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Target
Bromodomain-containing protein 2
Ligand
BDBM50603097
Substrate
n/a
Meas. Tech.
ChEMBL_2243030 (CHEMBL5157240)
Kd
7.9±n/a nM
Citation
 Humphreys, PG; Atkinson, SJ; Bamborough, P; Bit, RA; Chung, CW; Craggs, PD; Cutler, L; Davis, R; Ferrie, A; Gong, G; Gordon, LJ; Gray, M; Harrison, LA; Hayhow, TG; Haynes, A; Henley, N; Hirst, DJ; Holyer, ID; Lindon, MJ; Lovatt, C; Lugo, D; McCleary, S; Molnar, J; Osmani, Q; Patten, C; Preston, A; Rioja, I; Seal, JT; Smithers, N; Sun, F; Tang, D; Taylor, S; Theodoulou, NH; Thomas, C; Watson, RJ; Wellaway, CR; Zhu, L; Tomkinson, NCO; Prinjha, RK Design, Synthesis, and Characterization of I-BET567, a Pan-Bromodomain and Extra Terminal (BET) Bromodomain Oral Candidate. J Med Chem 65:2262-2287 (2022) [PubMed] 
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:
BDBM50603097
Synonyms:
CHEMBL5195288
Type:
Small organic molecule
Emp. Form.:
C17H18ClN5O2
Mol. Mass.:
359.81
SMILES:
C[C@H]1C[C@@H](Nc2ncc(Cl)cn2)c2cc(ccc2N1C(C)=O)C(N)=O |r|
Structure:
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