Target
Cyclin-dependent kinase 9
Ligand
BDBM164883
Substrate
n/a
Meas. Tech.
ChEMBL_2025113 (CHEMBL4678926)
EC50
220±n/a nM
Citation
 Barlaam, BCasella, RCidado, JCook, CDe Savi, CDishington, ADonald, CSDrew, LFerguson, ADFerguson, DGlossop, SGrebe, TGu, CHande, SHawkins, JHird, AWHolmes, JHorstick, JJiang, YLamb, MLMcGuire, TMMoore, JEO'Connell, NPike, APike, KGProia, TRoberts, BSan Martin, MSarkar, UShao, WStead, DSumner, NThakur, KVasbinder, MMVarnes, JGWang, JWang, LWu, DWu, LYang, BYao, T Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies. J Med Chem 63:15564-15590 (2020) [PubMed]  Article 
Target
Name:
Cyclin-dependent kinase 9
Synonyms:
C-2K | CDC2L4 | CDK9 | CDK9_HUMAN | Cell division cycle 2-like protein kinase 4 | Cell division protein kinase 9 | Cyclin-Dependent Kinase 9 (CDK9) | Cyclin-dependent kinase 9 (CDK9) | Serine/threonine-protein kinase PITALRE | TAK | Tat-associated kinase complex catalytic subunit
Type:
Enzyme Subunit
Mol. Mass.:
42789.13
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
372
Sequence:
MAKQYDSVECPFCDEVSKYEKLAKIGQGTFGEVFKARHRKTGQKVALKKVLMENEKEGFPITALREIKILQLLKHENVVNLIEICRTKASPYNRCKGSIYLVFDFCEHDLAGLLSNVLVKFTLSEIKRVMQMLLNGLYYIHRNKILHRDMKAANVLITRDGVLKLADFGLARAFSLAKNSQPNRYTNRVVTLWYRPPELLLGERDYGPPIDLWGAGCIMAEMWTRSPIMQGNTEQHQLALISQLCGSITPEVWPNVDNYELYEKLELVKGQKRKVKDRLKAYVRDPYALDLIDKLLVLDPAQRIDSDDALNHDFFWSDPMPSDLKGMLSTHLTSMFEYLAPPRRKGSQITQQSTNQSRNPATTNQTEFERVF
  
Inhibitor
Name:
BDBM164883
Synonyms:
US9067888, 33
Type:
Small organic molecule
Emp. Form.:
C21H24FN3O3
Mol. Mass.:
385.432
SMILES:
COc1cc(F)ccc1-c1ccnc(NC(=O)[C@H]2CCC[C@H](C2)NC(C)=O)c1 |r|
Structure:
Search PDB for entries with ligand similarity: