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 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]