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Target
CDK-activating kinase assembly factor MAT1/Cyclin-H/Cyclin-dependent kinase 7
Ligand
BDBM144315
Substrate
n/a
Meas. Tech.
ChEMBL_2106555 (CHEMBL4815230)
Ki
>5000±n/a nM
Citation
 Long, Y; Yu, M; Ochnik, AM; Karanjia, JD; Basnet, SK; Kebede, AA; Kou, L; Wang, S Discovery of novel 4-azaaryl-N-phenylpyrimidin-2-amine derivatives as potent and selective FLT3 inhibitors for acute myeloid leukaemia with FLT3 mutations. Eur J Med Chem 213:0 (2021) [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 | 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:
BDBM144315
Synonyms:
Gilteritinib | US11512074, Example T-9 | US8969336, 547 | US8969336, 577
Type:
Small organic molecule
Emp. Form.:
C29H44N8O3
Mol. Mass.:
552.7115
SMILES:
CCc1nc(C(N)=O)c(Nc2ccc(N3CCC(CC3)N3CCN(C)CC3)c(OC)c2)nc1NC1CCOCC1
Structure:
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