Reaction Details |
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Target | Cyclin-dependent kinase 8 |
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Ligand | BDBM50163767 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1572641 (CHEMBL3803436) |
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IC50 | 1.6±n/a nM |
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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 |
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More Info.: | Get all data from this article, Assay Method |
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Cyclin-dependent kinase 8 |
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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
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BDBM50163767 |
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n/a |
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Name | BDBM50163767 |
Synonyms: | CHEMBL3798944 |
Type | Small organic molecule |
Emp. Form. | C26H30ClN5O2 |
Mol. Mass. | 480.002 |
SMILES | CC(C)(O)Cn1cc(cn1)-c1ccc(cc1)-c1cncc(Cl)c1N1CCC2(CCNC2=O)CC1 |
Structure |
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