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TargetCyclin-Dependent Kinase 9 (CDK9)
LigandBDBM50347388
Substrate/Competitorn/a
Meas. Tech.ChEMBL_755649
IC50 90±n/a nM
Citation Heathcote DAPatel HKroll SHHazel PPeriyasamy MAlikian MKanneganti SKJogalekar ASScheiper BBarbazanges MBlum ABrackow JSiwicka APace RDFuchter MJSnyder JPLiotta DCFreemont PSAboagye EOCoombes RCBarrett AGAli S A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. J Med Chem 53:8508-22 (2010) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Cyclin-Dependent Kinase 9 (CDK9)
Name:Cyclin-Dependent Kinase 9 (CDK9)
Synonyms:CDK9/ Cyclin-T1 | CDK9/CycT1 | CDK9/Cyclin T | CDK9/Cyclin T1 | Cyclin T1/dependent kinase 9
Type:Protein Complex
Mol. Mass.:n/a
Description:n/a
Components:This complex has 2 components.
Component 1
Name:Cyclin-T1
Synonyms:CycT | CycT1 | Cyclin T | Cyclin T1 | Cyclin-T
Type:Enzyme Subunit
Mol. Mass.:80712.40
Organism:Homo sapiens (Human)
Description:n/a
Residue:726
Sequence:
MEGERKNNNKRWYFTREQLENSPSRRFGVDPDKELSYRQQAANLLQDMGQRLNVSQLTIN
TAIVYMHRFYMIQSFTQFPGNSVAPAALFLAAKVEEQPKKLEHVIKVAHTCLHPQESLPD
TRSEAYLQQVQDLVILESIILQTLGFELTIDHPHTHVVKCTQLVRASKDLAQTSYFMATN
SLHLTTFSLQYTPPVVACVCIHLACKWSNWEIPVSTDGKHWWEYVDATVTLELLDELTHE
FLQILEKTPNRLKRIWNWRACEAAKKTKADDRGTDEKTSEQTILNMISQSSSDTTIAGLM
SMSTSTTSAVPSLPVSEESSSNLTSVEMLPGKRWLSSQPSFKLEPTQGHRTSENLALTGV
DHSLPQDGSNAFISQKQNSKSVPSAKVSLKEYRAKHAEELAAQKRQLENMEANVKSQYAY
AAQNLLSHHDSHSSVILKMPIEGSENPERPFLEKADKTALKMRIPVAGGDKAASSKPEEI
KMRIKVHAAADKHNSVEDSVTKSREHKEKHKTHPSNHHHHHNHHSHKHSHSQLPVGTGNK
RPGDPKHSSQTSNLAHKTYSLSSSFSSSSSTRKRGPSEETGGAVFDHPAKIAKSTKSSSL
NFSFPSLPTMGQMPGHSSDTSGLSFSQPSCKTRVPHSKLDKGPTGANGHNTTQTIDYQDT
VNMLHSLLSAQGVQPTQPTAFEFVRPYSDYLNPRSGGISSRSGNTDKPRPPPLPSEPPPP
LPPLPK
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Component 2
Name:Cyclin-dependent kinase 9
Synonyms:C-2K | CDC2L4 | CDK9 | 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:
MAKQYDSVECPFCDEVSKYEKLAKIGQGTFGEVFKARHRKTGQKVALKKVLMENEKEGFP
ITALREIKILQLLKHENVVNLIEICRTKASPYNRCKGSIYLVFDFCEHDLAGLLSNVLVK
FTLSEIKRVMQMLLNGLYYIHRNKILHRDMKAANVLITRDGVLKLADFGLARAFSLAKNS
QPNRYTNRVVTLWYRPPELLLGERDYGPPIDLWGAGCIMAEMWTRSPIMQGNTEQHQLAL
ISQLCGSITPEVWPNVDNYELYEKLELVKGQKRKVKDRLKAYVRDPYALDLIDKLLVLDP
AQRIDSDDALNHDFFWSDPMPSDLKGMLSTHLTSMFEYLAPPRRKGSQITQQSTNQSRNP
ATTNQTEFERVF
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BDBM50347388
n/a
NameBDBM50347388
Synonyms:CHEMBL1234833
TypeSmall organic molecule
Emp. Form.C20H27N5O3
Mol. Mass.385.4601
SMILESCC(C)c1cnn2c(NCc3ccccc3)cc(N[C@@H](CO)[C@H](O)CO)nc12 |r|
Structure
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