Reaction Details |
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Target | Bromodomain-containing protein 4 [44-477] |
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Ligand | BDBM274318 |
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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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BDBM274318 |
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n/a |
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Name | BDBM274318 |
Synonyms: | 6-(4-chlorophenyl)-3-cyclopropyl-2-(3,6-dihydro-2H-pyran-4-yl)-5-(3,8-di methyl-[1,2,4]triazolo[4,3-a]pyridin-6-yl)-1-methyl-5,6-dihydropyrrolo[3,4-b]pyrrol-4(1H)-one | US9550796, Example 119 |
Type | Small organic molecule |
Emp. Form. | C29H28ClN5O2 |
Mol. Mass. | 514.018 |
SMILES | Cc1nnc2c(C)cc(cn12)N1C(c2c(C1=O)c(C1CC1)c(C1=CCOCC1)n2C)c1ccc(Cl)cc1 |t:26| |
Structure |
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