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 P2X4R (unknown origin) expressed in 1321N1 cells	B	5.71	pIC50	1950	nM	IC50	J Med Chem (2022) 65: 13967-13987 [PMID:36150180]
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 against human P2X4R stably transfected in human 1321N1 cells incubated for 30 mins by Fura-2 AM staining based calcium influx assay	B	6.04	pIC50	904	nM	IC50	Eur J Med Chem (2022) 238: 114491-114491 [PMID:35660250]
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 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]