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Target
Cyclin-H/Cyclin-dependent kinase 7
Ligand
BDBM50583929
Substrate
n/a
Meas. Tech.
ChEMBL_2158414 (CHEMBL5043164)
Kd
0.070000±n/a nM
Citation
 Marineau, JJ; Hamman, KB; Hu, S; Alnemy, S; Mihalich, J; Kabro, A; Whitmore, KM; Winter, DK; Roy, S; Ciblat, S; Ke, N; Savinainen, A; Wilsily, A; Malojcic, G; Zahler, R; Schmidt, D; Bradley, MJ; Waters, NJ; Chuaqui, C Discovery of SY-5609: A Selective, Noncovalent Inhibitor of CDK7. J Med Chem 65:1458-1480 (2022) [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:
Cyclin H | MO15-associated protein | p34 | p37 | CCNH_HUMAN | CCNH
Type:
Enzyme Subunit
Mol. Mass.:
37646.05
Organism:
Human
Description:
n/a
Residue:
323
Sequence:
MYHNSSQKRHWTFSSEEQLARLRADANRKFRCKAVANGKVLPNDPVFLEPHEEMTLCKYYEKRLLEFCSVFKPAMPRSVVGTACMYFKRFYLNNSVMEYHPRIIMLTCAFLACKVDEFNVSSPQFVGNLRESPLGQEKALEQILEYELLLIQQLNFHLIVHNPYRPFEGFLIDLKTRYPILENPEILRKTADDFLNRIALTDAYLLYTPSQIALTAILSSASRAGITMESYLSESLMLKENRTCLSQLLDIMKSMRNLVKKYEPPRSEEVAVLKQKLERCHSAELALNVITKKRKGYEDDDYVSKKSKHEEEEWTDDDLVESL
  
Component 2
Name:
Cyclin-dependent kinase 7
Synonyms:
39 kDa protein kinase | CDK-activating kinase | CDK-activating kinase 1 (CAK) | Cell division protein kinase 7 | Cyclin-Dependent Kinase 7 (CDK7) | Cyclin-dependent kinase 7 (CDK7/cyclin H) | P39 Mo15 | TFIIH basal transcription factor complex kinase subunit | CDK7_HUMAN | CDK7 | CAK | CAK1 | CDKN7 | MO15 | STK1
Type:
Enzyme Subunit
Mol. Mass.:
39047.01
Organism:
Human
Description:
n/a
Residue:
346
Sequence:
MALDVKSRAKRYEKLDFLGEGQFATVYKARDKNTNQIVAIKKIKLGHRSEAKDGINRTALREIKLLQELSHPNIIGLLDAFGHKSNISLVFDFMETDLEVIIKDNSLVLTPSHIKAYMLMTLQGLEYLHQHWILHRDLKPNNLLLDENGVLKLADFGLAKSFGSPNRAYTHQVVTRWYRAPELLFGARMYGVGVDMWAVGCILAELLLRVPFLPGDSDLDQLTRIFETLGTPTEEQWPDMCSLPDYVTFKSFPGIPLHHIFSAAGDDLLDLIQGLFLFNPCARITATQALKMKYFSNRPGPTPGCQLPRPNCPVETLKEQSNPALAIKRKRTEALEQGGLPKKLIF
  
Inhibitor
Name:
BDBM50583929
Synonyms:
Sy 5609 | Sy-5609 | SY5609 | SY-5609
Type:
Small organic molecule
Emp. Form.:
C23H26F3N6OP
Mol. Mass.:
490.47
SMILES:
CC1(C)CC[C@@H](CN1)Nc1ncc(c(n1)-c1c[nH]c2c(c(ccc12)C#N)P(C)(C)=O)C(F)(F)F |r|
Structure:
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