Reaction Details
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Bromodomain-containing protein 2 [60-463]
Ligand
BDBM274224
Substrate
n/a
Meas. Tech.
TR-FRET In-Vitro Binding Assay
pH
7.5±n/a
IC50
23.0±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:
BDBM274224
Synonyms:
6-(4-chlorophenyl)-5-(3,7-di methyl-3H-[1,2,3]triazolo[4,5-b]pyridin-5-yl)-3-methyl-1-(1-methylazetidin-3-yl)-5,6-dihydropyrrolo[3,4-b]pyrrol-4(1H)-one | US9550796, Example 20
Type:
Small organic molecule
Emp. Form.:
C24H24ClN7O
Mol. Mass.:
461.947
SMILES:
CN1CC(C1)n1cc(C)c2C(=O)N(C(c12)c1ccc(Cl)cc1)c1cc(C)c2nnn(C)c2n1
Structure:
