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TargetCyclin-Dependent Kinase 7 (CDK7)
LigandBDBM50347388
Substrate/Competitorn/a
Meas. Tech.ChEMBL_755648
IC50 250±n/a nM
Citation Heathcote DAPatel HKroll SHHazel PPeriyasamy MAlikian MKanneganti SKJogalekar ASScheiper BBarbazanges MBlum ABrackow JSiwicka APace RDFuchter MJSnyder JPLiotta DCFreemont PSAboagye EOCoombes RCBarrett AGAli 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 Chem 53:8508-22 (2010) [PubMed]  Article
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Cyclin-Dependent Kinase 7 (CDK7)
Name:Cyclin-Dependent Kinase 7 (CDK7)
Synonyms:CDK-activating kinase assembly factor MAT1/Cyclin H/Cyclin-dependent kinase 7 | CDK7/Cyclin H | Cyclin H/dependent kinase 7 | Cyclin-dependent kinase 7/ cyclin H | Cyclin-dependent kinase 7/cyclin H
Type:Protein Complex
Mol. Mass.:n/a
Description:n/a
Components:This complex has 2 components.
Component 1
Name:CDK7/Cyclin H/MNAT1
Synonyms:Cyclin H | Cyclin-H | MO15-associated protein | p34 | p37
Type:Enzyme Subunit
Mol. Mass.:37646.05
Organism:Homo sapiens (Human)
Description:n/a
Residue:323
Sequence:
MYHNSSQKRHWTFSSEEQLARLRADANRKFRCKAVANGKVLPNDPVFLEPHEEMTLCKYY
EKRLLEFCSVFKPAMPRSVVGTACMYFKRFYLNNSVMEYHPRIIMLTCAFLACKVDEFNV
SSPQFVGNLRESPLGQEKALEQILEYELLLIQQLNFHLIVHNPYRPFEGFLIDLKTRYPI
LENPEILRKTADDFLNRIALTDAYLLYTPSQIALTAILSSASRAGITMESYLSESLMLKE
NRTCLSQLLDIMKSMRNLVKKYEPPRSEEVAVLKQKLERCHSAELALNVITKKRKGYEDD
DYVSKKSKHEEEEWTDDDLVESL
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Component 2
Name:CDK7/Cyclin H/MNAT1
Synonyms:39 kDa protein kinase | CAK1 | CDK-activating kinase | CDK-activating kinase 1 (CAK) | CDK7 | Cell division protein kinase 7 | Cyclin-Dependent Kinase 7 (CDK7) | Cyclin-dependent kinase 7 | Cyclin-dependent kinase 7 (CDK7/cyclin H) | P39 Mo15 | STK1 | TFIIH basal transcription factor complex kinase subunit
Type:Enzyme Subunit
Mol. Mass.:39047.01
Organism:Homo sapiens (Human)
Description:n/a
Residue:346
Sequence:
MALDVKSRAKRYEKLDFLGEGQFATVYKARDKNTNQIVAIKKIKLGHRSEAKDGINRTAL
REIKLLQELSHPNIIGLLDAFGHKSNISLVFDFMETDLEVIIKDNSLVLTPSHIKAYMLM
TLQGLEYLHQHWILHRDLKPNNLLLDENGVLKLADFGLAKSFGSPNRAYTHQVVTRWYRA
PELLFGARMYGVGVDMWAVGCILAELLLRVPFLPGDSDLDQLTRIFETLGTPTEEQWPDM
CSLPDYVTFKSFPGIPLHHIFSAAGDDLLDLIQGLFLFNPCARITATQALKMKYFSNRPG
PTPGCQLPRPNCPVETLKEQSNPALAIKRKRTEALEQGGLPKKLIF
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BDBM50347388
n/a
NameBDBM50347388
Synonyms:CHEMBL1234833
TypeSmall organic molecule
Emp. Form.C20H27N5O3
Mol. Mass.385.4601
SMILESCC(C)c1cnn2c(NCc3ccccc3)cc(N[C@@H](CO)[C@H](O)CO)nc12 |r|
Structure
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