ChEMBL ligand: CHEMBL334966 (AR-C69931XX, Cangrelor, Kengreal)
P2Y12 receptor/P2Y purinoceptor 12 in Human [ChEMBL: CHEMBL2001] [GtoPdb: 328] [UniProtKB: Q9H244] 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!
GPR17 in Mouse [GtoPdb: 88] [UniProtKB: Q6NS65] 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/P2Y purinoceptor 12 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	Antagonist activity at P2Y12 receptor (unknown origin)	F	9.4	pIC50	0.4	nM	IC50	Eur J Med Chem (2024) 275: 116593-116593 [PMID:38889609]
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]
P2Y13 receptor/P2Y purinoceptor 13 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3321651] [GtoPdb: 329] [UniProtKB: Q9BPV8]
GtoPdb	-	-	8.3	pIC50	-	-	-	Mol Pharmacol (2003) 64: 104-12 [PMID:12815166]
ChEMBL	Ca++ flux assay: Compounds were assayed for their agonist activity on P2Y13 GPCR transfected cells using a Ca++ flux assay (associated to fluorescent dye detection) with the Reference Compound as positive reference. Two cell lines, 1321N1-P2Y13 stably expressing human P2Y13 receptor, and 1321N1 parental cell line as control, were used in this assay. 1321N1 Parental and 1321N1 P2Y13 were seeded into T25 flasks at 3 million cells per flask, respectively. Cells were incubated at 37 degrees Celsius in 5% CO2 overnight. The day after, cells were transfected with Gqi5 protein using Fugene transfection reagent (Roche's Fugene Reagent).After 24 hours of transfection, cells were collected from flasks and seeded in 384-well plates at 8000 cells per well. The assays were carried out 48 hours after Gqi5 transfection.Methods: The Ca++ flux assay was conducted according to the manufacturer's protocol (Molecular Devices FLIPR Calcium 4 Assay kit (R8142). Briefly, cell culture media were aspirated from the wells and replaced with 25 μL of Hank's buffer or PBS buffer. 25 μL of Ca++ dye was added into each assay well. The plate was incubated for 1 hour at 37° C. in 5% CO2. After the incubation, the plate was transferred to FlexStation III (FlexStation III (Molecular Devices)). The compounds were automatically injected into each well.	B	5.2	pEC50	6322	nM	EC50	US-10220040-B2. Compounds, compositions and methods useful for cholesterol mobilization (2019)
GPR17 in Mouse [GtoPdb: 88] [UniProtKB: Q6NS65]
GtoPdb	-	-	8.92	pIC50	1.2	nM	IC50	PLoS ONE (2008) 3: e3579 [PMID:18974869]

ChEMBL data shown on this page come from version 36:

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]