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Target
Cyclin-A2 [171-432]/Cyclin-dependent kinase 2
Ligand
BDBM5594
Substrate
Histone H1
Meas. Tech.
Kinase Inhibition Assay
pH
7.5±n/a
Temperature
303.15±n/a K
IC50
34±8 nM
Citation
 Sayle, KL; Bentley, J; Boyle, FT; Calvert, AH; Cheng, Y; Curtin, NJ; Endicott, JA; Golding, BT; Hardcastle, IR; Jewsbury, P; Mesguiche, V; Newell, DR; Noble, ME; Parsons, RJ; Pratt, DJ; Wang, LZ; Griffin, RJ Structure-based design of 2-arylamino-4-cyclohexylmethyl-5-nitroso-6-aminopyrimidine inhibitors of cyclin-dependent kinases 1 and 2. Bioorg Med Chem Lett 13:3079-82 (2003) [PubMed]  Article 
Target
Name:
Cyclin-A2 [171-432]/Cyclin-dependent kinase 2
Synonyms:
CDK2/cyclin A3 | Cyclin-Dependent Kinase 2 (CDK2) | p33cdk2/cyclin A3
Type:
Protein Complex
Mol. Mass.:
n/a
Description:
Binary complex of CDK2-cyclin A3 was formed by adding cyclin A3 in slight molar excess to the CDK2 subunit and purified by Superdex 75 gel filtration chromatography.
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:
Cyclin-A2 [171-432]
Synonyms:
CCN1 | CCNA | CCNA2 | CCNA2_HUMAN | cyclin A2
Type:
Enzyme Subunit
Mol. Mass.:
30018.91
Organism:
Homo sapiens (Human)
Description:
cyclin A2 is a c-terminal cyclin A fragment encoding residues 171-432.
Residue:
262
Sequence:
SVNEVPDYHEDIHTYLREMEVKCKPKVGYMKKQPDITNSMRAILVDWLVEVGEEYKLQNETLHLAVNYIDRFLSSMSVLRGKLQLVGTAAMLLASKFEEIYPPEVAEFVYITDDTYTKKQVLRMEHLVLKVLTFDLAAPTVNQFLTQYFLHQQPANCKVESLAMFLGELSLIDADPYLKYLPSVIAGAAFHLALYTVTGQSWPESLIRKTGYTLESLKPCLMDLHQTYLKAPQHAQQSIREKYKNSKYHGVSLLNPPETLNL
  
Inhibitor
Name:
BDBM5594
Synonyms:
2-arylamino-pyrimidine deriv. 9d | 4-{[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino}benzamide | CHEMBL101801
Type:
Small organic molecule
Emp. Form.:
C18H22N6O3
Mol. Mass.:
370.4057
SMILES:
NC(=O)c1ccc(Nc2nc(N)c(N=O)c(OCC3CCCCC3)n2)cc1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Histone H1
Synonyms:
Sigma Type IIIS
Type:
Other Protein Type
Mol. Mass.:
358.43
Organism:
Bos taurus (bovine)
Description:
12.5 uM ATP as co-substrate.
Residue:
3
Sequence:
NA