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ChEMBL ligand: CHEMBL596234 (A-317491) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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P2X3/P2X2/P2X2/P2X3 heterotrimeric receptor in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3831281] [GtoPdb: 480, 479] [UniProtKB: P56373, Q9UBL9] | ||||||||
ChEMBL | Antagonist activity at human P2X2/3 expressed in human1321N1 cells assessed as inhibition of alpha,beta-methylene-ATP-stimulated Ca2+ influx preincubated for 3 mins followed by alpha,beta-methylene-ATP addition measured after 3 mins by Fluo-4 assay | B | 8.05 | pKi | 9 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 3896-3904 [PMID:27423478] |
GtoPdb | - | - | 7.5 | pIC50 | ~31 | nM | IC50 | Proc Natl Acad Sci USA (2002) 99: 17179-84 [PMID:12482951] |
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 | 6.66 | pIC50 | 220 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 3896-3904 [PMID:27423478] |
ChEMBL | Antagonist activity at recombinant human P2X3 receptor transfected in human 1321N1 cells assessed as inhibition of alpha, beta me-ATP-induced current by whole-cell patch-clamp method | B | 7.01 | pIC50 | 97 | nM | IC50 | Eur J Med Chem (2013) 70: 811-830 [PMID:24246730] |
ChEMBL | Antagonist activity at human P2X3 receptor expressed in C6-BU-1 cells assessed as inhibition of calcium flux after 1 hr by Fluo-3AM dye based FLIPR assay | B | 7.04 | pIC50 | 92 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 2338-2342 [PMID:29805055] |
ChEMBL | Antagonist activity at recombinant human P2X3 receptor expressed in Xenopus oocytes assessed as inhibition of ATP-induced ion current preincubated for 20 mins followed by ATP addition by two-electrode voltage clamp assay | B | 7.46 | pIC50 | 35 | nM | IC50 | Eur J Med Chem (2013) 70: 811-830 [PMID:24246730] |
GtoPdb | - | - | 7.5 | pIC50 | ~31 | nM | IC50 | Proc Natl Acad Sci USA (2002) 99: 17179-84 [PMID:12482951] |
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]