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Target
Cyclin-dependent kinase 2/G1/S-specific cyclin-E1
Ligand
BDBM5445
Substrate
n/a
Meas. Tech.
ChEMBL_1746300 (CHEMBL4180810)
IC50
>20000±n/a nM
Citation
 Malínková, V; ?ezní?ková, E; Jorda, R; Gucký, T; Kry?tof, V Trisubstituted purine inhibitors of PDGFR? and their antileukemic activity in the human eosinophilic cell line EOL-1. Bioorg Med Chem 25:6523-6535 (2017) [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:
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:
Human
Description:
n/a
Residue:
410
Sequence:
MPRERRERDAKERDTMKEDGGAEFSARSRKRKANVTVFLQDPDEEMAKIDRTARDQCGSQPWDNNAVCADPCSLIPTPDKEDDDRVYPNSTCKPRIIAPSRGSPLPVLSWANREEVWKIMLNKEKTYLRDQHFLEQHPLLQPKMRAILLDWLMEVCEVYKLHRETFYLAQDFFDRYMATQENVVKTLLQLIGISSLFIAAKLEEIYPPKLHQFAYVTDGACSGDEILTMELMIMKALKWRLSPLTIVSWLNVYMQVAYLNDLHEVLLPQYPQQIFIQIAELLDLCVLDVDCLEFPYGILAASALYHFSSSELMQKVSGYQWCDIENCVKWMVPFAMVIRETGSSKLKHFRGVADEDAHNIQTHRDSLDLLDKARAKKAMLSEQNRASPLPSGLLTPPQSGKKQSSGPEMA
  
Inhibitor
Name:
BDBM5445
Synonyms:
CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapatinib | N-{3-chloro-4-[(3-fluoro-benzyl)oxy]phenyl}-6-[5-({2-(methylsulfonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine | N-{3-chloro-4-[(3-fluorophenyl)methoxy]phenyl}-6-(5-{[(2-methanesulfonylethyl)amino]methyl}furan-2-yl)quinazolin-4-amine | Tykerb | US10507209, Compound Lapatinib | US10822334, Compound Lapatinib | US9730934, Lapatinib ditosylate | cid_208908
Type:
Small organic molecule
Emp. Form.:
C29H26ClFN4O4S
Mol. Mass.:
581.058
SMILES:
CS(=O)(=O)CCNCc1ccc(o1)-c1ccc2ncnc(Nc3ccc(OCc4cccc(F)c4)c(Cl)c3)c2c1
Structure:
Search PDB for entries with ligand similarity: