Reaction Details |
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Target | Cyclin-dependent kinase/G2/mitotic-specific cyclin- 1 |
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Ligand | BDBM50361088 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_795082 (CHEMBL1936508) |
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IC50 | >10000±n/a nM |
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Citation | Caruso, M; Valsasina, B; Ballinari, D; Bertrand, J; Brasca, MG; Caldarelli, M; Cappella, P; Fiorentini, F; Gianellini, LM; Scolaro, A; Beria, I 5-(2-amino-pyrimidin-4-yl)-1H-pyrrole and 2-(2-amino-pyrimidin-4-yl)-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one derivatives as new classes of selective and orally available Polo-like kinase 1 inhibitors. Bioorg Med Chem Lett22:96-101 (2011) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Cyclin-dependent kinase/G2/mitotic-specific cyclin- 1 |
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Name: | Cyclin-dependent kinase/G2/mitotic-specific cyclin- 1 |
Synonyms: | CDK1/B | CDK1/Cyclin B | CDK1/CyclinB | Cyclin B/Dependent Kinase 1 (CDK1) | Cyclin-Dependent Kinase 1 (CDK1) | Cyclin-dependent kinase 1/cyclin B1 | Cyclin-dependent kinase/G2/mitotic-specific cyclin 1 | cdk1 |
Type: | Protein Complex |
Mol. Mass.: | n/a |
Description: | CDK1/Cyclin B complexes were purified from insect cells co-infected with baculovirus vectors containing each of the components. |
Components: | This complex has 2 components. |
Component 1 |
Name: | Cyclin-dependent kinase 1 |
Synonyms: | CDC2 | CDC28A | CDK1 | CDK1_HUMAN | CDKN1 | Cell division control protein 2 homolog | Cell division protein kinase 1 | Cyclin-dependent kinase 1 (CDK1) | P34CDC2 | p34 protein kinase |
Type: | Enzyme Subunit |
Mol. Mass.: | 34101.08 |
Organism: | Homo sapiens (Human) |
Description: | P06493 |
Residue: | 297 |
Sequence: | MEDYTKIEKIGEGTYGVVYKGRHKTTGQVVAMKKIRLESEEEGVPSTAIREISLLKELRH
PNIVSLQDVLMQDSRLYLIFEFLSMDLKKYLDSIPPGQYMDSSLVKSYLYQILQGIVFCH
SRRVLHRDLKPQNLLIDDKGTIKLADFGLARAFGIPIRVYTHEVVTLWYRSPEVLLGSAR
YSTPVDIWSIGTIFAELATKKPLFHGDSEIDQLFRIFRALGTPNNEVWPEVESLQDYKNT
FPKWKPGSLASHVKNLDENGLDLLSKMLIYDPAKRISGKMALNHPYFNDLDNQIKKM
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Component 2 |
Name: | G2/mitotic-specific cyclin-B1 |
Synonyms: | CCNB | CCNB1 | CCNB1_HUMAN |
Type: | Enzyme Subunit |
Mol. Mass.: | 48340.95 |
Organism: | Homo sapiens (Human) |
Description: | P14635 |
Residue: | 433 |
Sequence: | MALRVTRNSKINAENKAKINMAGAKRVPTAPAATSKPGLRPRTALGDIGNKVSEQLQAKM
PMKKEAKPSATGKVIDKKLPKPLEKVPMLVPVPVSEPVPEPEPEPEPEPVKEEKLSPEPI
LVDTASPSPMETSGCAPAEEDLCQAFSDVILAVNDVDAEDGADPNLCSEYVKDIYAYLRQ
LEEEQAVRPKYLLGREVTGNMRAILIDWLVQVQMKFRLLQETMYMTVSIIDRFMQNNCVP
KKMLQLVGVTAMFIASKYEEMYPPEIGDFAFVTDNTYTKHQIRQMEMKILRALNFGLGRP
LPLHFLRRASKIGEVDVEQHTLAKYLMELTMLDYDMVHFPPSQIAAGAFCLALKILDNGE
WTPTLQHYLSYTEESLLPVMQHLAKNVVMVNQGLTKHMTVKNKYATSKHAKISTLPQLNS
ALVQDLAKAVAKV
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BDBM50361088 |
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n/a |
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Name | BDBM50361088 |
Synonyms: | CHEMBL1933582 |
Type | Small organic molecule |
Emp. Form. | C24H26F3N7O2 |
Mol. Mass. | 501.5041 |
SMILES | CN1CCN(CC1)c1ccc(OC(F)(F)F)c(Nc2nccc(n2)-c2cc3c(CCNC3=O)n2C)c1 |
Structure |
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