Finalizing display...
Ligand source activities (1 row/activity)
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
| 2-methyl-3-phenethyl-3H-pyrimidin-4-one | 80 | None | 0 | Human | Binding | IC50 | = | 97.00 | 7.01 | - | 1 | Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor | ChEMBL | 352.2 | 4 | 1 | 3 | 3.39 | CCC1=C(C)N/C(=C2/C=CC=CC2=O)N(CCc2ccccc2F)C1=O | https://dx.doi.org/10.1016/j.bmcl.2005.03.054 | |
| Ca2+ | 806 | None | 0 | Human | Binding | pKd | None | - | 2.40 | -1 | 3 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/7531693 | |
| Ca2+ | 806 | None | 0 | Mouse | Binding | pKd | None | - | 2.50 | 1 | 3 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/16199532 | |
| Ca2+ | 806 | None | 0 | Rat | Binding | pKd | None | - | 2.50 | -1 | 3 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/7816802 | |
| calindol | 784 | None | 4 | Human | Binding | pKd | = | - | 6.25 | - | 3 | Unclassified | Guide to Pharmacology | 300.2 | 4 | 2 | 1 | 5.17 | C[C@@H](NCc1cc2ccccc2[nH]1)c1cccc2ccccc12 | https://pubmed.ncbi.nlm.nih.gov/15149704 | |
| calindol | 784 | None | 4 | Human | Binding | pKd | = | - | 6.25 | - | 3 | Unclassified | Guide to Pharmacology | 300.2 | 4 | 2 | 1 | 5.17 | C[C@@H](NCc1cc2ccccc2[nH]1)c1cccc2ccccc12 | https://pubmed.ncbi.nlm.nih.gov/14976203 | |
| CHEMBL1083694 | 6728 | None | 0 | Human | Binding | IC50 | = | 97.00 | 7.01 | - | 1 | Inhibition of CaSR | ChEMBL | 402.2 | 5 | 1 | 4 | 5.02 | CCc1cc2c(=O)n(CCc3ccccc3F)c(-c3ccccc3O)nc2cc1C | https://dx.doi.org/10.1021/jm9018756 | |
| CHEMBL1084514 | 6952 | None | 14 | Human | Binding | IC50 | = | 520.00 | 6.28 | - | 1 | Inhibition of CaSR | ChEMBL | 464.3 | 12 | 2 | 6 | 3.97 | CCOC(=O)CCc1ccc(C#N)c(OC[C@H](O)CNC(C)(C)CC2Cc3ccccc3C2)c1 | https://dx.doi.org/10.1021/jm9018756 | |
| CHEMBL178442 | 62897 | None | 0 | Human | Binding | IC50 | = | 1600.00 | 5.80 | - | 1 | Inhibitory concentration against human calcium receptor expressed in HEK 293 cells | ChEMBL | 394.1 | 4 | 1 | 4 | 4.80 | O=c1c2ccc(Cl)cc2nc(-c2ccccc2O)n1CCc1cccc(F)c1 | https://dx.doi.org/10.1016/j.bmcl.2005.01.078 | |
| CHEMBL179333 | 63322 | None | 0 | Human | Binding | IC50 | = | 2800.00 | 5.55 | - | 1 | Inhibitory concentration against human calcium receptor expressed in HEK 293 cells | ChEMBL | 342.1 | 4 | 1 | 4 | 4.01 | O=c1c2ccccc2nc(-c2cccc(O)c2)n1CCc1ccccc1 | https://dx.doi.org/10.1016/j.bmcl.2005.01.078 | |
| CHEMBL179907 | 63504 | None | 0 | Human | Binding | IC50 | = | 700.00 | 6.16 | - | 1 | Inhibitory concentration against human calcium receptor expressed in HEK 293 cells | ChEMBL | 356.2 | 4 | 1 | 4 | 4.32 | Cc1cccc2c(=O)n(CCc3ccccc3)c(-c3ccccc3O)nc12 | https://dx.doi.org/10.1016/j.bmcl.2005.01.078 | |
