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Target
Cyclin-dependent kinase 8
Ligand
BDBM50459995
Substrate
n/a
Meas. Tech.
ChEMBL_1910725 (CHEMBL4413171)
IC50
4.4±n/a nM
Citation
 Xi, M; Chen, T; Wu, C; Gao, X; Wu, Y; Luo, X; Du, K; Yu, L; Cai, T; Shen, R; Sun, H CDK8 as a therapeutic target for cancers and recent developments in discovery of CDK8 inhibitors. Eur J Med Chem 164:77-91 (2019) [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:
BDBM50459995
Synonyms:
CHEMBL4225966 | US11471446, Compound DBA-10
Type:
Small organic molecule
Emp. Form.:
C15H18Br2N4
Mol. Mass.:
414.138
SMILES:
Cc1c(Br)c(Br)c2CCCn3c(nc1c23)N1CCNCC1
Structure:
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