diquafosol [Ligand Id: 1736] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL221326 (Dicuafosol, Diquafosol, INS-365) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| 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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
