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Target
Bromodomain-containing protein 2
Ligand
BDBM264438
Substrate
n/a
Meas. Tech.
TR-FRET In-Vitro Binding Assays for BRD2, BRD3, and BRD4
pH
7.5±n/a
IC50
32.0±n/a nM
Comments
extracted
Citation
 Blank, J; Cotesta, S; Guagnano, V; Rueeger, H Pyrazolo-pyrrolidin-4-one derivatives and their use in the treatment of disease US Patent  US9714249 Publication Date 7/25/2017 
Target
Name:
Bromodomain-containing protein 2
Synonyms:
BRD2 | BRD2_HUMAN | Bromodomain and extra-terminal motif (BET) | Bromodomain-containing protein 2 | Bromodomain-containing protein 2 (BRD2) | KIAA9001 | RING3
Type:
Protein
Mol. Mass.:
88085.95
Organism:
Homo sapiens (Human)
Description:
P25440
Residue:
801
Sequence:
MLQNVTPHNKLPGEGNAGLLGLGPEAAAPGKRIRKPSLLYEGFESPTMASVPALQLTPANPPPPEVSNPKKPGRVTNQLQYLHKVVMKALWKHQFAWPFRQPVDAVKLGLPDYHKIIKQPMDMGTIKRRLENNYYWAASECMQDFNTMFTNCYIYNKPTDDIVLMAQTLEKIFLQKVASMPQEEQELVVTIPKNSHKKGAKLAALQGSVTSAHQVPAVSSVSHTALYTPPPEIPTTVLNIPHPSVISSPLLKSLHSAGPPLLAVTAAPPAQPLAKKKGVKRKADTTTPTPTAILAPGSPASPPGSLEPKAARLPPMRRESGRPIKPPRKDLPDSQQQHQSSKKGKLSEQLKHCNGILKELLSKKHAAYAWPFYKPVDASALGLHDYHDIIKHPMDLSTVKRKMENRDYRDAQEFAADVRLMFSNCYKYNPPDHDVVAMARKLQDVFEFRYAKMPDEPLEPGPLPVSTAMPPGLAKSSSESSSEESSSESSSEEEEEEDEEDEEEEESESSDSEEERAHRLAELQEQLRAVHEQLAALSQGPISKPKRKREKKEKKKKRKAEKHRGRAGADEDDKGPRAPRPPQPKKSKKASGSGGGSAALGPSGFGPSGGSGTKLPKKATKTAPPALPTGYDSEEEEESRPMSYDEKRQLSLDINKLPGEKLGRVVHIIQAREPSLRDSNPEEIEIDFETLKPSTLRELERYVLSCLRKKPRKPYTIKKPVGKTKEELALEKKRELEKRLQDVSGQLNSTKKPPKKANEKTESSSAQQVAVSRLSASSSSSDSSSSSSSSSSSDTSDSDSG
  
Inhibitor
Name:
BDBM264438
Synonyms:
5-(5-chloro-1-methyl-6-oxo-1,6-dihydropyridin-3-yl)-6-(4-chlorophenyl)-2-(2-methoxypyridin-3-yl)-3-methyl-5,6-dihydropyrrolo[3,4-c]pyrazol-4(2H)-one | US9714249, 7b
Type:
Small organic molecule
Emp. Form.:
C24H19Cl2N5O3
Mol. Mass.:
496.345
SMILES:
COc1ncccc1-n1nc(C)c2C(=O)N([C@@H](c12)c1ccc(Cl)cc1)c1cc(Cl)c(=O)n(C)c1 |r|
Structure:
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