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Target
Bromodomain-containing protein 2 [60-463]
Ligand
BDBM274248
Substrate
n/a
Meas. Tech.
TR-FRET In-Vitro Binding Assay
pH
7.5±n/a
IC50
22.0±n/a nM
Comments
extracted
Citation
 Rueger, H; Blank, J; Bordas, V; Cotesta, S; Bold, G; Guagnano, V; Vaupel, A Pyrrolopyrrolone derivatives and their use as BET inhibitors US Patent  US9550796 Publication Date 1/24/2017 
Target
Name:
Bromodomain-containing protein 2 [60-463]
Synonyms:
BRD2 | BRD2_HUMAN | Bromodomain-containing protein 2 | KIAA9001 | RING3
Type:
Enzyme Catalytic Domain (aa 60-463)
Mol. Mass.:
45228.55
Organism:
Human
Description:
P25440[60-463]
Residue:
404
Sequence:
NPPPPEVSNPKKPGRVTNQLQYLHKVVMKALWKHQFAWPFRQPVDAVKLGLPDYHKIIKQPMDMGTIKRRLENNYYWAASECMQDFNTMFTNCYIYNKPTDDIVLMAQTLEKIFLQKVASMPQEEQELVVTIPKNSHKKGAKLAALQGSVTSAHQVPAVSSVSHTALYTPPPEIPTTVLNIPHPSVISSPLLKSLHSAGPPLLAVTAAPPAQPLAKKKGVKRKADTTTPTPTAILAPGSPASPPGSLEPKAARLPPMRRESGRPIKPPRKDLPDSQQQHQSSKKGKLSEQLKHCNGILKELLSKKHAAYAWPFYKPVDASALGLHDYHDIIKHPMDLSTVKRKMENRDYRDAQEFAADVRLMFSNCYKYNPPDHDVVAMARKLQDVFEFRYAKMPDEPLEPGPL
  
Inhibitor
Name:
BDBM274248
Synonyms:
6-(4-chlorophenyl)-5-(1,5-dimethyl-6-oxo-1,6-dihydropyridin-3-yl)-1-methyl-2-(1-methyl-2-oxo-1,2-dihydropyridin-4-yl)-5,6-dihydropyrrolo[3,4-b]pyrrol-4(1H)-one | US9550796, Example 45
Type:
Small organic molecule
Emp. Form.:
C26H23ClN4O3
Mol. Mass.:
474.939
SMILES:
Cc1cc(cn(C)c1=O)N1C(c2c(cc(-c3ccn(C)c(=O)c3)n2C)C1=O)c1ccc(Cl)cc1
Structure:
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