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Cyclin-dependent kinase 2/G1/S-specific cyclin-E1
Ligand
BDBM50521930
Substrate
n/a
Meas. Tech.
ChEMBL_1885555 (CHEMBL4387137)
Ki
15000±n/a nM
Citation
Bronner, SM; Merrick, KA; Murray, J; Salphati, L; Moffat, JG; Pang, J; Sneeringer, CJ; Dompe, N; Cyr, P; Purkey, H; Boenig, GL; Li, J; Kolesnikov, A; Larouche-Gauthier, R; Lai, KW; Shen, X; Aubert-Nicol, S; Chen, YC; Cheong, J; Crawford, JJ; Hafner, M; Haghshenas, P; Jakalian, A; Leclerc, JP; Lim, NK; O'Brien, T; Plise, EG; Shalan, H; Sturino, C; Wai, J; Xiao, Y; Yin, J; Zhao, L; Gould, S; Olivero, A; Heffron, TP Design of a brain-penetrant CDK4/6 inhibitor for glioblastoma. Bioorg Med Chem Lett 29:2294-2301 (2019) [PubMed] ArticleMore Info.:
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:
BDBM50521930
Synonyms:
CHEMBL4447396
Type:
Small organic molecule
Emp. Form.:
C21H26N8
Mol. Mass.:
390.4847
SMILES:
CN1CCN(CC1)c1ccc(Nc2nccc(n2)-c2cnn3CCCCc23)nc1
Structure:
