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ChEMBL ligand: CHEMBL398435 (AR-C126532XX, AZD-6140, AZD6140, Brilinta, Brilique, Possia, Ticagrelor) |
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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 | - | - | 7.85 | pKi | 14 | nM | Ki | J Med Chem (2012) 55: 8615-29 [PMID:22984835] |
ChEMBL | Displacement of [33P]2-MeS-ADP from human recombinant P2Y12 receptor expressed in CHO cell membranes by scintillation counting method | B | 7.85 | pKi | 14 | nM | Ki | J Med Chem (2012) 55: 8615-8629 [PMID:22984835] |
GtoPdb | Binding data obtained using washed platelets in 96-well plates, with [125I]-P2Y12 antagonist as radioligand. | - | 8.7 | pKi | 1.99 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 6013-8 [PMID:17827008] |
ChEMBL | Displacement of [125I] labeled ligand from human P2Y12 receptor in human platelets | B | 8.7 | pKi | 2 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 6013-6018 [PMID:17827008] |
ChEMBL | Antagonist activity at P2Y12 in human whole blood assessed as suppression of ADP-induced decrease in PGE1-induced VASP phosphorylation measured after 10 mins by immunostaining based flow cytometric analysis | B | 5.29 | pIC50 | 5140 | nM | IC50 | J Med Chem (2020) 63: 15752-15772 [PMID:33307675] |
ChEMBL | Antagonist activity at P2Y12 receptor in human platelet-rich plasma assessed as inhibition of ADP-induced platelet aggregation incubated for 5 mins prior to ADP-challenge by light transmission-based assay | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 141-146 [PMID:24332627] |
ChEMBL | Inhibition of P2Y12 in human platelet rich plasma assessed as reduction in ADP-induced platelet aggregation pre-incubated before ADP addition and measured after 10 mins by Bruker spectrophotometry | B | 6.49 | pIC50 | 320 | nM | IC50 | Bioorg Med Chem (2017) 25: 5260-5267 [PMID:28789912] |
ChEMBL | Antagonist activity at P2Y12 receptor (unknown origin) | B | 8.3 | pIC50 | 5.01 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 2739-2754 [PMID:27133596] |
P2Y12 receptor/Purinergic receptor P2Y12 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2188] [GtoPdb: 328] [UniProtKB: Q9EPX4] | ||||||||
ChEMBL | Antagonist activity at P2Y12 receptor in Sprague-Dawley rat platelet rich plasma assessed as inhibition of ADP-induced aggregation | B | 5.38 | pIC50 | 4160 | nM | IC50 | J Med Chem (2014) 57: 7293-7316 [PMID:25075638] |
ChEMBL | Antagonist activity at P2Y12 receptor in rat platelet-rich plasma assessed as inhibition of ADP-induced platelet aggregation incubated for 5 mins prior to ADP-challenge by light transmission-based assay | B | 6 | pIC50 | <1000 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 141-146 [PMID:24332627] |
Equilibrative nucleoside transporter 1 in Human [GtoPdb: 1117] [UniProtKB: Q99808] | ||||||||
GtoPdb | - | - | 7.3 | pKi | - | - | - | J Cardiovasc Pharmacol Ther (2014) 19: 209-19 [PMID:24414167] |
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]