Reaction Details |
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Target | Estrogen receptor [298-554,Y537S] |
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Ligand | BDBM521182 |
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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 | 8.00±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] |
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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BDBM521182 |
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n/a |
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Name | BDBM521182 |
Synonyms: | 7-(2-fluoro-4- hydroxy- phenyl)-8-[4- [(3S)-1-(3- fluoropropyl)pyr- rolidin-3- yl]oxyphenyl]- 5,6- dihydronaphtha- len-2-ol | US11149031, Example 6 |
Type | Small organic molecule |
Emp. Form. | C29H29F2NO3 |
Mol. Mass. | 477.5423 |
SMILES | Oc1ccc(C2=C(c3ccc(O[C@H]4CCN(CCCF)C4)cc3)c3cc(O)ccc3CC2)c(F)c1 |r,c:5| |
Structure |
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