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 17165 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 17165 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 156723 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 156723 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 17159 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 17159 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 17172 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 17172 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 89590 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 89590 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
719 781 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 781 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 781 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 148432 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 148432 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 151647 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 151647 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 89591 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 89591 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 89819 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 89819 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 137536 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 137536 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 137536 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 137536 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 16217 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 16217 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 167590 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 167590 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 167590 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 149789 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 149789 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 152058 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 152058 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 137420 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 137420 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 137420 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 137420 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 198422 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 198422 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 155814 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 155814 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 156468 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 156468 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 167716 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 167716 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 167716 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 154202 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 154202 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 16168 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 16168 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 161166 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 161166 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 161166 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 13353 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 13353 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 13353 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 16202 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 16202 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 148815 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 148815 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 137390 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 137390 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
719 781 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 781 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 781 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 137390 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 137390 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
719 781 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 781 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 781 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 137439 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 137439 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 137439 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 137439 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 16189 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 16189 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 197814 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 197814 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 159313 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 159313 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 89830 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 89830 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 151023 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 151023 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 157503 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 157503 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 157503 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 17164 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 17164 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 197644 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 197644 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 156675 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 156675 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 16203 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 16203 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 146845 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 146845 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 167717 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 167717 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 167717 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 16215 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 16215 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 16170 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 16170 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 16214 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 16214 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 89826 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 89826 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 142401 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 142401 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 935 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 935 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
647 935 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 935 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 935 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 149111 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 149111 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 149513 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 149513 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 150632 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 150632 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 156945 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 156945 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 935 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 935 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
647 935 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 935 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 935 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 167696 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 167696 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 167696 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 198787 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 198787 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 3742 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 3742 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 3742 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 17622 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 17622 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 137387 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 137387 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 89828 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 89828 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 89833 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 89833 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 137387 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 137387 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 89592 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 89592 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 89823 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 89823 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 89825 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 89825 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 89843 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 89843 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 89844 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 89844 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 16215 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 16215 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 146617 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 146617 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 16188 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 16188 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 197343 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 197343 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 16200 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 16200 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 167624 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 167624 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 167624 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 147273 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 147273 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 151507 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 151507 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 198794 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 198794 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 197813 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 197813 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 241 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 241 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 241 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 152570 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 152570 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 156830 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 156830 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 17161 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 17161 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 17179 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 17179 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 16201 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 16201 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 16187 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 16187 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 16204 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 16204 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 157503 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 157503 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 157503 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 148390 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 148390 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 152673 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 152673 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 153615 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 153615 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 89834 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 89834 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 89836 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 89836 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 89841 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 89841 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 89842 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 89842 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 89824 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 89824 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 89831 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 89831 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 16216 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 16216 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 157701 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 157701 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 17171 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 17171 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
719 781 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 781 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 781 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 149858 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 149858 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 152825 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 152825 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 156830 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 156830 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 17107 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 17107 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 157198 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 157198 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 167499 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 167499 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 167499 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 152935 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 152935 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 16170 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 16170 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 146096 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 146096 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 16202 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 16202 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 16171 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 16171 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 144039 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 144039 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 16169 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 16169 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 167510 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 167510 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 167510 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 152810 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 152810 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 157061 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 157061 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 158603 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 158603 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 158813 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 158813 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 150851 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 150851 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 159093 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 159093 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 17158 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 17158 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 17160 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 17160 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 143074 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 143074 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 153379 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 153379 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 89837 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 89837 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 89822 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 89822 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 89827 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 89827 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 197706 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 197706 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 167606 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 167606 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 167606 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 16203 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 16203 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 167489 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 167489 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 167489 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 89821 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 89821 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 150046 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 150046 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 158033 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 158033 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 167599 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 167599 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 167599 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 156830 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 156830 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 156830 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 156830 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 146453 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 146453 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 158559 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 158559 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 198424 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 198424 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 16214 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 16214 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 147588 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 147588 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 89829 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 89829 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 89839 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 89839 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 