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Compound class: Synthetic organic
Comment: Compound 20 is a type II inhibitor (binds in a DMG-out mode) of CDK8, with an improved selectivity profile compared to sorafenib . It is one of the compounds claimed in patent WO2015049325 .
Ligand Activity Visualisation Charts
These 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.✖
1. Bergeron P, Koehler M. (2015)
Therapeutic inhibitors of cdk8 and uses thereof.
Patent number: WO2015049325. Assignee: F. Hoffmann-La Roche Ag, Genentech, Inc.. Priority date: 03/10/2013. Publication date: 09/04/2015.
2. Bergeron P, Koehler MF, Blackwood EM, Bowman K, Clark K, Firestein R, Kiefer JR, Maskos K, McCleland ML, Orren L et al.. (2016)
Design and Development of a Series of Potent and Selective Type II Inhibitors of CDK8.
ACS Med Chem Lett, 7 (6): 595-600. [PMID:27326333]
3. Dale T, Clarke PA, Esdar C, Waalboer D, Adeniji-Popoola O, Ortiz-Ruiz MJ, Mallinger A, Samant RS, Czodrowski P, Musil D et al.. (2015)
A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.
Nat Chem Biol, 11 (12): 973-80. [PMID:26502155]