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 359 5 1 3 5.3 C[C@@H](N[C@H](C)c1ccn(-c2ccc(C(F)(F)F)cc2)n1)c1ccccc1 10.1021/jm9012278
44543087 204615 0 None - 1 Human 5.6 pEC50 = 5.6 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 387 6 1 3 5.9 CC(C)[C@@H](N[C@H](C)c1ccccc1)c1ccn(-c2ccc(C(F)(F)F)cc2)n1 10.1021/jm9012278
CHEMBL572362 204615 0 None - 1 Human 5.6 pEC50 = 5.6 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 387 6 1 3 5.9 CC(C)[C@@H](N[C@H](C)c1ccccc1)c1ccn(-c2ccc(C(F)(F)F)cc2)n1 10.1021/jm9012278
3947 7029 27 None - 1 Human 7.6 pEC50 = 7.6 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(c1)C)C(c1nc2c(s1)cccc2)(O)C 10.1016/j.bmcl.2010.07.077
52943938 7029 27 None - 1 Human 7.6 pEC50 = 7.6 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(c1)C)C(c1nc2c(s1)cccc2)(O)C 10.1016/j.bmcl.2010.07.077
CHEMBL1256367 7029 27 None - 1 Human 7.6 pEC50 = 7.6 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(c1)C)C(c1nc2c(s1)cccc2)(O)C 10.1016/j.bmcl.2010.07.077
89449921 159373 0 None - 1 Human 6.6 pEC50 = 6.6 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 484 8 6 7 0.7 N[C@@H](CCC(=O)Nc1cc(Cl)cc(S(=O)(=O)O)c1O)C(=O)NNC(=O)Cc1ccccc1 nan
CHEMBL3971904 159373 0 None - 1 Human 6.6 pEC50 = 6.6 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 484 8 6 7 0.7 N[C@@H](CCC(=O)Nc1cc(Cl)cc(S(=O)(=O)O)c1O)C(=O)NNC(=O)Cc1ccccc1 nan
137628638 163633 8 None -5 3 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse CaSR expressed in HEK293 cells assessed as increase in intracellular calcium mobilization by fluo-4AM dye based FLIPR assayAgonist activity at mouse CaSR expressed in HEK293 cells assessed as increase in intracellular calcium mobilization by fluo-4AM dye based FLIPR assay
ChEMBL 528 10 3 5 4.7 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCCCN3CCC(C(=O)O)CC3)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
CHEMBL4071600 163633 8 None -5 3 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse CaSR expressed in HEK293 cells assessed as increase in intracellular calcium mobilization by fluo-4AM dye based FLIPR assayAgonist activity at mouse CaSR expressed in HEK293 cells assessed as increase in intracellular calcium mobilization by fluo-4AM dye based FLIPR assay
ChEMBL 528 10 3 5 4.7 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCCCN3CCC(C(=O)O)CC3)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
52942726 23965 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
ChEMBL 269 2 1 3 3.9 Cc1ccccc1C(C)(O)c1nc2ccccc2s1 10.1016/j.bmcl.2010.07.077
CHEMBL1256331 23965 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
ChEMBL 269 2 1 3 3.9 Cc1ccccc1C(C)(O)c1nc2ccccc2s1 10.1016/j.bmcl.2010.07.077
52942774 23983 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
ChEMBL 267 2 0 2 5.1 Cc1ccc(C(C)c2nc3ccccc3s2)c(C)c1 10.1016/j.bmcl.2010.07.077
CHEMBL1256486 23983 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
ChEMBL 267 2 0 2 5.1 Cc1ccc(C(C)c2nc3ccccc3s2)c(C)c1 10.1016/j.bmcl.2010.07.077
11545487 23005 0 None - 1 Human 7.6 pEC50 = 7.6 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 385 6 1 2 6.2 COc1ccc(CN[C@H](C)c2ccccc2)cc1-c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2010.07.060
CHEMBL1224341 23005 0 None - 1 Human 7.6 pEC50 = 7.6 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 385 6 1 2 6.2 COc1ccc(CN[C@H](C)c2ccccc2)cc1-c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2010.07.060
49866000 22991 0 None - 1 Human 5.6 pEC50 = 5.6 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 335 6 1 2 5.4 COc1cccc([C@@H](C)NCc2cccc(-c3ccccc3F)c2)c1 10.1016/j.bmcl.2010.07.060
CHEMBL1224260 22991 0 None - 1 Human 5.6 pEC50 = 5.6 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 335 6 1 2 5.4 COc1cccc([C@@H](C)NCc2cccc(-c3ccccc3F)c2)c1 10.1016/j.bmcl.2010.07.060
49866054 23008 0 None - 1 Human 6.6 pEC50 = 6.6 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 419 6 1 2 6.9 COc1cccc([C@@H](C)NCc2ccc(Cl)c(-c3ccc(C(F)(F)F)cc3)c2)c1 10.1016/j.bmcl.2010.07.060
CHEMBL1224344 23008 0 None - 1 Human 6.6 pEC50 = 6.6 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 419 6 1 2 6.9 COc1cccc([C@@H](C)NCc2ccc(Cl)c(-c3ccc(C(F)(F)F)cc3)c2)c1 10.1016/j.bmcl.2010.07.060
58973485 164306 0 None -26 2 Human 6.5 pEC50 = 6.5 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 360 5 2 3 4.5 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)O)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4079960 164306 0 None -26 2 Human 6.5 pEC50 = 6.5 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 360 5 2 3 4.5 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)O)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4126482 164306 0 None -26 2 Human 6.5 pEC50 = 6.5 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 360 5 2 3 4.5 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)O)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
89346541 155193 0 None - 1 Human 8.5 pEC50 = 8.5 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 367 5 5 7 -0.1 COC(=O)[C@@H](N)CNC(=O)Nc1cc(Cl)cc(S(=O)(=O)O)c1O nan
CHEMBL3937671 155193 0 None - 1 Human 8.5 pEC50 = 8.5 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 367 5 5 7 -0.1 COC(=O)[C@@H](N)CNC(=O)Nc1cc(Cl)cc(S(=O)(=O)O)c1O nan
76026235 159476 7 None - 1 Human 8.5 pEC50 = 8.5 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 351 5 5 5 0.4 Cc1c(Cl)cc(S(=O)(=O)O)cc1NC(=O)NCC(N)C(=O)O nan
CHEMBL3972910 159476 7 None - 1 Human 8.5 pEC50 = 8.5 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 351 5 5 5 0.4 Cc1c(Cl)cc(S(=O)(=O)O)cc1NC(=O)NCC(N)C(=O)O nan
53377991 160418 0 None - 1 Human 8.5 pEC50 = 8.5 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 353 5 6 6 -0.2 N[C@@H](CNC(=O)Nc1cc(Cl)cc(S(=O)(=O)O)c1O)C(=O)O nan
CHEMBL3980928 160418 0 None - 1 Human 8.5 pEC50 = 8.5 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 353 5 6 6 -0.2 N[C@@H](CNC(=O)Nc1cc(Cl)cc(S(=O)(=O)O)c1O)C(=O)O nan
11955188 96638 0 None - 1 Human 7.5 pEC50 = 7.5 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 530 10 1 6 5.7 COc1cccc2sc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)nc12 10.1016/j.bmcl.2013.01.077
CHEMBL2377741 96638 0 None - 1 Human 7.5 pEC50 = 7.5 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 530 10 1 6 5.7 COc1cccc2sc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)nc12 10.1016/j.bmcl.2013.01.077
73347323 96640 0 None - 1 Human 7.5 pEC50 = 7.5 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 593 11 2 7 5.1 CS(=O)(=O)Nc1ccc2sc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)nc2c1 10.1016/j.bmcl.2013.01.077
CHEMBL2377743 96640 0 None - 1 Human 7.5 pEC50 = 7.5 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 593 11 2 7 5.1 CS(=O)(=O)Nc1ccc2sc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)nc2c1 10.1016/j.bmcl.2013.01.077
73353385 96645 0 None - 1 Human 7.5 pEC50 = 7.5 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 593 11 2 7 5.1 CS(=O)(=O)Nc1ccc2nc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)sc2c1 10.1016/j.bmcl.2013.01.077
CHEMBL2377748 96645 0 None - 1 Human 7.5 pEC50 = 7.5 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 593 11 2 7 5.1 CS(=O)(=O)Nc1ccc2nc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)sc2c1 10.1016/j.bmcl.2013.01.077
73350407 96646 0 None - 1 Human 7.5 pEC50 = 7.5 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 514 9 1 5 6.0 Cc1ccc2nc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)sc2c1 10.1016/j.bmcl.2013.01.077
CHEMBL2377749 96646 0 None - 1 Human 7.5 pEC50 = 7.5 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 514 9 1 5 6.0 Cc1ccc2nc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)sc2c1 10.1016/j.bmcl.2013.01.077
59499339 96628 0 None - 1 Human 6.5 pEC50 = 6.5 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 450 9 1 5 4.5 O=C(Nc1nccs1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.077
CHEMBL2377731 96628 0 None - 1 Human 6.5 pEC50 = 6.5 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 450 9 1 5 4.5 O=C(Nc1nccs1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.077
16735431 96635 0 None - 1 Human 6.5 pEC50 = 6.5 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 573 11 1 5 6.5 O=C(Nc1nc2ccccc2n1Cc1ccccc1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.077
CHEMBL2377738 96635 0 None - 1 Human 6.5 pEC50 = 6.5 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 573 11 1 5 6.5 O=C(Nc1nc2ccccc2n1Cc1ccccc1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.077
49866113 23020 0 None - 1 Human 5.5 pEC50 = 5.5 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 399 6 1 2 6.8 COc1ccc([C@H](C)N[C@H](C)c2ccccc2)cc1-c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2010.07.060
CHEMBL1224425 23020 0 None - 1 Human 5.5 pEC50 = 5.5 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 399 6 1 2 6.8 COc1ccc([C@H](C)N[C@H](C)c2ccccc2)cc1-c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2010.07.060
137646931 164504 0 None - 1 Human 7.5 pEC50 = 7.5 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 523 10 6 8 1.2 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)N(C)[C@@H](O)[C@H](O)[C@H](O)[C@@H](O)CO)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
CHEMBL4082125 164504 0 None - 1 Human 7.5 pEC50 = 7.5 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 523 10 6 8 1.2 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)N(C)[C@@H](O)[C@H](O)[C@H](O)[C@@H](O)CO)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
52946369 23975 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
ChEMBL 303 2 1 3 4.5 Cc1cc(Cl)ccc1C(C)(O)c1nc2ccccc2s1 10.1016/j.bmcl.2010.07.077
CHEMBL1256403 23975 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
ChEMBL 303 2 1 3 4.5 Cc1cc(Cl)ccc1C(C)(O)c1nc2ccccc2s1 10.1016/j.bmcl.2010.07.077
719 7571 5 None -1 3 Human 6.5 pEC50 = 6.5 Functional
Ability to stimulate [3H]inositol phosphates accumulation in HEK293 cells expressing the human calcium sensing receptor (CaSR) at 2 mM [Ca2+]Ability to stimulate [3H]inositol phosphates accumulation in HEK293 cells expressing the human 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 7571 5 None -1 3 Human 6.5 pEC50 = 6.5 Functional
Ability to stimulate [3H]inositol phosphates accumulation in HEK293 cells expressing the human calcium sensing receptor (CaSR) at 2 mM [Ca2+]Ability to stimulate [3H]inositol phosphates accumulation in HEK293 cells expressing the human 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 7571 5 None -1 3 Human 6.5 pEC50 = 6.5 Functional
Ability to stimulate [3H]inositol phosphates accumulation in HEK293 cells expressing the human calcium sensing receptor (CaSR) at 2 mM [Ca2+]Ability to stimulate [3H]inositol phosphates accumulation in HEK293 cells expressing the human 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
76026313 156661 0 None - 1 Human 5.5 pEC50 = 5.5 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 421 6 4 7 0.2 NC(CCC(=O)Nc1cc(Cl)cc(S(=O)(=O)O)c1O)C(=O)N1CCOCC1 nan
CHEMBL3949209 156661 0 None - 1 Human 5.5 pEC50 = 5.5 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 421 6 4 7 0.2 NC(CCC(=O)Nc1cc(Cl)cc(S(=O)(=O)O)c1O)C(=O)N1CCOCC1 nan
86679037 159628 2 None - 1 Human 6.5 pEC50 = 6.5 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 365 6 5 5 0.7 CN[C@@H](CNC(=O)Nc1cc(Cl)c(C)c(S(=O)(=O)O)c1)C(=O)O nan
CHEMBL3974155 159628 2 None - 1 Human 6.5 pEC50 = 6.5 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 365 6 5 5 0.7 CN[C@@H](CNC(=O)Nc1cc(Cl)c(C)c(S(=O)(=O)O)c1)C(=O)O nan
137628638 163633 8 None -6 3 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat CaSR expressed in HEK293 cells assessed as increase in intracellular calcium mobilization by fluo-4AM dye based FLIPR assayAgonist activity at rat CaSR expressed in HEK293 cells assessed as increase in intracellular calcium mobilization by fluo-4AM dye based FLIPR assay
ChEMBL 528 10 3 5 4.7 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCCCN3CCC(C(=O)O)CC3)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
CHEMBL4071600 163633 8 None -6 3 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat CaSR expressed in HEK293 cells assessed as increase in intracellular calcium mobilization by fluo-4AM dye based FLIPR assayAgonist activity at rat CaSR expressed in HEK293 cells assessed as increase in intracellular calcium mobilization by fluo-4AM dye based FLIPR assay
ChEMBL 528 10 3 5 4.7 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCCCN3CCC(C(=O)O)CC3)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
52945768 23911 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
ChEMBL 309 1 1 3 4.5 Cc1cc(C)c2c(c1)C(O)(c1nc3ccccc3s1)CCC2 10.1016/j.bmcl.2010.07.077
CHEMBL1255602 23911 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
ChEMBL 309 1 1 3 4.5 Cc1cc(C)c2c(c1)C(O)(c1nc3ccccc3s1)CCC2 10.1016/j.bmcl.2010.07.077
137649972 164001 0 None - 1 Human 5.5 pEC50 = 5.5 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 396 5 3 3 3.6 C[C@@H](N[C@H]1CCN(c2ccc(P(=O)(O)O)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
CHEMBL4076239 164001 0 None - 1 Human 5.5 pEC50 = 5.5 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 396 5 3 3 3.6 C[C@@H](N[C@H]1CCN(c2ccc(P(=O)(O)O)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
145946257 174302 0 None -74 2 Human 6.5 pEC50 = 6.5 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(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4126057 174302 0 None -74 2 Human 6.5 pEC50 = 6.5 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(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4300082 174302 0 None -74 2 Human 6.5 pEC50 = 6.5 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(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
76026312 159738 0 None - 1 Human 5.5 pEC50 = 5.5 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 447 7 5 6 2.2 NC(CCC(=O)Nc1cc(Cl)cc(S(=O)(=O)O)c1O)C(=O)NC1CCCCCC1 nan
CHEMBL3975131 159738 0 None - 1 Human 5.5 pEC50 = 5.5 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 447 7 5 6 2.2 NC(CCC(=O)Nc1cc(Cl)cc(S(=O)(=O)O)c1O)C(=O)NC1CCCCCC1 nan
49865952 22974 0 None - 1 Human 6.5 pEC50 = 6.5 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 351 6 1 2 5.9 COc1cccc([C@@H](C)NCc2cccc(-c3ccccc3Cl)c2)c1 10.1016/j.bmcl.2010.07.060
CHEMBL1224192 22974 0 None - 1 Human 6.5 pEC50 = 6.5 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 351 6 1 2 5.9 COc1cccc([C@@H](C)NCc2cccc(-c3ccccc3Cl)c2)c1 10.1016/j.bmcl.2010.07.060
53374569 152899 0 None - 1 Human 5.4 pEC50 = 5.4 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 297 6 5 5 -0.1 COc1cc(NC(=O)NC[C@H](N)C(=O)O)cc(C(=O)O)c1 nan
CHEMBL3919534 152899 0 None - 1 Human 5.4 pEC50 = 5.4 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 297 6 5 5 -0.1 COc1cc(NC(=O)NC[C@H](N)C(=O)O)cc(C(=O)O)c1 nan
10408861 23006 0 None - 1 Human 7.4 pEC50 = 7.4 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 403 6 1 2 6.4 COc1ccc(CN[C@H](C)c2cccc(F)c2)cc1-c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2010.07.060
CHEMBL1224342 23006 0 None - 1 Human 7.4 pEC50 = 7.4 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 403 6 1 2 6.4 COc1ccc(CN[C@H](C)c2cccc(F)c2)cc1-c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2010.07.060
28447518 22975 2 None - 1 Human 6.4 pEC50 = 6.4 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 271 6 1 3 3.6 COc1ccc(CN[C@H](C)c2cccc(OC)c2)cc1 10.1016/j.bmcl.2010.07.060
CHEMBL1224193 22975 2 None - 1 Human 6.4 pEC50 = 6.4 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 271 6 1 3 3.6 COc1ccc(CN[C@H](C)c2cccc(OC)c2)cc1 10.1016/j.bmcl.2010.07.060
71542723 150842 0 None - 1 Human 5.4 pEC50 = 5.4 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(NC(=O)NC[C@H](N)C(=O)O)cc1S(=O)(=O)O nan
CHEMBL3903207 150842 0 None - 1 Human 5.4 pEC50 = 5.4 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(NC(=O)NC[C@H](N)C(=O)O)cc1S(=O)(=O)O nan
28446917 22973 2 None - 1 Human 5.4 pEC50 = 5.4 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 275 5 1 2 4.2 COc1cccc([C@@H](C)NCc2ccccc2Cl)c1 10.1016/j.bmcl.2010.07.060
CHEMBL1224191 22973 2 None - 1 Human 5.4 pEC50 = 5.4 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 275 5 1 2 4.2 COc1cccc([C@@H](C)NCc2ccccc2Cl)c1 10.1016/j.bmcl.2010.07.060
145946194 174313 0 None -181 2 Human 6.4 pEC50 = 6.4 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 398 4 1 2 6.2 C[C@@H](N[C@@H]1CCCN(c2cccc(C(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4125917 174313 0 None -181 2 Human 6.4 pEC50 = 6.4 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 398 4 1 2 6.2 C[C@@H](N[C@@H]1CCCN(c2cccc(C(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4300173 174313 0 None -181 2 Human 6.4 pEC50 = 6.4 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 398 4 1 2 6.2 C[C@@H](N[C@@H]1CCCN(c2cccc(C(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
89449907 159613 0 None - 1 Human 7.4 pEC50 = 7.4 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 367 6 6 7 -0.2 N[C@@H](CCC(=O)Nc1cc(Cl)cc(S(=O)(=O)O)c1O)C(=O)NO nan
CHEMBL3974015 159613 0 None - 1 Human 7.4 pEC50 = 7.4 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 367 6 6 7 -0.2 N[C@@H](CCC(=O)Nc1cc(Cl)cc(S(=O)(=O)O)c1O)C(=O)NO nan
137641303 163864 0 None - 1 Human 7.4 pEC50 = 7.4 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 463 9 5 6 2.2 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NC(CO)(CO)CO)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
CHEMBL4074358 163864 0 None - 1 Human 7.4 pEC50 = 7.4 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 463 9 5 6 2.2 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NC(CO)(CO)CO)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
137656029 165406 0 None - 1 Human 7.4 pEC50 = 7.4 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 467 8 3 5 3.4 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCCS(=O)(=O)O)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
CHEMBL4092377 165406 0 None - 1 Human 7.4 pEC50 = 7.4 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 467 8 3 5 3.4 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCCS(=O)(=O)O)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
137653796 165616 0 None - 1 Human 7.4 pEC50 = 7.4 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 453 8 3 5 3.1 C[C@@H](N[C@H]1CCN(c2ccc(S(=O)(=O)NCC(=O)O)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
CHEMBL4094738 165616 0 None - 1 Human 7.4 pEC50 = 7.4 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 453 8 3 5 3.1 C[C@@H](N[C@H]1CCN(c2ccc(S(=O)(=O)NCC(=O)O)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
53377769 157654 0 None - 1 Human 6.4 pEC50 = 6.4 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 429 7 5 8 -0.6 CS(=O)(=O)NC(=O)[C@@H](N)CCC(=O)Nc1cc(Cl)cc(S(=O)(=O)O)c1O nan
CHEMBL3957364 157654 0 None - 1 Human 6.4 pEC50 = 6.4 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 429 7 5 8 -0.6 CS(=O)(=O)NC(=O)[C@@H](N)CCC(=O)Nc1cc(Cl)cc(S(=O)(=O)O)c1O nan
137658989 165896 0 None - 1 Human 6.4 pEC50 = 6.4 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 475 9 4 5 3.4 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)N[C@H](CC(=O)O)C(=O)O)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
CHEMBL4097717 165896 0 None - 1 Human 6.4 pEC50 = 6.4 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 475 9 4 5 3.4 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)N[C@H](CC(=O)O)C(=O)O)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
52949984 23962 1 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
ChEMBL 289 2 1 3 4.2 CC(O)(c1ccc(Cl)cc1)c1nc2ccccc2s1 10.1016/j.bmcl.2010.07.077
CHEMBL1256301 23962 1 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
ChEMBL 289 2 1 3 4.2 CC(O)(c1ccc(Cl)cc1)c1nc2ccccc2s1 10.1016/j.bmcl.2010.07.077
52944111 23964 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
ChEMBL 285 3 1 4 3.6 COc1ccccc1C(C)(O)c1nc2ccccc2s1 10.1016/j.bmcl.2010.07.077
CHEMBL1256330 23964 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
ChEMBL 285 3 1 4 3.6 COc1ccccc1C(C)(O)c1nc2ccccc2s1 10.1016/j.bmcl.2010.07.077
89346558 149877 0 None - 1 Human 8.4 pEC50 = 8.4 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 367 5 5 5 0.6 Cc1c(Cl)cc(S(=O)(=O)O)cc1NC(=S)NC[C@H](N)C(=O)O nan
CHEMBL3895461 149877 0 None - 1 Human 8.4 pEC50 = 8.4 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 367 5 5 5 0.6 Cc1c(Cl)cc(S(=O)(=O)O)cc1NC(=S)NC[C@H](N)C(=O)O nan
86679031 160182 0 None - 1 Human 7.4 pEC50 = 7.4 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 320 5 4 6 0.6 N[C@@H](CSC(=O)Nc1cccc(S(=O)(=O)O)c1)C(=O)O nan
CHEMBL3978873 160182 0 None - 1 Human 7.4 pEC50 = 7.4 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 320 5 4 6 0.6 N[C@@H](CSC(=O)Nc1cccc(S(=O)(=O)O)c1)C(=O)O nan
11955187 96641 0 None - 1 Human 7.4 pEC50 = 7.4 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 530 10 1 6 5.7 COc1ccc2nc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)sc2c1 10.1016/j.bmcl.2013.01.077
CHEMBL2377744 96641 0 None - 1 Human 7.4 pEC50 = 7.4 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 530 10 1 6 5.7 COc1ccc2nc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)sc2c1 10.1016/j.bmcl.2013.01.077
16735877 96626 0 None - 1 Human 6.4 pEC50 = 6.4 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 489 10 1 6 4.2 COc1cc(C)nc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)n1 10.1016/j.bmcl.2013.01.077
CHEMBL2377729 96626 0 None - 1 Human 6.4 pEC50 = 6.4 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 489 10 1 6 4.2 COc1cc(C)nc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)n1 10.1016/j.bmcl.2013.01.077
16735429 96631 0 None - 1 Human 6.4 pEC50 = 6.4 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 507 10 1 6 4.9 COC(=O)c1sccc1NC(=O)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.077
CHEMBL2377734 96631 0 None - 1 Human 6.4 pEC50 = 6.4 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 507 10 1 6 4.9 COC(=O)c1sccc1NC(=O)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.077
44543243 204508 0 None - 1 Human 7.4 pEC50 = 7.4 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 423 6 1 4 6.0 COc1cc([C@@H](C)N[C@H](C)c2cccc(Cl)c2)nn1-c1ccc(C(F)(F)F)cc1 10.1021/jm9012278
CHEMBL571476 204508 0 None - 1 Human 7.4 pEC50 = 7.4 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 423 6 1 4 6.0 COc1cc([C@@H](C)N[C@H](C)c2cccc(Cl)c2)nn1-c1ccc(C(F)(F)F)cc1 10.1021/jm9012278
145947114 174409 0 None -43 2 Human 6.4 pEC50 = 6.4 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 384 4 1 2 5.8 C[C@@H](N[C@@H]1CCN(c2cccc(C(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4125688 174409 0 None -43 2 Human 6.4 pEC50 = 6.4 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 384 4 1 2 5.8 C[C@@H](N[C@@H]1CCN(c2cccc(C(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4301528 174409 0 None -43 2 Human 6.4 pEC50 = 6.4 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 384 4 1 2 5.8 C[C@@H](N[C@@H]1CCN(c2cccc(C(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
10453544 23007 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calciumPositive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calcium
ChEMBL 399 6 1 2 6.5 COc1ccc(CNC(C)c2cccc(C)c2)cc1-c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2010.07.060
CHEMBL1224343 23007 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calciumPositive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calcium
ChEMBL 399 6 1 2 6.5 COc1ccc(CNC(C)c2cccc(C)c2)cc1-c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2010.07.060
145946247 174292 0 None -33 2 Human 6.4 pEC50 = 6.4 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 384 4 1 2 5.8 C[C@@H](N[C@H]1CCN(c2cccc(C(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4127153 174292 0 None -33 2 Human 6.4 pEC50 = 6.4 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 384 4 1 2 5.8 C[C@@H](N[C@H]1CCN(c2cccc(C(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4299885 174292 0 None -33 2 Human 6.4 pEC50 = 6.4 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 384 4 1 2 5.8 C[C@@H](N[C@H]1CCN(c2cccc(C(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
58938087 96625 0 None - 1 Human 6.4 pEC50 = 6.4 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 445 9 1 5 3.9 O=C(Nc1cnccn1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.077
CHEMBL2377728 96625 0 None - 1 Human 6.4 pEC50 = 6.4 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 445 9 1 5 3.9 O=C(Nc1cnccn1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.077
53374566 156849 0 None - 1 Human 6.3 pEC50 = 6.3 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 321 5 5 5 -0.4 N[C@@H](CNC(=O)Nc1cc(S(=O)(=O)O)ccc1F)C(=O)O nan
CHEMBL3950758 156849 0 None - 1 Human 6.3 pEC50 = 6.3 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 321 5 5 5 -0.4 N[C@@H](CNC(=O)Nc1cc(S(=O)(=O)O)ccc1F)C(=O)O nan
137644557 164836 0 None - 1 Human 8.3 pEC50 = 8.3 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 541 10 4 7 3.8 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCCn3cnc(C(=O)O)c3C(=O)O)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
CHEMBL4086045 164836 0 None - 1 Human 8.3 pEC50 = 8.3 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 541 10 4 7 3.8 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCCn3cnc(C(=O)O)c3C(=O)O)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
58973499 174402 0 None -54 2 Human 7.3 pEC50 = 7.3 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 403 7 3 4 3.5 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCCO)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4126877 174402 0 None -54 2 Human 7.3 pEC50 = 7.3 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 403 7 3 4 3.5 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCCO)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4301421 174402 0 None -54 2 Human 7.3 pEC50 = 7.3 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 403 7 3 4 3.5 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCCO)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
137628638 163633 8 None 5 3 Human 7.3 pEC50 = 7.3 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 528 10 3 5 4.7 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCCCN3CCC(C(=O)O)CC3)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
CHEMBL4071600 163633 8 None 5 3 Human 7.3 pEC50 = 7.3 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 528 10 3 5 4.7 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCCCN3CCC(C(=O)O)CC3)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
137628638 163633 8 None 5 3 Human 7.3 pEC50 = 7.3 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 528 10 3 5 4.7 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCCCN3CCC(C(=O)O)CC3)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
CHEMBL4071600 163633 8 None 5 3 Human 7.3 pEC50 = 7.3 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 528 10 3 5 4.7 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCCCN3CCC(C(=O)O)CC3)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
71179021 153256 0 None - 1 Human 5.3 pEC50 = 5.3 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 281 5 5 4 0.2 Cc1ccc(C(=O)O)cc1NC(=O)NC[C@H](N)C(=O)O nan
CHEMBL3922323 153256 0 None - 1 Human 5.3 pEC50 = 5.3 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 281 5 5 4 0.2 Cc1ccc(C(=O)O)cc1NC(=O)NC[C@H](N)C(=O)O nan
137652733 165362 0 None - 1 Human 6.3 pEC50 = 6.3 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 495 9 3 6 3.4 C[C@@H](N[C@H]1CCN(c2ccc(S(=O)(=O)NC(=O)CCC(=O)O)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
CHEMBL4091950 165362 0 None - 1 Human 6.3 pEC50 = 6.3 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 495 9 3 6 3.4 C[C@@H](N[C@H]1CCN(c2ccc(S(=O)(=O)NC(=O)CCC(=O)O)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
44543375 205226 0 None - 1 Human 7.2 pEC50 = 7.2 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 389 6 1 4 5.6 COc1cc([C@@H](C)N[C@H](C)c2cccc(Cl)c2)nn1-c1cccc(Cl)c1 10.1021/jm9012278
CHEMBL577333 205226 0 None - 1 Human 7.2 pEC50 = 7.2 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 389 6 1 4 5.6 COc1cc([C@@H](C)N[C@H](C)c2cccc(Cl)c2)nn1-c1cccc(Cl)c1 10.1021/jm9012278
49866112 23018 0 None - 1 Human 7.2 pEC50 = 7.2 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 403 6 1 2 6.4 COc1ccc(CN[C@H](C)c2ccc(F)cc2)cc1-c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2010.07.060
CHEMBL1224423 23018 0 None - 1 Human 7.2 pEC50 = 7.2 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 403 6 1 2 6.4 COc1ccc(CN[C@H](C)c2ccc(F)cc2)cc1-c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2010.07.060
53374570 154391 0 None - 1 Human 5.2 pEC50 = 5.2 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 297 6 5 5 -0.1 COc1c(NC(=O)NC[C@H](N)C(=O)O)cccc1C(=O)O nan
CHEMBL3931232 154391 0 None - 1 Human 5.2 pEC50 = 5.2 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 297 6 5 5 -0.1 COc1c(NC(=O)NC[C@H](N)C(=O)O)cccc1C(=O)O nan
58938040 96633 0 None - 1 Human 7.2 pEC50 = 7.2 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 483 9 2 4 5.0 O=C(Nc1nc2ccccc2[nH]1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.077
CHEMBL2377736 96633 0 None - 1 Human 7.2 pEC50 = 7.2 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 483 9 2 4 5.0 O=C(Nc1nc2ccccc2[nH]1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.077
11955172 96643 0 None - 1 Human 7.2 pEC50 = 7.2 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 534 9 1 5 6.3 O=C(Nc1nc2ccc(Cl)cc2s1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.077
CHEMBL2377746 96643 0 None - 1 Human 7.2 pEC50 = 7.2 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 534 9 1 5 6.3 O=C(Nc1nc2ccc(Cl)cc2s1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.077
58973555 174312 0 None -19 2 Human 6.2 pEC50 = 6.2 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 414 5 1 3 6.1 C[C@@H](N[C@H]1CCCN(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4130093 174312 0 None -19 2 Human 6.2 pEC50 = 6.2 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 414 5 1 3 6.1 C[C@@H](N[C@H]1CCCN(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4300172 174312 0 None -19 2 Human 6.2 pEC50 = 6.2 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 414 5 1 3 6.1 C[C@@H](N[C@H]1CCCN(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
145947623 174469 0 None -51 2 Human 6.2 pEC50 = 6.2 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(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4125724 174469 0 None -51 2 Human 6.2 pEC50 = 6.2 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(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4302236 174469 0 None -51 2 Human 6.2 pEC50 = 6.2 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(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
73350406 96639 0 None - 1 Human 6.2 pEC50 = 6.2 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 514 9 1 5 6.0 Cc1cccc2sc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)nc12 10.1016/j.bmcl.2013.01.077
CHEMBL2377742 96639 0 None - 1 Human 6.2 pEC50 = 6.2 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 514 9 1 5 6.0 Cc1cccc2sc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)nc12 10.1016/j.bmcl.2013.01.077
49866004 22995 0 None - 1 Human 6.2 pEC50 = 6.2 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 385 6 1 2 6.2 COc1cccc([C@@H](C)NCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)c1 10.1016/j.bmcl.2010.07.060
CHEMBL1224264 22995 0 None - 1 Human 6.2 pEC50 = 6.2 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 385 6 1 2 6.2 COc1cccc([C@@H](C)NCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)c1 10.1016/j.bmcl.2010.07.060
52945075 24427 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
ChEMBL 305 2 1 3 4.7 CC(O)(c1ccc2ccccc2c1)c1nc2ccccc2s1 10.1016/j.bmcl.2010.07.077
CHEMBL1258390 24427 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
ChEMBL 305 2 1 3 4.7 CC(O)(c1ccc2ccccc2c1)c1nc2ccccc2s1 10.1016/j.bmcl.2010.07.077
137645663 164725 0 None - 1 Human 8.1 pEC50 = 8.1 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 577 11 4 8 3.3 C[C@@H](N[C@H]1CCN(c2ccc(S(=O)(=O)NCCn3cnc(C(=O)O)c3C(=O)O)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
CHEMBL4084641 164725 0 None - 1 Human 8.1 pEC50 = 8.1 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 577 11 4 8 3.3 C[C@@H](N[C@H]1CCN(c2ccc(S(=O)(=O)NCCn3cnc(C(=O)O)c3C(=O)O)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
137660522 166213 0 None - 1 Human 8.1 pEC50 = 8.1 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 506 12 6 7 1.8 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCCNC(CO)(CO)CO)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
CHEMBL4101097 166213 0 None - 1 Human 8.1 pEC50 = 8.1 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 506 12 6 7 1.8 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCCNC(CO)(CO)CO)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
44542630 204251 0 None - 1 Human 7.2 pEC50 = 7.2 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 389 6 1 4 5.3 COc1cc([C@@H](C)N[C@H](C)c2ccccc2)nn1-c1ccc(C(F)(F)F)cc1 10.1021/jm9012278
CHEMBL569863 204251 0 None - 1 Human 7.2 pEC50 = 7.2 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 389 6 1 4 5.3 COc1cc([C@@H](C)N[C@H](C)c2ccccc2)nn1-c1ccc(C(F)(F)F)cc1 10.1021/jm9012278
89346602 158767 0 None - 1 Human 5.2 pEC50 = 5.2 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 318 5 4 6 0.3 C[C@H](OC(=O)Nc1cccc(S(=O)(=O)O)c1)[C@H](N)C(=O)O nan
CHEMBL3966753 158767 0 None - 1 Human 5.2 pEC50 = 5.2 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 318 5 4 6 0.3 C[C@H](OC(=O)Nc1cccc(S(=O)(=O)O)c1)[C@H](N)C(=O)O nan
10341785 23004 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calciumPositive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calcium
ChEMBL 415 7 1 3 6.2 COc1cccc([C@@H](C)NCc2ccc(OC)c(-c3ccc(C(F)(F)F)cc3)c2)c1 10.1016/j.bmcl.2010.07.060
CHEMBL1224340 23004 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calciumPositive allosteric modulation of calcium sensing receptor by FLIPR assay in absence of extracellular calcium
ChEMBL 415 7 1 3 6.2 COc1cccc([C@@H](C)NCc2ccc(OC)c(-c3ccc(C(F)(F)F)cc3)c2)c1 10.1016/j.bmcl.2010.07.060
58973543 163319 0 None - 1 Human 7.1 pEC50 = 7.1 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 417 7 3 4 3.6 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCC(=O)O)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
CHEMBL4068107 163319 0 None - 1 Human 7.1 pEC50 = 7.1 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 417 7 3 4 3.6 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCC(=O)O)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2017.09.008
52947600 23974 1 None - 1 Human 7.1 pEC50 = 7.1 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
CHEMBL1256402 23974 1 None - 1 Human 7.1 pEC50 = 7.1 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
158797 10543 24 None - 1 Human 7.1 pEC50 = 7.1 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 303 7 1 2 4.6 COc1cccc(c1)[C@H](NCCCc1ccccc1Cl)C 10.1016/j.bmcl.2013.01.077
718 10543 24 None - 1 Human 7.1 pEC50 = 7.1 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 303 7 1 2 4.6 COc1cccc(c1)[C@H](NCCCc1ccccc1Cl)C 10.1016/j.bmcl.2013.01.077
CHEMBL292376 10543 24 None - 1 Human 7.1 pEC50 = 7.1 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 303 7 1 2 4.6 COc1cccc(c1)[C@H](NCCCc1ccccc1Cl)C 10.1016/j.bmcl.2013.01.077
58938054 96624 0 None - 1 Human 7.1 pEC50 = 7.1 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 472 9 1 4 5.1 Cc1cc(C)nc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1 10.1016/j.bmcl.2013.01.077
CHEMBL2377727 96624 0 None - 1 Human 7.1 pEC50 = 7.1 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 472 9 1 4 5.1 Cc1cc(C)nc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1 10.1016/j.bmcl.2013.01.077
59499356 96636 0 None - 1 Human 7.1 pEC50 = 7.1 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 518 9 1 5 5.9 O=C(Nc1nc2cc(Cl)ccc2o1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.077
CHEMBL2377739 96636 0 None - 1 Human 7.1 pEC50 = 7.1 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 518 9 1 5 5.9 O=C(Nc1nc2cc(Cl)ccc2o1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.077
73353384 96644 0 None - 1 Human 7.1 pEC50 = 7.1 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 530 10 2 6 5.2 O=C(Nc1nc2ccc(CO)cc2s1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.077
CHEMBL2377747 96644 0 None - 1 Human 7.1 pEC50 = 7.1 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 530 10 2 6 5.2 O=C(Nc1nc2ccc(CO)cc2s1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.077
73348831 96649 0 None - 1 Human 7.1 pEC50 = 7.1 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 578 10 1 7 5.1 CS(=O)(=O)c1ccc2nc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)sc2c1 10.1016/j.bmcl.2013.01.077
CHEMBL2377752 96649 0 None - 1 Human 7.1 pEC50 = 7.1 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 578 10 1 7 5.1 CS(=O)(=O)c1ccc2nc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)sc2c1 10.1016/j.bmcl.2013.01.077
49866003 22994 0 None - 1 Human 6.1 pEC50 = 6.1 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 347 7 1 3 5.2 COc1ccc(-c2cccc(CN[C@H](C)c3cccc(OC)c3)c2)cc1 10.1016/j.bmcl.2010.07.060
CHEMBL1224263 22994 0 None - 1 Human 6.1 pEC50 = 6.1 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 347 7 1 3 5.2 COc1ccc(-c2cccc(CN[C@H](C)c3cccc(OC)c3)c2)cc1 10.1016/j.bmcl.2010.07.060
89449903 150103 0 None - 1 Human 6.1 pEC50 = 6.1 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 466 8 4 8 2.7 N[C@@H](CCC(=O)Nc1cc(Cl)cc(S(=O)(=O)O)c1O)c1nnc(Cc2ccccc2)o1 nan
CHEMBL3897239 150103 0 None - 1 Human 6.1 pEC50 = 6.1 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 466 8 4 8 2.7 N[C@@H](CCC(=O)Nc1cc(Cl)cc(S(=O)(=O)O)c1O)c1nnc(Cc2ccccc2)o1 nan
145946926 174380 0 None - 1 Human 5.1 pEC50 = 5.1 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 360 5 2 3 4.5 C[C@@H](N[C@@H]1CCN(c2ccc(C(=O)O)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4127295 174380 0 None - 1 Human 5.1 pEC50 = 5.1 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 360 5 2 3 4.5 C[C@@H](N[C@@H]1CCN(c2ccc(C(=O)O)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4300972 174380 0 None - 1 Human 5.1 pEC50 = 5.1 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 360 5 2 3 4.5 C[C@@H](N[C@@H]1CCN(c2ccc(C(=O)O)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
59499324 96642 0 None - 1 Human 7.1 pEC50 = 7.1 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 584 10 1 6 6.6 O=C(Nc1nc2ccc(OC(F)(F)F)cc2s1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.077
CHEMBL2377745 96642 0 None - 1 Human 7.1 pEC50 = 7.1 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 584 10 1 6 6.6 O=C(Nc1nc2ccc(OC(F)(F)F)cc2s1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.077
44543088 204042 0 None - 1 Human 7.0 pEC50 = 7.0 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 393 5 1 3 6.0 C[C@@H](N[C@H](C)c1ccn(-c2ccc(C(F)(F)F)cc2)n1)c1cccc(Cl)c1 10.1021/jm9012278
CHEMBL568485 204042 0 None - 1 Human 7.0 pEC50 = 7.0 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 393 5 1 3 6.0 C[C@@H](N[C@H](C)c1ccn(-c2ccc(C(F)(F)F)cc2)n1)c1cccc(Cl)c1 10.1021/jm9012278
5307 8387 29 None -1 2 Human 7.0 pEC50 = 7.0 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 6 2 3 4.4 OC(=O)Cc1ccc(cc1)N1CC[C@@H](C1)N[C@@H](c1cccc2c1cccc2)C 10.1016/j.bmcl.2018.04.055
71242808 8387 29 None -1 2 Human 7.0 pEC50 = 7.0 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 6 2 3 4.4 OC(=O)Cc1ccc(cc1)N1CC[C@@H](C1)N[C@@H](c1cccc2c1cccc2)C 10.1016/j.bmcl.2018.04.055
9042 8387 29 None -1 2 Human 7.0 pEC50 = 7.0 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 6 2 3 4.4 OC(=O)Cc1ccc(cc1)N1CC[C@@H](C1)N[C@@H](c1cccc2c1cccc2)C 10.1016/j.bmcl.2018.04.055
CHEMBL4297621 8387 29 None -1 2 Human 7.0 pEC50 = 7.0 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 6 2 3 4.4 OC(=O)Cc1ccc(cc1)N1CC[C@@H](C1)N[C@@H](c1cccc2c1cccc2)C 10.1016/j.bmcl.2018.04.055
DB12388 8387 29 None -1 2 Human 7.0 pEC50 = 7.0 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 6 2 3 4.4 OC(=O)Cc1ccc(cc1)N1CC[C@@H](C1)N[C@@H](c1cccc2c1cccc2)C 10.1016/j.bmcl.2018.04.055
44405840 147907 0 None - 1 Human 10.7 pIC50 = 10.7 Functional
Antagonist activity at human calcium receptor expressed in HEK293 4.0-7 cells assessed as inhibition of intracellular calcium release by FLIPR assayAntagonist activity at human calcium receptor expressed in HEK293 4.0-7 cells assessed as inhibition of intracellular calcium release by FLIPR assay
ChEMBL 374 8 2 4 4.1 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COc1ccccc1C#N 10.1021/jm900563e
CHEMBL382741 147907 0 None - 1 Human 10.7 pIC50 = 10.7 Functional
Antagonist activity at human calcium receptor expressed in HEK293 4.0-7 cells assessed as inhibition of intracellular calcium release by FLIPR assayAntagonist activity at human calcium receptor expressed in HEK293 4.0-7 cells assessed as inhibition of intracellular calcium release by FLIPR assay
ChEMBL 374 8 2 4 4.1 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COc1ccccc1C#N 10.1021/jm900563e
9956563 205639 1 None 416 2 Human 10.5 pIC50 = 10.5 Functional
Antagonist activity at human calcium receptor expressed in HEK293 4.0-7 cells assessed as inhibition of intracellular calcium release by FLIPR assayAntagonist activity at human calcium receptor expressed in HEK293 4.0-7 cells assessed as inhibition of intracellular calcium release by FLIPR assay
ChEMBL 474 12 2 6 4.6 CCOC(=O)CCc1ccc(OC[C@H](O)CNC(C)(C)Cc2ccc3ccccc3c2)c(C#N)c1 10.1021/jm900563e
CHEMBL1204009 205639 1 None 416 2 Human 10.5 pIC50 = 10.5 Functional
Antagonist activity at human calcium receptor expressed in HEK293 4.0-7 cells assessed as inhibition of intracellular calcium release by FLIPR assayAntagonist activity at human calcium receptor expressed in HEK293 4.0-7 cells assessed as inhibition of intracellular calcium release by FLIPR assay
ChEMBL 474 12 2 6 4.6 CCOC(=O)CCc1ccc(OC[C@H](O)CNC(C)(C)Cc2ccc3ccccc3c2)c(C#N)c1 10.1021/jm900563e
CHEMBL583889 205639 1 None 416 2 Human 10.5 pIC50 = 10.5 Functional
Antagonist activity at human calcium receptor expressed in HEK293 4.0-7 cells assessed as inhibition of intracellular calcium release by FLIPR assayAntagonist activity at human calcium receptor expressed in HEK293 4.0-7 cells assessed as inhibition of intracellular calcium release by FLIPR assay
ChEMBL 474 12 2 6 4.6 CCOC(=O)CCc1ccc(OC[C@H](O)CNC(C)(C)Cc2ccc3ccccc3c2)c(C#N)c1 10.1021/jm900563e
6918446 9654 56 None 2 6 Human 10.2 pIC50 = 10.2 Functional
Antagonist activity at human calcium receptor expressed in HEK293 4.0-7 cells assessed as inhibition of intracellular calcium release by FLIPR assayAntagonist activity at human calcium receptor expressed in HEK293 4.0-7 cells assessed as inhibition of intracellular calcium release by FLIPR assay
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1021/jm900563e
716 9654 56 None 2 6 Human 10.2 pIC50 = 10.2 Functional
Antagonist activity at human calcium receptor expressed in HEK293 4.0-7 cells assessed as inhibition of intracellular calcium release by FLIPR assayAntagonist activity at human calcium receptor expressed in HEK293 4.0-7 cells assessed as inhibition of intracellular calcium release by FLIPR assay
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1021/jm900563e
CHEMBL180672 9654 56 None 2 6 Human 10.2 pIC50 = 10.2 Functional
Antagonist activity at human calcium receptor expressed in HEK293 4.0-7 cells assessed as inhibition of intracellular calcium release by FLIPR assayAntagonist activity at human calcium receptor expressed in HEK293 4.0-7 cells assessed as inhibition of intracellular calcium release by FLIPR assay
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1021/jm900563e
DB05695 9654 56 None 2 6 Human 10.2 pIC50 = 10.2 Functional
Antagonist activity at human calcium receptor expressed in HEK293 4.0-7 cells assessed as inhibition of intracellular calcium release by FLIPR assayAntagonist activity at human calcium receptor expressed in HEK293 4.0-7 cells assessed as inhibition of intracellular calcium release by FLIPR assay
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1021/jm900563e
24769038 204375 1 None - 1 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at human calcium receptor expressed in HEK293 4.0-7 cells assessed as inhibition of intracellular calcium release by FLIPR assayAntagonist activity at human calcium receptor expressed in HEK293 4.0-7 cells assessed as inhibition of intracellular calcium release by FLIPR assay
ChEMBL 446 11 3 5 4.1 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COc1ccc(CCC(=O)O)cc1C#N 10.1021/jm900563e
CHEMBL570593 204375 1 None - 1 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at human calcium receptor expressed in HEK293 4.0-7 cells assessed as inhibition of intracellular calcium release by FLIPR assayAntagonist activity at human calcium receptor expressed in HEK293 4.0-7 cells assessed as inhibition of intracellular calcium release by FLIPR assay
ChEMBL 446 11 3 5 4.1 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COc1ccc(CCC(=O)O)cc1C#N 10.1021/jm900563e
10028311 207085 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 484 9 1 6 6.0 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=S)n2Cc1cccc(OCCO)c1 10.1021/jm901811v
CHEMBL597397 207085 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 484 9 1 6 6.0 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=S)n2Cc1cccc(OCCO)c1 10.1021/jm901811v
145948146 174520 0 None 36 2 Rat 9.3 pIC50 = 9.3 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
ChEMBL 384 5 2 5 3.9 C[C@@H](N[C@H]1CCN(c2ccc(-c3nn[nH]n3)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4126450 174520 0 None 36 2 Rat 9.3 pIC50 = 9.3 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
ChEMBL 384 5 2 5 3.9 C[C@@H](N[C@H]1CCN(c2ccc(-c3nn[nH]n3)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4302858 174520 0 None 36 2 Rat 9.3 pIC50 = 9.3 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
ChEMBL 384 5 2 5 3.9 C[C@@H](N[C@H]1CCN(c2ccc(-c3nn[nH]n3)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
58973499 174402 0 None 54 2 Rat 9.0 pIC50 = 9.0 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
ChEMBL 403 7 3 4 3.5 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCCO)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4126877 174402 0 None 54 2 Rat 9.0 pIC50 = 9.0 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
ChEMBL 403 7 3 4 3.5 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCCO)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4301421 174402 0 None 54 2 Rat 9.0 pIC50 = 9.0 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
ChEMBL 403 7 3 4 3.5 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCCO)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
135565656 66967 1 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 458 7 2 4 6.5 CCc1ccc(C(CC)(CC)NC(=O)c2c(C)nn3c2N[C@@H](c2ccccc2)CC3(C)C)cc1 10.1016/j.bmc.2011.02.001
CHEMBL1689050 66967 1 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 458 7 2 4 6.5 CCc1ccc(C(CC)(CC)NC(=O)c2c(C)nn3c2N[C@@H](c2ccccc2)CC3(C)C)cc1 10.1016/j.bmc.2011.02.001
CHEMBL1689060 66967 1 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 458 7 2 4 6.5 CCc1ccc(C(CC)(CC)NC(=O)c2c(C)nn3c2N[C@@H](c2ccccc2)CC3(C)C)cc1 10.1016/j.bmc.2011.02.001
CHEMBL1739917 66967 1 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 458 7 2 4 6.5 CCc1ccc(C(CC)(CC)NC(=O)c2c(C)nn3c2N[C@@H](c2ccccc2)CC3(C)C)cc1 10.1016/j.bmc.2011.02.001
67406779 174499 0 None 134 2 Rat 8.9 pIC50 = 8.9 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
ChEMBL 414 5 1 3 6.1 C[C@@H](N[C@@H]1CCCN(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4128542 174499 0 None 134 2 Rat 8.9 pIC50 = 8.9 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
ChEMBL 414 5 1 3 6.1 C[C@@H](N[C@@H]1CCCN(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4302632 174499 0 None 134 2 Rat 8.9 pIC50 = 8.9 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
ChEMBL 414 5 1 3 6.1 C[C@@H](N[C@@H]1CCCN(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
44201334 207145 2 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 482 9 0 6 5.7 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1ccc(OC)c(OCC)c1 10.1021/jm901811v
CHEMBL597800 207145 2 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 482 9 0 6 5.7 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1ccc(OC)c(OCC)c1 10.1021/jm901811v
45140595 206204 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 422 6 0 4 5.6 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1ccc(C)cc1 10.1021/jm901811v
CHEMBL591240 206204 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 422 6 0 4 5.6 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1ccc(C)cc1 10.1021/jm901811v
24753619 22819 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 529 9 0 6 7.2 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(C(F)(F)F)c(Cc3cccnc3SC)cc(OC)c21 10.1016/j.bmcl.2010.07.016
CHEMBL1223714 22819 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 529 9 0 6 7.2 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(C(F)(F)F)c(Cc3cccnc3SC)cc(OC)c21 10.1016/j.bmcl.2010.07.016
136188835 66944 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 494 7 2 5 6.6 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(OC)c(Cl)c1 10.1016/j.bmc.2011.02.001
CHEMBL1689057 66944 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 494 7 2 5 6.6 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(OC)c(Cl)c1 10.1016/j.bmc.2011.02.001
CHEMBL1739758 66944 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 494 7 2 5 6.6 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(OC)c(Cl)c1 10.1016/j.bmc.2011.02.001
136030692 66968 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 472 7 2 4 7.1 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(C(C)C)cc1 10.1016/j.bmc.2011.02.001
CHEMBL1689051 66968 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 472 7 2 4 7.1 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(C(C)C)cc1 10.1016/j.bmc.2011.02.001
CHEMBL1739918 66968 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 472 7 2 4 7.1 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(C(C)C)cc1 10.1016/j.bmc.2011.02.001
45140794 207234 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 422 6 0 4 5.6 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1cccc(C)c1 10.1021/jm901811v
CHEMBL598436 207234 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 422 6 0 4 5.6 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1cccc(C)c1 10.1021/jm901811v
136032587 26046 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation counting
ChEMBL 404 3 2 4 4.9 CC1(C)C[C@@H](c2ccccc2)Nc2c(C(=O)NC34CC5CC(CC(C5)C3)C4)cnn21 10.1016/j.bmc.2010.10.035
CHEMBL1290328 26046 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation counting
ChEMBL 404 3 2 4 4.9 CC1(C)C[C@@H](c2ccccc2)Nc2c(C(=O)NC34CC5CC(CC(C5)C3)C4)cnn21 10.1016/j.bmc.2010.10.035
136032587 26046 0 None - 1 Human 8.0 pIC50 = 8 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 404 3 2 4 4.9 CC1(C)C[C@@H](c2ccccc2)Nc2c(C(=O)NC34CC5CC(CC(C5)C3)C4)cnn21 10.1021/jm101452x
CHEMBL1290328 26046 0 None - 1 Human 8.0 pIC50 = 8 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 404 3 2 4 4.9 CC1(C)C[C@@H](c2ccccc2)Nc2c(C(=O)NC34CC5CC(CC(C5)C3)C4)cnn21 10.1021/jm101452x
44405808 141753 0 None - 1 Human 7.0 pIC50 = 7 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 363 8 3 4 3.4 CC(C)(Cc1cc2ccccc2[nH]1)NC[C@H](O)COc1ccccc1C#N 10.1016/j.bmcl.2005.08.095
CHEMBL371936 141753 0 None - 1 Human 7.0 pIC50 = 7 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 363 8 3 4 3.4 CC(C)(Cc1cc2ccccc2[nH]1)NC[C@H](O)COc1ccccc1C#N 10.1016/j.bmcl.2005.08.095
25218712 194315 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 558 14 2 9 4.6 COc1cccc(CCNc2ncc(C(=O)NCCOc3ccccc3)c(-c3cc(OC)c(OC)c(OC)c3)n2)c1 10.1021/jm801178c
CHEMBL494441 194315 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 558 14 2 9 4.6 COc1cccc(CCNc2ncc(C(=O)NCCOc3ccccc3)c(-c3cc(OC)c(OC)c(OC)c3)n2)c1 10.1021/jm801178c
11775322 22751 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 450 5 0 3 6.0 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(Br)ccc(Br)c21 10.1016/j.bmcl.2010.07.016
CHEMBL1223437 22751 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 450 5 0 3 6.0 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(Br)ccc(Br)c21 10.1016/j.bmcl.2010.07.016
44405884 79566 1 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 433 8 2 5 4.7 CC(C)(Cc1csc2ccccc12)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(C#N)c1 10.1016/j.bmcl.2005.08.095
CHEMBL200041 79566 1 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 433 8 2 5 4.7 CC(C)(Cc1csc2ccccc12)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(C#N)c1 10.1016/j.bmcl.2005.08.095
25218703 180392 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 528 12 2 8 4.9 COc1cc(-c2nc(NCc3ccccc3C)ncc2C(=O)NCCOc2ccccc2)cc(OC)c1OC 10.1021/jm801178c
CHEMBL453360 180392 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 528 12 2 8 4.9 COc1cc(-c2nc(NCc3ccccc3C)ncc2C(=O)NCCOc2ccccc2)cc(OC)c1OC 10.1021/jm801178c
45141174 208114 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 411 6 1 4 6.4 CC(C)c1ccc(-c2nc(=O)n(C(C)C)c3ccc(NCc4ccccc4)cc23)cc1 10.1021/jm901811v
CHEMBL604302 208114 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 411 6 1 4 6.4 CC(C)c1ccc(-c2nc(=O)n(C(C)C)c3ccc(NCc4ccccc4)cc23)cc1 10.1021/jm901811v
25218733 181243 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 512 12 1 7 5.0 CCN(Cc1ccccc1)c1ccc(C(=O)NCCOc2ccccc2)c(-c2ccc(OC)nc2OC)n1 10.1021/jm801178c
CHEMBL455406 181243 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 512 12 1 7 5.0 CCN(Cc1ccccc1)c1ccc(C(=O)NCCOc2ccccc2)c(-c2ccc(OC)nc2OC)n1 10.1021/jm801178c
136188841 66940 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 490 8 2 6 5.9 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(OC)c(OC)c1 10.1016/j.bmc.2011.02.001
CHEMBL1689054 66940 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 490 8 2 6 5.9 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(OC)c(OC)c1 10.1016/j.bmc.2011.02.001
CHEMBL1739754 66940 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 490 8 2 6 5.9 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(OC)c(OC)c1 10.1016/j.bmc.2011.02.001
136188842 66943 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 478 7 2 5 6.1 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(F)c(OC)c1 10.1016/j.bmc.2011.02.001
CHEMBL1689056 66943 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 478 7 2 5 6.1 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(F)c(OC)c1 10.1016/j.bmc.2011.02.001
CHEMBL1739757 66943 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 478 7 2 5 6.1 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(F)c(OC)c1 10.1016/j.bmc.2011.02.001
136141561 66977 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 486 9 2 4 7.3 CCCCc1nn2c(c1C(=O)NC(CC)(CC)c1ccc(C)cc1)NC(c1ccccc1)CC2(C)C 10.1016/j.bmc.2011.02.001
CHEMBL1689043 66977 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 486 9 2 4 7.3 CCCCc1nn2c(c1C(=O)NC(CC)(CC)c1ccc(C)cc1)NC(c1ccccc1)CC2(C)C 10.1016/j.bmc.2011.02.001
CHEMBL1739942 66977 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 486 9 2 4 7.3 CCCCc1nn2c(c1C(=O)NC(CC)(CC)c1ccc(C)cc1)NC(c1ccccc1)CC2(C)C 10.1016/j.bmc.2011.02.001
11328907 22770 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 470 6 0 4 6.3 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(Br)c(C(F)(F)F)cc(OC)c21 10.1016/j.bmcl.2010.07.016
CHEMBL1223507 22770 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 470 6 0 4 6.3 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(Br)c(C(F)(F)F)cc(OC)c21 10.1016/j.bmcl.2010.07.016
53318971 64850 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assay
ChEMBL 497 11 3 4 6.3 CC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1-c1ccc(C(=O)O)cc1 10.1021/ml100268k
CHEMBL1672969 64850 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assay
ChEMBL 497 11 3 4 6.3 CC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1-c1ccc(C(=O)O)cc1 10.1021/ml100268k
44583033 192309 0 None -457 4 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human calcium receptor expressed in HEK293 4.0-7 cells assessed as inhibition of intracellular calcium release by FLIPR assayAntagonist activity at human calcium receptor expressed in HEK293 4.0-7 cells assessed as inhibition of intracellular calcium release by FLIPR assay
ChEMBL 385 9 4 5 2.2 COc1ccc(CC(C)(C)NC[C@H](O)COc2cccc3[nH]c(=O)[nH]c23)cc1 10.1021/jm900563e
CHEMBL486278 192309 0 None -457 4 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human calcium receptor expressed in HEK293 4.0-7 cells assessed as inhibition of intracellular calcium release by FLIPR assayAntagonist activity at human calcium receptor expressed in HEK293 4.0-7 cells assessed as inhibition of intracellular calcium release by FLIPR assay
ChEMBL 385 9 4 5 2.2 COc1ccc(CC(C)(C)NC[C@H](O)COc2cccc3[nH]c(=O)[nH]c23)cc1 10.1021/jm900563e
145947623 174469 0 None 51 2 Rat 7.9 pIC50 = 7.9 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
ChEMBL 400 5 1 3 5.7 C[C@@H](N[C@H]1CCN(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4125724 174469 0 None 51 2 Rat 7.9 pIC50 = 7.9 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
ChEMBL 400 5 1 3 5.7 C[C@@H](N[C@H]1CCN(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4302236 174469 0 None 51 2 Rat 7.9 pIC50 = 7.9 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
ChEMBL 400 5 1 3 5.7 C[C@@H](N[C@H]1CCN(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
136032596 25934 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation counting
ChEMBL 478 3 2 4 5.9 O=C(NC12CC3CC(CC(C3)C1)C2)c1cnn2c1N[C@H](c1ccccc1Cl)C[C@@H]2C(F)(F)F 10.1016/j.bmc.2010.10.035
CHEMBL1289573 25934 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation counting
ChEMBL 478 3 2 4 5.9 O=C(NC12CC3CC(CC(C3)C1)C2)c1cnn2c1N[C@H](c1ccccc1Cl)C[C@@H]2C(F)(F)F 10.1016/j.bmc.2010.10.035
135903265 191940 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CaSR in human HEK293 cells measured after 5 mins by FLIPR assayAntagonist activity at human CaSR in human HEK293 cells measured after 5 mins by FLIPR assay
ChEMBL 404 5 1 4 6.1 Cc1ccc(-c2nc(CCc3ccccc3)c(-c3cccc(F)c3O)nc2C)s1 10.1021/acsmedchemlett.1c00187
CHEMBL4857145 191940 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CaSR in human HEK293 cells measured after 5 mins by FLIPR assayAntagonist activity at human CaSR in human HEK293 cells measured after 5 mins by FLIPR assay
ChEMBL 404 5 1 4 6.1 Cc1ccc(-c2nc(CCc3ccccc3)c(-c3cccc(F)c3O)nc2C)s1 10.1021/acsmedchemlett.1c00187
45140005 207415 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 364 6 0 4 5.6 CCCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
CHEMBL599467 207415 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 364 6 0 4 5.6 CCCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
45140973 207471 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 363 6 1 4 5.6 CCCNc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
CHEMBL599858 207471 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 363 6 1 4 5.6 CCCNc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
21388140 175211 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 421 10 2 6 2.8 COc1ccc(CC(C)(C)NCC(O)COc2ccc(S(C)(=O)=O)c(C)c2)cc1 10.1016/j.bmcl.2005.08.095
CHEMBL434937 175211 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 421 10 2 6 2.8 COc1ccc(CC(C)(C)NCC(O)COc2ccc(S(C)(=O)=O)c(C)c2)cc1 10.1016/j.bmcl.2005.08.095
145947416 174427 0 None 1 2 Rat 6.9 pIC50 = 6.9 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
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
CHEMBL4129371 174427 0 None 1 2 Rat 6.9 pIC50 = 6.9 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
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
CHEMBL4301708 174427 0 None 1 2 Rat 6.9 pIC50 = 6.9 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
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
44405909 79644 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 418 8 3 4 4.5 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(O)c1 10.1016/j.bmcl.2005.08.095
CHEMBL200297 79644 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 418 8 3 4 4.5 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(O)c1 10.1016/j.bmcl.2005.08.095
118163891 147947 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 479 10 3 5 4.2 Cc1ccc(C(C)OC[C@H](O)CNC(C)(C)CC2Cc3ccccc3C2)c2c1OC1C(C(=O)O)C21 10.1016/j.bmcl.2016.06.073
CHEMBL3827912 147947 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 479 10 3 5 4.2 Cc1ccc(C(C)OC[C@H](O)CNC(C)(C)CC2Cc3ccccc3C2)c2c1OC1C(C(=O)O)C21 10.1016/j.bmcl.2016.06.073
44405908 103632 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 432 9 2 4 4.8 COc1cccc(CN2CCC[C@@H]2[C@H](O)CNC(C)(C)Cc2ccc3ccccc3c2)c1 10.1016/j.bmcl.2005.08.095
CHEMBL265362 103632 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 432 9 2 4 4.8 COc1cccc(CN2CCC[C@@H]2[C@H](O)CNC(C)(C)Cc2ccc3ccccc3c2)c1 10.1016/j.bmcl.2005.08.095
46917559 8340 12 None 138 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assay
ChEMBL 513 11 3 4 6.2 O[C@H](CNC(Cc1ccc(c(c1)F)Cl)(C)C)CO[C@@H](c1ccccc1c1ccc(c(c1)C)C(=O)O)C 10.1021/ml100268k
9474 8340 12 None 138 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assay
ChEMBL 513 11 3 4 6.2 O[C@H](CNC(Cc1ccc(c(c1)F)Cl)(C)C)CO[C@@H](c1ccccc1c1ccc(c(c1)C)C(=O)O)C 10.1021/ml100268k
CHEMBL1672973 8340 12 None 138 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assay
ChEMBL 513 11 3 4 6.2 O[C@H](CNC(Cc1ccc(c(c1)F)Cl)(C)C)CO[C@@H](c1ccccc1c1ccc(c(c1)C)C(=O)O)C 10.1021/ml100268k
136030746 65565 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 434 6 2 4 5.8 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccccc1F 10.1021/jm101452x
CHEMBL1688086 65565 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 434 6 2 4 5.8 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccccc1F 10.1021/jm101452x
136030747 65570 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 488 8 2 6 5.9 CCC(=O)Oc1ccc(C(CC)(CC)NC(=O)c2cnn3c2NC(c2ccccc2)CC3(C)C)cc1 10.1021/jm101452x
CHEMBL1688092 65570 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 488 8 2 6 5.9 CCC(=O)Oc1ccc(C(CC)(CC)NC(=O)c2cnn3c2NC(c2ccccc2)CC3(C)C)cc1 10.1021/jm101452x
45140793 207930 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 482 9 1 6 4.7 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1ccc(OCC(=O)O)cc1 10.1021/jm901811v
CHEMBL603248 207930 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 482 9 1 6 4.7 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1ccc(OCC(=O)O)cc1 10.1021/jm901811v
45141173 207147 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 397 6 0 4 4.8 C#CCN(CC#C)c1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
CHEMBL597812 207147 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 397 6 0 4 4.8 C#CCN(CC#C)c1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
10272812 13404 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 407 10 2 4 4.9 COc1ccccc1C(C)OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1 10.1016/j.bmcl.2010.04.035
CHEMBL1083313 13404 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 407 10 2 4 4.9 COc1ccccc1C(C)OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1 10.1016/j.bmcl.2010.04.035
44405852 79547 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 427 8 2 4 4.6 CC(C)(Cc1ccc2ccccc2c1)NC[C@H](O)[C@H]1CCCN1Cc1ccccc1C#N 10.1016/j.bmcl.2005.08.095
CHEMBL199964 79547 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 427 8 2 4 4.6 CC(C)(Cc1ccc2ccccc2c1)NC[C@H](O)[C@H]1CCCN1Cc1ccccc1C#N 10.1016/j.bmcl.2005.08.095
136188843 65693 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 474 7 3 5 6.0 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(C(C)O)cc1 10.1016/j.bmc.2011.02.001
CHEMBL1689107 65693 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 474 7 3 5 6.0 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(C(C)O)cc1 10.1016/j.bmc.2011.02.001
10210971 206103 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 607 12 1 8 4.5 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1cccc(NC(=O)CN2CCN(CCOC)CC2)c1 10.1021/jm901811v
CHEMBL590552 206103 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 607 12 1 8 4.5 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1cccc(NC(=O)CN2CCN(CCOC)CC2)c1 10.1021/jm901811v
45140795 207268 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 436 7 0 4 5.8 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1cccc(CC)c1 10.1021/jm901811v
CHEMBL598637 207268 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 436 7 0 4 5.8 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1cccc(CC)c1 10.1021/jm901811v
11442305 22734 1 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 450 6 0 4 5.1 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(I)ccc(OC)c21 10.1016/j.bmcl.2010.07.016
CHEMBL1223368 22734 1 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 450 6 0 4 5.1 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(I)ccc(OC)c21 10.1016/j.bmcl.2010.07.016
145946247 174292 0 None 33 2 Rat 7.9 pIC50 = 7.9 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
ChEMBL 384 4 1 2 5.8 C[C@@H](N[C@H]1CCN(c2cccc(C(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4127153 174292 0 None 33 2 Rat 7.9 pIC50 = 7.9 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
ChEMBL 384 4 1 2 5.8 C[C@@H](N[C@H]1CCN(c2cccc(C(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4299885 174292 0 None 33 2 Rat 7.9 pIC50 = 7.9 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
ChEMBL 384 4 1 2 5.8 C[C@@H](N[C@H]1CCN(c2cccc(C(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
25218734 179587 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 557 12 2 9 4.9 COc1cc(-c2nc(NCc3ccc4c(c3)OCO4)ccc2C(=O)NCCOc2ccccc2)cc(OC)c1OC 10.1021/jm801178c
CHEMBL451383 179587 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 557 12 2 9 4.9 COc1cc(-c2nc(NCc3ccc4c(c3)OCO4)ccc2C(=O)NCCOc2ccccc2)cc(OC)c1OC 10.1021/jm801178c
122636680 147980 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 465 9 2 5 4.1 Cc1ccc([C@@H](C)OC[C@H](O)CN2CCCC2(C)Cc2ccccc2)c2c1O[C@@H]1[C@@H](C(=O)O)[C@H]21 10.1016/j.bmcl.2016.06.073
CHEMBL3828329 147980 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 465 9 2 5 4.1 Cc1ccc([C@@H](C)OC[C@H](O)CN2CCCC2(C)Cc2ccccc2)c2c1O[C@@H]1[C@@H](C(=O)O)[C@H]21 10.1016/j.bmcl.2016.06.073
44405885 147484 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 434 8 2 6 4.1 CC(C)(Cc1nc2ccccc2s1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(C#N)c1 10.1016/j.bmcl.2005.08.095
CHEMBL381685 147484 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 434 8 2 6 4.1 CC(C)(Cc1nc2ccccc2s1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(C#N)c1 10.1016/j.bmcl.2005.08.095
44405851 80141 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 359 10 2 5 3.1 COc1ccc(CC(C)(C)NC[C@H](O)COc2cccc(OC)c2)cc1 10.1016/j.bmcl.2005.08.095
CHEMBL201381 80141 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 359 10 2 5 3.1 COc1ccc(CC(C)(C)NC[C@H](O)COc2cccc(OC)c2)cc1 10.1016/j.bmcl.2005.08.095
11155912 22768 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 480 6 0 4 6.0 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(Br)c(Br)cc(OC)c21 10.1016/j.bmcl.2010.07.016
CHEMBL1223505 22768 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 480 6 0 4 6.0 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(Br)c(Br)cc(OC)c21 10.1016/j.bmcl.2010.07.016
136059339 65568 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 488 8 2 6 5.7 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(COC(C)=O)cc1 10.1021/jm101452x
CHEMBL1688090 65568 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 488 8 2 6 5.7 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(COC(C)=O)cc1 10.1021/jm101452x
25198729 196516 12 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 528 13 3 8 4.0 COc1ccc(-c2nc(N[C@H](CO)Cc3ccccc3)ccc2C(=O)NCCOc2ccccc2)c(OC)n1 10.1021/jm801178c
CHEMBL515828 196516 12 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 528 13 3 8 4.0 COc1ccc(-c2nc(N[C@H](CO)Cc3ccccc3)ccc2C(=O)NCCOc2ccccc2)c(OC)n1 10.1021/jm801178c
46891590 13332 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 391 9 2 3 5.2 Cc1ccc(C(C)OC[C@H](O)CNC(C)(C)Cc2ccc3ccccc3c2)cc1 10.1016/j.bmcl.2010.04.035
CHEMBL1082999 13332 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 391 9 2 3 5.2 Cc1ccc(C(C)OC[C@H](O)CNC(C)(C)Cc2ccc3ccccc3c2)cc1 10.1016/j.bmcl.2010.04.035
46891532 13400 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 411 9 2 3 5.5 CC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1Cl 10.1016/j.bmcl.2010.04.035
CHEMBL1083307 13400 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 411 9 2 3 5.5 CC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1Cl 10.1016/j.bmcl.2010.04.035
10094574 79417 0 None 18 2 Human 6.9 pIC50 = 6.9 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 436 8 3 4 4.6 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(F)c1O 10.1016/j.bmcl.2005.08.095
CHEMBL199495 79417 0 None 18 2 Human 6.9 pIC50 = 6.9 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 436 8 3 4 4.6 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(F)c1O 10.1016/j.bmcl.2005.08.095
44405889 142001 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 463 9 3 6 4.4 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc([N+](=O)[O-])c1O 10.1016/j.bmcl.2005.08.095
CHEMBL372321 142001 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 463 9 3 6 4.4 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc([N+](=O)[O-])c1O 10.1016/j.bmcl.2005.08.095
44405894 142209 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 447 9 2 5 4.7 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc([N+](=O)[O-])c1 10.1016/j.bmcl.2005.08.095
CHEMBL372820 142209 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 447 9 2 5 4.7 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc([N+](=O)[O-])c1 10.1016/j.bmcl.2005.08.095
46228785 207059 21 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 336 4 0 4 4.8 COc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
CHEMBL597206 207059 21 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 336 4 0 4 4.8 COc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
10345214 10142 13 None 1 2 Human 6.8 pIC50 = 6.8 Functional
Negative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cellsNegative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cells
ChEMBL 447 11 3 4 3.9 O[C@@H](COc1cc(CCC(=O)O)cc(c1F)F)CNC(CC1Cc2c(C1)cccc2)(C)C 10.1016/j.bmcl.2009.04.044
9473 10142 13 None 1 2 Human 6.8 pIC50 = 6.8 Functional
Negative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cellsNegative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cells
ChEMBL 447 11 3 4 3.9 O[C@@H](COc1cc(CCC(=O)O)cc(c1F)F)CNC(CC1Cc2c(C1)cccc2)(C)C 10.1016/j.bmcl.2009.04.044
CHEMBL1198855 10142 13 None 1 2 Human 6.8 pIC50 = 6.8 Functional
Negative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cellsNegative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cells
ChEMBL 447 11 3 4 3.9 O[C@@H](COc1cc(CCC(=O)O)cc(c1F)F)CNC(CC1Cc2c(C1)cccc2)(C)C 10.1016/j.bmcl.2009.04.044
DB05255 10142 13 None 1 2 Human 6.8 pIC50 = 6.8 Functional
Negative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cellsNegative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cells
ChEMBL 447 11 3 4 3.9 O[C@@H](COc1cc(CCC(=O)O)cc(c1F)F)CNC(CC1Cc2c(C1)cccc2)(C)C 10.1016/j.bmcl.2009.04.044
11214076 22816 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 493 8 0 5 6.2 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(Br)c(Cc3cccnc3)cc(OC)c21 10.1016/j.bmcl.2010.07.016
CHEMBL1223711 22816 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 493 8 0 5 6.2 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(Br)c(Cc3cccnc3)cc(OC)c21 10.1016/j.bmcl.2010.07.016
25218731 180829 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 561 10 2 9 4.9 COc1ccc(-c2nc(NCc3ccc4c(c3)OCO4)ncc2C(=O)NC(C)Cc2ccc(Cl)cc2)c(OC)n1 10.1021/jm801178c
CHEMBL454385 180829 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 561 10 2 9 4.9 COc1ccc(-c2nc(NCc3ccc4c(c3)OCO4)ncc2C(=O)NC(C)Cc2ccc(Cl)cc2)c(OC)n1 10.1021/jm801178c
11478504 194479 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 558 14 3 9 4.0 COc1cc(-c2nc(N[C@H](CO)Cc3ccccc3)ncc2C(=O)NCCOc2ccccc2)cc(OC)c1OC 10.1021/jm801178c
CHEMBL495263 194479 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 558 14 3 9 4.0 COc1cc(-c2nc(N[C@H](CO)Cc3ccccc3)ncc2C(=O)NCCOc2ccccc2)cc(OC)c1OC 10.1021/jm801178c
25218706 195824 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 558 12 2 10 4.3 COc1cc(-c2nc(NCc3ccc4c(c3)OCO4)ncc2C(=O)NCCOc2ccccc2)cc(OC)c1OC 10.1021/jm801178c
CHEMBL509410 195824 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 558 12 2 10 4.3 COc1cc(-c2nc(NCc3ccc4c(c3)OCO4)ncc2C(=O)NCCOc2ccccc2)cc(OC)c1OC 10.1021/jm801178c
46891415 13168 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 405 11 2 3 5.7 CCCC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1 10.1016/j.bmcl.2010.04.035
CHEMBL1082306 13168 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 405 11 2 3 5.7 CCCC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1 10.1016/j.bmcl.2010.04.035
136059345 65759 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 592 6 2 4 9.0 CC1(C)CC(c2ccccc2)Nc2c(C(=O)NC(c3ccc(C(F)(F)F)cc3)(C3CCCCC3)C3CCCCC3)cnn21 10.1021/jm101452x
CHEMBL1689814 65759 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 592 6 2 4 9.0 CC1(C)CC(c2ccccc2)Nc2c(C(=O)NC(c3ccc(C(F)(F)F)cc3)(C3CCCCC3)C3CCCCC3)cnn21 10.1021/jm101452x
25218710 194360 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 542 13 1 8 4.7 COc1cc(-c2nc(N(C)CCc3ccccc3)ncc2C(=O)NCCOc2ccccc2)cc(OC)c1OC 10.1021/jm801178c
CHEMBL494646 194360 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 542 13 1 8 4.7 COc1cc(-c2nc(N(C)CCc3ccccc3)ncc2C(=O)NCCOc2ccccc2)cc(OC)c1OC 10.1021/jm801178c
53326826 64848 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assay
ChEMBL 497 11 3 4 6.3 CC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccc(-c2ccc(C(=O)O)cc2)cc1 10.1021/ml100268k
CHEMBL1672967 64848 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assay
ChEMBL 497 11 3 4 6.3 CC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccc(-c2ccc(C(=O)O)cc2)cc1 10.1021/ml100268k
25218732 180830 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 541 13 1 7 5.6 CCN(Cc1ccccc1)c1ccc(C(=O)NCCOc2ccccc2)c(-c2cc(OC)c(OC)c(OC)c2)n1 10.1021/jm801178c
CHEMBL454386 180830 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 541 13 1 7 5.6 CCN(Cc1ccccc1)c1ccc(C(=O)NCCOc2ccccc2)c(-c2cc(OC)c(OC)c(OC)c2)n1 10.1021/jm801178c
44405861 79682 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 448 9 3 5 4.5 COc1cccc(CN2CCC[C@@H]2[C@H](O)CNC(C)(C)Cc2ccc3ccccc3c2)c1O 10.1016/j.bmcl.2005.08.095
CHEMBL200422 79682 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 448 9 3 5 4.5 COc1cccc(CN2CCC[C@@H]2[C@H](O)CNC(C)(C)Cc2ccc3ccccc3c2)c1O 10.1016/j.bmcl.2005.08.095
44405853 103442 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 480 8 2 3 5.5 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(Br)c1 10.1016/j.bmcl.2005.08.095
CHEMBL263828 103442 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 480 8 2 3 5.5 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(Br)c1 10.1016/j.bmcl.2005.08.095
45140003 207032 45 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 322 3 1 4 4.5 CC(C)c1ccc(-c2nc(=O)n(C(C)C)c3ccc(O)cc23)cc1 10.1021/jm901811v
CHEMBL597011 207032 45 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 322 3 1 4 4.5 CC(C)c1ccc(-c2nc(=O)n(C(C)C)c3ccc(O)cc23)cc1 10.1021/jm901811v
49865533 22771 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 470 6 0 4 6.3 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(C(F)(F)F)c(Br)cc(OC)c21 10.1016/j.bmcl.2010.07.016
CHEMBL1223508 22771 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 470 6 0 4 6.3 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(C(F)(F)F)c(Br)cc(OC)c21 10.1016/j.bmcl.2010.07.016
10111740 13292 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 402 9 2 4 4.8 CC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1C#N 10.1016/j.bmcl.2010.04.035
CHEMBL1082787 13292 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 402 9 2 4 4.8 CC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1C#N 10.1016/j.bmcl.2010.04.035
44405874 78910 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 447 9 2 5 4.7 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1ccccc1[N+](=O)[O-] 10.1016/j.bmcl.2005.08.095
CHEMBL197863 78910 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 447 9 2 5 4.7 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1ccccc1[N+](=O)[O-] 10.1016/j.bmcl.2005.08.095
25218735 196343 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 547 12 2 7 5.8 COc1cc(-c2nc(NCc3cccc(Cl)c3)ccc2C(=O)NCCOc2ccccc2)cc(OC)c1OC 10.1021/jm801178c
CHEMBL514434 196343 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 547 12 2 7 5.8 COc1cc(-c2nc(NCc3cccc(Cl)c3)ccc2C(=O)NCCOc2ccccc2)cc(OC)c1OC 10.1021/jm801178c
136059347 65762 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 450 6 2 4 6.3 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1cccc(Cl)c1 10.1021/jm101452x
CHEMBL1689817 65762 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 450 6 2 4 6.3 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1cccc(Cl)c1 10.1021/jm101452x
122636590 147917 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 467 10 3 5 4.2 Cc1ccc(CC(C)(C)NC[C@@H](O)CO[C@H](C)c2ccc(C)c3c2[C@@H]2[C@H](O3)[C@H]2C(=O)O)cc1C 10.1016/j.bmcl.2016.06.073
CHEMBL3827570 147917 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 467 10 3 5 4.2 Cc1ccc(CC(C)(C)NC[C@@H](O)CO[C@H](C)c2ccc(C)c3c2[C@@H]2[C@H](O3)[C@H]2C(=O)O)cc1C 10.1016/j.bmcl.2016.06.073
45140212 206205 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 374 5 0 4 5.2 CC#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
CHEMBL591241 206205 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 374 5 0 4 5.2 CC#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
46891417 13272 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 419 12 2 3 6.1 CCCCC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1 10.1016/j.bmcl.2010.04.035
CHEMBL1082718 13272 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 419 12 2 3 6.1 CCCCC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1 10.1016/j.bmcl.2010.04.035
10111057 13331 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 391 9 2 3 5.2 Cc1cccc(C(C)OC[C@H](O)CNC(C)(C)Cc2ccc3ccccc3c2)c1 10.1016/j.bmcl.2010.04.035
CHEMBL1082998 13331 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 391 9 2 3 5.2 Cc1cccc(C(C)OC[C@H](O)CNC(C)(C)Cc2ccc3ccccc3c2)c1 10.1016/j.bmcl.2010.04.035
11849382 20687 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Activity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulationActivity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulation
ChEMBL 456 6 2 3 6.1 C[C@@H](N[C@@H]1CCCC[C@H]1NC(=O)c1ccc(OC(F)(F)F)cc1)c1cccc2ccccc12 10.1021/jm051233+
CHEMBL1196384 20687 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Activity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulationActivity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulation
ChEMBL 456 6 2 3 6.1 C[C@@H](N[C@@H]1CCCC[C@H]1NC(=O)c1ccc(OC(F)(F)F)cc1)c1cccc2ccccc12 10.1021/jm051233+
CHEMBL556781 20687 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Activity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulationActivity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulation
ChEMBL 456 6 2 3 6.1 C[C@@H](N[C@@H]1CCCC[C@H]1NC(=O)c1ccc(OC(F)(F)F)cc1)c1cccc2ccccc12 10.1021/jm051233+
49865390 22709 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 294 5 0 3 4.5 COCCn1c(-c2ccc(C(C)C)cc2)nc2ccccc21 10.1016/j.bmcl.2010.07.016
CHEMBL1223299 22709 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 294 5 0 3 4.5 COCCn1c(-c2ccc(C(C)C)cc2)nc2ccccc21 10.1016/j.bmcl.2010.07.016
9910748 64844 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assay
ChEMBL 433 11 3 4 4.8 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)CO[C@@H](c1ccccc1CO)C1CC1 10.1021/ml100268k
CHEMBL1672960 64844 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assay
ChEMBL 433 11 3 4 4.8 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)CO[C@@H](c1ccccc1CO)C1CC1 10.1021/ml100268k
53318993 64849 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assay
ChEMBL 497 11 3 4 6.3 CC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1cccc(-c2ccc(C(=O)O)cc2)c1 10.1021/ml100268k
CHEMBL1672968 64849 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assay
ChEMBL 497 11 3 4 6.3 CC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1cccc(-c2ccc(C(=O)O)cc2)c1 10.1021/ml100268k
54584449 69489 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Negative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cellsNegative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cells
ChEMBL 525 11 3 4 5.8 Cc1ccc(CC(C)(C)NC[C@@H](O)CO[C@H](C)c2ccccc2C2CC3CC2C2C(C(=O)O)C32)cc1Cl 10.1016/j.bmcl.2009.04.044
CHEMBL1783935 69489 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Negative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cellsNegative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cells
ChEMBL 525 11 3 4 5.8 Cc1ccc(CC(C)(C)NC[C@@H](O)CO[C@H](C)c2ccccc2C2CC3CC2C2C(C(=O)O)C32)cc1Cl 10.1016/j.bmcl.2009.04.044
10133274 207379 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 362 6 0 4 5.3 C=CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
CHEMBL599228 207379 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 362 6 0 4 5.3 C=CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
25218721 195998 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 554 14 1 7 5.9 CCN(Cc1ccccc1)c1ncc(C(=O)NCCCCc2ccccc2)c(-c2cc(OC)c(OC)c(OC)c2)n1 10.1021/jm801178c
CHEMBL511485 195998 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 554 14 1 7 5.9 CCN(Cc1ccccc1)c1ncc(C(=O)NCCCCc2ccccc2)c(-c2cc(OC)c(OC)c(OC)c2)n1 10.1021/jm801178c
49865441 22736 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 354 7 0 5 4.5 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(OC)ccc(OC)c21 10.1016/j.bmcl.2010.07.016
CHEMBL1223370 22736 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 354 7 0 5 4.5 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(OC)ccc(OC)c21 10.1016/j.bmcl.2010.07.016
25218725 186010 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 506 9 1 5 5.6 CN(Cc1ccccc1)c1ncc(C(=O)NCCOc2ccccc2)c(-c2ccc(C(F)(F)F)cc2)n1 10.1021/jm801178c
CHEMBL472731 186010 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 506 9 1 5 5.6 CN(Cc1ccccc1)c1ncc(C(=O)NCCOc2ccccc2)c(-c2ccc(C(F)(F)F)cc2)n1 10.1021/jm801178c
45140792 206997 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 452 8 0 5 5.6 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1ccc(OCC)cc1 10.1021/jm901811v
CHEMBL596789 206997 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 452 8 0 5 5.6 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1ccc(OCC)cc1 10.1021/jm901811v
122636679 147969 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 503 11 3 6 4.3 COc1ccc(CC(C)(C)NC[C@@H](O)CO[C@H](C)c2ccc(C)c3c2[C@@H]2[C@H](O3)[C@H]2C(=O)O)c(Cl)c1 10.1016/j.bmcl.2016.06.073
CHEMBL3828187 147969 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 503 11 3 6 4.3 COc1ccc(CC(C)(C)NC[C@@H](O)CO[C@H](C)c2ccc(C)c3c2[C@@H]2[C@H](O3)[C@H]2C(=O)O)c(Cl)c1 10.1016/j.bmcl.2016.06.073
11430368 22475 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 430 7 0 4 5.8 CCc1cc(OC)c2c(nc(-c3ccc(C(C)C)cc3)n2CCOC)c1Br 10.1016/j.bmcl.2010.07.016
CHEMBL1222424 22475 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 430 7 0 4 5.8 CCc1cc(OC)c2c(nc(-c3ccc(C(C)C)cc3)n2CCOC)c1Br 10.1016/j.bmcl.2010.07.016
11486852 22752 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 415 6 0 4 5.2 COc1ccc(Br)c2nc(-c3ccc(C(C)C)cc3)n(CCN(C)C)c12 10.1016/j.bmcl.2010.07.016
CHEMBL1223438 22752 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 415 6 0 4 5.2 COc1ccc(Br)c2nc(-c3ccc(C(C)C)cc3)n(CCN(C)C)c12 10.1016/j.bmcl.2010.07.016
10387815 79476 0 None 11 2 Human 6.7 pIC50 = 6.7 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 427 8 2 4 4.6 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(C#N)c1 10.1016/j.bmcl.2005.08.095
CHEMBL199716 79476 0 None 11 2 Human 6.7 pIC50 = 6.7 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 427 8 2 4 4.6 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(C#N)c1 10.1016/j.bmcl.2005.08.095
49865391 22711 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 324 6 0 4 4.5 COCCn1c(-c2ccc(C(C)C)cc2)nc2cccc(OC)c21 10.1016/j.bmcl.2010.07.016
CHEMBL1223300 22711 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 324 6 0 4 4.5 COCCn1c(-c2ccc(C(C)C)cc2)nc2cccc(OC)c21 10.1016/j.bmcl.2010.07.016
49865393 22713 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 338 6 0 4 4.8 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(OC)ccc(C)c21 10.1016/j.bmcl.2010.07.016
CHEMBL1223302 22713 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 338 6 0 4 4.8 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(OC)ccc(C)c21 10.1016/j.bmcl.2010.07.016
49865337 22678 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 336 6 0 3 5.6 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(C(C)C)cccc21 10.1016/j.bmcl.2010.07.016
CHEMBL1223222 22678 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 336 6 0 3 5.6 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(C(C)C)cccc21 10.1016/j.bmcl.2010.07.016
25218736 183580 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 518 11 2 7 5.2 COc1ccc(-c2nc(NCc3cccc(Cl)c3)ccc2C(=O)NCCOc2ccccc2)c(OC)n1 10.1021/jm801178c
CHEMBL460726 183580 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 518 11 2 7 5.2 COc1ccc(-c2nc(NCc3cccc(Cl)c3)ccc2C(=O)NCCOc2ccccc2)c(OC)n1 10.1021/jm801178c
136030753 66969 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 460 7 2 5 5.9 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(OC)cc1 10.1016/j.bmc.2011.02.001
CHEMBL1689052 66969 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 460 7 2 5 5.9 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(OC)cc1 10.1016/j.bmc.2011.02.001
CHEMBL1739919 66969 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 460 7 2 5 5.9 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(OC)cc1 10.1016/j.bmc.2011.02.001
49865681 22837 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 489 8 0 6 6.5 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(C(F)(F)F)c(Cc3nccs3)cc(OC)c21 10.1016/j.bmcl.2010.07.016
CHEMBL1223772 22837 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 489 8 0 6 6.5 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(C(F)(F)F)c(Cc3nccs3)cc(OC)c21 10.1016/j.bmcl.2010.07.016
145946194 174313 0 None 181 2 Rat 8.7 pIC50 = 8.7 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
ChEMBL 398 4 1 2 6.2 C[C@@H](N[C@@H]1CCCN(c2cccc(C(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4125917 174313 0 None 181 2 Rat 8.7 pIC50 = 8.7 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
ChEMBL 398 4 1 2 6.2 C[C@@H](N[C@@H]1CCCN(c2cccc(C(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4300173 174313 0 None 181 2 Rat 8.7 pIC50 = 8.7 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
ChEMBL 398 4 1 2 6.2 C[C@@H](N[C@@H]1CCCN(c2cccc(C(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
136141575 66941 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 536 9 2 5 7.5 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(OCc2ccccc2)cc1 10.1016/j.bmc.2011.02.001
CHEMBL1689055 66941 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 536 9 2 5 7.5 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(OCc2ccccc2)cc1 10.1016/j.bmc.2011.02.001
CHEMBL1739755 66941 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 536 9 2 5 7.5 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(OCc2ccccc2)cc1 10.1016/j.bmc.2011.02.001
136059370 66951 1 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 430 6 2 4 5.9 CCC(CC)(NC(=O)c1cnn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(C)cc1 10.1016/j.bmc.2011.02.001
CHEMBL1688099 66951 1 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 430 6 2 4 5.9 CCC(CC)(NC(=O)c1cnn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(C)cc1 10.1016/j.bmc.2011.02.001
CHEMBL1739780 66951 1 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 430 6 2 4 5.9 CCC(CC)(NC(=O)c1cnn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(C)cc1 10.1016/j.bmc.2011.02.001
136030703 66966 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 430 6 2 4 5.9 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccccc1 10.1016/j.bmc.2011.02.001
CHEMBL1689049 66966 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 430 6 2 4 5.9 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccccc1 10.1016/j.bmc.2011.02.001
CHEMBL1739916 66966 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 430 6 2 4 5.9 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccccc1 10.1016/j.bmc.2011.02.001
136059370 66951 1 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 430 6 2 4 5.9 CCC(CC)(NC(=O)c1cnn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(C)cc1 10.1021/jm101452x
CHEMBL1688099 66951 1 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 430 6 2 4 5.9 CCC(CC)(NC(=O)c1cnn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(C)cc1 10.1021/jm101452x
CHEMBL1739780 66951 1 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 430 6 2 4 5.9 CCC(CC)(NC(=O)c1cnn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(C)cc1 10.1021/jm101452x
136071339 66937 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 444 6 2 4 6.2 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(C)cc1 10.1016/j.bmc.2011.02.001
CHEMBL1689047 66937 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 444 6 2 4 6.2 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(C)cc1 10.1016/j.bmc.2011.02.001
CHEMBL1739733 66937 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 444 6 2 4 6.2 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(C)cc1 10.1016/j.bmc.2011.02.001
10120467 206099 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 563 9 1 7 4.4 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1cccc(NC(=O)CN2CCN(C)CC2)c1 10.1021/jm901811v
CHEMBL590539 206099 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 563 9 1 7 4.4 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1cccc(NC(=O)CN2CCN(C)CC2)c1 10.1021/jm901811v
45141391 207060 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 424 6 1 4 5.9 CC(C)c1ccc(-c2nc(=O)n(Cc3ccccc3)c3ccc(O)c(CC4CC4)c23)cc1 10.1021/jm901811v
CHEMBL597208 207060 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 424 6 1 4 5.9 CC(C)c1ccc(-c2nc(=O)n(Cc3ccccc3)c3ccc(O)c(CC4CC4)c23)cc1 10.1021/jm901811v
24753707 22836 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 545 9 0 6 6.2 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(C(F)(F)F)c(Cc3cccnc3[S+](C)[O-])cc(OC)c21 10.1016/j.bmcl.2010.07.016
CHEMBL1223771 22836 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 545 9 0 6 6.2 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(C(F)(F)F)c(Cc3cccnc3[S+](C)[O-])cc(OC)c21 10.1016/j.bmcl.2010.07.016
45140969 208151 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 438 7 0 5 5.3 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1cccc(OC)c1 10.1021/jm901811v
CHEMBL604506 208151 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 438 7 0 5 5.3 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1cccc(OC)c1 10.1021/jm901811v
122636646 147939 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 479 10 3 5 4.2 Cc1ccc([C@@H](C)OC[C@H](O)CNC(C)(C)CC2Cc3ccccc3C2)c2c1O[C@@H]1[C@@H](C(=O)O)[C@H]21 10.1016/j.bmcl.2016.06.073
CHEMBL3827736 147939 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 479 10 3 5 4.2 Cc1ccc([C@@H](C)OC[C@H](O)CNC(C)(C)CC2Cc3ccccc3C2)c2c1O[C@@H]1[C@@H](C(=O)O)[C@H]21 10.1016/j.bmcl.2016.06.073
25218698 195721 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 542 13 1 8 5.0 CCN(Cc1ccccc1)c1ncc(C(=O)NCCOc2ccccc2)c(-c2cc(OC)c(OC)c(OC)c2)n1 10.1021/jm801178c
CHEMBL508063 195721 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 542 13 1 8 5.0 CCN(Cc1ccccc1)c1ncc(C(=O)NCCOc2ccccc2)c(-c2cc(OC)c(OC)c(OC)c2)n1 10.1021/jm801178c
46891416 13271 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 405 10 2 3 5.5 CC(C)C(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1 10.1016/j.bmcl.2010.04.035
CHEMBL1082717 13271 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 405 10 2 3 5.5 CC(C)C(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1 10.1016/j.bmcl.2010.04.035
10222076 13476 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 391 9 2 3 5.2 Cc1ccccc1C(C)OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1 10.1016/j.bmcl.2010.04.035
CHEMBL1083610 13476 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 391 9 2 3 5.2 Cc1ccccc1C(C)OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1 10.1016/j.bmcl.2010.04.035
46891465 13651 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 431 10 2 3 6.1 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COC(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2010.04.035
CHEMBL1084200 13651 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 431 10 2 3 6.1 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COC(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2010.04.035
118181526 147968 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 491 10 3 5 4.4 Cc1ccc(C(C)OC[C@H](O)CNC(C)(C)Cc2ccc(Cl)c(F)c2)c2c1OC1C(C(=O)O)C21 10.1016/j.bmcl.2016.06.073
CHEMBL3828182 147968 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 491 10 3 5 4.4 Cc1ccc(C(C)OC[C@H](O)CNC(C)(C)Cc2ccc(Cl)c(F)c2)c2c1OC1C(C(=O)O)C21 10.1016/j.bmcl.2016.06.073
122636753 147992 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 489 10 3 5 4.8 Cc1ccc([C@@H](C)OC[C@H](O)CNC(C)(C)Cc2ccc3ccccc3c2)c2c1O[C@@H]1[C@H]2[C@H]1C(=O)O 10.1016/j.bmcl.2016.06.073
CHEMBL3828483 147992 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 489 10 3 5 4.8 Cc1ccc([C@@H](C)OC[C@H](O)CNC(C)(C)Cc2ccc3ccccc3c2)c2c1O[C@@H]1[C@H]2[C@H]1C(=O)O 10.1016/j.bmcl.2016.06.073
122636665 147911 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 497 10 3 7 3.4 Cc1ccc([C@@H](C)OC[C@H](O)CNC(C)(C)Cc2ccc3c(c2)OCCO3)c2c1O[C@@H]1[C@@H](C(=O)O)[C@H]21 10.1016/j.bmcl.2016.06.073
CHEMBL3827475 147911 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 497 10 3 7 3.4 Cc1ccc([C@@H](C)OC[C@H](O)CNC(C)(C)Cc2ccc3c(c2)OCCO3)c2c1O[C@@H]1[C@@H](C(=O)O)[C@H]21 10.1016/j.bmcl.2016.06.073
11427732 22753 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 338 6 0 4 4.8 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(C)ccc(OC)c21 10.1016/j.bmcl.2010.07.016
CHEMBL1223439 22753 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 338 6 0 4 4.8 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(C)ccc(OC)c21 10.1016/j.bmcl.2010.07.016
46891365 13269 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 389 10 2 3 5.1 C=CC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1 10.1016/j.bmcl.2010.04.035
CHEMBL1082712 13269 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 389 10 2 3 5.1 C=CC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1 10.1016/j.bmcl.2010.04.035
25218720 185972 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 540 13 1 7 5.6 CCN(Cc1ccccc1)c1ncc(C(=O)NCCCc2ccccc2)c(-c2cc(OC)c(OC)c(OC)c2)n1 10.1021/jm801178c
CHEMBL472406 185972 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 540 13 1 7 5.6 CCN(Cc1ccccc1)c1ncc(C(=O)NCCCc2ccccc2)c(-c2cc(OC)c(OC)c(OC)c2)n1 10.1021/jm801178c
45139807 207442 1 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 322 4 0 4 4.2 CCc1ccc(-c2nc(=O)n(C(C)C)c3ccc(OC)cc23)cc1 10.1021/jm901811v
CHEMBL599664 207442 1 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 322 4 0 4 4.2 CCc1ccc(-c2nc(=O)n(C(C)C)c3ccc(OC)cc23)cc1 10.1021/jm901811v
45139809 207473 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 350 3 0 4 5.0 COc1ccc2c(c1)c(-c1ccc(C(C)(C)C)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
CHEMBL599868 207473 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 350 3 0 4 5.0 COc1ccc2c(c1)c(-c1ccc(C(C)(C)C)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
49865392 22712 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 308 5 0 3 4.8 COCCn1c(-c2ccc(C(C)C)cc2)nc2cccc(C)c21 10.1016/j.bmcl.2010.07.016
CHEMBL1223301 22712 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 308 5 0 3 4.8 COCCn1c(-c2ccc(C(C)C)cc2)nc2cccc(C)c21 10.1016/j.bmcl.2010.07.016
11281119 22733 1 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 402 6 0 4 5.2 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(Br)ccc(OC)c21 10.1016/j.bmcl.2010.07.016
CHEMBL1223367 22733 1 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 402 6 0 4 5.2 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(Br)ccc(OC)c21 10.1016/j.bmcl.2010.07.016
25218729 182614 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 529 11 2 10 3.7 COc1ccc(-c2nc(NCc3ccc4c(c3)OCO4)ncc2C(=O)NCCOc2ccccc2)c(OC)n1 10.1021/jm801178c
CHEMBL458516 182614 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 529 11 2 10 3.7 COc1ccc(-c2nc(NCc3ccc4c(c3)OCO4)ncc2C(=O)NCCOc2ccccc2)c(OC)n1 10.1021/jm801178c
46891533 13401 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 411 9 2 3 5.5 CC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.035
CHEMBL1083308 13401 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 411 9 2 3 5.5 CC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.035
46891266 13780 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 377 9 2 3 4.9 CC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1 10.1016/j.bmcl.2010.04.035
CHEMBL1084757 13780 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 377 9 2 3 4.9 CC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1 10.1016/j.bmcl.2010.04.035
25218699 180825 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 494 13 2 8 4.4 COc1cc(-c2nc(NCCC(C)C)ncc2C(=O)NCCOc2ccccc2)cc(OC)c1OC 10.1021/jm801178c
CHEMBL454375 180825 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 494 13 2 8 4.4 COc1cc(-c2nc(NCCC(C)C)ncc2C(=O)NCCOc2ccccc2)cc(OC)c1OC 10.1021/jm801178c
45140004 208854 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 350 5 0 4 5.2 CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
CHEMBL608721 208854 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 350 5 0 4 5.2 CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
53324273 64846 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assay
ChEMBL 435 11 3 4 4.5 C[C@@H](OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1CC(=O)O 10.1021/ml100268k
CHEMBL1672965 64846 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assay
ChEMBL 435 11 3 4 4.5 C[C@@H](OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1CC(=O)O 10.1021/ml100268k
10387815 79476 0 None -11 2 Rat 5.7 pIC50 = 5.7 Functional
Inhibition of extracellular calcium-induced inositol triphosphate generation in rat MTC cells expressing calcium-sensing receptorInhibition of extracellular calcium-induced inositol triphosphate generation in rat MTC cells expressing calcium-sensing receptor
ChEMBL 427 8 2 4 4.6 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(C#N)c1 10.1016/j.bmcl.2005.08.095
CHEMBL199716 79476 0 None -11 2 Rat 5.7 pIC50 = 5.7 Functional
Inhibition of extracellular calcium-induced inositol triphosphate generation in rat MTC cells expressing calcium-sensing receptorInhibition of extracellular calcium-induced inositol triphosphate generation in rat MTC cells expressing calcium-sensing receptor
ChEMBL 427 8 2 4 4.6 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(C#N)c1 10.1016/j.bmcl.2005.08.095
46891319 13595 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 391 9 2 3 5.1 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COC(C)(C)c1ccccc1 10.1016/j.bmcl.2010.04.035
CHEMBL1083949 13595 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 391 9 2 3 5.1 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COC(C)(C)c1ccccc1 10.1016/j.bmcl.2010.04.035
46871629 14126 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 417 10 2 3 5.6 Cc1ccccc1[C@H](OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)C1CC1 10.1016/j.bmcl.2010.04.035
CHEMBL1086282 14126 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 417 10 2 3 5.6 Cc1ccccc1[C@H](OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)C1CC1 10.1016/j.bmcl.2010.04.035
46871629 14126 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assay
ChEMBL 417 10 2 3 5.6 Cc1ccccc1[C@H](OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)C1CC1 10.1021/ml100268k
CHEMBL1086282 14126 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assay
ChEMBL 417 10 2 3 5.6 Cc1ccccc1[C@H](OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)C1CC1 10.1021/ml100268k
53325543 64852 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assay
ChEMBL 499 11 3 4 5.9 C[C@@H](OC[C@H](O)CNC(C)(C)Cc1ccc(Cl)c(F)c1)c1ccccc1-c1ccc(C(=O)O)cc1 10.1021/ml100268k
CHEMBL1672971 64852 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assay
ChEMBL 499 11 3 4 5.9 C[C@@H](OC[C@H](O)CNC(C)(C)Cc1ccc(Cl)c(F)c1)c1ccccc1-c1ccc(C(=O)O)cc1 10.1021/ml100268k
136059342 65757 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 540 10 2 4 8.2 CCCCC(CCCC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C(F)(F)F)cc1 10.1021/jm101452x
CHEMBL1689812 65757 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 540 10 2 4 8.2 CCCCC(CCCC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C(F)(F)F)cc1 10.1021/jm101452x
6918446 9654 56 None 2 6 Human 7.6 pIC50 = 7.6 Functional
Negative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cellsNegative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cells
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1016/j.bmcl.2009.04.044
716 9654 56 None 2 6 Human 7.6 pIC50 = 7.6 Functional
Negative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cellsNegative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cells
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1016/j.bmcl.2009.04.044
CHEMBL180672 9654 56 None 2 6 Human 7.6 pIC50 = 7.6 Functional
Negative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cellsNegative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cells
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1016/j.bmcl.2009.04.044
