| Reaction Details |
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 | Report a problem with these data |
| Target | Estrogen receptor |
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| Ligand | BDBM22435 |
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| Substrate/Competitor | [3H]]estradiol |
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| Meas. Tech. | Radioligand Displacement Assay |
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| pH | 7.4±n/a |
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| Temperature | 295.15±n/a K |
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| IC50 | 320 ±n/a nM |
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| Citation |  Chao, EY; Collins, JL; Gaillard, S; Miller, AB; Wang, L; Orband-Miller, LA; Nolte, RT; McDonnell, DP; Willson, TM; Zuercher, WJ Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma. Bioorg Med Chem Lett16:821-4 (2006) [PubMed] Article |
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| More Info.: | Get all data from this article, Solution Info, Assay Method |
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| Estrogen receptor |
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| Name: | Estrogen receptor |
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| Synonyms: | ER | ER-alpha | ESR | ESR1 | ESR1_HUMAN | Estradiol receptor | Estrogen receptor | Estrogen receptor (ER alpha) | Estrogen receptor (ER-alpha) | Estrogen receptor alpha (ER alpha) | Estrogen receptor alpha (ER) | NR3A1 | Nuclear receptor subfamily 3 group A member 1 |
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| Type: | Protein |
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| Mol. Mass.: | 66230.44 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P03372 |
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| Residue: | 595 |
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| Sequence: | MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAY
EFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPF
LQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAK
ETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQAC
RLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKR
SKKNSLALSLTADQMVSALLDAEPPILYSEYDPTRPFSEASMMGLLTNLADRELVHMINW
AKRVPGFVDLTLHDQVHLLECAWLEILMIGLVWRSMEHPGKLLFAPNLLLDRNQGKCVEG
MVEIFDMLLATSSRFRMMNLQGEEFVCLKSIILLNSGVYTFLSSTLKSLEEKDHIHRVLD
KITDTLIHLMAKAGLTLQQQHQRLAQLLLILSHIRHMSNKGMEHLYSMKCKNVVPLYDLL
LEMLDAHRLHAPTSRGGASVEETDQSHLATAGSTSSHSLQKYYITGEAEGFPATV
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| BDBM22435 |
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| [3H]]estradiol |
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| Name | BDBM22435 |
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| Synonyms: | 4-[(1Z)-1-{4-[2-(dimethylamino)ethoxy]phenyl}-5-hydroxy-2-phenylpent-1-en-1-yl]phenol | 4-hydroxytamoxifen (4-OHT) analog, 15 | GSK 5182 | US10934303, Example GSK5182 | US11285226, Compound GSK5182 |
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| Type | Small organic molecule |
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| Emp. Form. | C27H31NO3 |
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| Mol. Mass. | 417.5399 |
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| SMILES | CN(C)CCOc1ccc(cc1)C(=C(\CCCO)c1ccccc1)\c1ccc(O)cc1 |
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| Structure | 
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