[3H]A317491 [Ligand Id: 5407] 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: CHEMBL596234 (A-317491) |
|---|
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 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] |
| 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] |
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]