DB05695 9654 56 None 2 6 Human 7.6 pIC50 = 7.6 Functional
Negative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cellsNegative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cells
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1016/j.bmcl.2009.04.044
54586367 69485 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Negative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cellsNegative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cells
ChEMBL 506 10 3 5 4.4 Cc1ccc(CC(C)(C)NC[C@@H](O)COc2cc(C3CC4CC3C3C(C(=O)O)C43)ccc2C#N)cc1F 10.1016/j.bmcl.2009.04.044
CHEMBL1783931 69485 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Negative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cellsNegative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cells
ChEMBL 506 10 3 5 4.4 Cc1ccc(CC(C)(C)NC[C@@H](O)COc2cc(C3CC4CC3C3C(C(=O)O)C43)ccc2C#N)cc1F 10.1016/j.bmcl.2009.04.044
45141171 209123 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 375 6 0 4 5.4 C=CCN(C)c1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
CHEMBL610511 209123 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 375 6 0 4 5.4 C=CCN(C)c1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
11408302 64847 1 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assay
ChEMBL 449 12 3 4 4.9 C[C@@H](OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1CCC(=O)O 10.1021/ml100268k
CHEMBL1672966 64847 1 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assay
ChEMBL 449 12 3 4 4.9 C[C@@H](OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1CCC(=O)O 10.1021/ml100268k
44405849 81812 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 461 8 2 4 5.3 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(Cl)c1C#N 10.1016/j.bmcl.2005.08.095
CHEMBL203479 81812 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 461 8 2 4 5.3 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(Cl)c1C#N 10.1016/j.bmcl.2005.08.095
44405892 172776 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 478 9 2 3 6.4 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(-c2ccccc2)c1 10.1016/j.bmcl.2005.08.095
CHEMBL425394 172776 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 478 9 2 3 6.4 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(-c2ccccc2)c1 10.1016/j.bmcl.2005.08.095
11384835 22772 1 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 427 6 0 5 5.1 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(Br)c(C#N)cc(OC)c21 10.1016/j.bmcl.2010.07.016
CHEMBL1223509 22772 1 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 427 6 0 5 5.1 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(Br)c(C#N)cc(OC)c21 10.1016/j.bmcl.2010.07.016
136059356 65564 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 434 6 2 4 5.8 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1cccc(F)c1 10.1021/jm101452x
CHEMBL1688085 65564 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 434 6 2 4 5.8 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1cccc(F)c1 10.1021/jm101452x
54585407 69487 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Negative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cellsNegative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cells
ChEMBL 509 11 3 4 5.3 Cc1ccc(CC(C)(C)NC[C@@H](O)CO[C@H](C)c2ccccc2C2CC3CC2C2C(C(=O)O)C32)cc1F 10.1016/j.bmcl.2009.04.044
CHEMBL1783933 69487 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Negative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cellsNegative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cells
ChEMBL 509 11 3 4 5.3 Cc1ccc(CC(C)(C)NC[C@@H](O)CO[C@H](C)c2ccccc2C2CC3CC2C2C(C(=O)O)C32)cc1F 10.1016/j.bmcl.2009.04.044
11849473 19628 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Activity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulationActivity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulation
ChEMBL 456 6 2 3 6.1 C[C@@H](N[C@H]1CCCC[C@@H]1NC(=O)c1ccc(OC(F)(F)F)cc1)c1cccc2ccccc12 10.1021/jm051233+
CHEMBL1188646 19628 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Activity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulationActivity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulation
ChEMBL 456 6 2 3 6.1 C[C@@H](N[C@H]1CCCC[C@@H]1NC(=O)c1ccc(OC(F)(F)F)cc1)c1cccc2ccccc12 10.1021/jm051233+
CHEMBL536975 19628 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Activity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulationActivity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulation
ChEMBL 456 6 2 3 6.1 C[C@@H](N[C@H]1CCCC[C@@H]1NC(=O)c1ccc(OC(F)(F)F)cc1)c1cccc2ccccc12 10.1021/jm051233+
136054392 192126 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CaSR in human HEK293 cells measured after 5 mins by FLIPR assayAntagonist activity at human CaSR in human HEK293 cells measured after 5 mins by FLIPR assay
ChEMBL 482 6 1 5 6.7 Cc1nc(-c2cccc(F)c2O)n(CCc2ccccc2)c(=O)c1-c1ccc(-c2ccccc2)s1 10.1021/acsmedchemlett.1c00187
CHEMBL4860070 192126 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CaSR in human HEK293 cells measured after 5 mins by FLIPR assayAntagonist activity at human CaSR in human HEK293 cells measured after 5 mins by FLIPR assay
ChEMBL 482 6 1 5 6.7 Cc1nc(-c2cccc(F)c2O)n(CCc2ccccc2)c(=O)c1-c1ccc(-c2ccccc2)s1 10.1021/acsmedchemlett.1c00187
136334632 192513 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CaSR in human HEK293 cells measured after 5 mins by FLIPR assayAntagonist activity at human CaSR in human HEK293 cells measured after 5 mins by FLIPR assay
ChEMBL 414 6 1 4 4.9 Cc1nc(-c2cccc(F)c2O)n(CCc2ccccc2)c(=O)c1Cc1ccccc1 10.1021/acsmedchemlett.1c00187
CHEMBL4866041 192513 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CaSR in human HEK293 cells measured after 5 mins by FLIPR assayAntagonist activity at human CaSR in human HEK293 cells measured after 5 mins by FLIPR assay
ChEMBL 414 6 1 4 4.9 Cc1nc(-c2cccc(F)c2O)n(CCc2ccccc2)c(=O)c1Cc1ccccc1 10.1021/acsmedchemlett.1c00187
44405873 79432 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 427 8 2 4 4.6 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1ccc(C#N)cc1 10.1016/j.bmcl.2005.08.095
CHEMBL199548 79432 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 427 8 2 4 4.6 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1ccc(C#N)cc1 10.1016/j.bmcl.2005.08.095
49865336 22677 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 334 6 0 2 6.8 CCCCn1c(-c2ccc(C(C)C)cc2)nc2c(C(C)C)cccc21 10.1016/j.bmcl.2010.07.016
CHEMBL1223221 22677 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 334 6 0 2 6.8 CCCCn1c(-c2ccc(C(C)C)cc2)nc2c(C(C)C)cccc21 10.1016/j.bmcl.2010.07.016
10094574 79417 0 None -18 2 Rat 5.6 pIC50 = 5.6 Functional
Inhibition of extracellular calcium-induced inositol triphosphate generation in rat MTC cells expressing calcium-sensing receptorInhibition of extracellular calcium-induced inositol triphosphate generation in rat MTC cells expressing calcium-sensing receptor
ChEMBL 436 8 3 4 4.6 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(F)c1O 10.1016/j.bmcl.2005.08.095
CHEMBL199495 79417 0 None -18 2 Rat 5.6 pIC50 = 5.6 Functional
Inhibition of extracellular calcium-induced inositol triphosphate generation in rat MTC cells expressing calcium-sensing receptorInhibition of extracellular calcium-induced inositol triphosphate generation in rat MTC cells expressing calcium-sensing receptor
ChEMBL 436 8 3 4 4.6 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(F)c1O 10.1016/j.bmcl.2005.08.095
49864798 22490 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 512 9 0 5 7.1 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(C(F)(F)F)c(Cc3ccccc3OC)cc(OC)c21 10.1016/j.bmcl.2010.07.016
CHEMBL1222489 22490 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 512 9 0 5 7.1 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(C(F)(F)F)c(Cc3ccccc3OC)cc(OC)c21 10.1016/j.bmcl.2010.07.016
6918446 9654 56 None 2 6 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1016/j.bmcl.2010.04.035
716 9654 56 None 2 6 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1016/j.bmcl.2010.04.035
CHEMBL180672 9654 56 None 2 6 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1016/j.bmcl.2010.04.035
DB05695 9654 56 None 2 6 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1016/j.bmcl.2010.04.035
11849440 19652 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Activity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulationActivity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulation
ChEMBL 492 7 2 4 5.7 C[C@@H](N[C@H]1CCCC[C@@H]1NS(=O)(=O)c1ccc(OC(F)(F)F)cc1)c1cccc2ccccc12 10.1021/jm051233+
CHEMBL1188810 19652 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Activity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulationActivity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulation
ChEMBL 492 7 2 4 5.7 C[C@@H](N[C@H]1CCCC[C@@H]1NS(=O)(=O)c1ccc(OC(F)(F)F)cc1)c1cccc2ccccc12 10.1021/jm051233+
CHEMBL537427 19652 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Activity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulationActivity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulation
ChEMBL 492 7 2 4 5.7 C[C@@H](N[C@H]1CCCC[C@@H]1NS(=O)(=O)c1ccc(OC(F)(F)F)cc1)c1cccc2ccccc12 10.1021/jm051233+
44405900 140241 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 407 9 2 5 3.5 COc1ccc(CC(C)(C)NC[C@@H](O)[C@H]2CCCN2Cc2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.08.095
CHEMBL370671 140241 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 407 9 2 5 3.5 COc1ccc(CC(C)(C)NC[C@@H](O)[C@H]2CCCN2Cc2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.08.095
45140790 208195 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 450 7 0 4 6.4 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1ccc(C(C)C)cc1 10.1021/jm901811v
CHEMBL604713 208195 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 450 7 0 4 6.4 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1ccc(C(C)C)cc1 10.1021/jm901811v
122636684 147880 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 503 11 3 6 4.5 CSc1ccc(CC(C)(C)NC[C@@H](O)CO[C@H](C)c2ccc(C)c3c2[C@@H]2[C@H](O3)[C@H]2C(=O)O)cc1F 10.1016/j.bmcl.2016.06.073
CHEMBL3827041 147880 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 503 11 3 6 4.5 CSc1ccc(CC(C)(C)NC[C@@H](O)CO[C@H](C)c2ccc(C)c3c2[C@@H]2[C@H](O3)[C@H]2C(=O)O)cc1F 10.1016/j.bmcl.2016.06.073
44405854 6818 0 None 186 2 Human 6.6 pIC50 = 6.6 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 433 8 2 5 4.7 N#Cc1cccc(c1)CN1CCC[C@@H]1[C@@H](CNC(Cc1cc2c(s1)cccc2)(C)C)O 10.1016/j.bmcl.2005.08.095
711 6818 0 None 186 2 Human 6.6 pIC50 = 6.6 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 433 8 2 5 4.7 N#Cc1cccc(c1)CN1CCC[C@@H]1[C@@H](CNC(Cc1cc2c(s1)cccc2)(C)C)O 10.1016/j.bmcl.2005.08.095
CHEMBL200312 6818 0 None 186 2 Human 6.6 pIC50 = 6.6 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 433 8 2 5 4.7 N#Cc1cccc(c1)CN1CCC[C@@H]1[C@@H](CNC(Cc1cc2c(s1)cccc2)(C)C)O 10.1016/j.bmcl.2005.08.095
44405890 140300 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 422 8 1 4 5.1 CN(C[C@@H](O)COc1cccc(Cl)c1C#N)C(C)(C)Cc1ccc2ccccc2c1 10.1016/j.bmcl.2005.08.095
CHEMBL370811 140300 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 422 8 1 4 5.1 CN(C[C@@H](O)COc1cccc(Cl)c1C#N)C(C)(C)Cc1ccc2ccccc2c1 10.1016/j.bmcl.2005.08.095
45140006 207336 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 364 5 0 4 5.6 CC(C)Oc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
CHEMBL599025 207336 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 364 5 0 4 5.6 CC(C)Oc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
122636663 147942 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 467 12 3 5 4.4 Cc1ccc([C@@H](C)OC[C@H](O)CNC(C)(C)CCCc2ccccc2)c2c1O[C@@H]1[C@@H](C(=O)O)[C@H]21 10.1016/j.bmcl.2016.06.073
CHEMBL3827830 147942 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 467 12 3 5 4.4 Cc1ccc([C@@H](C)OC[C@H](O)CNC(C)(C)CCCc2ccccc2)c2c1O[C@@H]1[C@@H](C(=O)O)[C@H]21 10.1016/j.bmcl.2016.06.073
25218713 200014 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 558 14 2 9 4.6 COc1ccc(CCNc2ncc(C(=O)NCCOc3ccccc3)c(-c3cc(OC)c(OC)c(OC)c3)n2)cc1 10.1021/jm801178c
CHEMBL523701 200014 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 558 14 2 9 4.6 COc1ccc(CCNc2ncc(C(=O)NCCOc3ccccc3)c(-c3cc(OC)c(OC)c(OC)c3)n2)cc1 10.1021/jm801178c
44405899 148128 1 None - 1 Human 5.6 pIC50 = 5.6 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 417 8 3 5 3.4 CC(C)(Cc1nc2ccccc2[nH]1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(C#N)c1 10.1016/j.bmcl.2005.08.095
CHEMBL383609 148128 1 None - 1 Human 5.6 pIC50 = 5.6 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 417 8 3 5 3.4 CC(C)(Cc1nc2ccccc2[nH]1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(C#N)c1 10.1016/j.bmcl.2005.08.095
45140974 207337 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 405 8 0 4 6.4 CCCN(CCC)c1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
CHEMBL599039 207337 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 405 8 0 4 6.4 CCCN(CCC)c1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
136030677 65571 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 468 4 2 4 5.5 O=C(NCc1ccc(C(F)(F)F)cc1)c1cnn2c1N[C@H](c1ccccc1)C[C@@H]2C(F)(F)F 10.1021/jm101452x
CHEMBL1688101 65571 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 468 4 2 4 5.5 O=C(NCc1ccc(C(F)(F)F)cc1)c1cnn2c1N[C@H](c1ccccc1)C[C@@H]2C(F)(F)F 10.1021/jm101452x
136188836 66970 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 474 8 2 5 6.3 CCOc1ccc(C(CC)(CC)NC(=O)c2c(C)nn3c2N[C@@H](c2ccccc2)CC3(C)C)cc1 10.1016/j.bmc.2011.02.001
CHEMBL1689053 66970 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 474 8 2 5 6.3 CCOc1ccc(C(CC)(CC)NC(=O)c2c(C)nn3c2N[C@@H](c2ccccc2)CC3(C)C)cc1 10.1016/j.bmc.2011.02.001
CHEMBL1739920 66970 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 474 8 2 5 6.3 CCOc1ccc(C(CC)(CC)NC(=O)c2c(C)nn3c2N[C@@H](c2ccccc2)CC3(C)C)cc1 10.1016/j.bmc.2011.02.001
45140970 207058 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 482 9 1 6 4.7 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1cccc(OCC(=O)O)c1 10.1021/jm901811v
CHEMBL597194 207058 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 482 9 1 6 4.7 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1cccc(OCC(=O)O)c1 10.1021/jm901811v
136059346 65760 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 416 6 2 4 5.6 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccccc1 10.1021/jm101452x
CHEMBL1689815 65760 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 416 6 2 4 5.6 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccccc1 10.1021/jm101452x
136030614 65754 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 456 4 2 4 5.9 CC(C)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C(F)(F)F)cc1 10.1021/jm101452x
CHEMBL1689809 65754 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 456 4 2 4 5.9 CC(C)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C(F)(F)F)cc1 10.1021/jm101452x
45141389 207269 1 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 410 6 1 4 5.7 C=CCc1c(O)ccc2c1c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1ccccc1 10.1021/jm901811v
CHEMBL598638 207269 1 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 410 6 1 4 5.7 C=CCc1c(O)ccc2c1c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1ccccc1 10.1021/jm901811v
45141172 207146 39 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 359 5 1 4 4.8 C#CCNc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
CHEMBL597811 207146 39 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 359 5 1 4 4.8 C#CCNc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
136059343 65758 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 512 6 2 4 7.1 CC(C)C(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)(c1ccc(C(F)(F)F)cc1)C(C)C 10.1021/jm101452x
CHEMBL1689813 65758 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 512 6 2 4 7.1 CC(C)C(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)(c1ccc(C(F)(F)F)cc1)C(C)C 10.1021/jm101452x
44405840 147907 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 374 8 2 4 4.1 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COc1ccccc1C#N 10.1016/j.bmcl.2005.08.095
CHEMBL382741 147907 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 374 8 2 4 4.1 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COc1ccccc1C#N 10.1016/j.bmcl.2005.08.095
5307 8387 29 None 1 2 Rat 7.5 pIC50 = 7.5 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
ChEMBL 374 6 2 3 4.4 OC(=O)Cc1ccc(cc1)N1CC[C@@H](C1)N[C@@H](c1cccc2c1cccc2)C 10.1016/j.bmcl.2018.04.055
71242808 8387 29 None 1 2 Rat 7.5 pIC50 = 7.5 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
ChEMBL 374 6 2 3 4.4 OC(=O)Cc1ccc(cc1)N1CC[C@@H](C1)N[C@@H](c1cccc2c1cccc2)C 10.1016/j.bmcl.2018.04.055
9042 8387 29 None 1 2 Rat 7.5 pIC50 = 7.5 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
ChEMBL 374 6 2 3 4.4 OC(=O)Cc1ccc(cc1)N1CC[C@@H](C1)N[C@@H](c1cccc2c1cccc2)C 10.1016/j.bmcl.2018.04.055
CHEMBL4297621 8387 29 None 1 2 Rat 7.5 pIC50 = 7.5 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
ChEMBL 374 6 2 3 4.4 OC(=O)Cc1ccc(cc1)N1CC[C@@H](C1)N[C@@H](c1cccc2c1cccc2)C 10.1016/j.bmcl.2018.04.055
DB12388 8387 29 None 1 2 Rat 7.5 pIC50 = 7.5 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
ChEMBL 374 6 2 3 4.4 OC(=O)Cc1ccc(cc1)N1CC[C@@H](C1)N[C@@H](c1cccc2c1cccc2)C 10.1016/j.bmcl.2018.04.055
46891321 13597 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 405 11 2 3 5.3 CC(CCOC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1 10.1016/j.bmcl.2010.04.035
CHEMBL1083951 13597 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 405 11 2 3 5.3 CC(CCOC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1 10.1016/j.bmcl.2010.04.035
54587337 69416 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Negative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cellsNegative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cells
ChEMBL 499 10 3 4 4.7 Cc1ccc(CC(C)(C)NC[C@@H](O)COc2cc(C3CC4CC3C3C(C(=O)O)C43)ccc2F)cc1F 10.1016/j.bmcl.2009.04.044
CHEMBL1783766 69416 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Negative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cellsNegative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cells
ChEMBL 499 10 3 4 4.7 Cc1ccc(CC(C)(C)NC[C@@H](O)COc2cc(C3CC4CC3C3C(C(=O)O)C43)ccc2F)cc1F 10.1016/j.bmcl.2009.04.044
136071244 66938 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 444 6 2 4 6.2 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@H](c1ccccc1)CC2(C)C)c1ccc(C)cc1 10.1016/j.bmc.2011.02.001
CHEMBL1689048 66938 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 444 6 2 4 6.2 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@H](c1ccccc1)CC2(C)C)c1ccc(C)cc1 10.1016/j.bmc.2011.02.001
CHEMBL1739734 66938 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 444 6 2 4 6.2 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@H](c1ccccc1)CC2(C)C)c1ccc(C)cc1 10.1016/j.bmc.2011.02.001
136059376 65569 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 474 7 2 6 5.5 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(OC(C)=O)cc1 10.1021/jm101452x
CHEMBL1688091 65569 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 474 7 2 6 5.5 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(OC(C)=O)cc1 10.1021/jm101452x
136059372 66952 1 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 430 6 2 4 5.9 CCC(CC)(NC(=O)c1cnn2c1N[C@H](c1ccccc1)CC2(C)C)c1ccc(C)cc1 10.1021/jm101452x
CHEMBL1688100 66952 1 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 430 6 2 4 5.9 CCC(CC)(NC(=O)c1cnn2c1N[C@H](c1ccccc1)CC2(C)C)c1ccc(C)cc1 10.1021/jm101452x
CHEMBL1739781 66952 1 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 430 6 2 4 5.9 CCC(CC)(NC(=O)c1cnn2c1N[C@H](c1ccccc1)CC2(C)C)c1ccc(C)cc1 10.1021/jm101452x
58973555 174312 0 None 19 2 Rat 7.5 pIC50 = 7.5 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
ChEMBL 414 5 1 3 6.1 C[C@@H](N[C@H]1CCCN(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4130093 174312 0 None 19 2 Rat 7.5 pIC50 = 7.5 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
ChEMBL 414 5 1 3 6.1 C[C@@H](N[C@H]1CCCN(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4300172 174312 0 None 19 2 Rat 7.5 pIC50 = 7.5 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
ChEMBL 414 5 1 3 6.1 C[C@@H](N[C@H]1CCCN(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
46890830 13913 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 417 10 2 3 5.6 Cc1ccccc1[C@H](OC[C@@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)C1CC1 10.1016/j.bmcl.2010.04.035
CHEMBL1085334 13913 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 417 10 2 3 5.6 Cc1ccccc1[C@H](OC[C@@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)C1CC1 10.1016/j.bmcl.2010.04.035
25218704 200010 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 544 13 2 9 4.6 COc1ccc(CNc2ncc(C(=O)NCCOc3ccccc3)c(-c3cc(OC)c(OC)c(OC)c3)n2)cc1 10.1021/jm801178c
CHEMBL523682 200010 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 544 13 2 9 4.6 COc1ccc(CNc2ncc(C(=O)NCCOc3ccccc3)c(-c3cc(OC)c(OC)c(OC)c3)n2)cc1 10.1021/jm801178c
136032598 25954 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation counting
ChEMBL 478 3 2 4 5.9 O=C(NC12CC3CC(CC(C3)C1)C2)c1cnn2c1N[C@H](c1cccc(Cl)c1)C[C@@H]2C(F)(F)F 10.1016/j.bmc.2010.10.035
CHEMBL1289679 25954 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation counting
ChEMBL 478 3 2 4 5.9 O=C(NC12CC3CC(CC(C3)C1)C2)c1cnn2c1N[C@H](c1cccc(Cl)c1)C[C@@H]2C(F)(F)F 10.1016/j.bmc.2010.10.035
136071531 65690 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 474 7 3 5 5.6 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(C(=O)O)cc1 10.1016/j.bmc.2011.02.001
CHEMBL1689061 65690 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 474 7 3 5 5.6 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(C(=O)O)cc1 10.1016/j.bmc.2011.02.001
10345214 10142 13 None -1 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulator activity at rat calcium sensing receptor expressed in HEK cellsNegative allosteric modulator activity at rat calcium sensing receptor expressed in HEK cells
ChEMBL 447 11 3 4 3.9 O[C@@H](COc1cc(CCC(=O)O)cc(c1F)F)CNC(CC1Cc2c(C1)cccc2)(C)C 10.1016/j.bmcl.2009.04.044
9473 10142 13 None -1 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulator activity at rat calcium sensing receptor expressed in HEK cellsNegative allosteric modulator activity at rat calcium sensing receptor expressed in HEK cells
ChEMBL 447 11 3 4 3.9 O[C@@H](COc1cc(CCC(=O)O)cc(c1F)F)CNC(CC1Cc2c(C1)cccc2)(C)C 10.1016/j.bmcl.2009.04.044
CHEMBL1198855 10142 13 None -1 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulator activity at rat calcium sensing receptor expressed in HEK cellsNegative allosteric modulator activity at rat calcium sensing receptor expressed in HEK cells
ChEMBL 447 11 3 4 3.9 O[C@@H](COc1cc(CCC(=O)O)cc(c1F)F)CNC(CC1Cc2c(C1)cccc2)(C)C 10.1016/j.bmcl.2009.04.044
DB05255 10142 13 None -1 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulator activity at rat calcium sensing receptor expressed in HEK cellsNegative allosteric modulator activity at rat calcium sensing receptor expressed in HEK cells
ChEMBL 447 11 3 4 3.9 O[C@@H](COc1cc(CCC(=O)O)cc(c1F)F)CNC(CC1Cc2c(C1)cccc2)(C)C 10.1016/j.bmcl.2009.04.044
44414943 19674 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Activity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulationActivity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulation
ChEMBL 440 5 2 2 6.5 C[C@@H](N[C@H]1CCCC[C@@H]1NC(=O)c1ccc(Cl)c(Cl)c1)c1cccc2ccccc12 10.1021/jm051233+
CHEMBL1188986 19674 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Activity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulationActivity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulation
ChEMBL 440 5 2 2 6.5 C[C@@H](N[C@H]1CCCC[C@@H]1NC(=O)c1ccc(Cl)c(Cl)c1)c1cccc2ccccc12 10.1021/jm051233+
CHEMBL537870 19674 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Activity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulationActivity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulation
ChEMBL 440 5 2 2 6.5 C[C@@H](N[C@H]1CCCC[C@@H]1NC(=O)c1ccc(Cl)c(Cl)c1)c1cccc2ccccc12 10.1021/jm051233+
45139808 207443 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 334 4 0 4 4.5 COc1ccc2c(c1)c(-c1ccc(C3CC3)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
CHEMBL599665 207443 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 334 4 0 4 4.5 COc1ccc2c(c1)c(-c1ccc(C3CC3)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
44405902 79820 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 401 9 2 4 4.1 CC(C)(Cc1ccc(F)cc1)NC[C@@H](O)COc1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2005.08.095
CHEMBL201065 79820 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 401 9 2 4 4.1 CC(C)(Cc1ccc(F)cc1)NC[C@@H](O)COc1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2005.08.095
25218705 194124 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 544 13 2 9 4.6 COc1cccc(CNc2ncc(C(=O)NCCOc3ccccc3)c(-c3cc(OC)c(OC)c(OC)c3)n2)c1 10.1021/jm801178c
CHEMBL493228 194124 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 544 13 2 9 4.6 COc1cccc(CNc2ncc(C(=O)NCCOc3ccccc3)c(-c3cc(OC)c(OC)c(OC)c3)n2)c1 10.1021/jm801178c
25218711 194316 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 558 14 2 9 4.6 COc1ccccc1CCNc1ncc(C(=O)NCCOc2ccccc2)c(-c2cc(OC)c(OC)c(OC)c2)n1 10.1021/jm801178c
CHEMBL494442 194316 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 558 14 2 9 4.6 COc1ccccc1CCNc1ncc(C(=O)NCCOc2ccccc2)c(-c2cc(OC)c(OC)c(OC)c2)n1 10.1021/jm801178c
49864799 22492 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 520 8 0 4 7.5 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(Br)c(Cc3ccc(C)c(C)c3)cc(OC)c21 10.1016/j.bmcl.2010.07.016
CHEMBL1222491 22492 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 520 8 0 4 7.5 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(Br)c(Cc3ccc(C)c(C)c3)cc(OC)c21 10.1016/j.bmcl.2010.07.016
44405856 79662 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 427 8 2 4 4.6 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1ccccc1C#N 10.1016/j.bmcl.2005.08.095
CHEMBL200361 79662 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 427 8 2 4 4.6 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1ccccc1C#N 10.1016/j.bmcl.2005.08.095
135513459 192062 0 None 1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CaSR in human HEK293 cells measured after 5 mins by FLIPR assayAntagonist activity at human CaSR in human HEK293 cells measured after 5 mins by FLIPR assay
ChEMBL 420 5 1 5 5.3 Cc1ccc(-c2c(C)nc(-c3cccc(F)c3O)n(CCc3ccccc3)c2=O)s1 10.1021/acsmedchemlett.1c00187
CHEMBL4859029 192062 0 None 1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CaSR in human HEK293 cells measured after 5 mins by FLIPR assayAntagonist activity at human CaSR in human HEK293 cells measured after 5 mins by FLIPR assay
ChEMBL 420 5 1 5 5.3 Cc1ccc(-c2c(C)nc(-c3cccc(F)c3O)n(CCc3ccccc3)c2=O)s1 10.1021/acsmedchemlett.1c00187
54583478 69486 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Negative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cellsNegative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cells
ChEMBL 529 10 3 6 3.4 CC(C)(CN1Cc2ccccc2C1=O)NC[C@@H](O)COc1cc(C2CC3CC2C2C(C(=O)O)C32)ccc1C#N 10.1016/j.bmcl.2009.04.044
CHEMBL1783932 69486 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Negative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cellsNegative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cells
ChEMBL 529 10 3 6 3.4 CC(C)(CN1Cc2ccccc2C1=O)NC[C@@H](O)COc1cc(C2CC3CC2C2C(C(=O)O)C32)ccc1C#N 10.1016/j.bmcl.2009.04.044
54587336 69415 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Negative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cellsNegative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cells
ChEMBL 481 10 3 4 4.6 Cc1ccc(CC(C)(C)NC[C@@H](O)COc2cccc(C3CC4CC3C3C(C(=O)O)C43)c2)cc1F 10.1016/j.bmcl.2009.04.044
CHEMBL1783765 69415 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Negative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cellsNegative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cells
ChEMBL 481 10 3 4 4.6 Cc1ccc(CC(C)(C)NC[C@@H](O)COc2cccc(C3CC4CC3C3C(C(=O)O)C43)c2)cc1F 10.1016/j.bmcl.2009.04.044
54583479 69490 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Negative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cellsNegative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cells
ChEMBL 517 11 3 4 5.4 C[C@@H](OC[C@H](O)CNC(C)(C)CC1Cc2ccccc2C1)c1ccccc1C1CC2CC1C1C(C(=O)O)C21 10.1016/j.bmcl.2009.04.044
CHEMBL1783936 69490 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Negative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cellsNegative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cells
ChEMBL 517 11 3 4 5.4 C[C@@H](OC[C@H](O)CNC(C)(C)CC1Cc2ccccc2C1)c1ccccc1C1CC2CC1C1C(C(=O)O)C21 10.1016/j.bmcl.2009.04.044
25218730 182613 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 525 7 1 9 4.1 COc1ccc(-c2nc(NCc3ccc4c(c3)OCO4)ncc2C(=O)N2CCc3ccccc3C2)c(OC)n1 10.1021/jm801178c
CHEMBL458515 182613 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 525 7 1 9 4.1 COc1ccc(-c2nc(NCc3ccc4c(c3)OCO4)ncc2C(=O)N2CCc3ccccc3C2)c(OC)n1 10.1021/jm801178c
25218728 183785 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 513 12 1 8 4.4 CCN(Cc1ccccc1)c1ncc(C(=O)NCCOc2ccccc2)c(-c2ccc(OC)nc2OC)n1 10.1021/jm801178c
CHEMBL462661 183785 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 513 12 1 8 4.4 CCN(Cc1ccccc1)c1ncc(C(=O)NCCOc2ccccc2)c(-c2ccc(OC)nc2OC)n1 10.1021/jm801178c
49864756 22476 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 392 6 0 4 5.5 COCCn1c(-c2ccc(C(C)C)cc2)nc2cc(C(F)(F)F)cc(OC)c21 10.1016/j.bmcl.2010.07.016
CHEMBL1222425 22476 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 392 6 0 4 5.5 COCCn1c(-c2ccc(C(C)C)cc2)nc2cc(C(F)(F)F)cc(OC)c21 10.1016/j.bmcl.2010.07.016
46891363 13267 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 427 9 2 3 6.0 CC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1cccc2ccccc12 10.1016/j.bmcl.2010.04.035
CHEMBL1082710 13267 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 427 9 2 3 6.0 CC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1cccc2ccccc12 10.1016/j.bmcl.2010.04.035
44405855 79747 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 438 8 2 3 5.1 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(F)c1F 10.1016/j.bmcl.2005.08.095
CHEMBL200690 79747 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 438 8 2 3 5.1 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(F)c1F 10.1016/j.bmcl.2005.08.095
10180249 13293 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 417 10 2 3 5.6 Cc1ccccc1C(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)C1CC1 10.1016/j.bmcl.2010.04.035
CHEMBL1082788 13293 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 417 10 2 3 5.6 Cc1ccccc1C(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)C1CC1 10.1016/j.bmcl.2010.04.035
45140210 207378 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 378 7 0 4 5.9 CCCCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
CHEMBL599227 207378 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 378 7 0 4 5.9 CCCCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
136188834 65572 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 476 5 2 4 6.1 O=C(NC(c1ccccc1)c1ccccc1)c1cnn2c1N[C@H](c1ccccc1)C[C@@H]2C(F)(F)F 10.1021/jm101452x
CHEMBL1688102 65572 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 476 5 2 4 6.1 O=C(NC(c1ccccc1)c1ccccc1)c1cnn2c1N[C@H](c1ccccc1)C[C@@H]2C(F)(F)F 10.1021/jm101452x
44405917 142211 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 380 8 2 4 3.9 N#Cc1c(Cl)cccc1OC[C@H](O)CNCCc1ccc2ccccc2c1 10.1016/j.bmcl.2005.08.095
CHEMBL372821 142211 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 380 8 2 4 3.9 N#Cc1c(Cl)cccc1OC[C@H](O)CNCCc1ccc2ccccc2c1 10.1016/j.bmcl.2005.08.095
122636704 147892 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 485 11 3 6 4.3 CSc1ccc(CC(C)(C)NC[C@@H](O)CO[C@H](C)c2ccc(C)c3c2[C@@H]2[C@H](O3)[C@H]2C(=O)O)cc1 10.1016/j.bmcl.2016.06.073
CHEMBL3827209 147892 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 485 11 3 6 4.3 CSc1ccc(CC(C)(C)NC[C@@H](O)CO[C@H](C)c2ccc(C)c3c2[C@@H]2[C@H](O3)[C@H]2C(=O)O)cc1 10.1016/j.bmcl.2016.06.073
24753709 22817 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 513 9 0 6 6.5 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(C(F)(F)F)c(Cc3cccnc3OC)cc(OC)c21 10.1016/j.bmcl.2010.07.016
CHEMBL1223712 22817 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 513 9 0 6 6.5 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(C(F)(F)F)c(Cc3cccnc3OC)cc(OC)c21 10.1016/j.bmcl.2010.07.016
24753618 22818 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 539 9 0 6 7.0 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(Br)c(Cc3cccnc3SC)cc(OC)c21 10.1016/j.bmcl.2010.07.016
CHEMBL1223713 22818 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 539 9 0 6 7.0 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(Br)c(Cc3cccnc3SC)cc(OC)c21 10.1016/j.bmcl.2010.07.016
51346981 64851 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assay
ChEMBL 497 11 3 4 6.3 C[C@@H](OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1-c1ccc(C(=O)O)cc1 10.1021/ml100268k
CHEMBL1672970 64851 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assay
ChEMBL 497 11 3 4 6.3 C[C@@H](OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1-c1ccc(C(=O)O)cc1 10.1021/ml100268k
135434106 66964 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 444 6 2 4 6.2 CCC(CC)(NC(=O)c1c(C)nn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C)cc1 10.1016/j.bmc.2011.02.001
CHEMBL1689040 66964 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 444 6 2 4 6.2 CCC(CC)(NC(=O)c1c(C)nn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C)cc1 10.1016/j.bmc.2011.02.001
CHEMBL1739914 66964 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 444 6 2 4 6.2 CCC(CC)(NC(=O)c1c(C)nn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C)cc1 10.1016/j.bmc.2011.02.001
