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TargetCyclin-dependent kinase 8
LigandBDBM50163854
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1572641
IC50 2.1±n/a nM
Citation Mallinger ASchiemann KRink CStieber FCalderini MCrumpler SStubbs MAdeniji-Popoola OPoeschke OBusch MCzodrowski PMusil DSchwarz DOrtiz-Ruiz MJSchneider RThai CValenti Mde Haven Brandon ABurke RWorkman PDale TWienke DClarke PAEsdar CRaynaud FIEccles SARohdich FBlagg J Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. J Med Chem 59:1078-101 (2016) [PubMed]
More Info.:Get all data from this article,  Assay Method
 
Cyclin-dependent kinase 8
Name:Cyclin-dependent kinase 8
Synonyms:CDK8 | Cell division protein kinase 8 | Cyclin-Dependent Kinase 8 (CDK8) | Mediator complex subunit CDK8 | Mediator of RNA polymerase II transcription subunit CDK8 | Protein kinase K35
Type:Serine/threonine-protein kinase
Mol. Mass.:53300.21
Organism:Homo sapiens (Human)
Description:P49336
Residue:464
Sequence:
MDYDFKVKLSSERERVEDLFEYEGCKVGRGTYGHVYKAKRKDGKDDKDYALKQIEGTGIS
MSACREIALLRELKHPNVISLQKVFLSHADRKVWLLFDYAEHDLWHIIKFHRASKANKKP
VQLPRGMVKSLLYQILDGIHYLHANWVLHRDLKPANILVMGEGPERGRVKIADMGFARLF
NSPLKPLADLDPVVVTFWYRAPELLLGARHYTKAIDIWAIGCIFAELLTSEPIFHCRQED
IKTSNPYHHDQLDRIFNVMGFPADKDWEDIKKMPEHSTLMKDFRRNTYTNCSLIKYMEKH
KVKPDSKAFHLLQKLLTMDPIKRITSEQAMQDPYFLEDPLPTSDVFAGCQIPYPKREFLT
EEEPDDKGDKKNQQQQQGNNHTNGTGHPGNQDSSHTQGPPLKKVRVVPPTTTSGGLIMTS
DYQRSNPHAAYPNPGPSTSQPQSSMGYSATSQQPPQYSHQTHRY
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  Blast E-value cutoff:
BDBM50163854
n/a
NameBDBM50163854
Synonyms:CHEMBL3799581
TypeSmall organic molecule
Emp. Form.C20H22ClN7O
Mol. Mass.411.888
SMILESNc1n[nH]c2cc(ccc12)-c1cnc(N)c(Cl)c1N1CCC2(CCNC2=O)CC1
Structure
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