| Reaction Details |
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 | Report a problem with these data |
| Target | Cyclin-Dependent Kinase 2 (CDK2) |
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| Ligand | BDBM11449 |
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| Substrate/Competitor | Histone H1 |
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| Meas. Tech. | CDK Inhibition Assay |
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| pH | 7.5±n/a |
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| Temperature | 295.15±n/a K |
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| IC50 | 730±n/a nM |
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| 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 Lett16:1353-7 (2006) [PubMed] Article |
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| More Info.: | Get all data from this article, Solution Info, Assay Method |
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| Cyclin-Dependent Kinase 2 (CDK2) |
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| Name: | Cyclin-Dependent Kinase 2 (CDK2) |
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| Synonyms: | CDK2-CyclinA | CDK2/A | CDK2/Cyclin A | Cyclin A2/dependent kinase 2 | Cyclin-Dependent Kinase 2 (CDK2A) |
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| Type: | Protein Complex |
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| Mol. Mass.: | n/a |
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| Description: | Cdk2/Cyclin A kinase was purified from insect cells coinfected with Cyclin A/Cdk2 baculovirus. |
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| Components: | This complex has 2 components. |
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| Component 1 |
| Name: | Protein cereblon/Cyclin-dependent kinase 2 |
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| Synonyms: | CDK2 | CDK2-Kinase | Cell division protein kinase 2 | Cyclin-dependent kinase 2 (CDK2) | 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 |
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| Synonyms: | CCN1 | CCNA | CCNA1 | Cyclin A | Cyclin-A |
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| Type: | Enzyme Subunit |
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| Mol. Mass.: | 48550.19 |
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| Organism: | Homo sapiens (Human) |
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| Description: | n/a |
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| Residue: | 432 |
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| Sequence: | MLGNSAPGPATREAGSALLALQQTALQEDQENINPEKAAPVQQPRTRAALAVLKSGNPRG
LAQQQRPKTRRVAPLKDLPVNDEHVTVPPWKANSKQPAFTIHVDEAEKEAQKKPAESQKI
EREDALAFNSAISLPGPRKPLVPLDYPMDGSFESPHTMDMSIILEDEKPVSVNEVPDYHE
DIHTYLREMEVKCKPKVGYMKKQPDITNSMRAILVDWLVEVGEEYKLQNETLHLAVNYID
RFLSSMSVLRGKLQLVGTAAMLLASKFEEIYPPEVAEFVYITDDTYTKKQVLRMEHLVLK
VLTFDLAAPTVNQFLTQYFLHQQPANCKVESLAMFLGELSLIDADPYLKYLPSVIAGAAF
HLALYTVTGQSWPESLIRKTGYTLESLKPCLMDLHQTYLKAPQHAQQSIREKYKNSKYHG
VSLLNPPETLNL
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| BDBM11449 |
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| Name | BDBM11449 |
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| Synonyms: | 4-{[5-(cyclohexylamino)-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl]amino}benzene-1-sulfonamide | triazolo[1,5-a]pyrimidine 11 |
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| Type | Small organic molecule |
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| Emp. Form. | C17H21N7O2S |
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| Mol. Mass. | 387.459 |
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| SMILES | NS(=O)(=O)c1ccc(Nc2cc(NC3CCCCC3)nc3ncnn23)cc1 |
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| Structure |  |
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| Histone H1 |
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| Name: | Histone H1 |
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| Synonyms: | n/a |
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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: | n/a |
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| Residue: | 3 |
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| Sequence: | |
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