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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 |
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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 28:
Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]