cangrelor [Ligand Id: 1776] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL334966 (AR-C69931XX, Cangrelor) |
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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 | Inhibition of P2Y12 (unknown origin) | B | 9.35 | pIC50 | 0.45 | nM | IC50 | Bioorg Med Chem Lett (2022) 71: 128837-128837 [PMID:35640763] |
| 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] |
| ChEMBL | Antagonist activity at P2Y12 (unknown origin) | B | 9.4 | pIC50 | 0.4 | nM | IC50 | J Med Chem (2016) 59: 9981-10005 [PMID:27413802] |
| 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 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]
