Reaction Details |
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Target | Cyclin-dependent kinase/G2/mitotic-specific cyclin- 1 |
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Ligand | BDBM7533 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_755643 (CHEMBL1805468) |
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IC50 | 2100±n/a nM |
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Citation | Heathcote, DA; Patel, H; Kroll, SH; Hazel, P; Periyasamy, M; Alikian, M; Kanneganti, SK; Jogalekar, AS; Scheiper, B; Barbazanges, M; Blum, A; Brackow, J; Siwicka, A; Pace, RD; Fuchter, MJ; Snyder, JP; Liotta, DC; Freemont, PS; Aboagye, EO; Coombes, RC; Barrett, AG; Ali, S A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. J Med Chem53:8508-22 (2010) [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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BDBM7533 |
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n/a |
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Name | BDBM7533 |
Synonyms: | (2R)-2-[[6-(benzylamino)-9-isopropyl-purin-2-yl]amino]butan-1-ol | (2R)-2-[[6-(benzylamino)-9-propan-2-ylpurin-2-yl]amino]butan-1-ol | (2R)-2-[[6-[(phenylmethyl)amino]-9-propan-2-yl-2-purinyl]amino]-1-butanol | (2R)-2-[[6-[(phenylmethyl)amino]-9-propan-2-yl-purin-2-yl]amino]butan-1-ol | (2R)-2-{[6-(benzylamino)-9-(propan-2-yl)-9H-purin-2-yl]amino}butan-1-ol | (R)-Roscovitine | 2,6,9-Trisubstituted purine deriv. 28 | CHEMBL14762 | CYC-202 | Roscovitine | cid_160355 |
Type | Small organic molecule |
Emp. Form. | C19H26N6O |
Mol. Mass. | 354.4493 |
SMILES | CC[C@H](CO)Nc1nc(NCc2ccccc2)c2ncn(C(C)C)c2n1 |r| |
Structure |
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