Purchasability


Ligand source activities (1 row/activity)

Select all ChEMBL ID Receptor Species Purchasable p-value
(-log)
Activity
Type
Activity
Relation
Activity
Value
Unit Assay Type Assay Description Mol
weight
Rot
Bonds
H don H acc LogP Smiles
CHEMBL3093427 casr_human Human No 8.0 EC50 = 10 nM Bind
Activation of human CaSRActivation of human CaSR
675 11 2 7 5.8 NS(=O)(=O)c1ccc(-c2nc(NC(=O)N(CCC(c3ccc(F)cc3)c3ccc(F)cc3)CCN3CCOCC3)sc2Cl)cc1
CHEMBL1256368 casr_human Human No 8.0 EC50 = 10 nM Funct
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
283 2 1 3 4.2 Cc1ccc([C@](C)(O)c2nc3ccccc3s2)c(C)c1
CHEMBL4070562 casr_human Human No 7.0 EC50 = 100 nM Funct
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
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
CHEMBL1256303 casr_human Human No 7.0 EC50 = 100 nM Funct
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
323 2 1 3 4.9 CC(O)(c1ccc(Cl)c(Cl)c1)c1nc2ccccc2s1
CHEMBL1256404 casr_human Human No 7.0 EC50 = 100 nM Funct
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
323 2 1 3 4.9 CC(O)(c1nc2ccccc2s1)c1ccc(Cl)cc1Cl
CHEMBL2375383 casr_human Human No 7.0 EC50 = 100 nM Funct
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
544 10 2 6 5.4 O=C(O)c1ccc2nc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)sc2c1
CHEMBL2346786 casr_human Human No 7.0 EC50 = 100 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
501 10 1 5 4.9 COC(=O)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1
CHEMBL2349577 casr_human Human No 7.0 EC50 = 100 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
528 11 1 5 5.2 COC(=O)c1cccc(NC(=O)N(CCCN2CCN(C)CC2)CCC(c2ccccc2)c2ccccc2)c1
CHEMBL1801356 casr_rat Rat No 6.0 EC50 = 1000 nM Funct
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+]
300 4 2 1 5.2 C[C@H](c1cccc2c1cccc2)NCc1cc2c([nH]1)cccc2
CHEMBL3937957 casr_human Human No 6.0 EC50 = 1000 nM Funct
Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 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.
283 5 6 5 -0.4 N[C@@H](CNC(=O)Nc1cccc(C(=O)O)c1O)C(=O)O
CHEMBL3964061 casr_human Human No 6.0 EC50 = 1000 nM Funct
Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 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.
333 6 5 6 -0.5 COc1ccc(S(=O)(=O)O)cc1NC(=O)NC[C@H](N)C(=O)O
CHEMBL2375385 casr_human Human No 6.0 EC50 = 1000 nM Funct
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
544 11 1 6 6.1 CCOc1ccc2nc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)sc2c1
CHEMBL2377726 casr_human Human No 6.0 EC50 = 1000 nM Funct
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
444 9 1 4 4.5 O=C(Nc1cccnc1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1
CHEMBL2349574 casr_human Human No 6.0 EC50 = 1000 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
526 11 3 7 4.3 O=C(Nc1cccc(Nc2nnn[nH]2)c1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1
CHEMBL2349582 casr_human Human No 6.0 EC50 = 1000 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
571 11 1 5 6.7 CC(OC(=O)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1)C(C)(C)C
CHEMBL2349593 casr_human Human No 6.0 EC50 = 1000 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
521 10 1 5 4.5 CS(=O)(=O)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1
CHEMBL1405922 casr_human Human Yes 6.0 EC50 = 1000 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
315 7 1 1 5.6 CC(NCCC(c1ccccc1)c1ccccc1)c1ccccc1
CHEMBL254832 casr_human Human Yes 6.0 EC50 = 1000 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
315 7 1 1 5.6 CC(NCCC(c1ccccc1)c1ccccc1)c1ccccc1
CHEMBL2346781 casr_human Human No 5.0 EC50 = 10000 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
501 10 1 5 4.5 COC(=O)c1cccc(N(CCN2CCOCC2)C(=O)NCCC(c2ccccc2)c2ccccc2)c1
CHEMBL2346785 casr_human Human No 5.0 EC50 = 10000 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
498 10 1 3 7.5 COC(=O)c1cccc(NC(=O)N(CCC2CCCCC2)CCC(c2ccccc2)c2ccccc2)c1
CHEMBL3754639 casr_rat Rat No 7.0 EC50 = 102 nM Funct
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
316 4 3 2 4.9 C[C@@H](NCc1cc2c(O)cccc2[nH]1)c1cccc2ccccc12
CHEMBL3754639 casr_rat Rat No 7.0 EC50 = 102.3 nM Funct
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
316 4 3 2 4.9 C[C@@H](NCc1cc2c(O)cccc2[nH]1)c1cccc2ccccc12
CHEMBL3093413 casr_human Human No 6.0 EC50 = 1030 nM Bind
Activation of human CaSRActivation of human CaSR
511 10 1 6 5.1 O=C(Nc1nnc(-c2ccccc2)o1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1
CHEMBL1224426 casr_human Human No 7.0 EC50 = 110 nM Funct
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
439 6 1 2 7.1 C[C@@H](NCc1ccc(OC(F)(F)F)c(-c2ccc(C(F)(F)F)cc2)c1)c1ccccc1
CHEMBL4130141 casr_human Human No 6.0 EC50 = 1100 nM Funct
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
374 5 2 3 4.9 C[C@@H](N[C@H]1CCCN(c2ccc(C(=O)O)cc2)C1)c1cccc2ccccc12
CHEMBL4301203 casr_human Human No 6.0 EC50 = 1100 nM Funct
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
374 5 2 3 4.9 C[C@@H](N[C@H]1CCCN(c2ccc(C(=O)O)cc2)C1)c1cccc2ccccc12
CHEMBL3948703 casr_human Human No 6.0 EC50 = 1100 nM Funct
Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 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.
363 6 4 7 1.5 N#CCC[C@H](N)COC(=O)Nc1cc(Cl)cc(S(=O)(=O)O)c1O
CHEMBL3967566 casr_human Human No 6.0 EC50 = 1100 nM Funct
Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 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.
331 5 5 5 0.1 Cc1cc(C)c(S(=O)(=O)O)cc1NC(=O)NC[C@H](N)C(=O)O
CHEMBL3753595 casr_rat Rat No 7.0 EC50 = 112 nM Funct
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
316 4 3 2 4.9 C[C@@H](NCc1cc2cc(O)ccc2[nH]1)c1cccc2ccccc12
CHEMBL3753595 casr_rat Rat No 7.0 EC50 = 112.2 nM Funct
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
316 4 3 2 4.9 C[C@@H](NCc1cc2cc(O)ccc2[nH]1)c1cccc2ccccc12
CHEMBL577306 casr_human Human No 5.9 EC50 = 1180 nM Funct
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
373 6 1 3 5.7 CC[C@@H](N[C@H](C)c1ccccc1)c1ccn(-c2ccc(C(F)(F)F)cc2)n1
CHEMBL4060025 casr_human Human No 7.9 EC50 = 12.6 nM Funct
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
402 7 3 4 3.5 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCCN)cc2)C1)c1cccc2ccccc12
CHEMBL4067601 casr_human Human No 7.9 EC50 = 12.6 nM Funct
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
466 9 2 5 3.6 C[C@@H](N[C@H]1CCN(c2ccc(S(=O)(=O)NCCN(C)C)cc2)C1)c1cccc2ccccc12
CHEMBL4129011 casr_human Human No 6.9 EC50 = 120 nM Funct
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
400 5 1 3 5.7 C[C@@H](N[C@H]1CCN(c2ccc(OC(F)(F)F)cc2)C1)c1cccc2ccccc12
CHEMBL4302857 casr_human Human No 6.9 EC50 = 120 nM Funct
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
400 5 1 3 5.7 C[C@@H](N[C@H]1CCN(c2ccc(OC(F)(F)F)cc2)C1)c1cccc2ccccc12
CHEMBL3986052 casr_human Human No 5.9 EC50 = 1200 nM Funct
Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 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.
489 9 5 6 2.4 N[C@@H](CCC(=O)Nc1cc(Cl)cc(S(=O)(=O)O)c1O)C(=O)NCCc1cccc(Cl)c1
CHEMBL1224190 casr_human Human Yes 5.9 EC50 = 1200 nM Funct
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
241 5 1 2 3.5 COc1cccc([C@@H](C)NCc2ccccc2)c1
CHEMBL4062970 casr_human Human No 6.9 EC50 = 125.9 nM Funct
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
445 8 2 3 4.2 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCC[N+](C)(C)C)cc2)C1)c1cccc2ccccc12
CHEMBL4117685 casr_human Human No 6.9 EC50 = 125.9 nM Funct
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
445 8 2 3 4.2 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCC[N+](C)(C)C)cc2)C1)c1cccc2ccccc12
CHEMBL2349590 casr_human Human No 6.9 EC50 = 130 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
489 10 1 4 5.8 CSc1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1
CHEMBL1192611 casr_rat Rat No 5.9 EC50 = 1300 nM Funct
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+]
300 4 2 1 5.2 CC(NCc1cc2ccccc2[nH]1)c1cccc2ccccc12
CHEMBL543875 casr_rat Rat No 5.9 EC50 = 1300 nM Funct
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+]
300 4 2 1 5.2 CC(NCc1cc2ccccc2[nH]1)c1cccc2ccccc12
CHEMBL1224342 casr_human Human No 5.9 EC50 = 1300 nM Funct
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
403 6 1 2 6.4 COc1ccc(CN[C@H](C)c2cccc(F)c2)cc1-c1ccc(C(F)(F)F)cc1
CHEMBL3941122 casr_human Human No 4.9 EC50 = 13000 nM Funct
Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 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.
303 6 4 6 -0.5 N[C@@H](CCC(=O)Nc1cccc(S(=O)(=O)O)n1)C(=O)O
CHEMBL3753320 casr_rat Rat No 6.9 EC50 = 131 nM Funct
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
318 4 2 1 5.3 CC(NCc1cc2ccccc2[nH]1)c1ccc(F)c2ccccc12
CHEMBL1801356 casr_rat Rat No 6.9 EC50 = 131.8 nM Funct
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
300 4 2 1 5.2 C[C@H](c1cccc2c1cccc2)NCc1cc2c([nH]1)cccc2
CHEMBL3753320 casr_rat Rat No 6.9 EC50 = 131.8 nM Funct
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
318 4 2 1 5.3 CC(NCc1cc2ccccc2[nH]1)c1ccc(F)c2ccccc12
CHEMBL1801356 casr_rat Rat No 6.9 EC50 = 132 nM Funct
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
300 4 2 1 5.2 C[C@H](c1cccc2c1cccc2)NCc1cc2c([nH]1)cccc2
CHEMBL3753729 casr_rat Rat No 6.9 EC50 = 134.9 nM Funct
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
376 5 2 1 6.8 C[C@@H](NCc1cc2c(-c3ccccc3)cccc2[nH]1)c1cccc2ccccc12
CHEMBL3753729 casr_rat Rat No 6.9 EC50 = 136 nM Funct
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
376 5 2 1 6.8 C[C@@H](NCc1cc2c(-c3ccccc3)cccc2[nH]1)c1cccc2ccccc12
CHEMBL1224262 casr_human Human No 5.9 EC50 = 1400 nM Funct
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
347 7 1 3 5.2 COc1cccc([C@@H](C)NCc2cccc(-c3ccccc3OC)c2)c1
CHEMBL572363 casr_human Human No 6.8 EC50 = 148 nM Funct
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
377 5 1 3 5.4 C[C@@H](N[C@H](C)c1ccn(-c2ccc(C(F)(F)F)cc2)n1)c1cccc(F)c1
CHEMBL4100132 casr_human Human No 7.8 EC50 = 15.9 nM Funct
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
534 14 6 7 2.6 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCCCCNC(CO)(CO)CO)cc2)C1)c1cccc2ccccc12
CHEMBL2377737 casr_human Human No 6.8 EC50 = 150 nM Funct
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
497 9 1 5 5.0 Cn1c(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)nc2ccccc21
CHEMBL2346787 casr_human Human No 6.8 EC50 = 150 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
515 11 1 5 5.3 COC(=O)c1cccc(NC(=O)N(CCCN2CCOCC2)CCC(c2ccccc2)c2ccccc2)c1
CHEMBL2349573 casr_human Human No 6.8 EC50 = 150 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
576 10 1 5 7.4 O=C(Nc1cccc(-c2nc3ccccc3s2)c1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1
CHEMBL2349580 casr_human Human No 6.8 EC50 = 150 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
529 11 1 5 5.6 CC(C)OC(=O)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1
CHEMBL2349584 casr_human Human No 6.8 EC50 = 150 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
531 12 2 6 4.2 O=C(OCCO)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1
CHEMBL2349586 casr_human Human No 6.8 EC50 = 150 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
499 11 1 4 5.7 CCC(=O)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1
CHEMBL2349602 casr_human Human No 6.8 EC50 = 150 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
509 10 1 4 6.3 O=C(Nc1cccc(-c2ccco2)c1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1
CHEMBL2349604 casr_human Human No 6.8 EC50 = 150 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
524 10 1 5 6.0 Cc1cc(-c2cccc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)c2)on1
CHEMBL2346782 casr_human Human No 5.8 EC50 = 1500 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
444 9 1 3 6.2 COC(=O)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CC(C)C)c1
CHEMBL3958734 casr_human Human No 4.8 EC50 = 15000 nM Funct
Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 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.
281 5 5 4 0.2 Cc1ccc(NC(=O)NC[C@H](N)C(=O)O)cc1C(=O)O
CHEMBL2346767 casr_human Human No 4.8 EC50 = 15000 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
360 7 2 2 5.0 COc1ccc(NC(=O)NCCC(c2ccccc2)c2ccccc2)cc1
CHEMBL2346775 casr_human Human No 4.8 EC50 = 15000 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
406 7 2 1 6.7 O=C(NCCC(c1ccccc1)c1ccccc1)Nc1cccc(-c2ccccc2)c1
CHEMBL2346779 casr_human Human No 4.8 EC50 = 15000 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
374 8 2 2 4.7 COc1ccc(CNC(=O)NCCC(c2ccccc2)c2ccccc2)cc1
CHEMBL3091483 casr_human Human No 6.8 EC50 = 157 nM Bind
Activation of human CaSRActivation of human CaSR
551 10 1 6 6.1 N#Cc1sc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)nc1-c1ccccc1
CHEMBL4079960 casr_human Human No 6.8 EC50 = 158.5 nM Funct
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
360 5 2 3 4.5 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)O)cc2)C1)c1cccc2ccccc12
CHEMBL4126482 casr_human Human No 6.8 EC50 = 158.5 nM Funct
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
360 5 2 3 4.5 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)O)cc2)C1)c1cccc2ccccc12
CHEMBL1256366 casr_human Human No 6.8 EC50 = 158.5 nM Funct
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
287 2 1 3 4.0 Cc1cc(C(C)(O)c2nc3ccccc3s2)ccc1F
CHEMBL571048 casr_human Human Yes 5.8 EC50 = 1580 nM Funct
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
277 5 1 3 3.7 C[C@@H](NCc1ccn(-c2ccccc2)n1)c1ccccc1
CHEMBL4069946 casr_human Human No 5.8 EC50 = 1584.9 nM Funct
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
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
CHEMBL3093411 casr_human Human No 7.8 EC50 = 16 nM Bind
Activation of human CaSRActivation of human CaSR
619 12 2 7 5.6 CS(=O)(=O)Nc1ccc(-c2csc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)n2)cc1
CHEMBL1224343 casr_human Human No 6.8 EC50 = 160 nM Funct
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
399 6 1 2 6.5 COc1ccc(CNC(C)c2cccc(C)c2)cc1-c1ccc(C(F)(F)F)cc1
CHEMBL3925295 casr_human Human No 5.8 EC50 = 1600 nM Funct
Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 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.
267 5 5 4 -0.1 N[C@@H](CNC(=O)Nc1cccc(C(=O)O)c1)C(=O)O
CHEMBL3093419 casr_human Human No 7.8 EC50 = 17 nM Bind
Activation of human CaSRActivation of human CaSR
604 11 1 7 5.6 CS(=O)(=O)c1sc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)nc1-c1ccccc1
CHEMBL4126450 casr_human Human No 7.8 EC50 = 17 nM Funct
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
384 5 2 5 3.9 C[C@@H](N[C@H]1CCN(c2ccc(-c3nn[nH]n3)cc2)C1)c1cccc2ccccc12
CHEMBL4302858 casr_human Human No 7.8 EC50 = 17 nM Funct
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
384 5 2 5 3.9 C[C@@H](N[C@H]1CCN(c2ccc(-c3nn[nH]n3)cc2)C1)c1cccc2ccccc12
CHEMBL1224424 casr_human Human No 7.8 EC50 = 17 nM Funct
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
399 6 1 2 6.8 COc1ccc([C@@H](C)N[C@H](C)c2ccccc2)cc1-c1ccc(C(F)(F)F)cc1
CHEMBL1224192 casr_human Human No 5.8 EC50 = 1700 nM Funct
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
351 6 1 2 5.9 COc1cccc([C@@H](C)NCc2cccc(-c3ccccc3Cl)c2)c1
CHEMBL1224423 casr_human Human No 5.8 EC50 = 1700 nM Funct
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
403 6 1 2 6.4 COc1ccc(CN[C@H](C)c2ccc(F)cc2)cc1-c1ccc(C(F)(F)F)cc1
CHEMBL2377733 casr_human Human No 5.8 EC50 = 1700 nM Funct
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
462 9 1 5 4.7 Cc1noc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1C
CHEMBL3093415 casr_human Human No 6.8 EC50 = 175 nM Bind
Activation of human CaSRActivation of human CaSR
527 10 1 6 5.6 O=C(Nc1nsc(-c2ccccc2)n1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1
CHEMBL3093420 casr_human Human No 7.8 EC50 = 18 nM Bind
Activation of human CaSRActivation of human CaSR
560 10 1 5 6.9 O=C(Nc1nc(-c2ccccc2)c(Cl)s1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1
CHEMBL3889990 casr_human Human No 7.8 EC50 = 18 nM Funct
Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 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.
