ChEMBL ligand: CHEMBL1532400
P2X4/P2X purinoceptor 4 in Human [ChEMBL: CHEMBL2104] [GtoPdb: 481] [UniProtKB: Q99571] 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
P2X4/P2X purinoceptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2104] [GtoPdb: 481] [UniProtKB: Q99571]
ChEMBL	Antagonist activity at human P2X4R transfected in 1321N1 cells	B	5.8	pIC50	1600	nM	IC50	J Nat Prod (2019) 82: 2559-2567 [PMID:31532206]
ChEMBL	Antagonist activity at human P2X4R transfected in HEK293 cells assessed as inhibition of ATP-mediated calcium influx measured after 10 mins by YOPRO-1 dye uptake assay	B	5.89	pIC50	1300	nM	IC50	J Nat Prod (2019) 82: 2559-2567 [PMID:31532206]
GtoPdb	-	-	6	pIC50	-	-	-	Mol Pharmacol (2013) 83: 759-69 [PMID:23253448]; Neuropharmacology (2016) 104: 31-49 [PMID:26686393]
ChEMBL	Antagonist activity at human P2X4 receptor tranfected in human HEK293 cells assessed as inhibition of ATP-induced calcium influx by Fluo2-AM staining based inverted fluorescence microscopic method	B	6.11	pIC50	780	nM	IC50	J Med Chem (2019) 62: 11194-11217 [PMID:31746599]
ChEMBL	Antagonist activity at human P2X4R transfected in 1321N1 cells assessed as inhibition of ATP-mediated calcium influx measured after 10 mins by Fura-2AM assay	B	6.26	pIC50	550	nM	IC50	J Nat Prod (2019) 82: 2559-2567 [PMID:31532206]
ChEMBL	Antagonist activity at human P2X4R transfected in HEK293 cells assessed as inhibition of ATP-evoked current by patch clamp assay	B	6.27	pIC50	540	nM	IC50	J Nat Prod (2019) 82: 2559-2567 [PMID:31532206]
ChEMBL	Antagonist activity at human P2X4 receptor tranfected in human HEK293 cells at -60 mv holding potential by Whole cell patch-clamp method	B	6.3	pIC50	500	nM	IC50	J Med Chem (2019) 62: 11194-11217 [PMID:31746599]

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]