Reaction Details |
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Target | Cyclin-A2/Cyclin-dependent kinase 2 |
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Ligand | BDBM7152 |
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Substrate/Competitor | Histone H1 |
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Meas. Tech. | Kinase SPA Assay |
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IC50 | >10000±n/a nM |
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Citation | Pevarello, P; Brasca, MG; Amici, R; Orsini, P; Traquandi, G; Corti, L; Piutti, C; Sansonna, P; Villa, M; Pierce, BS; Pulici, M; Giordano, P; Martina, K; Fritzen, EL; Nugent, RA; Casale, E; Cameron, A; Ciomei, M; Roletto, F; Isacchi, A; Fogliatto, G; Pesenti, E; Pastori, W; Marsiglio, A; Leach, KL; Clare, PM; Fiorentini, F; Varasi, M; Vulpetti, A; Warpehoski, MA 3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 1. Lead finding. J Med Chem47:3367-80 (2004) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Cyclin-A2/Cyclin-dependent kinase 2 |
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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: | MENFQKVEKIGEGTYGVVYKARNKLTGEVVALKKIRLDTETEGVPSTAIREISLLKELNH
PNIVKLLDVIHTENKLYLVFEFLHQDLKKFMDASALTGIPLPLIKSYLFQLLQGLAFCHS
HRVLHRDLKPQNLLINTEGAIKLADFGLARAFGVPVRTYTHEVVTLWYRAPEILLGCKYY
STAVDIWSLGCIFAEMVTRRALFPGDSEIDQLFRIFRTLGTPDEVVWPGVTSMPDYKPSF
PKWARQDFSKVVPPLDEDGRSLLSQMLHYDPNKRISAKAALAHPFFQDVTKPVPHLRL
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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: | MLGNSAPGPATREAGSALLALQQTALQEDQENINPEKAAPVQQPRTRAALAVLKSGNPRG
LAQQQRPKTRRVAPLKDLPVNDEHVTVPPWKANSKQPAFTIHVDEAEKEAQKKPAESQKI
EREDALAFNSAISLPGPRKPLVPLDYPMDGSFESPHTMDMSIILEDEKPVSVNEVPDYHE
DIHTYLREMEVKCKPKVGYMKKQPDITNSMRAILVDWLVEVGEEYKLQNETLHLAVNYID
RFLSSMSVLRGKLQLVGTAAMLLASKFEEIYPPEVAEFVYITDDTYTKKQVLRMEHLVLK
VLTFDLAAPTVNQFLTQYFLHQQPANCKVESLAMFLGELSLIDADPYLKYLPSVIAGAAF
HLALYTVTGQSWPESLIRKTGYTLESLKPCLMDLHQTYLKAPQHAQQSIREKYKNSKYHG
VSLLNPPETLNL
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BDBM7152 |
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Histone H1 |
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Name: | Histone H1 |
Synonyms: | n/a |
Type: | Other Protein Type |
Mol. Mass.: | 358.43 |
Organism: | Bos taurus (bovine) |
Description: | n/a |
Residue: | 3 |
Sequence: | |