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Target
Cyclin-C/Cyclin-dependent kinase 8
Ligand
BDBM540063
Substrate
n/a
Meas. Tech.
CDK8 Biochemical Assay
IC50
1.30±n/a nM
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 
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:
BDBM540063
Synonyms:
US11261184, Example I-010
Type:
Small organic molecule
Emp. Form.:
C22H23ClN4O3
Mol. Mass.:
426.896
SMILES:
CN(CCO)C(=O)[C@H]1CCN(C1)c1ccc(Oc2ccnc3c(Cl)cncc23)cc1 |r|
Structure:
Search PDB for entries with ligand similarity: