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 17000 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 17000 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 156194 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 156194 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 16994 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 16994 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 17007 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 17007 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 89175 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 89175 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
719 770 2 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 770 2 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 770 2 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 147912 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 147912 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 151127 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 151127 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 89176 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 89176 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 89404 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 89404 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 137023 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 137023 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 137023 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 137023 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 16058 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 16058 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 167042 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 167042 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 167042 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 149269 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 149269 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 151538 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 151538 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 136907 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 136907 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 136907 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 136907 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 196758 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 196758 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 155285 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 155285 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 155939 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 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 155939 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 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 167168 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 167168 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 167168 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 153680 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 153680 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 16009 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 16009 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 160631 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 160631 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 160631 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 13259 1 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 13259 1 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 13259 1 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 16043 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 16043 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 148295 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 148295 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 136877 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 136877 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
719 770 2 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 770 2 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 770 2 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 136877 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 136877 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
719 770 2 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 770 2 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 770 2 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 136926 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 136926 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 136926 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 136926 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 16030 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 16030 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 196150 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 196150 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 158778 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 158778 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 89415 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 89415 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 150503 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 150503 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 156973 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 156973 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 156973 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 16999 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 16999 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 195980 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 195980 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 156146 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 156146 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 16044 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 16044 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 146325 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 146325 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 167169 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 167169 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 167169 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 16056 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 16056 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 16011 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 16011 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 16055 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 16055 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 89411 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 89411 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 141882 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 141882 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 923 68 None - 1 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 923 68 None - 1 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
647 923 68 None - 1 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 923 68 None - 1 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 923 68 None - 1 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 148591 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 148591 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 148993 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 148993 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 150111 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 150111 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 156415 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 156415 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 923 68 None - 1 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 923 68 None - 1 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
647 923 68 None - 1 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 923 68 None - 1 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 923 68 None - 1 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 167148 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 167148 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 167148 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 197122 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 197122 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 3700 20 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 3700 20 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 3700 20 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 17457 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 17457 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 136874 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 136874 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 89413 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 89413 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 89418 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 89418 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 136874 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 136874 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 89177 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 89177 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 89408 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 89408 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 89410 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 89410 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 89428 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 89428 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 89429 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 89429 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 16056 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 16056 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 146097 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 146097 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 16029 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 16029 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 195680 7 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 195680 7 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 16041 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 16041 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 167076 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 167076 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 167076 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 146753 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 146753 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 150987 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 150987 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 197129 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 197129 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 196149 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 196149 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 239 21 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 239 21 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 239 21 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 152050 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 152050 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 156300 3 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 156300 3 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 16996 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 16996 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 17014 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 17014 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 16042 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 16042 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 16028 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 16028 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 16045 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 16045 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 156973 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 156973 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 156973 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 147870 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 147870 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 152153 4 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 152153 4 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 153093 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 153093 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 89419 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 89419 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 89421 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 89421 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 89426 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 89426 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 89427 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 89427 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 89409 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 89409 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 89416 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 89416 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 16057 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 16057 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 157171 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 157171 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 17006 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 17006 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
719 770 2 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 770 2 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 770 2 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 149338 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 149338 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 152305 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 152305 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 156300 3 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 156300 3 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 16943 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 16943 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 156668 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 156668 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 166951 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 166951 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 166951 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 152414 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 152414 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 16011 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 16011 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 145576 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 145576 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 16043 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 16043 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 16012 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 16012 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 143520 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 143520 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 16010 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 16010 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 166962 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 166962 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 166962 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 152290 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 152290 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 156531 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 156531 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 158069 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 158069 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 158279 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 158279 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 150330 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 150330 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 158559 