ChEMBL ligand: CHEMBL2180179
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 HEK293 cells assessed as inhibition of ATP-mediated calcium influx measured after 10 mins by YOPRO-1 dye uptake assay	B	5.04	pIC50	9200	nM	IC50	J Nat Prod (2019) 82: 2559-2567 [PMID:31532206]
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	5.24	pIC50	5700	nM	IC50	J Nat Prod (2019) 82: 2559-2567 [PMID:31532206]
ChEMBL	Antagonist activity at human P2X4 receptor expressed in HEK cells by Qpatch method	B	5.4	pIC50	3990	nM	IC50	J Med Chem (2019) 62: 11194-11217 [PMID:31746599]
ChEMBL	Antagonist activity at human P2X4 receptor expressed in HEK cells assessed as reduction in ATP induced calcium influx	B	5.43	pIC50	3710	nM	IC50	J Med Chem (2019) 62: 11194-11217 [PMID:31746599]
ChEMBL	Antagonist activity at human P2X4R transfected in HEK293 cells	B	5.92	pIC50	1200	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 expressed in CHO cells assessed as inhibition of ATP-induced calcium influx	B	6.3	pIC50	500	nM	IC50	J Med Chem (2016) 59: 7410-7430 [PMID:27427902]
ChEMBL	Antagonist activity at human P2X4 receptor expressed in CHO cells	B	6.3	pIC50	500	nM	IC50	Eur J Med Chem (2018) 151: 462-481 [PMID:29649742]
ChEMBL	Antagonist activity at human P2X4 receptor expressed in CHO cells assessed as reduction in ATP induced calcium influx	B	6.3	pIC50	500	nM	IC50	J Med Chem (2019) 62: 11194-11217 [PMID:31746599]
ChEMBL	Antagonist activity at human P2X4 receptor expressed in 1321N1 cells assessed as inhibition of ATP-induced cytosolic calcium influx compound preincubated for 30 mins before ATP treatment by Fluo-4 AM fluorescence method	F	6.3	pIC50	500	nM	IC50	J Med Chem (2012) 55: 9576-9588 [PMID:23075067]
ChEMBL	Antagonist activity at human P2X4 receptor expressed in 1321N1 cells assessed as inhibition of ATP-induced calcium flux measured for 30 secs at 0.4 secs intervals by Flou-4-AM dye based fluorescence assay	B	6.46	pIC50	350	nM	IC50	Eur J Med Chem (2018) 151: 462-481 [PMID:29649742]
ChEMBL	Antagonist activity at human P2X4 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced calcium influx preincubated for 30 mins prior to ATP-stimulation by calcium influx assay	B	6.46	pIC50	348	nM	IC50	J Med Chem (2016) 59: 7410-7430 [PMID:27427902]

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]