303 5 5 5 -0.5 N[C@@H](CNC(=O)Nc1cccc(S(=O)(=O)O)c1)C(=O)O
CHEMBL1201284 casr_human Human Yes 6.8 EC50 = 180 nM Funct
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
357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F
CHEMBL3943365 casr_human Human No 6.8 EC50 = 180 nM Funct
Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 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.
390 6 4 8 1.4 Cc1nnc([C@@H](N)CCC(=O)Nc2cc(Cl)cc(S(=O)(=O)O)c2O)o1
CHEMBL3946636 casr_human Human No 5.8 EC50 = 1800 nM Funct
Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 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.
312 6 5 6 -0.2 N[C@@H](CNC(=O)Nc1cc(C(=O)O)cc([N+](=O)[O-])c1)C(=O)O
CHEMBL3955623 casr_human Human No 5.8 EC50 = 1800 nM Funct
Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 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.
380 7 4 6 1.0 CN(C)[C@@H](CCC(=O)Nc1cc(Cl)cc(S(=O)(=O)O)c1O)C(=O)O
CHEMBL3093426 casr_human Human No 7.7 EC50 = 19 nM Bind
Activation of human CaSRActivation of human CaSR
675 11 2 7 5.8 NS(=O)(=O)c1ccc(-c2nc(NC(=O)N(CCC(c3cccc(F)c3)c3cccc(F)c3)CCN3CCOCC3)sc2Cl)cc1
CHEMBL4072950 casr_human Human No 7.7 EC50 = 20.0 nM Funct
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
395 5 2 4 3.4 C[C@@H](N[C@H]1CCN(c2ccc(S(N)(=O)=O)cc2)C1)c1cccc2ccccc12
CHEMBL1201284 casr_human Human Yes 7.7 EC50 = 20.0 nM Funct
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F
CHEMBL4128542 casr_human Human No 6.7 EC50 = 190 nM Funct
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
414 5 1 3 6.1 C[C@@H](N[C@@H]1CCCN(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12
CHEMBL4302632 casr_human Human No 6.7 EC50 = 190 nM Funct
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
414 5 1 3 6.1 C[C@@H](N[C@@H]1CCCN(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12
CHEMBL583469 casr_human Human No 5.7 EC50 = 1920 nM Funct
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
399 7 2 5 4.6 COc1cc([C@@H](C)N[C@H](C)c2cccc(Cl)c2)nn1-c1ccc(C(=O)O)cc1
CHEMBL292376 casr_human Human Yes 6.7 EC50 = 194 nM Funct
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
303 7 1 2 4.6 COc1cccc(c1)[C@H](NCCCc1ccccc1Cl)C
CHEMBL1258389 casr_human Human No 6.7 EC50 = 199.5 nM Funct
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
309 3 1 3 4.6 Cc1ccc(C(O)(c2nc3ccccc3s2)C2CC2)c(C)c1
CHEMBL3093422 casr_human Human No 8.7 EC50 = 2 nM Bind
Activation of human CaSRActivation of human CaSR
639 11 2 7 5.5 NS(=O)(=O)c1ccc(-c2nc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)sc2Cl)cc1
CHEMBL3093430 casr_human Human No 7.7 EC50 = 20 nM Bind
Activation of human CaSRActivation of human CaSR
656 12 2 8 5.2 CS(=O)(=O)Nc1ccc(-c2nsc(NC(=O)N(CCC(c3ccc(F)cc3)c3ccc(F)cc3)CCN3CCOCC3)n2)cc1
CHEMBL3753306 casr_rat Rat No 7.7 EC50 = 20 nM Funct
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
345 5 2 3 5.1 C[C@@H](NCc1cc2cccc([N+](=O)[O-])c2[nH]1)c1cccc2ccccc12
CHEMBL2377735 casr_human Human No 7.7 EC50 = 20 nM Funct
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
500 9 1 5 5.7 O=C(Nc1nc2ccccc2s1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1
CHEMBL2377740 casr_human Human No 7.7 EC50 = 20 nM Funct
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
534 9 1 5 6.3 O=C(Nc1nc2c(Cl)cccc2s1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1
CHEMBL3753306 casr_rat Rat No 7.7 EC50 = 20.4 nM Funct
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
345 5 2 3 5.1 C[C@@H](NCc1cc2cccc([N+](=O)[O-])c2[nH]1)c1cccc2ccccc12
CHEMBL2375386 casr_human Human No 6.7 EC50 = 200 nM Funct
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
518 9 1 5 5.8 O=C(Nc1nc2ccc(F)cc2s1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1
CHEMBL2377730 casr_human Human No 6.7 EC50 = 200 nM Funct
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
528 10 1 7 5.0 O=C(Nc1nccc(-c2nccs2)n1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1
CHEMBL2377732 casr_human Human No 6.7 EC50 = 200 nM Funct
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
448 9 1 5 4.4 Cc1cc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)no1
CHEMBL2377750 casr_human Human No 6.7 EC50 = 200 nM Funct
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
572 11 1 7 5.9 CCOC(=O)c1ccc2nc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)sc2c1
CHEMBL2377751 casr_human Human No 6.7 EC50 = 200 nM Funct
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
614 13 2 7 5.0 CN(C)CCNC(=O)c1ccc2nc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)sc2c1
CHEMBL2349576 casr_human Human No 6.7 EC50 = 200 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
525 10 1 7 4.3 Cn1nnnc1-c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1
CHEMBL2349581 casr_human Human No 6.7 EC50 = 200 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
577 12 1 5 6.4 O=C(OCc1ccccc1)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1
CHEMBL2349595 casr_human Human No 6.7 EC50 = 200 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
527 10 1 4 6.0 O=C(Nc1cccc(OC(F)(F)F)c1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1
CHEMBL2349600 casr_human Human No 6.7 EC50 = 200 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
519 10 1 3 6.7 O=C(Nc1cccc(-c2ccccc2)c1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1
CHEMBL2349601 casr_human Human No 6.7 EC50 = 200 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
520 10 1 4 6.1 O=C(Nc1cccc(-c2cccnc2)c1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1
CHEMBL2346771 casr_human Human Yes 5.7 EC50 = 2000 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
388 7 2 3 4.8 COC(=O)c1cccc(NC(=O)NCCC(c2ccccc2)c2ccccc2)c1
CHEMBL2346776 casr_human Human No 5.7 EC50 = 2000 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
422 7 2 3 5.5 COC(=O)c1cc(NC(=O)NCCC(c2ccccc2)c2ccccc2)ccc1Cl
CHEMBL2346783 casr_human Human No 5.7 EC50 = 2000 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
478 9 1 3 6.7 COC(=O)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)Cc2ccccc2)c1
CHEMBL2349579 casr_human Human No 5.7 EC50 = 2000 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
487 10 2 4 4.8 O=C(O)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1
CHEMBL2346778 casr_human Human No 4.7 EC50 = 20000 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
374 7 3 2 4.7 O=C(NCCC(c1ccccc1)c1ccccc1)Nc1cccc(C(=O)O)c1
CHEMBL1224424 casr_human Human No 5.7 EC50 = 2100 nM Funct
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
399 6 1 2 6.8 COc1ccc([C@@H](C)N[C@H](C)c2ccccc2)cc1-c1ccc(C(F)(F)F)cc1
CHEMBL3923504 casr_human Human No 4.7 EC50 = 21100 nM Funct
Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 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.
376 6 7 7 -0.9 CC(=O)Nc1cc(S(=O)(=O)O)cc(NC(=O)NC[C@H](N)C(=O)O)c1O
CHEMBL1224261 casr_human Human No 5.7 EC50 = 2200 nM Funct
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
331 6 1 2 5.5 COc1cccc([C@@H](C)NCc2cccc(-c3ccccc3C)c2)c1
CHEMBL3093416 casr_human Human No 7.6 EC50 = 23 nM Bind
Activation of human CaSRActivation of human CaSR
527 10 1 6 5.6 O=C(Nc1nc(-c2ccccc2)ns1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1
CHEMBL569182 casr_human Human Yes 7.6 EC50 = 23 nM Funct
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
433 6 1 4 5.7 COc1cc([C@@H](C)N[C@H](C)c2cccc(Cl)c2)nn1-c1ccc(Br)cc1
CHEMBL1224340 casr_human Human No 7.6 EC50 = 23 nM Funct
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
415 7 1 3 6.2 COc1cccc([C@@H](C)NCc2ccc(OC)c(-c3ccc(C(F)(F)F)cc3)c2)c1
CHEMBL4129371 casr_human Human No 6.6 EC50 = 230 nM Funct
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
400 5 1 3 5.7 C[C@@H](N[C@@H]1CCN(c2ccc(OC(F)(F)F)cc2)C1)c1cccc2ccccc12
CHEMBL4301708 casr_human Human No 6.6 EC50 = 230 nM Funct
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
400 5 1 3 5.7 C[C@@H](N[C@@H]1CCN(c2ccc(OC(F)(F)F)cc2)C1)c1cccc2ccccc12
CHEMBL3928924 casr_human Human No 5.6 EC50 = 2300 nM Funct
Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 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.
301 5 5 4 0.6 N[C@@H](CNC(=O)Nc1cc(C(=O)O)ccc1Cl)C(=O)O
CHEMBL3962913 casr_human Human No 5.6 EC50 = 2300 nM Funct
Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 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.
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
CHEMBL583522 casr_human Human No 6.6 EC50 = 233 nM Funct
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
359 5 1 3 5.3 C[C@@H](N[C@H](C)c1ccn(-c2ccc(C(F)(F)F)cc2)n1)c1ccccc1
CHEMBL572362 casr_human Human No 5.6 EC50 = 2340 nM Funct
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
387 6 1 3 5.9 CC(C)[C@@H](N[C@H](C)c1ccccc1)c1ccn(-c2ccc(C(F)(F)F)cc2)n1
CHEMBL1256367 casr_human Human Yes 7.6 EC50 = 25.1 nM Funct
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
283 2 1 3 4.2 Cc1ccc(c(c1)C)C(c1nc2c(s1)cccc2)(O)C
CHEMBL3971904 casr_human Human No 6.6 EC50 = 250 nM Funct
Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 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.
484 8 6 7 0.7 N[C@@H](CCC(=O)Nc1cc(Cl)cc(S(=O)(=O)O)c1O)C(=O)NNC(=O)Cc1ccccc1
CHEMBL4071600 casr_mouse Mouse Yes 6.6 EC50 = 251.2 nM Funct
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
528 10 3 5 4.7 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCCCN3CCC(C(=O)O)CC3)cc2)C1)c1cccc2ccccc12
CHEMBL1256331 casr_human Human No 6.6 EC50 = 251.2 nM Funct
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
269 2 1 3 3.9 Cc1ccccc1C(C)(O)c1nc2ccccc2s1
CHEMBL1256486 casr_human Human No 5.6 EC50 = 2511.9 nM Funct
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
267 2 0 2 5.1 Cc1ccc(C(C)c2nc3ccccc3s2)c(C)c1
CHEMBL1224341 casr_human Human No 7.6 EC50 = 27 nM Funct
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
385 6 1 2 6.2 COc1ccc(CN[C@H](C)c2ccccc2)cc1-c1ccc(C(F)(F)F)cc1
CHEMBL1224260 casr_human Human No 5.6 EC50 = 2700 nM Funct
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
335 6 1 2 5.4 COc1cccc([C@@H](C)NCc2cccc(-c3ccccc3F)c2)c1
CHEMBL1224344 casr_human Human No 6.6 EC50 = 280 nM Funct
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
419 6 1 2 6.9 COc1cccc([C@@H](C)NCc2ccc(Cl)c(-c3ccc(C(F)(F)F)cc3)c2)c1
CHEMBL3093414 casr_human Human No 6.5 EC50 = 286 nM Bind
Activation of human CaSRActivation of human CaSR
527 10 1 6 5.6 O=C(Nc1nnc(-c2ccccc2)s1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1
CHEMBL4079960 casr_human Human No 6.5 EC50 = 290 nM Funct
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
360 5 2 3 4.5 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)O)cc2)C1)c1cccc2ccccc12
CHEMBL4126482 casr_human Human No 6.5 EC50 = 290 nM Funct
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
360 5 2 3 4.5 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)O)cc2)C1)c1cccc2ccccc12
CHEMBL3093421 casr_human Human No 8.5 EC50 = 3 nM Bind
Activation of human CaSRActivation of human CaSR
653 12 2 7 6.2 CS(=O)(=O)Nc1ccc(-c2nc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)sc2Cl)cc1
CHEMBL3093424 casr_human Human No 8.5 EC50 = 3 nM Bind
Activation of human CaSRActivation of human CaSR
606 11 2 8 4.2 NS(=O)(=O)c1ccc(-c2nsc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)n2)cc1
CHEMBL3937671 casr_human Human No 8.5 EC50 = 3 nM Funct
Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 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.
367 5 5 7 -0.1 COC(=O)[C@@H](N)CNC(=O)Nc1cc(Cl)cc(S(=O)(=O)O)c1O
CHEMBL3972910 casr_human Human No 8.5 EC50 = 3 nM Funct
Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 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.
351 5 5 5 0.4 Cc1c(Cl)cc(S(=O)(=O)O)cc1NC(=O)NCC(N)C(=O)O
CHEMBL3980928 casr_human Human No 8.5 EC50 = 3 nM Funct
Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 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.
353 5 6 6 -0.2 N[C@@H](CNC(=O)Nc1cc(Cl)cc(S(=O)(=O)O)c1O)C(=O)O
CHEMBL2377741 casr_human Human No 7.5 EC50 = 30 nM Funct
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
530 10 1 6 5.7 COc1cccc2sc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)nc12
CHEMBL2377743 casr_human Human No 7.5 EC50 = 30 nM Funct
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
593 11 2 7 5.1 CS(=O)(=O)Nc1ccc2sc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)nc2c1
CHEMBL2377748 casr_human Human No 7.5 EC50 = 30 nM Funct
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
593 11 2 7 5.1 CS(=O)(=O)Nc1ccc2nc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)sc2c1
CHEMBL2377749 casr_human Human No 7.5 EC50 = 30 nM Funct
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
514 9 1 5 6.0 Cc1ccc2nc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)sc2c1
CHEMBL3093412 casr_human Human No 6.5 EC50 = 300 nM Bind
Activation of human CaSRActivation of human CaSR
520 10 1 4 6.1 O=C(Nc1cccc(-c2ccccc2)n1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1
CHEMBL2377731 casr_human Human No 6.5 EC50 = 300 nM Funct
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
450 9 1 5 4.5 O=C(Nc1nccs1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1
CHEMBL2377738 casr_human Human No 6.5 EC50 = 300 nM Funct
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
573 11 1 5 6.5 O=C(Nc1nc2ccccc2n1Cc1ccccc1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1
CHEMBL2349583 casr_human Human No 6.5 EC50 = 300 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
543 10 1 5 6.0 CC(C)(C)OC(=O)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1
CHEMBL2349598 casr_human Human No 6.5 EC50 = 300 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
473 10 1 4 5.1 COc1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1
CHEMBL2349599 casr_human Human No 6.5 EC50 = 300 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
486 10 1 4 5.1 CN(C)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1
CHEMBL2349605 casr_human Human No 6.5 EC50 = 300 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
526 10 1 5 6.2 O=C(Nc1cccc(-c2nccs2)c1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1
CHEMBL1224425 casr_human Human No 5.5 EC50 = 3000 nM Funct
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
399 6 1 2 6.8 COc1ccc([C@H](C)N[C@H](C)c2ccccc2)cc1-c1ccc(C(F)(F)F)cc1
CHEMBL2346772 casr_human Human No 5.5 EC50 = 3000 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
402 8 2 3 5.2 CCOC(=O)c1ccc(NC(=O)NCCC(c2ccccc2)c2ccccc2)cc1
CHEMBL2346777 casr_human Human No 5.5 EC50 = 3000 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
432 6 2 1 6.7 O=C(NCCC(c1ccccc1)c1ccccc1)Nc1ccc(Cl)c(C(F)(F)F)c1
CHEMBL4082125 casr_human Human No 7.5 EC50 = 31.6 nM Funct
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
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
CHEMBL1256403 casr_human Human No 7.5 EC50 = 31.6 nM Funct
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
303 2 1 3 4.5 Cc1cc(Cl)ccc1C(C)(O)c1nc2ccccc2s1
CHEMBL1801356 casr_human Human No 6.5 EC50 = 310 nM Funct
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+]
300 4 2 1 5.2 C[C@H](c1cccc2c1cccc2)NCc1cc2c([nH]1)cccc2
CHEMBL3949209 casr_human Human No 5.5 EC50 = 3100 nM Funct
Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 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.
421 6 4 7 0.2 NC(CCC(=O)Nc1cc(Cl)cc(S(=O)(=O)O)c1O)C(=O)N1CCOCC1
CHEMBL3974155 casr_human Human Yes 6.5 EC50 = 313 nM Funct
Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 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.
