Reaction Details Report a problem with these data
Target
Cyclin-A2/Cyclin-dependent kinase 2
Ligand
BDBM11444
Substrate
Histone H1
Meas. Tech.
CDK Inhibition Assay
pH
7.5±n/a
Temperature
295.15±n/a K
IC50
1800±n/a nM
Citation
 Richardson, CM; Williamson, DS; Parratt, MJ; Borgognoni, J; Cansfield, AD; Dokurno, P; Francis, GL; Howes, R; Moore, JD; Murray, JB; Robertson, A; Surgenor, AE; Torrance, CJ Triazolo[1,5-a]pyrimidines as novel CDK2 inhibitors: protein structure-guided design and SAR. Bioorg Med Chem Lett 16:1353-7 (2006) [PubMed]  Article 
Target
Name:
Cyclin-A2/Cyclin-dependent kinase 2
Synonyms:
CDK2-CyclinA | CDK2/A | CDK2/Cyclin A | CDK2/Cyclin A2 | Cyclin A2/dependent kinase 2 | Cyclin-Dependent Kinase 2 (CDK2) | Cyclin-Dependent Kinase 2 (CDK2A)
Type:
Protein Complex
Mol. Mass.:
n/a
Description:
Cdk2/Cyclin A kinase was purified from insect cells coinfected with Cyclin A/Cdk2 baculovirus.
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
Synonyms:
CCN1 | CCNA | CCNA1 | CCNA2 | CCNA2_HUMAN | Cyclin A | Cyclin-A
Type:
Enzyme Subunit
Mol. Mass.:
48550.19
Organism:
Homo sapiens (Human)
Description:
P20248
Residue:
432
Sequence:
MLGNSAPGPATREAGSALLALQQTALQEDQENINPEKAAPVQQPRTRAALAVLKSGNPRGLAQQQRPKTRRVAPLKDLPVNDEHVTVPPWKANSKQPAFTIHVDEAEKEAQKKPAESQKIEREDALAFNSAISLPGPRKPLVPLDYPMDGSFESPHTMDMSIILEDEKPVSVNEVPDYHEDIHTYLREMEVKCKPKVGYMKKQPDITNSMRAILVDWLVEVGEEYKLQNETLHLAVNYIDRFLSSMSVLRGKLQLVGTAAMLLASKFEEIYPPEVAEFVYITDDTYTKKQVLRMEHLVLKVLTFDLAAPTVNQFLTQYFLHQQPANCKVESLAMFLGELSLIDADPYLKYLPSVIAGAAFHLALYTVTGQSWPESLIRKTGYTLESLKPCLMDLHQTYLKAPQHAQQSIREKYKNSKYHGVSLLNPPETLNL
  
Inhibitor
Name:
BDBM11444
Synonyms:
5-(3-bromophenyl)-N-(pyridin-4-ylmethyl)pyrazolo[1,5-a]pyrimidin-7-amine | pyrazolo[1,5-a]pyrimidine 2 | pyrazolo[1,5-a]pyrimidine 4
Type:
Small Organic Molecule
Emp. Form.:
C18H14BrN5
Mol. Mass.:
380.241
SMILES:
Brc1cccc(c1)-c1cc(NCc2ccncc2)n2nccc2n1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Histone H1
Synonyms:
n/a
Type:
Other Protein Type
Mol. Mass.:
358.43
Organism:
Bos taurus (bovine)
Description:
n/a
Residue:
3
Sequence:
NA