BCL3 inhibitor JS6 [Ligand Id: 12672] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4558803
  • BCL3 transcription coactivator/B-cell lymphoma 3 protein in Human [ChEMBL: CHEMBL4523197] [GtoPdb: 3232] [UniProtKB: P20749]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
BCL3 transcription coactivator/B-cell lymphoma 3 protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523197] [GtoPdb: 3232] [UniProtKB: P20749]
ChEMBL Inhibition of FLAG-tagged Bcl-3 (unknown origin) expressed in HEK293 cells assessed as reduction in Bcl3 binding to its cognate protein partner NFKB1 (p50) incubated for 24 hrs by indirect sandwich ELISA B 6.41 pIC50 385.5 nM IC50 US-20160185740-A1. 2-benzoylaminobenzamide derivatives as bcl-3 inhibitors (null)
ChEMBL Inhibition of Bcl-3 (unknown origin) in HEK293 cells co-expressing p52 assessed as reduction in NF-kappaB signalling incubated for 24 hrs by NF-kappaB promoter dependent luciferase reporter gene assay B 6.68 pIC50 210.6 nM IC50 US-20160185740-A1. 2-benzoylaminobenzamide derivatives as bcl-3 inhibitors (null)
ChEMBL Inhibition of Bcl-3 (unknown origin) in HEK293 cells assessed as reduction in NF-kappaB signalling incubated for 24 hrs by NF-kappaB promoter dependent luciferase reporter gene assay B 6.81 pIC50 156.6 nM IC50 US-20160185740-A1. 2-benzoylaminobenzamide derivatives as bcl-3 inhibitors (null)
GtoPdb Inhibition of Bcl3-mediated NF-kappaB signalling in human MDA-MB-231 cells, using a NF-kappaB promoter dependent luciferase reporter gene assay - 7.34 pIC50 45.4 nM IC50 WO2015014972A1. 2-benzoylaminobenzamide derivatives as bcl-3 inhibitors (2015)
ChEMBL Inhibition of Bcl-3 in human MDA-MB-231 cells assessed as reduction in NF-kappaB signalling incubated for 24 hrs by NF-kappaB promoter dependent luciferase reporter gene assay B 7.34 pIC50 45.43 nM IC50 US-20160185740-A1. 2-benzoylaminobenzamide derivatives as bcl-3 inhibitors (null)

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]