Reaction Details |
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Target | Bromodomain-containing protein 4 [44-477] |
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Ligand | BDBM274222 |
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Substrate/Competitor | n/a |
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Meas. Tech. | TR-FRET In-Vitro Binding Assay |
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pH | 7.5±n/a |
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IC50 | <11.0±n/a nM |
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Comments | extracted |
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Citation | Rueger, H; Blank, J; Bordas, V; Cotesta, S; Bold, G; Guagnano, V; Vaupel, A Pyrrolopyrrolone derivatives and their use as BET inhibitors US Patent US9550796 Publication Date 1/24/2017 |
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More Info.: | Get all data from this article, Assay Method |
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Bromodomain-containing protein 4 [44-477] |
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Name: | Bromodomain-containing protein 4 [44-477] |
Synonyms: | BRD4 | BRD4_HUMAN | Bromodomain-containing protein 4 | HUNK1 |
Type: | Enzyme Catalytic Domain (aa 44-477) |
Mol. Mass.: | 48692.13 |
Organism: | Homo sapiens (Human) |
Description: | O60885[44-477] |
Residue: | 434 |
Sequence: | NPPPPETSNPNKPKRQTNQLQYLLRVVLKTLWKHQFAWPFQQPVDAVKLNLPDYYKIIKT
PMDMGTIKKRLENNYYWNAQECIQDFNTMFTNCYIYNKPGDDIVLMAEALEKLFLQKINE
LPTEETEIMIVQAKGRGRGRKETGTAKPGVSTVPNTTQASTPPQTQTPQPNPPPVQATPH
PFPAVTPDLIVQTPVMTVVPPQPLQTPPPVPPQPQPPPAPAPQPVQSHPPIIAATPQPVK
TKKGVKRKADTTTPTTIDPIHEPPSLPPEPKTTKLGQRRESSRPVKPPKKDVPDSQQHPA
PEKSSKVSEQLKCCSGILKEMFAKKHAAYAWPFYKPVDVEALGLHDYCDIIKHPMDMSTI
KSKLEAREYRDAQEFGADVRLMFSNCYKYNPPDHEVVAMARKLQDVFEMRFAKMPDEPEE
PVVAVSSPAVPPPT
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BDBM274222 |
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n/a |
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Name | BDBM274222 |
Synonyms: | 1-(1-acetylazetidin-3-yl)-6-(4-chlorophenyl)-3-cyclopropyl-5-(3,8-dimethyl-[1,2,4]triazolo[4,3-a]pyridin-6-yl)-5,6-dihydropyrrolo[3,4-b]pyrrol-4(1H)-one | US9550796, Example 17 |
Type | Small organic molecule |
Emp. Form. | C28H27ClN6O2 |
Mol. Mass. | 515.006 |
SMILES | CC(=O)N1CC(C1)n1cc(C2CC2)c2C(=O)N(C(c12)c1ccc(Cl)cc1)c1cc(C)c2nnc(C)n2c1 |
Structure |
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