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ChEMBL ligand: CHEMBL64130 (2-Acetylfuranonaphthoquinone, 2-acetylfuro-1,4-naphthoquinone, BBI-608, BBI608, Napabucasin) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Aldehyde dehydrogenase 1A1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3577] [UniProtKB: P00352] | ||||||||
ChEMBL | Inhibition of ALDH1A1 in human drug-tolerant MDA-MB-231/lapatinib cells assessed as after 24 hrs | B | 6.37 | pIC50 | 425.32 | nM | IC50 | J Med Chem (2021) 64: 12877-12892 [PMID:34435487] |
signal transducer and activator of transcription 3/Signal transducer and activator of transcription 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4026] [GtoPdb: 2994] [UniProtKB: P40763] | ||||||||
ChEMBL | Inhibition of IL-6 induced STAT3 transcriptional activity in human HEK293 cells expressing SIE-luc2P preincubated for overnight followed by IL-6 stimulation and measured after 24 hr by Bio-Glo luciferase reagent based microplate reader assay | B | 5.49 | pIC50 | 3200 | nM | IC50 | J Med Chem (2021) 64: 1626-1648 [PMID:33506674] |
ChEMBL | Inhibition of IL-6 induced STAT3 phosphorylation at Tyr705 residue in human MCF7 cells preincubated for 1 hr followed by IL-6 stimulation and measured after 1 hr by Western blot analysis | B | 6 | pIC50 | <1000 | nM | IC50 | Bioorg Med Chem (2020) 28: 115347-115347 [PMID:32044231] |
ChEMBL | Inhibition of STAT3 phosphorylation at Y705 in human MDA-MB-231 cells after 4 hrs by HTRF assay | B | 5.7 | pEC50 | 2000 | nM | EC50 | J Nat Prod (2018) 81: 1636-1644 [PMID:30003778] |
ChEMBL | Inhibition of STAT3 phosphorylation at Y705 in human MDA-MB-231 cells assessed as reduction in ratio of phosphorylated STAT3 to total STAT3 level after 4 hrs by HTRF assay | B | 5.72 | pEC50 | 1900 | nM | EC50 | J Nat Prod (2018) 81: 1636-1644 [PMID:30003778] |
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]