AF353 [Ligand Id: 4125] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL526307
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
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
P2X3/P2X2/P2X2/P2X3 heterotrimeric receptor in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3831281] [GtoPdb: 480, 479] [UniProtKB: P56373, Q9UBL9]
ChEMBL Antagonist activity against human P2X2/3 receptor expressed in CHOK1 cells assessed as inhibition of alpha,beta-meATP-induced calcium response incubated for 20 mins by Fluo-3AM dye based FLIPR assay F 7.38 pKi 41.69 nM Ki US-20080207655-A1. Diaminopyrimidines as P2X3 and P2X2/3 modulators (2008)
ChEMBL Antagonist activity at human recombinant P2X2/3 receptor expressed in human 1321N1 cells by FLIPR assay F 7.1 pIC50 79.43 nM IC50 Bioorg Med Chem Lett (2009) 19: 1628-1631 [PMID:19231180]
ChEMBL Antagonist activity at human P2X2/3 receptor expressed in 1321n1c cells by FLIPR F 7.4 pIC50 39.81 nM IC50 Bioorg Med Chem Lett (2009) 19: 1632-1635 [PMID:19231178]
ChEMBL Antagonist activity at human P2X2/3 receptor expressed in 1321n1c cells by FLIPR F 7.6 pIC50 25 nM IC50 Bioorg Med Chem Lett (2009) 19: 1632-1635 [PMID:19231178]
GtoPdb - - 8 pIC50 ~10 nM IC50 Br J Pharmacol (2010) 160: 1387-98 [PMID:20590629]
P2X1/P2X purinoceptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2094] [GtoPdb: 478] [UniProtKB: P51575]
ChEMBL Inhibition of P2X1 receptor B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2009) 19: 1628-1631 [PMID:19231180]
P2X2/P2X purinoceptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2531] [GtoPdb: 479] [UniProtKB: Q9UBL9]
ChEMBL Inhibition of P2X2 receptor B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2009) 19: 1628-1631 [PMID:19231180]
P2X3/P2X purinoceptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2998] [GtoPdb: 480] [UniProtKB: P56373]
ChEMBL Antagonist activity at human recombinant P2X3 receptor expressed in HEK293-Tet-on cells assessed as alpha,beta-methylene-ATP-stimulated Ca2+ influx by Fluo-4 assay B 7.7 pIC50 20 nM IC50 Bioorg Med Chem Lett (2016) 26: 3896-3904 [PMID:27423478]
GtoPdb - - 8 pIC50 ~10 nM IC50 Br J Pharmacol (2010) 160: 1387-98 [PMID:20590629]
P2X3/P2X purinoceptor 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4824] [GtoPdb: 480] [UniProtKB: P49654]
ChEMBL Antagonist activity against rat P2X3 receptor expressed in CHOK1 cells assessed as inhibition of alpha,beta-meATP-induced calcium response incubated for 20 mins by Fluo-3AM dye based FLIPR assay F 8.01 pKi 9.77 nM Ki US-20080207655-A1. Diaminopyrimidines as P2X3 and P2X2/3 modulators (2008)
ChEMBL Antagonist activity at rat P2X3 receptor expressed in CHO cells by FLIPR F 7.89 pIC50 13 nM IC50 Bioorg Med Chem Lett (2009) 19: 1632-1635 [PMID:19231178]
ChEMBL Antagonist activity at rat P2X3 receptor expressed in CHO cells by FLIPR F 8 pIC50 10 nM IC50 Bioorg Med Chem Lett (2009) 19: 1632-1635 [PMID:19231178]
ChEMBL Antagonist activity at rat recombinant P2X3 receptor expressed in CHO cells by FLIPR assay F 8 pIC50 10 nM IC50 Bioorg Med Chem Lett (2009) 19: 1628-1631 [PMID:19231180]
P2X4/P2X purinoceptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2104] [GtoPdb: 481] [UniProtKB: Q99571]
ChEMBL Inhibition of P2X4 receptor B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2009) 19: 1628-1631 [PMID:19231180]
P2X5/P2X purinoceptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4942] [GtoPdb: 482] [UniProtKB: Q93086]
ChEMBL Inhibition of P2X5 receptor B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2009) 19: 1628-1631 [PMID:19231180]
P2X7/P2X purinoceptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4805] [GtoPdb: 484] [UniProtKB: Q99572]
ChEMBL Inhibition of P2X7 receptor B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2009) 19: 1628-1631 [PMID:19231180]

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]