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Target
Cyclin-C/Cyclin-dependent kinase 8
Ligand
BDBM640350
Substrate
n/a
Meas. Tech.
Recombinant CDK8 Protein-Cyclin C Complex In Vitro
IC50
0.960±n/a nM
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 
Target
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:
MDYDFKVKLSSERERVEDLFEYEGCKVGRGTYGHVYKAKRKDGKDDKDYALKQIEGTGISMSACREIALLRELKHPNVISLQKVFLSHADRKVWLLFDYAEHDLWHIIKFHRASKANKKPVQLPRGMVKSLLYQILDGIHYLHANWVLHRDLKPANILVMGEGPERGRVKIADMGFARLFNSPLKPLADLDPVVVTFWYRAPELLLGARHYTKAIDIWAIGCIFAELLTSEPIFHCRQEDIKTSNPYHHDQLDRIFNVMGFPADKDWEDIKKMPEHSTLMKDFRRNTYTNCSLIKYMEKHKVKPDSKAFHLLQKLLTMDPIKRITSEQAMQDPYFLEDPLPTSDVFAGCQIPYPKREFLTEEEPDDKGDKKNQQQQQGNNHTNGTGHPGNQDSSHTQGPPLKKVRVVPPTTTSGGLIMTSDYQRSNPHAAYPNPGPSTSQPQSSMGYSATSQQPPQYSHQTHRY
  
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:
MAGNFWQSSHYLQWILDKQDLLKERQKDLKFLSEEEYWKLQIFFTNVIQALGEHLKLRQQVIATATVYFKRFYARYSLKSIDPVLMAPTCVFLASKVEEFGVVSNTRLIAAATSVLKTRFSYAFPKEFPYRMNHILECEFYLLELMDCCLIVYHPYRPLLQYVQDMGQEDMLLPLAWRIVNDTYRTDLCLLYPPFMIALACLHVACVVQQKDARQWFAELSVDMEKILEIIRVILKLYEQWKNFDERKEMATILSKMPKPKPPPNSEGEQGPNGSQNSSYSQS
  
Inhibitor
Name:
BDBM640350
Synonyms:
2-(4-(4-(8-amino-3-(azetidine-1- carbonyl)-1,7-naphthyridine-5-yl) phenyl)-1H-pyrazole-1-yl)-N,N- dimethylacetamide | US11840531, Compound 3.52
Type:
Small organic molecule
Emp. Form.:
C25H25N7O2
Mol. Mass.:
455.5117
SMILES:
CN(C)C(=O)Cn1cc(cn1)-c1ccc(cc1)-c1cnc(N)c2ncc(cc12)C(=O)N1CCC1
Structure:
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