167509 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 167509 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 167509 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 167666 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 167666 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 167666 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 89835 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 89835 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 16191 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 16191 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 17623 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 17623 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 157922 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 157922 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 159410 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 159410 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 197449 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 197449 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 151964 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 151964 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 16200 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 16200 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 156516 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 156516 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 17170 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 17170 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 3742 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 3742 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 3742 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 89820 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 89820 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 89832 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 89832 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 89840 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 89840 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 89845 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 89845 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 16190 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 16190 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 143300 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 143300 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 167577 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 167577 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 167577 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 89838 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 89838 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 197240 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 197240 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 1593 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 1593 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 1593 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 1593 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 1593 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 141104 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 141104 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 198837 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 198837 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 198837 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 2859 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 2859 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 2859 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 2859 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 197573 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 197573 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 200283 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 200283 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 167717 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 167717 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 167717 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 167599 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 167599 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 167599 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 60163 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 60163 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 60163 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 60163 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 167696 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 167696 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 167696 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 200343 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 200343 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 199402 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 199402 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 16015 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 16015 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 60140 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 60140 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 60140 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 60164 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 60164 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 60164 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 200432 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 200432 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 19242 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 19242 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 19242 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 19242 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 134950 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 134950 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 187512 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 187512 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 15947 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 15947 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 72762 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 72762 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 173589 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 173589 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 201312 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 201312 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 174440 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 174440 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 60136 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 60136 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 60136 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 60139 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 60139 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 60139 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 60173 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 60173 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 60173 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 15966 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 15966 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 58046 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 58046 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 185506 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 185506 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 167666 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 167666 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 167666 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 19130 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 19130 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 185137 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 185137 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 200613 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 200613 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 200669 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 200669 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 168408 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 168408 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 167624 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 167624 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 167624 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 72840 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 72840 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 141144 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 141144 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 96828 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 96828 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 1546 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 1546 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 1546 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 58761 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 58761 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 58766 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 58766 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 201128 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 201128 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 200345 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 200345 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 6600 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 6600 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 72743 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 72743 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 58889 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 58889 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 199301 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 199301 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 200466 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 200466 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 15930 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 15930 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 167489 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 167489 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 167489 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 172784 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 172784 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 141177 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 141177 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 140681 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 140681 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 73337 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 73337 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 15964 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 15964 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 58764 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 58764 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 189713 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 189713 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 6528 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 6528 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 6596 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 6596 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 72613 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 72613 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 135198 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 135198 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 135406 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 135406 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 200257 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 200257 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 3344 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 3344 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 3344 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 3344 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 16012 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 16012 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 174026 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 174026 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 187676 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 187676 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 189021 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 189021 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 6364 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 6364 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 58955 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 58955 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 187557 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 187557 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 58044 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 58044 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 174027 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 174027 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 72878 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 72878 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 96638 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 96638 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 200230 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 200230 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 15967 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 15967 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 6488 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 6488 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 72106 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 72106 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 189540 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 189540 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 58958 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 58958 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 141114 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 141114 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 199403 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 199403 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 6468 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 6468 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 6527 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 6527 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 13883 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 13883 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 13883 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 15905 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 15905 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 58040 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 58040 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 58045 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 58045 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 62685 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 62685 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 200577 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 200577 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 189195 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 189195 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 15932 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 15932 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 179207 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 179207 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 200195 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 200195 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 141166 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 141166 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 15671 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 15671 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 15948 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 15948 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 72672 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 72672 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 15907 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 15907 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 15909 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 15909 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 15874 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 15874 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 176777 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 176777 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 60165 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 60165 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 60165 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 16033 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 16033 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 167510 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 167510 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 167510 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 60137 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 60137 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 60137 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 60147 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 60147 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 60147 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 60162 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 60162 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 60162 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 60147 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 60147 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 60147 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 60133 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 60133 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 60133 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 199297 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 199297 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 200258 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 200258 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 16032 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 16032 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 201349 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 201349 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 141136 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 141136 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 188918 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 188918 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 6467 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 6467 