365 6 5 5 0.7 CN[C@@H](CNC(=O)Nc1cc(Cl)c(C)c(S(=O)(=O)O)c1)C(=O)O
CHEMBL4071600 casr_rat Rat Yes 6.5 EC50 = 316.2 nM Funct
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
528 10 3 5 4.7 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCCCN3CCC(C(=O)O)CC3)cc2)C1)c1cccc2ccccc12
CHEMBL1255602 casr_human Human No 6.5 EC50 = 316.2 nM Funct
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
309 1 1 3 4.5 Cc1cc(C)c2c(c1)C(O)(c1nc3ccccc3s1)CCC2
CHEMBL4076239 casr_human Human No 5.5 EC50 = 3162.3 nM Funct
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
396 5 3 3 3.6 C[C@@H](N[C@H]1CCN(c2ccc(P(=O)(O)O)cc2)C1)c1cccc2ccccc12
CHEMBL4126057 casr_human Human No 6.5 EC50 = 320 nM Funct
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
400 5 1 3 5.7 C[C@@H](N[C@@H]1CCN(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12
CHEMBL4300082 casr_human Human No 6.5 EC50 = 320 nM Funct
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
400 5 1 3 5.7 C[C@@H](N[C@@H]1CCN(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12
CHEMBL3975131 casr_human Human No 5.5 EC50 = 3400 nM Funct
Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 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.
447 7 5 6 2.2 NC(CCC(=O)Nc1cc(Cl)cc(S(=O)(=O)O)c1O)C(=O)NC1CCCCCC1
CHEMBL1224192 casr_human Human No 6.5 EC50 = 350 nM Funct
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
351 6 1 2 5.9 COc1cccc([C@@H](C)NCc2cccc(-c3ccccc3Cl)c2)c1
CHEMBL2349591 casr_human Human No 6.5 EC50 = 350 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
543 10 1 4 6.7 O=C(Nc1cccc(SC(F)(F)F)c1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1
CHEMBL3093417 casr_human Human No 7.4 EC50 = 36 nM Bind
Activation of human CaSRActivation of human CaSR
526 10 1 5 6.2 O=C(Nc1nc(-c2ccccc2)cs1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1
CHEMBL3919534 casr_human Human No 5.4 EC50 = 3600 nM Funct
Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 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.
297 6 5 5 -0.1 COc1cc(NC(=O)NC[C@H](N)C(=O)O)cc(C(=O)O)c1
CHEMBL1224342 casr_human Human No 7.4 EC50 = 37 nM Funct
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
403 6 1 2 6.4 COc1ccc(CN[C@H](C)c2cccc(F)c2)cc1-c1ccc(C(F)(F)F)cc1
CHEMBL1224193 casr_human Human Yes 6.4 EC50 = 370 nM Funct
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
271 6 1 3 3.6 COc1ccc(CN[C@H](C)c2cccc(OC)c2)cc1
CHEMBL3903207 casr_human Human No 5.4 EC50 = 3700 nM Funct
Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 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.
333 6 5 6 -0.5 COc1ccc(NC(=O)NC[C@H](N)C(=O)O)cc1S(=O)(=O)O
CHEMBL1224191 casr_human Human Yes 5.4 EC50 = 3700 nM Funct
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
275 5 1 2 4.2 COc1cccc([C@@H](C)NCc2ccccc2Cl)c1
CHEMBL4125917 casr_human Human No 6.4 EC50 = 380 nM Funct
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
398 4 1 2 6.2 C[C@@H](N[C@@H]1CCCN(c2cccc(C(F)(F)F)c2)C1)c1cccc2ccccc12
CHEMBL4300173 casr_human Human No 6.4 EC50 = 380 nM Funct
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
398 4 1 2 6.2 C[C@@H](N[C@@H]1CCCN(c2cccc(C(F)(F)F)c2)C1)c1cccc2ccccc12
CHEMBL3974015 casr_human Human No 7.4 EC50 = 39 nM Funct
Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 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.
367 6 6 7 -0.2 N[C@@H](CCC(=O)Nc1cc(Cl)cc(S(=O)(=O)O)c1O)C(=O)NO
CHEMBL4074358 casr_human Human No 7.4 EC50 = 39.8 nM Funct
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
463 9 5 6 2.2 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NC(CO)(CO)CO)cc2)C1)c1cccc2ccccc12
CHEMBL4092377 casr_human Human No 7.4 EC50 = 39.8 nM Funct
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
467 8 3 5 3.4 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCCS(=O)(=O)O)cc2)C1)c1cccc2ccccc12
CHEMBL4094738 casr_human Human No 7.4 EC50 = 39.8 nM Funct
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
453 8 3 5 3.1 C[C@@H](N[C@H]1CCN(c2ccc(S(=O)(=O)NCC(=O)O)cc2)C1)c1cccc2ccccc12
CHEMBL3957364 casr_human Human No 6.4 EC50 = 390 nM Funct
Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 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.
429 7 5 8 -0.6 CS(=O)(=O)NC(=O)[C@@H](N)CCC(=O)Nc1cc(Cl)cc(S(=O)(=O)O)c1O
CHEMBL4097717 casr_human Human No 6.4 EC50 = 398.1 nM Funct
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
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
CHEMBL1256301 casr_human Human Yes 6.4 EC50 = 398.1 nM Funct
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
289 2 1 3 4.2 CC(O)(c1ccc(Cl)cc1)c1nc2ccccc2s1
CHEMBL1256330 casr_human Human No 5.4 EC50 = 3981.1 nM Funct
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
285 3 1 4 3.6 COc1ccccc1C(C)(O)c1nc2ccccc2s1
CHEMBL3093425 casr_human Human No 8.4 EC50 = 4 nM Bind
Activation of human CaSRActivation of human CaSR
675 11 2 7 5.8 NS(=O)(=O)c1ccc(-c2nc(NC(=O)N(CCC(c3ccccc3F)c3ccccc3F)CCN3CCOCC3)sc2Cl)cc1
CHEMBL3895461 casr_human Human No 8.4 EC50 = 4 nM Funct
Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 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.
367 5 5 5 0.6 Cc1c(Cl)cc(S(=O)(=O)O)cc1NC(=S)NC[C@H](N)C(=O)O
CHEMBL3978873 casr_human Human No 7.4 EC50 = 40 nM Funct
Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 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.
320 5 4 6 0.6 N[C@@H](CSC(=O)Nc1cccc(S(=O)(=O)O)c1)C(=O)O
CHEMBL2377744 casr_human Human No 7.4 EC50 = 40 nM Funct
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
530 10 1 6 5.7 COc1ccc2nc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)sc2c1
CHEMBL2377729 casr_human Human No 6.4 EC50 = 400 nM Funct
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
489 10 1 6 4.2 COc1cc(C)nc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)n1
CHEMBL2377734 casr_human Human No 6.4 EC50 = 400 nM Funct
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
507 10 1 6 4.9 COC(=O)c1sccc1NC(=O)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1
CHEMBL2349578 casr_human Human No 6.4 EC50 = 400 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
572 11 1 6 5.3 COC(=O)c1cccc(NC(=O)N(CCCN2CCN(C(=O)OC)CC2)CCC(c2ccccc2)c2ccccc2)c1
CHEMBL2349585 casr_human Human No 6.4 EC50 = 400 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
647 14 1 5 7.2 O=C(OCCCC(F)(F)C(F)(F)F)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1
CHEMBL2349589 casr_human Human No 6.4 EC50 = 400 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
487 11 1 4 5.2 COCc1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1
CHEMBL2349594 casr_human Human No 6.4 EC50 = 400 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
575 10 1 5 5.4 O=C(Nc1cccc(S(=O)(=O)C(F)(F)F)c1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1
CHEMBL2349597 casr_human Human No 6.4 EC50 = 400 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
511 9 1 3 6.1 O=C(Nc1cccc(C(F)(F)F)c1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1
CHEMBL2346769 casr_human Human Yes 5.4 EC50 = 4000 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
364 6 2 1 5.7 O=C(NCCC(c1ccccc1)c1ccccc1)Nc1ccc(Cl)cc1
CHEMBL2346770 casr_human Human Yes 5.4 EC50 = 4000 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
364 6 2 1 5.7 O=C(NCCC(c1ccccc1)c1ccccc1)Nc1cccc(Cl)c1
CHEMBL2346773 casr_human Human Yes 5.4 EC50 = 4000 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
344 6 2 1 5.3 Cc1ccc(NC(=O)NCCC(c2ccccc2)c2ccccc2)cc1
CHEMBL2346774 casr_human Human No 5.4 EC50 = 4000 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
406 7 2 1 6.7 O=C(NCCC(c1ccccc1)c1ccccc1)Nc1ccc(-c2ccccc2)cc1
CHEMBL2346780 casr_human Human No 5.4 EC50 = 4000 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
378 7 2 1 5.4 O=C(NCCC(c1ccccc1)c1ccccc1)NCc1ccccc1Cl
CHEMBL571476 casr_human Human No 7.4 EC50 = 41 nM Funct
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
423 6 1 4 6.0 COc1cc([C@@H](C)N[C@H](C)c2cccc(Cl)c2)nn1-c1ccc(C(F)(F)F)cc1
CHEMBL180672 casr_bovin Bovine Yes 7.4 EC50 = 41 nM Bind
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
408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O
CHEMBL4125688 casr_human Human No 6.4 EC50 = 430 nM Funct
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
384 4 1 2 5.8 C[C@@H](N[C@@H]1CCN(c2cccc(C(F)(F)F)c2)C1)c1cccc2ccccc12
CHEMBL4301528 casr_human Human No 6.4 EC50 = 430 nM Funct
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
384 4 1 2 5.8 C[C@@H](N[C@@H]1CCN(c2cccc(C(F)(F)F)c2)C1)c1cccc2ccccc12
CHEMBL1224343 casr_human Human No 6.4 EC50 = 430 nM Funct
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
399 6 1 2 6.5 COc1ccc(CNC(C)c2cccc(C)c2)cc1-c1ccc(C(F)(F)F)cc1
CHEMBL4127153 casr_human Human No 6.4 EC50 = 450 nM Funct
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
384 4 1 2 5.8 C[C@@H](N[C@H]1CCN(c2cccc(C(F)(F)F)c2)C1)c1cccc2ccccc12
CHEMBL4299885 casr_human Human No 6.4 EC50 = 450 nM Funct
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
384 4 1 2 5.8 C[C@@H](N[C@H]1CCN(c2cccc(C(F)(F)F)c2)C1)c1cccc2ccccc12
CHEMBL2377728 casr_human Human No 6.4 EC50 = 450 nM Funct
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
445 9 1 5 3.9 O=C(Nc1cnccn1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1
CHEMBL3950758 casr_human Human No 6.3 EC50 = 490 nM Funct
Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 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.
321 5 5 5 -0.4 N[C@@H](CNC(=O)Nc1cc(S(=O)(=O)O)ccc1F)C(=O)O
CHEMBL4086045 casr_human Human No 8.3 EC50 = 5.0 nM Funct
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
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
CHEMBL4126877 casr_human Human No 7.3 EC50 = 50 nM Funct
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
403 7 3 4 3.5 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCCO)cc2)C1)c1cccc2ccccc12
CHEMBL4301421 casr_human Human No 7.3 EC50 = 50 nM Funct
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
403 7 3 4 3.5 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCCO)cc2)C1)c1cccc2ccccc12
CHEMBL4071600 casr_human Human Yes 7.3 EC50 = 50 nM Funct
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
528 10 3 5 4.7 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCCCN3CCC(C(=O)O)CC3)cc2)C1)c1cccc2ccccc12
CHEMBL4071600 casr_human Human Yes 7.3 EC50 = 50.1 nM Funct
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
528 10 3 5 4.7 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCCCN3CCC(C(=O)O)CC3)cc2)C1)c1cccc2ccccc12
CHEMBL3922323 casr_human Human No 5.3 EC50 = 5000 nM Funct
Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 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.
281 5 5 4 0.2 Cc1ccc(C(=O)O)cc1NC(=O)NC[C@H](N)C(=O)O
CHEMBL4091950 casr_human Human No 6.3 EC50 = 501.2 nM Funct
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
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
CHEMBL3093418 casr_human Human No 7.3 EC50 = 53 nM Bind
Activation of human CaSRActivation of human CaSR
544 10 1 5 6.3 O=C(Nc1nc(-c2ccccc2)c(F)s1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1
CHEMBL2349587 casr_human Human No 6.3 EC50 = 550 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
485 10 1 4 5.3 CC(=O)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1
CHEMBL577333 casr_human Human No 7.2 EC50 = 57 nM Funct
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
389 6 1 4 5.6 COc1cc([C@@H](C)N[C@H](C)c2cccc(Cl)c2)nn1-c1cccc(Cl)c1
CHEMBL1224423 casr_human Human No 7.2 EC50 = 58 nM Funct
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
403 6 1 2 6.4 COc1ccc(CN[C@H](C)c2ccc(F)cc2)cc1-c1ccc(C(F)(F)F)cc1
CHEMBL3931232 casr_human Human No 5.2 EC50 = 5800 nM Funct
Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 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.
297 6 5 5 -0.1 COc1c(NC(=O)NC[C@H](N)C(=O)O)cccc1C(=O)O
CHEMBL3093423 casr_human Human No 8.2 EC50 = 6 nM Bind
Activation of human CaSRActivation of human CaSR
620 12 2 8 5.0 CS(=O)(=O)Nc1ccc(-c2nsc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)n2)cc1
CHEMBL2377736 casr_human Human No 7.2 EC50 = 60 nM Funct
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
483 9 2 4 5.0 O=C(Nc1nc2ccccc2[nH]1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1
CHEMBL2377746 casr_human Human No 7.2 EC50 = 60 nM Funct
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
534 9 1 5 6.3 O=C(Nc1nc2ccc(Cl)cc2s1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1
CHEMBL2346788 casr_human Human No 7.2 EC50 = 60 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
514 11 2 5 4.8 COC(=O)c1cccc(NC(=O)N(CCCN2CCNCC2)CCC(c2ccccc2)c2ccccc2)c1
CHEMBL2349575 casr_human Human No 7.2 EC50 = 60 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
525 10 1 7 4.3 Cn1nnc(-c2cccc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)c2)n1
CHEMBL2349603 casr_human Human No 7.2 EC50 = 60 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
510 10 1 5 5.7 O=C(Nc1cccc(-c2cnco2)c1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1
CHEMBL4130093 casr_human Human No 6.2 EC50 = 600 nM Funct
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
414 5 1 3 6.1 C[C@@H](N[C@H]1CCCN(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12
CHEMBL4300172 casr_human Human No 6.2 EC50 = 600 nM Funct
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
414 5 1 3 6.1 C[C@@H](N[C@H]1CCCN(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12
CHEMBL4125724 casr_human Human No 6.2 EC50 = 600 nM Funct
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
400 5 1 3 5.7 C[C@@H](N[C@H]1CCN(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12
CHEMBL4302236 casr_human Human No 6.2 EC50 = 600 nM Funct
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
400 5 1 3 5.7 C[C@@H](N[C@H]1CCN(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12
CHEMBL2377742 casr_human Human No 6.2 EC50 = 600 nM Funct
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
514 9 1 5 6.0 Cc1cccc2sc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)nc12
CHEMBL2346765 casr_human Human No 6.2 EC50 = 600 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
574 11 3 5 6.7 O=C(Nc1cccc(Nc2nc3ccccc3[nH]2)c1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1
CHEMBL2346666 casr_human Human No 5.2 EC50 = 6000 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
358 7 2 1 5.3 C[C@@H](NC(=O)NCCC(c1ccccc1)c1ccccc1)c1ccccc1
CHEMBL2346768 casr_human Human No 5.2 EC50 = 6000 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
364 6 2 1 5.7 O=C(NCCC(c1ccccc1)c1ccccc1)Nc1ccccc1Cl
CHEMBL1224264 casr_human Human No 6.2 EC50 = 620 nM Funct
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
385 6 1 2 6.2 COc1cccc([C@@H](C)NCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)c1
CHEMBL1258390 casr_human Human No 6.2 EC50 = 631.0 nM Funct
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
305 2 1 3 4.7 CC(O)(c1ccc2ccccc2c1)c1nc2ccccc2s1
CHEMBL4084641 casr_human Human No 8.1 EC50 = 7.9 nM Funct
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
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
CHEMBL4101097 casr_human Human No 8.1 EC50 = 7.9 nM Funct
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
506 12 6 7 1.8 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCCNC(CO)(CO)CO)cc2)C1)c1cccc2ccccc12
CHEMBL569863 casr_human Human No 7.2 EC50 = 70 nM Funct
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
389 6 1 4 5.3 COc1cc([C@@H](C)N[C@H](C)c2ccccc2)nn1-c1ccc(C(F)(F)F)cc1
CHEMBL3966753 casr_human Human No 5.2 EC50 = 7000 nM Funct
Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 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.