135565656 66967 1 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 458 7 2 4 6.5 CCc1ccc(C(CC)(CC)NC(=O)c2c(C)nn3c2N[C@@H](c2ccccc2)CC3(C)C)cc1 10.1016/j.bmc.2011.02.001
CHEMBL1689050 66967 1 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 458 7 2 4 6.5 CCc1ccc(C(CC)(CC)NC(=O)c2c(C)nn3c2N[C@@H](c2ccccc2)CC3(C)C)cc1 10.1016/j.bmc.2011.02.001
CHEMBL1689060 66967 1 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 458 7 2 4 6.5 CCc1ccc(C(CC)(CC)NC(=O)c2c(C)nn3c2N[C@@H](c2ccccc2)CC3(C)C)cc1 10.1016/j.bmc.2011.02.001
CHEMBL1739917 66967 1 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 458 7 2 4 6.5 CCc1ccc(C(CC)(CC)NC(=O)c2c(C)nn3c2N[C@@H](c2ccccc2)CC3(C)C)cc1 10.1016/j.bmc.2011.02.001
45140596 207087 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 436 7 0 4 5.8 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1ccc(CC)cc1 10.1021/jm901811v
CHEMBL597400 207087 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 436 7 0 4 5.8 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1ccc(CC)cc1 10.1021/jm901811v
45140791 207088 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 438 7 0 5 5.3 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1ccc(OC)cc1 10.1021/jm901811v
CHEMBL597401 207088 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 438 7 0 5 5.3 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1ccc(OC)cc1 10.1021/jm901811v
145946257 174302 0 None 74 2 Rat 8.4 pIC50 = 8.4 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
ChEMBL 400 5 1 3 5.7 C[C@@H](N[C@@H]1CCN(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4126057 174302 0 None 74 2 Rat 8.4 pIC50 = 8.4 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
ChEMBL 400 5 1 3 5.7 C[C@@H](N[C@@H]1CCN(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4300082 174302 0 None 74 2 Rat 8.4 pIC50 = 8.4 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
ChEMBL 400 5 1 3 5.7 C[C@@H](N[C@@H]1CCN(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
10158373 7301 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 408 6 0 4 5.2 C#CCOc1ccc2c(c1)c(nc(=O)n2Cc1ccccc1)c1ccc(cc1)C(C)C 10.1021/jm901811v
9475 7301 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 408 6 0 4 5.2 C#CCOc1ccc2c(c1)c(nc(=O)n2Cc1ccccc1)c1ccc(cc1)C(C)C 10.1021/jm901811v
CHEMBL591475 7301 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 408 6 0 4 5.2 C#CCOc1ccc2c(c1)c(nc(=O)n2Cc1ccccc1)c1ccc(cc1)C(C)C 10.1021/jm901811v
136059341 65756 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 512 8 2 4 7.4 CCCC(CCC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C(F)(F)F)cc1 10.1021/jm101452x
CHEMBL1689811 65756 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 512 8 2 4 7.4 CCCC(CCC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C(F)(F)F)cc1 10.1021/jm101452x
136030755 66971 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 478 7 2 5 6.1 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(OC)c(F)c1 10.1016/j.bmc.2011.02.001
CHEMBL1689058 66971 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 478 7 2 5 6.1 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(OC)c(F)c1 10.1016/j.bmc.2011.02.001
CHEMBL1739921 66971 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 478 7 2 5 6.1 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(OC)c(F)c1 10.1016/j.bmc.2011.02.001
136071254 66936 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 476 7 2 5 6.7 CCC(CC)(NC(=O)c1c(SC)nn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C)cc1 10.1016/j.bmc.2011.02.001
CHEMBL1689046 66936 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 476 7 2 5 6.7 CCC(CC)(NC(=O)c1c(SC)nn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C)cc1 10.1016/j.bmc.2011.02.001
CHEMBL1739732 66936 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 476 7 2 5 6.7 CCC(CC)(NC(=O)c1c(SC)nn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C)cc1 10.1016/j.bmc.2011.02.001
136188838 65691 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 472 7 2 5 6.1 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(C(C)=O)cc1 10.1016/j.bmc.2011.02.001
CHEMBL1689062 65691 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 472 7 2 5 6.1 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(C(C)=O)cc1 10.1016/j.bmc.2011.02.001
135464340 65562 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 430 6 2 4 5.9 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C)cc1 10.1021/jm101452x
CHEMBL1687946 65562 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 430 6 2 4 5.9 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C)cc1 10.1021/jm101452x
CHEMBL1688097 65562 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 430 6 2 4 5.9 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C)cc1 10.1021/jm101452x
135903547 25899 1 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation counting
ChEMBL 444 3 2 4 5.2 O=C(NC12CC3CC(CC(C3)C1)C2)c1cnn2c1N[C@H](c1ccccc1)C[C@@H]2C(F)(F)F 10.1016/j.bmc.2010.10.035
CHEMBL1289345 25899 1 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation counting
ChEMBL 444 3 2 4 5.2 O=C(NC12CC3CC(CC(C3)C1)C2)c1cnn2c1N[C@H](c1ccccc1)C[C@@H]2C(F)(F)F 10.1016/j.bmc.2010.10.035
135903547 25899 1 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 444 3 2 4 5.2 O=C(NC12CC3CC(CC(C3)C1)C2)c1cnn2c1N[C@H](c1ccccc1)C[C@@H]2C(F)(F)F 10.1021/jm101452x
CHEMBL1289345 25899 1 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 444 3 2 4 5.2 O=C(NC12CC3CC(CC(C3)C1)C2)c1cnn2c1N[C@H](c1ccccc1)C[C@@H]2C(F)(F)F 10.1021/jm101452x
136199397 25981 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation counting
ChEMBL 434 3 2 5 4.8 O=C(NC12CC3CC(CC(C3)C1)C2)c1cnn2c1N[C@H](c1ccco1)C[C@@H]2C(F)(F)F 10.1016/j.bmc.2010.10.035
CHEMBL1289892 25981 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation counting
ChEMBL 434 3 2 5 4.8 O=C(NC12CC3CC(CC(C3)C1)C2)c1cnn2c1N[C@H](c1ccco1)C[C@@H]2C(F)(F)F 10.1016/j.bmc.2010.10.035
25218709 194361 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 528 13 2 8 4.6 COc1cc(-c2nc(NCCc3ccccc3)ncc2C(=O)NCCOc2ccccc2)cc(OC)c1OC 10.1021/jm801178c
CHEMBL494647 194361 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 528 13 2 8 4.6 COc1cc(-c2nc(NCCc3ccccc3)ncc2C(=O)NCCOc2ccccc2)cc(OC)c1OC 10.1021/jm801178c
10113741 14125 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 433 11 2 4 5.3 COc1ccccc1C(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)C1CC1 10.1016/j.bmcl.2010.04.035
CHEMBL1086281 14125 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 433 11 2 4 5.3 COc1ccccc1C(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)C1CC1 10.1016/j.bmcl.2010.04.035
46891322 14162 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 378 9 2 4 4.3 CC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccn1 10.1016/j.bmcl.2010.04.035
CHEMBL1086472 14162 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 378 9 2 4 4.3 CC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccn1 10.1016/j.bmcl.2010.04.035
11786197 22491 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 552 10 0 6 6.9 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(Br)c(Cc3ccc(OC)c(OC)c3)cc(OC)c21 10.1016/j.bmcl.2010.07.016
CHEMBL1222490 22491 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 552 10 0 6 6.9 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(Br)c(Cc3ccc(OC)c(OC)c3)cc(OC)c21 10.1016/j.bmcl.2010.07.016
46891320 13596 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 391 10 2 3 4.8 CC(Cc1ccccc1)OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1 10.1016/j.bmcl.2010.04.035
CHEMBL1083950 13596 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 391 10 2 3 4.8 CC(Cc1ccccc1)OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1 10.1016/j.bmcl.2010.04.035
44405839 201548 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 416 8 3 4 4.0 CC(C)(Cc1cc2ccccc2[nH]1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(C#N)c1 10.1016/j.bmcl.2005.08.095
CHEMBL538155 201548 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 416 8 3 4 4.0 CC(C)(Cc1cc2ccccc2[nH]1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(C#N)c1 10.1016/j.bmcl.2005.08.095
136141563 66935 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 520 8 2 4 7.5 CCC(CC)(NC(=O)c1c(Cc2ccccc2)nn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C)cc1 10.1016/j.bmc.2011.02.001
CHEMBL1689045 66935 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 520 8 2 4 7.5 CCC(CC)(NC(=O)c1c(Cc2ccccc2)nn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C)cc1 10.1016/j.bmc.2011.02.001
CHEMBL1739731 66935 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 520 8 2 4 7.5 CCC(CC)(NC(=O)c1c(Cc2ccccc2)nn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C)cc1 10.1016/j.bmc.2011.02.001
122636593 147967 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 479 10 3 5 4.2 Cc1ccc([C@@H](C)OC[C@H](O)CNC(C)(C)CC2Cc3ccccc3C2)c2c1O[C@@H]1[C@H]2[C@H]1C(=O)O 10.1016/j.bmcl.2016.06.073
CHEMBL3828154 147967 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 479 10 3 5 4.2 Cc1ccc([C@@H](C)OC[C@H](O)CNC(C)(C)CC2Cc3ccccc3C2)c2c1O[C@@H]1[C@H]2[C@H]1C(=O)O 10.1016/j.bmcl.2016.06.073
122636607 147908 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 490 10 3 6 4.2 Cc1ccc([C@@H](C)OC[C@H](O)CNC(C)(C)Cc2ccc3ncccc3c2)c2c1O[C@@H]1[C@@H](C(=O)O)[C@H]21 10.1016/j.bmcl.2016.06.073
CHEMBL3827410 147908 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 490 10 3 6 4.2 Cc1ccc([C@@H](C)OC[C@H](O)CNC(C)(C)Cc2ccc3ncccc3c2)c2c1O[C@@H]1[C@@H](C(=O)O)[C@H]21 10.1016/j.bmcl.2016.06.073
6918446 9654 56 None -30 6 Rat 6.3 pIC50 = 6.3 Functional
Activity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulationActivity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulation
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1021/jm051233+
716 9654 56 None -30 6 Rat 6.3 pIC50 = 6.3 Functional
Activity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulationActivity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulation
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1021/jm051233+
CHEMBL180672 9654 56 None -30 6 Rat 6.3 pIC50 = 6.3 Functional
Activity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulationActivity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulation
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1021/jm051233+
DB05695 9654 56 None -30 6 Rat 6.3 pIC50 = 6.3 Functional
Activity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulationActivity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulation
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1021/jm051233+
45140971 206008 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 349 5 1 4 5.2 CCNc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
CHEMBL589977 206008 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 349 5 1 4 5.2 CCNc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
44405912 79683 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 352 6 2 4 4.2 N#Cc1c(Cl)cccc1OC[C@H](O)CNc1ccc2ccccc2c1 10.1016/j.bmcl.2005.08.095
CHEMBL200423 79683 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 352 6 2 4 4.2 N#Cc1c(Cl)cccc1OC[C@H](O)CNc1ccc2ccccc2c1 10.1016/j.bmcl.2005.08.095
49865389 22708 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 322 6 0 3 5.6 CCCCn1c(-c2ccc(C(C)C)cc2)nc2c(OC)cccc21 10.1016/j.bmcl.2010.07.016
CHEMBL1223298 22708 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 322 6 0 3 5.6 CCCCn1c(-c2ccc(C(C)C)cc2)nc2c(OC)cccc21 10.1016/j.bmcl.2010.07.016
25218701 195912 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 528 12 1 8 4.6 COc1cc(-c2nc(N(C)Cc3ccccc3)ncc2C(=O)NCCOc2ccccc2)cc(OC)c1OC 10.1021/jm801178c
CHEMBL510598 195912 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 528 12 1 8 4.6 COc1cc(-c2nc(N(C)Cc3ccccc3)ncc2C(=O)NCCOc2ccccc2)cc(OC)c1OC 10.1021/jm801178c
122636757 147910 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 451 9 2 5 3.7 Cc1ccc([C@@H](C)OC[C@H](O)CN2CCCC2Cc2ccccc2)c2c1O[C@@H]1[C@@H](C(=O)O)[C@H]21 10.1016/j.bmcl.2016.06.073
CHEMBL3827473 147910 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 451 9 2 5 3.7 Cc1ccc([C@@H](C)OC[C@H](O)CN2CCCC2Cc2ccccc2)c2c1O[C@@H]1[C@@H](C(=O)O)[C@H]21 10.1016/j.bmcl.2016.06.073
25218702 180743 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 548 12 2 8 5.2 COc1cc(-c2nc(NCc3ccccc3Cl)ncc2C(=O)NCCOc2ccccc2)cc(OC)c1OC 10.1021/jm801178c
CHEMBL454158 180743 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 548 12 2 8 5.2 COc1cc(-c2nc(NCc3ccccc3Cl)ncc2C(=O)NCCOc2ccccc2)cc(OC)c1OC 10.1021/jm801178c
11488770 22478 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 492 8 0 4 6.8 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(Br)c(Cc3ccccc3)cc(OC)c21 10.1016/j.bmcl.2010.07.016
CHEMBL1222427 22478 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 492 8 0 4 6.8 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(Br)c(Cc3ccccc3)cc(OC)c21 10.1016/j.bmcl.2010.07.016
11398805 22493 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 554 9 0 5 6.6 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(Br)c(Cc3ccccc3[S+](C)[O-])cc(OC)c21 10.1016/j.bmcl.2010.07.016
CHEMBL1222492 22493 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 554 9 0 5 6.6 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(Br)c(Cc3ccccc3[S+](C)[O-])cc(OC)c21 10.1016/j.bmcl.2010.07.016
51347014 64853 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assay
ChEMBL 511 11 3 4 6.6 Cc1cc(-c2ccccc2[C@@H](C)OC[C@H](O)CNC(C)(C)Cc2ccc3ccccc3c2)ccc1C(=O)O 10.1021/ml100268k
CHEMBL1672972 64853 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assay
ChEMBL 511 11 3 4 6.6 Cc1cc(-c2ccccc2[C@@H](C)OC[C@H](O)CNC(C)(C)Cc2ccc3ccccc3c2)ccc1C(=O)O 10.1021/ml100268k
136059337 65573 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 488 8 2 6 5.8 CCOC(=O)c1ccc(C(CC)(CC)NC(=O)c2cnn3c2NC(c2ccccc2)CC3(C)C)cc1 10.1021/jm101452x
CHEMBL1688103 65573 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 488 8 2 6 5.8 CCOC(=O)c1ccc(C(CC)(CC)NC(=O)c2cnn3c2NC(c2ccccc2)CC3(C)C)cc1 10.1021/jm101452x
135464340 65562 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 430 6 2 4 5.9 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C)cc1 10.1021/jm101452x
CHEMBL1687946 65562 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 430 6 2 4 5.9 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C)cc1 10.1021/jm101452x
CHEMBL1688097 65562 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 430 6 2 4 5.9 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C)cc1 10.1021/jm101452x
11462501 22714 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 358 6 0 4 5.1 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(Cl)ccc(OC)c21 10.1016/j.bmcl.2010.07.016
CHEMBL1223303 22714 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 358 6 0 4 5.1 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(Cl)ccc(OC)c21 10.1016/j.bmcl.2010.07.016
135930343 192563 2 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CaSR in human HEK293 cells measured after 5 mins by FLIPR assayAntagonist activity at human CaSR in human HEK293 cells measured after 5 mins by FLIPR assay
ChEMBL 497 6 1 6 6.4 Cc1nc(-c2cccc(F)c2O)n(CCc2ccccc2)c(=O)c1-c1cc(-c2ccccn2)c(C)s1 10.1021/acsmedchemlett.1c00187
CHEMBL4866668 192563 2 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CaSR in human HEK293 cells measured after 5 mins by FLIPR assayAntagonist activity at human CaSR in human HEK293 cells measured after 5 mins by FLIPR assay
ChEMBL 497 6 1 6 6.4 Cc1nc(-c2cccc(F)c2O)n(CCc2ccccc2)c(=O)c1-c1cc(-c2ccccn2)c(C)s1 10.1021/acsmedchemlett.1c00187
135956388 193066 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CaSR in human HEK293 cells measured after 5 mins by FLIPR assayAntagonist activity at human CaSR in human HEK293 cells measured after 5 mins by FLIPR assay
ChEMBL 483 6 1 6 6.1 Cc1nc(-c2cccc(F)c2O)n(CCc2ccccc2)c(=O)c1-c1ccc(-c2ccccn2)s1 10.1021/acsmedchemlett.1c00187
CHEMBL4874182 193066 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CaSR in human HEK293 cells measured after 5 mins by FLIPR assayAntagonist activity at human CaSR in human HEK293 cells measured after 5 mins by FLIPR assay
ChEMBL 483 6 1 6 6.1 Cc1nc(-c2cccc(F)c2O)n(CCc2ccccc2)c(=O)c1-c1ccc(-c2ccccn2)s1 10.1021/acsmedchemlett.1c00187
6918446 9654 56 None 2 6 Human 7.3 pIC50 = 7.3 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1016/j.bmcl.2005.08.095
716 9654 56 None 2 6 Human 7.3 pIC50 = 7.3 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1016/j.bmcl.2005.08.095
CHEMBL180672 9654 56 None 2 6 Human 7.3 pIC50 = 7.3 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1016/j.bmcl.2005.08.095
DB05695 9654 56 None 2 6 Human 7.3 pIC50 = 7.3 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1016/j.bmcl.2005.08.095
44405886 79646 1 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 408 8 2 4 4.7 CC(C)(Cc1ccc2ccccc2c1)NC[C@H](O)COc1cccc(Cl)c1C#N 10.1016/j.bmcl.2005.08.095
CHEMBL200311 79646 1 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 408 8 2 4 4.7 CC(C)(Cc1ccc2ccccc2c1)NC[C@H](O)COc1cccc(Cl)c1C#N 10.1016/j.bmcl.2005.08.095
54586368 69488 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Negative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cellsNegative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cells
ChEMBL 529 11 3 4 5.6 C[C@@H](OC[C@H](O)CNC(C)(C)Cc1ccc(Cl)cc1F)c1ccccc1C1CC2CC1C1C(C(=O)O)C21 10.1016/j.bmcl.2009.04.044
CHEMBL1783934 69488 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Negative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cellsNegative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cells
ChEMBL 529 11 3 4 5.6 C[C@@H](OC[C@H](O)CNC(C)(C)Cc1ccc(Cl)cc1F)c1ccccc1C1CC2CC1C1C(C(=O)O)C21 10.1016/j.bmcl.2009.04.044
122636699 147918 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 485 12 3 6 4.5 Cc1ccc([C@@H](C)OC[C@H](O)CNC(C)(C)CCSc2ccccc2)c2c1O[C@@H]1[C@@H](C(=O)O)[C@H]21 10.1016/j.bmcl.2016.06.073
CHEMBL3827577 147918 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 485 12 3 6 4.5 Cc1ccc([C@@H](C)OC[C@H](O)CNC(C)(C)CCSc2ccccc2)c2c1O[C@@H]1[C@@H](C(=O)O)[C@H]21 10.1016/j.bmcl.2016.06.073
49865440 22735 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 392 6 0 4 5.5 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(C(F)(F)F)ccc(OC)c21 10.1016/j.bmcl.2010.07.016
CHEMBL1223369 22735 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 392 6 0 4 5.5 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(C(F)(F)F)ccc(OC)c21 10.1016/j.bmcl.2010.07.016
135513459 192062 0 None -1 2 Mouse 7.3 pIC50 = 7.3 Functional
Antagonist activity at mouse CaSRAntagonist activity at mouse CaSR
ChEMBL 420 5 1 5 5.3 Cc1ccc(-c2c(C)nc(-c3cccc(F)c3O)n(CCc3ccccc3)c2=O)s1 10.1021/acsmedchemlett.1c00187
CHEMBL4859029 192062 0 None -1 2 Mouse 7.3 pIC50 = 7.3 Functional
Antagonist activity at mouse CaSRAntagonist activity at mouse CaSR
ChEMBL 420 5 1 5 5.3 Cc1ccc(-c2c(C)nc(-c3cccc(F)c3O)n(CCc3ccccc3)c2=O)s1 10.1021/acsmedchemlett.1c00187
45140972 207470 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 377 6 0 4 5.6 CCN(CC)c1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
CHEMBL599857 207470 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 377 6 0 4 5.6 CCN(CC)c1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
6918446 9654 56 None -30 6 Rat 6.3 pIC50 = 6.3 Functional
Inhibition of extracellular calcium-induced inositol triphosphate generation in rat MTC cells expressing calcium-sensing receptorInhibition of extracellular calcium-induced inositol triphosphate generation in rat MTC cells expressing calcium-sensing receptor
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1016/j.bmcl.2005.08.095
716 9654 56 None -30 6 Rat 6.3 pIC50 = 6.3 Functional
Inhibition of extracellular calcium-induced inositol triphosphate generation in rat MTC cells expressing calcium-sensing receptorInhibition of extracellular calcium-induced inositol triphosphate generation in rat MTC cells expressing calcium-sensing receptor
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1016/j.bmcl.2005.08.095
CHEMBL180672 9654 56 None -30 6 Rat 6.3 pIC50 = 6.3 Functional
Inhibition of extracellular calcium-induced inositol triphosphate generation in rat MTC cells expressing calcium-sensing receptorInhibition of extracellular calcium-induced inositol triphosphate generation in rat MTC cells expressing calcium-sensing receptor
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1016/j.bmcl.2005.08.095
DB05695 9654 56 None -30 6 Rat 6.3 pIC50 = 6.3 Functional
Inhibition of extracellular calcium-induced inositol triphosphate generation in rat MTC cells expressing calcium-sensing receptorInhibition of extracellular calcium-induced inositol triphosphate generation in rat MTC cells expressing calcium-sensing receptor
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1016/j.bmcl.2005.08.095
136032634 26027 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation counting
ChEMBL 376 3 2 4 4.1 O=C(NC12CC3CC(CC(C3)C1)C2)c1cnn2c1N[C@H](c1ccccc1)CC2 10.1016/j.bmc.2010.10.035
CHEMBL1290216 26027 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation counting
ChEMBL 376 3 2 4 4.1 O=C(NC12CC3CC(CC(C3)C1)C2)c1cnn2c1N[C@H](c1ccccc1)CC2 10.1016/j.bmc.2010.10.035
46891591 13405 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 422 10 2 5 4.8 CC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1[N+](=O)[O-] 10.1016/j.bmcl.2010.04.035
CHEMBL1083314 13405 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 422 10 2 5 4.8 CC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1[N+](=O)[O-] 10.1016/j.bmcl.2010.04.035
44415166 19651 0 None - 1 Rat 5.3 pIC50 = 5.3 Functional
Activity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulationActivity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulation
ChEMBL 492 7 2 4 5.7 CC(N[C@@H]1CCCC[C@H]1NS(=O)(=O)c1ccc(OC(F)(F)F)cc1)c1cccc2ccccc12 10.1021/jm051233+
CHEMBL1188809 19651 0 None - 1 Rat 5.3 pIC50 = 5.3 Functional
Activity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulationActivity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulation
ChEMBL 492 7 2 4 5.7 CC(N[C@@H]1CCCC[C@H]1NS(=O)(=O)c1ccc(OC(F)(F)F)cc1)c1cccc2ccccc12 10.1021/jm051233+
CHEMBL537426 19651 0 None - 1 Rat 5.3 pIC50 = 5.3 Functional
Activity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulationActivity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulation
ChEMBL 492 7 2 4 5.7 CC(N[C@@H]1CCCC[C@H]1NS(=O)(=O)c1ccc(OC(F)(F)F)cc1)c1cccc2ccccc12 10.1021/jm051233+
46891362 13191 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 427 9 2 3 6.0 CC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.04.035
CHEMBL1082379 13191 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 427 9 2 3 6.0 CC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.04.035
45139810 207474 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 370 4 0 4 5.3 COc1ccc2c(c1)c(-c1ccc(-c3ccccc3)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
CHEMBL599869 207474 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 370 4 0 4 5.3 COc1ccc2c(c1)c(-c1ccc(-c3ccccc3)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
54587335 69412 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Negative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cellsNegative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cells
ChEMBL 525 10 3 4 4.9 CC(C)(CC1Cc2ccccc2C1)NC[C@@H](O)COc1cc(C2CC3CC2C2C(C(=O)O)C32)cc(F)c1F 10.1016/j.bmcl.2009.04.044
CHEMBL1783762 69412 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Negative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cellsNegative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cells
ChEMBL 525 10 3 4 4.9 CC(C)(CC1Cc2ccccc2C1)NC[C@@H](O)COc1cc(C2CC3CC2C2C(C(=O)O)C32)cc(F)c1F 10.1016/j.bmcl.2009.04.044
46891265 13779 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 363 9 2 3 4.3 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COCc1ccccc1 10.1016/j.bmcl.2010.04.035
CHEMBL1084756 13779 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 363 9 2 3 4.3 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COCc1ccccc1 10.1016/j.bmcl.2010.04.035
122195446 130887 0 None -6 5 Rat 4.3 pIC50 = 4.3 Functional
Antagonist activity at rat CaSR expressed in HEK293 cells assessed as inhibition of Ca2+-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at rat CaSR expressed in HEK293 cells assessed as inhibition of Ca2+-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 421 7 1 5 2.8 COc1ccc(-c2[nH]c3ccccc3c2C(=O)CN(C)CC(=O)N2CCOCC2)cc1 10.1021/acs.jmedchem.5b01254
CHEMBL3633656 130887 0 None -6 5 Rat 4.3 pIC50 = 4.3 Functional
Antagonist activity at rat CaSR expressed in HEK293 cells assessed as inhibition of Ca2+-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at rat CaSR expressed in HEK293 cells assessed as inhibition of Ca2+-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 421 7 1 5 2.8 COc1ccc(-c2[nH]c3ccccc3c2C(=O)CN(C)CC(=O)N2CCOCC2)cc1 10.1021/acs.jmedchem.5b01254
122195446 130887 0 None -6 5 Rat 4.3 pIC50 = 4.3 Functional
Antagonist activity at rat CaSR expressed in HEK293 cells assessed as inhibition of Ca2+-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at rat CaSR expressed in HEK293 cells assessed as inhibition of Ca2+-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 421 7 1 5 2.8 COc1ccc(-c2[nH]c3ccccc3c2C(=O)CN(C)CC(=O)N2CCOCC2)cc1 10.1021/acs.jmedchem.5b01254
CHEMBL3633656 130887 0 None -6 5 Rat 4.3 pIC50 = 4.3 Functional
Antagonist activity at rat CaSR expressed in HEK293 cells assessed as inhibition of Ca2+-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at rat CaSR expressed in HEK293 cells assessed as inhibition of Ca2+-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 421 7 1 5 2.8 COc1ccc(-c2[nH]c3ccccc3c2C(=O)CN(C)CC(=O)N2CCOCC2)cc1 10.1021/acs.jmedchem.5b01254
46891418 13273 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 419 9 2 3 5.9 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COC(c1ccccc1)C(C)(C)C 10.1016/j.bmcl.2010.04.035
CHEMBL1082719 13273 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 419 9 2 3 5.9 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COC(c1ccccc1)C(C)(C)C 10.1016/j.bmcl.2010.04.035
122636658 147885 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 491 10 3 5 4.4 Cc1ccc([C@@H](C)OC[C@H](O)CNC(C)(C)Cc2ccc(Cl)c(F)c2)c2c1O[C@@H]1[C@@H](C(=O)O)[C@H]21 10.1016/j.bmcl.2016.06.073
CHEMBL3827154 147885 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 491 10 3 5 4.4 Cc1ccc([C@@H](C)OC[C@H](O)CNC(C)(C)Cc2ccc(Cl)c(F)c2)c2c1O[C@@H]1[C@@H](C(=O)O)[C@H]21 10.1016/j.bmcl.2016.06.073
136203774 26047 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation counting
ChEMBL 402 3 2 4 4.8 CC1(C)C=C(c2ccccc2)Nc2c(C(=O)NC34CC5CC(CC(C5)C3)C4)cnn21 10.1016/j.bmc.2010.10.035
CHEMBL1290329 26047 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation counting
ChEMBL 402 3 2 4 4.8 CC1(C)C=C(c2ccccc2)Nc2c(C(=O)NC34CC5CC(CC(C5)C3)C4)cnn21 10.1016/j.bmc.2010.10.035
136188839 66976 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 472 8 2 4 6.9 CCCc1nn2c(c1C(=O)NC(CC)(CC)c1ccc(C)cc1)NC(c1ccccc1)CC2(C)C 10.1016/j.bmc.2011.02.001
CHEMBL1689042 66976 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 472 8 2 4 6.9 CCCc1nn2c(c1C(=O)NC(CC)(CC)c1ccc(C)cc1)NC(c1ccccc1)CC2(C)C 10.1016/j.bmc.2011.02.001
CHEMBL1739941 66976 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 472 8 2 4 6.9 CCCc1nn2c(c1C(=O)NC(CC)(CC)c1ccc(C)cc1)NC(c1ccccc1)CC2(C)C 10.1016/j.bmc.2011.02.001
11191770 22769 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 528 6 0 4 5.8 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(I)c(Br)cc(OC)c21 10.1016/j.bmcl.2010.07.016
CHEMBL1223506 22769 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 528 6 0 4 5.8 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(I)c(Br)cc(OC)c21 10.1016/j.bmcl.2010.07.016
54582453 69414 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Negative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cellsNegative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cells
ChEMBL 514 10 3 5 4.5 CC(C)(CC1Cc2ccccc2C1)NC[C@@H](O)COc1cc(C2CC3CC2C2C(C(=O)O)C32)ccc1C#N 10.1016/j.bmcl.2009.04.044
CHEMBL1783764 69414 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Negative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cellsNegative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cells
ChEMBL 514 10 3 5 4.5 CC(C)(CC1Cc2ccccc2C1)NC[C@@H](O)COc1cc(C2CC3CC2C2C(C(=O)O)C32)ccc1C#N 10.1016/j.bmcl.2009.04.044
136188840 66942 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 494 7 2 5 6.6 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(Cl)c(OC)c1 10.1016/j.bmc.2011.02.001
CHEMBL1687956 66942 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 494 7 2 5 6.6 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(Cl)c(OC)c1 10.1016/j.bmc.2011.02.001
CHEMBL1739756 66942 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 494 7 2 5 6.6 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(Cl)c(OC)c1 10.1016/j.bmc.2011.02.001
45141390 207174 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 412 6 1 4 5.9 CCCc1c(O)ccc2c1c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1ccccc1 10.1021/jm901811v
CHEMBL598016 207174 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 412 6 1 4 5.9 CCCc1c(O)ccc2c1c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1ccccc1 10.1021/jm901811v
136059349 65566 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 446 7 2 5 5.6 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(OC)cc1 10.1021/jm101452x
CHEMBL1688087 65566 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 446 7 2 5 5.6 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(OC)cc1 10.1021/jm101452x
136072082 66965 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 458 7 2 4 6.5 CCc1nn2c(c1C(=O)NC(CC)(CC)c1ccc(C)cc1)NC(c1ccccc1)CC2(C)C 10.1016/j.bmc.2011.02.001
CHEMBL1689041 66965 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 458 7 2 4 6.5 CCc1nn2c(c1C(=O)NC(CC)(CC)c1ccc(C)cc1)NC(c1ccccc1)CC2(C)C 10.1016/j.bmc.2011.02.001
CHEMBL1739915 66965 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 458 7 2 4 6.5 CCc1nn2c(c1C(=O)NC(CC)(CC)c1ccc(C)cc1)NC(c1ccccc1)CC2(C)C 10.1016/j.bmc.2011.02.001
11203324 182043 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 528 11 2 9 4.3 COc1ccc(-c2nc(NCc3ccc4c(c3)OCO4)ccc2C(=O)NCCOc2ccccc2)c(OC)n1 10.1021/jm801178c
CHEMBL457249 182043 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 528 11 2 9 4.3 COc1ccc(-c2nc(NCc3ccc4c(c3)OCO4)ccc2C(=O)NCCOc2ccccc2)c(OC)n1 10.1021/jm801178c
11477141 22477 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 478 7 0 4 6.9 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(Br)c(-c3ccccc3)cc(OC)c21 10.1016/j.bmcl.2010.07.016
CHEMBL1222426 22477 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 478 7 0 4 6.9 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(Br)c(-c3ccccc3)cc(OC)c21 10.1016/j.bmcl.2010.07.016
44405804 79525 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 380 8 2 5 4.1 CC(C)(Cc1cc2ccccc2s1)NC[C@H](O)COc1ccccc1C#N 10.1016/j.bmcl.2005.08.095
CHEMBL199894 79525 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 380 8 2 5 4.1 CC(C)(Cc1cc2ccccc2s1)NC[C@H](O)COc1ccccc1C#N 10.1016/j.bmcl.2005.08.095
44405809 79379 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 376 8 2 4 3.7 CC(C)(Cc1ccc(F)cc1)NC[C@@H](O)COc1cccc(Cl)c1C#N 10.1016/j.bmcl.2005.08.095
CHEMBL199363 79379 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 376 8 2 4 3.7 CC(C)(Cc1ccc(F)cc1)NC[C@@H](O)COc1cccc(Cl)c1C#N 10.1016/j.bmcl.2005.08.095
46891466 13652 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 445 10 2 3 6.5 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COC(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2010.04.035
CHEMBL1084201 13652 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 445 10 2 3 6.5 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COC(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2010.04.035
44405815 79412 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 401 8 2 3 5.2 CC(C)(Cc1ccc(F)cc1)NC[C@@H](O)CSc1cccc(Cl)c1Cl 10.1016/j.bmcl.2005.08.095
CHEMBL199473 79412 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 401 8 2 3 5.2 CC(C)(Cc1ccc(F)cc1)NC[C@@H](O)CSc1cccc(Cl)c1Cl 10.1016/j.bmcl.2005.08.095
136054358 191604 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CaSR in human HEK293 cells measured after 5 mins by FLIPR assayAntagonist activity at human CaSR in human HEK293 cells measured after 5 mins by FLIPR assay
ChEMBL 421 5 1 6 4.7 Cc1ncc(-c2c(C)nc(-c3cccc(F)c3O)n(CCc3ccccc3)c2=O)s1 10.1021/acsmedchemlett.1c00187
CHEMBL4851971 191604 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CaSR in human HEK293 cells measured after 5 mins by FLIPR assayAntagonist activity at human CaSR in human HEK293 cells measured after 5 mins by FLIPR assay
ChEMBL 421 5 1 6 4.7 Cc1ncc(-c2c(C)nc(-c3cccc(F)c3O)n(CCc3ccccc3)c2=O)s1 10.1021/acsmedchemlett.1c00187
118173981 147937 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 489 10 3 5 4.8 Cc1ccc(C(C)OC[C@H](O)CNC(C)(C)Cc2ccc3ccccc3c2)c2c1OC1C(C(=O)O)C21 10.1016/j.bmcl.2016.06.073
CHEMBL3827723 147937 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 489 10 3 5 4.8 Cc1ccc(C(C)OC[C@H](O)CNC(C)(C)Cc2ccc3ccccc3c2)c2c1OC1C(C(=O)O)C21 10.1016/j.bmcl.2016.06.073
46228881 207380 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 376 7 0 4 5.7 C=CCCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
CHEMBL599229 207380 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 376 7 0 4 5.7 C=CCCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
44405841 79783 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 446 9 3 4 4.5 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(C(=O)O)c1 10.1016/j.bmcl.2005.08.095
CHEMBL200878 79783 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 446 9 3 4 4.5 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(C(=O)O)c1 10.1016/j.bmcl.2005.08.095
25218726 186089 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 498 11 1 7 4.6 COc1ccc(-c2nc(N(C)Cc3ccccc3)ncc2C(=O)NCCOc2ccccc2)cc1OC 10.1021/jm801178c
CHEMBL473345 186089 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 498 11 1 7 4.6 COc1ccc(-c2nc(N(C)Cc3ccccc3)ncc2C(=O)NCCOc2ccccc2)cc1OC 10.1021/jm801178c
10115992 207084 1 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 468 9 1 6 4.6 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1cccc(OCCO)c1 10.1021/jm901811v
CHEMBL597396 207084 1 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 468 9 1 6 4.6 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1cccc(OCCO)c1 10.1021/jm901811v
136059348 65763 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 434 6 2 4 5.8 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(F)cc1 10.1021/jm101452x
CHEMBL1689818 65763 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 434 6 2 4 5.8 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(F)cc1 10.1021/jm101452x
136030602 65761 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 450 6 2 4 6.3 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(Cl)cc1 10.1021/jm101452x
CHEMBL1689816 65761 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 450 6 2 4 6.3 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(Cl)cc1 10.1021/jm101452x
122636685 147894 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 489 10 3 5 4.8 Cc1ccc([C@@H](C)OC[C@H](O)CNC(C)(C)Cc2ccc3ccccc3c2)c2c1O[C@@H]1[C@@H](C(=O)O)[C@H]21 10.1016/j.bmcl.2016.06.073
CHEMBL3827259 147894 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 489 10 3 5 4.8 Cc1ccc([C@@H](C)OC[C@H](O)CNC(C)(C)Cc2ccc3ccccc3c2)c2c1O[C@@H]1[C@@H](C(=O)O)[C@H]21 10.1016/j.bmcl.2016.06.073
136059340 65755 4 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 484 6 2 4 6.6 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C(F)(F)F)cc1 10.1021/jm101452x
CHEMBL1689810 65755 4 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 484 6 2 4 6.6 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C(F)(F)F)cc1 10.1021/jm101452x
11682773 174519 0 None 15 2 Rat 8.1 pIC50 = 8.1 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
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 174519 0 None 15 2 Rat 8.1 pIC50 = 8.1 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
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 174519 0 None 15 2 Rat 8.1 pIC50 = 8.1 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
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
11307362 194179 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 548 12 2 8 5.2 COc1cc(-c2nc(NCc3cccc(Cl)c3)ncc2C(=O)NCCOc2ccccc2)cc(OC)c1OC 10.1021/jm801178c
CHEMBL493638 194179 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 548 12 2 8 5.2 COc1cc(-c2nc(NCc3cccc(Cl)c3)ncc2C(=O)NCCOc2ccccc2)cc(OC)c1OC 10.1021/jm801178c
11451283 207338 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 361 6 1 4 5.4 C=CCNc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
CHEMBL599040 207338 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 361 6 1 4 5.4 C=CCNc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
10135815 13392 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 403 10 2 3 5.3 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COC(c1ccccc1)C1CC1 10.1016/j.bmcl.2010.04.035
CHEMBL1083288 13392 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 403 10 2 3 5.3 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COC(c1ccccc1)C1CC1 10.1016/j.bmcl.2010.04.035
136199399 25998 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation counting
ChEMBL 452 4 2 4 5.7 O=C(NC12CC3CC(CC(C3)C1)C2)c1cnn2c1N[C@H](c1ccccc1)C[C@@H]2c1ccccc1 10.1016/j.bmc.2010.10.035
CHEMBL1290007 25998 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation counting
ChEMBL 452 4 2 4 5.7 O=C(NC12CC3CC(CC(C3)C1)C2)c1cnn2c1N[C@H](c1ccccc1)C[C@@H]2c1ccccc1 10.1016/j.bmc.2010.10.035
25218700 180824 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 514 12 2 8 4.6 COc1cc(-c2nc(NCc3ccccc3)ncc2C(=O)NCCOc2ccccc2)cc(OC)c1OC 10.1021/jm801178c
CHEMBL454374 180824 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 514 12 2 8 4.6 COc1cc(-c2nc(NCc3ccccc3)ncc2C(=O)NCCOc2ccccc2)cc(OC)c1OC 10.1021/jm801178c
46891531 13399 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 439 10 2 3 5.9 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COC(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2010.04.035
CHEMBL1083306 13399 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 439 10 2 3 5.9 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COC(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2010.04.035
46891464 13393 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 417 10 2 3 5.7 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COC(c1ccccc1)C1CCC1 10.1016/j.bmcl.2010.04.035
CHEMBL1083289 13393 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 417 10 2 3 5.7 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COC(c1ccccc1)C1CCC1 10.1016/j.bmcl.2010.04.035
44405848 79897 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 420 8 2 3 4.9 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(F)c1 10.1016/j.bmcl.2005.08.095
CHEMBL201137 79897 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 420 8 2 3 4.9 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(F)c1 10.1016/j.bmcl.2005.08.095
136032621 26011 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation counting
ChEMBL 390 3 2 4 4.7 C[C@H]1C[C@@H](c2ccccc2)Nc2c(C(=O)NC34CC5CC(CC(C5)C3)C4)cnn21 10.1016/j.bmc.2010.10.035
CHEMBL1290106 26011 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation counting
ChEMBL 390 3 2 4 4.7 C[C@H]1C[C@@H](c2ccccc2)Nc2c(C(=O)NC34CC5CC(CC(C5)C3)C4)cnn21 10.1016/j.bmc.2010.10.035
10589 7793 11 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 557 14 3 8 4.6 OC[C@@H](Nc1ccc(c(n1)c1cc(OC)c(c(c1)OC)OC)C(=O)NCCOc1ccccc1)Cc1ccccc1 10.1021/jm801178c
11410354 7793 11 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 557 14 3 8 4.6 OC[C@@H](Nc1ccc(c(n1)c1cc(OC)c(c(c1)OC)OC)C(=O)NCCOc1ccccc1)Cc1ccccc1 10.1021/jm801178c
CHEMBL457071 7793 11 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assayAntagonist activity at calcium-sensing receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 557 14 3 8 4.6 OC[C@@H](Nc1ccc(c(n1)c1cc(OC)c(c(c1)OC)OC)C(=O)NCCOc1ccccc1)Cc1ccccc1 10.1021/jm801178c
46890831 13914 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 417 10 2 3 5.6 Cc1ccccc1[C@@H](OC[C@@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)C1CC1 10.1016/j.bmcl.2010.04.035
CHEMBL1085335 13914 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 417 10 2 3 5.6 Cc1ccccc1[C@@H](OC[C@@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)C1CC1 10.1016/j.bmcl.2010.04.035
122636769 147904 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 491 10 3 5 4.4 Cc1ccc([C@@H](C)OC[C@H](O)CNC(C)(C)Cc2ccc(Cl)c(F)c2)c2c1O[C@@H]1[C@H]2[C@H]1C(=O)O 10.1016/j.bmcl.2016.06.073
CHEMBL3827356 147904 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 491 10 3 5 4.4 Cc1ccc([C@@H](C)OC[C@H](O)CNC(C)(C)Cc2ccc(Cl)c(F)c2)c2c1O[C@@H]1[C@H]2[C@H]1C(=O)O 10.1016/j.bmcl.2016.06.073
49865442 22737 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 358 6 0 4 5.1 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(OC)ccc(Cl)c21 10.1016/j.bmcl.2010.07.016
CHEMBL1223371 22737 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 358 6 0 4 5.1 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(OC)ccc(Cl)c21 10.1016/j.bmcl.2010.07.016
49865483 22754 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 322 5 0 3 5.6 CCCn1c(-c2ccc(C(C)C)cc2)nc2c(C)ccc(OC)c21 10.1016/j.bmcl.2010.07.016
CHEMBL1223440 22754 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilizationAntagonist activity at human CaSR expressed in hamster fibroblasts assessed as inhibition of calcium mobilization
ChEMBL 322 5 0 3 5.6 CCCn1c(-c2ccc(C(C)C)cc2)nc2c(C)ccc(OC)c21 10.1016/j.bmcl.2010.07.016
10366358 79427 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 447 9 2 5 4.7 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1ccc([N+](=O)[O-])cc1 10.1016/j.bmcl.2005.08.095
CHEMBL199529 79427 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 447 9 2 5 4.7 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1ccc([N+](=O)[O-])cc1 10.1016/j.bmcl.2005.08.095
58973485 164306 0 None 26 2 Rat 8.1 pIC50 = 8.1 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
ChEMBL 360 5 2 3 4.5 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)O)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4079960 164306 0 None 26 2 Rat 8.1 pIC50 = 8.1 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
ChEMBL 360 5 2 3 4.5 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)O)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4126482 164306 0 None 26 2 Rat 8.1 pIC50 = 8.1 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
ChEMBL 360 5 2 3 4.5 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)O)cc2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
45141392 206104 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 634 13 1 8 4.8 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1cccc(NC(=O)CN2CCN(CCCN(C)C)CC2)c1 10.1021/jm901811v
CHEMBL590560 206104 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 634 13 1 8 4.8 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1cccc(NC(=O)CN2CCN(CCCN(C)C)CC2)c1 10.1021/jm901811v
136059351 65567 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 522 9 2 5 7.2 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(OCc2ccccc2)cc1 10.1021/jm101452x
CHEMBL1688088 65567 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assayInhibition of CaSR expressed in CHO cells incubated with compound for 10 mins measured after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 522 9 2 5 7.2 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(OCc2ccccc2)cc1 10.1021/jm101452x
44415153 7790 0 None - 1 Rat 5.1 pIC50 = 5.1 Functional
Activity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulationActivity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulation
ChEMBL 438 7 2 4 4.8 COc1ccc(cc1)S(=O)(=O)N[C@@H]1CCCC[C@H]1NC(c1cccc2c1cccc2)C 10.1021/jm051233+
715 7790 0 None - 1 Rat 5.1 pIC50 = 5.1 Functional
Activity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulationActivity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulation
ChEMBL 438 7 2 4 4.8 COc1ccc(cc1)S(=O)(=O)N[C@@H]1CCCC[C@H]1NC(c1cccc2c1cccc2)C 10.1021/jm051233+
CHEMBL1197056 7790 0 None - 1 Rat 5.1 pIC50 = 5.1 Functional
Activity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulationActivity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulation
ChEMBL 438 7 2 4 4.8 COc1ccc(cc1)S(=O)(=O)N[C@@H]1CCCC[C@H]1NC(c1cccc2c1cccc2)C 10.1021/jm051233+
136188844 65689 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 506 7 2 4 7.6 CCC(CC)(NC(=O)c1c(-c2ccccc2)nn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C)cc1 10.1016/j.bmc.2011.02.001
CHEMBL1689044 65689 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 10 mins by scintillation counting
ChEMBL 506 7 2 4 7.6 CCC(CC)(NC(=O)c1c(-c2ccccc2)nn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C)cc1 10.1016/j.bmc.2011.02.001
46891263 14044 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 391 10 2 3 4.9 CC(COC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1 10.1016/j.bmcl.2010.04.035
CHEMBL1085987 14044 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 391 10 2 3 4.9 CC(COC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1 10.1016/j.bmcl.2010.04.035
46890829 14016 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 417 10 2 3 5.6 Cc1ccccc1[C@@H](OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)C1CC1 10.1016/j.bmcl.2010.04.035
CHEMBL1085807 14016 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 417 10 2 3 5.6 Cc1ccccc1[C@@H](OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)C1CC1 10.1016/j.bmcl.2010.04.035
44405850 148158 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 441 7 2 4 4.3 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1C(=O)c1cccc(C#N)c1 10.1016/j.bmcl.2005.08.095
CHEMBL383842 148158 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 441 7 2 4 4.3 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1C(=O)c1cccc(C#N)c1 10.1016/j.bmcl.2005.08.095
44405891 79488 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 392 8 1 3 5.7 CC(C)(Cc1ccc2ccccc2c1)NCCCOc1cccc(Cl)c1C#N 10.1016/j.bmcl.2005.08.095
CHEMBL199785 79488 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 392 8 1 3 5.7 CC(C)(Cc1ccc2ccccc2c1)NCCCOc1cccc(Cl)c1C#N 10.1016/j.bmcl.2005.08.095
10109178 206312 50 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 360 5 0 4 4.8 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
CHEMBL592176 206312 50 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
ChEMBL 360 5 0 4 4.8 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C 10.1021/jm901811v
122636728 147900 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 495 10 3 6 4.8 Cc1ccc([C@@H](C)OC[C@H](O)CNC(C)(C)Cc2ccc3sccc3c2)c2c1O[C@@H]1[C@@H](C(=O)O)[C@H]21 10.1016/j.bmcl.2016.06.073
CHEMBL3827304 147900 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assayAntagonist activity at calcium sensing receptor (unknown origin) by cell based FLIPR assay
ChEMBL 495 10 3 6 4.8 Cc1ccc([C@@H](C)OC[C@H](O)CNC(C)(C)Cc2ccc3sccc3c2)c2c1O[C@@H]1[C@@H](C(=O)O)[C@H]21 10.1016/j.bmcl.2016.06.073
145947114 174409 0 None 43 2 Rat 8.0 pIC50 = 8.0 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
ChEMBL 384 4 1 2 5.8 C[C@@H](N[C@@H]1CCN(c2cccc(C(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4125688 174409 0 None 43 2 Rat 8.0 pIC50 = 8.0 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
ChEMBL 384 4 1 2 5.8 C[C@@H](N[C@@H]1CCN(c2cccc(C(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
CHEMBL4301528 174409 0 None 43 2 Rat 8.0 pIC50 = 8.0 Functional
Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISAAgonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
ChEMBL 384 4 1 2 5.8 C[C@@H](N[C@@H]1CCN(c2cccc(C(F)(F)F)c2)C1)c1cccc2ccccc12 10.1016/j.bmcl.2018.04.055
44415018 20715 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Activity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulationActivity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulation
ChEMBL 456 6 2 3 6.1 CC(N[C@@H]1CCCC[C@H]1NC(=O)c1ccc(OC(F)(F)F)cc1)c1cccc2ccccc12 10.1021/jm051233+
CHEMBL1196590 20715 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Activity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulationActivity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulation
ChEMBL 456 6 2 3 6.1 CC(N[C@@H]1CCCC[C@H]1NC(=O)c1ccc(OC(F)(F)F)cc1)c1cccc2ccccc12 10.1021/jm051233+
CHEMBL557567 20715 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Activity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulationActivity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulation
ChEMBL 456 6 2 3 6.1 CC(N[C@@H]1CCCC[C@H]1NC(=O)c1ccc(OC(F)(F)F)cc1)c1cccc2ccccc12 10.1021/jm051233+
54583429 69413 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Negative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cellsNegative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cells
ChEMBL 489 10 3 4 4.7 CC(C)(CC1Cc2ccccc2C1)NC[C@@H](O)COc1cccc(C2CC3CC2C2C(C(=O)O)C32)c1 10.1016/j.bmcl.2009.04.044
CHEMBL1783763 69413 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Negative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cellsNegative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cells
ChEMBL 489 10 3 4 4.7 CC(C)(CC1Cc2ccccc2C1)NC[C@@H](O)COc1cccc(C2CC3CC2C2C(C(=O)O)C32)c1 10.1016/j.bmcl.2009.04.044
46891364 13268 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 391 10 2 3 5.3 CCC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1 10.1016/j.bmcl.2010.04.035
CHEMBL1082711 13268 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
ChEMBL 391 10 2 3 5.3 CCC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1 10.1016/j.bmcl.2010.04.035
44405904 79630 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 377 9 2 5 2.4 CC(C)(Cc1ccccc1)NC[C@H](O)COc1ccccc1S(C)(=O)=O 10.1016/j.bmcl.2005.08.095
CHEMBL200248 79630 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 377 9 2 5 2.4 CC(C)(Cc1ccccc1)NC[C@H](O)COc1ccccc1S(C)(=O)=O 10.1016/j.bmcl.2005.08.095
53317658 64845 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assay
ChEMBL 447 11 3 4 5.0 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COC(c1cccc(C(=O)O)c1)C1CC1 10.1021/ml100268k
CHEMBL1672962 64845 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assayAntagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assay
ChEMBL 447 11 3 4 5.0 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COC(c1cccc(C(=O)O)c1)C1CC1 10.1021/ml100268k
136199394 25900 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation counting
ChEMBL 445 3 1 5 5.7 O=C(OC12CC3CC(CC(C3)C1)C2)c1cnn2c1N[C@H](c1ccccc1)C[C@@H]2C(F)(F)F 10.1016/j.bmc.2010.10.035
CHEMBL1289346 25900 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation countingAntagonist activity at CaSR expressed in CHO cells assessed as [35S]-GTPgammaS binding by scintillation counting
ChEMBL 445 3 1 5 5.7 O=C(OC12CC3CC(CC(C3)C1)C2)c1cnn2c1N[C@H](c1ccccc1)C[C@@H]2C(F)(F)F 10.1016/j.bmc.2010.10.035
44405847 79844 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 418 8 3 4 4.5 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1ccccc1O 10.1016/j.bmcl.2005.08.095
CHEMBL201085 79844 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPRInhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
ChEMBL 418 8 3 4 4.5 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1ccccc1O 10.1016/j.bmcl.2005.08.095
71511839 8370 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Measuring ligand induced IP<sub>1</sub> accumulation.Measuring ligand induced IP<sub>1</sub> accumulation.
Drug Central None None None None None
8375 8370 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Measuring ligand induced IP<sub>1</sub> accumulation.Measuring ligand induced IP<sub>1</sub> accumulation.
Drug Central None None None None None
CHEMBL3545184 8370 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Measuring ligand induced IP<sub>1</sub> accumulation.Measuring ligand induced IP<sub>1</sub> accumulation.
Drug Central None None None None None
DB12865 8370 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Measuring ligand induced IP<sub>1</sub> accumulation.Measuring ligand induced IP<sub>1</sub> accumulation.
Drug Central None None None None None
3336 101776 30 None 15 14 Bovine 8.3 pEC50 = 8.3 Functional
increase in intracellular Ca2+ in bovine parathyroid cellsincrease in intracellular Ca2+ in bovine parathyroid cells
Drug Central 315 7 1 1 5.6 CC(NCCC(c1ccccc1)c1ccccc1)c1ccccc1 None
CHEMBL1405922 101776 30 None 15 14 Bovine 8.3 pEC50 = 8.3 Functional
increase in intracellular Ca2+ in bovine parathyroid cellsincrease in intracellular Ca2+ in bovine parathyroid cells
Drug Central 315 7 1 1 5.6 CC(NCCC(c1ccccc1)c1ccccc1)c1ccccc1 None
CHEMBL254832 101776 30 None 15 14 Bovine 8.3 pEC50 = 8.3 Functional
increase in intracellular Ca2+ in bovine parathyroid cellsincrease in intracellular Ca2+ in bovine parathyroid cells
Drug Central 315 7 1 1 5.6 CC(NCCC(c1ccccc1)c1ccccc1)c1ccccc1 None
3336 101776 30 None -15 14 Human 8.2 pEC50 = 8.2 Functional
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
Drug Central 315 7 1 1 5.6 CC(NCCC(c1ccccc1)c1ccccc1)c1ccccc1 None
CHEMBL1405922 101776 30 None -15 14 Human 8.2 pEC50 = 8.2 Functional
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
Drug Central 315 7 1 1 5.6 CC(NCCC(c1ccccc1)c1ccccc1)c1ccccc1 None
CHEMBL254832 101776 30 None -15 14 Human 8.2 pEC50 = 8.2 Functional
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
Drug Central 315 7 1 1 5.6 CC(NCCC(c1ccccc1)c1ccccc1)c1ccccc1 None
5307 8387 29 None -1 2 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 374 6 2 3 4.4 OC(=O)Cc1ccc(cc1)N1CC[C@@H](C1)N[C@@H](c1cccc2c1cccc2)C None
71242808 8387 29 None -1 2 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 374 6 2 3 4.4 OC(=O)Cc1ccc(cc1)N1CC[C@@H](C1)N[C@@H](c1cccc2c1cccc2)C None
9042 8387 29 None -1 2 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 374 6 2 3 4.4 OC(=O)Cc1ccc(cc1)N1CC[C@@H](C1)N[C@@H](c1cccc2c1cccc2)C None
CHEMBL4297621 8387 29 None -1 2 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 374 6 2 3 4.4 OC(=O)Cc1ccc(cc1)N1CC[C@@H](C1)N[C@@H](c1cccc2c1cccc2)C None
DB12388 8387 29 None -1 2 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 374 6 2 3 4.4 OC(=O)Cc1ccc(cc1)N1CC[C@@H](C1)N[C@@H](c1cccc2c1cccc2)C None
156419 7725 74 None 11 15 Human 8.1 pEC50 = 8.1 Functional
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
Drug Central 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F None
3308 7725 74 None 11 15 Human 8.1 pEC50 = 8.1 Functional
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
Drug Central 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F None
647 7725 74 None 11 15 Human 8.1 pEC50 = 8.1 Functional
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
Drug Central 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F None
CHEMBL1201284 7725 74 None 11 15 Human 8.1 pEC50 = 8.1 Functional
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
Drug Central 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F None
DB01012 7725 74 None 11 15 Human 8.1 pEC50 = 8.1 Functional
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
Drug Central 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F None
71511839 8370 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Measuring ligand induced IP<sub>1</sub> accumulation.Measuring ligand induced IP<sub>1</sub> accumulation.
Guide to Pharmacology None None None None 23674604
8375 8370 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Measuring ligand induced IP<sub>1</sub> accumulation.Measuring ligand induced IP<sub>1</sub> accumulation.
Guide to Pharmacology None None None None 23674604
CHEMBL3545184 8370 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Measuring ligand induced IP<sub>1</sub> accumulation.Measuring ligand induced IP<sub>1</sub> accumulation.
Guide to Pharmacology None None None None 23674604
DB12865 8370 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Measuring ligand induced IP<sub>1</sub> accumulation.Measuring ligand induced IP<sub>1</sub> accumulation.
Guide to Pharmacology None None None None 23674604
5307 8387 29 None -1 2 Human 7.0 pEC50 = 7.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 374 6 2 3 4.4 OC(=O)Cc1ccc(cc1)N1CC[C@@H](C1)N[C@@H](c1cccc2c1cccc2)C 29724589
71242808 8387 29 None -1 2 Human 7.0 pEC50 = 7.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 374 6 2 3 4.4 OC(=O)Cc1ccc(cc1)N1CC[C@@H](C1)N[C@@H](c1cccc2c1cccc2)C 29724589
9042 8387 29 None -1 2 Human 7.0 pEC50 = 7.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 374 6 2 3 4.4 OC(=O)Cc1ccc(cc1)N1CC[C@@H](C1)N[C@@H](c1cccc2c1cccc2)C 29724589
CHEMBL4297621 8387 29 None -1 2 Human 7.0 pEC50 = 7.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 374 6 2 3 4.4 OC(=O)Cc1ccc(cc1)N1CC[C@@H](C1)N[C@@H](c1cccc2c1cccc2)C 29724589
DB12388 8387 29 None -1 2 Human 7.0 pEC50 = 7.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 374 6 2 3 4.4 OC(=O)Cc1ccc(cc1)N1CC[C@@H](C1)N[C@@H](c1cccc2c1cccc2)C 29724589
156419 7725 74 None 11 15 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 14593085
3308 7725 74 None 11 15 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 14593085
647 7725 74 None 11 15 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 14593085
CHEMBL1201284 7725 74 None 11 15 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 14593085
DB01012 7725 74 None 11 15 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 14593085
3947 7029 27 None - 1 Human 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 283 2 1 3 4.2 Cc1ccc(c(c1)C)C(c1nc2c(s1)cccc2)(O)C 21239511
52943938 7029 27 None - 1 Human 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 283 2 1 3 4.2 Cc1ccc(c(c1)C)C(c1nc2c(s1)cccc2)(O)C 21239511
CHEMBL1256367 7029 27 None - 1 Human 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 283 2 1 3 4.2 Cc1ccc(c(c1)C)C(c1nc2c(s1)cccc2)(O)C 21239511
10158373 7301 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Inhibition of 2.5 mM Ca<sup>2+</sup>-mediated Ca<sup>2+</sup><sub>i</sub> releaseInhibition of 2.5 mM Ca<sup>2+</sup>-mediated Ca<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 408 6 0 4 5.2 C#CCOc1ccc2c(c1)c(nc(=O)n2Cc1ccccc1)c1ccc(cc1)C(C)C 20158186
9475 7301 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Inhibition of 2.5 mM Ca<sup>2+</sup>-mediated Ca<sup>2+</sup><sub>i</sub> releaseInhibition of 2.5 mM Ca<sup>2+</sup>-mediated Ca<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 408 6 0 4 5.2 C#CCOc1ccc2c(c1)c(nc(=O)n2Cc1ccccc1)c1ccc(cc1)C(C)C 20158186
CHEMBL591475 7301 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Inhibition of 2.5 mM Ca<sup>2+</sup>-mediated Ca<sup>2+</sup><sub>i</sub> releaseInhibition of 2.5 mM Ca<sup>2+</sup>-mediated Ca<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 408 6 0 4 5.2 C#CCOc1ccc2c(c1)c(nc(=O)n2Cc1ccccc1)c1ccc(cc1)C(C)C 20158186
46917559 8340 12 None 138 2 Human 7.9 pIC50 = 7.9 Functional
Inhibition of 5 mM Ca<sup>2+</sup>-mediated luciferase reporter activityInhibition of 5 mM Ca<sup>2+</sup>-mediated luciferase reporter activity
Guide to Pharmacology 513 11 3 4 6.2 O[C@H](CNC(Cc1ccc(c(c1)F)Cl)(C)C)CO[C@@H](c1ccccc1c1ccc(c(c1)C)C(=O)O)C 24900301
9474 8340 12 None 138 2 Human 7.9 pIC50 = 7.9 Functional
Inhibition of 5 mM Ca<sup>2+</sup>-mediated luciferase reporter activityInhibition of 5 mM Ca<sup>2+</sup>-mediated luciferase reporter activity
Guide to Pharmacology 513 11 3 4 6.2 O[C@H](CNC(Cc1ccc(c(c1)F)Cl)(C)C)CO[C@@H](c1ccccc1c1ccc(c(c1)C)C(=O)O)C 24900301
CHEMBL1672973 8340 12 None 138 2 Human 7.9 pIC50 = 7.9 Functional
Inhibition of 5 mM Ca<sup>2+</sup>-mediated luciferase reporter activityInhibition of 5 mM Ca<sup>2+</sup>-mediated luciferase reporter activity
Guide to Pharmacology 513 11 3 4 6.2 O[C@H](CNC(Cc1ccc(c(c1)F)Cl)(C)C)CO[C@@H](c1ccccc1c1ccc(c(c1)C)C(=O)O)C 24900301
11849514 7570 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Inhibition of 9mM Ca<sup>2+</sup><sub>o</sub>-mediated IP accumulationInhibition of 9mM Ca<sup>2+</sup><sub>o</sub>-mediated IP accumulation
Guide to Pharmacology 406 5 2 2 5.9 Clc1ccc(cc1)C(=O)N[C@H]1CCCC[C@@H]1N[C@@H](c1cccc2c1cccc2)C 14506236
714 7570 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Inhibition of 9mM Ca<sup>2+</sup><sub>o</sub>-mediated IP accumulationInhibition of 9mM Ca<sup>2+</sup><sub>o</sub>-mediated IP accumulation
Guide to Pharmacology 406 5 2 2 5.9 Clc1ccc(cc1)C(=O)N[C@H]1CCCC[C@@H]1N[C@@H](c1cccc2c1cccc2)C 14506236
CHEMBL4303565 7570 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Inhibition of 9mM Ca<sup>2+</sup><sub>o</sub>-mediated IP accumulationInhibition of 9mM Ca<sup>2+</sup><sub>o</sub>-mediated IP accumulation
Guide to Pharmacology 406 5 2 2 5.9 Clc1ccc(cc1)C(=O)N[C@H]1CCCC[C@@H]1N[C@@H](c1cccc2c1cccc2)C 14506236
10589 7793 11 None - 1 Human 7.1 pIC50 = 7.1 Functional
Measuring antagonism of internal calcium mobilization in HEK293 cells expressing human CaSR in a FLIPR assay, using external calcium as agonist.Measuring antagonism of internal calcium mobilization in HEK293 cells expressing human CaSR in a FLIPR assay, using external calcium as agonist.
Guide to Pharmacology 557 14 3 8 4.6 OC[C@@H](Nc1ccc(c(n1)c1cc(OC)c(c(c1)OC)OC)C(=O)NCCOc1ccccc1)Cc1ccccc1 19143533
11410354 7793 11 None - 1 Human 7.1 pIC50 = 7.1 Functional
Measuring antagonism of internal calcium mobilization in HEK293 cells expressing human CaSR in a FLIPR assay, using external calcium as agonist.Measuring antagonism of internal calcium mobilization in HEK293 cells expressing human CaSR in a FLIPR assay, using external calcium as agonist.
Guide to Pharmacology 557 14 3 8 4.6 OC[C@@H](Nc1ccc(c(n1)c1cc(OC)c(c(c1)OC)OC)C(=O)NCCOc1ccccc1)Cc1ccccc1 19143533
CHEMBL457071 7793 11 None - 1 Human 7.1 pIC50 = 7.1 Functional
Measuring antagonism of internal calcium mobilization in HEK293 cells expressing human CaSR in a FLIPR assay, using external calcium as agonist.Measuring antagonism of internal calcium mobilization in HEK293 cells expressing human CaSR in a FLIPR assay, using external calcium as agonist.
Guide to Pharmacology 557 14 3 8 4.6 OC[C@@H](Nc1ccc(c(n1)c1cc(OC)c(c(c1)OC)OC)C(=O)NCCOc1ccccc1)Cc1ccccc1 19143533
10345214 10142 13 None 1 2 Human 6.7 pIC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 447 11 3 4 3.9 O[C@@H](COc1cc(CCC(=O)O)cc(c1F)F)CNC(CC1Cc2c(C1)cccc2)(C)C 19442519
9473 10142 13 None 1 2 Human 6.7 pIC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 447 11 3 4 3.9 O[C@@H](COc1cc(CCC(=O)O)cc(c1F)F)CNC(CC1Cc2c(C1)cccc2)(C)C 19442519
CHEMBL1198855 10142 13 None 1 2 Human 6.7 pIC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 447 11 3 4 3.9 O[C@@H](COc1cc(CCC(=O)O)cc(c1F)F)CNC(CC1Cc2c(C1)cccc2)(C)C 19442519
DB05255 10142 13 None 1 2 Human 6.7 pIC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 447 11 3 4 3.9 O[C@@H](COc1cc(CCC(=O)O)cc(c1F)F)CNC(CC1Cc2c(C1)cccc2)(C)C 19442519
9476 10298 35 None - 1 Human 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 436 11 3 5 3.5 N#Cc1ccc(cc1OC[C@@H](CNC(CC1Cc2c(C1)cccc2)(C)C)O)CCC(=O)O 19786130
9910902 10298 35 None - 1 Human 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 436 11 3 5 3.5 N#Cc1ccc(cc1OC[C@@H](CNC(CC1Cc2c(C1)cccc2)(C)C)O)CCC(=O)O 19786130
CHEMBL1084513 10298 35 None - 1 Human 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 436 11 3 5 3.5 N#Cc1ccc(cc1OC[C@@H](CNC(CC1Cc2c(C1)cccc2)(C)C)O)CCC(=O)O 19786130
6918446 9654 56 None 2 6 Human 7.3 pIC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 11561095
6918446 9654 56 None 2 6 Human 7.3 pIC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 15686947
716 9654 56 None 2 6 Human 7.3 pIC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 11561095
716 9654 56 None 2 6 Human 7.3 pIC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 15686947
CHEMBL180672 9654 56 None 2 6 Human 7.3 pIC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 11561095
CHEMBL180672 9654 56 None 2 6 Human 7.3 pIC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 15686947
DB05695 9654 56 None 2 6 Human 7.3 pIC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 11561095
DB05695 9654 56 None 2 6 Human 7.3 pIC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 15686947
10590 10044 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 425 4 1 5 5.0 Oc1ccccc1c1nc2ccnc(c2c(=O)n1[C@@H](Cc1ccccc1)C)C(F)(F)F 19625189
135948915 10044 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 425 4 1 5 5.0 Oc1ccccc1c1nc2ccnc(c2c(=O)n1[C@@H](Cc1ccccc1)C)C(F)(F)F 19625189
CHEMBL565122 10044 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 425 4 1 5 5.0 Oc1ccccc1c1nc2ccnc(c2c(=O)n1[C@@H](Cc1ccccc1)C)C(F)(F)F 19625189
10696 7320 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 486 6 0 4 6.0 CC(C)C1=CC=C(C=C1)C2=NC(=O)N(CC3=CC=C(Br)C=C3)C4=CC=C(OCC#C)C=C24 21526895
59259095 7320 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 486 6 0 4 6.0 CC(C)C1=CC=C(C=C1)C2=NC(=O)N(CC3=CC=C(Br)C=C3)C4=CC=C(OCC#C)C=C24 21526895
44405854 6818 0 None -186 2 Rat 4.3 pIC50 None 4.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 433 8 2 5 4.7 N#Cc1cccc(c1)CN1CCC[C@@H]1[C@@H](CNC(Cc1cc2c(s1)cccc2)(C)C)O 16216508
711 6818 0 None -186 2 Rat 4.3 pIC50 None 4.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 433 8 2 5 4.7 N#Cc1cccc(c1)CN1CCC[C@@H]1[C@@H](CNC(Cc1cc2c(s1)cccc2)(C)C)O 16216508
CHEMBL200312 6818 0 None -186 2 Rat 4.3 pIC50 None 4.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 433 8 2 5 4.7 N#Cc1cccc(c1)CN1CCC[C@@H]1[C@@H](CNC(Cc1cc2c(s1)cccc2)(C)C)O 16216508
44415153 7790 0 None - 1 Rat 5.3 pIC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 438 7 2 4 4.8 COc1ccc(cc1)S(=O)(=O)N[C@@H]1CCCC[C@H]1NC(c1cccc2c1cccc2)C 15300839
715 7790 0 None - 1 Rat 5.3 pIC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 438 7 2 4 4.8 COc1ccc(cc1)S(=O)(=O)N[C@@H]1CCCC[C@H]1NC(c1cccc2c1cccc2)C 15300839
CHEMBL1197056 7790 0 None - 1 Rat 5.3 pIC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 438 7 2 4 4.8 COc1ccc(cc1)S(=O)(=O)N[C@@H]1CCCC[C@H]1NC(c1cccc2c1cccc2)C 15300839
11710462 7944 0 None - 1 Human 6.9 pIC50 None 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 370 7 1 4 3.7 N#Cc1c(cccc1Cl)OC[C@@H](CN1CCC[C@H]1Cc1ccccc1)O 15686947
712 7944 0 None - 1 Human 6.9 pIC50 None 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 370 7 1 4 3.7 N#Cc1c(cccc1Cl)OC[C@@H](CN1CCC[C@H]1Cc1ccccc1)O 15686947
CHEMBL178083 7944 0 None - 1 Human 6.9 pIC50 None 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 370 7 1 4 3.7 N#Cc1c(cccc1Cl)OC[C@@H](CN1CCC[C@H]1Cc1ccccc1)O 15686947
135515453 6868 0 None - 1 Human 7.0 pIC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 352 4 1 3 3.4 CCc1c(C)[nH]/c(=C\2/C=CC=CC2=O)/n(c1=O)CCc1ccccc1F 15863312
713 6868 0 None - 1 Human 7.0 pIC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 352 4 1 3 3.4 CCc1c(C)[nH]/c(=C\2/C=CC=CC2=O)/n(c1=O)CCc1ccccc1F 15863312
CHEMBL194764 6868 0 None - 1 Human 7.0 pIC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 352 4 1 3 3.4 CCc1c(C)[nH]/c(=C\2/C=CC=CC2=O)/n(c1=O)CCc1ccccc1F 15863312
156419 7725 74 None 11 15 Human 6.3 pKB = 6.3 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 22210744
156419 7725 74 None 11 15 Human 6.3 pKB = 6.3 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 23372019
156419 7725 74 None 11 15 Human 6.3 pKB = 6.3 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 25220431
156419 7725 74 None 11 15 Human 6.3 pKB = 6.3 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 27002221
3308 7725 74 None 11 15 Human 6.3 pKB = 6.3 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 22210744
3308 7725 74 None 11 15 Human 6.3 pKB = 6.3 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 23372019
3308 7725 74 None 11 15 Human 6.3 pKB = 6.3 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 25220431
3308 7725 74 None 11 15 Human 6.3 pKB = 6.3 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 27002221
647 7725 74 None 11 15 Human 6.3 pKB = 6.3 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 22210744
647 7725 74 None 11 15 Human 6.3 pKB = 6.3 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 23372019
