Reaction Details |
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Target | Cyclin-dependent kinase 8 |
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Ligand | BDBM50191357 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1613022 (CHEMBL3854822) |
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IC50 | 8.0±n/a nM |
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Citation | Czodrowski, P; Mallinger, A; Wienke, D; Esdar, C; Pöschke, O; Busch, M; Rohdich, F; Eccles, SA; Ortiz-Ruiz, MJ; Schneider, R; Raynaud, FI; Clarke, PA; Musil, D; Schwarz, D; Dale, T; Urbahns, K; Blagg, J; Schiemann, K Structure-Based Optimization of Potent, Selective, and Orally Bioavailable CDK8 Inhibitors Discovered by High-Throughput Screening. J Med Chem59:9337-9349 (2016) [PubMed] |
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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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BDBM50191357 |
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n/a |
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Name | BDBM50191357 |
Synonyms: | CHEMBL3903492 |
Type | Small organic molecule |
Emp. Form. | C18H17ClN4O |
Mol. Mass. | 340.807 |
SMILES | Cc1n[nH]c2ncc(cc12)C(=O)N1CCC[C@H]1c1ccc(Cl)cc1 |r| |
Structure |
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