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Target
Bromodomain-containing protein 2
Ligand
BDBM50558065
Substrate
n/a
Meas. Tech.
ChEMBL_2061742 (CHEMBL4716995)
IC50
3.0±n/a nM
Citation
 Taylor, AM; Vaswani, RG; Gehling, VS; Hewitt, MC; Leblanc, Y; Audia, JE; Bellon, S; Cummings, RT; Côté, A; Harmange, JC; Jayaram, H; Joshi, S; Lora, JM; Mertz, JA; Neiss, A; Pardo, E; Nasveschuk, CG; Poy, F; Sandy, P; Setser, JW; Sims, RJ; Tang, Y; Albrecht, BK Discovery of Benzotriazolo[4,3-d][1,4]diazepines as Orally Active Inhibitors of BET Bromodomains. ACS Med Chem Lett 7:145-50 (2016) [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:
BDBM50558065
Synonyms:
CHEMBL4780530
Type:
Small organic molecule
Emp. Form.:
C23H21ClN6
Mol. Mass.:
416.906
SMILES:
C[C@@H]1CN(c2ccc(Cl)cc2)c2cc(ccc2-n2c(C)nnc12)-c1ccc(N)nc1 |r|
Structure:
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