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ChEMBL ligand: CHEMBL2218759 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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P2X7/P2X purinoceptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4805] [GtoPdb: 484] [UniProtKB: Q99572] | ||||||||
ChEMBL | Displacement of [3H]-A804598 from human P2X7 expressed in human HEK293 cell membrane incubated for 1 hr by microplate scintillation counting method | B | 6.75 | pKi | 176 | nM | Ki | J Med Chem (2020) 63: 2074-2094 [PMID:31525963] |
ChEMBL | Displacement of [3H]-A804598 from human P2X7 expressed in human HEK293 cell membrane incubated for 1 hr by microplate scintillation counting method | B | 6.06 | pIC50 | 861.8 | nM | IC50 | J Med Chem (2020) 63: 2074-2094 [PMID:31525963] |
GtoPdb | - | - | 6.32 | pIC50 | 474 | nM | IC50 | J Med Chem (2020) 63: 2074-2094 [PMID:31525963] |
ChEMBL | Inhibition of human P2X7 expressed in human HEK293 cells assessed as reduction in BzATP-stimulated TO-PRO-3 incorporation preincubated with compound and TO-PRO-3 for 15 mins prior to BzATP addition and measured after 1 hr by Fluo-3AM dye based flow cytometry | B | 6.32 | pIC50 | 474 | nM | IC50 | J Med Chem (2020) 63: 2074-2094 [PMID:31525963] |
ChEMBL | SUPPLEMENTARY: Inhibition of human P2X7 receptor assessed as inhibition of ethidium bromide accumulation. Same assay as CHEMBL1103860 | B | 7.9 | pIC50 | 12.59 | nM | IC50 | Structure-activity relationship data for chemical series of antagonists of the P2X7 receptor (Supplementary Bioactivity Data for publication CHEMBL1157114) |
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]