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Target
Cyclin-dependent kinase 8
Ligand
BDBM50532627
Substrate
n/a
Meas. Tech.
ChEMBL_1923386 (CHEMBL4426342)
IC50
4200±n/a nM
Citation
 Bergeron, P; Koehler, MF; Blackwood, EM; Bowman, K; Clark, K; Firestein, R; Kiefer, JR; Maskos, K; McCleland, ML; Orren, L; Ramaswamy, S; Salphati, L; Schmidt, S; Schneider, EV; Wu, J; Beresini, M Design and Development of a Series of Potent and Selective Type II Inhibitors of CDK8. ACS Med Chem Lett 7:595-600 (2016) [PubMed]  Article 
Target
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:
MDYDFKVKLSSERERVEDLFEYEGCKVGRGTYGHVYKAKRKDGKDDKDYALKQIEGTGISMSACREIALLRELKHPNVISLQKVFLSHADRKVWLLFDYAEHDLWHIIKFHRASKANKKPVQLPRGMVKSLLYQILDGIHYLHANWVLHRDLKPANILVMGEGPERGRVKIADMGFARLFNSPLKPLADLDPVVVTFWYRAPELLLGARHYTKAIDIWAIGCIFAELLTSEPIFHCRQEDIKTSNPYHHDQLDRIFNVMGFPADKDWEDIKKMPEHSTLMKDFRRNTYTNCSLIKYMEKHKVKPDSKAFHLLQKLLTMDPIKRITSEQAMQDPYFLEDPLPTSDVFAGCQIPYPKREFLTEEEPDDKGDKKNQQQQQGNNHTNGTGHPGNQDSSHTQGPPLKKVRVVPPTTTSGGLIMTSDYQRSNPHAAYPNPGPSTSQPQSSMGYSATSQQPPQYSHQTHRY
  
Inhibitor
Name:
BDBM50532627
Synonyms:
CHEMBL4514427
Type:
Small organic molecule
Emp. Form.:
C23H31F3N8O
Mol. Mass.:
492.5404
SMILES:
CNc1nccc(n1)N1CC[C@@H](C1)NC(=O)Nc1ccc(CN2CCN(C)CC2)c(c1)C(F)(F)F |r|
Structure:
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