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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-chloroadenosine-5-triphosphate | 59 | None | 11 | Human | Binding | pKi | None | - | 5.60 | - | 4 | Unclassified | Guide to Pharmacology | 541.0 | 8 | 7 | 14 | -0.98 | Nc1nc(Cl)nc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O | https://pubmed.ncbi.nlm.nih.gov/9547364 | |
2-chloroadenosine-5-triphosphate | 59 | None | 11 | Human | Binding | EC50 | = | 770.00 | 6.11 | - | 4 | Accumulation of inositol phosphate in 1321N1 astrocytoma cells expressing human P2Y1 purinoceptor | ChEMBL | 541.0 | 8 | 7 | 14 | -0.98 | Nc1nc(Cl)nc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O | https://dx.doi.org/10.1021/jm010538v | |
2-chloroadenosine-5-triphosphate | 59 | None | 11 | Wild turkey | Binding | EC50 | = | 720.00 | 6.14 | - | 4 | Activation of Purinoceptor P2Y1-mediated phospholipase C in turkey erythrocyte membranes | ChEMBL | 541.0 | 8 | 7 | 14 | -0.98 | Nc1nc(Cl)nc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O | https://dx.doi.org/10.1021/jm010538v | |
2MeSADP | 75 | None | 11 | Human | Binding | pKd | = | - | 7.30 | -10 | 5 | Unclassified | Guide to Pharmacology | 473.0 | 7 | 6 | 13 | -1.02 | CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c2n1 | https://pubmed.ncbi.nlm.nih.gov/11502873 | |
2MeSADP | 75 | None | 11 | Human | Binding | EC50 | = | 6.40 | 8.19 | -10 | 5 | Accumulation of inositol phosphate in 1321N1 astrocytoma cells expressing human P2Y1 purinoceptor | ChEMBL | 473.0 | 7 | 6 | 13 | -1.02 | CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c2n1 | https://dx.doi.org/10.1021/jm010538v | |
2MeSADP | 75 | None | 11 | Human | Binding | EC50 | = | 6.00 | 8.22 | -10 | 5 | Effective concentration to activate human Y273F mutant strain P2Y1 receptor expressed in COS-7 cells for the accumulation of inositol phosphate | ChEMBL | 473.0 | 7 | 6 | 13 | -1.02 | CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c2n1 | https://dx.doi.org/10.1021/jm049914c | |
2MeSADP | 75 | None | 11 | Human | Binding | IC50 | = | 360.00 | 6.44 | -10 | 5 | Inhibition concentration required against human Y306F mutant strain P2Y1 receptor expressed in COS-7 cells is determined using [3H]MRS2279 as radioligand | ChEMBL | 473.0 | 7 | 6 | 13 | -1.02 | CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c2n1 | https://dx.doi.org/10.1021/jm049914c | |
2MeSADP | 75 | None | 11 | Human | Binding | EC50 | = | 1.27 | 8.90 | -10 | 5 | Effective concentration required for the activation of wild-type P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | ChEMBL | 473.0 | 7 | 6 | 13 | -1.02 | CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c2n1 | https://dx.doi.org/10.1021/jm049914c | |
2MeSADP | 75 | None | 11 | Human | Binding | EC50 | = | 2.20 | 8.66 | -10 | 5 | Effective concentration required for the activation of wild-type P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate is determined in separate experiment | ChEMBL | 473.0 | 7 | 6 | 13 | -1.02 | CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c2n1 | https://dx.doi.org/10.1021/jm049914c | |
2MeSADP | 75 | None | 11 | Human | Binding | EC50 | = | 18.20 | 7.74 | -10 | 5 | Effective concentration required for the activation of human F131A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | ChEMBL | 473.0 | 7 | 6 | 13 | -1.02 | CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c2n1 | https://dx.doi.org/10.1021/jm049914c | |
2MeSADP | 75 | None | 11 | Human | Binding | EC50 | = | 15.90 | 7.80 | -10 | 5 | Effective concentration required for the activation of human H132A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | ChEMBL | 473.0 | 7 | 6 | 13 | -1.02 | CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c2n1 | https://dx.doi.org/10.1021/jm049914c | |
2MeSADP | 75 | None | 11 | Human | Binding | EC50 | = | 12.60 | 7.90 | -10 | 5 | Effective concentration required for the activation of human Y136A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | ChEMBL | 473.0 | 7 | 6 | 13 | -1.02 | CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c2n1 | https://dx.doi.org/10.1021/jm049914c | |
2MeSADP | 75 | None | 11 | Human | Binding | EC50 | = | 15.90 | 7.80 | -10 | 5 | Effective concentration required for the activation of human T221A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | ChEMBL | 473.0 | 7 | 6 | 13 | -1.02 | CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c2n1 | https://dx.doi.org/10.1021/jm049914c | |
