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TargetCyclin-dependent kinase 2/G1/S-specific cyclin-E1
LigandBDBM50347388
Substrate/Competitorn/a
Meas. Tech.ChEMBL_755644 (CHEMBL1805469)
IC50 3±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 Chem53:8508-22 (2010) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Cyclin-dependent kinase 2/G1/S-specific cyclin-E1
Name:Cyclin-dependent kinase 2/G1/S-specific cyclin-E1
Synonyms:CDK2/CycE | CDK2/Cyclin E | CDK2/E | CDK2/E1 | Cyclin-Dependent Kinase 2 (CDK2) | Cyclin-dependent kinase 2/G1/S-specific cyclin E1 | Cyclin-dependent kinase 2/cyclin E1
Type:Protein
Mol. Mass.:n/a
Description:n/a
Components:This complex has 2 components.
Component 1
Name:Cyclin-dependent kinase 2
Synonyms:CDK2 | CDK2-Kinase | CDK2_HUMAN | CDKN2 | Cell division protein kinase 2 | Cyclin-dependent kinase 2 (CDK2) | Protein cereblon/Cyclin-dependent kinase 2 | p33 protein kinase
Type:Enzyme Subunit
Mol. Mass.:33938.17
Organism:Homo sapiens (Human)
Description:P24941
Residue:298
Sequence:
MENFQKVEKIGEGTYGVVYKARNKLTGEVVALKKIRLDTETEGVPSTAIREISLLKELNH
PNIVKLLDVIHTENKLYLVFEFLHQDLKKFMDASALTGIPLPLIKSYLFQLLQGLAFCHS
HRVLHRDLKPQNLLINTEGAIKLADFGLARAFGVPVRTYTHEVVTLWYRAPEILLGCKYY
STAVDIWSLGCIFAEMVTRRALFPGDSEIDQLFRIFRTLGTPDEVVWPGVTSMPDYKPSF
PKWARQDFSKVVPPLDEDGRSLLSQMLHYDPNKRISAKAALAHPFFQDVTKPVPHLRL
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Component 2
Name:G1/S-specific cyclin-E1
Synonyms:CCNE | CCNE1 | CCNE1_HUMAN
Type:Enzyme Subunit
Mol. Mass.:47073.17
Organism:Homo sapiens (Human)
Description:n/a
Residue:410
Sequence:
MPRERRERDAKERDTMKEDGGAEFSARSRKRKANVTVFLQDPDEEMAKIDRTARDQCGSQ
PWDNNAVCADPCSLIPTPDKEDDDRVYPNSTCKPRIIAPSRGSPLPVLSWANREEVWKIM
LNKEKTYLRDQHFLEQHPLLQPKMRAILLDWLMEVCEVYKLHRETFYLAQDFFDRYMATQ
ENVVKTLLQLIGISSLFIAAKLEEIYPPKLHQFAYVTDGACSGDEILTMELMIMKALKWR
LSPLTIVSWLNVYMQVAYLNDLHEVLLPQYPQQIFIQIAELLDLCVLDVDCLEFPYGILA
ASALYHFSSSELMQKVSGYQWCDIENCVKWMVPFAMVIRETGSSKLKHFRGVADEDAHNI
QTHRDSLDLLDKARAKKAMLSEQNRASPLPSGLLTPPQSGKKQSSGPEMA
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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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