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TargetCyclin-dependent kinase 8
LigandBDBM50155240
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1562015 (CHEMBL3779189)
IC50 27±n/a nM
Citation Schiemann, KMallinger, AWienke, DEsdar, CPoeschke, OBusch, MRohdich, FEccles, SASchneider, RRaynaud, FICzodrowski, PMusil, DSchwarz, DUrbahns, KBlagg, J Discovery of potent and selective CDK8 inhibitors from an HSP90 pharmacophore. Bioorg Med Chem Lett26:1443-51 (2016) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Cyclin-dependent kinase 8
Name:Cyclin-dependent kinase 8
Synonyms:CDK8 | CDK8_HUMAN | 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:
BDBM50155240
n/a
NameBDBM50155240
Synonyms:CHEMBL3775773
TypeSmall organic molecule
Emp. Form.C23H21F2N5O
Mol. Mass.421.4425
SMILESCn1cc(cn1)-c1ccc(Cc2n[nH]c3ccc(cc23)C(=O)N2CCC(F)(F)C2)cc1
Structure
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