Reaction Details
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Bromodomain-containing protein 2 [60-463]
Ligand
BDBM274257
Substrate
n/a
Meas. Tech.
TR-FRET In-Vitro Binding Assay
pH
7.5±n/a
IC50
27.0±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 More Info.:
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:
Homo sapiens (Human)
Description:
P25440[60-463]
Residue:
404
Sequence:
NPPPPEVSNPKKPGRVTNQLQYLHKVVMKALWKHQFAWPFRQPVDAVKLGLPDYHKIIKQPMDMGTIKRRLENNYYWAASECMQDFNTMFTNCYIYNKPTDDIVLMAQTLEKIFLQKVASMPQEEQELVVTIPKNSHKKGAKLAALQGSVTSAHQVPAVSSVSHTALYTPPPEIPTTVLNIPHPSVISSPLLKSLHSAGPPLLAVTAAPPAQPLAKKKGVKRKADTTTPTPTAILAPGSPASPPGSLEPKAARLPPMRRESGRPIKPPRKDLPDSQQQHQSSKKGKLSEQLKHCNGILKELLSKKHAAYAWPFYKPVDASALGLHDYHDIIKHPMDLSTVKRKMENRDYRDAQEFAADVRLMFSNCYKYNPPDHDVVAMARKLQDVFEFRYAKMPDEPLEPGPL
Inhibitor
Name:
BDBM274257
Synonyms:
(R)-6-(4-chlorophenyl)-2-(2,4-dimethoxypyrimidin-5-yl)-5-(1,5-dimethyl-6-oxo-1,6-dihydropyridin-3-yl)-1-methyl-5,6-dihydropyrrolo[3,4-b]pyrrol-4(1H)-one | US9550796, Example 54
Type:
Small organic molecule
Emp. Form.:
C26H24ClN5O4
Mol. Mass.:
505.953
SMILES:
COc1ncc(-c2cc3C(=O)N([C@@H](c3n2C)c2ccc(Cl)cc2)c2cc(C)c(=O)n(C)c2)c(OC)n1 |r|
Structure:
