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Target
Cyclin-dependent kinase 8
Ligand
BDBM50191472
Substrate
n/a
Meas. Tech.
ChEMBL_1613002 (CHEMBL3854802)
IC50
0.600000±n/a nM
Citation
 Czodrowski, P; Mallinger, A; Wienke, D; Esdar, C; Pöschke, O; Busch, M; Rohdich, F; Eccles, SA; Ortiz-Ruiz, MJ; Schneider, R; Raynaud, FI; Clarke, PA; Musil, D; Schwarz, D; Dale, T; Urbahns, K; Blagg, J; Schiemann, K Structure-Based Optimization of Potent, Selective, and Orally Bioavailable CDK8 Inhibitors Discovered by High-Throughput Screening. J Med Chem 59:9337-9349 (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:
BDBM50191472
Synonyms:
CHEMBL3956719
Type:
Small organic molecule
Emp. Form.:
C19H18ClN3O
Mol. Mass.:
339.819
SMILES:
Cc1n[nH]c2ccc(cc12)C(=O)N1CCC[C@H]1c1ccc(Cl)cc1 |r|
Structure:
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