318 5 4 6 0.3 C[C@H](OC(=O)Nc1cccc(S(=O)(=O)O)c1)[C@H](N)C(=O)O
CHEMBL1224340 casr_human Human No 6.1 EC50 = 720 nM Funct
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
415 7 1 3 6.2 COc1cccc([C@@H](C)NCc2ccc(OC)c(-c3ccc(C(F)(F)F)cc3)c2)c1
CHEMBL4068107 casr_human Human No 7.1 EC50 = 79.4 nM Funct
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
417 7 3 4 3.6 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCC(=O)O)cc2)C1)c1cccc2ccccc12
CHEMBL1256402 casr_human Human No 7.1 EC50 = 79.4 nM Funct
Positive allosteric modulation of calcium sensing receptor by cell based assayPositive allosteric modulation of calcium sensing receptor by cell based assay
283 2 1 3 4.2 Cc1ccc([C@@](C)(O)c2nc3ccccc3s2)c(C)c1
CHEMBL292376 casr_human Human Yes 7.1 EC50 = 80 nM Funct
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
303 7 1 2 4.6 COc1cccc(c1)[C@H](NCCCc1ccccc1Cl)C
CHEMBL2377727 casr_human Human No 7.1 EC50 = 80 nM Funct
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
472 9 1 4 5.1 Cc1cc(C)nc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1
CHEMBL2377739 casr_human Human No 7.1 EC50 = 80 nM Funct
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
518 9 1 5 5.9 O=C(Nc1nc2cc(Cl)ccc2o1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1
CHEMBL2377747 casr_human Human No 7.1 EC50 = 80 nM Funct
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
530 10 2 6 5.2 O=C(Nc1nc2ccc(CO)cc2s1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1
CHEMBL2377752 casr_human Human No 7.1 EC50 = 80 nM Funct
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
578 10 1 7 5.1 CS(=O)(=O)c1ccc2nc(NC(=O)N(CCC(c3ccccc3)c3ccccc3)CCN3CCOCC3)sc2c1
CHEMBL1201284 casr_human Human Yes 7.1 EC50 = 80 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F
CHEMBL292376 casr_human Human Yes 7.1 EC50 = 80 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
303 7 1 2 4.6 COc1cccc(c1)[C@H](NCCCc1ccccc1Cl)C
CHEMBL2346784 casr_human Human No 6.1 EC50 = 800 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
502 9 1 5 5.9 COC(=O)c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CC(=O)OC(C)(C)C)c1
CHEMBL2349588 casr_human Human No 6.1 EC50 = 800 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
473 10 2 4 4.6 O=C(Nc1cccc(CO)c1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1
CHEMBL2349592 casr_human Human No 6.1 EC50 = 800 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
505 10 1 4 4.8 C[S+]([O-])c1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1
CHEMBL2349596 casr_human Human No 6.1 EC50 = 800 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
468 9 1 4 4.9 N#Cc1cccc(NC(=O)N(CCC(c2ccccc2)c2ccccc2)CCN2CCOCC2)c1
CHEMBL2346766 casr_human Human No 5.1 EC50 = 8000 nM Bind
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayPositive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
360 7 2 2 5.0 COc1cccc(NC(=O)NCCC(c2ccccc2)c2ccccc2)c1
CHEMBL1224263 casr_human Human No 6.1 EC50 = 870 nM Funct
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
347 7 1 3 5.2 COc1ccc(-c2cccc(CN[C@H](C)c3cccc(OC)c3)c2)cc1
CHEMBL3897239 casr_human Human No 6.1 EC50 = 880 nM Funct
Agonistic Activity Assay: 293E cells (EBNA1-expressing IIEK293 cells, ATCC No. CRL-10852) were cultured in DMEM (1.0 g/ml Glucose-containing Dulbecco's modified Eagle medium, Nacalai Tesque) containing 10% bovine fetal serum in the presence of 250 ug/ml of G418. The cells were seeded on a 10 cm-diameter petri dish at 1.8ÿ106 cells/15 ml, and left to stand in a CO2 incubator (5% CO2, 37° C.) for 24 hours. Thereafter, human CaSR expression plasmid hCaSR/pcDNA3.1 was transfected with transfection reagent Mirus Trans IT 293 (Takara Bio). Following static culture in a CO2 incubator for 24 hours, the cells were harvested with 10% bovine fetal serum-containing DMEM and seeded on a poly-D-lysine coat 384 well plate (Falcon) at 15,000 cells/well. Following static culture in a CO2 incubator for 24 hours, the medium was removed and the resultant was added with 50 ul/well of Ca2+ fluorescent indicator Calcium 4 Assay Kit (Molecular Devices) dissolved in an assay buffer (146 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mg/ml Glucose, 20 mM HEPES (PH 7.2), 1.5 mM CaCl2), and left to stand at 37° C. for an hour and then at room temperature for 30 minutes to allow intake of the indicator. The above-mentioned 384-well plate was transferred to FLIPR (Molecular Devices) and added with 12.5 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.
466 8 4 8 2.7 N[C@@H](CCC(=O)Nc1cc(Cl)cc(S(=O)(=O)O)c1O)c1nnc(Cc2ccccc2)o1
CHEMBL4127295 casr_human Human No 5.1 EC50 = 8800 nM Funct
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
360 5 2 3 4.5 C[C@@H](N[C@@H]1CCN(c2ccc(C(=O)O)cc2)C1)c1cccc2ccccc12
CHEMBL4300972 casr_human Human No 5.1 EC50 = 8800 nM Funct
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
360 5 2 3 4.5 C[C@@H](N[C@@H]1CCN(c2ccc(C(=O)O)cc2)C1)c1cccc2ccccc12
CHEMBL3093428 casr_human Human No 8.1 EC50 = 9 nM Bind
Activation of human CaSRActivation of human CaSR
689 12 2 7 6.5 CS(=O)(=O)Nc1ccc(-c2nc(NC(=O)N(CCC(c3ccc(F)cc3)c3ccc(F)cc3)CCN3CCOCC3)sc2Cl)cc1
CHEMBL3093429 casr_human Human No 8.1 EC50 = 9 nM Bind
Activation of human CaSRActivation of human CaSR
642 11 2 8 4.5 NS(=O)(=O)c1ccc(-c2nsc(NC(=O)N(CCC(c3ccc(F)cc3)c3ccc(F)cc3)CCN3CCOCC3)n2)cc1
CHEMBL2377745 casr_human Human No 7.1 EC50 = 90 nM Funct
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
584 10 1 6 6.6 O=C(Nc1nc2ccc(OC(F)(F)F)cc2s1)N(CCC(c1ccccc1)c1ccccc1)CCN1CCOCC1
CHEMBL568485 casr_human Human No 7.0 EC50 = 92 nM Funct
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
393 5 1 3 6.0 C[C@@H](N[C@H](C)c1ccn(-c2ccc(C(F)(F)F)cc2)n1)c1cccc(Cl)c1
CHEMBL4297621 casr_human Human Yes 7.0 EC50 = 93 nM Funct
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
374 6 2 3 4.4 OC(=O)Cc1ccc(cc1)N1CC[C@@H](C1)N[C@@H](c1cccc2c1cccc2)C
CHEMBL382741 casr_human Human No 10.7 IC50 = 0.0 nM Funct
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
374 8 2 4 4.1 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COc1ccccc1C#N
CHEMBL570593 casr_human Human No 10.7 IC50 = 0.0 nM Bind
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
446 11 3 5 4.1 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COc1ccc(CCC(=O)O)cc1C#N
CHEMBL1204009 casr_human Human No 10.5 IC50 = 0.0 nM Funct
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
474 12 2 6 4.6 CCOC(=O)CCc1ccc(OC[C@H](O)CNC(C)(C)Cc2ccc3ccccc3c2)c(C#N)c1
CHEMBL583889 casr_human Human No 10.5 IC50 = 0.0 nM Funct
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
474 12 2 6 4.6 CCOC(=O)CCc1ccc(OC[C@H](O)CNC(C)(C)Cc2ccc3ccccc3c2)c(C#N)c1
CHEMBL180672 casr_human Human Yes 10.2 IC50 = 0.1 nM Funct
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
408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O
CHEMBL570593 casr_human Human No 9.7 IC50 = 0.2 nM Funct
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
446 11 3 5 4.1 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COc1ccc(CCC(=O)O)cc1C#N
CHEMBL597397 casr_human Human No 9.4 IC50 = 0.4 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
484 9 1 6 6.0 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=S)n2Cc1cccc(OCCO)c1
CHEMBL4126450 casr_rat Rat No 9.3 IC50 = 0.5 nM Funct
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
384 5 2 5 3.9 C[C@@H](N[C@H]1CCN(c2ccc(-c3nn[nH]n3)cc2)C1)c1cccc2ccccc12
CHEMBL4302858 casr_rat Rat No 9.3 IC50 = 0.5 nM Funct
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
384 5 2 5 3.9 C[C@@H](N[C@H]1CCN(c2ccc(-c3nn[nH]n3)cc2)C1)c1cccc2ccccc12
CHEMBL4126877 casr_rat Rat No 9.0 IC50 = 0.9 nM Funct
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
403 7 3 4 3.5 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCCO)cc2)C1)c1cccc2ccccc12
CHEMBL4301421 casr_rat Rat No 9.0 IC50 = 0.9 nM Funct
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
403 7 3 4 3.5 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)NCCO)cc2)C1)c1cccc2ccccc12
CHEMBL1689050 casr_human Human No 9.0 IC50 = 0.9 nM Funct
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
458 7 2 4 6.5 CCc1ccc(C(CC)(CC)NC(=O)c2c(C)nn3c2N[C@@H](c2ccccc2)CC3(C)C)cc1
CHEMBL1689060 casr_human Human No 9.0 IC50 = 0.9 nM Funct
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
458 7 2 4 6.5 CCc1ccc(C(CC)(CC)NC(=O)c2c(C)nn3c2N[C@@H](c2ccccc2)CC3(C)C)cc1
CHEMBL1739917 casr_human Human No 9.0 IC50 = 0.9 nM Funct
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
458 7 2 4 6.5 CCc1ccc(C(CC)(CC)NC(=O)c2c(C)nn3c2N[C@@H](c2ccccc2)CC3(C)C)cc1
CHEMBL4128542 casr_rat Rat No 8.9 IC50 = 1.4 nM Funct
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
414 5 1 3 6.1 C[C@@H](N[C@@H]1CCCN(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12
CHEMBL4302632 casr_rat Rat No 8.9 IC50 = 1.4 nM Funct
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
414 5 1 3 6.1 C[C@@H](N[C@@H]1CCCN(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12
CHEMBL597800 casr_human Human No 8.9 IC50 = 1.4 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
482 9 0 6 5.7 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1ccc(OC)c(OCC)c1
CHEMBL591240 casr_human Human No 8.8 IC50 = 1.6 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
422 6 0 4 5.6 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1ccc(C)cc1
CHEMBL1223714 casr_human Human No 8.8 IC50 = 1.6 nM Funct
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
529 9 0 6 7.2 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(C(F)(F)F)c(Cc3cccnc3SC)cc(OC)c21
CHEMBL1689057 casr_human Human No 8.8 IC50 = 1.7 nM Funct
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
494 7 2 5 6.6 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(OC)c(Cl)c1
CHEMBL1739758 casr_human Human No 8.8 IC50 = 1.7 nM Funct
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
494 7 2 5 6.6 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(OC)c(Cl)c1
CHEMBL1689051 casr_human Human No 8.8 IC50 = 1.7 nM Funct
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
472 7 2 4 7.1 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(C(C)C)cc1
CHEMBL1739918 casr_human Human No 8.8 IC50 = 1.7 nM Funct
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
472 7 2 4 7.1 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(C(C)C)cc1
CHEMBL598436 casr_human Human No 8.7 IC50 = 1.8 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
422 6 0 4 5.6 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1cccc(C)c1
CHEMBL1290328 casr_human Human No 8.0 IC50 = 10 nM Funct
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
404 3 2 4 4.9 CC1(C)C[C@@H](c2ccccc2)Nc2c(C(=O)NC34CC5CC(CC(C5)C3)C4)cnn21
CHEMBL1290328 casr_human Human No 8.0 IC50 = 10 nM Funct
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
404 3 2 4 4.9 CC1(C)C[C@@H](c2ccccc2)Nc2c(C(=O)NC34CC5CC(CC(C5)C3)C4)cnn21
CHEMBL371936 casr_human Human No 7.0 IC50 = 100 nM Funct
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
363 8 3 4 3.4 CC(C)(Cc1cc2ccccc2[nH]1)NC[C@H](O)COc1ccccc1C#N
CHEMBL195859 casr_human Human No 7.0 IC50 = 100 nM Bind
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
334 5 1 4 3.7 CCc1c(C)nc(-c2ccccc2O)n(CCc2ccccc2)c1=O
CHEMBL494441 casr_human Human No 6.0 IC50 = 1000 nM Funct
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
558 14 2 9 4.6 COc1cccc(CCNc2ncc(C(=O)NCCOc3ccccc3)c(-c3cc(OC)c(OC)c(OC)c3)n2)c1
CHEMBL1223437 casr_human Human No 6.0 IC50 = 1000 nM Funct
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
450 5 0 3 6.0 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(Br)ccc(Br)c21
CHEMBL488997 casr_human Human No 6.0 IC50 = 1000 nM Bind
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
363 9 2 4 3.7 COc1ccc(CC(C)(C)NCC(O)COc2ccccc2Cl)cc1
CHEMBL521907 casr_human Human No 6.0 IC50 = 1000 nM Bind
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
363 9 2 4 3.7 COc1ccc(CC(C)(C)NCC(O)COc2cccc(Cl)c2)cc1
CHEMBL200041 casr_human Human No 6.0 IC50 = 1000 nM Funct
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
433 8 2 5 4.7 CC(C)(Cc1csc2ccccc12)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(C#N)c1
CHEMBL453360 casr_human Human No 5.0 IC50 = 10000 nM Funct
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
528 12 2 8 4.9 COc1cc(-c2nc(NCc3ccccc3C)ncc2C(=O)NCCOc2ccccc2)cc(OC)c1OC
CHEMBL604302 casr_human Human No 5.0 IC50 = 10000 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
411 6 1 4 6.4 CC(C)c1ccc(-c2nc(=O)n(C(C)C)c3ccc(NCc4ccccc4)cc23)cc1
CHEMBL482873 casr_human Human No 5.0 IC50 = 10000 nM Bind
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
295 9 2 4 2.4 COc1ccc(CC(C)(C)NCC(O)COC(C)C)cc1
CHEMBL455406 casr_human Human No 6.0 IC50 = 1050 nM Funct
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
512 12 1 7 5.0 CCN(Cc1ccccc1)c1ccc(C(=O)NCCOc2ccccc2)c(-c2ccc(OC)nc2OC)n1
CHEMBL1689054 casr_human Human No 8.0 IC50 = 11 nM Funct
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
490 8 2 6 5.9 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(OC)c(OC)c1
CHEMBL1739754 casr_human Human No 8.0 IC50 = 11 nM Funct
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
490 8 2 6 5.9 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(OC)c(OC)c1
CHEMBL1689056 casr_human Human No 8.0 IC50 = 11 nM Funct
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
478 7 2 5 6.1 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(F)c(OC)c1
CHEMBL1739757 casr_human Human No 8.0 IC50 = 11 nM Funct
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
478 7 2 5 6.1 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(F)c(OC)c1
CHEMBL1689043 casr_human Human No 8.0 IC50 = 11 nM Funct
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
486 9 2 4 7.3 CCCCc1nn2c(c1C(=O)NC(CC)(CC)c1ccc(C)cc1)NC(c1ccccc1)CC2(C)C
CHEMBL1739942 casr_human Human No 8.0 IC50 = 11 nM Funct
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
486 9 2 4 7.3 CCCCc1nn2c(c1C(=O)NC(CC)(CC)c1ccc(C)cc1)NC(c1ccccc1)CC2(C)C
CHEMBL1223507 casr_human Human No 8.0 IC50 = 11 nM Funct
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
470 6 0 4 6.3 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(Br)c(C(F)(F)F)cc(OC)c21
CHEMBL1672969 casr_human Human No 8.0 IC50 = 11 nM Funct
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
497 11 3 4 6.3 CC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1-c1ccc(C(=O)O)cc1
CHEMBL486278 casr_human Human No 8.0 IC50 = 11 nM Funct
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
385 9 4 5 2.2 COc1ccc(CC(C)(C)NC[C@H](O)COc2cccc3[nH]c(=O)[nH]c23)cc1
CHEMBL4125724 casr_rat Rat No 7.9 IC50 = 11.7 nM Funct
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
400 5 1 3 5.7 C[C@@H](N[C@H]1CCN(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12
CHEMBL4302236 casr_rat Rat No 7.9 IC50 = 11.7 nM Funct
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
400 5 1 3 5.7 C[C@@H](N[C@H]1CCN(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12
CHEMBL1289573 casr_human Human No 7.0 IC50 = 110 nM Funct
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
478 3 2 4 5.9 O=C(NC12CC3CC(CC(C3)C1)C2)c1cnn2c1N[C@H](c1ccccc1Cl)C[C@@H]2C(F)(F)F
CHEMBL599467 casr_human Human No 6.0 IC50 = 1100 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
364 6 0 4 5.6 CCCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C
CHEMBL599858 casr_human Human No 6.0 IC50 = 1100 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
363 6 1 4 5.6 CCCNc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C
CHEMBL194063 casr_human Human No 6.0 IC50 = 1100 nM Bind
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
324 4 1 4 3.3 Cc1cc(=O)n(CCc2cccc(F)c2)c(-c2ccccc2O)n1
CHEMBL434937 casr_human Human No 5.0 IC50 = 11360 nM Funct
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
421 10 2 6 2.8 COc1ccc(CC(C)(C)NCC(O)COc2ccc(S(C)(=O)=O)c(C)c2)cc1
CHEMBL4129371 casr_rat Rat No 6.9 IC50 = 116 nM Funct
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
400 5 1 3 5.7 C[C@@H](N[C@@H]1CCN(c2ccc(OC(F)(F)F)cc2)C1)c1cccc2ccccc12
CHEMBL4301708 casr_rat Rat No 6.9 IC50 = 116 nM Funct
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
400 5 1 3 5.7 C[C@@H](N[C@@H]1CCN(c2ccc(OC(F)(F)F)cc2)C1)c1cccc2ccccc12
CHEMBL200297 casr_human Human No 5.9 IC50 = 1160 nM Funct
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
418 8 3 4 4.5 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(O)c1
CHEMBL3827912 casr_human Human No 6.9 IC50 = 117.3 nM Funct
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
479 10 3 5 4.2 Cc1ccc(C(C)OC[C@H](O)CNC(C)(C)CC2Cc3ccccc3C2)c2c1OC1C(C(=O)O)C21
CHEMBL265362 casr_human Human No 5.9 IC50 = 1190 nM Funct
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
432 9 2 4 4.8 COc1cccc(CN2CCC[C@@H]2[C@H](O)CNC(C)(C)Cc2ccc3ccccc3c2)c1
