Target
Cyclin-A2 [171-432]/Cyclin-dependent kinase 2 [F82H,L83V,H84D]
Ligand
BDBM12082
Substrate
Histone H1
Meas. Tech.
CDK Inhibition Assay
pH
7.5±n/a
Temperature
303.15±n/a K
IC50
7300±n/a nM
Citation
 Pratt, DJBentley, JJewsbury, PBoyle, FTEndicott, JANoble, ME Dissecting the determinants of cyclin-dependent kinase 2 and cyclin-dependent kinase 4 inhibitor selectivity. J Med Chem 49:5470-7 (2006) [PubMed]  Article 
Target
Name:
Cyclin-A2 [171-432]/Cyclin-dependent kinase 2 [F82H,L83V,H84D]
Synonyms:
Cyclin-Dependent Kinase 2 (CDK2) Mutant (F82H/L83V/H84D)
Type:
Protein Complex
Mol. Mass.:
n/a
Description:
n/a
Components:
This complex has 2 components.
Component 1
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
  
Component 2
Name:
Cyclin-dependent kinase 2 [F82H,L83V,H84D]
Synonyms:
CDK2 | CDK2_HUMAN | CDKN2 | Cyclin-Dependent Kinase 2 (CDK2) Mutant (F82H/L83V/H84D)
Type:
Enzyme Subunit
Mol. Mass.:
33891.05
Organism:
Homo sapiens (Human)
Description:
P24941[F82H,L83V,H84D]
Residue:
298
Sequence:
MENFQKVEKIGEGTYGVVYKARNKLTGEVVALKKIRLDTETEGVPSTAIREISLLKELNHPNIVKLLDVIHTENKLYLVFEHVDQDLKKFMDASALTGIPLPLIKSYLFQLLQGLAFCHSHRVLHRDLKPQNLLINTEGAIKLADFGLARAFGVPVRTYTHEVVTLWYRAPEILLGCKYYSTAVDIWSLGCIFAEMVTRRALFPGDSEIDQLFRIFRTLGTPDEVVWPGVTSMPDYKPSFPKWARQDFSKVVPPLDEDGRSLLSQMLHYDPNKRISAKAALAHPFFQDVTKPVPHLRL
  
Inhibitor
Name:
BDBM12082
Synonyms:
((2-chloro-5-methyl-phenyl)-{6-[4-(3-(dimethylamino)-2-hydroxy-propoxy)-phenylamino]-pyrimidin-4-yl}-amino)-acetonitrile | 2-[(2-chloro-5-methylphenyl)[6-({4-[(2R)-3-(dimethylamino)-2-hydroxypropoxy]phenyl}amino)pyrimidin-4-yl]amino]acetonitrile | AZ2
Type:
Small organic molecule
Emp. Form.:
C24H27ClN6O2
Mol. Mass.:
466.963
SMILES:
CN(C)C[C@@H](O)COc1ccc(Nc2cc(ncn2)N(CC#N)c2cc(C)ccc2Cl)cc1 |r|
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