| CHEMBL180030 | 63566 | None | 0 | Human | Binding | IC50 | = | 300.00 | 6.52 | - | 1 | Inhibitory concentration against human calcium receptor expressed in HEK 293 cells | ChEMBL | 342.1 | 4 | 1 | 4 | 4.01 | O=c1c2ccccc2nc(-c2ccccc2O)n1CCc1ccccc1 | https://dx.doi.org/10.1016/j.bmcl.2005.01.078 | |
| CHEMBL180030 | 63566 | None | 0 | Human | Binding | IC50 | = | 300.00 | 6.52 | - | 1 | Inhibition of CaSR | ChEMBL | 342.1 | 4 | 1 | 4 | 4.01 | O=c1c2ccccc2nc(-c2ccccc2O)n1CCc1ccccc1 | https://dx.doi.org/10.1021/jm9018756 | |
| CHEMBL180057 | 63575 | None | 0 | Human | Binding | IC50 | = | 520.00 | 6.28 | - | 1 | Inhibitory concentration against human calcium receptor expressed in HEK 293 cells | ChEMBL | 374.1 | 4 | 1 | 4 | 4.46 | Cc1ccc2nc(-c3ccccc3O)n(CCc3cccc(F)c3)c(=O)c2c1 | https://dx.doi.org/10.1016/j.bmcl.2005.01.078 | |
| CHEMBL180250 | 63852 | None | 0 | Human | Binding | IC50 | = | 800.00 | 6.10 | - | 1 | Inhibitory concentration against human calcium receptor expressed in HEK 293 cells | ChEMBL | 376.1 | 4 | 1 | 4 | 4.67 | O=c1c2ccccc2nc(-c2ccccc2O)n1CCc1cccc(Cl)c1 | https://dx.doi.org/10.1016/j.bmcl.2005.01.078 | |
| CHEMBL180336 | 63884 | None | 8 | Human | Binding | IC50 | = | 3500.00 | 5.46 | - | 1 | Inhibitory concentration against human calcium receptor expressed in HEK 293 cells | ChEMBL | 316.1 | 4 | 0 | 4 | 3.90 | O=c1c2ccccc2nc(-c2ccco2)n1CCc1ccccc1 | https://dx.doi.org/10.1016/j.bmcl.2005.01.078 | |
| CHEMBL180336 | 63884 | None | 8 | Human | Binding | IC50 | = | 3500.00 | 5.46 | - | 1 | Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor | ChEMBL | 316.1 | 4 | 0 | 4 | 3.90 | O=c1c2ccccc2nc(-c2ccco2)n1CCc1ccccc1 | https://dx.doi.org/10.1016/j.bmcl.2005.03.054 | |
| CHEMBL180391 | 63899 | None | 7 | Human | Binding | IC50 | = | 14000.00 | 4.85 | - | 1 | Inhibitory concentration against human calcium receptor expressed in HEK 293 cells | ChEMBL | 326.1 | 4 | 0 | 3 | 4.31 | O=c1c2ccccc2nc(-c2ccccc2)n1CCc1ccccc1 | https://dx.doi.org/10.1016/j.bmcl.2005.01.078 | |
| CHEMBL180463 | 63914 | None | 0 | Human | Binding | IC50 | = | 190.00 | 6.72 | - | 1 | Inhibitory concentration against human calcium receptor expressed in HEK 293 cells | ChEMBL | 378.1 | 4 | 1 | 4 | 4.29 | O=c1c2cc(F)ccc2nc(-c2ccccc2O)n1CCc1cccc(F)c1 | https://dx.doi.org/10.1016/j.bmcl.2005.01.078 | |
| CHEMBL182107 | 64880 | None | 0 | Human | Binding | IC50 | = | 1600.00 | 5.80 | - | 1 | Inhibitory concentration against human calcium receptor expressed in HEK 293 cells | ChEMBL | 358.1 | 4 | 2 | 5 | 3.72 | O=c1c2ccccc2nc(-c2cc(O)ccc2O)n1CCc1ccccc1 | https://dx.doi.org/10.1016/j.bmcl.2005.01.078 | |
Showing 1 to 20 of 159 entries
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
| (R)-2h [PMID:19625189] | 3270 | None | 0 | Human | Functional | pIC50 | = | - | 7.39 | - | 1 | Unclassified | Guide to Pharmacology | 425.1 | 4 | 1 | 5 | 4.99 | C[C@H](Cc1ccccc1)n1c(-c2ccccc2O)nc2ccnc(C(F)(F)F)c2c1=O | https://pubmed.ncbi.nlm.nih.gov/19625189 | |
