| Reaction Details |
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 | Report a problem with these data |
| Target | Cyclin-A2 [171-432]/Cyclin-dependent kinase 2 |
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| Ligand | BDBM5566 |
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| Substrate/Competitor | Histone H1 |
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| Meas. Tech. | Kinase Inhibition Assay |
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| pH | 7.5±n/a |
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| Temperature | 303.15±n/a K |
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| Ki | 1300±200 nM |
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| Comments | To obtain Ki value, the assay was performed in the absence of inhibitor and at two fixed inhibitor concentrations, 5 and 10 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. |
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| Citation |  Arris, CE; Boyle, FT; Calvert, AH; Curtin, NJ; Endicott, JA; Garman, EF; Gibson, AE; Golding, BT; Grant, S; Griffin, RJ; Jewsbury, P; Johnson, LN; Lawrie, AM; Newell, DR; Noble, ME; Sausville, EA; Schultz, R; Yu, 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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| More Info.: | Get all data from this article, Solution Info, Assay Method |
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| |
| Cyclin-A2 [171-432]/Cyclin-dependent kinase 2 |
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| Name: | Cyclin-A2 [171-432]/Cyclin-dependent kinase 2 |
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| Synonyms: | CDK2/cyclin A3 | Cyclin-Dependent Kinase 2 (CDK2) | p33cdk2/cyclin A3 |
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| Type: | Protein Complex |
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| Mol. Mass.: | n/a |
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| 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. |
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| Components: | This complex has 2 components. |
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| Component 1 |
| Name: | Cyclin-dependent kinase 2 |
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| 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 |
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| Type: | Enzyme Subunit |
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| Mol. Mass.: | 33938.17 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P24941 |
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| Residue: | 298 |
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| Sequence: | MENFQKVEKIGEGTYGVVYKARNKLTGEVVALKKIRLDTETEGVPSTAIREISLLKELNH
PNIVKLLDVIHTENKLYLVFEFLHQDLKKFMDASALTGIPLPLIKSYLFQLLQGLAFCHS
HRVLHRDLKPQNLLINTEGAIKLADFGLARAFGVPVRTYTHEVVTLWYRAPEILLGCKYY
STAVDIWSLGCIFAEMVTRRALFPGDSEIDQLFRIFRTLGTPDEVVWPGVTSMPDYKPSF
PKWARQDFSKVVPPLDEDGRSLLSQMLHYDPNKRISAKAALAHPFFQDVTKPVPHLRL
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| Component 2 |
| Name: | Cyclin-A2 [171-432] |
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| Synonyms: | CCN1 | CCNA | CCNA2 | CCNA2_HUMAN | cyclin A2 |
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| Type: | Enzyme Subunit |
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| Mol. Mass.: | 30018.91 |
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| Organism: | Homo sapiens (Human) |
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| Description: | cyclin A2 is a c-terminal cyclin A fragment encoding residues 171-432. |
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| Residue: | 262 |
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| Sequence: | SVNEVPDYHEDIHTYLREMEVKCKPKVGYMKKQPDITNSMRAILVDWLVEVGEEYKLQNE
TLHLAVNYIDRFLSSMSVLRGKLQLVGTAAMLLASKFEEIYPPEVAEFVYITDDTYTKKQ
VLRMEHLVLKVLTFDLAAPTVNQFLTQYFLHQQPANCKVESLAMFLGELSLIDADPYLKY
LPSVIAGAAFHLALYTVTGQSWPESLIRKTGYTLESLKPCLMDLHQTYLKAPQHAQQSIR
EKYKNSKYHGVSLLNPPETLNL
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| BDBM5566 |
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| Histone H1 |
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| Name: | Histone H1 |
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| Synonyms: | Sigma Type IIIS |
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| Type: | Other Protein Type |
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| Mol. Mass.: | 358.43 |
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| Organism: | Bos taurus (bovine) |
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| Description: | 12.5 uM ATP as co-substrate. |
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| Residue: | 3 |
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| Sequence: | |
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