AZD1283 [Ligand Id: 7360] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2419490 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| P2Y12 receptor/Purinergic receptor P2Y12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2001] [GtoPdb: 328] [UniProtKB: Q9H244] | ||||||||
| GtoPdb | - | - | 8 | pKi | - | - | - |
Nature (2014) 509: 115-8 [PMID:24670650]; Future Med Chem (2013) 5: 2037-56 [PMID:24215345] |
| ChEMBL | Antagonist activity at P2Y12 receptor in human whole blood assessed as inhibition of ADP-induced platelet aggregation after 5 mins by residual platelet count assay | B | 5.49 | pIC50 | 3200 | nM | IC50 | J Med Chem (2013) 56: 7015-7024 [PMID:23899349] |
| ChEMBL | Antagonist activity P2Y12 receptor in human blood assessed as inhibition of ADP-induced platelet aggregation measured as residual platelet count after 5 mins by flow cytometric analysis | B | 5.49 | pIC50 | 3200 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 2963-2968 [PMID:24835983] |
| ChEMBL | Displacement of [125I]AZ11931285 from human P2Y12 receptor expressed in CHOK1 cell membrane after 10 seconds | B | 7.36 | pIC50 | 44 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 2963-2968 [PMID:24835983] |
| ChEMBL | Antagonist activity at P2Y12 receptor (unknown origin) expressed in CHO cell membrane by [35S]GTPgammaS binding assay | F | 7.6 | pIC50 | 25 | nM | IC50 | J Med Chem (2013) 56: 7015-7024 [PMID:23899349] |
| ChEMBL | Antagonist activity at P2Y12 receptor (unknown origin) assessed as inhibition of ADP-induced [35S]GTPgammaS binding after 45 mins by scintillation counting analysis | F | 7.6 | pIC50 | 25 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 2963-2968 [PMID:24835983] |
| ChEMBL | Displacement of [125I]AZ11931285 from human P2Y12 receptor expressed in CHOK1 cell membrane after 30 seconds | B | 7.66 | pIC50 | 22 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 2963-2968 [PMID:24835983] |
| ChEMBL | Displacement of [125I]AZ11931285 from human P2Y12 receptor expressed in CHOK1 cell membrane after 60 seconds | B | 7.85 | pIC50 | 14 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 2963-2968 [PMID:24835983] |
| ChEMBL | Displacement of [125I]-AZ11931285 from P2Y12 receptor (unknown origin) expressed in CHO cell membrane after 1 hr by scintillation counting analysis | B | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (2013) 56: 7015-7024 [PMID:23899349] |
| ChEMBL | Displacement of [125I]AZ11931285 from human P2Y12 receptor expressed in CHOK1 cell membrane after 60 mins | B | 8.05 | pIC50 | 9 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 2963-2968 [PMID:24835983] |
| ChEMBL | Antagonist activity P2Y12 receptor in human washed platelets assessed as inhibition of ADP-induced platelet aggregation after 5 to 90 mins by spectrophotometric analysis | B | 8.05 | pIC50 | 9 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 2963-2968 [PMID:24835983] |
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]