CHEMBL1672973 casr_human Human Yes 7.9 IC50 = 12 nM Funct
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
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
CHEMBL1688086 casr_human Human No 7.9 IC50 = 12 nM Funct
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
434 6 2 4 5.8 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccccc1F
CHEMBL1688092 casr_human Human No 7.9 IC50 = 12 nM Funct
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
488 8 2 6 5.9 CCC(=O)Oc1ccc(C(CC)(CC)NC(=O)c2cnn3c2NC(c2ccccc2)CC3(C)C)cc1
CHEMBL603248 casr_human Human No 7.9 IC50 = 12.6 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
482 9 1 6 4.7 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1ccc(OCC(=O)O)cc1
CHEMBL597812 casr_human Human No 6.9 IC50 = 120 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
397 6 0 4 4.8 C#CCN(CC#C)c1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C
CHEMBL1083313 casr_human Human No 6.9 IC50 = 120 nM Funct
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
407 10 2 4 4.9 COc1ccccc1C(C)OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1
CHEMBL195305 casr_human Human No 6.9 IC50 = 120 nM Bind
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
364 5 1 4 4.2 Cc1nc(-c2ccccc2O)n(CCc2cccc(F)c2)c(=O)c1C1CC1
CHEMBL199964 casr_human Human No 5.9 IC50 = 1270 nM Funct
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
427 8 2 4 4.6 CC(C)(Cc1ccc2ccccc2c1)NC[C@H](O)[C@H]1CCCN1Cc1ccccc1C#N
CHEMBL1689107 casr_human Human No 7.9 IC50 = 13 nM Funct
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
474 7 3 5 6.0 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(C(C)O)cc1
CHEMBL590552 casr_human Human No 7.9 IC50 = 13 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
607 12 1 8 4.5 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1cccc(NC(=O)CN2CCN(CCOC)CC2)c1
CHEMBL598637 casr_human Human No 7.9 IC50 = 13 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
436 7 0 4 5.8 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1cccc(CC)c1
CHEMBL1223368 casr_human Human No 7.9 IC50 = 13 nM Funct
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
450 6 0 4 5.1 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(I)ccc(OC)c21
CHEMBL4127153 casr_rat Rat No 7.9 IC50 = 13.1 nM Funct
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
384 4 1 2 5.8 C[C@@H](N[C@H]1CCN(c2cccc(C(F)(F)F)c2)C1)c1cccc2ccccc12
CHEMBL4299885 casr_rat Rat No 7.9 IC50 = 13.1 nM Funct
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
384 4 1 2 5.8 C[C@@H](N[C@H]1CCN(c2cccc(C(F)(F)F)c2)C1)c1cccc2ccccc12
CHEMBL451383 casr_human Human No 6.9 IC50 = 130 nM Funct
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
557 12 2 9 4.9 COc1cc(-c2nc(NCc3ccc4c(c3)OCO4)ccc2C(=O)NCCOc2ccccc2)cc(OC)c1OC
CHEMBL487511 casr_human Human No 5.9 IC50 = 1300 nM Bind
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
379 9 2 4 4.2 COc1ccc(CC(C)(C)NCC(O)COc2ccc3ccccc3c2)cc1
CHEMBL3828329 casr_human Human No 5.9 IC50 = 1332 nM Funct
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
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
CHEMBL381685 casr_human Human No 5.9 IC50 = 1350 nM Funct
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
434 8 2 6 4.1 CC(C)(Cc1nc2ccccc2s1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(C#N)c1
CHEMBL201381 casr_human Human No 5.9 IC50 = 1390 nM Funct
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
359 10 2 5 3.1 COc1ccc(CC(C)(C)NC[C@H](O)COc2cccc(OC)c2)cc1
CHEMBL1223505 casr_human Human No 7.9 IC50 = 14 nM Funct
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
480 6 0 4 6.0 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(Br)c(Br)cc(OC)c21
CHEMBL1688090 casr_human Human No 7.9 IC50 = 14 nM Funct
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
488 8 2 6 5.7 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(COC(C)=O)cc1
CHEMBL515828 casr_human Human Yes 6.9 IC50 = 140 nM Funct
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
528 13 3 8 4.0 COc1ccc(-c2nc(N[C@H](CO)Cc3ccccc3)ccc2C(=O)NCCOc2ccccc2)c(OC)n1
CHEMBL1082999 casr_human Human No 6.9 IC50 = 140 nM Funct
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
391 9 2 3 5.2 Cc1ccc(C(C)OC[C@H](O)CNC(C)(C)Cc2ccc3ccccc3c2)cc1
CHEMBL1083307 casr_human Human No 6.9 IC50 = 140 nM Funct
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
411 9 2 3 5.5 CC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1Cl
CHEMBL504479 casr_human Human No 6.9 IC50 = 140 nM Bind
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
354 9 2 5 2.9 COc1ccc(CC(C)(C)NCC(O)COc2ccccc2C#N)cc1
CHEMBL199495 casr_human Human No 6.9 IC50 = 140 nM Funct
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
436 8 3 4 4.6 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(F)c1O
CHEMBL372321 casr_human Human No 6.9 IC50 = 140 nM Funct
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
463 9 3 6 4.4 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc([N+](=O)[O-])c1O
CHEMBL372820 casr_human Human No 6.9 IC50 = 140 nM Funct
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
447 9 2 5 4.7 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc([N+](=O)[O-])c1
CHEMBL195566 casr_human Human No 6.9 IC50 = 140 nM Bind
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
366 6 1 4 4.3 CCCc1c(C)nc(-c2ccccc2O)n(CCc2cccc(F)c2)c1=O
CHEMBL369998 casr_human Human No 6.9 IC50 = 140 nM Bind
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
348 4 1 3 3.8 O=C1C2CCCCC2N=C(c2ccccc2O)N1CCc1ccccc1
CHEMBL597206 casr_human Human Yes 5.9 IC50 = 1400 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
336 4 0 4 4.8 COc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C
CHEMBL180391 casr_human Human Yes 4.9 IC50 = 14000 nM Bind
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
326 4 0 3 4.3 O=c1c2ccccc2nc(-c2ccccc2)n1CCc1ccccc1
CHEMBL1198855 casr_human Human Yes 6.8 IC50 = 146 nM Funct
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
447 11 3 4 3.9 O[C@@H](COc1cc(CCC(=O)O)cc(c1F)F)CNC(CC1Cc2c(C1)cccc2)(C)C
CHEMBL1223711 casr_human Human No 7.8 IC50 = 15 nM Funct
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
493 8 0 5 6.2 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(Br)c(Cc3cccnc3)cc(OC)c21
CHEMBL454385 casr_human Human No 6.8 IC50 = 150 nM Funct
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
561 10 2 9 4.9 COc1ccc(-c2nc(NCc3ccc4c(c3)OCO4)ncc2C(=O)NC(C)Cc2ccc(Cl)cc2)c(OC)n1
CHEMBL495263 casr_human Human No 6.8 IC50 = 150 nM Funct
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
558 14 3 9 4.0 COc1cc(-c2nc(N[C@H](CO)Cc3ccccc3)ncc2C(=O)NCCOc2ccccc2)cc(OC)c1OC
CHEMBL509410 casr_human Human No 6.8 IC50 = 150 nM Funct
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
558 12 2 10 4.3 COc1cc(-c2nc(NCc3ccc4c(c3)OCO4)ncc2C(=O)NCCOc2ccccc2)cc(OC)c1OC
CHEMBL1082306 casr_human Human No 6.8 IC50 = 150 nM Funct
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
405 11 2 3 5.7 CCCC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1
CHEMBL1689814 casr_human Human No 6.8 IC50 = 150 nM Funct
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
592 6 2 4 9.0 CC1(C)CC(c2ccccc2)Nc2c(C(=O)NC(c3ccc(C(F)(F)F)cc3)(C3CCCCC3)C3CCCCC3)cnn21
CHEMBL494646 casr_human Human No 5.8 IC50 = 1500 nM Funct
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
542 13 1 8 4.7 COc1cc(-c2nc(N(C)CCc3ccccc3)ncc2C(=O)NCCOc2ccccc2)cc(OC)c1OC
CHEMBL1672967 casr_human Human No 5.8 IC50 = 1500 nM Funct
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
497 11 3 4 6.3 CC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccc(-c2ccc(C(=O)O)cc2)cc1
CHEMBL454386 casr_human Human No 6.8 IC50 = 154 nM Funct
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
541 13 1 7 5.6 CCN(Cc1ccccc1)c1ccc(C(=O)NCCOc2ccccc2)c(-c2cc(OC)c(OC)c(OC)c2)n1
CHEMBL200422 casr_human Human No 5.8 IC50 = 1560 nM Funct
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
448 9 3 5 4.5 COc1cccc(CN2CCC[C@@H]2[C@H](O)CNC(C)(C)Cc2ccc3ccccc3c2)c1O
CHEMBL263828 casr_human Human No 5.8 IC50 = 1570 nM Funct
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
480 8 2 3 5.5 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(Br)c1
CHEMBL597011 casr_human Human Yes 4.8 IC50 = 15900 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
322 3 1 4 4.5 CC(C)c1ccc(-c2nc(=O)n(C(C)C)c3ccc(O)cc23)cc1
CHEMBL1223508 casr_human Human No 7.8 IC50 = 16 nM Funct
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
470 6 0 4 6.3 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(C(F)(F)F)c(Br)cc(OC)c21
CHEMBL1082787 casr_human Human No 6.8 IC50 = 160 nM Funct
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
402 9 2 4 4.8 CC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1C#N
CHEMBL197863 casr_human Human No 6.8 IC50 = 160 nM Funct
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
447 9 2 5 4.7 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1ccccc1[N+](=O)[O-]
CHEMBL194490 casr_human Human No 6.8 IC50 = 160 nM Bind
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
366 4 1 3 3.9 O=C1C2CCCCC2N=C(c2ccccc2O)N1CCc1cccc(F)c1
CHEMBL178442 casr_human Human No 5.8 IC50 = 1600 nM Bind
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
394 4 1 4 4.8 O=c1c2ccc(Cl)cc2nc(-c2ccccc2O)n1CCc1cccc(F)c1
CHEMBL182107 casr_human Human No 5.8 IC50 = 1600 nM Bind
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
358 4 2 5 3.7 O=c1c2ccccc2nc(-c2cc(O)ccc2O)n1CCc1ccccc1
CHEMBL373306 casr_human Human No 5.8 IC50 = 1600 nM Bind
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
324 4 1 4 3.3 Cc1cc(=O)n(CCc2ccccc2F)c(-c2ccccc2O)n1
CHEMBL514434 casr_human Human No 6.8 IC50 = 162 nM Funct
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
547 12 2 7 5.8 COc1cc(-c2nc(NCc3cccc(Cl)c3)ccc2C(=O)NCCOc2ccccc2)cc(OC)c1OC
CHEMBL1689817 casr_human Human No 7.8 IC50 = 17 nM Funct
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
450 6 2 4 6.3 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1cccc(Cl)c1
CHEMBL3827570 casr_human Human No 7.8 IC50 = 17.7 nM Funct
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
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
CHEMBL591241 casr_human Human No 6.8 IC50 = 170 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
374 5 0 4 5.2 CC#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C
CHEMBL1082718 casr_human Human No 6.8 IC50 = 170 nM Funct
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
419 12 2 3 6.1 CCCCC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1
CHEMBL1082998 casr_human Human No 6.8 IC50 = 170 nM Funct
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
391 9 2 3 5.2 Cc1cccc(C(C)OC[C@H](O)CNC(C)(C)Cc2ccc3ccccc3c2)c1
CHEMBL193498 casr_human Human No 6.8 IC50 = 170 nM Bind
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
338 4 1 4 3.6 Cc1nc(-c2ccccc2O)n(CCc2cccc(F)c2)c(=O)c1C
CHEMBL1196384 casr_rat Rat No 5.8 IC50 = 1700 nM Funct
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
456 6 2 3 6.1 C[C@@H](N[C@@H]1CCCC[C@H]1NC(=O)c1ccc(OC(F)(F)F)cc1)c1cccc2ccccc12
CHEMBL556781 casr_rat Rat No 5.8 IC50 = 1700 nM Funct
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
456 6 2 3 6.1 C[C@@H](N[C@@H]1CCCC[C@H]1NC(=O)c1ccc(OC(F)(F)F)cc1)c1cccc2ccccc12
CHEMBL1223299 casr_human Human No 4.8 IC50 = 17000 nM Funct
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
294 5 0 3 4.5 COCCn1c(-c2ccc(C(C)C)cc2)nc2ccccc21
CHEMBL1672960 casr_human Human No 7.8 IC50 = 18 nM Funct
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
433 11 3 4 4.8 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)CO[C@@H](c1ccccc1CO)C1CC1
CHEMBL1672968 casr_human Human No 7.8 IC50 = 18 nM Funct
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
497 11 3 4 6.3 CC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1cccc(-c2ccc(C(=O)O)cc2)c1
CHEMBL1783935 casr_human Human No 7.8 IC50 = 18 nM Funct
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
525 11 3 4 5.8 Cc1ccc(CC(C)(C)NC[C@@H](O)CO[C@H](C)c2ccccc2C2CC3CC2C2C(C(=O)O)C32)cc1Cl
CHEMBL599228 casr_human Human No 6.8 IC50 = 180 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
362 6 0 4 5.3 C=CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C
CHEMBL511485 casr_human Human No 5.8 IC50 = 1800 nM Funct
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
554 14 1 7 5.9 CCN(Cc1ccccc1)c1ncc(C(=O)NCCCCc2ccccc2)c(-c2cc(OC)c(OC)c(OC)c2)n1
CHEMBL1223370 casr_human Human No 5.7 IC50 = 1820 nM Funct
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
354 7 0 5 4.5 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(OC)ccc(OC)c21
CHEMBL472731 casr_human Human No 4.7 IC50 = 18900 nM Funct
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
506 9 1 5 5.6 CN(Cc1ccccc1)c1ncc(C(=O)NCCOc2ccccc2)c(-c2ccc(C(F)(F)F)cc2)n1
CHEMBL596789 casr_human Human No 7.7 IC50 = 19 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
452 8 0 5 5.6 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1ccc(OCC)cc1
CHEMBL3828187 casr_human Human No 7.7 IC50 = 19.6 nM Funct
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
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
CHEMBL1222424 casr_human Human No 6.7 IC50 = 190 nM Funct
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
430 7 0 4 5.8 CCc1cc(OC)c2c(nc(-c3ccc(C(C)C)cc3)n2CCOC)c1Br
CHEMBL1223438 casr_human Human No 6.7 IC50 = 190 nM Funct
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
415 6 0 4 5.2 COc1ccc(Br)c2nc(-c3ccc(C(C)C)cc3)n(CCN(C)C)c12
CHEMBL199716 casr_human Human No 6.7 IC50 = 190 nM Funct
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
427 8 2 4 4.6 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(C#N)c1
CHEMBL180463 casr_human Human No 6.7 IC50 = 190 nM Bind
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
378 4 1 4 4.3 O=c1c2cc(F)ccc2nc(-c2ccccc2O)n1CCc1cccc(F)c1
CHEMBL1223300 casr_human Human No 5.7 IC50 = 1900 nM Funct
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
324 6 0 4 4.5 COCCn1c(-c2ccc(C(C)C)cc2)nc2cccc(OC)c21
CHEMBL1223302 casr_human Human No 5.7 IC50 = 1900 nM Funct
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
338 6 0 4 4.8 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(OC)ccc(C)c21
CHEMBL195176 casr_human Human No 5.7 IC50 = 1900 nM Bind
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
306 4 1 4 3.2 Cc1cc(=O)n(CCc2ccccc2)c(-c2ccccc2O)n1
CHEMBL1223222 casr_human Human No 5.7 IC50 = 1950 nM Funct
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
336 6 0 3 5.6 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(C(C)C)cccc21
CHEMBL460726 casr_human Human No 6.7 IC50 = 197 nM Funct
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
518 11 2 7 5.2 COc1ccc(-c2nc(NCc3cccc(Cl)c3)ccc2C(=O)NCCOc2ccccc2)c(OC)n1
CHEMBL1689052 casr_human Human No 8.7 IC50 = 2 nM Funct
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
460 7 2 5 5.9 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(OC)cc1
CHEMBL1739919 casr_human Human No 8.7 IC50 = 2 nM Funct
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
460 7 2 5 5.9 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(OC)cc1
CHEMBL1223772 casr_human Human No 8.7 IC50 = 2 nM Funct
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
489 8 0 6 6.5 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(C(F)(F)F)c(Cc3nccs3)cc(OC)c21
CHEMBL4125917 casr_rat Rat No 8.7 IC50 = 2.1 nM Funct
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
398 4 1 2 6.2 C[C@@H](N[C@@H]1CCCN(c2cccc(C(F)(F)F)c2)C1)c1cccc2ccccc12
CHEMBL4300173 casr_rat Rat No 8.7 IC50 = 2.1 nM Funct
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
398 4 1 2 6.2 C[C@@H](N[C@@H]1CCCN(c2cccc(C(F)(F)F)c2)C1)c1cccc2ccccc12
CHEMBL1689055 casr_human Human No 8.7 IC50 = 2.2 nM Funct
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
536 9 2 5 7.5 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(OCc2ccccc2)cc1
CHEMBL1739755 casr_human Human No 8.7 IC50 = 2.2 nM Funct
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
536 9 2 5 7.5 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(OCc2ccccc2)cc1
CHEMBL1688099 casr_human Human No 8.6 IC50 = 2.3 nM Funct
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
430 6 2 4 5.9 CCC(CC)(NC(=O)c1cnn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(C)cc1
CHEMBL1739780 casr_human Human No 8.6 IC50 = 2.3 nM Funct
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
430 6 2 4 5.9 CCC(CC)(NC(=O)c1cnn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(C)cc1
CHEMBL1689049 casr_human Human No 8.6 IC50 = 2.3 nM Funct
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
430 6 2 4 5.9 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccccc1
CHEMBL1739916 casr_human Human No 8.6 IC50 = 2.3 nM Funct
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
430 6 2 4 5.9 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccccc1
