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

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ChEMBL ligand: CHEMBL526307
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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: 480479] [UniProtKB: P56373Q9UBL9]
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 in Human [GtoPdb: 480] [UniProtKB: P56373]
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 26:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]