diquafosol [Ligand Id: 1736] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL221326 (Diquafosol, INS-365) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| P2Y1 receptor/Purinergic receptor P2Y1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4315] [GtoPdb: 323] [UniProtKB: P47900] | ||||||||
| ChEMBL | Agonist activity at human cloned P2Y1 receptor expressed in human 1321N1 by FLIPR assay | F | 4.7 | pEC50 | >20000 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 562-565 [PMID:17011188] |
| P2Y2 receptor/Purinergic receptor P2Y2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4398] [GtoPdb: 324] [UniProtKB: P41231] | ||||||||
| ChEMBL | Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level | F | 6.24 | pEC50 | 572 | nM | EC50 | J Med Chem (2009) 52: 2762-2775 [PMID:19419204] |
| ChEMBL | Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level | F | 6.38 | pEC50 | 419 | nM | EC50 | J Med Chem (2009) 52: 2762-2775 [PMID:19419204] |
| ChEMBL | Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level | F | 6.4 | pEC50 | 394 | nM | EC50 | J Med Chem (2009) 52: 2762-2775 [PMID:19419204] |
| ChEMBL | Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level | F | 6.64 | pEC50 | 231 | nM | EC50 | J Med Chem (2009) 52: 2762-2775 [PMID:19419204] |
| ChEMBL | Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level | F | 6.67 | pEC50 | 216 | nM | EC50 | J Med Chem (2009) 52: 2762-2775 [PMID:19419204] |
| ChEMBL | Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C | F | 6.68 | pEC50 | 210 | nM | EC50 | J Med Chem (2007) 50: 1166-1176 [PMID:17302398] |
| ChEMBL | Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay | F | 6.68 | pEC50 | 210 | nM | EC50 | Bioorg Med Chem (2008) 16: 6319-6332 [PMID:18514530] |
| ChEMBL | Agonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level | F | 6.75 | pEC50 | 179 | nM | EC50 | J Med Chem (2009) 52: 2762-2775 [PMID:19419204] |
| ChEMBL | Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level | F | 6.84 | pEC50 | 145 | nM | EC50 | J Med Chem (2009) 52: 2762-2775 [PMID:19419204] |
| ChEMBL | Agonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level | F | 6.95 | pEC50 | 112 | nM | EC50 | J Med Chem (2009) 52: 2762-2775 [PMID:19419204] |
| GtoPdb | - | - | 7 | pEC50 | - | - | - | Bioorg Med Chem Lett (2001) 11: 157-60 [PMID:11206448] |
| ChEMBL | Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assay | F | 7 | pEC50 | 100 | nM | EC50 | J Med Chem (2010) 53: 1673-1685 [PMID:20095577] |
| ChEMBL | Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level | F | 7.02 | pEC50 | 94.5 | nM | EC50 | J Med Chem (2009) 52: 2762-2775 [PMID:19419204] |
| ChEMBL | Agonist activity at human P2Y purinoceptor 2 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetry | F | 7.22 | pEC50 | 60 | nM | EC50 | J Med Chem (2012) 55: 437-448 [PMID:22107038] |
| P2Y4 receptor/Pyrimidinergic receptor P2Y4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2123] [GtoPdb: 325] [UniProtKB: P51582] | ||||||||
| GtoPdb | - | - | 6.4 | pEC50 | - | - | - | Curr Med Chem (2006) 13: 289-312 [PMID:16475938] |
| ChEMBL | Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C | F | 6.89 | pEC50 | 130 | nM | EC50 | J Med Chem (2007) 50: 1166-1176 [PMID:17302398] |
| ChEMBL | Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay | F | 6.89 | pEC50 | 130 | nM | EC50 | Bioorg Med Chem (2008) 16: 6319-6332 [PMID:18514530] |
| P2Y6 receptor/Pyrimidinergic receptor P2Y6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4714] [GtoPdb: 326] [UniProtKB: Q15077] | ||||||||
| ChEMBL | Agonist activity at human recombinant P2Y6 receptor expressed in 1321N1 cells assessed as intracellular calcium mobilization | F | 4.7 | pEC50 | 20000 | nM | EC50 | J Med Chem (2007) 50: 1166-1176 [PMID:17302398] |
| ChEMBL | Agonist activity at human P2Y6 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay | F | 5.94 | pEC50 | 1160 | nM | EC50 | Bioorg Med Chem (2008) 16: 6319-6332 [PMID:18514530] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