CHEMBL1688099 casr_human Human No 8.6 IC50 = 2.3 nM Funct
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
430 6 2 4 5.9 CCC(CC)(NC(=O)c1cnn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(C)cc1
CHEMBL1739780 casr_human Human No 8.6 IC50 = 2.3 nM Funct
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
430 6 2 4 5.9 CCC(CC)(NC(=O)c1cnn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(C)cc1
CHEMBL1689047 casr_human Human No 8.6 IC50 = 2.4 nM Funct
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
444 6 2 4 6.2 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(C)cc1
CHEMBL1739733 casr_human Human No 8.6 IC50 = 2.4 nM Funct
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
444 6 2 4 6.2 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(C)cc1
CHEMBL590539 casr_human Human No 8.6 IC50 = 2.4 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
563 9 1 7 4.4 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1cccc(NC(=O)CN2CCN(C)CC2)c1
CHEMBL597208 casr_human Human No 8.6 IC50 = 2.5 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
424 6 1 4 5.9 CC(C)c1ccc(-c2nc(=O)n(Cc3ccccc3)c3ccc(O)c(CC4CC4)c23)cc1
CHEMBL1223771 casr_human Human No 8.6 IC50 = 2.6 nM Funct
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
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
CHEMBL604506 casr_human Human No 8.6 IC50 = 2.7 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
438 7 0 5 5.3 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1cccc(OC)c1
CHEMBL3827736 casr_human Human No 7.7 IC50 = 20 nM Funct
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
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
CHEMBL508063 casr_human Human No 6.7 IC50 = 200 nM Funct
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
542 13 1 8 5.0 CCN(Cc1ccccc1)c1ncc(C(=O)NCCOc2ccccc2)c(-c2cc(OC)c(OC)c(OC)c2)n1
CHEMBL1082717 casr_human Human No 6.7 IC50 = 200 nM Funct
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
405 10 2 3 5.5 CC(C)C(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1
CHEMBL1083610 casr_human Human No 6.7 IC50 = 200 nM Funct
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
391 9 2 3 5.2 Cc1ccccc1C(C)OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1
CHEMBL1084200 casr_human Human No 6.7 IC50 = 200 nM Funct
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
431 10 2 3 6.1 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COC(c1ccccc1)C1CCCC1
CHEMBL491251 casr_human Human No 6.7 IC50 = 200 nM Bind
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
397 9 2 4 4.4 COc1ccc(CC(C)(C)NCC(O)COc2cccc(Cl)c2Cl)cc1
CHEMBL195375 casr_human Human No 6.7 IC50 = 200 nM Bind
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
352 4 1 3 3.5 O=C1C2CCCC2N=C(c2ccccc2O)N1CCc1cccc(F)c1
CHEMBL370503 casr_human Human No 6.7 IC50 = 200 nM Bind
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
334 4 1 3 3.4 O=C1C2CCCC2N=C(c2ccccc2O)N1CCc1ccccc1
CHEMBL371828 casr_human Human No 6.7 IC50 = 200 nM Bind
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
320 4 1 4 3.5 Cc1nc(-c2ccccc2O)n(CCc2ccccc2)c(=O)c1C
CHEMBL3828182 casr_human Human No 6.7 IC50 = 202.7 nM Funct
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
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
CHEMBL3828483 casr_human Human No 7.7 IC50 = 21.6 nM Funct
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
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
CHEMBL3827475 casr_human Human No 7.7 IC50 = 21.8 nM Funct
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
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
CHEMBL1223439 casr_human Human No 6.7 IC50 = 210 nM Funct
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
338 6 0 4 4.8 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(C)ccc(OC)c21
CHEMBL1082712 casr_human Human No 6.7 IC50 = 210 nM Funct
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
389 10 2 3 5.1 C=CC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1
CHEMBL488736 casr_human Human No 6.7 IC50 = 210 nM Bind
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
349 8 2 3 4.2 CC(C)(Cc1cccc2ccccc12)NCC(O)COc1ccccc1
CHEMBL183287 casr_human Human No 6.7 IC50 = 210 nM Bind
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
360 4 1 4 4.2 O=c1c2cc(F)ccc2nc(-c2ccccc2O)n1CCc1ccccc1
CHEMBL472406 casr_human Human No 5.7 IC50 = 2100 nM Funct
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
540 13 1 7 5.6 CCN(Cc1ccccc1)c1ncc(C(=O)NCCCc2ccccc2)c(-c2cc(OC)c(OC)c(OC)c2)n1
CHEMBL599664 casr_human Human No 5.7 IC50 = 2100 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
322 4 0 4 4.2 CCc1ccc(-c2nc(=O)n(C(C)C)c3ccc(OC)cc23)cc1
CHEMBL599868 casr_human Human No 5.7 IC50 = 2100 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
350 3 0 4 5.0 COc1ccc2c(c1)c(-c1ccc(C(C)(C)C)cc1)nc(=O)n2C(C)C
CHEMBL1223301 casr_human Human No 5.7 IC50 = 2100 nM Funct
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
308 5 0 3 4.8 COCCn1c(-c2ccc(C(C)C)cc2)nc2cccc(C)c21
CHEMBL1223367 casr_human Human Yes 7.7 IC50 = 22 nM Funct
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
402 6 0 4 5.2 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(Br)ccc(OC)c21
CHEMBL458516 casr_human Human No 6.7 IC50 = 220 nM Funct
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
529 11 2 10 3.7 COc1ccc(-c2nc(NCc3ccc4c(c3)OCO4)ncc2C(=O)NCCOc2ccccc2)c(OC)n1
CHEMBL1083308 casr_human Human No 6.7 IC50 = 220 nM Funct
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
411 9 2 3 5.5 CC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1cccc(Cl)c1
CHEMBL1084757 casr_human Human No 6.7 IC50 = 220 nM Funct
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
377 9 2 3 4.9 CC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1
CHEMBL454375 casr_human Human No 5.7 IC50 = 2200 nM Funct
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
494 13 2 8 4.4 COc1cc(-c2nc(NCCC(C)C)ncc2C(=O)NCCOc2ccccc2)cc(OC)c1OC
CHEMBL608721 casr_human Human No 5.7 IC50 = 2200 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
350 5 0 4 5.2 CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C
CHEMBL1672965 casr_human Human No 5.7 IC50 = 2200 nM Funct
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
435 11 3 4 4.5 C[C@@H](OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1CC(=O)O
CHEMBL199716 casr_rat Rat No 5.7 IC50 = 2200 nM Funct
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
427 8 2 4 4.6 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(C#N)c1
CHEMBL1083949 casr_human Human No 5.7 IC50 = 2240 nM Funct
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
391 9 2 3 5.1 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COC(C)(C)c1ccccc1
CHEMBL1086282 casr_human Human No 7.6 IC50 = 23 nM Funct
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
417 10 2 3 5.6 Cc1ccccc1[C@H](OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)C1CC1
CHEMBL1086282 casr_human Human No 7.6 IC50 = 23 nM Funct
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
417 10 2 3 5.6 Cc1ccccc1[C@H](OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)C1CC1
CHEMBL1672971 casr_human Human No 7.6 IC50 = 23 nM Funct
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
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
CHEMBL1689812 casr_human Human No 7.6 IC50 = 23 nM Funct
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
540 10 2 4 8.2 CCCCC(CCCC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C(F)(F)F)cc1
CHEMBL180672 casr_human Human Yes 7.6 IC50 = 23 nM Funct
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
408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O
CHEMBL1783931 casr_human Human No 7.6 IC50 = 23 nM Funct
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
506 10 3 5 4.4 Cc1ccc(CC(C)(C)NC[C@@H](O)COc2cc(C3CC4CC3C3C(C(=O)O)C43)ccc2C#N)cc1F
CHEMBL610511 casr_human Human No 6.6 IC50 = 230 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
375 6 0 4 5.4 C=CCN(C)c1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C
CHEMBL488337 casr_human Human No 5.6 IC50 = 2300 nM Bind
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
329 9 2 4 3.0 COc1ccc(CC(C)(C)NCC(O)COc2ccccc2)cc1
CHEMBL488737 casr_human Human No 5.6 IC50 = 2300 nM Bind
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
411 9 1 4 4.7 COc1ccc(CC(C)(C)N(C)CC(O)COc2cccc(Cl)c2Cl)cc1
CHEMBL1672966 casr_human Human No 7.6 IC50 = 24 nM Funct
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
449 12 3 4 4.9 C[C@@H](OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1CCC(=O)O
CHEMBL203479 casr_human Human No 6.6 IC50 = 240 nM Funct
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
461 8 2 4 5.3 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(Cl)c1C#N
CHEMBL425394 casr_human Human No 5.6 IC50 = 2470 nM Funct
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
478 9 2 3 6.4 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(-c2ccccc2)c1
CHEMBL1223509 casr_human Human No 7.6 IC50 = 25 nM Funct
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
427 6 0 5 5.1 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(Br)c(C#N)cc(OC)c21
CHEMBL2368751 casr_human Human No 7.6 IC50 = 25 nM Bind
Inhibition of CaSRInhibition of CaSR
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
CHEMBL1688085 casr_human Human No 7.6 IC50 = 25 nM Funct
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
434 6 2 4 5.8 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1cccc(F)c1
CHEMBL1783933 casr_human Human No 7.6 IC50 = 25 nM Funct
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
509 11 3 4 5.3 Cc1ccc(CC(C)(C)NC[C@@H](O)CO[C@H](C)c2ccccc2C2CC3CC2C2C(C(=O)O)C32)cc1F
CHEMBL1188646 casr_rat Rat No 6.6 IC50 = 250 nM Funct
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
456 6 2 3 6.1 C[C@@H](N[C@H]1CCCC[C@@H]1NC(=O)c1ccc(OC(F)(F)F)cc1)c1cccc2ccccc12
CHEMBL536975 casr_rat Rat No 6.6 IC50 = 250 nM Funct
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
456 6 2 3 6.1 C[C@@H](N[C@H]1CCCC[C@@H]1NC(=O)c1ccc(OC(F)(F)F)cc1)c1cccc2ccccc12
CHEMBL199548 casr_human Human No 6.6 IC50 = 250 nM Funct
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
427 8 2 4 4.6 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1ccc(C#N)cc1
CHEMBL360226 casr_human Human No 6.6 IC50 = 250 nM Bind
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
374 4 1 4 4.5 Cc1cccc2nc(-c3ccccc3O)n(CCc3cccc(F)c3)c(=O)c12
CHEMBL361623 casr_human Human No 6.6 IC50 = 250 nM Bind
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
356 4 1 4 4.3 Cc1cccc2nc(-c3ccccc3O)n(CCc3ccccc3)c(=O)c12
CHEMBL1223221 casr_human Human No 5.6 IC50 = 2550 nM Funct
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
334 6 0 2 6.8 CCCCn1c(-c2ccc(C(C)C)cc2)nc2c(C(C)C)cccc21
CHEMBL199495 casr_rat Rat No 5.6 IC50 = 2560 nM Funct
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
436 8 3 4 4.6 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(F)c1O
CHEMBL1222489 casr_human Human No 7.6 IC50 = 26 nM Funct
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
512 9 0 5 7.1 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(C(F)(F)F)c(Cc3ccccc3OC)cc(OC)c21
CHEMBL180672 casr_human Human Yes 7.6 IC50 = 26 nM Funct
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
408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O
CHEMBL1188810 casr_rat Rat No 5.6 IC50 = 2600 nM Funct
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
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
CHEMBL537427 casr_rat Rat No 5.6 IC50 = 2600 nM Funct
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
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
CHEMBL370671 casr_human Human No 5.6 IC50 = 2670 nM Funct
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
407 9 2 5 3.5 COc1ccc(CC(C)(C)NC[C@@H](O)[C@H]2CCCN2Cc2cccc(C#N)c2)cc1
CHEMBL604713 casr_human Human No 7.6 IC50 = 27 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
450 7 0 4 6.4 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1ccc(C(C)C)cc1
CHEMBL3827041 casr_human Human No 7.6 IC50 = 27.6 nM Funct
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
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
CHEMBL200312 casr_human Human No 6.6 IC50 = 270 nM Funct
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
433 8 2 5 4.7 N#Cc1cccc(c1)CN1CCC[C@@H]1[C@@H](CNC(Cc1cc2c(s1)cccc2)(C)C)O
CHEMBL370811 casr_human Human No 6.6 IC50 = 270 nM Funct
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
422 8 1 4 5.1 CN(C[C@@H](O)COc1cccc(Cl)c1C#N)C(C)(C)Cc1ccc2ccccc2c1
CHEMBL599025 casr_human Human No 5.6 IC50 = 2700 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
364 5 0 4 5.6 CC(C)Oc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C
CHEMBL483080 casr_human Human No 5.6 IC50 = 2780 nM Bind
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
343 10 2 4 3.4 COc1ccc(CCC(C)(C)NCC(O)COc2ccccc2)cc1
CHEMBL3827830 casr_human Human No 7.6 IC50 = 28.4 nM Funct
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
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
CHEMBL523701 casr_human Human No 5.6 IC50 = 2800 nM Funct
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
558 14 2 9 4.6 COc1ccc(CCNc2ncc(C(=O)NCCOc3ccccc3)c(-c3cc(OC)c(OC)c(OC)c3)n2)cc1
CHEMBL179333 casr_human Human Yes 5.6 IC50 = 2800 nM Bind
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
342 4 1 4 4.0 O=c1c2ccccc2nc(-c2cccc(O)c2)n1CCc1ccccc1
CHEMBL383609 casr_human Human No 5.6 IC50 = 2840 nM Funct
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
417 8 3 5 3.4 CC(C)(Cc1nc2ccccc2[nH]1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(C#N)c1
CHEMBL599039 casr_human Human No 5.5 IC50 = 2900 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
405 8 0 4 6.4 CCCN(CCC)c1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C
CHEMBL1688101 casr_human Human No 5.5 IC50 = 2900 nM Funct
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
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
CHEMBL1689053 casr_human Human No 8.5 IC50 = 3 nM Funct
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
474 8 2 5 6.3 CCOc1ccc(C(CC)(CC)NC(=O)c2c(C)nn3c2N[C@@H](c2ccccc2)CC3(C)C)cc1
CHEMBL1739920 casr_human Human No 8.5 IC50 = 3 nM Funct
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
474 8 2 5 6.3 CCOc1ccc(C(CC)(CC)NC(=O)c2c(C)nn3c2N[C@@H](c2ccccc2)CC3(C)C)cc1
CHEMBL180672 casr_human Human Yes 8.5 IC50 = 3 nM Bind
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
408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O
CHEMBL597194 casr_human Human No 8.5 IC50 = 3.4 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
482 9 1 6 4.7 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1cccc(OCC(=O)O)c1
CHEMBL1689815 casr_human Human No 8.5 IC50 = 3.4 nM Funct
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
416 6 2 4 5.6 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccccc1
CHEMBL1689809 casr_human Human No 8.5 IC50 = 3.5 nM Funct
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
456 4 2 4 5.9 CC(C)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C(F)(F)F)cc1
CHEMBL598638 casr_human Human No 8.4 IC50 = 3.9 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
410 6 1 4 5.7 C=CCc1c(O)ccc2c1c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1ccccc1
CHEMBL597811 casr_human Human Yes 7.5 IC50 = 30 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
359 5 1 4 4.8 C#CCNc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C
CHEMBL1689813 casr_human Human No 7.5 IC50 = 30 nM Funct
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
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
CHEMBL382741 casr_human Human No 7.5 IC50 = 30 nM Funct
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
374 8 2 4 4.1 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COc1ccccc1C#N
CHEMBL4297621 casr_rat Rat Yes 7.5 IC50 = 30.8 nM Funct
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
374 6 2 3 4.4 OC(=O)Cc1ccc(cc1)N1CC[C@@H](C1)N[C@@H](c1cccc2c1cccc2)C
CHEMBL1083951 casr_human Human No 6.5 IC50 = 300 nM Funct
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
405 11 2 3 5.3 CC(CCOC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1
CHEMBL487508 casr_human Human No 6.5 IC50 = 300 nM Bind
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
397 9 2 4 4.4 COc1ccc(CC(C)(C)NC[C@H](O)COc2cccc(Cl)c2Cl)cc1
CHEMBL180030 casr_human Human No 6.5 IC50 = 300 nM Bind
Inhibition of CaSRInhibition of CaSR
342 4 1 4 4.0 O=c1c2ccccc2nc(-c2ccccc2O)n1CCc1ccccc1
CHEMBL180030 casr_human Human No 6.5 IC50 = 300 nM Bind
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
342 4 1 4 4.0 O=c1c2ccccc2nc(-c2ccccc2O)n1CCc1ccccc1
CHEMBL361333 casr_human Human No 6.5 IC50 = 300 nM Bind
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
376 4 1 4 4.7 O=c1c2cc(Cl)ccc2nc(-c2ccccc2O)n1CCc1ccccc1
CHEMBL1783766 casr_human Human No 6.5 IC50 = 300 nM Funct
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
499 10 3 4 4.7 Cc1ccc(CC(C)(C)NC[C@@H](O)COc2cc(C3CC4CC3C3C(C(=O)O)C43)ccc2F)cc1F
CHEMBL1689048 casr_human Human No 7.5 IC50 = 31 nM Funct
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
444 6 2 4 6.2 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@H](c1ccccc1)CC2(C)C)c1ccc(C)cc1
CHEMBL1739734 casr_human Human No 7.5 IC50 = 31 nM Funct
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
444 6 2 4 6.2 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@H](c1ccccc1)CC2(C)C)c1ccc(C)cc1
CHEMBL1688091 casr_human Human No 7.5 IC50 = 31 nM Funct
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
474 7 2 6 5.5 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(OC(C)=O)cc1
CHEMBL1688100 casr_human Human No 7.5 IC50 = 31 nM Funct
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
430 6 2 4 5.9 CCC(CC)(NC(=O)c1cnn2c1N[C@H](c1ccccc1)CC2(C)C)c1ccc(C)cc1
CHEMBL1739781 casr_human Human No 7.5 IC50 = 31 nM Funct
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
430 6 2 4 5.9 CCC(CC)(NC(=O)c1cnn2c1N[C@H](c1ccccc1)CC2(C)C)c1ccc(C)cc1
CHEMBL4130093 casr_rat Rat No 7.5 IC50 = 31.8 nM Funct
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
414 5 1 3 6.1 C[C@@H](N[C@H]1CCCN(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12
CHEMBL4300172 casr_rat Rat No 7.5 IC50 = 31.8 nM Funct
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
414 5 1 3 6.1 C[C@@H](N[C@H]1CCCN(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12
CHEMBL486278 casr_human Human No 7.5 IC50 = 31.8 nM Bind
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
385 9 4 5 2.2 COc1ccc(CC(C)(C)NC[C@H](O)COc2cccc3[nH]c(=O)[nH]c23)cc1
CHEMBL1085334 casr_human Human No 6.5 IC50 = 310 nM Funct
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
417 10 2 3 5.6 Cc1ccccc1[C@H](OC[C@@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)C1CC1
CHEMBL523682 casr_human Human No 5.5 IC50 = 3100 nM Funct
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
544 13 2 9 4.6 COc1ccc(CNc2ncc(C(=O)NCCOc3ccccc3)c(-c3cc(OC)c(OC)c(OC)c3)n2)cc1
CHEMBL486278 casr_human Human No 4.5 IC50 = 31800 nM Bind
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
385 9 4 5 2.2 COc1ccc(CC(C)(C)NC[C@H](O)COc2cccc3[nH]c(=O)[nH]c23)cc1
CHEMBL1289679 casr_human Human No 6.5 IC50 = 320 nM Funct
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
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
CHEMBL1689061 casr_human Human No 6.5 IC50 = 320 nM Funct
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
474 7 3 5 5.6 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(C(=O)O)cc1
CHEMBL1198855 casr_rat Rat Yes 6.5 IC50 = 320 nM Funct
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
447 11 3 4 3.9 O[C@@H](COc1cc(CCC(=O)O)cc(c1F)F)CNC(CC1Cc2c(C1)cccc2)(C)C
CHEMBL482874 casr_human Human No 5.5 IC50 = 3200 nM Bind
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
309 11 2 4 2.8 CCCCOCC(O)CNC(C)(C)Cc1ccc(OC)cc1
CHEMBL1188986 casr_rat Rat No 6.5 IC50 = 330 nM Funct
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
440 5 2 2 6.5 C[C@@H](N[C@H]1CCCC[C@@H]1NC(=O)c1ccc(Cl)c(Cl)c1)c1cccc2ccccc12
CHEMBL537870 casr_rat Rat No 6.5 IC50 = 330 nM Funct
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
440 5 2 2 6.5 C[C@@H](N[C@H]1CCCC[C@@H]1NC(=O)c1ccc(Cl)c(Cl)c1)c1cccc2ccccc12
CHEMBL599665 casr_human Human No 5.5 IC50 = 3300 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
334 4 0 4 4.5 COc1ccc2c(c1)c(-c1ccc(C3CC3)cc1)nc(=O)n2C(C)C
CHEMBL201065 casr_human Human No 5.5 IC50 = 3300 nM Funct
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
401 9 2 4 4.1 CC(C)(Cc1ccc(F)cc1)NC[C@@H](O)COc1ccc(OC(F)(F)F)cc1
CHEMBL493228 casr_human Human No 6.5 IC50 = 340 nM Funct
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
544 13 2 9 4.6 COc1cccc(CNc2ncc(C(=O)NCCOc3ccccc3)c(-c3cc(OC)c(OC)c(OC)c3)n2)c1
CHEMBL494442 casr_human Human No 6.5 IC50 = 340 nM Funct
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
558 14 2 9 4.6 COc1ccccc1CCNc1ncc(C(=O)NCCOc2ccccc2)c(-c2cc(OC)c(OC)c(OC)c2)n1
CHEMBL1222491 casr_human Human No 6.5 IC50 = 340 nM Funct
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
520 8 0 4 7.5 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(Br)c(Cc3ccc(C)c(C)c3)cc(OC)c21
CHEMBL200361 casr_human Human No 6.5 IC50 = 340 nM Funct
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
427 8 2 4 4.6 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1ccccc1C#N
CHEMBL1783932 casr_human Human No 6.5 IC50 = 350 nM Funct
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
529 10 3 6 3.4 CC(C)(CN1Cc2ccccc2C1=O)NC[C@@H](O)COc1cc(C2CC3CC2C2C(C(=O)O)C32)ccc1C#N
CHEMBL4106263 casr_human Human No 5.5 IC50 = 3500 nM Bind
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
359 10 2 5 3.1 COc1ccc(CC(C)(C)NCC(O)COc2ccccc2OC)cc1
CHEMBL180336 casr_human Human Yes 5.5 IC50 = 3500 nM Bind
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
316 4 0 4 3.9 O=c1c2ccccc2nc(-c2ccco2)n1CCc1ccccc1
CHEMBL180336 casr_human Human Yes 5.5 IC50 = 3500 nM Bind
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
316 4 0 4 3.9 O=c1c2ccccc2nc(-c2ccco2)n1CCc1ccccc1
CHEMBL1783765 casr_human Human No 5.5 IC50 = 3500 nM Funct
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
481 10 3 4 4.6 Cc1ccc(CC(C)(C)NC[C@@H](O)COc2cccc(C3CC4CC3C3C(C(=O)O)C43)c2)cc1F
CHEMBL1783936 casr_human Human No 5.5 IC50 = 3500 nM Funct
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
517 11 3 4 5.4 C[C@@H](OC[C@H](O)CNC(C)(C)CC1Cc2ccccc2C1)c1ccccc1C1CC2CC1C1C(C(=O)O)C21
CHEMBL458515 casr_human Human No 6.4 IC50 = 360 nM Funct
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
525 7 1 9 4.1 COc1ccc(-c2nc(NCc3ccc4c(c3)OCO4)ncc2C(=O)N2CCc3ccccc3C2)c(OC)n1
CHEMBL462661 casr_human Human No 6.4 IC50 = 360 nM Funct
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
513 12 1 8 4.4 CCN(Cc1ccccc1)c1ncc(C(=O)NCCOc2ccccc2)c(-c2ccc(OC)nc2OC)n1
CHEMBL1222425 casr_human Human No 6.4 IC50 = 360 nM Funct
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
392 6 0 4 5.5 COCCn1c(-c2ccc(C(C)C)cc2)nc2cc(C(F)(F)F)cc(OC)c21
CHEMBL1082710 casr_human Human No 6.4 IC50 = 360 nM Funct
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
427 9 2 3 6.0 CC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1cccc2ccccc12
CHEMBL200690 casr_human Human No 6.4 IC50 = 360 nM Funct
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
438 8 2 3 5.1 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(F)c1F
CHEMBL1082788 casr_human Human No 7.4 IC50 = 37 nM Funct
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
417 10 2 3 5.6 Cc1ccccc1C(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)C1CC1
CHEMBL599227 casr_human Human No 5.4 IC50 = 3700 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
378 7 0 4 5.9 CCCCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C
CHEMBL1688102 casr_human Human No 6.4 IC50 = 380 nM Funct
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
476 5 2 4 6.1 O=C(NC(c1ccccc1)c1ccccc1)c1cnn2c1N[C@H](c1ccccc1)C[C@@H]2C(F)(F)F
CHEMBL372821 casr_human Human No 5.4 IC50 = 3860 nM Funct
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
380 8 2 4 3.9 N#Cc1c(Cl)cccc1OC[C@H](O)CNCCc1ccc2ccccc2c1
CHEMBL3827209 casr_human Human No 7.4 IC50 = 39.3 nM Funct
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
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
CHEMBL1223712 casr_human Human No 8.4 IC50 = 4 nM Funct
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
513 9 0 6 6.5 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(C(F)(F)F)c(Cc3cccnc3OC)cc(OC)c21
CHEMBL1223713 casr_human Human No 8.4 IC50 = 4 nM Funct
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
539 9 0 6 7.0 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(Br)c(Cc3cccnc3SC)cc(OC)c21
CHEMBL1672970 casr_human Human No 8.4 IC50 = 4 nM Funct
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
497 11 3 4 6.3 C[C@@H](OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1-c1ccc(C(=O)O)cc1
CHEMBL1689040 casr_human Human No 8.4 IC50 = 4.1 nM Funct
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
444 6 2 4 6.2 CCC(CC)(NC(=O)c1c(C)nn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C)cc1
CHEMBL1739914 casr_human Human No 8.4 IC50 = 4.1 nM Funct
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
444 6 2 4 6.2 CCC(CC)(NC(=O)c1c(C)nn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C)cc1
CHEMBL1689050 casr_human Human No 8.4 IC50 = 4.2 nM Funct
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
458 7 2 4 6.5 CCc1ccc(C(CC)(CC)NC(=O)c2c(C)nn3c2N[C@@H](c2ccccc2)CC3(C)C)cc1
CHEMBL1689060 casr_human Human No 8.4 IC50 = 4.2 nM Funct
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
458 7 2 4 6.5 CCc1ccc(C(CC)(CC)NC(=O)c2c(C)nn3c2N[C@@H](c2ccccc2)CC3(C)C)cc1
CHEMBL1739917 casr_human Human No 8.4 IC50 = 4.2 nM Funct
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
458 7 2 4 6.5 CCc1ccc(C(CC)(CC)NC(=O)c2c(C)nn3c2N[C@@H](c2ccccc2)CC3(C)C)cc1
CHEMBL597400 casr_human Human No 8.4 IC50 = 4.2 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
436 7 0 4 5.8 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1ccc(CC)cc1
CHEMBL597401 casr_human Human No 8.4 IC50 = 4.2 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
438 7 0 5 5.3 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1ccc(OC)cc1
CHEMBL4126057 casr_rat Rat No 8.4 IC50 = 4.3 nM Funct
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
400 5 1 3 5.7 C[C@@H](N[C@@H]1CCN(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12
CHEMBL4300082 casr_rat Rat No 8.4 IC50 = 4.3 nM Funct
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
400 5 1 3 5.7 C[C@@H](N[C@@H]1CCN(c2cccc(OC(F)(F)F)c2)C1)c1cccc2ccccc12
CHEMBL591475 casr_human Human No 8.4 IC50 = 4.4 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
408 6 0 4 5.2 C#CCOc1ccc2c(c1)c(nc(=O)n2Cc1ccccc1)c1ccc(cc1)C(C)C
CHEMBL1689811 casr_human Human No 8.4 IC50 = 4.4 nM Funct
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
512 8 2 4 7.4 CCCC(CCC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C(F)(F)F)cc1
CHEMBL1689058 casr_human Human No 8.3 IC50 = 4.6 nM Funct
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
478 7 2 5 6.1 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(OC)c(F)c1
CHEMBL1739921 casr_human Human No 8.3 IC50 = 4.6 nM Funct
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
478 7 2 5 6.1 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(OC)c(F)c1
CHEMBL1689046 casr_human Human No 8.3 IC50 = 4.7 nM Funct
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
476 7 2 5 6.7 CCC(CC)(NC(=O)c1c(SC)nn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C)cc1
CHEMBL1739732 casr_human Human No 8.3 IC50 = 4.7 nM Funct
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
476 7 2 5 6.7 CCC(CC)(NC(=O)c1c(SC)nn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C)cc1
CHEMBL1689062 casr_human Human No 8.3 IC50 = 4.8 nM Funct
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
472 7 2 5 6.1 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(C(C)=O)cc1
CHEMBL572163 casr_human Human No 8.3 IC50 = 4.8 nM Bind
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
421 11 3 4 4.2 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COc1ccc(CCC(=O)O)cc1
CHEMBL1687946 casr_human Human No 8.3 IC50 = 4.9 nM Funct
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
430 6 2 4 5.9 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C)cc1
CHEMBL1688097 casr_human Human No 8.3 IC50 = 4.9 nM Funct
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
430 6 2 4 5.9 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C)cc1
CHEMBL1289345 casr_human Human No 7.4 IC50 = 40 nM Funct
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
444 3 2 4 5.2 O=C(NC12CC3CC(CC(C3)C1)C2)c1cnn2c1N[C@H](c1ccccc1)C[C@@H]2C(F)(F)F
CHEMBL1289345 casr_human Human No 7.4 IC50 = 40 nM Funct
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
444 3 2 4 5.2 O=C(NC12CC3CC(CC(C3)C1)C2)c1cnn2c1N[C@H](c1ccccc1)C[C@@H]2C(F)(F)F
CHEMBL1289892 casr_human Human No 6.4 IC50 = 400 nM Funct
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
434 3 2 5 4.8 O=C(NC12CC3CC(CC(C3)C1)C2)c1cnn2c1N[C@H](c1ccco1)C[C@@H]2C(F)(F)F
CHEMBL494647 casr_human Human No 6.4 IC50 = 400 nM Funct
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
528 13 2 8 4.6 COc1cc(-c2nc(NCCc3ccccc3)ncc2C(=O)NCCOc2ccccc2)cc(OC)c1OC
CHEMBL1086281 casr_human Human No 7.4 IC50 = 41 nM Funct
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
433 11 2 4 5.3 COc1ccccc1C(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)C1CC1
CHEMBL1086472 casr_human Human No 6.4 IC50 = 420 nM Funct
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
378 9 2 4 4.3 CC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccn1
CHEMBL1222490 casr_human Human No 7.4 IC50 = 43 nM Funct
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
552 10 0 6 6.9 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(Br)c(Cc3ccc(OC)c(OC)c3)cc(OC)c21
CHEMBL180672 casr_human Human Yes 7.4 IC50 = 43 nM Bind
Inhibition of human CaSR expressed in HEK293 cellsInhibition of human CaSR expressed in HEK293 cells
408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O
CHEMBL180672 casr_human Human Yes 7.4 IC50 = 43 nM Bind
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O
CHEMBL180672 casr_human Human Yes 7.4 IC50 = 43 nM Bind
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
408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O
CHEMBL1083950 casr_human Human No 6.4 IC50 = 440 nM Funct
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
391 10 2 3 4.8 CC(Cc1ccccc1)OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1
CHEMBL538155 casr_human Human No 6.4 IC50 = 440 nM Funct
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
416 8 3 4 4.0 CC(C)(Cc1cc2ccccc2[nH]1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(C#N)c1
CHEMBL1689045 casr_human Human No 7.4 IC50 = 45 nM Funct
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
520 8 2 4 7.5 CCC(CC)(NC(=O)c1c(Cc2ccccc2)nn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C)cc1
CHEMBL1739731 casr_human Human No 7.4 IC50 = 45 nM Funct
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
520 8 2 4 7.5 CCC(CC)(NC(=O)c1c(Cc2ccccc2)nn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C)cc1
CHEMBL3828154 casr_human Human No 7.3 IC50 = 45.7 nM Funct
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
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
CHEMBL3827410 casr_human Human No 6.3 IC50 = 457.1 nM Funct
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
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
CHEMBL180672 casr_rat Rat Yes 6.3 IC50 = 460 nM Funct
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
408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O
CHEMBL589977 casr_human Human No 6.3 IC50 = 460 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
349 5 1 4 5.2 CCNc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C
CHEMBL200423 casr_human Human No 5.3 IC50 = 4600 nM Funct
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
352 6 2 4 4.2 N#Cc1c(Cl)cccc1OC[C@H](O)CNc1ccc2ccccc2c1
CHEMBL1223298 casr_human Human No 5.3 IC50 = 4690 nM Funct
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
322 6 0 3 5.6 CCCCn1c(-c2ccc(C(C)C)cc2)nc2c(OC)cccc21
CHEMBL510598 casr_human Human No 6.3 IC50 = 470 nM Funct
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
528 12 1 8 4.6 COc1cc(-c2nc(N(C)Cc3ccccc3)ncc2C(=O)NCCOc2ccccc2)cc(OC)c1OC
CHEMBL3827473 casr_human Human No 6.3 IC50 = 489.1 nM Funct
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
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
CHEMBL454158 casr_human Human No 5.3 IC50 = 4900 nM Funct
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
548 12 2 8 5.2 COc1cc(-c2nc(NCc3ccccc3Cl)ncc2C(=O)NCCOc2ccccc2)cc(OC)c1OC
CHEMBL1222427 casr_human Human No 8.3 IC50 = 5 nM Funct
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
492 8 0 4 6.8 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(Br)c(Cc3ccccc3)cc(OC)c21
CHEMBL1222492 casr_human Human No 8.3 IC50 = 5 nM Funct
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
554 9 0 5 6.6 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(Br)c(Cc3ccccc3[S+](C)[O-])cc(OC)c21
CHEMBL1672972 casr_human Human No 8.3 IC50 = 5 nM Funct
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
511 11 3 4 6.6 Cc1cc(-c2ccccc2[C@@H](C)OC[C@H](O)CNC(C)(C)Cc2ccc3ccccc3c2)ccc1C(=O)O
CHEMBL1688103 casr_human Human No 8.3 IC50 = 5.2 nM Funct
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
