5-BDBD [Ligand Id: 9541] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2180179
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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 P2X4R (unknown origin) expressed in 1321N1 cells B 5.28 pIC50 5200 nM IC50 J Med Chem (2022) 65: 13967-13987 [PMID:36150180]
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 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 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 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 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]
P2X4/P2X purinoceptor 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2818] [GtoPdb: 481] [UniProtKB: P51577]
ChEMBL Antagonist activity at rat P2X4R expressed in HEK293 cells preincubated for 2 mins followed by ATP addition and measured after 4 mins B 6.12 pIC50 750 nM IC50 J Med Chem (2022) 65: 13967-13987 [PMID:36150180]

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]