Reaction Details |
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Target | Estrogen receptor [298-554,Y537S] |
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Ligand | BDBM521194 |
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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 | 15.0±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] |
Synonyms: | ESR | ESR1 | ESR1_HUMAN | Estrogen Receptor alpha (aa 298-554, Y537S) | NR3A1 |
Type: | Enzyme Catalytic Domain |
Mol. Mass.: | 29151.56 |
Organism: | Homo sapiens (Human) |
Description: | P03372[298-554,Y537S] |
Residue: | 256 |
Sequence: | KRSKKNSLALSLTADQMVSALLDAEPPILYSEYDPTRPFSEASMMGLLTNLADRELVHMI
NWAKRVPGFVDLTLHDQVHLLECAWLEILMIGLVWRSMEHPGKLLFAPNLLLDRNQGKCV
EGMVEIFDMLLATSSRFRMMNLQGEEFVCLKSIILLNSGVYTFLSSTLKSLEEKDHIHRV
LDKITDTLIHLMAKAGLTLQQQHQRLAQLLLILSHIRHMSNKGMEHLYSMKCKNVVPLSD
LLLEMLDAHRLHAPTS
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BDBM521194 |
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n/a |
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Name | BDBM521194 |
Synonyms: | 3-(4-chloro-2- fluoro-phenyl)- 4-[4-[(3S)-1-(3- fluoropropyl)pyr- rolidin-3- yl]oxyphenyl]- 2H- thiochromen-7- ol | US11149031, Example 18 |
Type | Small organic molecule |
Emp. Form. | C28H26ClF2NO2S |
Mol. Mass. | 514.026 |
SMILES | Oc1ccc2C(=C(CSc2c1)c1ccc(Cl)cc1F)c1ccc(O[C@H]2CCN(CCCF)C2)cc1 |r,c:5| |
Structure |
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