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Target
Cyclin-dependent kinase 8
Ligand
BDBM50155238
Substrate
n/a
Meas. Tech.
ChEMBL_1562015 (CHEMBL3779189)
IC50
9.0±n/a nM
Citation
 Schiemann, K; Mallinger, A; Wienke, D; Esdar, C; Poeschke, O; Busch, M; Rohdich, F; Eccles, SA; Schneider, R; Raynaud, FI; Czodrowski, P; Musil, D; Schwarz, D; Urbahns, K; Blagg, J Discovery of potent and selective CDK8 inhibitors from an HSP90 pharmacophore. Bioorg Med Chem Lett 26:1443-51 (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:
BDBM50155238
Synonyms:
CHEMBL3774402
Type:
Small organic molecule
Emp. Form.:
C23H23N5O2
Mol. Mass.:
401.461
SMILES:
COC1CN(C1)C(=O)c1ccc2[nH]nc(Cc3ccc(cc3)-c3cnn(C)c3)c2c1
Structure:
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