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Target
Cyclin-dependent kinase 8
Ligand
BDBM50189415
Substrate
n/a
Meas. Tech.
ChEMBL_1838810 (CHEMBL4338943)
IC50
0.900000±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:
BDBM50189415
Synonyms:
CHEMBL3828637
Type:
Small organic molecule
Emp. Form.:
C18H16N4O3S
Mol. Mass.:
368.41
SMILES:
CNC(=O)c1ccc2cncc(-c3ccc4N(C)S(=O)(=O)Cc4c3)c2n1
Structure:
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