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Target
Cyclin-H/Cyclin-dependent kinase 7
Ligand
BDBM31545
Substrate
n/a
Meas. Tech.
ChEMBL_1846265 (CHEMBL4346806)
IC50
150±n/a nM
Citation
 Tadesse, S; Caldon, EC; Tilley, W; Wang, S Cyclin-Dependent Kinase 2 Inhibitors in Cancer Therapy: An Update. J Med Chem 62:4233-4251 (2019) [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:
BDBM31545
Synonyms:
Milciclib | pyrazolo[4,3-h]quinazoline-3-carboxamide, 28
Type:
Small organic molecule
Emp. Form.:
C25H32N8O
Mol. Mass.:
460.5746
SMILES:
CNC(=O)c1nn(C)c-2c1C(C)(C)Cc1cnc(Nc3ccc(cc3)N3CCN(C)CC3)nc-21
Structure:
Search PDB for entries with ligand similarity: