ChEMBL ligand: CHEMBL2419490
D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] There should be some charts here, you may need to enable JavaScript!
M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] 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] 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
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL	PDSP Secondary Binding target: DRD3 - 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	5.55	pKi	2812.87	nM	Ki	EUbOPEN Chemogenomics Library - PDSP Secondary Binding
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL	PDSP Secondary Binding target: CHRM2 - 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	5.04	pKi	9065.67	nM	Ki	EUbOPEN Chemogenomics Library - PDSP Secondary Binding
P2Y12 receptor/Purinergic receptor P2Y12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2001] [GtoPdb: 328] [UniProtKB: Q9H244]
GtoPdb	-	-	8	pKi	-	-	-	Nature (2014) 509: 115-8 [PMID:24670650]; Future Med Chem (2013) 5: 2037-56 [PMID:24215345]
ChEMBL	Antagonist activity at P2Y12 receptor in human platelet rich plasma	F	5.44	pIC50	3600	nM	IC50	Bioorg Med Chem (2022) 56: 116614-116614 [PMID:35033884]
ChEMBL	Antagonist activity at P2Y12 receptor in human whole blood assessed as inhibition of ADP-induced platelet aggregation after 5 mins by residual platelet count assay	B	5.49	pIC50	3200	nM	IC50	J Med Chem (2013) 56: 7015-7024 [PMID:23899349]
ChEMBL	Antagonist activity P2Y12 receptor in human blood assessed as inhibition of ADP-induced platelet aggregation measured as residual platelet count after 5 mins by flow cytometric analysis	B	5.49	pIC50	3200	nM	IC50	Bioorg Med Chem Lett (2014) 24: 2963-2968 [PMID:24835983]
ChEMBL	Displacement of [125I]AZ11931285 from human P2Y12 receptor expressed in CHOK1 cell membrane after 10 seconds	B	7.36	pIC50	44	nM	IC50	Bioorg Med Chem Lett (2014) 24: 2963-2968 [PMID:24835983]
ChEMBL	Antagonist activity at P2Y12 receptor (unknown origin) expressed in CHO cell membrane by [35S]GTPgammaS binding assay	F	7.6	pIC50	25	nM	IC50	J Med Chem (2013) 56: 7015-7024 [PMID:23899349]
ChEMBL	Antagonist activity at P2Y12 receptor (unknown origin) assessed as inhibition of ADP-induced [35S]GTPgammaS binding after 45 mins by scintillation counting analysis	F	7.6	pIC50	25	nM	IC50	Bioorg Med Chem Lett (2014) 24: 2963-2968 [PMID:24835983]
ChEMBL	Displacement of [125I]AZ11931285 from human P2Y12 receptor expressed in CHOK1 cell membrane after 30 seconds	B	7.66	pIC50	22	nM	IC50	Bioorg Med Chem Lett (2014) 24: 2963-2968 [PMID:24835983]
ChEMBL	Displacement of [125I]AZ11931285 from human P2Y12 receptor expressed in CHOK1 cell membrane after 60 seconds	B	7.85	pIC50	14	nM	IC50	Bioorg Med Chem Lett (2014) 24: 2963-2968 [PMID:24835983]
ChEMBL	Displacement of [125I]-AZ11931285 from P2Y12 receptor (unknown origin) expressed in CHO cell membrane after 1 hr by scintillation counting analysis	B	7.96	pIC50	11	nM	IC50	J Med Chem (2013) 56: 7015-7024 [PMID:23899349]
ChEMBL	Antagonist activity P2Y12 receptor in human washed platelets assessed as inhibition of ADP-induced platelet aggregation after 5 to 90 mins by spectrophotometric analysis	B	8.05	pIC50	9	nM	IC50	Bioorg Med Chem Lett (2014) 24: 2963-2968 [PMID:24835983]
ChEMBL	Displacement of [125I]AZ11931285 from human P2Y12 receptor expressed in CHOK1 cell membrane after 60 mins	B	8.05	pIC50	9	nM	IC50	Bioorg Med Chem Lett (2014) 24: 2963-2968 [PMID:24835983]

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]