Reaction Details Report a problem with these data
Target
Cyclin-dependent kinase 8
Ligand
BDBM50509567
Substrate
n/a
Meas. Tech.
ChEMBL_1838813 (CHEMBL4338946)
Kd
0.770000±n/a nM
Citation
 Grandjean, JM; Jiu, AY; West, JW; Aoyagi, A; Droege, DG; Elepano, M; Hirasawa, M; Hirouchi, M; Murakami, R; Lee, J; Sasaki, K; Hirano, S; Ohyama, T; Tang, BC; Vaz, RJ; Inoue, M; Olson, SH; Prusiner, SB; Conrad, J; Paras, NA Discovery of 4-Piperazine Isoquinoline Derivatives as Potent and Brain-Permeable Tau Prion Inhibitors with CDK8 Activity. ACS Med Chem Lett 11:127-132 (2020) [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:
BDBM50509567
Synonyms:
CHEMBL4455382 | US11213520, Example I-003
Type:
Small organic molecule
Emp. Form.:
C22H20N4O
Mol. Mass.:
356.4204
SMILES:
CN(C)C(=O)Cn1cc(cn1)-c1ccc(cc1)-c1cncc2ccccc12
Structure:
Search PDB for entries with ligand similarity: