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Target
Cyclin-dependent kinase 8
Ligand
BDBM50241864
Substrate
n/a
Meas. Tech.
ChEMBL_1670928 (CHEMBL4020957)
EC50
8.4±n/a nM
Citation
 Fujimoto, J; Hirayama, T; Hirata, Y; Hikichi, Y; Murai, S; Hasegawa, M; Hasegawa, Y; Yonemori, K; Hata, A; Aoyama, K; Cary, DR Studies of CDK 8/19 inhibitors: Discovery of novel and selective CDK8/19 dual inhibitors and elimination of their CYP3A4 time-dependent inhibition potential. Bioorg Med Chem 25:3018-3033 (2017) [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:
BDBM50241864
Synonyms:
CHEMBL4069244
Type:
Small organic molecule
Emp. Form.:
C23H22F3N5O
Mol. Mass.:
441.4489
SMILES:
Cn1cc(cn1)-c1ccncc1\C=C\C(=O)Nc1ccc2CCN(CC(F)(F)F)Cc2c1
Structure:
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