- Advanced search
- Immuno Portal
- Malaria Portal
Compound class: Synthetic organic
Comment: Compound 51 is a potent and selective CDK8/19 inhibitor . It is one of the compounds claimed in patent WO2016009076 . Compound 51 hasa similar inhibitory potency as CCT251545, but is built on a modified chemical scaffold . This is a type I inhibitor, binding in a DMG-in mode.
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. Firestein R, Bass AJ, Kim SY, Dunn IF, Silver SJ, Guney I, Freed E, Ligon AH, Vena N, Ogino S et al.. (2008)
CDK8 is a colorectal cancer oncogene that regulates beta-catenin activity.
Nature, 455 (7212): 547-51. [PMID:18794900]
2. Kapoor A, Goldberg MS, Cumberland LK, Ratnakumar K, Segura MF, Emanuel PO, Menendez S, Vardabasso C, Leroy G, Vidal CI et al.. (2010)
The histone variant macroH2A suppresses melanoma progression through regulation of CDK8.
Nature, 468 (7327): 1105-9. [PMID:21179167]
3. Mallinger A, Schiemann K, Rink C, Sejberg J, Honey MA, Czodrowski P, Stubbs M, Poeschke O, Busch M, Schneider R et al.. (2016)
2,8-Disubstituted-1,6-Naphthyridines and 4,6-Disubstituted-Isoquinolines with Potent, Selective Affinity for CDK8/19.
ACS Med Chem Lett, 7 (6): 573-8. [PMID:27326329]
4. Schiemann K, Blagg J, Mallinger A, Rink C, Sejberg J, Honey M. (2016)
Novel naphthryidines and isoquinolines and their use as cdk8/19 inhibitors.
Patent number: WO2016009076. Assignee: Merck Patent Gmbh, Cancer Research Technology Limited. Priority date: 17/07/2014. Publication date: 21/01/2016.