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 6672 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 6672 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 6847 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 6847 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 141165 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 141165 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 141189 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 141189 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 141108 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 141108 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 15949 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 15949 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 6465 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 6465 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 179169 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 179169 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 200640 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 200640 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 200671 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 200671 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 15908 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 15908 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 15929 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 15929 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 175811 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 175811 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 6597 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 6597 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 6976 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 6976 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 174022 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 174022 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 202052 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 202052 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 58042 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 58042 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 72672 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 72672 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 6791 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 6791 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 7322 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 7322 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 7322 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 7322 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 58048 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 58048 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 58953 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 58953 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 2859 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 2859 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 2859 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 2859 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 62681 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 62681 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 202321 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 202321 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 58043 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 58043 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 75008 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 75008 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 165973 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 165973 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 15968 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 15968 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 58760 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 58760 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 62683 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 62683 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 12824 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 12824 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 12824 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 185323 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 185323 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 185710 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 185710 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 72628 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 72628 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 15873 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 15873 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 72613 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 72613 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 15686 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 15686 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 2859 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 2859 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 2859 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 2859 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 12848 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 12848 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 12848 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 133438 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 133438 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 201393 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 201393 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 141077 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 141077 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 30 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 30 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 30 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 133497 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 133497 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 200534 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 200534 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 141139 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 141139 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 193211 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 193211 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 141325 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 141325 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 200535 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 200535 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 58767 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 58767 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 60166 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 60166 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 60166 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 200256 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 200256 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 58956 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 58956 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 58950 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 58950 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 200467 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 200467 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 200344 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 200344 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 58954 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 58954 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 141104 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 141104 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 1593 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 1593 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 1593 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 1593 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 1593 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 6793 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 6793 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 62612 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 62612 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 60134 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 60134 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 60134 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 58765 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 58765 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 60148 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 60148 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 60148 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 167509 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 167509 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 167509 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 7109 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 7109 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 193207 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 193207 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 19150 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 19150 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 58886 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 58886 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 3344 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 3344 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 3344 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 3344 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 12870 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 12870 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 12870 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 200641 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 200641 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 73016 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 73016 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 187321 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 187321 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 187513 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 187513 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 15688 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 15688 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 72858 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 72858 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 185259 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 185259 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 62682 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 62682 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 62611 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 62611 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 62686 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 62686 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 175810 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 175810 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 176982 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 176982 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 15672 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 15672 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 6463 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 6463 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 72943 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 72943 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 6489 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 6489 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 200576 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 200576 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 58768 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 58768 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 135408 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 135408 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 141089 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 141089 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 16013 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 16013 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 16014 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 16014 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 58047 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 58047 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 60160 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 60160 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 60160 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 60163 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 60163 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 60163 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 60163 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 200285 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 200285 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 200286 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 200286 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 167499 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 167499 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 167499 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 512 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 512 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 512 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 58952 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 58952 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 60167 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 60167 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 60167 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 60132 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 60132 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 60132 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 58887 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 58887 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 58758 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 58758 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 58758 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 19095 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 19095 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 19095 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 19095 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 19177 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 19177 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 187558 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 187558 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 7321 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 7321 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 7358 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 7358 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 15687 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 15687 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 6792 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 6792 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 194746 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 194746 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 60131 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 60131 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 60131 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 141164 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 141164 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 141105 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 141105 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 2859 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 2859 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 2859 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 2859 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 199206 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 199206 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 72879 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 72879 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 15904 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 15904 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 189109 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 189109 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 141107 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 141107 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 173940 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 173940 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 15674 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 15674 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 15689 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 15689 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 58049 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 58049 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 58769 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 58769 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 58758 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 58758 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 58758 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 15910 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 15910 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 185760 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 185760 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 186263 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 186263 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 2859 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 2859 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 2859 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 2859 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 72842 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 72842 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 62684 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 62684 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 141115 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 141115 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 15931 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 15931 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 185259 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 185259 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 200668 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 200668 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 2859 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 2859 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 2859 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 2859 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 19223 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 