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Target
Bromodomain-containing protein 2
Ligand
BDBM50441172
Substrate
n/a
Meas. Tech.
ChEMBL_985088 (CHEMBL2433593)
IC50
1585±n/a nM
Citation
 Mirguet, O; Gosmini, R; Toum, J; Clément, CA; Barnathan, M; Brusq, JM; Mordaunt, JE; Grimes, RM; Crowe, M; Pineau, O; Ajakane, M; Daugan, A; Jeffrey, P; Cutler, L; Haynes, AC; Smithers, NN; Chung, CW; Bamborough, P; Uings, IJ; Lewis, A; Witherington, J; Parr, N; Prinjha, RK; Nicodème, E Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains. J Med Chem 56:7501-15 (2013) [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:
BDBM50441172
Synonyms:
CHEMBL2430896
Type:
Small organic molecule
Emp. Form.:
C26H23N5O2
Mol. Mass.:
437.4931
SMILES:
Cc1nnc2C(NC(=O)OCc3ccccc3)N=C(c3ccc(C)cc3)c3ccccc3-n12 |t:18|
Structure:
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