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Target
Bromodomain-containing protein 4
Ligand
BDBM50200384
Substrate
n/a
Meas. Tech.
ChEMBL_1622038 (CHEMBL3864390)
IC50
13000±n/a nM
Citation
 Crawford, TD; Romero, FA; Lai, KW; Tsui, V; Taylor, AM; de Leon Boenig, G; Noland, CL; Murray, J; Ly, J; Choo, EF; Hunsaker, TL; Chan, EW; Merchant, M; Kharbanda, S; Gascoigne, KE; Kaufman, S; Beresini, MH; Liao, J; Liu, W; Chen, KX; Chen, Z; Conery, AR; Côté, A; Jayaram, H; Jiang, Y; Kiefer, JR; Kleinheinz, T; Li, Y; Maher, J; Pardo, E; Poy, F; Spillane, KL; Wang, F; Wang, J; Wei, X; Xu, Z; Xu, Z; Yen, I; Zawadzke, L; Zhu, X; Bellon, S; Cummings, R; Cochran, AG; Albrecht, BK; Magnuson, S Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300. J Med Chem 59:10549-10563 (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:
BDBM50200384
Synonyms:
CHEMBL3968533 | US9763922, Example 299
Type:
Small organic molecule
Emp. Form.:
C22H25FN6O2
Mol. Mass.:
424.4713
SMILES:
CC(=O)N1CCc2c(C1)c(Nc1ccc(cc1F)-c1cnn(C)c1)nn2[C@@H]1CCOC1 |r|
Structure:
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