| 1-arylmethylpyrrolidin-2-yl ethanol amine | 29 | None | 0 | Human | Functional | IC50 | = | 270.00 | 6.57 | 186 | 2 | Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR | ChEMBL | 433.2 | 8 | 2 | 5 | 4.71 | CC(C)(Cc1cc2ccccc2s1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(C#N)c1 | https://dx.doi.org/10.1016/j.bmcl.2005.08.095 | |
| 1-arylmethylpyrrolidin-2-yl ethanol amine | 29 | None | 0 | Rat | Functional | pIC50 | None | - | 4.30 | -186 | 2 | Unclassified | Guide to Pharmacology | 433.2 | 8 | 2 | 5 | 4.71 | CC(C)(Cc1cc2ccccc2s1)NC[C@@H](O)[C@H]1CCCN1Cc1cccc(C#N)c1 | https://pubmed.ncbi.nlm.nih.gov/16216508 | |
| 2-methyl-3-phenethyl-3H-pyrimidin-4-one | 80 | None | 0 | Human | Functional | pIC50 | None | - | 7.00 | - | 1 | Unclassified | Guide to Pharmacology | 352.2 | 4 | 1 | 3 | 3.39 | CCC1=C(C)N/C(=C2/C=CC=CC2=O)N(CCc2ccccc2F)C1=O | https://pubmed.ncbi.nlm.nih.gov/15863312 | |
| AC265347 | 241 | None | 25 | Human | Functional | pEC50 | = | - | 7.85 | - | 1 | Unclassified | Guide to Pharmacology | 283.1 | 2 | 1 | 3 | 4.17 | Cc1ccc(C(C)(O)c2nc3ccccc3s2)c(C)c1 | https://pubmed.ncbi.nlm.nih.gov/21239511 | |
| AC265347 | 241 | None | 25 | Human | Functional | EC50 | = | 25.12 | 7.60 | - | 1 | Positive allosteric modulation of calcium sensing receptor by cell based assay | ChEMBL | 283.1 | 2 | 1 | 3 | 4.17 | Cc1ccc(C(C)(O)c2nc3ccccc3s2)c(C)c1 | https://dx.doi.org/10.1016/j.bmcl.2010.07.077 | |
| AC265347 | 241 | None | 25 | Human | Functional | pKB | = | - | 6.35 | - | 1 | Ca2+i release | Guide to Pharmacology | 283.1 | 2 | 1 | 3 | 4.17 | Cc1ccc(C(C)(O)c2nc3ccccc3s2)c(C)c1 | https://pubmed.ncbi.nlm.nih.gov/25220431 | |
| AC265347 | 241 | None | 25 | Human | Functional | pKB | = | - | 6.35 | - | 1 | Ca2+i release | Guide to Pharmacology | 283.1 | 2 | 1 | 3 | 4.17 | Cc1ccc(C(C)(O)c2nc3ccccc3s2)c(C)c1 | https://pubmed.ncbi.nlm.nih.gov/27002221 | |
| ATF-936 | 202822 | None | 2 | Human | Functional | IC50 | = | 1.40 | 8.85 | - | 1 | Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay | ChEMBL | 482.2 | 9 | 0 | 6 | 5.65 | C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1ccc(OC)c(OCC)c1 | https://dx.doi.org/10.1021/jm901811v | |
| ATF936 | 513 | None | 0 | Human | Functional | IC50 | = | 4.40 | 8.36 | - | 1 | Antagonist activity at human CaSR expressed in CCL39 cells assessed as inhibition of extracellular calcium-induced intracellular calcium transient by FLIPR assay | ChEMBL | 408.2 | 6 | 0 | 4 | 5.25 | C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1ccccc1 | https://dx.doi.org/10.1021/jm901811v | |
| ATF936 | 513 | None | 0 | Human | Functional | pIC50 | = | - | 8.90 | - | 1 | Inhibition of 2.5 mM Ca2+-mediated Ca2+i release | Guide to Pharmacology | 408.2 | 6 | 0 | 4 | 5.25 | C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1ccccc1 | https://pubmed.ncbi.nlm.nih.gov/20158186 | |