19223 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 6601 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 6601 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 12847 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 12847 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 12847 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 6387 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 6387 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 200672 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 200672 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 62608 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 62608 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 6975 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 6975 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 124083 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 124083 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 124083 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 124083 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 6469 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 6469 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 141082 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 141082 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 19243 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 19243 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 60172 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 60172 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 60172 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 15965 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 15965 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 62610 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 62610 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 60138 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 60138 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 60138 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 200372 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 200372 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 58762 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 58762 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 60161 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 60161 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 60161 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 175240 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 175240 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 15673 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 15673 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 72721 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 72721 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 72575 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 72575 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 6848 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 6848 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 72608 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 72608 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 184801 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 184801 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 141134 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 141134 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 200578 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 200578 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 72979 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 72979 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 179286 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 179286 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 200282 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 200282 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 58959 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 58959 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 58957 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 58957 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 141091 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 141091 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 58951 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 58951 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 167716 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 167716 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 167716 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 187376 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 187376 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 200536 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 200536 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 6588 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 6588 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 19194 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 19194 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 174021 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 174021 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 6595 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 6595 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 6589 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 6589 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 73093 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 73093 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 19207 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 19207 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 1003 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 1003 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 1003 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 7110 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 7110 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 141101 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 141101 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 15933 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 15933 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 15950 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 15950 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 72623 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 72623 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 157503 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 157503 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 157503 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 199302 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 199302 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 58763 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 58763 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 1000 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 1000 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 1000 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 58885 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 58885 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 7240 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 7240 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 7212 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 7212 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 141355 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 141355 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 72684 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 72684 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 199510 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 199510 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 141097 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 141097 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 167606 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 167606 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 167606 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 13911 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 13911 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 13911 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 62609 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 62609 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 6464 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 6464 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 72826 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 72826 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 58041 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 58041 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 19096 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 19096 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 73040 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 73040 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 1576 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 1576 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 1576 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 1576 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 94972 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 94972 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 94972 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 94972 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 94972 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 94972 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 1593 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 1593 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 1593 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 1593 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 1593 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 935 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 935 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
647 935 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 935 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 935 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 1576 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 1576 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 1576 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 1576 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 1593 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 1593 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 1593 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 1593 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 1593 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 935 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 935 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
647 935 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 935 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 935 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 241 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 241 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 241 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 512 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 512 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 512 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 1546 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 1546 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 1546 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 780 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
714 780 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 780 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 1003 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 1003 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 1003 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 3344 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 3344 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 3344 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 3344 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 3499 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 3499 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 3499 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 2859 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 2859 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 2859 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 2859 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 2859 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 2859 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 2859 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 2859 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 3246 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 3246 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 3246 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 530 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 530 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 30 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 30 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 30 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 1000 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 1000 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 1000 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 1153 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 1153 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 1153 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 80 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 80 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 80 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 935 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 935 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 935 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 935 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 935 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 935 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 935 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 935 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
647 935 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
647 935 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
647 935 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
647 935 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 935 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 935 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 935 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 935 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 935 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 935 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 935 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 935 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
719 781 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 781 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 781 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 241 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 241 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 241 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 241 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 241 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 241 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 3742 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 3742 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 3742 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 3742 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 3742 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 3742 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 2859 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 2859 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 2859 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 2859 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 2859 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 2859 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 2859 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 2859 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 2859 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 2859 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 2859 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 2859 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 104047 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 104047 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 88109 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 88109 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 88421 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 88421 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 88418 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 88418 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 88426 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 88426 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 88437 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 88437 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 94972 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 94972 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 94972 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 88104 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 88104 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 88108 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 88108 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 104033 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 104033 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 88434 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 88434 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 88110 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 88110 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 88417 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 88417 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 88424 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 88424 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 88428 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 88428 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 88430 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 88430 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 88447 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 88447 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 88449 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 88449 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 88105 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 88105 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 88088 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 88088 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 88097 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 88097 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 88101 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 88101 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 103793 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 103793 