Target
Cyclin-dependent kinase 8
Ligand
BDBM50163765
Substrate
n/a
Meas. Tech.
ChEMBL_1572641 (CHEMBL3803436)
IC50
3.8±n/a nM
Citation
 Mallinger, ASchiemann, KRink, CStieber, FCalderini, MCrumpler, SStubbs, MAdeniji-Popoola, OPoeschke, OBusch, MCzodrowski, PMusil, DSchwarz, DOrtiz-Ruiz, MJSchneider, RThai, CValenti, Mde Haven Brandon, ABurke, RWorkman, PDale, TWienke, DClarke, PAEsdar, CRaynaud, FIEccles, SARohdich, FBlagg, J Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. J Med Chem 59:1078-101 (2016) [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:
BDBM50163765
Synonyms:
CHEMBL3799116
Type:
Small organic molecule
Emp. Form.:
C21H23FN4O3S
Mol. Mass.:
430.496
SMILES:
CN1c2ccc(cc2CS1(=O)=O)-c1cncc(F)c1N1CCC2(CCNC2=O)CC1
Structure:
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