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Target
Cyclin-H/Cyclin-dependent kinase 7
Ligand
BDBM59227
Substrate
n/a
Meas. Tech.
ChEMBL_473687 (CHEMBL936786)
IC50
71±n/a nM
Citation
 Fedorov, O; Marsden, B; Pogacic, V; Rellos, P; Müller, S; Bullock, AN; Schwaller, J; Sundström, M; Knapp, S A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. Proc Natl Acad Sci U S A 104:20523-8 (2007) [PubMed]  Article
Target
Name:
Cyclin-H/Cyclin-dependent kinase 7
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
Type:
Protein Complex
Mol. Mass.:
n/a
Description:
n/a
Components:
This complex has 2 components.
Component 1
Name:
Cyclin-H
Synonyms:
CCNH | CCNH_HUMAN | Cyclin H | MO15-associated protein | p34 | p37
Type:
Enzyme Subunit
Mol. Mass.:
37646.05
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
323
Sequence:
MYHNSSQKRHWTFSSEEQLARLRADANRKFRCKAVANGKVLPNDPVFLEPHEEMTLCKYYEKRLLEFCSVFKPAMPRSVVGTACMYFKRFYLNNSVMEYHPRIIMLTCAFLACKVDEFNVSSPQFVGNLRESPLGQEKALEQILEYELLLIQQLNFHLIVHNPYRPFEGFLIDLKTRYPILENPEILRKTADDFLNRIALTDAYLLYTPSQIALTAILSSASRAGITMESYLSESLMLKENRTCLSQLLDIMKSMRNLVKKYEPPRSEEVAVLKQKLERCHSAELALNVITKKRKGYEDDDYVSKKSKHEEEEWTDDDLVESL
  
Component 2
Name:
Cyclin-dependent kinase 7
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
Type:
Enzyme Subunit
Mol. Mass.:
39047.01
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
346
Sequence:
MALDVKSRAKRYEKLDFLGEGQFATVYKARDKNTNQIVAIKKIKLGHRSEAKDGINRTALREIKLLQELSHPNIIGLLDAFGHKSNISLVFDFMETDLEVIIKDNSLVLTPSHIKAYMLMTLQGLEYLHQHWILHRDLKPNNLLLDENGVLKLADFGLAKSFGSPNRAYTHQVVTRWYRAPELLFGARMYGVGVDMWAVGCILAELLLRVPFLPGDSDLDQLTRIFETLGTPTEEQWPDMCSLPDYVTFKSFPGIPLHHIFSAAGDDLLDLIQGLFLFNPCARITATQALKMKYFSNRPGPTPGCQLPRPNCPVETLKEQSNPALAIKRKRTEALEQGGLPKKLIF
  
Inhibitor
Name:
BDBM59227
Synonyms:
Pyrazolopyrimidone analog, RGB-286147
Type:
Small organic molecule
Emp. Form.:
C23H22Cl2N4O3
Mol. Mass.:
473.352
SMILES:
CC(C)c1nn(-c2c(Cl)cccc2Cl)c2nc(Cc3ccc(OCCO)cc3)[nH]c(=O)c12 |(-2.33,5.73,;-1.56,4.39,;-.02,4.39,;-2.33,3.06,;-1.43,1.81,;-2.33,.57,;-1.93,-.92,;-.44,-1.32,;.64,-.23,;-.05,-2.8,;-1.13,-3.89,;-2.62,-3.49,;-3.02,-2.01,;-4.51,-1.61,;-3.79,1.04,;-5.13,.27,;-6.46,1.04,;-7.8,.27,;-9.13,1.04,;-10.46,.27,;-11.8,1.04,;-11.8,2.58,;-13.13,3.35,;-14.46,2.58,;-15.8,3.35,;-17.13,2.58,;-10.46,3.35,;-9.13,2.58,;-6.46,2.58,;-5.13,3.35,;-5.13,4.89,;-3.79,2.58,)|
Structure:
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