488 8 2 6 5.8 CCOC(=O)c1ccc(C(CC)(CC)NC(=O)c2cnn3c2NC(c2ccccc2)CC3(C)C)cc1
CHEMBL1687946 casr_human Human No 8.3 IC50 = 5.5 nM Funct
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
430 6 2 4 5.9 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C)cc1
CHEMBL1688097 casr_human Human No 8.3 IC50 = 5.5 nM Funct
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
430 6 2 4 5.9 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C)cc1
CHEMBL1223303 casr_human Human No 7.3 IC50 = 50 nM Funct
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
358 6 0 4 5.1 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(Cl)ccc(OC)c21
CHEMBL180672 casr_human Human Yes 7.3 IC50 = 50 nM Funct
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
408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O
CHEMBL200311 casr_human Human No 7.3 IC50 = 50 nM Funct
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
408 8 2 4 4.7 CC(C)(Cc1ccc2ccccc2c1)NC[C@H](O)COc1cccc(Cl)c1C#N
CHEMBL1783934 casr_human Human No 7.3 IC50 = 50 nM Funct
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
529 11 3 4 5.6 C[C@@H](OC[C@H](O)CNC(C)(C)Cc1ccc(Cl)cc1F)c1ccccc1C1CC2CC1C1C(C(=O)O)C21
CHEMBL3827577 casr_human Human No 7.3 IC50 = 50.8 nM Funct
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
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
CHEMBL1223369 casr_human Human No 7.3 IC50 = 51 nM Funct
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
392 6 0 4 5.5 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(C(F)(F)F)ccc(OC)c21
CHEMBL599857 casr_human Human No 6.3 IC50 = 520 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
377 6 0 4 5.6 CCN(CC)c1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C
CHEMBL1084514 casr_human Human Yes 6.3 IC50 = 520 nM Bind
Inhibition of CaSRInhibition of CaSR
464 12 2 6 4.0 CCOC(=O)CCc1ccc(C#N)c(OC[C@H](O)CNC(C)(C)CC2Cc3ccccc3C2)c1
CHEMBL180057 casr_human Human No 6.3 IC50 = 520 nM Bind
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
374 4 1 4 4.5 Cc1ccc2nc(-c3ccccc3O)n(CCc3cccc(F)c3)c(=O)c2c1
CHEMBL180672 casr_rat Rat Yes 6.3 IC50 = 530 nM Funct
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
408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O
CHEMBL1290216 casr_human Human No 5.3 IC50 = 5300 nM Funct
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
376 3 2 4 4.1 O=C(NC12CC3CC(CC(C3)C1)C2)c1cnn2c1N[C@H](c1ccccc1)CC2
CHEMBL1083314 casr_human Human No 6.3 IC50 = 540 nM Funct
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
422 10 2 5 4.8 CC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1[N+](=O)[O-]
CHEMBL1188809 casr_rat Rat No 5.3 IC50 = 5400 nM Funct
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
492 7 2 4 5.7 CC(N[C@@H]1CCCC[C@H]1NS(=O)(=O)c1ccc(OC(F)(F)F)cc1)c1cccc2ccccc12
CHEMBL537426 casr_rat Rat No 5.3 IC50 = 5400 nM Funct
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
492 7 2 4 5.7 CC(N[C@@H]1CCCC[C@H]1NS(=O)(=O)c1ccc(OC(F)(F)F)cc1)c1cccc2ccccc12
CHEMBL1082379 casr_human Human No 6.3 IC50 = 550 nM Funct
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
427 9 2 3 6.0 CC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccc2ccccc2c1
CHEMBL599869 casr_human Human No 5.3 IC50 = 5500 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
370 4 0 4 5.3 COc1ccc2c(c1)c(-c1ccc(-c3ccccc3)cc1)nc(=O)n2C(C)C
CHEMBL1783762 casr_human Human No 7.3 IC50 = 56 nM Funct
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
525 10 3 4 4.9 CC(C)(CC1Cc2ccccc2C1)NC[C@@H](O)COc1cc(C2CC3CC2C2C(C(=O)O)C32)cc(F)c1F
CHEMBL1084756 casr_human Human No 6.3 IC50 = 560 nM Funct
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
363 9 2 3 4.3 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COCc1ccccc1
CHEMBL3633656 casr_rat Rat No 4.3 IC50 = 56200 nM Funct
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
421 7 1 5 2.8 COc1ccc(-c2[nH]c3ccccc3c2C(=O)CN(C)CC(=O)N2CCOCC2)cc1
CHEMBL3633656 casr_rat Rat No 4.3 IC50 = 56234.1 nM Funct
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
421 7 1 5 2.8 COc1ccc(-c2[nH]c3ccccc3c2C(=O)CN(C)CC(=O)N2CCOCC2)cc1
CHEMBL1082719 casr_human Human No 6.2 IC50 = 570 nM Funct
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
419 9 2 3 5.9 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COC(c1ccccc1)C(C)(C)C
CHEMBL3827154 casr_human Human No 7.2 IC50 = 58.7 nM Funct
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
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
CHEMBL1290329 casr_human Human No 6.2 IC50 = 580 nM Funct
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
402 3 2 4 4.8 CC1(C)C=C(c2ccccc2)Nc2c(C(=O)NC34CC5CC(CC(C5)C3)C4)cnn21
CHEMBL1689042 casr_human Human No 8.2 IC50 = 6 nM Funct
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
472 8 2 4 6.9 CCCc1nn2c(c1C(=O)NC(CC)(CC)c1ccc(C)cc1)NC(c1ccccc1)CC2(C)C
CHEMBL1739941 casr_human Human No 8.2 IC50 = 6 nM Funct
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
472 8 2 4 6.9 CCCc1nn2c(c1C(=O)NC(CC)(CC)c1ccc(C)cc1)NC(c1ccccc1)CC2(C)C
CHEMBL1223506 casr_human Human No 8.2 IC50 = 6 nM Funct
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
528 6 0 4 5.8 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(I)c(Br)cc(OC)c21
CHEMBL1783764 casr_human Human No 8.2 IC50 = 6 nM Funct
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
514 10 3 5 4.5 CC(C)(CC1Cc2ccccc2C1)NC[C@@H](O)COc1cc(C2CC3CC2C2C(C(=O)O)C32)ccc1C#N
CHEMBL1687956 casr_human Human No 8.2 IC50 = 6.1 nM Funct
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
494 7 2 5 6.6 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(Cl)c(OC)c1
CHEMBL1739756 casr_human Human No 8.2 IC50 = 6.1 nM Funct
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
494 7 2 5 6.6 CCC(CC)(NC(=O)c1c(C)nn2c1N[C@@H](c1ccccc1)CC2(C)C)c1ccc(Cl)c(OC)c1
CHEMBL598016 casr_human Human No 8.2 IC50 = 6.6 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
412 6 1 4 5.9 CCCc1c(O)ccc2c1c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1ccccc1
CHEMBL1688087 casr_human Human No 8.2 IC50 = 6.6 nM Funct
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
446 7 2 5 5.6 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(OC)cc1
CHEMBL1689041 casr_human Human No 8.2 IC50 = 6.7 nM Funct
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
458 7 2 4 6.5 CCc1nn2c(c1C(=O)NC(CC)(CC)c1ccc(C)cc1)NC(c1ccccc1)CC2(C)C
CHEMBL1739915 casr_human Human No 8.2 IC50 = 6.7 nM Funct
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
458 7 2 4 6.5 CCc1nn2c(c1C(=O)NC(CC)(CC)c1ccc(C)cc1)NC(c1ccccc1)CC2(C)C
CHEMBL457249 casr_human Human No 7.2 IC50 = 60 nM Funct
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
528 11 2 9 4.3 COc1ccc(-c2nc(NCc3ccc4c(c3)OCO4)ccc2C(=O)NCCOc2ccccc2)c(OC)n1
CHEMBL1222426 casr_human Human No 7.2 IC50 = 60 nM Funct
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
478 7 0 4 6.9 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(Br)c(-c3ccccc3)cc(OC)c21
CHEMBL199894 casr_human Human No 7.2 IC50 = 60 nM Funct
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
380 8 2 5 4.1 CC(C)(Cc1cc2ccccc2s1)NC[C@H](O)COc1ccccc1C#N
CHEMBL199363 casr_human Human No 6.2 IC50 = 600 nM Funct
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
376 8 2 4 3.7 CC(C)(Cc1ccc(F)cc1)NC[C@@H](O)COc1cccc(Cl)c1C#N
CHEMBL361316 casr_human Human No 6.2 IC50 = 600 nM Bind
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
360 4 1 4 4.2 O=c1c2ccc(F)cc2nc(-c2ccccc2O)n1CCc1ccccc1
CHEMBL1084201 casr_human Human No 6.2 IC50 = 610 nM Funct
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
445 10 2 3 6.5 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COC(c1ccccc1)C1CCCCC1
CHEMBL199473 casr_human Human No 5.2 IC50 = 6180 nM Funct
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
401 8 2 3 5.2 CC(C)(Cc1ccc(F)cc1)NC[C@@H](O)CSc1cccc(Cl)c1Cl
CHEMBL3827723 casr_human Human No 7.2 IC50 = 64.3 nM Funct
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
489 10 3 5 4.8 Cc1ccc(C(C)OC[C@H](O)CNC(C)(C)Cc2ccc3ccccc3c2)c2c1OC1C(C(=O)O)C21
CHEMBL599229 casr_human Human No 5.2 IC50 = 6600 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
376 7 0 4 5.7 C=CCCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C
CHEMBL487507 casr_human Human No 7.2 IC50 = 68 nM Bind
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
397 9 2 4 4.4 COc1ccc(CC(C)(C)NC[C@@H](O)COc2cccc(Cl)c2Cl)cc1
CHEMBL200878 casr_human Human No 5.2 IC50 = 6840 nM Funct
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
446 9 3 4 4.5 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(C(=O)O)c1
CHEMBL473345 casr_human Human No 5.2 IC50 = 6900 nM Funct
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
498 11 1 7 4.6 COc1ccc(-c2nc(N(C)Cc3ccccc3)ncc2C(=O)NCCOc2ccccc2)cc1OC
CHEMBL597396 casr_human Human No 8.1 IC50 = 7.3 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
468 9 1 6 4.6 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1cccc(OCCO)c1
CHEMBL1689818 casr_human Human No 8.1 IC50 = 7.3 nM Funct
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
434 6 2 4 5.8 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(F)cc1
CHEMBL1689816 casr_human Human No 8.1 IC50 = 7.4 nM Funct
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
450 6 2 4 6.3 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(Cl)cc1
CHEMBL3827259 casr_human Human No 8.1 IC50 = 7.5 nM Funct
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
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
CHEMBL1689810 casr_human Human Yes 8.1 IC50 = 7.6 nM Funct
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
484 6 2 4 6.6 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C(F)(F)F)cc1
CHEMBL4129011 casr_rat Rat No 8.1 IC50 = 7.8 nM Funct
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
400 5 1 3 5.7 C[C@@H](N[C@H]1CCN(c2ccc(OC(F)(F)F)cc2)C1)c1cccc2ccccc12
CHEMBL4302857 casr_rat Rat No 8.1 IC50 = 7.8 nM Funct
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
400 5 1 3 5.7 C[C@@H](N[C@H]1CCN(c2ccc(OC(F)(F)F)cc2)C1)c1cccc2ccccc12
CHEMBL493638 casr_human Human No 7.2 IC50 = 70 nM Funct
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
548 12 2 8 5.2 COc1cc(-c2nc(NCc3cccc(Cl)c3)ncc2C(=O)NCCOc2ccccc2)cc(OC)c1OC
CHEMBL599040 casr_human Human No 7.2 IC50 = 70 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
361 6 1 4 5.4 C=CCNc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C
CHEMBL1083288 casr_human Human No 7.2 IC50 = 70 nM Funct
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
403 10 2 3 5.3 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COC(c1ccccc1)C1CC1
CHEMBL523475 casr_human Human No 7.2 IC50 = 70 nM Bind
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
388 9 2 5 3.6 COc1ccc(CC(C)(C)NCC(O)COc2cccc(Cl)c2C#N)cc1
CHEMBL1290007 casr_human Human No 6.2 IC50 = 700 nM Funct
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
452 4 2 4 5.7 O=C(NC12CC3CC(CC(C3)C1)C2)c1cnn2c1N[C@H](c1ccccc1)C[C@@H]2c1ccccc1
CHEMBL179907 casr_human Human No 6.2 IC50 = 700 nM Bind
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
356 4 1 4 4.3 Cc1cccc2c(=O)n(CCc3ccccc3)c(-c3ccccc3O)nc12
CHEMBL482462 casr_human Human No 5.2 IC50 = 7000 nM Bind
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
295 10 2 4 2.4 CCCOCC(O)CNC(C)(C)Cc1ccc(OC)cc1
CHEMBL1084513 casr_human Human Yes 7.1 IC50 = 73 nM Bind
Inhibition of CaSRInhibition of CaSR
436 11 3 5 3.5 N#Cc1ccc(cc1OC[C@@H](CNC(CC1Cc2c(C1)cccc2)(C)C)O)CCC(=O)O
CHEMBL454374 casr_human Human No 6.1 IC50 = 730 nM Funct
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
514 12 2 8 4.6 COc1cc(-c2nc(NCc3ccccc3)ncc2C(=O)NCCOc2ccccc2)cc(OC)c1OC
CHEMBL1083306 casr_human Human No 6.1 IC50 = 730 nM Funct
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
439 10 2 3 5.9 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COC(c1ccccc1)c1ccccc1
CHEMBL1083289 casr_human Human No 7.1 IC50 = 74 nM Funct
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
417 10 2 3 5.7 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COC(c1ccccc1)C1CCC1
CHEMBL201137 casr_human Human No 6.1 IC50 = 750 nM Funct
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
420 8 2 3 4.9 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(F)c1
CHEMBL1290106 casr_human Human No 7.1 IC50 = 76 nM Funct
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
390 3 2 4 4.7 C[C@H]1C[C@@H](c2ccccc2)Nc2c(C(=O)NC34CC5CC(CC(C5)C3)C4)cnn21
CHEMBL457071 casr_human Human Yes 7.1 IC50 = 76 nM Funct
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
557 14 3 8 4.6 OC[C@@H](Nc1ccc(c(n1)c1cc(OC)c(c(c1)OC)OC)C(=O)NCCOc1ccccc1)Cc1ccccc1
CHEMBL1085335 casr_human Human No 6.1 IC50 = 760 nM Funct
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
417 10 2 3 5.6 Cc1ccccc1[C@@H](OC[C@@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)C1CC1
CHEMBL3827356 casr_human Human No 7.1 IC50 = 77.2 nM Funct
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
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
CHEMBL1223371 casr_human Human No 6.1 IC50 = 770 nM Funct
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
358 6 0 4 5.1 COCCn1c(-c2ccc(C(C)C)cc2)nc2c(OC)ccc(Cl)c21
CHEMBL1223440 casr_human Human No 6.1 IC50 = 790 nM Funct
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
322 5 0 3 5.6 CCCn1c(-c2ccc(C(C)C)cc2)nc2c(C)ccc(OC)c21
CHEMBL199529 casr_human Human No 6.1 IC50 = 790 nM Funct
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
447 9 2 5 4.7 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1Cc1ccc([N+](=O)[O-])cc1
CHEMBL4079960 casr_rat Rat No 8.1 IC50 = 8 nM Funct
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
360 5 2 3 4.5 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)O)cc2)C1)c1cccc2ccccc12
CHEMBL4126482 casr_rat Rat No 8.1 IC50 = 8 nM Funct
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
360 5 2 3 4.5 C[C@@H](N[C@H]1CCN(c2ccc(C(=O)O)cc2)C1)c1cccc2ccccc12
CHEMBL590560 casr_human Human No 8.1 IC50 = 8.1 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
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
CHEMBL1688088 casr_human Human No 8.1 IC50 = 8.5 nM Funct
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
522 9 2 5 7.2 CCC(CC)(NC(=O)c1cnn2c1NC(c1ccccc1)CC2(C)C)c1ccc(OCc2ccccc2)cc1
CHEMBL180250 casr_human Human No 6.1 IC50 = 800 nM Bind
Inhibitory concentration against human calcium receptor expressed in HEK 293 cellsInhibitory concentration against human calcium receptor expressed in HEK 293 cells
376 4 1 4 4.7 O=c1c2ccccc2nc(-c2ccccc2O)n1CCc1cccc(Cl)c1
CHEMBL195045 casr_human Human No 6.1 IC50 = 800 nM Bind
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
374 4 1 4 4.2 Cc1c(C(F)(F)F)nc(-c2ccccc2O)n(CCc2ccccc2)c1=O
CHEMBL1197056 casr_rat Rat No 5.1 IC50 = 8000 nM Funct
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
438 7 2 4 4.8 COc1ccc(cc1)S(=O)(=O)N[C@@H]1CCCC[C@H]1NC(c1cccc2c1cccc2)C
CHEMBL1689044 casr_human Human No 7.1 IC50 = 81 nM Funct
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
506 7 2 4 7.6 CCC(CC)(NC(=O)c1c(-c2ccccc2)nn2c1NC(c1ccccc1)CC2(C)C)c1ccc(C)cc1
CHEMBL1085987 casr_human Human No 6.1 IC50 = 810 nM Funct
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
391 10 2 3 4.9 CC(COC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1
CHEMBL1085807 casr_human Human No 7.1 IC50 = 83 nM Funct
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
417 10 2 3 5.6 Cc1ccccc1[C@@H](OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)C1CC1
CHEMBL383842 casr_human Human No 5.1 IC50 = 8430 nM Funct
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
441 7 2 4 4.3 CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)[C@H]1CCCN1C(=O)c1cccc(C#N)c1
CHEMBL199785 casr_human Human No 6.1 IC50 = 880 nM Funct
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
392 8 1 3 5.7 CC(C)(Cc1ccc2ccccc2c1)NCCCOc1cccc(Cl)c1C#N
CHEMBL592176 casr_human Human Yes 8.1 IC50 = 9 nM Funct
Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assayAntagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay
360 5 0 4 4.8 C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2C(C)C
CHEMBL3827304 casr_human Human No 8.0 IC50 = 9.6 nM Funct
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
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
CHEMBL4125688 casr_rat Rat No 8.0 IC50 = 9.7 nM Funct
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
384 4 1 2 5.8 C[C@@H](N[C@@H]1CCN(c2cccc(C(F)(F)F)c2)C1)c1cccc2ccccc12
CHEMBL4301528 casr_rat Rat No 8.0 IC50 = 9.7 nM Funct
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
384 4 1 2 5.8 C[C@@H](N[C@@H]1CCN(c2cccc(C(F)(F)F)c2)C1)c1cccc2ccccc12
CHEMBL1196590 casr_rat Rat No 6.1 IC50 = 900 nM Funct
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
456 6 2 3 6.1 CC(N[C@@H]1CCCC[C@H]1NC(=O)c1ccc(OC(F)(F)F)cc1)c1cccc2ccccc12