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TargetCyclin-dependent kinase 8
LigandBDBM50163774
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1572641
IC50 1.7±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 Chem59:1078-101 (2016) [PubMed]  Article
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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50163774
NameBDBM50163774
Synonyms:CHEMBL3797855
TypeSmall organic molecule
Emp. Form.C20H21ClN6O
Mol. Mass.396.873
SMILESNc1n[nH]c2cc(ccc12)-c1cncc(Cl)c1N1CCC2(CCNC2=O)CC1
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least:
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