Target
CDK-activating kinase assembly factor MAT1
Ligand
BDBM59227
Substrate
n/a
Meas. Tech.
In Vitro Kinase Assay
IC50
71±n/a nM
Citation
 Caligiuri, MBecker, FMurthi, KKaplan, FDedier, SKaufmann, CMachl, AZybarth, GRichard, JBockovich, NKluge, AKley, N A proteome-wide CDK/CRK-specific kinase inhibitor promotes tumor cell death in the absence of cell cycle progression. Chem Biol 12:1103-15 (2005) [PubMed]  Article 
Target
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:
BDBM59227
Synonyms:
Pyrazolopyrimidone analog, RGB-286147
Type:
Small organic molecule
Emp. Form.:
C23H22Cl2N4O3
Mol. Mass.:
473.352
SMILES:
CC(C)c1nn(-c2c(Cl)cccc2Cl)c2nc(Cc3ccc(OCCO)cc3)[nH]c(=O)c12 |(-2.33,5.73,;-1.56,4.39,;-.02,4.39,;-2.33,3.06,;-1.43,1.81,;-2.33,.57,;-1.93,-.92,;-.44,-1.32,;.64,-.23,;-.05,-2.8,;-1.13,-3.89,;-2.62,-3.49,;-3.02,-2.01,;-4.51,-1.61,;-3.79,1.04,;-5.13,.27,;-6.46,1.04,;-7.8,.27,;-9.13,1.04,;-10.46,.27,;-11.8,1.04,;-11.8,2.58,;-13.13,3.35,;-14.46,2.58,;-15.8,3.35,;-17.13,2.58,;-10.46,3.35,;-9.13,2.58,;-6.46,2.58,;-5.13,3.35,;-5.13,4.89,;-3.79,2.58,)|
Structure:
Search PDB for entries with ligand similarity: