cangrelor [Ligand Id: 1776] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL334966 (AR-C69931XX, Cangrelor)
  • P2Y12 receptor/Purinergic receptor P2Y12 in Human [ChEMBL: CHEMBL2001] [GtoPdb: 328] [UniProtKB: Q9H244]
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  • GPR17 in Mouse [GtoPdb: 88] [UniProtKB: Q6NS65]
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  • P2Y13 receptor in Human [GtoPdb: 329] [UniProtKB: Q9BPV8]
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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]
ChEMBL Antagonist activity at human platelet P2Y12 receptor assessed as inhibition of ADP-mediated decrease in intra-platelet phosphorylated VASP by FLUO-4 staining based flow cytometric analysis B 7.74 pIC50 18.3 nM IC50 Eur J Med Chem (2016) 107: 204-218 [PMID:26588064]
GtoPdb - - 8 pIC50 - - - Mol Pharmacol (2001) 60: 432-439 [PMID:11502873]
ChEMBL Antagonist activity at P2Y12 receptor in human washed platelets assessed as inhibition of ADP-induced aggregation preincubated for 5 mins followed by ADP addition by turbidimetric analysis B 8.7 pIC50 2 nM IC50 Bioorg Med Chem (2015) 23: 3880-3906 [PMID:25638496]
ChEMBL The compound was evaluated for antagonist activity against platelet P2Y purinoceptor 12 (P2Y12) F 9.4 pIC50 0.4 nM IC50 J Med Chem (2002) 45: 4057-4093 [PMID:12213051]
GtoPdb - - 9.4 pIC50 0.4 nM IC50 J Med Chem (2002) 45: 4057-93 [PMID:12213051]
ChEMBL Antagonist activity at P2Y12 receptor in human platelets assessed as inhibition of ADP-induced platelet aggregation by turbidimetric method B 9.4 pIC50 0.4 nM IC50 Bioorg Med Chem Lett (2016) 26: 2739-2754 [PMID:27133596]
GPR17 in Mouse [GtoPdb: 88] [UniProtKB: Q6NS65]
GtoPdb - - 8.92 pIC50 1.2 nM IC50 PLoS ONE (2008) 3: e3579 [PMID:18974869]
P2Y13 receptor in Human [GtoPdb: 329] [UniProtKB: Q9BPV8]
GtoPdb - - 8.3 pIC50 - - - Mol Pharmacol (2003) 64: 104-12 [PMID:12815166]

ChEMBL data shown on this page come from version 32:

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]