| Reaction Details |
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 | Report a problem with these data |
| Target | Estrogen receptor |
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| Ligand | BDBM50180684 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1674615 (CHEMBL4024644) |
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| IC50 | 3.0±n/a nM |
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| Citation |  Tria, GS; Abrams, T; Baird, J; Burks, HE; Firestone, B; Gaither, LA; Hamann, LG; He, G; Kirby, CA; Kim, S; Lombardo, F; Macchi, KJ; McDonnell, DP; Mishina, Y; Norris, JD; Nunez, J; Springer, C; Sun, Y; Thomsen, NM; Wang, C; Wang, J; Yu, B; Tiong-Yip, CL; Peukert, S Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer. J Med Chem61:2837-2864 (2018) [PubMed] Article |
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| More Info.: | Get all data from this article, 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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| BDBM50180684 |
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| n/a |
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| Name | BDBM50180684 |
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| Synonyms: | 4-OHT | Afimoxifene | TamoGel |
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| Type | Small organic molecule |
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| Emp. Form. | C26H29NO2 |
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| Mol. Mass. | 387.514 |
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| SMILES | CC\C(=C(/c1ccccc1)c1ccc(OCCN(C)C)cc1)c1ccc(O)cc1 |
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| Structure | 
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