Target
Bromodomain-containing protein 4
Ligand
BDBM50178163
Substrate
n/a
Meas. Tech.
ChEMBL_1582082 (CHEMBL3817159)
IC50
7000±n/a nM
Citation
 Taylor, AMCôté, AHewitt, MCPastor, RLeblanc, YNasveschuk, CGRomero, FACrawford, TDCantone, NJayaram, HSetser, JMurray, JBeresini, MHde Leon Boenig, GChen, ZConery, ARCummings, RTDakin, LAFlynn, EMHuang, OWKaufman, SKeller, PJKiefer, JRLai, TLi, YLiao, JLiu, WLu, HPardo, ETsui, VWang, JWang, YXu, ZYan, FYu, DZawadzke, LZhu, XZhu, XSims, RJCochran, AGBellon, SAudia, JEMagnuson, SAlbrecht, BK Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637). ACS Med Chem Lett 7:531-6 (2016) [PubMed]  Article 
Target
Name:
Bromodomain-containing protein 4
Synonyms:
BRD4 | BRD4_HUMAN | Bromodomain-containing protein 4 (BRD4) | HUNK1 | Protein HUNK1
Type:
Protein
Mol. Mass.:
152264.84
Organism:
Homo sapiens (Human)
Description:
O60885
Residue:
1362
Sequence:
MSAESGPGTRLRNLPVMGDGLETSQMSTTQAQAQPQPANAASTNPPPPETSNPNKPKRQTNQLQYLLRVVLKTLWKHQFAWPFQQPVDAVKLNLPDYYKIIKTPMDMGTIKKRLENNYYWNAQECIQDFNTMFTNCYIYNKPGDDIVLMAEALEKLFLQKINELPTEETEIMIVQAKGRGRGRKETGTAKPGVSTVPNTTQASTPPQTQTPQPNPPPVQATPHPFPAVTPDLIVQTPVMTVVPPQPLQTPPPVPPQPQPPPAPAPQPVQSHPPIIAATPQPVKTKKGVKRKADTTTPTTIDPIHEPPSLPPEPKTTKLGQRRESSRPVKPPKKDVPDSQQHPAPEKSSKVSEQLKCCSGILKEMFAKKHAAYAWPFYKPVDVEALGLHDYCDIIKHPMDMSTIKSKLEAREYRDAQEFGADVRLMFSNCYKYNPPDHEVVAMARKLQDVFEMRFAKMPDEPEEPVVAVSSPAVPPPTKVVAPPSSSDSSSDSSSDSDSSTDDSEEERAQRLAELQEQLKAVHEQLAALSQPQQNKPKKKEKDKKEKKKEKHKRKEEVEENKKSKAKEPPPKKTKKNNSSNSNVSKKEPAPMKSKPPPTYESEEEDKCKPMSYEEKRQLSLDINKLPGEKLGRVVHIIQSREPSLKNSNPDEIEIDFETLKPSTLRELERYVTSCLRKKRKPQAEKVDVIAGSSKMKGFSSSESESSSESSSSDSEDSETEMAPKSKKKGHPGREQKKHHHHHHQQMQQAPAPVPQQPPPPPQQPPPPPPPQQQQQPPPPPPPPSMPQQAAPAMKSSPPPFIATQVPVLEPQLPGSVFDPIGHFTQPILHLPQPELPPHLPQPPEHSTPPHLNQHAVVSPPALHNALPQQPSRPSNRAAALPPKPARPPAVSPALTQTPLLPQPPMAQPPQVLLEDEEPPAPPLTSMQMQLYLQQLQKVQPPTPLLPSVKVQSQPPPPLPPPPHPSVQQQLQQQPPPPPPPQPQPPPQQQHQPPPRPVHLQPMQFSTHIQQPPPPQGQQPPHPPPGQQPPPPQPAKPQQVIQHHHSPRHHKSDPYSTGHLREAPSPLMIHSPQMSQFQSLTHQSPPQQNVQPKKQELRAASVVQPQPLVVVKEEKIHSPIIRSEPFSPSLRPEPPKHPESIKAPVHLPQRPEMKPVDVGRPVIRPPEQNAPPPGAPDKDKQKQEPKTPVAPKKDLKIKNMGSWASLVQKHPTTPSSTAKSSSDSFEQFRRAAREKEEREKALKAQAEHAEKEKERLRQERMRSREDEDALEQARRAHEEARRRQEQQQQQRQEQQQQQQQQAAAVAAAATPQAQSSQPQSMLDQQRELARKREQERRRREAMAATIDMNFQSDLLSIFEENLF
  
Inhibitor
Name:
BDBM50178163
Synonyms:
CHEMBL3813846 | US10206931, Example 286
Type:
Small organic molecule
Emp. Form.:
C23H22N2O2
Mol. Mass.:
358.433
SMILES:
C[C@@H]1CC(=O)Nc2cccc(-c3cccc(OCc4ccccc4)c3)c2N1 |r|
Structure:
Search PDB for entries with ligand similarity: