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Target
CDK-activating kinase assembly factor MAT1/Cyclin-H/Cyclin-dependent kinase 7
Ligand
BDBM476738
Substrate
n/a
Meas. Tech.
Inhibition of Kinase Activity
IC50
<100±n/a nM
Citation
 Gray, NS; Liang, Y; Zhang, T; Kwiatkowski, NP Inhibitors of cyclin-dependent kinase 7 (CDK7) US Patent  US10870651 Publication Date 12/22/2020 
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 | 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
  
Component 2
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 3
Name:
CDK-activating kinase assembly factor MAT1
Synonyms:
CAP35 | CDK7/cyclin-H assembly factor | Cyclin-G1-interacting protein | MAT1 | MAT1_HUMAN | MNAT1 | Menage a trois | RING finger protein 66 | RING finger protein MAT1 | RNF66 | p35 | p36
Type:
Enzyme
Mol. Mass.:
35820.03
Organism:
Homo sapiens (Human)
Description:
P51948
Residue:
309
Sequence:
MDDQGCPRCKTTKYRNPSLKLMVNVCGHTLCESCVDLLFVRGAGNCPECGTPLRKSNFRVQLFEDPTVDKEVEIRKKVLKIYNKREEDFPSLREYNDFLEEVEEIVFNLTNNVDLDNTKKKMEIYQKENKDVIQKNKLKLTREQEELEEALEVERQENEQRRLFIQKEEQLQQILKRKNKQAFLDELESSDLPVALLLAQHKDRSTQLEMQLEKPKPVKPVTFSTGIKMGQHISLAPIHKLEEALYEYQPLQIETYGPHVPELEMLGRLGYLNHVRAASPQDLAGGYTSSLACHRALQDAFSGLFWQPS
  
Inhibitor
Name:
BDBM476738
Synonyms:
US10870651, Compound 222
Type:
Small organic molecule
Emp. Form.:
C28H39N7O3
Mol. Mass.:
521.6544
SMILES:
CN(C)C[C@@H](NC(=O)N1Cc2c(NC(=O)[C@H]3CC[C@@H](CC3)NC(=O)C=C)n[nH]c2C1(C)C)c1ccccc1 |r,wU:4.4,15.14,wD:18.21,(6.9,7.14,;6.9,5.6,;8.23,4.83,;5.56,4.83,;4.23,5.6,;2.9,4.83,;1.56,5.6,;1.56,7.14,;.23,4.83,;.07,3.3,;-1.44,2.98,;-2.47,1.83,;-2.15,.33,;-3.29,-.7,;-4.76,-.23,;-2.97,-2.21,;-1.51,-2.69,;-1.19,-4.19,;-2.33,-5.22,;-3.8,-4.75,;-4.12,-3.24,;-2.01,-6.73,;-3.16,-7.76,;-4.62,-7.28,;-2.84,-9.27,;-3.98,-10.3,;-3.88,2.46,;-3.72,3.99,;-2.21,4.31,;-1.18,5.45,;-.72,6.92,;-2.2,6.61,;4.23,7.14,;2.9,7.91,;2.9,9.45,;4.23,10.22,;5.56,9.45,;5.56,7.91,)|
Structure:
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