Reaction Details |
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Target | Bromodomain-containing protein 4 [44-168]/Histone H4 |
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Ligand | BDBM209499 |
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Substrate/Competitor | n/a |
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Meas. Tech. | AlphaScreen Assay |
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IC50 | 18±n/a nM |
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Citation | Engelhardt, H; Gianni, D; Smethurst, C Substituted [1,2,4]triazolo[4,3-A]pyrazines that are BRD4 inhibitors US Patent US9266891 Publication Date 2/23/2016 |
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More Info.: | Get all data from this article, Assay Method |
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Bromodomain-containing protein 4 [44-168]/Histone H4 |
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Name: | Bromodomain-containing protein 4 [44-168]/Histone H4 |
Synonyms: | BRD4-BD1 and Histone H4 |
Type: | Protein |
Mol. Mass.: | n/a |
Description: | n/a |
Components: | This complex has 2 components. |
Component 1 |
Name: | Bromodomain-containing protein 4 [44-168] |
Synonyms: | BET bromodomain 4(1) (BRD4(1)) | BRD4 | BRD4-BD1 protein (aa 44-168) | BRD4_HUMAN | Bromodomain protein 4 (BRD4-BD1) | Bromodomain-containing protein 4 (BRD4-BD1) | Bromodomain-containing protein 4 (BRD4) (aa 44-168) | Bromodomain-containing protein 4 (BRD4-BD1) | Bromodomain-containing protein 4 bromodomain 1 (BRD4-BD1) | HUNK1 |
Type: | Enzyme Catalytic Domain |
Mol. Mass.: | 14866.49 |
Organism: | Homo sapiens (Human) |
Description: | aa (44-168) |
Residue: | 125 |
Sequence: | NPPPPETSNPNKPKRQTNQLQYLLRVVLKTLWKHQFAWPFQQPVDAVKLNLPDYYKIIKT
PMDMGTIKKRLENNYYWNAQECIQDFNTMFTNCYIYNKPGDDIVLMAEALEKLFLQKINE
LPTEE
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Component 2 |
Name: | Histone H4 |
Synonyms: | H4-16 | H4/A | H4/B | H4/C | H4/D | H4/E | H4/G | H4/H | H4/I | H4/J | H4/K | H4/M | H4/N | H4/O | H4C1 | H4F2 | H4FA | H4FB | H4FC | H4FD | H4FE | H4FG | H4FH | H4FI | H4FJ | H4FK | H4FM | H4FN | H4FO | H4_HUMAN | HIST1H4A | HIST1H4B | HIST1H4C | HIST1H4D | HIST1H4E | HIST1H4F | HIST1H4H | HIST1H4I | HIST1H4J | HIST1H4K | HIST1H4L | HIST2H4 | HIST2H4A | HIST2H4B | HIST4H4 | and | andH4/B | andH4/C | andH4/D | andH4/E | andH4/G | andH4/H | andH4/I | andH4/J | andH4/K | andH4/M | andH4/N | andH4/O |
Type: | Protein |
Mol. Mass.: | 11386.36 |
Organism: | Homo sapiens (Human) |
Description: | P62805 |
Residue: | 103 |
Sequence: | MSGRGKGGKGLGKGGAKRHRKVLRDNIQGITKPAIRRLARRGGVKRISGLIYEETRGVLK
VFLENVIRDAVTYTEHAKRKTVTAMDVVYALKRQGRTLYGFGG
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BDBM209499 |
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n/a |
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Name | BDBM209499 |
Synonyms: | US10328074, Example III-40 | US11077107, Example III-40 | US9266891, III-40 |
Type | Small organic molecule |
Emp. Form. | C24H27N9 |
Mol. Mass. | 441.5315 |
SMILES | CC(C)Nc1nc(cn2c(C)nnc12)-c1nc2cnc(cc2n1Cc1ccccn1)C(C)C |
Structure |
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