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Target
CDK-activating kinase assembly factor MAT1/Cyclin-H/Cyclin-dependent kinase 7
Ligand
BDBM454519
Substrate
n/a
Meas. Tech.
ChEMBL_2025081 (CHEMBL4678894)
IC50
5900±n/a nM
Citation
 Barlaam, B; Casella, R; Cidado, J; Cook, C; De Savi, C; Dishington, A; Donald, CS; Drew, L; Ferguson, AD; Ferguson, D; Glossop, S; Grebe, T; Gu, C; Hande, S; Hawkins, J; Hird, AW; Holmes, J; Horstick, J; Jiang, Y; Lamb, ML; McGuire, TM; Moore, JE; O'Connell, N; Pike, A; Pike, KG; Proia, T; Roberts, B; San Martin, M; Sarkar, U; Shao, W; Stead, D; Sumner, N; Thakur, K; Vasbinder, MM; Varnes, JG; Wang, J; Wang, L; Wu, D; Wu, L; Yang, B; Yao, T Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies. J Med Chem 63:15564-15590 (2020) [PubMed]  Article 
Target
Name:
CDK-activating kinase assembly factor MAT1/Cyclin-H/Cyclin-dependent kinase 7
Synonyms:
CDK-activating kinase assembly factor MAT1/Cyclin H/Cyclin-dependent kinase 7 | CDK7/Cyclin H/MNAT1
Type:
Protein
Mol. Mass.:
n/a
Description:
n/a
Components:
This complex has 3 components.
Component 1
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
  
Component 2
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 3
Name:
CDK-activating kinase assembly factor MAT1
Synonyms:
MAT1_HUMAN | MNAT1 | CAP35 | MAT1 | RNF66 | CDK7/cyclin-H assembly factor | Cyclin-G1-interacting protein | Menage a trois | RING finger protein 66 | RING finger protein MAT1 | p35 | p36
Type:
Enzyme
Mol. Mass.:
35820.03
Organism:
Human
Description:
P51948
Residue:
309
Sequence:
MDDQGCPRCKTTKYRNPSLKLMVNVCGHTLCESCVDLLFVRGAGNCPECGTPLRKSNFRVQLFEDPTVDKEVEIRKKVLKIYNKREEDFPSLREYNDFLEEVEEIVFNLTNNVDLDNTKKKMEIYQKENKDVIQKNKLKLTREQEELEEALEVERQENEQRRLFIQKEEQLQQILKRKNKQAFLDELESSDLPVALLLAQHKDRSTQLEMQLEKPKPVKPVTFSTGIKMGQHISLAPIHKLEEALYEYQPLQIETYGPHVPELEMLGRLGYLNHVRAASPQDLAGGYTSSLACHRALQDAFSGLFWQPS
  
Inhibitor
Name:
BDBM454519
Synonyms:
US10717746, Example 2
Type:
Small organic molecule
Emp. Form.:
TBD
Mol. Mass.:
TBD
SMILES:
TBD
Structure:
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