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Target
Bromodomain-containing protein 2
Ligand
BDBM50210164
Substrate
n/a
Meas. Tech.
ChEMBL_1728754 (CHEMBL4144032)
IC50
16±n/a nM
Citation
 Sharp, PP; Garnier, JM; Hatfaludi, T; Xu, Z; Segal, D; Jarman, KE; Jousset, H; Garnham, A; Feutrill, JT; Cuzzupe, A; Hall, P; Taylor, S; Walkley, CR; Tyler, D; Dawson, MA; Czabotar, P; Wilks, AF; Glaser, S; Huang, DCS; Burns, CJ Design, Synthesis, and Biological Activity of 1,2,3-Triazolobenzodiazepine BET Bromodomain Inhibitors. ACS Med Chem Lett 8:1298-1303 (2017) [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:
BDBM50210164
Synonyms:
CHEMBL2132936
Type:
Small organic molecule
Emp. Form.:
C23H25ClN4O2S
Mol. Mass.:
456.988
SMILES:
Cc1nnc2C(CC(=O)OC(C)(C)C)N=C(c3c(C)c(C)sc3-n12)c1ccc(Cl)cc1 |c:14|
Structure:
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