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 104031 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 104031 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 104039 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 104039 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 104035 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 104035 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 104040 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 104040 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 104046 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 104046 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 104042 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 104042 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 104050 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 104050 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 88420 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 88420 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 88425 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 88425 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 88439 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 88439 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 88445 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 88445 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 88446 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 88446 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 88093 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 88093 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 88098 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 88098 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 88106 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 88106 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 88423 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 88423 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 88100 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 88100 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 104036 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 104036 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 104034 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 104034 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 104041 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 104041 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 104044 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 104044 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 104032 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 104032 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 88427 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 88427 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 88442 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 88442 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 88443 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 88443 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 88450 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 88450 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 88094 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 88094 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 88099 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 88099 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 88435 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 88435 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 104037 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 104037 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 104045 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 104045 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 88422 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 88422 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 88429 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 88429 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 88433 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 88433 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 88438 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 88438 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 88441 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 88441 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 88090 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 88090 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 88092 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 88092 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 88095 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 88095 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 88096 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 88096 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 88103 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 88103 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 2859 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 2859 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 2859 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 2859 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 104038 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 104038 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 88431 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 88431 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 104043 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 104043 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 88111 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 88111 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 88419 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 88419 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 88448 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 88448 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 88086 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 88086 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 88049 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 88049 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 88089 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 88089 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 935 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 935 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
647 935 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 935 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 935 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 3742 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 3742 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 3742 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 88107 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 88107 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 88432 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 88432 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 88436 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 88436 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 88440 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 88440 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 88087 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 88087 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 104048 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 104048 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 104049 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 104049 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 197573 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 197573 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 71371 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 71371 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 186752 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 186752 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 192656 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 192656 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 184122 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 184122 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 70171 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 70171 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 71056 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 71056 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 186327 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 186327 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 188682 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 188682 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 71115 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 71115 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 132728 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 132728 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 63848 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 63848 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 70317 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 70317 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 62847 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 62847 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 64829 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 64829 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 136205 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 136205 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 69622 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 69622 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 63863 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 63863 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 70978 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 70978 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 187051 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 187051 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 71074 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 71074 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 133389 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 133389 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 134624 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 134624 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 186715 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 186715 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 65569 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 65569 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 186658 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 186658 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 186716 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 186716 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 89287 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 89287 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 122577 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 122577 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 123299 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 123299 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 184150 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 184150 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 63272 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 63272 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 2859 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 2859 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 2859 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 2859 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 186322 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 186322 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 63515 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 63515 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 63515 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 63515 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 123209 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 123209 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 185506 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 185506 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 184123 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 184123 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 159793 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 159793 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 63833 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 63833 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 63833 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 63833 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 197793 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 197793 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 2859 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 2859 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 2859 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 2859 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 2859 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 2859 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 2859 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 2859 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 2859 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 2859 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 2859 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 2859 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 6918 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 6918 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 63524 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 63524 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 123206 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 123206 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 186321 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 186321 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 193185 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 193185 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 63454 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 63454 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 184058 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 184058 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 3499 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 3499 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 3499 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 63801 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 63801 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 70640 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 70640 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 192137 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 192137 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 71267 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 71267 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 186717 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 186717 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 6694 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 6694 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 80 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 80 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 80 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 3913 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 3913 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 2743 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 2743 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 2743 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 2743 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 2743 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 2743 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 2743 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 2358 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 2358 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 2358 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 2358 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 2358 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 2358 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
719 781 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
719 781 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 781 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 781 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 781 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 781 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 3742 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 3742 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 3742 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
707 803 0 None -1 3 Human 2.4 pKd None 2.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7531693
708 2513 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 2513 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 2513 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 2513 0 None - 1 Rat 2.4 pKd None 2.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 24 0 0 0 -0.4 [Mg+2] 7816802
707 803 0 None 1 3 Mouse 2.5 pKd None 2.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 16199532
707 803 0 None -1 3 Rat 2.5 pKd None 2.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7816802
2780 2358 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 2358 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 2358 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 2358 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 2358 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 2358 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 2358 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 2358 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 2358 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 2358 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 2358 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 2358 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 3620 96 None - 1 Human 3.5 pKd None 3.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 202 11 4 4 -0.4 NCCCNCCCCNCCCN 9357776
710 3620 96 None - 1 Human 3.5 pKd None 3.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 202 11 4 4 -0.4 NCCCNCCCCNCCCN 9357776
CHEMBL23194 3620 96 None - 1 Human 3.5 pKd None 3.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 202 11 4 4 -0.4 NCCCNCCCCNCCCN 9357776
DB00127 3620 96 None - 1 Human 3.5 pKd None 3.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 202 11 4 4 -0.4 NCCCNCCCCNCCCN 9357776
126969137 2743 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 2743 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 2743 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 2743 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 2743 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 2743 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 2743 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