ChEMBL ligand: CHEMBL398435 (AR-C126532XX, AZD-6140, AZD6140, Brilinta, Brilique, Possia, Ticagrelor)
P2Y12 receptor/Purinergic receptor P2Y12 in Human [ChEMBL: CHEMBL2001] [GtoPdb: 328] [UniProtKB: Q9H244] P2Y12 receptor/Purinergic receptor P2Y12 in Rat [ChEMBL: CHEMBL2188] [GtoPdb: 328] [UniProtKB: Q9EPX4] There should be some charts here, you may need to enable JavaScript!
Equilibrative nucleoside transporter 1 in Human [GtoPdb: 1117] [UniProtKB: Q99808] There should be some charts here, you may need to enable JavaScript!

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	-	-	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]