PHA-408 [Ligand Id: 9398] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL592893 (PHA-408)
  • component of inhibitor of nuclear factor kappa B kinase complex/Inhibitor of nuclear factor kappa B kinase alpha subunit in Human [ChEMBL: CHEMBL3476] [GtoPdb: 1989] [UniProtKB: O15111]
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  • inhibitor of nuclear factor kappa B kinase subunit beta/Inhibitor of nuclear factor kappa B kinase beta subunit in Human [ChEMBL: CHEMBL1991] [GtoPdb: 2039] [UniProtKB: O14920]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
component of inhibitor of nuclear factor kappa B kinase complex/Inhibitor of nuclear factor kappa B kinase alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3476] [GtoPdb: 1989] [UniProtKB: O15111]
GtoPdb - - 4.85 pIC50 14100 nM IC50 J Pharmacol Exp Ther (2009) 329: 14-25 [PMID:19168710]
ChEMBL Inhibition of IKK1 B 4.85 pIC50 14000 nM IC50 Bioorg Med Chem (2010) 18: 403-414 [PMID:19914076]
inhibitor of nuclear factor kappa B kinase subunit beta/Inhibitor of nuclear factor kappa B kinase beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1991] [GtoPdb: 2039] [UniProtKB: O14920]
ChEMBL Inhibition of human recombinant C-terminal FLAG-epitope-tagged IKK2 expressed in baculovirus using biotinylated IkappaBalpha peptide as substrate assessed as decrease in [gamma-33P]-ATP incorporation in substrate after 30 mins by scintillation counting method B 6 pIC50 <=1000 nM IC50 EP-1501805-A1. Substituted pyrazolyl compounds for the treatment of inflammation (2005)
GtoPdb - - 7.4 pIC50 40 nM IC50 J Pharmacol Exp Ther (2009) 329: 14-25 [PMID:19168710]
ChEMBL Inhibition of human recombinant IKK2-mediated transfer of [gamma33P]ATP to biotinylated IkappaBalpha after 30 mins by scintillation counting B 7.6 pIC50 25 nM IC50 Bioorg Med Chem (2010) 18: 403-414 [PMID:19914076]
ChEMBL Inhibition of human recombinant IKK2 in human PBMC B 8.8 pIC50 1.6 nM IC50 Bioorg Med Chem (2011) 19: 1242-1255 [PMID:21236687]

ChEMBL data shown on this page come from version 32:

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]