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Target
Cyclin-dependent kinase 2/G1/S-specific cyclin-E1
Ligand
BDBM59228
Substrate
n/a
Meas. Tech.
In Vitro Kinase Assay
IC50
7±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 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:
MENFQKVEKIGEGTYGVVYKARNKLTGEVVALKKIRLDTETEGVPSTAIREISLLKELNHPNIVKLLDVIHTENKLYLVFEFLHQDLKKFMDASALTGIPLPLIKSYLFQLLQGLAFCHSHRVLHRDLKPQNLLINTEGAIKLADFGLARAFGVPVRTYTHEVVTLWYRAPEILLGCKYYSTAVDIWSLGCIFAEMVTRRALFPGDSEIDQLFRIFRTLGTPDEVVWPGVTSMPDYKPSFPKWARQDFSKVVPPLDEDGRSLLSQMLHYDPNKRISAKAALAHPFFQDVTKPVPHLRL
  
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:
BDBM59228
Synonyms:
Pyrazolopyrimidone analog, RGB-285940
Type:
Small organic molecule
Emp. Form.:
C22H19Cl3N4O2
Mol. Mass.:
477.771
SMILES:
COc1ccc(Cc2nc3n(nc(C(C)C)c3c(=O)[nH]2)-c2c(Cl)cc(Cl)cc2Cl)cc1 |(-14.46,2.58,;-13.13,3.35,;-11.8,2.58,;-11.8,1.04,;-10.46,.27,;-9.13,1.04,;-7.8,.27,;-6.46,1.04,;-5.13,.27,;-3.79,1.04,;-2.33,.57,;-1.43,1.81,;-2.33,3.06,;-1.56,4.39,;-2.33,5.73,;-.02,4.39,;-3.79,2.58,;-5.13,3.35,;-5.13,4.89,;-6.46,2.58,;-1.93,-.92,;-.44,-1.32,;.64,-.23,;-.05,-2.8,;-1.13,-3.89,;-.74,-5.38,;-2.62,-3.49,;-3.02,-2.01,;-4.51,-1.61,;-9.13,2.58,;-10.46,3.35,)|
Structure:
Search PDB for entries with ligand similarity: