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Target
Bromodomain-containing protein 2
Ligand
BDBM50457496
Substrate
n/a
Meas. Tech.
ChEMBL_1759896 (CHEMBL4194904)
Ki
2.5±n/a nM
Citation
 Fidanze, SD; Liu, D; Mantei, RA; Hasvold, LA; Pratt, JK; Sheppard, GS; Wang, L; Holms, JH; Dai, Y; Aguirre, A; Bogdan, A; Dietrich, JD; Marjanovic, J; Park, CH; Hutchins, CW; Lin, X; Bui, MH; Huang, X; Wilcox, D; Li, L; Wang, R; Kovar, P; Magoc, TJ; Rajaraman, G; Albert, DH; Shen, Y; Kati, WM; McDaniel, KF Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors. Bioorg Med Chem Lett 28:1804-1810 (2018) [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:
BDBM50457496
Synonyms:
CHEMBL4217457
Type:
Small organic molecule
Emp. Form.:
C23H19F2N3O3S
Mol. Mass.:
455.477
SMILES:
Cn1cc2-c3cc(CS(C)(=O)=O)ccc3N(Cc3c[nH]c(c23)c1=O)c1ccc(F)cc1F
Structure:
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