Reaction Details |
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Target | Bromodomain-containing protein 4 |
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Ligand | BDBM50028125 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1434714 (CHEMBL3382829) |
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IC50 | 501±n/a nM |
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Citation | Gosmini, R; Nguyen, VL; Toum, J; Simon, C; Brusq, JM; Krysa, G; Mirguet, O; Riou-Eymard, AM; Boursier, EV; Trottet, L; Bamborough, P; Clark, H; Chung, CW; Cutler, L; Demont, EH; Kaur, R; Lewis, AJ; Schilling, MB; Soden, PE; Taylor, S; Walker, AL; Walker, MD; Prinjha, RK; Nicodème, E The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor. J Med Chem57:8111-31 (2014) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Bromodomain-containing protein 4 |
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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: | MSAESGPGTRLRNLPVMGDGLETSQMSTTQAQAQPQPANAASTNPPPPETSNPNKPKRQT
NQLQYLLRVVLKTLWKHQFAWPFQQPVDAVKLNLPDYYKIIKTPMDMGTIKKRLENNYYW
NAQECIQDFNTMFTNCYIYNKPGDDIVLMAEALEKLFLQKINELPTEETEIMIVQAKGRG
RGRKETGTAKPGVSTVPNTTQASTPPQTQTPQPNPPPVQATPHPFPAVTPDLIVQTPVMT
VVPPQPLQTPPPVPPQPQPPPAPAPQPVQSHPPIIAATPQPVKTKKGVKRKADTTTPTTI
DPIHEPPSLPPEPKTTKLGQRRESSRPVKPPKKDVPDSQQHPAPEKSSKVSEQLKCCSGI
LKEMFAKKHAAYAWPFYKPVDVEALGLHDYCDIIKHPMDMSTIKSKLEAREYRDAQEFGA
DVRLMFSNCYKYNPPDHEVVAMARKLQDVFEMRFAKMPDEPEEPVVAVSSPAVPPPTKVV
APPSSSDSSSDSSSDSDSSTDDSEEERAQRLAELQEQLKAVHEQLAALSQPQQNKPKKKE
KDKKEKKKEKHKRKEEVEENKKSKAKEPPPKKTKKNNSSNSNVSKKEPAPMKSKPPPTYE
SEEEDKCKPMSYEEKRQLSLDINKLPGEKLGRVVHIIQSREPSLKNSNPDEIEIDFETLK
PSTLRELERYVTSCLRKKRKPQAEKVDVIAGSSKMKGFSSSESESSSESSSSDSEDSETE
MAPKSKKKGHPGREQKKHHHHHHQQMQQAPAPVPQQPPPPPQQPPPPPPPQQQQQPPPPP
PPPSMPQQAAPAMKSSPPPFIATQVPVLEPQLPGSVFDPIGHFTQPILHLPQPELPPHLP
QPPEHSTPPHLNQHAVVSPPALHNALPQQPSRPSNRAAALPPKPARPPAVSPALTQTPLL
PQPPMAQPPQVLLEDEEPPAPPLTSMQMQLYLQQLQKVQPPTPLLPSVKVQSQPPPPLPP
PPHPSVQQQLQQQPPPPPPPQPQPPPQQQHQPPPRPVHLQPMQFSTHIQQPPPPQGQQPP
HPPPGQQPPPPQPAKPQQVIQHHHSPRHHKSDPYSTGHLREAPSPLMIHSPQMSQFQSLT
HQSPPQQNVQPKKQELRAASVVQPQPLVVVKEEKIHSPIIRSEPFSPSLRPEPPKHPESI
KAPVHLPQRPEMKPVDVGRPVIRPPEQNAPPPGAPDKDKQKQEPKTPVAPKKDLKIKNMG
SWASLVQKHPTTPSSTAKSSSDSFEQFRRAAREKEEREKALKAQAEHAEKEKERLRQERM
RSREDEDALEQARRAHEEARRRQEQQQQQRQEQQQQQQQQAAAVAAAATPQAQSSQPQSM
LDQQRELARKREQERRRREAMAATIDMNFQSDLLSIFEENLF
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BDBM50028125 |
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n/a |
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Name | BDBM50028125 |
Synonyms: | CHEMBL3353990 |
Type | Small organic molecule |
Emp. Form. | C29H33N3O2 |
Mol. Mass. | 455.5912 |
SMILES | C[C@H]1C[C@@H](Nc2ccccc2)c2cc(ccc2N1C(C)=O)-c1ccc(CN2CCOCC2)cc1 |r| |
Structure |
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