Reaction Details |
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Target | Bromodomain-containing protein 4 |
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Ligand | BDBM329747 |
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Substrate/Competitor | n/a |
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Meas. Tech. | Time-Resolved Fluorescence Resonance energy Transfer (TR-FRET) Assay |
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IC50 | 300±n/a nM |
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Citation | Schmees, N; Kuhnke, J; Haendler, B; Neuhaus, R; Lejeune, P; Siegel, S; Krüger, M; Fernandez-Montalvan, AE; Künzer, H; Gallenkamp, D BET protein-inhibiting 5-aryltriazoleazepines US Patent US9663523 Publication Date 5/30/2017 |
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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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BDBM329747 |
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n/a |
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Name | BDBM329747 |
Synonyms: | Preparation of (−)-2-[(4R)-6-(3-chlorophenyl)-1-methyl-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-4-yl]-1-(2-oxa-6-azaspiro[3.3]hept-6-yl)ethanone | US9663523, Example 11 |
Type | Small organic molecule |
Emp. Form. | C25H23ClN4O2 |
Mol. Mass. | 446.929 |
SMILES | Cc1nnc2[C@@H](CC(=O)N3CC4(COC4)C3)C=C(c3cccc(Cl)c3)c3ccccc3-n12 |r,t:18| |
Structure |
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