Synonyms: PHA408
Compound class:
Synthetic organic
Comment: PHA-408 is a selective, ATP-competitive inhibitor of Iκβ kinase β (IKKβ a.k.a. IKK-2; gene symbol IKBKB) [1-2], a drug target for asthma, chronic obstructive pulmonary disease (COPD) and arthritis.
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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References |
1. Mbalaviele G, Sommers CD, Bonar SL, Mathialagan S, Schindler JF, Guzova JA, Shaffer AF, Melton MA, Christine LJ, Tripp CS et al.. (2009)
A novel, highly selective, tight binding IkappaB kinase-2 (IKK-2) inhibitor: a tool to correlate IKK-2 activity to the fate and functions of the components of the nuclear factor-kappaB pathway in arthritis-relevant cells and animal models. J Pharmacol Exp Ther, 329 (1): 14-25. [PMID:19168710] |
2. Xie J, Poda GI, Hu Y, Chen NX, Heier RF, Wolfson SG, Reding MT, Lennon PJ, Kurumbail RG, Selness SR et al.. (2011)
Aminopyridinecarboxamide-based inhaled IKK-2 inhibitors for asthma and COPD: Structure-activity relationship. Bioorg Med Chem, 19 (3): 1242-55. [PMID:21236687] |