Reaction Details |
| Report a problem with these data |
Target | Cyclin-dependent kinase 8 |
---|
Ligand | BDBM50163786 |
---|
Substrate/Competitor | n/a |
---|
Meas. Tech. | ChEMBL_1572641 (CHEMBL3803436) |
---|
IC50 | 5.5±n/a nM |
---|
Citation | Mallinger, A; Schiemann, K; Rink, C; Stieber, F; Calderini, M; Crumpler, S; Stubbs, M; Adeniji-Popoola, O; Poeschke, O; Busch, M; Czodrowski, P; Musil, D; Schwarz, D; Ortiz-Ruiz, MJ; Schneider, R; Thai, C; Valenti, M; de Haven Brandon, A; Burke, R; Workman, P; Dale, T; Wienke, D; Clarke, PA; Esdar, C; Raynaud, FI; Eccles, SA; Rohdich, F; Blagg, J Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. J Med Chem59:1078-101 (2016) [PubMed] Article |
---|
More Info.: | Get all data from this article, Assay Method |
---|
|
Cyclin-dependent kinase 8 |
---|
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: | MDYDFKVKLSSERERVEDLFEYEGCKVGRGTYGHVYKAKRKDGKDDKDYALKQIEGTGIS
MSACREIALLRELKHPNVISLQKVFLSHADRKVWLLFDYAEHDLWHIIKFHRASKANKKP
VQLPRGMVKSLLYQILDGIHYLHANWVLHRDLKPANILVMGEGPERGRVKIADMGFARLF
NSPLKPLADLDPVVVTFWYRAPELLLGARHYTKAIDIWAIGCIFAELLTSEPIFHCRQED
IKTSNPYHHDQLDRIFNVMGFPADKDWEDIKKMPEHSTLMKDFRRNTYTNCSLIKYMEKH
KVKPDSKAFHLLQKLLTMDPIKRITSEQAMQDPYFLEDPLPTSDVFAGCQIPYPKREFLT
EEEPDDKGDKKNQQQQQGNNHTNGTGHPGNQDSSHTQGPPLKKVRVVPPTTTSGGLIMTS
DYQRSNPHAAYPNPGPSTSQPQSSMGYSATSQQPPQYSHQTHRY
|
|
|
BDBM50163786 |
---|
n/a |
---|
Name | BDBM50163786 |
Synonyms: | CHEMBL3797656 |
Type | Small organic molecule |
Emp. Form. | C20H22FN5O4S |
Mol. Mass. | 447.483 |
SMILES | CN1c2ccc(cc2CS1(=O)=O)-c1cnc(N)c(F)c1N1CCC2(CNC(=O)O2)CC1 |
Structure |
|