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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 |
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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 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 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]