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Target
Cyclin-dependent kinase 2/G1/S-specific cyclin-E1
Ligand
BDBM6859
Substrate
Rb(21)
Meas. Tech.
Kinase Inhibition Assay
pH
7±n/a
Temperature
295.15±n/a K
IC50
4300±n/a nM
Citation
 Zhu, G; Conner, SE; Zhou, X; Shih, C; Li, T; Anderson, BD; Brooks, HB; Campbell, RM; Considine, E; Dempsey, JA; Faul, MM; Ogg, C; Patel, B; Schultz, RM; Spencer, CD; Teicher, B; Watkins, SA Synthesis, structure-activity relationship, and biological studies of indolocarbazoles as potent cyclin D1-CDK4 inhibitors. J Med Chem 46:2027-30 (2003) [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:
BDBM6859
Synonyms:
7-bromo-3,13,23-triazahexacyclo[14.7.0.0^{2,10}.0^{4,9}.0^{11,15}.0^{17,22}]tricosa-1(16),2(10),4(9),5,7,11(15),17(22),18,20-nonaene-12,14-dione | Indolocarbazole deriv. 4(c)
Type:
Small Organic Molecule
Emp. Form.:
C20H10BrN3O2
Mol. Mass.:
404.216
SMILES:
Brc1ccc2[nH]c3c4[nH]c5ccccc5c4c4C(=O)NC(=O)c4c3c2c1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Rb(21)
Synonyms:
C-terminal retinoblastoma protein | RB1 | RB_HUMAN
Type:
Other Protein Type
Mol. Mass.:
17129.60
Organism:
Homo sapiens (Human)
Description:
Amino acids 769-921 of human retinoblastoma 1.
Residue:
153
Sequence:
LQYASTRPPTLSPIPHIPRSPYKFPSSPLRIPGGNIYISPLKSPYKISEGLPTPTKMTPRSRILVSIGESFGTSEKFQKINQMVCNSDRVLKRSAEGSNPPKPLKKLRFDIEGSDEADGSKHLPGESKFQQKLAEMTSTRTRMQKQKMNDSMD