| Reaction Details |
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 | Report a problem with these data |
| Target | Cyclin-C/Cyclin-dependent kinase 8 |
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| Ligand | BDBM640349 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | Recombinant CDK8 Protein-Cyclin C Complex In Vitro |
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| IC50 | 1.44±n/a nM |
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| Citation |  Mindich, AL; Chestnova, AJ; Kasatkina, MA; Alafinov, AI; Gavrilov, AS; Evdokimov, AA; Lenshmidt, LV; Maksimenko, EA; Mishina, MS; Silonov, SA; Smirnov, EJ; Iakovlev, PA; Morozov, DV CDK8/19 inhibitors US Patent US11840531 Publication Date 12/12/2023 |
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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 |
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| Synonyms: | CDK8/Cyclin C |
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| Type: | n/a |
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| Mol. Mass.: | n/a |
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| Description: | ASSAY_ID of ChEMBL is 1562017 |
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| Components: | This complex has 2 components. |
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| Component 1 |
| Name: | Cyclin-dependent kinase 8 |
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| 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 |
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| Type: | Serine/threonine-protein kinase |
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| Mol. Mass.: | 53300.21 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P49336 |
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| Residue: | 464 |
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| Sequence: | MDYDFKVKLSSERERVEDLFEYEGCKVGRGTYGHVYKAKRKDGKDDKDYALKQIEGTGIS
MSACREIALLRELKHPNVISLQKVFLSHADRKVWLLFDYAEHDLWHIIKFHRASKANKKP
VQLPRGMVKSLLYQILDGIHYLHANWVLHRDLKPANILVMGEGPERGRVKIADMGFARLF
NSPLKPLADLDPVVVTFWYRAPELLLGARHYTKAIDIWAIGCIFAELLTSEPIFHCRQED
IKTSNPYHHDQLDRIFNVMGFPADKDWEDIKKMPEHSTLMKDFRRNTYTNCSLIKYMEKH
KVKPDSKAFHLLQKLLTMDPIKRITSEQAMQDPYFLEDPLPTSDVFAGCQIPYPKREFLT
EEEPDDKGDKKNQQQQQGNNHTNGTGHPGNQDSSHTQGPPLKKVRVVPPTTTSGGLIMTS
DYQRSNPHAAYPNPGPSTSQPQSSMGYSATSQQPPQYSHQTHRY
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| Component 2 |
| Name: | Cyclin-C |
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| Synonyms: | CCNC | CCNC_HUMAN | Cyclin C | SRB11 homolog | hSRB11 |
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| Type: | PROTEIN |
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| Mol. Mass.: | 33244.88 |
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| Organism: | Homo sapiens (Human) |
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| Description: | ChEMBL_107900 |
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| Residue: | 283 |
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| Sequence: | MAGNFWQSSHYLQWILDKQDLLKERQKDLKFLSEEEYWKLQIFFTNVIQALGEHLKLRQQ
VIATATVYFKRFYARYSLKSIDPVLMAPTCVFLASKVEEFGVVSNTRLIAAATSVLKTRF
SYAFPKEFPYRMNHILECEFYLLELMDCCLIVYHPYRPLLQYVQDMGQEDMLLPLAWRIV
NDTYRTDLCLLYPPFMIALACLHVACVVQQKDARQWFAELSVDMEKILEIIRVILKLYEQ
WKNFDERKEMATILSKMPKPKPPPNSEGEQGPNGSQNSSYSQS
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| BDBM640349 |
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| n/a |
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| Name | BDBM640349 |
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| Synonyms: | (8-amino-5-(4-(1-(2-methoxyethyl)- 1H-pyrazole-4-yl)phenyl)-1,7- naphthyridin-3-yl)(4-methylpiperazine- 1-yl)methanone | US11840531, Compound 3.51 |
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| Type | Small organic molecule |
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| Emp. Form. | C26H29N7O2 |
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| Mol. Mass. | 471.5542 |
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| SMILES | COCCn1cc(cn1)-c1ccc(cc1)-c1cnc(N)c2ncc(cc12)C(=O)N1CCN(C)CC1 |
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| Structure | 
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