Reaction Details Report a problem with these data
Target
Cyclin-dependent kinase 8
Ligand
BDBM50241868
Substrate
n/a
Meas. Tech.
ChEMBL_1670928 (CHEMBL4020957)
EC50
11±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:
BDBM50241868
Synonyms:
CHEMBL4092865
Type:
Small organic molecule
Emp. Form.:
C25H27N5O2
Mol. Mass.:
429.5142
SMILES:
O=C(Nc1ccc(CN2CCOCC2)cc1)\C=C\c1cnccc1-c1cnn(c1)C1CC1
Structure:
Search PDB for entries with ligand similarity: