Reaction Details Report a problem with these data
Target
Cyclin-dependent kinase 8
Ligand
BDBM50532619
Substrate
n/a
Meas. Tech.
ChEMBL_1923386 (CHEMBL4426342)
IC50
4000±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:
BDBM50532619
Synonyms:
CHEMBL4568245
Type:
Small organic molecule
Emp. Form.:
C24H33F3N8O
Mol. Mass.:
506.567
SMILES:
CCN1CCN(Cc2ccc(NC(=O)N[C@H]3CCN(C3)c3ccnc(NC)n3)cc2C(F)(F)F)CC1 |r|
Structure:
Search PDB for entries with ligand similarity: