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TargetCyclin-Dependent Kinase 2 (CDK2)
LigandBDBM5485
Substrate/CompetitorHistone H1
Meas. Tech.Kinase Inhibition Assay
pH7.5±n/a
Temperature303.15±n/a K
Ki 12000±3000 nM
CommentsTo obtain Ki value, the assay was performed in the absence of inhibitor and at two fixed inhibitor concentrations, 25 and 50 uM, with ATP concentrations ranging from 6.25 to 800 uM. Data were fitted to the Michaelis-Menten equation using unweighted nonlinear least squares regression.
Citation Arris, CEBoyle, FTCalvert, AHCurtin, NJEndicott, JAGarman, EFGibson, AEGolding, BTGrant, SGriffin, RJJewsbury, PJohnson, LNLawrie, AMNewell, DRNoble, MESausville, EASchultz, RYu, W Identification of novel purine and pyrimidine cyclin-dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles. J Med Chem43:2797-804 (2000) [PubMed]  Article
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Cyclin-Dependent Kinase 2 (CDK2)
Name:Cyclin-Dependent Kinase 2 (CDK2)
Synonyms:CDK2/cyclin A3 | 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:CDK2/Bovine cyclin A
Synonyms:CDK2 | CDK2-Kinase | Cell division protein kinase 2 | Cyclin-dependent kinase 2 (CDK2) | p33 protein kinase
Type:Enzyme Subunit
Mol. Mass.:33938.17
Organism:Homo sapiens (Human)
Description:P24941
Residue:298
Sequence:
MENFQKVEKIGEGTYGVVYKARNKLTGEVVALKKIRLDTETEGVPSTAIREISLLKELNH
PNIVKLLDVIHTENKLYLVFEFLHQDLKKFMDASALTGIPLPLIKSYLFQLLQGLAFCHS
HRVLHRDLKPQNLLINTEGAIKLADFGLARAFGVPVRTYTHEVVTLWYRAPEILLGCKYY
STAVDIWSLGCIFAEMVTRRALFPGDSEIDQLFRIFRTLGTPDEVVWPGVTSMPDYKPSF
PKWARQDFSKVVPPLDEDGRSLLSQMLHYDPNKRISAKAALAHPFFQDVTKPVPHLRL
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Component 2
Name:cyclin A3
Synonyms:n/a
Type:Enzyme Subunit
Mol. Mass.:29930.91
Organism:Homo sapiens (Human)
Description:cyclin A3 is a c-terminal cyclin A fragment encoding residues 171-432.
Residue:261
Sequence:
VPDYHEDIHTYLREMEVKCKPKVGYMKKQPDITNSMRAILVDWLVEVGEEYKLQNETLHL
AVNYIDRFLSSMSVLRGKLQLVGTAAMLLASKFEEIYPPEVAEFVYITDDTYTKKQVLRM
EHLVLKVLTFDLAAPTVNQFLTQYFLHQQPANCKVESLAMFLGELSLIDADPYLKYLPSV
IAGAAFHLALYTVTGQSWPESLIRKTGYTLESLKPCLMDLHQTYLKAPQHAQQSIREKYK
NSKYHGVSLLNPPETLNLLNL
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BDBM5485
NameBDBM5485
Synonyms:6-(cyclohexylmethoxy)-9H-purin-2-amine | CHEMBL269881 | NU2058
TypeSmall organic molecule
Emp. Form.C12H17N5O
Mol. Mass.247.2963
SMILESNc1nc(OCC2CCCCC2)c2[nH]cnc2n1
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least:
Histone H1
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:
n/a