647 7725 74 None 11 15 Human 6.3 pKB = 6.3 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 25220431
647 7725 74 None 11 15 Human 6.3 pKB = 6.3 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 27002221
CHEMBL1201284 7725 74 None 11 15 Human 6.3 pKB = 6.3 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 22210744
CHEMBL1201284 7725 74 None 11 15 Human 6.3 pKB = 6.3 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 23372019
CHEMBL1201284 7725 74 None 11 15 Human 6.3 pKB = 6.3 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 25220431
CHEMBL1201284 7725 74 None 11 15 Human 6.3 pKB = 6.3 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 27002221
DB01012 7725 74 None 11 15 Human 6.3 pKB = 6.3 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 22210744
DB01012 7725 74 None 11 15 Human 6.3 pKB = 6.3 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 23372019
DB01012 7725 74 None 11 15 Human 6.3 pKB = 6.3 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 25220431
DB01012 7725 74 None 11 15 Human 6.3 pKB = 6.3 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 27002221
719 7571 5 None -1 3 Human 6.3 pKB = 6.3 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 300 4 2 1 5.2 C[C@H](c1cccc2c1cccc2)NCc1cc2c([nH]1)cccc2 25220431
9882793 7571 5 None -1 3 Human 6.3 pKB = 6.3 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 300 4 2 1 5.2 C[C@H](c1cccc2c1cccc2)NCc1cc2c([nH]1)cccc2 25220431
CHEMBL1801356 7571 5 None -1 3 Human 6.3 pKB = 6.3 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 300 4 2 1 5.2 C[C@H](c1cccc2c1cccc2)NCc1cc2c([nH]1)cccc2 25220431
3947 7029 27 None - 1 Human 6.4 pKB = 6.4 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 283 2 1 3 4.2 Cc1ccc(c(c1)C)C(c1nc2c(s1)cccc2)(O)C 25220431
3947 7029 27 None - 1 Human 6.4 pKB = 6.4 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 283 2 1 3 4.2 Cc1ccc(c(c1)C)C(c1nc2c(s1)cccc2)(O)C 27002221
52943938 7029 27 None - 1 Human 6.4 pKB = 6.4 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 283 2 1 3 4.2 Cc1ccc(c(c1)C)C(c1nc2c(s1)cccc2)(O)C 25220431
52943938 7029 27 None - 1 Human 6.4 pKB = 6.4 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 283 2 1 3 4.2 Cc1ccc(c(c1)C)C(c1nc2c(s1)cccc2)(O)C 27002221
CHEMBL1256367 7029 27 None - 1 Human 6.4 pKB = 6.4 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 283 2 1 3 4.2 Cc1ccc(c(c1)C)C(c1nc2c(s1)cccc2)(O)C 25220431
CHEMBL1256367 7029 27 None - 1 Human 6.4 pKB = 6.4 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 283 2 1 3 4.2 Cc1ccc(c(c1)C)C(c1nc2c(s1)cccc2)(O)C 27002221
158797 10543 24 None - 1 Human 6.4 pKB = 6.4 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 303 7 1 2 4.6 COc1cccc(c1)[C@H](NCCCc1ccccc1Cl)C 22210744
158797 10543 24 None - 1 Human 6.4 pKB = 6.4 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 303 7 1 2 4.6 COc1cccc(c1)[C@H](NCCCc1ccccc1Cl)C 25220431
718 10543 24 None - 1 Human 6.4 pKB = 6.4 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 303 7 1 2 4.6 COc1cccc(c1)[C@H](NCCCc1ccccc1Cl)C 22210744
718 10543 24 None - 1 Human 6.4 pKB = 6.4 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 303 7 1 2 4.6 COc1cccc(c1)[C@H](NCCCc1ccccc1Cl)C 25220431
CHEMBL292376 10543 24 None - 1 Human 6.4 pKB = 6.4 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 303 7 1 2 4.6 COc1cccc(c1)[C@H](NCCCc1ccccc1Cl)C 22210744
CHEMBL292376 10543 24 None - 1 Human 6.4 pKB = 6.4 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 303 7 1 2 4.6 COc1cccc(c1)[C@H](NCCCc1ccccc1Cl)C 25220431
6918446 9654 56 None 2 6 Human 6.5 pKB = 6.5 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 22210744
6918446 9654 56 None 2 6 Human 6.5 pKB = 6.5 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 23372019
6918446 9654 56 None 2 6 Human 6.5 pKB = 6.5 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 27002221
716 9654 56 None 2 6 Human 6.5 pKB = 6.5 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 22210744
716 9654 56 None 2 6 Human 6.5 pKB = 6.5 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 23372019
716 9654 56 None 2 6 Human 6.5 pKB = 6.5 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 27002221
CHEMBL180672 9654 56 None 2 6 Human 6.5 pKB = 6.5 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 22210744
CHEMBL180672 9654 56 None 2 6 Human 6.5 pKB = 6.5 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 23372019
CHEMBL180672 9654 56 None 2 6 Human 6.5 pKB = 6.5 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 27002221
DB05695 9654 56 None 2 6 Human 6.5 pKB = 6.5 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 22210744
DB05695 9654 56 None 2 6 Human 6.5 pKB = 6.5 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 23372019
DB05695 9654 56 None 2 6 Human 6.5 pKB = 6.5 Functional
Ca<sup>2+</sup><sub>i</sub> releaseCa<sup>2+</sup><sub>i</sub> release
Guide to Pharmacology 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 27002221




Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Affinity)
# tested GPCRs
(Affinity)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
72725441 110851 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 110851 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 94913 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 94913 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 95225 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 95225 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 95222 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 95222 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 95230 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 95230 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 95241 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 95241 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 101776 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 101776 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 101776 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 94908 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 94908 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 94912 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 94912 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 110837 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 110837 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 95238 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 95238 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 94914 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 94914 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 95221 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 95221 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 95228 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 95228 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 95232 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 95232 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 95234 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 95234 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 95251 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 95251 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 95253 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 95253 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 94909 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 94909 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 94892 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 94892 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 94901 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 94901 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 94905 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 94905 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 110597 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 110597 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 110835 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 110835 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 110843 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
CHEMBL3093419 110843 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
72725211 110839 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Activation of human CaSRActivation of human CaSR
ChEMBL 527 10 1 6 5.6 O=C(Nc1nsc(-c2ccccc2)n1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.10.050
CHEMBL3093415 110839 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Activation of human CaSRActivation of human CaSR
ChEMBL 527 10 1 6 5.6 O=C(Nc1nsc(-c2ccccc2)n1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.10.050
72725273 110844 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Activation of human CaSRActivation of human CaSR
ChEMBL 560 10 1 5 6.9 O=C(Nc1nc(-c2ccccc2)c(Cl)s1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.10.050
CHEMBL3093420 110844 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Activation of human CaSRActivation of human CaSR
ChEMBL 560 10 1 5 6.9 O=C(Nc1nc(-c2ccccc2)c(Cl)s1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.10.050
72725338 110850 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Activation of human CaSRActivation of human CaSR
ChEMBL 675 11 2 7 5.8 NS(=O)(=O)c1ccc(-c2nc(NC(=O)N(CCC(c3cccc(F)c3)c3cccc(F)c3)CCN3CCOCC3)sc2Cl)cc1 10.1016/j.bmcl.2013.10.050
CHEMBL3093426 110850 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Activation of human CaSRActivation of human CaSR
ChEMBL 675 11 2 7 5.8 NS(=O)(=O)c1ccc(-c2nc(NC(=O)N(CCC(c3cccc(F)c3)c3cccc(F)c3)CCN3CCOCC3)sc2Cl)cc1 10.1016/j.bmcl.2013.10.050
72725275 110846 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Activation of human CaSRActivation of human CaSR
ChEMBL 639 11 2 7 5.5 NS(=O)(=O)c1ccc(-c2nc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)sc2Cl)cc1 10.1016/j.bmcl.2013.10.050
CHEMBL3093422 110846 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Activation of human CaSRActivation of human CaSR
ChEMBL 639 11 2 7 5.5 NS(=O)(=O)c1ccc(-c2nc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)sc2Cl)cc1 10.1016/j.bmcl.2013.10.050
72725393 110854 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Activation of human CaSRActivation of human CaSR
ChEMBL 656 12 2 8 5.2 CS(=O)(=O)Nc1ccc(-c2nsc(NC(=O)N(CCC(c3ccc(F)cc3)c3ccc(F)cc3)CCN3CCOCC3)n2)cc1 10.1016/j.bmcl.2013.10.050
CHEMBL3093430 110854 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Activation of human CaSRActivation of human CaSR
ChEMBL 656 12 2 8 5.2 CS(=O)(=O)Nc1ccc(-c2nsc(NC(=O)N(CCC(c3ccc(F)cc3)c3ccc(F)cc3)CCN3CCOCC3)n2)cc1 10.1016/j.bmcl.2013.10.050
16735684 95224 0 None - 0 Human 6.7 pEC50 = 6.7 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 525 10 1 7 4.3 Cn1nnnc1-c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1 10.1016/j.bmcl.2013.01.078
CHEMBL2349576 95224 0 None - 0 Human 6.7 pEC50 = 6.7 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 525 10 1 7 4.3 Cn1nnnc1-c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1 10.1016/j.bmcl.2013.01.078
16737311 95229 0 None - 0 Human 6.7 pEC50 = 6.7 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 577 12 1 5 6.4 O=C(OCc1ccccc1)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1 10.1016/j.bmcl.2013.01.078
CHEMBL2349581 95229 0 None - 0 Human 6.7 pEC50 = 6.7 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 577 12 1 5 6.4 O=C(OCc1ccccc1)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1 10.1016/j.bmcl.2013.01.078
16737832 95243 0 None - 0 Human 6.7 pEC50 = 6.7 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 527 10 1 4 6.0 O=C(Nc1cccc(OC(F)(F)F)c1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.078
CHEMBL2349595 95243 0 None - 0 Human 6.7 pEC50 = 6.7 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 527 10 1 4 6.0 O=C(Nc1cccc(OC(F)(F)F)c1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.078
16735042 95249 0 None - 0 Human 6.7 pEC50 = 6.7 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 519 10 1 3 6.7 O=C(Nc1cccc(-c2ccccc2)c1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.078
CHEMBL2349600 95249 0 None - 0 Human 6.7 pEC50 = 6.7 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 519 10 1 3 6.7 O=C(Nc1cccc(-c2ccccc2)c1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.078
16735043 95250 0 None - 0 Human 6.7 pEC50 = 6.7 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 520 10 1 4 6.1 O=C(Nc1cccc(-c2cccnc2)c1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.078
CHEMBL2349601 95250 0 None - 0 Human 6.7 pEC50 = 6.7 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 520 10 1 4 6.1 O=C(Nc1cccc(-c2cccnc2)c1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.078
3781744 94897 1 None - 0 Human 5.7 pEC50 = 5.7 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 388 7 2 3 4.8 COC(=O)c1cccc(NC(=O)NCCC(c2ccccc2)c2ccccc2)c1 10.1016/j.bmcl.2013.01.078
CHEMBL2346771 94897 1 None - 0 Human 5.7 pEC50 = 5.7 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 388 7 2 3 4.8 COC(=O)c1cccc(NC(=O)NCCC(c2ccccc2)c2ccccc2)c1 10.1016/j.bmcl.2013.01.078
59729031 94902 0 None - 0 Human 5.7 pEC50 = 5.7 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 422 7 2 3 5.5 COC(=O)c1cc(NC(=O)NCCC(c2ccccc2)c2ccccc2)ccc1Cl 10.1016/j.bmcl.2013.01.078
CHEMBL2346776 94902 0 None - 0 Human 5.7 pEC50 = 5.7 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 422 7 2 3 5.5 COC(=O)c1cc(NC(=O)NCCC(c2ccccc2)c2ccccc2)ccc1Cl 10.1016/j.bmcl.2013.01.078
25175471 94910 0 None - 0 Human 5.7 pEC50 = 5.7 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 478 9 1 3 6.7 COC(=O)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)Cc2ccccc2)c1 10.1016/j.bmcl.2013.01.078
CHEMBL2346783 94910 0 None - 0 Human 5.7 pEC50 = 5.7 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 478 9 1 3 6.7 COC(=O)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)Cc2ccccc2)c1 10.1016/j.bmcl.2013.01.078
16737307 95227 0 None - 0 Human 5.7 pEC50 = 5.7 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 487 10 2 4 4.8 O=C(O)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1 10.1016/j.bmcl.2013.01.078
CHEMBL2349579 95227 0 None - 0 Human 5.7 pEC50 = 5.7 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 487 10 2 4 4.8 O=C(O)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1 10.1016/j.bmcl.2013.01.078
59729016 94904 0 None - 0 Human 4.7 pEC50 = 4.7 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 374 7 3 2 4.7 O=C(NCCC(c1ccccc1)c1ccccc1)Nc1cccc(C(=O)O)c1 10.1016/j.bmcl.2013.01.078
CHEMBL2346778 94904 0 None - 0 Human 4.7 pEC50 = 4.7 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 374 7 3 2 4.7 O=C(NCCC(c1ccccc1)c1ccccc1)Nc1cccc(C(=O)O)c1 10.1016/j.bmcl.2013.01.078
58938102 110840 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Activation of human CaSRActivation of human CaSR
ChEMBL 527 10 1 6 5.6 O=C(Nc1nc(-c2ccccc2)ns1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.10.050
CHEMBL3093416 110840 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Activation of human CaSRActivation of human CaSR
ChEMBL 527 10 1 6 5.6 O=C(Nc1nc(-c2ccccc2)ns1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.10.050
58938049 110838 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Activation of human CaSRActivation of human CaSR
ChEMBL 527 10 1 6 5.6 O=C(Nc1nnc(-c2ccccc2)s1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.10.050
CHEMBL3093414 110838 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Activation of human CaSRActivation of human CaSR
ChEMBL 527 10 1 6 5.6 O=C(Nc1nnc(-c2ccccc2)s1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.10.050
72725274 110845 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activation of human CaSRActivation of human CaSR
ChEMBL 653 12 2 7 6.2 CS(=O)(=O)Nc1ccc(-c2nc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)sc2Cl)cc1 10.1016/j.bmcl.2013.10.050
CHEMBL3093421 110845 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activation of human CaSRActivation of human CaSR
ChEMBL 653 12 2 7 6.2 CS(=O)(=O)Nc1ccc(-c2nc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)sc2Cl)cc1 10.1016/j.bmcl.2013.10.050
72725336 110848 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activation of human CaSRActivation of human CaSR
ChEMBL 606 11 2 8 4.2 NS(=O)(=O)c1ccc(-c2nsc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)n2)cc1 10.1016/j.bmcl.2013.10.050
CHEMBL3093424 110848 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activation of human CaSRActivation of human CaSR
ChEMBL 606 11 2 8 4.2 NS(=O)(=O)c1ccc(-c2nsc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)n2)cc1 10.1016/j.bmcl.2013.10.050
72725152 110836 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Activation of human CaSRActivation of human CaSR
ChEMBL 520 10 1 4 6.1 O=C(Nc1cccc(-c2ccccc2)n1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.10.050
CHEMBL3093412 110836 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Activation of human CaSRActivation of human CaSR
ChEMBL 520 10 1 4 6.1 O=C(Nc1cccc(-c2ccccc2)n1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.10.050
16737665 95231 0 None - 0 Human 6.5 pEC50 = 6.5 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 543 10 1 5 6.0 CC(C)(C)OC(=O)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1 10.1016/j.bmcl.2013.01.078
CHEMBL2349583 95231 0 None - 0 Human 6.5 pEC50 = 6.5 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 543 10 1 5 6.0 CC(C)(C)OC(=O)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1 10.1016/j.bmcl.2013.01.078
16737981 95246 0 None - 0 Human 6.5 pEC50 = 6.5 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 473 10 1 4 5.1 COc1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1 10.1016/j.bmcl.2013.01.078
CHEMBL2349598 95246 0 None - 0 Human 6.5 pEC50 = 6.5 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 473 10 1 4 5.1 COc1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1 10.1016/j.bmcl.2013.01.078
16737501 95247 0 None - 0 Human 6.5 pEC50 = 6.5 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 486 10 1 4 5.1 CN(C)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1 10.1016/j.bmcl.2013.01.078
CHEMBL2349599 95247 0 None - 0 Human 6.5 pEC50 = 6.5 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 486 10 1 4 5.1 CN(C)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1 10.1016/j.bmcl.2013.01.078
71579791 95254 0 None - 0 Human 6.5 pEC50 = 6.5 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 526 10 1 5 6.2 O=C(Nc1cccc(-c2nccs2)c1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.078
CHEMBL2349605 95254 0 None - 0 Human 6.5 pEC50 = 6.5 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 526 10 1 5 6.2 O=C(Nc1cccc(-c2nccs2)c1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.078
23934373 94898 0 None - 0 Human 5.5 pEC50 = 5.5 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 402 8 2 3 5.2 CCOC(=O)c1ccc(NC(=O)NCCC(c2ccccc2)c2ccccc2)cc1 10.1016/j.bmcl.2013.01.078
CHEMBL2346772 94898 0 None - 0 Human 5.5 pEC50 = 5.5 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 402 8 2 3 5.2 CCOC(=O)c1ccc(NC(=O)NCCC(c2ccccc2)c2ccccc2)cc1 10.1016/j.bmcl.2013.01.078
59729027 94903 0 None - 0 Human 5.5 pEC50 = 5.5 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 432 6 2 1 6.7 O=C(NCCC(c1ccccc1)c1ccccc1)Nc1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2013.01.078
CHEMBL2346777 94903 0 None - 0 Human 5.5 pEC50 = 5.5 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 432 6 2 1 6.7 O=C(NCCC(c1ccccc1)c1ccccc1)Nc1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2013.01.078
16737652 95239 0 None - 0 Human 6.5 pEC50 = 6.5 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 543 10 1 4 6.7 O=C(Nc1cccc(SC(F)(F)F)c1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.078
CHEMBL2349591 95239 0 None - 0 Human 6.5 pEC50 = 6.5 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 543 10 1 4 6.7 O=C(Nc1cccc(SC(F)(F)F)c1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.078
11955209 110841 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Activation of human CaSRActivation of human CaSR
ChEMBL 526 10 1 5 6.2 O=C(Nc1nc(-c2ccccc2)cs1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.10.050
CHEMBL3093417 110841 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Activation of human CaSRActivation of human CaSR
ChEMBL 526 10 1 5 6.2 O=C(Nc1nc(-c2ccccc2)cs1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.10.050
72725337 110849 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Activation of human CaSRActivation of human CaSR
ChEMBL 675 11 2 7 5.8 NS(=O)(=O)c1ccc(-c2nc(NC(=O)N(CCC(c3ccccc3F)c3ccccc3F)CCN3CCOCC3)sc2Cl)cc1 10.1016/j.bmcl.2013.10.050
CHEMBL3093425 110849 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Activation of human CaSRActivation of human CaSR
ChEMBL 675 11 2 7 5.8 NS(=O)(=O)c1ccc(-c2nc(NC(=O)N(CCC(c3ccccc3F)c3ccccc3F)CCN3CCOCC3)sc2Cl)cc1 10.1016/j.bmcl.2013.10.050
69028630 95226 0 None - 0 Human 6.4 pEC50 = 6.4 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 572 11 1 6 5.3 COC(=O)c1cccc(NC(=O)N(CCCN2CCN(C(=O)OC)CC2)CCC(c2ccccc2)c2ccccc2)c1 10.1016/j.bmcl.2013.01.078
CHEMBL2349578 95226 0 None - 0 Human 6.4 pEC50 = 6.4 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 572 11 1 6 5.3 COC(=O)c1cccc(NC(=O)N(CCCN2CCN(C(=O)OC)CC2)CCC(c2ccccc2)c2ccccc2)c1 10.1016/j.bmcl.2013.01.078
58938036 95233 0 None - 0 Human 6.4 pEC50 = 6.4 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 647 14 1 5 7.2 O=C(OCCCC(F)(F)C(F)(F)F)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1 10.1016/j.bmcl.2013.01.078
CHEMBL2349585 95233 0 None - 0 Human 6.4 pEC50 = 6.4 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 647 14 1 5 7.2 O=C(OCCCC(F)(F)C(F)(F)F)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1 10.1016/j.bmcl.2013.01.078
16737131 95237 0 None - 0 Human 6.4 pEC50 = 6.4 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 487 11 1 4 5.2 COCc1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1 10.1016/j.bmcl.2013.01.078
CHEMBL2349589 95237 0 None - 0 Human 6.4 pEC50 = 6.4 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 487 11 1 4 5.2 COCc1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1 10.1016/j.bmcl.2013.01.078
16737836 95242 0 None - 0 Human 6.4 pEC50 = 6.4 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 575 10 1 5 5.4 O=C(Nc1cccc(S(=O)(=O)C(F)(F)F)c1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.078
CHEMBL2349594 95242 0 None - 0 Human 6.4 pEC50 = 6.4 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 575 10 1 5 5.4 O=C(Nc1cccc(S(=O)(=O)C(F)(F)F)c1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.078
16737985 95245 0 None - 0 Human 6.4 pEC50 = 6.4 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 511 9 1 3 6.1 O=C(Nc1cccc(C(F)(F)F)c1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.078
CHEMBL2349597 95245 0 None - 0 Human 6.4 pEC50 = 6.4 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 511 9 1 3 6.1 O=C(Nc1cccc(C(F)(F)F)c1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.078
3431830 94894 5 None - 0 Human 5.4 pEC50 = 5.4 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 364 6 2 1 5.7 O=C(NCCC(c1ccccc1)c1ccccc1)Nc1ccc(Cl)cc1 10.1016/j.bmcl.2013.01.078
CHEMBL2346769 94894 5 None - 0 Human 5.4 pEC50 = 5.4 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 364 6 2 1 5.7 O=C(NCCC(c1ccccc1)c1ccccc1)Nc1ccc(Cl)cc1 10.1016/j.bmcl.2013.01.078
4341046 94896 5 None - 0 Human 5.4 pEC50 = 5.4 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 364 6 2 1 5.7 O=C(NCCC(c1ccccc1)c1ccccc1)Nc1cccc(Cl)c1 10.1016/j.bmcl.2013.01.078
CHEMBL2346770 94896 5 None - 0 Human 5.4 pEC50 = 5.4 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 364 6 2 1 5.7 O=C(NCCC(c1ccccc1)c1ccccc1)Nc1cccc(Cl)c1 10.1016/j.bmcl.2013.01.078
4564558 94899 5 None - 0 Human 5.4 pEC50 = 5.4 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 344 6 2 1 5.3 Cc1ccc(NC(=O)NCCC(c2ccccc2)c2ccccc2)cc1 10.1016/j.bmcl.2013.01.078
CHEMBL2346773 94899 5 None - 0 Human 5.4 pEC50 = 5.4 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 344 6 2 1 5.3 Cc1ccc(NC(=O)NCCC(c2ccccc2)c2ccccc2)cc1 10.1016/j.bmcl.2013.01.078
59729041 94900 0 None - 0 Human 5.4 pEC50 = 5.4 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)Nc1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2013.01.078
CHEMBL2346774 94900 0 None - 0 Human 5.4 pEC50 = 5.4 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)Nc1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2013.01.078
59729011 94907 0 None - 0 Human 5.4 pEC50 = 5.4 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 378 7 2 1 5.4 O=C(NCCC(c1ccccc1)c1ccccc1)NCc1ccccc1Cl 10.1016/j.bmcl.2013.01.078
CHEMBL2346780 94907 0 None - 0 Human 5.4 pEC50 = 5.4 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 378 7 2 1 5.4 O=C(NCCC(c1ccccc1)c1ccccc1)NCc1ccccc1Cl 10.1016/j.bmcl.2013.01.078
6918446 9654 56 None - 0 Bovine 7.4 pEC50 = 7.4 Binding
Inhibition of CaSR in bovine parathyroid cells assessed as increase in PTH levelInhibition of CaSR in bovine parathyroid cells assessed as increase in PTH level
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1021/jm9018756
716 9654 56 None - 0 Bovine 7.4 pEC50 = 7.4 Binding
Inhibition of CaSR in bovine parathyroid cells assessed as increase in PTH levelInhibition of CaSR in bovine parathyroid cells assessed as increase in PTH level
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1021/jm9018756
CHEMBL180672 9654 56 None - 0 Bovine 7.4 pEC50 = 7.4 Binding
Inhibition of CaSR in bovine parathyroid cells assessed as increase in PTH levelInhibition of CaSR in bovine parathyroid cells assessed as increase in PTH level
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1021/jm9018756
DB05695 9654 56 None - 0 Bovine 7.4 pEC50 = 7.4 Binding
Inhibition of CaSR in bovine parathyroid cells assessed as increase in PTH levelInhibition of CaSR in bovine parathyroid cells assessed as increase in PTH level
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1021/jm9018756
72725212 110842 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Activation of human CaSRActivation of human CaSR
ChEMBL 544 10 1 5 6.3 O=C(Nc1nc(-c2ccccc2)c(F)s1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.10.050
CHEMBL3093418 110842 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Activation of human CaSRActivation of human CaSR
ChEMBL 544 10 1 5 6.3 O=C(Nc1nc(-c2ccccc2)c(F)s1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.10.050
16737826 95235 0 None - 0 Human 6.3 pEC50 = 6.3 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 485 10 1 4 5.3 CC(=O)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1 10.1016/j.bmcl.2013.01.078
CHEMBL2349587 95235 0 None - 0 Human 6.3 pEC50 = 6.3 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 485 10 1 4 5.3 CC(=O)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1 10.1016/j.bmcl.2013.01.078
72725276 110847 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Activation of human CaSRActivation of human CaSR
ChEMBL 620 12 2 8 5.0 CS(=O)(=O)Nc1ccc(-c2nsc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)n2)cc1 10.1016/j.bmcl.2013.10.050
CHEMBL3093423 110847 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Activation of human CaSRActivation of human CaSR
ChEMBL 620 12 2 8 5.0 CS(=O)(=O)Nc1ccc(-c2nsc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)n2)cc1 10.1016/j.bmcl.2013.10.050
71579975 94915 0 None - 0 Human 7.2 pEC50 = 7.2 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 514 11 2 5 4.8 COC(=O)c1cccc(NC(=O)N(CCCN2CCNCC2)CCC(c2ccccc2)c2ccccc2)c1 10.1016/j.bmcl.2013.01.078
CHEMBL2346788 94915 0 None - 0 Human 7.2 pEC50 = 7.2 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 514 11 2 5 4.8 COC(=O)c1cccc(NC(=O)N(CCCN2CCNCC2)CCC(c2ccccc2)c2ccccc2)c1 10.1016/j.bmcl.2013.01.078
16736327 95223 0 None - 0 Human 7.2 pEC50 = 7.2 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 525 10 1 7 4.3 Cn1nnc(-c2cccc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)c2)n1 10.1016/j.bmcl.2013.01.078
CHEMBL2349575 95223 0 None - 0 Human 7.2 pEC50 = 7.2 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 525 10 1 7 4.3 Cn1nnc(-c2cccc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)c2)n1 10.1016/j.bmcl.2013.01.078
16112870 95252 0 None - 0 Human 7.2 pEC50 = 7.2 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 510 10 1 5 5.7 O=C(Nc1cccc(-c2cnco2)c1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.078
CHEMBL2349603 95252 0 None - 0 Human 7.2 pEC50 = 7.2 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 510 10 1 5 5.7 O=C(Nc1cccc(-c2cnco2)c1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.078
71717737 94890 0 None - 0 Human 6.2 pEC50 = 6.2 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 574 11 3 5 6.7 O=C(Nc1cccc(Nc2nc3ccccc3[nH]2)c1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.078
CHEMBL2346765 94890 0 None - 0 Human 6.2 pEC50 = 6.2 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 574 11 3 5 6.7 O=C(Nc1cccc(Nc2nc3ccccc3[nH]2)c1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.078
67404227 94853 0 None - 0 Human 5.2 pEC50 = 5.2 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 358 7 2 1 5.3 C[C@@H](NC(=O)NCCC(c1ccccc1)c1ccccc1)c1ccccc1 10.1016/j.bmcl.2013.01.078
CHEMBL2346666 94853 0 None - 0 Human 5.2 pEC50 = 5.2 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 358 7 2 1 5.3 C[C@@H](NC(=O)NCCC(c1ccccc1)c1ccccc1)c1ccccc1 10.1016/j.bmcl.2013.01.078
23742117 94893 0 None - 0 Human 5.2 pEC50 = 5.2 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 364 6 2 1 5.7 O=C(NCCC(c1ccccc1)c1ccccc1)Nc1ccccc1Cl 10.1016/j.bmcl.2013.01.078
CHEMBL2346768 94893 0 None - 0 Human 5.2 pEC50 = 5.2 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 364 6 2 1 5.7 O=C(NCCC(c1ccccc1)c1ccccc1)Nc1ccccc1Cl 10.1016/j.bmcl.2013.01.078
156419 7725 74 None - 1 Human 7.1 pEC50 = 7.1 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 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2013.01.078
3308 7725 74 None - 1 Human 7.1 pEC50 = 7.1 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 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2013.01.078
647 7725 74 None - 1 Human 7.1 pEC50 = 7.1 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 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2013.01.078
CHEMBL1201284 7725 74 None - 1 Human 7.1 pEC50 = 7.1 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 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2013.01.078
DB01012 7725 74 None - 1 Human 7.1 pEC50 = 7.1 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 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2013.01.078
158797 10543 24 None - 1 Human 7.1 pEC50 = 7.1 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 303 7 1 2 4.6 COc1cccc(c1)[C@H](NCCCc1ccccc1Cl)C 10.1016/j.bmcl.2013.01.078
718 10543 24 None - 1 Human 7.1 pEC50 = 7.1 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 303 7 1 2 4.6 COc1cccc(c1)[C@H](NCCCc1ccccc1Cl)C 10.1016/j.bmcl.2013.01.078
CHEMBL292376 10543 24 None - 1 Human 7.1 pEC50 = 7.1 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 303 7 1 2 4.6 COc1cccc(c1)[C@H](NCCCc1ccccc1Cl)C 10.1016/j.bmcl.2013.01.078
24852863 94911 0 None - 0 Human 6.1 pEC50 = 6.1 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 502 9 1 5 5.9 COC(=O)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CC(=O)OC(C)(C)C)c1 10.1016/j.bmcl.2013.01.078
CHEMBL2346784 94911 0 None - 0 Human 6.1 pEC50 = 6.1 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 502 9 1 5 5.9 COC(=O)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CC(=O)OC(C)(C)C)c1 10.1016/j.bmcl.2013.01.078
16737126 95236 0 None - 0 Human 6.1 pEC50 = 6.1 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 473 10 2 4 4.6 O=C(Nc1cccc(CO)c1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.078
CHEMBL2349588 95236 0 None - 0 Human 6.1 pEC50 = 6.1 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 473 10 2 4 4.6 O=C(Nc1cccc(CO)c1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1 10.1016/j.bmcl.2013.01.078
16737306 95240 0 None - 0 Human 6.1 pEC50 = 6.1 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 505 10 1 4 4.8 C[S+]([O-])c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1 10.1016/j.bmcl.2013.01.078
CHEMBL2349592 95240 0 None - 0 Human 6.1 pEC50 = 6.1 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 505 10 1 4 4.8 C[S+]([O-])c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1 10.1016/j.bmcl.2013.01.078
16737642 95244 0 None - 0 Human 6.1 pEC50 = 6.1 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 468 9 1 4 4.9 N#Cc1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1 10.1016/j.bmcl.2013.01.078
CHEMBL2349596 95244 0 None - 0 Human 6.1 pEC50 = 6.1 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 468 9 1 4 4.9 N#Cc1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1 10.1016/j.bmcl.2013.01.078
59729051 94891 0 None - 0 Human 5.1 pEC50 = 5.1 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 COc1cccc(NC(=O)NCCC(c2ccccc2)c2ccccc2)c1 10.1016/j.bmcl.2013.01.078
CHEMBL2346766 94891 0 None - 0 Human 5.1 pEC50 = 5.1 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 COc1cccc(NC(=O)NCCC(c2ccccc2)c2ccccc2)c1 10.1016/j.bmcl.2013.01.078
72725391 110852 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activation of human CaSRActivation of human CaSR
ChEMBL 689 12 2 7 6.5 CS(=O)(=O)Nc1ccc(-c2nc(NC(=O)N(CCC(c3ccc(F)cc3)c3ccc(F)cc3)CCN3CCOCC3)sc2Cl)cc1 10.1016/j.bmcl.2013.10.050
CHEMBL3093428 110852 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activation of human CaSRActivation of human CaSR
ChEMBL 689 12 2 7 6.5 CS(=O)(=O)Nc1ccc(-c2nc(NC(=O)N(CCC(c3ccc(F)cc3)c3ccc(F)cc3)CCN3CCOCC3)sc2Cl)cc1 10.1016/j.bmcl.2013.10.050
72725392 110853 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activation of human CaSRActivation of human CaSR
ChEMBL 642 11 2 8 4.5 NS(=O)(=O)c1ccc(-c2nsc(NC(=O)N(CCC(c3ccc(F)cc3)c3ccc(F)cc3)CCN3CCOCC3)n2)cc1 10.1016/j.bmcl.2013.10.050
CHEMBL3093429 110853 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activation of human CaSRActivation of human CaSR
ChEMBL 642 11 2 8 4.5 NS(=O)(=O)c1ccc(-c2nsc(NC(=O)N(CCC(c3ccc(F)cc3)c3ccc(F)cc3)CCN3CCOCC3)n2)cc1 10.1016/j.bmcl.2013.10.050
24769038 204375 1 None - 0 Human 10.7 pIC50 = 10.7 Binding
Displacement of [3H](2-(2-hydroxyphenyl)-6-methyl-5-(2-methylpropyl)-3-(2-phenylethyl)-4(3H)-pyrimidinone) from human calcium receptor expressed in human HEK293 4.0-7 cells by liquid scintillation countingDisplacement of [3H](2-(2-hydroxyphenyl)-6-methyl-5-(2-methylpropyl)-3-(2-phenylethyl)-4(3H)-pyrimidinone) from human calcium receptor expressed in human HEK293 4.0-7 cells by liquid scintillation counting
ChEMBL 446 11 3 5 4.1 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COc1ccc(CCC(=O)O)cc1C#N 10.1021/jm900563e
CHEMBL570593 204375 1 None - 0 Human 10.7 pIC50 = 10.7 Binding
Displacement of [3H](2-(2-hydroxyphenyl)-6-methyl-5-(2-methylpropyl)-3-(2-phenylethyl)-4(3H)-pyrimidinone) from human calcium receptor expressed in human HEK293 4.0-7 cells by liquid scintillation countingDisplacement of [3H](2-(2-hydroxyphenyl)-6-methyl-5-(2-methylpropyl)-3-(2-phenylethyl)-4(3H)-pyrimidinone) from human calcium receptor expressed in human HEK293 4.0-7 cells by liquid scintillation counting
ChEMBL 446 11 3 5 4.1 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COc1ccc(CCC(=O)O)cc1C#N 10.1021/jm900563e
135454814 78175 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptorInhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor
ChEMBL 334 5 1 4 3.7 CCc1c(C)nc(-c2ccccc2O)n(CCc2ccccc2)c1=O 10.1016/j.bmcl.2005.03.054
CHEMBL195859 78175 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptorInhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor
ChEMBL 334 5 1 4 3.7 CCc1c(C)nc(-c2ccccc2O)n(CCc2ccccc2)c1=O 10.1016/j.bmcl.2005.03.054
22640863 193555 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 363 9 2 4 3.7 COc1ccc(CC(C)(C)NCC(O)COc2ccccc2Cl)cc1 10.1021/jm900364m
CHEMBL488997 193555 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 363 9 2 4 3.7 COc1ccc(CC(C)(C)NCC(O)COc2ccccc2Cl)cc1 10.1021/jm900364m
18459606 199459 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 363 9 2 4 3.7 COc1ccc(CC(C)(C)NCC(O)COc2cccc(Cl)c2)cc1 10.1021/jm900364m
CHEMBL521907 199459 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 363 9 2 4 3.7 COc1ccc(CC(C)(C)NCC(O)COc2cccc(Cl)c2)cc1 10.1021/jm900364m
22640903 190925 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 295 9 2 4 2.4 COc1ccc(CC(C)(C)NCC(O)COC(C)C)cc1 10.1021/jm900364m
CHEMBL482873 190925 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 295 9 2 4 2.4 COc1ccc(CC(C)(C)NCC(O)COC(C)C)cc1 10.1021/jm900364m
135507431 76975 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptorInhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor
ChEMBL 324 4 1 4 3.3 Cc1cc(=O)n(CCc2cccc(F)c2)c(-c2ccccc2O)n1 10.1016/j.bmcl.2005.03.054
CHEMBL194063 76975 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptorInhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor
ChEMBL 324 4 1 4 3.3 Cc1cc(=O)n(CCc2cccc(F)c2)c(-c2ccccc2O)n1 10.1016/j.bmcl.2005.03.054
135508434 77860 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptorInhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor
ChEMBL 364 5 1 4 4.2 Cc1nc(-c2ccccc2O)n(CCc2cccc(F)c2)c(=O)c1C1CC1 10.1016/j.bmcl.2005.03.054
CHEMBL195305 77860 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptorInhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor
ChEMBL 364 5 1 4 4.2 Cc1nc(-c2ccccc2O)n(CCc2cccc(F)c2)c(=O)c1C1CC1 10.1016/j.bmcl.2005.03.054
22640916 193130 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 379 9 2 4 4.2 COc1ccc(CC(C)(C)NCC(O)COc2ccc3ccccc3c2)cc1 10.1021/jm900364m
CHEMBL487511 193130 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 379 9 2 4 4.2 COc1ccc(CC(C)(C)NCC(O)COc2ccc3ccccc3c2)cc1 10.1021/jm900364m
19360456 195485 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 354 9 2 5 2.9 COc1ccc(CC(C)(C)NCC(O)COc2ccccc2C#N)cc1 10.1021/jm900364m
CHEMBL504479 195485 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 354 9 2 5 2.9 COc1ccc(CC(C)(C)NCC(O)COc2ccccc2C#N)cc1 10.1021/jm900364m
135423282 77919 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptorInhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor
ChEMBL 366 6 1 4 4.3 CCCc1c(C)nc(-c2ccccc2O)n(CCc2cccc(F)c2)c1=O 10.1016/j.bmcl.2005.03.054
CHEMBL195566 77919 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptorInhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor
ChEMBL 366 6 1 4 4.3 CCCc1c(C)nc(-c2ccccc2O)n(CCc2cccc(F)c2)c1=O 10.1016/j.bmcl.2005.03.054
135964374 139531 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptorInhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor
ChEMBL 348 4 1 3 3.8 O=C1C2CCCCC2N=C(c2ccccc2O)N1CCc1ccccc1 10.1016/j.bmcl.2005.03.054
CHEMBL369998 139531 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptorInhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor
ChEMBL 348 4 1 3 3.8 O=C1C2CCCCC2N=C(c2ccccc2O)N1CCc1ccccc1 10.1016/j.bmcl.2005.03.054
947434 70652 11 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
ChEMBL 326 4 0 3 4.3 O=c1c2ccccc2nc(-c2ccccc2)n1CCc1ccccc1 10.1016/j.bmcl.2005.01.078
CHEMBL180391 70652 11 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
ChEMBL 326 4 0 3 4.3 O=c1c2ccccc2nc(-c2ccccc2)n1CCc1ccccc1 10.1016/j.bmcl.2005.01.078
135964376 77121 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptorInhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor
ChEMBL 366 4 1 3 3.9 O=C1C2CCCCC2N=C(c2ccccc2O)N1CCc1cccc(F)c1 10.1016/j.bmcl.2005.03.054
CHEMBL194490 77121 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptorInhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor
ChEMBL 366 4 1 3 3.9 O=C1C2CCCCC2N=C(c2ccccc2O)N1CCc1cccc(F)c1 10.1016/j.bmcl.2005.03.054
135464286 69651 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
ChEMBL 394 4 1 4 4.8 O=c1c2ccc(Cl)cc2nc(-c2ccccc2O)n1CCc1cccc(F)c1 10.1016/j.bmcl.2005.01.078
CHEMBL178442 69651 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
ChEMBL 394 4 1 4 4.8 O=c1c2ccc(Cl)cc2nc(-c2ccccc2O)n1CCc1cccc(F)c1 10.1016/j.bmcl.2005.01.078
135543639 71633 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
ChEMBL 358 4 2 5 3.7 O=c1c2ccccc2nc(-c2cc(O)ccc2O)n1CCc1ccccc1 10.1016/j.bmcl.2005.01.078
CHEMBL182107 71633 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
ChEMBL 358 4 2 5 3.7 O=c1c2ccccc2nc(-c2cc(O)ccc2O)n1CCc1ccccc1 10.1016/j.bmcl.2005.01.078
135483641 143008 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptorInhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor
ChEMBL 324 4 1 4 3.3 Cc1cc(=O)n(CCc2ccccc2F)c(-c2ccccc2O)n1 10.1016/j.bmcl.2005.03.054
CHEMBL373306 143008 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptorInhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor
ChEMBL 324 4 1 4 3.3 Cc1cc(=O)n(CCc2ccccc2F)c(-c2ccccc2O)n1 10.1016/j.bmcl.2005.03.054
135540474 76426 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptorInhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor
ChEMBL 338 4 1 4 3.6 Cc1nc(-c2ccccc2O)n(CCc2cccc(F)c2)c(=O)c1C 10.1016/j.bmcl.2005.03.054
CHEMBL193498 76426 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptorInhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor
ChEMBL 338 4 1 4 3.6 Cc1nc(-c2ccccc2O)n(CCc2cccc(F)c2)c(=O)c1C 10.1016/j.bmcl.2005.03.054
135492578 70667 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
ChEMBL 378 4 1 4 4.3 O=c1c2cc(F)ccc2nc(-c2ccccc2O)n1CCc1cccc(F)c1 10.1016/j.bmcl.2005.01.078
CHEMBL180463 70667 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
ChEMBL 378 4 1 4 4.3 O=c1c2cc(F)ccc2nc(-c2ccccc2O)n1CCc1cccc(F)c1 10.1016/j.bmcl.2005.01.078
135494510 77782 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptorInhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor
ChEMBL 306 4 1 4 3.2 Cc1cc(=O)n(CCc2ccccc2)c(-c2ccccc2O)n1 10.1016/j.bmcl.2005.03.054
CHEMBL195176 77782 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptorInhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor
ChEMBL 306 4 1 4 3.2 Cc1cc(=O)n(CCc2ccccc2)c(-c2ccccc2O)n1 10.1016/j.bmcl.2005.03.054
19360455 193854 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 397 9 2 4 4.4 COc1ccc(CC(C)(C)NCC(O)COc2cccc(Cl)c2Cl)cc1 10.1021/jm900364m
CHEMBL491251 193854 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 397 9 2 4 4.4 COc1ccc(CC(C)(C)NCC(O)COc2cccc(Cl)c2Cl)cc1 10.1021/jm900364m
135964371 77878 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptorInhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor
ChEMBL 352 4 1 3 3.5 O=C1C2CCCC2N=C(c2ccccc2O)N1CCc1cccc(F)c1 10.1016/j.bmcl.2005.03.054
CHEMBL195375 77878 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptorInhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor
ChEMBL 352 4 1 3 3.5 O=C1C2CCCC2N=C(c2ccccc2O)N1CCc1cccc(F)c1 10.1016/j.bmcl.2005.03.054
135964370 140192 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptorInhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor
ChEMBL 334 4 1 3 3.4 O=C1C2CCCC2N=C(c2ccccc2O)N1CCc1ccccc1 10.1016/j.bmcl.2005.03.054
CHEMBL370503 140192 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptorInhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor
ChEMBL 334 4 1 3 3.4 O=C1C2CCCC2N=C(c2ccccc2O)N1CCc1ccccc1 10.1016/j.bmcl.2005.03.054
135422953 141427 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptorInhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor
ChEMBL 320 4 1 4 3.5 Cc1nc(-c2ccccc2O)n(CCc2ccccc2)c(=O)c1C 10.1016/j.bmcl.2005.03.054
CHEMBL371828 141427 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptorInhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor
ChEMBL 320 4 1 4 3.5 Cc1nc(-c2ccccc2O)n(CCc2ccccc2)c(=O)c1C 10.1016/j.bmcl.2005.03.054
22640800 193518 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 349 8 2 3 4.2 CC(C)(Cc1cccc2ccccc12)NCC(O)COc1ccccc1 10.1021/jm900364m
CHEMBL488736 193518 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 349 8 2 3 4.2 CC(C)(Cc1cccc2ccccc12)NCC(O)COc1ccccc1 10.1021/jm900364m
135543644 72373 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
ChEMBL 360 4 1 4 4.2 O=c1c2cc(F)ccc2nc(-c2ccccc2O)n1CCc1ccccc1 10.1016/j.bmcl.2005.01.078
CHEMBL183287 72373 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
ChEMBL 360 4 1 4 4.2 O=c1c2cc(F)ccc2nc(-c2ccccc2O)n1CCc1ccccc1 10.1016/j.bmcl.2005.01.078
15461660 193461 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 329 9 2 4 3.0 COc1ccc(CC(C)(C)NCC(O)COc2ccccc2)cc1 10.1021/jm900364m
CHEMBL488337 193461 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 329 9 2 4 3.0 COc1ccc(CC(C)(C)NCC(O)COc2ccccc2)cc1 10.1021/jm900364m
44186435 193519 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 411 9 1 4 4.7 COc1ccc(CC(C)(C)N(C)CC(O)COc2cccc(Cl)c2Cl)cc1 10.1021/jm900364m
CHEMBL488737 193519 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 411 9 1 4 4.7 COc1ccc(CC(C)(C)N(C)CC(O)COc2cccc(Cl)c2Cl)cc1 10.1021/jm900364m
44610739 96091 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of CaSRInhibition of CaSR
ChEMBL 509 11 3 4 5.3 Cc1ccc(CC(C)(C)NC[C@@H](O)CO[C@H](C)c2ccccc2[C@@H]2C[C@@H]3C[C@H]2[C@@H]2[C@H]3[C@H]2C(=O)O)cc1F 10.1021/jm9018756
CHEMBL2368751 96091 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of CaSRInhibition of CaSR
ChEMBL 509 11 3 4 5.3 Cc1ccc(CC(C)(C)NC[C@@H](O)CO[C@H](C)c2ccccc2[C@@H]2C[C@@H]3C[C@H]2[C@@H]2[C@H]3[C@H]2C(=O)O)cc1F 10.1021/jm9018756
135430601 129381 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
ChEMBL 374 4 1 4 4.5 Cc1cccc2nc(-c3ccccc3O)n(CCc3cccc(F)c3)c(=O)c12 10.1016/j.bmcl.2005.01.078
CHEMBL360226 129381 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
ChEMBL 374 4 1 4 4.5 Cc1cccc2nc(-c3ccccc3O)n(CCc3cccc(F)c3)c(=O)c12 10.1016/j.bmcl.2005.01.078
135401099 130103 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
ChEMBL 356 4 1 4 4.3 Cc1cccc2nc(-c3ccccc3O)n(CCc3ccccc3)c(=O)c12 10.1016/j.bmcl.2005.01.078
CHEMBL361623 130103 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
ChEMBL 356 4 1 4 4.3 Cc1cccc2nc(-c3ccccc3O)n(CCc3ccccc3)c(=O)c12 10.1016/j.bmcl.2005.01.078
22640808 190953 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 343 10 2 4 3.4 COc1ccc(CCC(C)(C)NCC(O)COc2ccccc2)cc1 10.1021/jm900364m
CHEMBL483080 190953 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 343 10 2 4 3.4 COc1ccc(CCC(C)(C)NCC(O)COc2ccccc2)cc1 10.1021/jm900364m
10020257 70076 1 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
ChEMBL 342 4 1 4 4.0 O=c1c2ccccc2nc(-c2cccc(O)c2)n1CCc1ccccc1 10.1016/j.bmcl.2005.01.078
CHEMBL179333 70076 1 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
ChEMBL 342 4 1 4 4.0 O=c1c2ccccc2nc(-c2cccc(O)c2)n1CCc1ccccc1 10.1016/j.bmcl.2005.01.078
6918446 9654 56 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1021/jm900364m
716 9654 56 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1021/jm900364m
CHEMBL180672 9654 56 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1021/jm900364m
DB05695 9654 56 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1021/jm900364m
44186438 193125 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 397 9 2 4 4.4 COc1ccc(CC(C)(C)NC[C@H](O)COc2cccc(Cl)c2Cl)cc1 10.1021/jm900364m
CHEMBL487508 193125 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 397 9 2 4 4.4 COc1ccc(CC(C)(C)NC[C@H](O)COc2cccc(Cl)c2Cl)cc1 10.1021/jm900364m
135418418 70319 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of CaSRInhibition of CaSR
ChEMBL 342 4 1 4 4.0 O=c1c2ccccc2nc(-c2ccccc2O)n1CCc1ccccc1 10.1021/jm9018756
CHEMBL180030 70319 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of CaSRInhibition of CaSR
ChEMBL 342 4 1 4 4.0 O=c1c2ccccc2nc(-c2ccccc2O)n1CCc1ccccc1 10.1021/jm9018756
135418418 70319 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
ChEMBL 342 4 1 4 4.0 O=c1c2ccccc2nc(-c2ccccc2O)n1CCc1ccccc1 10.1016/j.bmcl.2005.01.078
CHEMBL180030 70319 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
ChEMBL 342 4 1 4 4.0 O=c1c2ccccc2nc(-c2ccccc2O)n1CCc1ccccc1 10.1016/j.bmcl.2005.01.078
135500059 130013 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
ChEMBL 376 4 1 4 4.7 O=c1c2cc(Cl)ccc2nc(-c2ccccc2O)n1CCc1ccccc1 10.1016/j.bmcl.2005.01.078
CHEMBL361333 130013 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
ChEMBL 376 4 1 4 4.7 O=c1c2cc(Cl)ccc2nc(-c2ccccc2O)n1CCc1ccccc1 10.1016/j.bmcl.2005.01.078
44583033 192309 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 385 9 4 5 2.2 COc1ccc(CC(C)(C)NC[C@H](O)COc2cccc3[nH]c(=O)[nH]c23)cc1 10.1021/jm900364m
CHEMBL486278 192309 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 385 9 4 5 2.2 COc1ccc(CC(C)(C)NC[C@H](O)COc2cccc3[nH]c(=O)[nH]c23)cc1 10.1021/jm900364m
22640957 190926 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 309 11 2 4 2.8 CCCCOCC(O)CNC(C)(C)Cc1ccc(OC)cc1 10.1021/jm900364m
CHEMBL482874 190926 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 309 11 2 4 2.8 CCCCOCC(O)CNC(C)(C)Cc1ccc(OC)cc1 10.1021/jm900364m
22640930 166596 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 359 10 2 5 3.1 COc1ccc(CC(C)(C)NCC(O)COc2ccccc2OC)cc1 10.1021/jm900364m
CHEMBL4106263 166596 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 359 10 2 5 3.1 COc1ccc(CC(C)(C)NCC(O)COc2ccccc2OC)cc1 10.1021/jm900364m
683379 70637 14 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
ChEMBL 316 4 0 4 3.9 O=c1c2ccccc2nc(-c2ccco2)n1CCc1ccccc1 10.1016/j.bmcl.2005.01.078
CHEMBL180336 70637 14 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
ChEMBL 316 4 0 4 3.9 O=c1c2ccccc2nc(-c2ccco2)n1CCc1ccccc1 10.1016/j.bmcl.2005.01.078
683379 70637 14 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptorInhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor
ChEMBL 316 4 0 4 3.9 O=c1c2ccccc2nc(-c2ccco2)n1CCc1ccccc1 10.1016/j.bmcl.2005.03.054
CHEMBL180336 70637 14 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptorInhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor
ChEMBL 316 4 0 4 3.9 O=c1c2ccccc2nc(-c2ccco2)n1CCc1ccccc1 10.1016/j.bmcl.2005.03.054
44541354 204595 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H](2-(2-hydroxyphenyl)-6-methyl-5-(2-methylpropyl)-3-(2-phenylethyl)-4(3H)-pyrimidinone) from human calcium receptor expressed in human HEK293 4.0-7 cells by liquid scintillation countingDisplacement of [3H](2-(2-hydroxyphenyl)-6-methyl-5-(2-methylpropyl)-3-(2-phenylethyl)-4(3H)-pyrimidinone) from human calcium receptor expressed in human HEK293 4.0-7 cells by liquid scintillation counting
ChEMBL 421 11 3 4 4.2 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COc1ccc(CCC(=O)O)cc1 10.1021/jm900563e
CHEMBL572163 204595 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H](2-(2-hydroxyphenyl)-6-methyl-5-(2-methylpropyl)-3-(2-phenylethyl)-4(3H)-pyrimidinone) from human calcium receptor expressed in human HEK293 4.0-7 cells by liquid scintillation countingDisplacement of [3H](2-(2-hydroxyphenyl)-6-methyl-5-(2-methylpropyl)-3-(2-phenylethyl)-4(3H)-pyrimidinone) from human calcium receptor expressed in human HEK293 4.0-7 cells by liquid scintillation counting
ChEMBL 421 11 3 4 4.2 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COc1ccc(CCC(=O)O)cc1 10.1021/jm900563e
6918446 9654 56 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human CaSR expressed in HEK293 cellsInhibition of human CaSR expressed in HEK293 cells
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1021/jm9018756
716 9654 56 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human CaSR expressed in HEK293 cellsInhibition of human CaSR expressed in HEK293 cells
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1021/jm9018756
CHEMBL180672 9654 56 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human CaSR expressed in HEK293 cellsInhibition of human CaSR expressed in HEK293 cells
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1021/jm9018756
DB05695 9654 56 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human CaSR expressed in HEK293 cellsInhibition of human CaSR expressed in HEK293 cells
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1021/jm9018756
6918446 9654 56 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1016/j.bmcl.2005.01.078
716 9654 56 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1016/j.bmcl.2005.01.078
CHEMBL180672 9654 56 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1016/j.bmcl.2005.01.078
DB05695 9654 56 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1016/j.bmcl.2005.01.078
6918446 9654 56 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptorInhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1016/j.bmcl.2005.03.054
716 9654 56 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptorInhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1016/j.bmcl.2005.03.054
CHEMBL180672 9654 56 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptorInhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1016/j.bmcl.2005.03.054
DB05695 9654 56 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptorInhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1016/j.bmcl.2005.03.054
10161939 13722 15 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of CaSRInhibition of CaSR
ChEMBL 464 12 2 6 4.0 CCOC(=O)CCc1ccc(C#N)c(OC[C@H](O)CNC(C)(C)CC2Cc3ccccc3C2)c1 10.1021/jm9018756
CHEMBL1084514 13722 15 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of CaSRInhibition of CaSR
ChEMBL 464 12 2 6 4.0 CCOC(=O)CCc1ccc(C#N)c(OC[C@H](O)CNC(C)(C)CC2Cc3ccccc3C2)c1 10.1021/jm9018756
135517367 70328 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
ChEMBL 374 4 1 4 4.5 Cc1ccc2nc(-c3ccccc3O)n(CCc3cccc(F)c3)c(=O)c2c1 10.1016/j.bmcl.2005.01.078
CHEMBL180057 70328 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
ChEMBL 374 4 1 4 4.5 Cc1ccc2nc(-c3ccccc3O)n(CCc3cccc(F)c3)c(=O)c2c1 10.1016/j.bmcl.2005.01.078
136048766 130010 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
ChEMBL 360 4 1 4 4.2 O=c1c2ccc(F)cc2nc(-c2ccccc2O)n1CCc1ccccc1 10.1016/j.bmcl.2005.01.078
CHEMBL361316 130010 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
ChEMBL 360 4 1 4 4.2 O=c1c2ccc(F)cc2nc(-c2ccccc2O)n1CCc1ccccc1 10.1016/j.bmcl.2005.01.078
9802994 193124 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 397 9 2 4 4.4 COc1ccc(CC(C)(C)NC[C@@H](O)COc2cccc(Cl)c2Cl)cc1 10.1021/jm900364m
CHEMBL487507 193124 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 397 9 2 4 4.4 COc1ccc(CC(C)(C)NC[C@@H](O)COc2cccc(Cl)c2Cl)cc1 10.1021/jm900364m
9930235 199988 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 388 9 2 5 3.6 COc1ccc(CC(C)(C)NCC(O)COc2cccc(Cl)c2C#N)cc1 10.1021/jm900364m
CHEMBL523475 199988 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 388 9 2 5 3.6 COc1ccc(CC(C)(C)NCC(O)COc2cccc(Cl)c2C#N)cc1 10.1021/jm900364m
135524612 70258 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
ChEMBL 356 4 1 4 4.3 Cc1cccc2c(=O)n(CCc3ccccc3)c(-c3ccccc3O)nc12 10.1016/j.bmcl.2005.01.078
CHEMBL179907 70258 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
ChEMBL 356 4 1 4 4.3 Cc1cccc2c(=O)n(CCc3ccccc3)c(-c3ccccc3O)nc12 10.1016/j.bmcl.2005.01.078
44186381 190861 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 295 10 2 4 2.4 CCCOCC(O)CNC(C)(C)Cc1ccc(OC)cc1 10.1021/jm900364m
CHEMBL482462 190861 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 295 10 2 4 2.4 CCCOCC(O)CNC(C)(C)Cc1ccc(OC)cc1 10.1021/jm900364m
9476 10298 35 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of CaSRInhibition of CaSR
ChEMBL 436 11 3 5 3.5 N#Cc1ccc(cc1OC[C@@H](CNC(CC1Cc2c(C1)cccc2)(C)C)O)CCC(=O)O 10.1021/jm9018756
9910902 10298 35 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of CaSRInhibition of CaSR
ChEMBL 436 11 3 5 3.5 N#Cc1ccc(cc1OC[C@@H](CNC(CC1Cc2c(C1)cccc2)(C)C)O)CCC(=O)O 10.1021/jm9018756
CHEMBL1084513 10298 35 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of CaSRInhibition of CaSR
ChEMBL 436 11 3 5 3.5 N#Cc1ccc(cc1OC[C@@H](CNC(CC1Cc2c(C1)cccc2)(C)C)O)CCC(=O)O 10.1021/jm9018756
135457428 70605 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
ChEMBL 376 4 1 4 4.7 O=c1c2ccccc2nc(-c2ccccc2O)n1CCc1cccc(Cl)c1 10.1016/j.bmcl.2005.01.078
CHEMBL180250 70605 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
ChEMBL 376 4 1 4 4.7 O=c1c2ccccc2nc(-c2ccccc2O)n1CCc1cccc(Cl)c1 10.1016/j.bmcl.2005.01.078
135537654 77444 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptorInhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor
ChEMBL 374 4 1 4 4.2 Cc1c(C(F)(F)F)nc(-c2ccccc2O)n(CCc2ccccc2)c1=O 10.1016/j.bmcl.2005.03.054
CHEMBL195045 77444 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptorInhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor
ChEMBL 374 4 1 4 4.2 Cc1c(C(F)(F)F)nc(-c2ccccc2O)n(CCc2ccccc2)c1=O 10.1016/j.bmcl.2005.03.054
44186437 198940 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 381 9 1 3 5.4 COc1ccc(CC(C)(C)NCCCOc2cccc(Cl)c2Cl)cc1 10.1021/jm900364m
CHEMBL520396 198940 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 381 9 1 3 5.4 COc1ccc(CC(C)(C)NCCCOc2cccc(Cl)c2Cl)cc1 10.1021/jm900364m
135430131 78071 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptorInhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor
ChEMBL 366 5 1 4 4.4 Cc1nc(-c2ccccc2O)n(CCc2cccc(F)c2)c(=O)c1C(C)C 10.1016/j.bmcl.2005.03.054
CHEMBL195711 78071 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptorInhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor
ChEMBL 366 5 1 4 4.4 Cc1nc(-c2ccccc2O)n(CCc2cccc(F)c2)c(=O)c1C(C)C 10.1016/j.bmcl.2005.03.054
44186436 193520 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 411 10 1 4 5.0 COc1ccc(CC(C)(C)NCC(COc2cccc(Cl)c2Cl)OC)cc1 10.1021/jm900364m
CHEMBL488738 193520 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assayBinding affinity to human parathyroid calcium receptor 1 expressed in HEK293 4.0-7 cells by radioligand binding assay
ChEMBL 411 10 1 4 5.0 COc1ccc(CC(C)(C)NCC(COc2cccc(Cl)c2Cl)OC)cc1 10.1021/jm900364m
136086811 13498 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of CaSRInhibition of CaSR
ChEMBL 402 5 1 4 5.0 CCc1cc2c(=O)n(CCc3ccccc3F)c(-c3ccccc3O)nc2cc1C 10.1021/jm9018756
CHEMBL1083694 13498 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of CaSRInhibition of CaSR
ChEMBL 402 5 1 4 5.0 CCc1cc2c(=O)n(CCc3ccccc3F)c(-c3ccccc3O)nc2cc1C 10.1021/jm9018756
135515453 6868 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptorInhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor
ChEMBL 352 4 1 3 3.4 CCc1c(C)[nH]/c(=C\2/C=CC=CC2=O)/n(c1=O)CCc1ccccc1F 10.1016/j.bmcl.2005.03.054
713 6868 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptorInhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor
ChEMBL 352 4 1 3 3.4 CCc1c(C)[nH]/c(=C\2/C=CC=CC2=O)/n(c1=O)CCc1ccccc1F 10.1016/j.bmcl.2005.03.054
CHEMBL194764 6868 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptorInhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor
ChEMBL 352 4 1 3 3.4 CCc1c(C)[nH]/c(=C\2/C=CC=CC2=O)/n(c1=O)CCc1ccccc1F 10.1016/j.bmcl.2005.03.054
12235 10716 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Competition binding assay, dispalcement of [3H]-upacicalcet from hCaSR by unlabelled upacicalcetCompetition binding assay, dispalcement of [3H]-upacicalcet from hCaSR by unlabelled upacicalcet
Guide to Pharmacology 351 5 5 5 0.4 Cc1c(cc(cc1Cl)S(=O)(=O)O)NC(=O)NC[C@@H](C(=O)O)N 36122913
53374467 10716 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Competition binding assay, dispalcement of [3H]-upacicalcet from hCaSR by unlabelled upacicalcetCompetition binding assay, dispalcement of [3H]-upacicalcet from hCaSR by unlabelled upacicalcet
Guide to Pharmacology 351 5 5 5 0.4 Cc1c(cc(cc1Cl)S(=O)(=O)O)NC(=O)NC[C@@H](C(=O)O)N 36122913
126969137 9539 0 None - 1 Rat 8.4 pKd = 8.4 Binding
NoneNone
Drug Central 614 9 13 19 -8.9 OC[C@H]1O[C@H]([C@@H]([C@@H]1O[C@H]1O[C@@H](CN)[C@H]([C@@H]([C@H]1N)O)O)O)O[C@@H]1[C@@H](O)[C@H](N)C[C@@H]([C@H]1O[C@H]1O[C@H](CN)[C@H]([C@@H]([C@H]1N)O)O)N None
1896 9539 0 None - 1 Rat 8.4 pKd = 8.4 Binding
NoneNone
Drug Central 614 9 13 19 -8.9 OC[C@H]1O[C@H]([C@@H]([C@@H]1O[C@H]1O[C@@H](CN)[C@H]([C@@H]([C@H]1N)O)O)O)O[C@@H]1[C@@H](O)[C@H](N)C[C@@H]([C@H]1O[C@H]1O[C@H](CN)[C@H]([C@@H]([C@H]1N)O)O)N None
709 9539 0 None - 1 Rat 8.4 pKd = 8.4 Binding
NoneNone
Drug Central 614 9 13 19 -8.9 OC[C@H]1O[C@H]([C@@H]([C@@H]1O[C@H]1O[C@@H](CN)[C@H]([C@@H]([C@H]1N)O)O)O)O[C@@H]1[C@@H](O)[C@H](N)C[C@@H]([C@H]1O[C@H]1O[C@H](CN)[C@H]([C@@H]([C@H]1N)O)O)N None
8378 9539 0 None - 1 Rat 8.4 pKd = 8.4 Binding
NoneNone
Drug Central 614 9 13 19 -8.9 OC[C@H]1O[C@H]([C@@H]([C@@H]1O[C@H]1O[C@@H](CN)[C@H]([C@@H]([C@H]1N)O)O)O)O[C@@H]1[C@@H](O)[C@H](N)C[C@@H]([C@H]1O[C@H]1O[C@H](CN)[C@H]([C@@H]([C@H]1N)O)O)N None
CHEMBL184618 9539 0 None - 1 Rat 8.4 pKd = 8.4 Binding
NoneNone
Drug Central 614 9 13 19 -8.9 OC[C@H]1O[C@H]([C@@H]([C@@H]1O[C@H]1O[C@@H](CN)[C@H]([C@@H]([C@H]1N)O)O)O)O[C@@H]1[C@@H](O)[C@H](N)C[C@@H]([C@H]1O[C@H]1O[C@H](CN)[C@H]([C@@H]([C@H]1N)O)O)N None
DB00452 9539 0 None - 1 Rat 8.4 pKd = 8.4 Binding
NoneNone
Drug Central 614 9 13 19 -8.9 OC[C@H]1O[C@H]([C@@H]([C@@H]1O[C@H]1O[C@@H](CN)[C@H]([C@@H]([C@H]1N)O)O)O)O[C@@H]1[C@@H](O)[C@H](N)C[C@@H]([C@H]1O[C@H]1O[C@H](CN)[C@H]([C@@H]([C@H]1N)O)O)N None
DB00994 9539 0 None - 1 Rat 8.4 pKd = 8.4 Binding
NoneNone
Drug Central 614 9 13 19 -8.9 OC[C@H]1O[C@H]([C@@H]([C@@H]1O[C@H]1O[C@@H](CN)[C@H]([C@@H]([C@H]1N)O)O)O)O[C@@H]1[C@@H](O)[C@H](N)C[C@@H]([C@H]1O[C@H]1O[C@H](CN)[C@H]([C@@H]([C@H]1N)O)O)N None
2780 9152 106 None 630 2 Human 8.4 pKd = 8.4 Binding
NoneNone
Drug Central 204 3 3 2 1.1 OC(=O)[C@H](Cc1c[nH]c2c1cccc2)N None
6305 9152 106 None 630 2 Human 8.4 pKd = 8.4 Binding
NoneNone
Drug Central 204 3 3 2 1.1 OC(=O)[C@H](Cc1c[nH]c2c1cccc2)N None
6923516 9152 106 None 630 2 Human 8.4 pKd = 8.4 Binding
NoneNone
Drug Central 204 3 3 2 1.1 OC(=O)[C@H](Cc1c[nH]c2c1cccc2)N None
717 9152 106 None 630 2 Human 8.4 pKd = 8.4 Binding
NoneNone
Drug Central 204 3 3 2 1.1 OC(=O)[C@H](Cc1c[nH]c2c1cccc2)N None
CHEMBL54976 9152 106 None 630 2 Human 8.4 pKd = 8.4 Binding
NoneNone
Drug Central 204 3 3 2 1.1 OC(=O)[C@H](Cc1c[nH]c2c1cccc2)N None
DB00150 9152 106 None 630 2 Human 8.4 pKd = 8.4 Binding
NoneNone
Drug Central 204 3 3 2 1.1 OC(=O)[C@H](Cc1c[nH]c2c1cccc2)N None
719 7571 5 None - 1 Human 6.3 pKd = 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 300 4 2 1 5.2 C[C@H](c1cccc2c1cccc2)NCc1cc2c([nH]1)cccc2 14976203
719 7571 5 None - 1 Human 6.3 pKd = 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 300 4 2 1 5.2 C[C@H](c1cccc2c1cccc2)NCc1cc2c([nH]1)cccc2 15149704
9882793 7571 5 None - 1 Human 6.3 pKd = 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 300 4 2 1 5.2 C[C@H](c1cccc2c1cccc2)NCc1cc2c([nH]1)cccc2 14976203
9882793 7571 5 None - 1 Human 6.3 pKd = 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 300 4 2 1 5.2 C[C@H](c1cccc2c1cccc2)NCc1cc2c([nH]1)cccc2 15149704
CHEMBL1801356 7571 5 None - 1 Human 6.3 pKd = 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 300 4 2 1 5.2 C[C@H](c1cccc2c1cccc2)NCc1cc2c([nH]1)cccc2 14976203
CHEMBL1801356 7571 5 None - 1 Human 6.3 pKd = 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 300 4 2 1 5.2 C[C@H](c1cccc2c1cccc2)NCc1cc2c([nH]1)cccc2 15149704
158797 10543 24 None - 1 Human 6.5 pKd = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 7 1 2 4.6 COc1cccc(c1)[C@H](NCCCc1ccccc1Cl)C 9520489
718 10543 24 None - 1 Human 6.5 pKd = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 7 1 2 4.6 COc1cccc(c1)[C@H](NCCCc1ccccc1Cl)C 9520489
CHEMBL292376 10543 24 None - 1 Human 6.5 pKd = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 7 1 2 4.6 COc1cccc(c1)[C@H](NCCCc1ccccc1Cl)C 9520489
707 7593 0 None -1 3 Human 2.4 pKd None 2.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7531693
708 9308 0 None - 1 Rat 2.4 pKd None 2.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 24 0 0 0 -0.4 [Mg+2] 2655774
708 9308 0 None - 1 Rat 2.4 pKd None 2.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 24 0 0 0 -0.4 [Mg+2] 7816802
888 9308 0 None - 1 Rat 2.4 pKd None 2.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 24 0 0 0 -0.4 [Mg+2] 2655774
888 9308 0 None - 1 Rat 2.4 pKd None 2.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 24 0 0 0 -0.4 [Mg+2] 7816802
707 7593 0 None 1 3 Mouse 2.5 pKd None 2.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 16199532
707 7593 0 None -1 3 Rat 2.5 pKd None 2.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7816802
2780 9152 106 None 630 2 Human 3.5 pKd None 3.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 3 2 1.1 OC(=O)[C@H](Cc1c[nH]c2c1cccc2)N 10781086
2780 9152 106 None 630 2 Human 3.5 pKd None 3.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 3 2 1.1 OC(=O)[C@H](Cc1c[nH]c2c1cccc2)N 15234970
6305 9152 106 None 630 2 Human 3.5 pKd None 3.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 3 2 1.1 OC(=O)[C@H](Cc1c[nH]c2c1cccc2)N 10781086
6305 9152 106 None 630 2 Human 3.5 pKd None 3.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 3 2 1.1 OC(=O)[C@H](Cc1c[nH]c2c1cccc2)N 15234970
6923516 9152 106 None 630 2 Human 3.5 pKd None 3.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 3 2 1.1 OC(=O)[C@H](Cc1c[nH]c2c1cccc2)N 10781086
6923516 9152 106 None 630 2 Human 3.5 pKd None 3.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 3 2 1.1 OC(=O)[C@H](Cc1c[nH]c2c1cccc2)N 15234970
717 9152 106 None 630 2 Human 3.5 pKd None 3.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 3 2 1.1 OC(=O)[C@H](Cc1c[nH]c2c1cccc2)N 10781086
717 9152 106 None 630 2 Human 3.5 pKd None 3.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 3 2 1.1 OC(=O)[C@H](Cc1c[nH]c2c1cccc2)N 15234970
CHEMBL54976 9152 106 None 630 2 Human 3.5 pKd None 3.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 3 2 1.1 OC(=O)[C@H](Cc1c[nH]c2c1cccc2)N 10781086
CHEMBL54976 9152 106 None 630 2 Human 3.5 pKd None 3.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 3 2 1.1 OC(=O)[C@H](Cc1c[nH]c2c1cccc2)N 15234970
DB00150 9152 106 None 630 2 Human 3.5 pKd None 3.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 3 2 1.1 OC(=O)[C@H](Cc1c[nH]c2c1cccc2)N 10781086
DB00150 9152 106 None 630 2 Human 3.5 pKd None 3.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 3 2 1.1 OC(=O)[C@H](Cc1c[nH]c2c1cccc2)N 15234970
1103 10419 96 None - 1 Human 3.5 pKd None 3.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 202 11 4 4 -0.4 NCCCNCCCCNCCCN 9357776
710 10419 96 None - 1 Human 3.5 pKd None 3.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 202 11 4 4 -0.4 NCCCNCCCCNCCCN 9357776
CHEMBL23194 10419 96 None - 1 Human 3.5 pKd None 3.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 202 11 4 4 -0.4 NCCCNCCCCNCCCN 9357776
DB00127 10419 96 None - 1 Human 3.5 pKd None 3.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 202 11 4 4 -0.4 NCCCNCCCCNCCCN 9357776
126969137 9539 0 None - 1 Rat 4.0 pKd None 4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 614 9 13 19 -8.9 OC[C@H]1O[C@H]([C@@H]([C@@H]1O[C@H]1O[C@@H](CN)[C@H]([C@@H]([C@H]1N)O)O)O)O[C@@H]1[C@@H](O)[C@H](N)C[C@@H]([C@H]1O[C@H]1O[C@H](CN)[C@H]([C@@H]([C@H]1N)O)O)N 7816802
1896 9539 0 None - 1 Rat 4.0 pKd None 4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 614 9 13 19 -8.9 OC[C@H]1O[C@H]([C@@H]([C@@H]1O[C@H]1O[C@@H](CN)[C@H]([C@@H]([C@H]1N)O)O)O)O[C@@H]1[C@@H](O)[C@H](N)C[C@@H]([C@H]1O[C@H]1O[C@H](CN)[C@H]([C@@H]([C@H]1N)O)O)N 7816802
709 9539 0 None - 1 Rat 4.0 pKd None 4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 614 9 13 19 -8.9 OC[C@H]1O[C@H]([C@@H]([C@@H]1O[C@H]1O[C@@H](CN)[C@H]([C@@H]([C@H]1N)O)O)O)O[C@@H]1[C@@H](O)[C@H](N)C[C@@H]([C@H]1O[C@H]1O[C@H](CN)[C@H]([C@@H]([C@H]1N)O)O)N 7816802
8378 9539 0 None - 1 Rat 4.0 pKd None 4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 614 9 13 19 -8.9 OC[C@H]1O[C@H]([C@@H]([C@@H]1O[C@H]1O[C@@H](CN)[C@H]([C@@H]([C@H]1N)O)O)O)O[C@@H]1[C@@H](O)[C@H](N)C[C@@H]([C@H]1O[C@H]1O[C@H](CN)[C@H]([C@@H]([C@H]1N)O)O)N 7816802
CHEMBL184618 9539 0 None - 1 Rat 4.0 pKd None 4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 614 9 13 19 -8.9 OC[C@H]1O[C@H]([C@@H]([C@@H]1O[C@H]1O[C@@H](CN)[C@H]([C@@H]([C@H]1N)O)O)O)O[C@@H]1[C@@H](O)[C@H](N)C[C@@H]([C@H]1O[C@H]1O[C@H](CN)[C@H]([C@@H]([C@H]1N)O)O)N 7816802
DB00452 9539 0 None - 1 Rat 4.0 pKd None 4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 614 9 13 19 -8.9 OC[C@H]1O[C@H]([C@@H]([C@@H]1O[C@H]1O[C@@H](CN)[C@H]([C@@H]([C@H]1N)O)O)O)O[C@@H]1[C@@H](O)[C@H](N)C[C@@H]([C@H]1O[C@H]1O[C@H](CN)[C@H]([C@@H]([C@H]1N)O)O)N 7816802
DB00994 9539 0 None - 1 Rat 4.0 pKd None 4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 614 9 13 19 -8.9 OC[C@H]1O[C@H]([C@@H]([C@@H]1O[C@H]1O[C@@H](CN)[C@H]([C@@H]([C@H]1N)O)O)O)O[C@@H]1[C@@H](O)[C@H](N)C[C@@H]([C@H]1O[C@H]1O[C@H](CN)[C@H]([C@@H]([C@H]1N)O)O)N 7816802