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 158559 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 16993 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 16993 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 16995 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 16995 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 142555 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 142555 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 152857 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 152857 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 89422 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 89422 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 89407 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 89407 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 89412 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 89412 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 196042 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 196042 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 167058 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 167058 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 167058 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 16044 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 16044 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 166941 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 166941 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 166941 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 89406 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 89406 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 149526 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 149526 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 157501 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 157501 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 167051 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 167051 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 167051 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 156300 3 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 156300 3 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 156300 3 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 156300 3 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 145933 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 145933 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 158025 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 158025 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 196760 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 196760 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 16055 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 16055 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 147068 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 147068 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 89414 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 89414 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 89424 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 89424 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 166961 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 166961 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 166961 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 167118 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 167118 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 167118 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 89420 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 89420 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 16032 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 16032 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 17458 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 17458 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 157391 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 157391 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 158875 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 158875 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 195786 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 195786 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 151444 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 151444 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 16041 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 16041 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 155987 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 155987 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 17005 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 17005 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 3700 20 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 3700 20 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 3700 20 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 89405 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 89405 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 89417 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 89417 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 89425 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 89425 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 89430 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 89430 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 16031 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 16031 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 142781 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 142781 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 167029 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 167029 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 167029 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 89423 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 89423 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 195577 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 195577 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 1570 21 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 1570 21 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 1570 21 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 1570 21 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 1570 21 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 140585 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 140585 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 197172 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 197172 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 197172 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 2823 52 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 2823 52 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 2823 52 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 2823 52 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 195909 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 195909 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 198612 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 198612 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 167169 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 167169 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 167169 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 167051 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 167051 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 167051 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 59862 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 59862 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 59862 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 59862 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 167148 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 167148 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 167148 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 198672 1 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 198672 1 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 197734 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 197734 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 15856 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 15856 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 59839 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 59839 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 59839 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 59863 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 59863 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 59863 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 198761 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 198761 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 19063 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 19063 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 19063 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 19063 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 134439 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 134439 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 186943 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 186943 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 15788 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 15788 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 72431 0 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 72431 0 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 173031 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 173031 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 199640 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 199640 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 173882 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 173882 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 59835 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 59835 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 59835 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 59838 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 59838 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 59838 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 59872 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 59872 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 59872 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 15807 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 15807 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 57755 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 57755 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 184938 0 None -173 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 184938 0 None -173 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 167118 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 167118 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 167118 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 18954 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 18954 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 184568 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 184568 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 198942 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 198942 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 198998 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 198998 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 167857 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 167857 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 167076 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 167076 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 167076 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 72509 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 72509 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 140625 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 140625 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 96396 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 96396 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 1523 8 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 1523 8 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 1523 8 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 58468 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 58468 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 58473 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 58473 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 199456 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 199456 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 198674 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 198674 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 6539 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 6539 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 72412 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 72412 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 58596 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 58596 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 197634 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 197634 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 198795 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 198795 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 15771 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 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 15771 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 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 166941 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 166941 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 166941 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 172229 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 172229 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 140658 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 140658 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 140162 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 140162 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 73004 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 73004 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 15805 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 15805 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 58471 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 58471 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 189135 11 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 189135 11 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 6467 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 6467 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 6535 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 6535 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 72282 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 72282 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 134687 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 134687 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 134895 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 134895 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 198586 18 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 198586 18 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 3305 10 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 3305 10 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 3305 10 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 3305 10 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 15853 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 15853 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 173468 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 173468 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 187107 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 187107 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 188448 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 188448 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 6304 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 6304 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 58661 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 58661 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 186988 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 186988 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 57753 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 57753 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 173469 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 173469 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 72547 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 72547 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 96206 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 96206 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 198559 37 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 198559 37 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 15808 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 15808 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 6427 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 6427 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 71776 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 71776 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 188963 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 188963 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 58664 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 58664 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 140595 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 140595 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 197735 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 197735 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 6407 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 6407 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 6466 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 6466 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 13787 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 13787 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 13787 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 15746 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 15746 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 57749 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 57749 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 57754 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 57754 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 62371 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 62371 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 198906 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 198906 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 188620 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 188620 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 15773 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 15773 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 178642 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 178642 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 198524 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 198524 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 140647 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 140647 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 15512 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 15512 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 15789 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 15789 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 72341 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 72341 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 15748 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 15748 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 15750 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 15750 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 15715 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 15715 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 176217 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 176217 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 59864 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 59864 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 59864 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 15874 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 15874 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 166962 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 166962 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 166962 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 59836 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 59836 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 59836 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 59846 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 59846 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 59846 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 59861 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 59861 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 59861 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 59846 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 59846 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 59846 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 59832 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 59832 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 59832 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 197630 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 197630 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 198587 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 198587 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 15873 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 15873 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 199677 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 199677 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 140617 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 140617 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 188345 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 188345 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 6406 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 6406 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 6611 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 6611 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 6786 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 6786 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 140646 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 140646 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 140670 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 140670 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 140589 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 140589 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 15790 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 15790 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 6404 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 6404 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 178604 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 178604 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 198969 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 322 4 0 4 4.2 CCc1ccc(-c2nc(=O)n(C(C)C)c3ccc(OC)cc23)cc1 10.1021/jm901811v
CHEMBL599664 198969 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 322 4 0 4 4.2 CCc1ccc(-c2nc(=O)n(C(C)C)c3ccc(OC)cc23)cc1 10.1021/jm901811v
45139809 199000 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 199000 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 15749 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 15749 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 15770 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 15770 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 175252 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 175252 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 6536 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 6536 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 6915 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 6915 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 173464 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 173464 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 200381 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 200381 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 57751 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 57751 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 72341 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 72341 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 6730 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 6730 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 7258 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 7258 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 7258 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 7258 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 57757 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 57757 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 58659 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 58659 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 2823 52 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 2823 52 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 2823 52 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 2823 52 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 62367 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 62367 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 200648 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 200648 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 57752 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 449 12 3 4 4.9 C[C@@H](OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1CCC(=O)O 10.1021/ml100268k
CHEMBL1672966 57752 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 449 12 3 4 4.9 C[C@@H](OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1CCC(=O)O 10.1021/ml100268k
44405849 74672 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 74672 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 165433 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 165433 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 15809 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 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 15809 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 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 58467 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 58467 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 62369 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 62369 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 12732 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 12732 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 12732 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 184755 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 184755 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 185142 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 185142 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 72297 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 72297 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 15714 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 15714 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 72282 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 72282 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 15527 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 15527 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 2823 52 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 2823 52 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 2823 52 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 2823 52 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 12756 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 12756 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 12756 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 132929 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 132929 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 199721 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 199721 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 140558 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 140558 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 132986 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 132986 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 198863 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 198863 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 140620 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 140620 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 192622 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 192622 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 140807 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 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 140807 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 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 198864 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 198864 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 58474 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 58474 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 59865 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 59865 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 59865 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 198585 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 198585 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 58662 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 58662 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 58656 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 58656 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 198796 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 410 6 1 4 5.7 C=CCc1c(O)ccc2c1c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1ccccc1 10.1021/jm901811v
CHEMBL598638 198796 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 410 6 1 4 5.7 C=CCc1c(O)ccc2c1c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1ccccc1 10.1021/jm901811v
