| Reaction Details |
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 | Report a problem with these data |
| Target | Estrogen receptor [298-554,Y537S] |
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| Ligand | BDBM521418 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | Biochemical Antagonist Activity on Wild Type (WT) and Mutants |
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| IC50 | 7.00±n/a nM |
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| Citation |  Bouaboula, M; Brollo, M; Certal, V; El-Ahmad, Y; Filoche-Romme, B; Halley, F; McCort, G; Schio, L; Tabart, M; Terrier, C; Thompson, F Substituted N-(3-fluoropropyl)-pyrrolidine compounds, processes for their preparation and therapeutic uses thereof US Patent US11149031 Publication Date 10/19/2021 |
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| More Info.: | Get all data from this article, Assay Method |
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| Estrogen receptor [298-554,Y537S] |
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| Name: | Estrogen receptor [298-554,Y537S] |
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| Synonyms: | ESR | ESR1 | ESR1_HUMAN | Estrogen Receptor alpha (aa 298-554, Y537S) | NR3A1 |
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| Type: | Enzyme Catalytic Domain |
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| Mol. Mass.: | 29151.56 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P03372[298-554,Y537S] |
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| Residue: | 256 |
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| Sequence: | KRSKKNSLALSLTADQMVSALLDAEPPILYSEYDPTRPFSEASMMGLLTNLADRELVHMI
NWAKRVPGFVDLTLHDQVHLLECAWLEILMIGLVWRSMEHPGKLLFAPNLLLDRNQGKCV
EGMVEIFDMLLATSSRFRMMNLQGEEFVCLKSIILLNSGVYTFLSSTLKSLEEKDHIHRV
LDKITDTLIHLMAKAGLTLQQQHQRLAQLLLILSHIRHMSNKGMEHLYSMKCKNVVPLSD
LLLEMLDAHRLHAPTS
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| BDBM521418 |
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| n/a |
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| Name | BDBM521418 |
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| Synonyms: | 6-(2,2- dimethylindolin- 5-yl)-5-[6-[(3S)- 1-(3- fluoropropyl)pyr- rolidin-3-yl]oxy- 3-pyridyl]-8,9- dihydro-7H- benzo[7]annulen- 2-ol | US11149031, Example 242 |
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| Type | Small organic molecule |
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| Emp. Form. | C33H38FN3O2 |
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| Mol. Mass. | 527.6721 |
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| SMILES | CC1(C)Cc2cc(ccc2N1)C1=C(c2ccc(O[C@H]3CCN(CCCF)C3)nc2)c2ccc(O)cc2CCC1 |r,c:13| |
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| Structure | 
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