Target
Bromodomain-containing protein 4 [44-477]
Ligand
BDBM274238
Substrate
n/a
Meas. Tech.
TR-FRET In-Vitro Binding Assay
pH
7.5±n/a
IC50
18.0±n/a nM
Comments
extracted
Citation
 Rueger, HBlank, JBordas, VCotesta, SBold, GGuagnano, VVaupel, A Pyrrolopyrrolone derivatives and their use as BET inhibitors US Patent  US9550796 Publication Date 1/24/2017 
Target
Name:
Bromodomain-containing protein 4 [44-477]
Synonyms:
BRD4 | BRD4_HUMAN | Bromodomain-containing protein 4 | HUNK1
Type:
Enzyme Catalytic Domain (aa 44-477)
Mol. Mass.:
48692.13
Organism:
Homo sapiens (Human)
Description:
O60885[44-477]
Residue:
434
Sequence:
NPPPPETSNPNKPKRQTNQLQYLLRVVLKTLWKHQFAWPFQQPVDAVKLNLPDYYKIIKTPMDMGTIKKRLENNYYWNAQECIQDFNTMFTNCYIYNKPGDDIVLMAEALEKLFLQKINELPTEETEIMIVQAKGRGRGRKETGTAKPGVSTVPNTTQASTPPQTQTPQPNPPPVQATPHPFPAVTPDLIVQTPVMTVVPPQPLQTPPPVPPQPQPPPAPAPQPVQSHPPIIAATPQPVKTKKGVKRKADTTTPTTIDPIHEPPSLPPEPKTTKLGQRRESSRPVKPPKKDVPDSQQHPAPEKSSKVSEQLKCCSGILKEMFAKKHAAYAWPFYKPVDVEALGLHDYCDIIKHPMDMSTIKSKLEAREYRDAQEFGADVRLMFSNCYKYNPPDHEVVAMARKLQDVFEMRFAKMPDEPEEPVVAVSSPAVPPPT
  
Inhibitor
Name:
BDBM274238
Synonyms:
6-(4-chlorophenyl)-3-cyclopropyl-5-(3,8-dimethyl-[1,2,4]triazolo[4,3-a]pyridin-6-yl)-1-methyl-5,6-dihydropyrrolo[3,4-b]pyrrol-4(1H)-one | US9550796, Example 35
Type:
Small organic molecule
Emp. Form.:
C24H22ClN5O
Mol. Mass.:
431.917
SMILES:
Cc1nnc2c(C)cc(cn12)N1C(c2c(C1=O)c(cn2C)C1CC1)c1ccc(Cl)cc1
Structure:
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