Reaction Details |
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Target | Cyclin-C/Cyclin-dependent kinase 8 |
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Ligand | BDBM540065 |
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Substrate/Competitor | n/a |
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Meas. Tech. | CDK8 Biochemical Assay |
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IC50 | 1.30±n/a nM |
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Citation | Engelhardt, H; Arnhof, H; Carotta, S; Hofmann, M; Kerenyi, M; Scharn, D [1,6]naphthyridine compounds and derivatives as CDK8/CDK19 inhibitors US Patent US11261184 Publication Date 3/1/2022 |
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More Info.: | Get all data from this article, Assay Method |
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Cyclin-C/Cyclin-dependent kinase 8 |
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Name: | Cyclin-C/Cyclin-dependent kinase 8 |
Synonyms: | CDK8/Cyclin C |
Type: | n/a |
Mol. Mass.: | n/a |
Description: | ASSAY_ID of ChEMBL is 1562017 |
Components: | This complex has 2 components. |
Component 1 |
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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Component 2 |
Name: | Cyclin-C |
Synonyms: | CCNC | CCNC_HUMAN | Cyclin C | SRB11 homolog | hSRB11 |
Type: | PROTEIN |
Mol. Mass.: | 33244.88 |
Organism: | Homo sapiens (Human) |
Description: | ChEMBL_107900 |
Residue: | 283 |
Sequence: | MAGNFWQSSHYLQWILDKQDLLKERQKDLKFLSEEEYWKLQIFFTNVIQALGEHLKLRQQ
VIATATVYFKRFYARYSLKSIDPVLMAPTCVFLASKVEEFGVVSNTRLIAAATSVLKTRF
SYAFPKEFPYRMNHILECEFYLLELMDCCLIVYHPYRPLLQYVQDMGQEDMLLPLAWRIV
NDTYRTDLCLLYPPFMIALACLHVACVVQQKDARQWFAELSVDMEKILEIIRVILKLYEQ
WKNFDERKEMATILSKMPKPKPPPNSEGEQGPNGSQNSSYSQS
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BDBM540065 |
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n/a |
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Name | BDBM540065 |
Synonyms: | US11261184, Example I-012 |
Type | Small organic molecule |
Emp. Form. | C24H26ClN5O2 |
Mol. Mass. | 451.949 |
SMILES | CN1CCN(CC1)C(=O)[C@H]1CCN(C1)c1ccc(Oc2ccnc3c(Cl)cncc23)cc1 |r| |
Structure |
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