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Target
Cyclin-dependent kinase 3/G1/S-specific cyclin-E1
Ligand
BDBM59227
Substrate
n/a
Meas. Tech.
In Vitro Kinase Assay
IC50
9±n/a nM
Citation
 Caligiuri, M; Becker, F; Murthi, K; Kaplan, F; Dedier, S; Kaufmann, C; Machl, A; Zybarth, G; Richard, J; Bockovich, N; Kluge, A; Kley, N A proteome-wide CDK/CRK-specific kinase inhibitor promotes tumor cell death in the absence of cell cycle progression. Chem Biol 12:1103-15 (2005) [PubMed]  Article 
Target
Name:
Cyclin-dependent kinase 3/G1/S-specific cyclin-E1
Synonyms:
CDK3/Cyclin E | CDK3/E
Type:
Protein
Mol. Mass.:
n/a
Description:
n/a
Components:
This complex has 2 components.
Component 1
Name:
Cyclin-dependent kinase 3
Synonyms:
CDK3 | CDK3/Cyclin E | CDK3_HUMAN | CDKN3 | Cyclin-dependent kinase 3 | Cyclin-dependent kinase 3 (CDK3)
Type:
Enzyme
Mol. Mass.:
35053.88
Organism:
Homo sapiens (Human)
Description:
Q00526
Residue:
305
Sequence:
MDMFQKVEKIGEGTYGVVYKAKNRETGQLVALKKIRLDLEMEGVPSTAIREISLLKELKHPNIVRLLDVVHNERKLYLVFEFLSQDLKKYMDSTPGSELPLHLIKSYLFQLLQGVSFCHSHRVIHRDLKPQNLLINELGAIKLADFGLARAFGVPLRTYTHEVVTLWYRAPEILLGSKFYTTAVDIWSIGCIFAEMVTRKALFPGDSEIDQLFRIFRMLGTPSEDTWPGVTQLPDYKGSFPKWTRKGLEEIVPNLEPEGRDLLMQLLQYDPSQRITAKTALAHPYFSSPEPSPAARQYVLQRFRH
  
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:
MPRERRERDAKERDTMKEDGGAEFSARSRKRKANVTVFLQDPDEEMAKIDRTARDQCGSQPWDNNAVCADPCSLIPTPDKEDDDRVYPNSTCKPRIIAPSRGSPLPVLSWANREEVWKIMLNKEKTYLRDQHFLEQHPLLQPKMRAILLDWLMEVCEVYKLHRETFYLAQDFFDRYMATQENVVKTLLQLIGISSLFIAAKLEEIYPPKLHQFAYVTDGACSGDEILTMELMIMKALKWRLSPLTIVSWLNVYMQVAYLNDLHEVLLPQYPQQIFIQIAELLDLCVLDVDCLEFPYGILAASALYHFSSSELMQKVSGYQWCDIENCVKWMVPFAMVIRETGSSKLKHFRGVADEDAHNIQTHRDSLDLLDKARAKKAMLSEQNRASPLPSGLLTPPQSGKKQSSGPEMA
  
Inhibitor
Name:
BDBM59227
Synonyms:
Pyrazolopyrimidone analog, RGB-286147
Type:
Small organic molecule
Emp. Form.:
C23H22Cl2N4O3
Mol. Mass.:
473.352
SMILES:
CC(C)c1nn(-c2c(Cl)cccc2Cl)c2nc(Cc3ccc(OCCO)cc3)[nH]c(=O)c12 |(-2.33,5.73,;-1.56,4.39,;-.02,4.39,;-2.33,3.06,;-1.43,1.81,;-2.33,.57,;-1.93,-.92,;-.44,-1.32,;.64,-.23,;-.05,-2.8,;-1.13,-3.89,;-2.62,-3.49,;-3.02,-2.01,;-4.51,-1.61,;-3.79,1.04,;-5.13,.27,;-6.46,1.04,;-7.8,.27,;-9.13,1.04,;-10.46,.27,;-11.8,1.04,;-11.8,2.58,;-13.13,3.35,;-14.46,2.58,;-15.8,3.35,;-17.13,2.58,;-10.46,3.35,;-9.13,2.58,;-6.46,2.58,;-5.13,3.35,;-5.13,4.89,;-3.79,2.58,)|
Structure:
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