45141172 198673 33 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 198673 33 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 58660 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 58660 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 140585 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 140585 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 1570 21 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 1570 21 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 1570 21 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 1570 21 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 1570 21 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 6732 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 6732 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 62298 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 62298 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 59833 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 59833 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 59833 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 58472 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 58472 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 59847 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 59847 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 59847 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 166961 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 166961 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 166961 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 7047 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 7047 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 192618 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 192618 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 18973 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 18973 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 58593 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 58593 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 3305 10 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 3305 10 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 3305 10 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 3305 10 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 12778 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 12778 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 12778 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 198970 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 198970 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 72683 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 72683 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 186752 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 186752 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 186944 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 186944 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 15529 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 15529 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 72527 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 72527 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 184691 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 184691 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 62368 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 62368 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 62297 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 62297 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 62372 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 62372 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 175251 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 175251 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 176422 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 176422 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 15513 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 15513 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 6402 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 6402 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 72611 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 72611 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 6428 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 6428 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 198905 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 198905 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 58475 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 58475 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 134897 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 134897 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 140570 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 140570 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 15854 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 15854 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 15855 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 15855 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 57756 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 57756 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 59859 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 59859 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 59859 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 59862 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 59862 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 59862 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 59862 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 198614 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 198614 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 198615 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 198615 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 166951 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 166951 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 166951 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 510 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 510 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 510 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 58658 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 58658 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 59866 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 59866 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 59866 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 59831 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 59831 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 59831 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 58594 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 58594 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 58465 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 58465 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 58465 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 18920 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 18920 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 18920 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 18920 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 18999 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 18999 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 186989 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 186989 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 7257 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 7257 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 7294 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 7294 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 15528 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 15528 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 6731 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 6731 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 193091 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 193091 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 59830 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 59830 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 59830 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 140645 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 140645 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 140586 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 140586 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 2823 52 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 2823 52 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 2823 52 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 2823 52 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 197540 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 197540 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 72548 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 72548 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 15745 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 15745 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 188534 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 188534 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 140588 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 140588 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 173382 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 173382 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 15515 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 15515 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 15530 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 15530 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 57758 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 57758 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 58476 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 58476 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 58465 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 58465 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 58465 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 15751 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 15751 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 185192 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 185192 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 185695 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 185695 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 2823 52 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 2823 52 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 2823 52 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 2823 52 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 72511 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 72511 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 62370 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 62370 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 140596 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 140596 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 15772 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 15772 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 184691 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 184691 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 198997 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 198997 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 2823 52 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 2823 52 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 2823 52 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 2823 52 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 19044 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 19044 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 6540 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 6540 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 12755 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 12755 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 12755 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 6327 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 6327 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 199001 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 199001 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 62294 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 62294 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 6914 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 6914 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 123577 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 123577 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 123577 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 123577 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 6408 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 6408 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 140563 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 140563 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 19064 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 19064 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 59871 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 59871 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 59871 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 15806 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 15806 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 62296 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 62296 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 59837 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 59837 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 59837 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 198701 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 198701 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 58469 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 58469 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 59860 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 59860 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 59860 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 174682 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 174682 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 15514 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 15514 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 72390 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 72390 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 72244 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 72244 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 6787 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 6787 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 72277 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 72277 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 184232 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 184232 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 140615 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 140615 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 198907 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 198907 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 72647 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 72647 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 178720 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 178720 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 198611 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 198611 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 58665 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 58665 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 58663 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 58663 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 140572 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 140572 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 58657 2 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 58657 2 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 167168 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 167168 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 167168 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 186807 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 186807 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 198865 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 198865 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 6527 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 6527 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 19015 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 19015 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 173463 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 173463 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 6534 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 6534 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 6528 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 6528 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 72760 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 72760 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 19028 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 19028 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 989 8 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 989 8 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 989 8 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 7048 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 7048 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 140582 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 140582 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 15774 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 15774 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 15791 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 15791 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 72292 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 72292 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 156973 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 156973 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 156973 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 197635 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 197635 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 58470 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 58470 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 986 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+
715 986 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 986 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 58592 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 58592 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 7177 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 7177 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 7149 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 7149 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 140836 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 140836 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 72353 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 72353 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 197842 42 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 197842 42 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 140578 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 140578 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 167058 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 167058 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 167058 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 13815 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 13815 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 13815 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 62295 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 62295 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 6403 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 6403 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 72495 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 72495 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 57750 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 57750 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 18921 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 18921 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 72707 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 72707 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 1552 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 1552 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 1552 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 1552 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 94547 27 None 15 4 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 94547 27 None 15 4 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 94547 27 None 15 4 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 94547 27 None -15 4 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 94547 27 None -15 4 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 94547 27 None -15 4 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 1570 21 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 1570 21 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 1570 21 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 1570 21 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 1570 21 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 923 68 None - 1 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 923 68 None - 1 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
647 923 68 None - 1 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 923 68 None - 1 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 923 68 None - 1 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 1552 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 1552 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 1552 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 1552 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 1570 21 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 1570 21 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 1570 21 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 1570 21 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 1570 21 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 923 68 None - 1 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 923 68 None - 1 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
647 923 68 None - 1 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 923 68 None - 1 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 923 68 None - 1 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 239 21 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 239 21 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 239 21 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 510 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 510 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 510 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 1523 8 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 1523 8 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 1523 8 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 769 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
714 769 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 769 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 989 8 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 989 8 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 989 8 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 3305 10 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 3305 10 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 3305 10 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 3305 10 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 3456 32 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 3456 32 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 3456 32 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 2823 52 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 2823 52 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 2823 52 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 2823 52 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 2823 52 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 2823 52 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 2823 52 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 2823 52 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 3207 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 3207 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 3207 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
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 986 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
715 986 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 986 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 1135 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 1135 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 1135 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 923 68 None - 1 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 923 68 None - 1 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 923 68 None - 1 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 923 68 None - 1 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 923 68 None - 1 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 923 68 None - 1 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 923 68 None - 1 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 923 68 None - 1 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
647 923 68 None - 1 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
647 923 68 None - 1 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
647 923 68 None - 1 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
647 923 68 None - 1 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 923 68 None - 1 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 923 68 None - 1 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 923 68 None - 1 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 923 68 None - 1 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 923 68 None - 1 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 923 68 None - 1 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 923 68 None - 1 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 923 68 None - 1 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
719 770 2 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 770 2 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 770 2 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 239 21 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 239 21 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 239 21 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 239 21 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 239 21 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 239 21 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 3700 20 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 3700 20 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 3700 20 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 3700 20 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 3700 20 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 3700 20 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 2823 52 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 2823 52 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 2823 52 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 2823 52 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 2823 52 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 2823 52 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 2823 52 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 2823 52 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 2823 52 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 2823 52 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 2823 52 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 2823 52 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 103584 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 103584 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 87696 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 87696 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 88008 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 88008 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 88005 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 88005 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 88013 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 88013 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 88024 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 88024 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 94547 27 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 94547 27 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 94547 27 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 87691 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 87691 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 87695 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 87695 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 103570 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 103570 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 88021 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 88021 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 87697 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 87697 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 88004 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 88004 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 88011 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 88011 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 88015 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 88015 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 88017 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 88017 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 88034 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 88034 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 88036 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 88036 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 87692 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 87692 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 87675 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 87675 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 87684 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 87684 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 87688 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 87688 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 103330 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 103330 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 103568 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 103568 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 103576 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 103576 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 103572 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 103572 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 103577 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 103577 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 103583 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 103583 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 103579 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 103579 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 103587 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 103587 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 88007 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 88007 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 88012 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 88012 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 88026 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 88026 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 88032 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 88032 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 88033 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 88033 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 87680 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 87680 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 87685 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 87685 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 87693 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 87693 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 88010 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 88010 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 87687 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 87687 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 103573 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 103573 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 103571 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 103571 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 103578 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 103578 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 103581 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 103581 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 103569 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 103569 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 88014 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 88014 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 88029 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 88029 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 88030 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 88030 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 88037 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 88037 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 87681 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 87681 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 87686 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 87686 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 88022 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 88022 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 103574 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 103574 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 103582 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 103582 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 88009 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 88009 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 88016 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 88016 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 88020 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 88020 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 88025 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 88025 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 88028 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 88028 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 87677 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 87677 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 87679 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 87679 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 87682 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 87682 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 87683 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 87683 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 87690 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 87690 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 2823 52 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 2823 52 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 2823 52 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 2823 52 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 103575 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 103575 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 88018 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 88018 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 103580 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 103580 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 87698 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 87698 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 88006 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 88006 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 88035 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 88035 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 87673 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 87673 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 87636 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 87636 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 87676 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 87676 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 923 68 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 923 68 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
647 923 68 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 923 68 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 923 68 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 3700 20 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 3700 20 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 3700 20 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 87694 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 87694 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 88019 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 88019 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 88023 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 88023 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 88027 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 88027 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 87674 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 87674 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 103585 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 103585 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 103586 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 103586 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 195909 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 195909 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 71041 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 71041 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 186184 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 186184 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 192069 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 192069 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 183554 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 183554 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 69842 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 69842 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 70726 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 70726 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 185759 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 185759 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 188110 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 188110 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 70785 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 70785 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 132219 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 132219 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 63532 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 63532 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 69988 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 69988 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 62533 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 62533 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 64513 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 64513 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 135694 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 135694 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 69293 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 69293 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 63547 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 63547 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 70648 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 70648 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 186482 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 186482 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 70744 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 70744 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 132880 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 132880 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 134113 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 134113 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 186147 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 186147 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 65253 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 65253 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 186090 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 186090 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 186148 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 186148 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 88872 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 88872 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 122075 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 122075 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 122796 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 122796 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 183582 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 183582 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 62957 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 62957 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 2823 52 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 2823 52 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 2823 52 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 2823 52 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 185754 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 185754 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 63199 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 63199 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 63199 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 63199 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 122706 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 122706 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 184938 0 None - 0 Human 7.5 pIC50 = 7.5 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 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 184938 0 None - 0 Human 7.5 pIC50 = 7.5 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 385 9 4 5 2.2 COc1ccc(CC(C)(C)NC[C@H](O)COc2cccc3[nH]c(=O)[nH]c23)cc1 10.1021/jm900563e
44583033 184938 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 184938 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 183555 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 183555 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 159258 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 159258 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 63517 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 63517 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 63517 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 63517 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 196129 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 196129 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 2823 52 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 2823 52 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 2823 52 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 2823 52 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 2823 52 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 2823 52 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 2823 52 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 2823 52 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 2823 52 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 2823 52 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 2823 52 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 2823 52 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 6857 7 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 6857 7 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 63208 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 63208 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 122703 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 122703 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 185753 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 185753 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 192596 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 192596 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 63139 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 63139 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 183490 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 183490 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 3456 32 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 3456 32 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 3456 32 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 63485 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 63485 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 70310 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 70310 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 191553 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 191553 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 70937 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 70937 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 186149 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 186149 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 6633 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 6633 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 3869 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 3869 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 2712 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 2712 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 2712 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 2712 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 2712 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 2712 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 2712 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 2331 101 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 2331 101 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 2331 101 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 2331 101 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 2331 101 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 2331 101 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
719 770 2 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
719 770 2 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 770 2 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 770 2 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 770 2 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 770 2 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 3700 20 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 3700 20 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 3700 20 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
707 791 0 None -1 3 Human 2.4 pKd None 2.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7531693
708 2484 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 2484 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 2484 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 2484 0 None - 1 Rat 2.4 pKd None 2.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 24 0 0 0 -0.4 [Mg+2] 7816802
707 791 0 None 1 3 Mouse 2.5 pKd None 2.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 16199532
707 791 0 None -1 3 Rat 2.5 pKd None 2.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7816802
2780 2331 101 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 2331 101 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 2331 101 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 2331 101 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 2331 101 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 2331 101 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 2331 101 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 2331 101 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 2331 101 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 2331 101 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 2331 101 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 2331 101 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 3577 90 None - 1 Human 3.5 pKd None 3.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 202 11 4 4 -0.4 NCCCNCCCCNCCCN 9357776
710 3577 90 None - 1 Human 3.5 pKd None 3.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 202 11 4 4 -0.4 NCCCNCCCCNCCCN 9357776
CHEMBL23194 3577 90 None - 1 Human 3.5 pKd None 3.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 202 11 4 4 -0.4 NCCCNCCCCNCCCN 9357776
DB00127 3577 90 None - 1 Human 3.5 pKd None 3.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 202 11 4 4 -0.4 NCCCNCCCCNCCCN 9357776
126969137 2712 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 2712 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 2712 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 2712 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 2712 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 2712 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 2712 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