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 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]