| AXT914 | 532 | None | 0 | Human | Functional | pIC50 | = | - | 8.85 | - | 1 | Unclassified | Guide to Pharmacology | 486.1 | 6 | 0 | 4 | 6.01 | C#CCOc1ccc2c(c1)c(-c1ccc(C(C)C)cc1)nc(=O)n2Cc1ccc(Br)cc1 | https://pubmed.ncbi.nlm.nih.gov/21526895 | |
| calhex 231 | 783 | None | 0 | Human | Functional | pIC50 | = | - | 6.40 | - | 1 | Inhibition of 9mM Ca2+o-mediated IP accumulation | Guide to Pharmacology | 406.2 | 5 | 2 | 2 | 5.88 | C[C@@H](N[C@H]1CCCC[C@@H]1NC(=O)c1ccc(Cl)cc1)c1cccc2ccccc12 | https://pubmed.ncbi.nlm.nih.gov/14506236 | |
| calindol | 784 | None | 4 | Human | Functional | EC50 | = | 310.00 | 6.51 | -1 | 3 | Ability to stimulate [3H]inositol phosphates accumulation in HEK293 cells expressing the human calcium sensing receptor (CaSR) at 2 mM [Ca2+] | ChEMBL | 300.2 | 4 | 2 | 1 | 5.17 | C[C@@H](NCc1cc2ccccc2[nH]1)c1cccc2ccccc12 | https://dx.doi.org/10.1016/j.bmcl.2004.03.056 | |
| calindol | 784 | None | 4 | Human | Functional | pKB | = | - | 6.30 | -1 | 3 | Ca2+i release | Guide to Pharmacology | 300.2 | 4 | 2 | 1 | 5.17 | C[C@@H](NCc1cc2ccccc2[nH]1)c1cccc2ccccc12 | https://pubmed.ncbi.nlm.nih.gov/25220431 | |
| calindol | 784 | None | 4 | Rat | Functional | EC50 | = | 132.00 | 6.88 | 1 | 3 | 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 assay | ChEMBL | 300.2 | 4 | 2 | 1 | 5.17 | C[C@@H](NCc1cc2ccccc2[nH]1)c1cccc2ccccc12 | https://dx.doi.org/10.1016/j.bmc.2015.12.019 | |
| calindol | 784 | None | 4 | Rat | Functional | EC50 | = | 131.83 | 6.88 | 1 | 3 | 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 assay | ChEMBL | 300.2 | 4 | 2 | 1 | 5.17 | C[C@@H](NCc1cc2ccccc2[nH]1)c1cccc2ccccc12 | https://dx.doi.org/10.1016/j.bmc.2015.12.019 | |
| calindol | 784 | None | 4 | Rat | Functional | EC50 | = | 1000.00 | 6.00 | 1 | 3 | Ability to stimulate [3H]inositol phosphates accumulation in CHO cells expressing rat Calcium sensing receptor (CaSR) at 2 mM [Ca2+] | ChEMBL | 300.2 | 4 | 2 | 1 | 5.17 | C[C@@H](NCc1cc2ccccc2[nH]1)c1cccc2ccccc12 | https://dx.doi.org/10.1016/j.bmcl.2004.03.056 | |
| CHEMBL1082306 | 6398 | None | 0 | Human | Functional | IC50 | = | 150.00 | 6.82 | - | 1 | Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay | ChEMBL | 405.3 | 11 | 2 | 3 | 5.67 | CCCC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccccc1 | https://dx.doi.org/10.1016/j.bmcl.2010.04.035 | |
| CHEMBL1082379 | 6421 | None | 0 | Human | Functional | IC50 | = | 550.00 | 6.26 | - | 1 | Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay | ChEMBL | 427.3 | 9 | 2 | 3 | 6.04 | CC(OC[C@H](O)CNC(C)(C)Cc1ccc2ccccc2c1)c1ccc2ccccc2c1 | https://dx.doi.org/10.1016/j.bmcl.2010.04.035 | |
Showing 1 to 20 of 573 entries