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Target
Cyclin-H/Cyclin-dependent kinase 7
Ligand
BDBM12028
Substrate
Biotinylated Peptide Substrate
Meas. Tech.
CDK Inhibition Assay
Temperature
303.15±n/a K
IC50
26000±n/a nM
Comments
extracted
Citation
 Krystof, V; Cankar, P; Frysova, I; Slouka, J; Kontopidis, G; Dzubak, P; Hajduch, M; Srovnal, J; de Azevedo, WF; Orsag, M; Paprskarova, M; Rolcik, J; Latr, A; Fischer, PM; Strnad, M 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. J Med Chem 49:6500-9 (2006) [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:
BDBM12028
Synonyms:
4-Arylazo-3,5-diamino-1H-pyrazole 31b | 4-[(E)-2-(3,5-diamino-1H-pyrazol-4-yl)diazen-1-yl]phenol | CAN508
Type:
Small organic molecule
Emp. Form.:
C9H10N6O
Mol. Mass.:
218.2153
SMILES:
Nc1n[nH]c(N)c1N=Nc1ccc(O)cc1 |w:8.9|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Biotinylated Peptide Substrate
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
10968.97
Organism:
n/a
Description:
n/a
Residue:
86
Sequence:
ITINYLAHTYRSERPRTHRSERPRSERTYRSERPRTHRSERPRSERTYRSERPRTHRSERPRSERTYRSERPRTHRSERPRSERNH