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Target
Bromodomain-containing protein 2
Ligand
BDBM50103503
Substrate
n/a
Meas. Tech.
ChEMBL_1903710 (CHEMBL4405932)
Kd
251±n/a nM
Citation
 Liu, Z; Chen, H; Wang, P; Li, Y; Wold, EA; Leonard, PG; Joseph, S; Brasier, AR; Tian, B; Zhou, J Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation. J Med Chem 63:5242-5256 (2020) [PubMed]  Article 
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:
BDBM50103503
Synonyms:
CHEMBL2393130 | US11117865, Compound RVX-208
Type:
Small organic molecule
Emp. Form.:
C20H22N2O5
Mol. Mass.:
370.3991
SMILES:
COc1cc(OC)c2c(c1)nc([nH]c2=O)-c1cc(C)c(OCCO)c(C)c1
Structure:
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