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Target
CDK-activating kinase assembly factor MAT1/Cyclin-H/Cyclin-dependent kinase 7
Ligand
BDBM50521533
Substrate
n/a
Meas. Tech.
ChEMBL_1884568 (CHEMBL4386150)
IC50
124±n/a nM
Citation
 Jorda, R; Havlí?ek, L; ?turc, A; Tu?ková, D; Daumová, L; Alam, M; ?kerlová, J; Nekardová, M; Pe?ina, M; Pospí?il, T; ?iroká, J; Urbánek, L; Pachl, P; ?ezá?ová, P; Strnad, M; Klener, P; Kry?tof, V 3,5,7-Substituted Pyrazolo[4,3- d]pyrimidine Inhibitors of Cyclin-Dependent Kinases and Their Evaluation in Lymphoma Models. J Med Chem 62:4606-4623 (2019) [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:
BDBM50521533
Synonyms:
CHEMBL4540226
Type:
Small organic molecule
Emp. Form.:
C22H25N7S
Mol. Mass.:
419.546
SMILES:
CC(C)c1n[nH]c2c(NCc3ccc(cc3)-c3ccccn3)nc(SCCN)nc12
Structure:
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