2MeSADP | 75 | None | 11 | Human | Binding | EC50 | = | 11.20 | 7.95 | -10 | 5 | Effective concentration required for the activation of human T222A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | ChEMBL | 473.0 | 7 | 6 | 13 | -1.02 | CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c2n1 | https://dx.doi.org/10.1021/jm049914c | |
2MeSADP | 75 | None | 11 | Human | Binding | EC50 | = | 20.70 | 7.68 | -10 | 5 | Effective concentration required for the activation of human F226A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | ChEMBL | 473.0 | 7 | 6 | 13 | -1.02 | CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c2n1 | https://dx.doi.org/10.1021/jm049914c | |
2MeSADP | 75 | None | 11 | Human | Binding | EC50 | = | 15.00 | 7.82 | -10 | 5 | Effective concentration to activate human Y306A mutant strain P2Y1 receptor expressed in COS-7 cells for the accumulation of inositol phosphate | ChEMBL | 473.0 | 7 | 6 | 13 | -1.02 | CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c2n1 | https://dx.doi.org/10.1021/jm049914c | |
2MeSADP | 75 | None | 11 | Human | Binding | EC50 | = | 100.00 | 7.00 | -10 | 5 | Effective concentration required for the activation of human H277A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | ChEMBL | 473.0 | 7 | 6 | 13 | -1.02 | CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c2n1 | https://dx.doi.org/10.1021/jm049914c | |
2MeSADP | 75 | None | 11 | Human | Binding | EC50 | = | 1790.00 | 5.75 | -10 | 5 | Effective concentration required for the activation of human K280A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | ChEMBL | 473.0 | 7 | 6 | 13 | -1.02 | CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c2n1 | https://dx.doi.org/10.1021/jm049914c | |
2MeSADP | 75 | None | 11 | Human | Binding | EC50 | = | 455.00 | 6.34 | -10 | 5 | Effective concentration required for the activation of human Q307A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | ChEMBL | 473.0 | 7 | 6 | 13 | -1.02 | CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c2n1 | https://dx.doi.org/10.1021/jm049914c | |
2MeSADP | 75 | None | 11 | Human | Binding | EC50 | = | 418.00 | 6.38 | -10 | 5 | Effective concentration required for the activation of human R310K mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate | ChEMBL | 473.0 | 7 | 6 | 13 | -1.02 | CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c2n1 | https://dx.doi.org/10.1021/jm049914c |
Showing 1 to 20 of 744 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 | |
2',3'-ddATP | 47 | None | 0 | Human | Functional | pIC50 | None | - | 8.00 | - | 1 | Unclassified | Guide to Pharmacology | 475.0 | 8 | 5 | 12 | 0.43 | Nc1ncnc2c1ncn2[C@H]1CC[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O1 | https://pubmed.ncbi.nlm.nih.gov/9154346 | |
2,2'-pyridylisatogen tosylate | 43 | None | 0 | Human | Functional | pIC50 | = | - | 6.85 | - | 1 | Unclassified | Guide to Pharmacology | 396.1 | 2 | 1 | 5 | 3.15 | Cc1ccc(S(=O)(=O)O)cc1.O=C1C(c2ccccn2)=[N+]([O-])c2ccccc21 | https://pubmed.ncbi.nlm.nih.gov/15193995 | |
2-chloroadenosine-5-triphosphate | 59 | None | 11 | Rat | Functional | EC50 | = | 3.60 | 8.44 | 199 | 4 | Agonists activity was evaluated by release of [Ca2+] release of HEK 293 cells stably transfected with rat-brain P2Y purinoceptor 1 (P2Y1-R) | ChEMBL | 541.0 | 8 | 7 | 14 | -0.98 | Nc1nc(Cl)nc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O | https://dx.doi.org/10.1021/jm020251d | |
2-Cl-ADP(α-BH3) | 60 | None | 0 | Human | Functional | pEC50 | = | - | 8.15 | - | 1 | Unclassified | Guide to Pharmacology | 455.0 | 6 | 5 | 12 | -0.92 | [B-][P@@](=O)(OC[C@H]1O[C@@H](n2cnc3c(N)nc(Cl)nc32)[C@H](O)[C@@H]1O)OP(=O)(O)O | https://pubmed.ncbi.nlm.nih.gov/23751098 | |
2MeSADP | 75 | None | 11 | Human | Functional | pIC50 | = | - | 6.20 | -39 | 5 | Unclassified | Guide to Pharmacology | 473.0 | 7 | 6 | 13 | -1.02 | CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c2n1 | https://pubmed.ncbi.nlm.nih.gov/9154346 | |
2MeSADP | 75 | None | 11 | Human | Functional | pIC50 | = | - | 6.20 | -39 | 5 | Unclassified | Guide to Pharmacology | 473.0 | 7 | 6 | 13 | -1.02 | CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c2n1 | https://pubmed.ncbi.nlm.nih.gov/12391289 | |
