| Reaction Details |
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 | Report a problem with these data |
| Target | Cyclin-H/Cyclin-dependent kinase 7 |
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| Ligand | BDBM7533 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_755648 (CHEMBL1805473) |
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| IC50 | 540±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-H/Cyclin-dependent kinase 7 |
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| Name: | Cyclin-H/Cyclin-dependent kinase 7 |
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| Synonyms: | CDK-activating kinase assembly factor MAT1/Cyclin H/Cyclin-dependent kinase 7 | CDK7/Cyclin H | CDK7/H | Cyclin H/dependent kinase 7 | Cyclin-Dependent Kinase 7 (CDK7) | Cyclin-dependent kinase 7/ cyclin H | Cyclin-dependent kinase 7/cyclin H |
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| Type: | Protein Complex |
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| Mol. Mass.: | n/a |
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| Description: | n/a |
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| Components: | This complex has 2 components. |
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| Component 1 |
| Name: | Cyclin-H |
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| Synonyms: | CCNH | CCNH_HUMAN | Cyclin H | MO15-associated protein | p34 | p37 |
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| Type: | Enzyme Subunit |
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| Mol. Mass.: | 37646.05 |
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| Organism: | Homo sapiens (Human) |
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| Description: | n/a |
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| Residue: | 323 |
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| Sequence: | MYHNSSQKRHWTFSSEEQLARLRADANRKFRCKAVANGKVLPNDPVFLEPHEEMTLCKYY
EKRLLEFCSVFKPAMPRSVVGTACMYFKRFYLNNSVMEYHPRIIMLTCAFLACKVDEFNV
SSPQFVGNLRESPLGQEKALEQILEYELLLIQQLNFHLIVHNPYRPFEGFLIDLKTRYPI
LENPEILRKTADDFLNRIALTDAYLLYTPSQIALTAILSSASRAGITMESYLSESLMLKE
NRTCLSQLLDIMKSMRNLVKKYEPPRSEEVAVLKQKLERCHSAELALNVITKKRKGYEDD
DYVSKKSKHEEEEWTDDDLVESL
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| Component 2 |
| Name: | Cyclin-dependent kinase 7 |
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| Synonyms: | 39 kDa protein kinase | CAK | CAK1 | CDK-activating kinase | CDK-activating kinase 1 (CAK) | CDK7 | CDK7_HUMAN | CDKN7 | Cell division protein kinase 7 | Cyclin-Dependent Kinase 7 (CDK7) | Cyclin-dependent kinase 7 (CDK7/cyclin H) | MO15 | P39 Mo15 | STK1 | TFIIH basal transcription factor complex kinase subunit |
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| Type: | Enzyme Subunit |
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| Mol. Mass.: | 39047.01 |
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| Organism: | Homo sapiens (Human) |
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| Description: | n/a |
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| Residue: | 346 |
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| Sequence: | MALDVKSRAKRYEKLDFLGEGQFATVYKARDKNTNQIVAIKKIKLGHRSEAKDGINRTAL
REIKLLQELSHPNIIGLLDAFGHKSNISLVFDFMETDLEVIIKDNSLVLTPSHIKAYMLM
TLQGLEYLHQHWILHRDLKPNNLLLDENGVLKLADFGLAKSFGSPNRAYTHQVVTRWYRA
PELLFGARMYGVGVDMWAVGCILAELLLRVPFLPGDSDLDQLTRIFETLGTPTEEQWPDM
CSLPDYVTFKSFPGIPLHHIFSAAGDDLLDLIQGLFLFNPCARITATQALKMKYFSNRPG
PTPGCQLPRPNCPVETLKEQSNPALAIKRKRTEALEQGGLPKKLIF
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| BDBM7533 |
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| n/a |
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| Name | BDBM7533 |
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| 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 |
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| Type | Small organic molecule |
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| Emp. Form. | C19H26N6O |
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| Mol. Mass. | 354.4493 |
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| SMILES | CC[C@H](CO)Nc1nc(NCc2ccccc2)c2ncn(C(C)C)c2n1 |r| |
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| Structure | 
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