A839977 [Ligand Id: 4122] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1628691 (A-839977) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| P2X7/P2X purinoceptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4805] [GtoPdb: 484] [UniProtKB: Q99572] | ||||||||
| ChEMBL | Antagonist activity at human P2X7 receptor expressed in human THP1 cells assessed as reduction in BzATP-induced IL-1beta levels preincubated for 30 mins followed by BzATP addition measured after 30 mins by ELISA | B | 7.43 | pIC50 | 37.15 | nM | IC50 | Eur J Med Chem (2017) 139: 698-717 [PMID:28858765] |
| ChEMBL | Antagonist activity at human P2X7 receptor expressed in human 1321N1 cells assessed as reduction in agonist-induced intracellular Ca2+ levels preincubated for 3 mins followed by agonist addition measured up to 2 mins by Fluo-4 dye-based FLIPR assay | B | 7.7 | pIC50 | 20 | nM | IC50 | Eur J Med Chem (2017) 139: 698-717 [PMID:28858765] |
| GtoPdb | - | - | 7.7 | pIC50 | ~20 | nM | IC50 |
Br J Pharmacol (2007) 151: 571-9 [PMID:17471177]; Br J Pharmacol (2009) 157: 1203-14 [PMID:19558545]; Behav Brain Res (2009) 204: 77-81 [PMID:19464323] |
| ChEMBL | Antagonist activity at human P2X7 receptor expressed in human THP1 cells assessed as reduction in BzATP-induced pore formation by measuring YO-PRO uptake by FLIPR assay | B | 8.18 | pIC50 | 6.61 | nM | IC50 | Eur J Med Chem (2017) 139: 698-717 [PMID:28858765] |
| P2X7/P2X purinoceptor 7 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5183] [GtoPdb: 484] [UniProtKB: Q9Z1M0] | ||||||||
| ChEMBL | Antagonist activity at mouse P2X7 receptor expressed in human 1321N1 cells assessed as reduction in agonist-induced intracellular Ca2+ levels preincubated for 3 mins followed by agonist addition measured up to 2 mins by Fluo-4 dye-based FLIPR assay | B | 7.7 | pIC50 | 20 | nM | IC50 | Eur J Med Chem (2017) 139: 698-717 [PMID:28858765] |
| P2X7/P2X purinoceptor 7 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2496] [GtoPdb: 484] [UniProtKB: Q64663] | ||||||||
| ChEMBL | Antagonist activity at rat P2X7 receptor expressed in human 1321N1 cells assessed as reduction in agonist-induced intracellular Ca2+ levels preincubated for 3 mins followed by agonist addition measured up to 2 mins by Fluo-4 dye-based FLIPR assay | B | 7.7 | pIC50 | 20 | nM | IC50 | Eur J Med Chem (2017) 139: 698-717 [PMID:28858765] |
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]
