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Target
Cyclin-C/Cyclin-dependent kinase 8
Ligand
BDBM50250180
Substrate
n/a
Meas. Tech.
ChEMBL_1681138 (CHEMBL4031415)
IC50
48±n/a nM
Citation
 Wang, A; Li, X; Chen, C; Wu, H; Qi, Z; Hu, C; Yu, K; Wu, J; Liu, J; Liu, X; Hu, Z; Wang, W; Wang, W; Wang, W; Wang, L; Wang, B; Liu, Q; Li, L; Ge, J; Ren, T; Zhang, S; Xia, R; Liu, J; Liu, Q Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutants in FLT3-ITD Positive AML. J Med Chem 60:8407-8424 (2017) [PubMed]  Article 
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:
BDBM50250180
Synonyms:
CHEMBL4101411
Type:
Small organic molecule
Emp. Form.:
C31H35N9O4
Mol. Mass.:
597.6675
SMILES:
CC(C)(C)c1cc(NC(=O)Nc2ccc(cc2)-n2nc(-c3ccc(OCCN4CCOCC4)cc3)c3c(N)ncnc23)no1
Structure:
Search PDB for entries with ligand similarity: