ChEMBL ligand: CHEMBL398435 (AR-C126532XX, AZD-6140, AZD6140, Brilinta, Brilique, Possia, Ticagrelor)
DAT/Dopamine transporter in Human [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959] There should be some charts here, you may need to enable JavaScript!
GPR183/G-protein coupled receptor 183 in Human [ChEMBL: CHEMBL3259470] [GtoPdb: 81] [UniProtKB: P32249] There should be some charts here, you may need to enable JavaScript!
FPR3/N-formyl peptide receptor 3 in Human [ChEMBL: CHEMBL5646] [GtoPdb: 224] [UniProtKB: P25089] There should be some charts here, you may need to enable JavaScript!
P2Y13 receptor/P2Y purinoceptor 13 in Human [ChEMBL: CHEMBL3321651] [GtoPdb: 329] [UniProtKB: Q9BPV8] There should be some charts here, you may need to enable JavaScript!
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!
σ2/Sigma intracellular receptor 2 in Human [ChEMBL: CHEMBL4105907] [GtoPdb: 2553] [UniProtKB: Q5BJF2] 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
DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
ChEMBL	PDSP Secondary Binding target: SLC6A3 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.	B	6.29	pKi	518.8	nM	Ki	EUbOPEN Chemogenomics Library - PDSP Secondary Binding
GPR183/G-protein coupled receptor 183 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3259470] [GtoPdb: 81] [UniProtKB: P32249]
ChEMBL	GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183	F	5.31	pIC50	4878.5	nM	IC50	EUbOPEN Chemogenomics Library - GPCR Dose-Respose
FPR3/N-formyl peptide receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5646] [GtoPdb: 224] [UniProtKB: P25089]
ChEMBL	GPCR PRESTO-Tango dose-response in antagonist mode with target: FPR3	F	5.43	pIC50	3750.52	nM	IC50	EUbOPEN Chemogenomics Library - GPCR Dose-Respose
P2Y13 receptor/P2Y purinoceptor 13 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3321651] [GtoPdb: 329] [UniProtKB: Q9BPV8]
ChEMBL	Antagonist activity at human P2Y13R expressed in HEK293 cells assessed as inhibition of 2MeSADP-induced cAMP production preincubated for 0.5 hrs followed by 2MeSADP stimulation by cAMP-glo assay	F	5.85	pIC50	1398	nM	IC50	J Med Chem (2022) 65: 15967-15990 [PMID:36394994]
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 human P2Y12R expressed in HEK293 cells assessed as inhibition of MeSADP-induced cAMP production preincubated for 0.5 hrs followed by MeSADP stimulation by cAMP-glo analysis	F	5.85	pIC50	1398	nM	IC50	J Med Chem (2023) 66: 6315-6332 [PMID:37078976]
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	Inhibition of P2Y12 receptor in human platelet assessed as reduction in ADP-induced VASP phosphorylation by flow cytometry	F	7.41	pIC50	39	nM	IC50	RSC Med Chem (2021) 12: 1414-1427 [PMID:34458743]
ChEMBL	Inhibition of P2Y12 (unknown origin)	B	8	pIC50	10	nM	IC50	Bioorg Med Chem Lett (2022) 71: 128837-128837 [PMID:35640763]
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]
σ2/Sigma intracellular receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105907] [GtoPdb: 2553] [UniProtKB: Q5BJF2]
ChEMBL	PDSP Secondary Binding target: TMEM97 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.	B	5.89	pKi	1295.39	nM	Ki	EUbOPEN Chemogenomics Library - PDSP Secondary Binding
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 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]