2MeSADP | 75 | None | 11 | Human | Functional | EC50 | = | 1.94 | 8.71 | -39 | 5 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(WT) human P2Y1 receptor. | ChEMBL | 473.0 | 7 | 6 | 13 | -1.02 | CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c2n1 | https://dx.doi.org/10.1021/jm970684u | |
2MeSADP | 75 | None | 11 | Human | Functional | EC50 | = | 19.20 | 7.72 | -39 | 5 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(F131A) human P2Y1 receptor. | ChEMBL | 473.0 | 7 | 6 | 13 | -1.02 | CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c2n1 | https://dx.doi.org/10.1021/jm970684u | |
2MeSADP | 75 | None | 11 | Human | Functional | EC50 | = | 17.70 | 7.75 | -39 | 5 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(H132A) human P2Y1 receptor. | ChEMBL | 473.0 | 7 | 6 | 13 | -1.02 | CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c2n1 | https://dx.doi.org/10.1021/jm970684u | |
2MeSADP | 75 | None | 11 | Human | Functional | EC50 | = | 12.30 | 7.91 | -39 | 5 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(Y136A) human P2Y1 receptor. | ChEMBL | 473.0 | 7 | 6 | 13 | -1.02 | CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c2n1 | https://dx.doi.org/10.1021/jm970684u | |
2MeSADP | 75 | None | 11 | Human | Functional | EC50 | = | 2.45 | 8.61 | -39 | 5 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(T221A) human P2Y1 receptor. | ChEMBL | 473.0 | 7 | 6 | 13 | -1.02 | CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c2n1 | https://dx.doi.org/10.1021/jm970684u | |
2MeSADP | 75 | None | 11 | Human | Functional | EC50 | = | 10.90 | 7.96 | -39 | 5 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(T222A) human P2Y1 receptor. | ChEMBL | 473.0 | 7 | 6 | 13 | -1.02 | CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c2n1 | https://dx.doi.org/10.1021/jm970684u | |
2MeSADP | 75 | None | 11 | Human | Functional | EC50 | = | 19.50 | 7.71 | -39 | 5 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(F226A) human P2Y1 receptor. | ChEMBL | 473.0 | 7 | 6 | 13 | -1.02 | CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c2n1 | https://dx.doi.org/10.1021/jm970684u | |
2MeSADP | 75 | None | 11 | Human | Functional | EC50 | = | 115.00 | 6.94 | -39 | 5 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(H277A) human P2Y1 receptor. | ChEMBL | 473.0 | 7 | 6 | 13 | -1.02 | CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c2n1 | https://dx.doi.org/10.1021/jm970684u | |
2MeSADP | 75 | None | 11 | Human | Functional | EC50 | = | 1520.00 | 5.82 | -39 | 5 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(K280A) human P2Y1 receptor. | ChEMBL | 473.0 | 7 | 6 | 13 | -1.02 | CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c2n1 | https://dx.doi.org/10.1021/jm970684u | |
2MeSADP | 75 | None | 11 | Human | Functional | EC50 | = | 323.00 | 6.49 | -39 | 5 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(Q307A) human P2Y1 receptor. | ChEMBL | 473.0 | 7 | 6 | 13 | -1.02 | CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c2n1 | https://dx.doi.org/10.1021/jm970684u | |
2MeSADP | 75 | None | 11 | Human | Functional | EC50 | = | 324.00 | 6.49 | -39 | 5 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(R310K) human P2Y1 receptor. | ChEMBL | 473.0 | 7 | 6 | 13 | -1.02 | CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c2n1 | https://dx.doi.org/10.1021/jm970684u | |
2MeSADP | 75 | None | 11 | Human | Functional | EC50 | = | 10.40 | 7.98 | -39 | 5 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(S314T) human P2Y1 receptor. | ChEMBL | 473.0 | 7 | 6 | 13 | -1.02 | CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c2n1 | https://dx.doi.org/10.1021/jm970684u | |
2MeSADP | 75 | None | 11 | Human | Functional | EC50 | = | 1.88 | 8.73 | -39 | 5 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(S317A) human P2Y1 receptor. | ChEMBL | 473.0 | 7 | 6 | 13 | -1.02 | CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c2n1 | https://dx.doi.org/10.1021/jm970684u | |
2MeSADP | 75 | None | 11 | Human | Functional | EC50 | = | 12.90 | 7.89 | -39 | 5 | Compound was measured for the antagonism of the activation of phospholipase C in mutant(WT) human P2Y1 receptor in presence of MRS2179 (P<0.005) | ChEMBL | 473.0 | 7 | 6 | 13 | -1.02 | CSc1nc(N)c2ncn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c2n1 | https://dx.doi.org/10.1021/jm970684u |
Showing 1 to 20 of 451 entries