Reaction Details |
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Target | Estrogen receptor |
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Ligand | BDBM269445 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1674615 (CHEMBL4024644) |
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IC50 | 669±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 |
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 |
Type: | Protein |
Mol. Mass.: | 66230.44 |
Organism: | Homo sapiens (Human) |
Description: | P03372 |
Residue: | 595 |
Sequence: | MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAY
EFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPF
LQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAK
ETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQAC
RLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKR
SKKNSLALSLTADQMVSALLDAEPPILYSEYDPTRPFSEASMMGLLTNLADRELVHMINW
AKRVPGFVDLTLHDQVHLLECAWLEILMIGLVWRSMEHPGKLLFAPNLLLDRNQGKCVEG
MVEIFDMLLATSSRFRMMNLQGEEFVCLKSIILLNSGVYTFLSSTLKSLEEKDHIHRVLD
KITDTLIHLMAKAGLTLQQQHQRLAQLLLILSHIRHMSNKGMEHLYSMKCKNVVPLYDLL
LEMLDAHRLHAPTSRGGASVEETDQSHLATAGSTSSHSLQKYYITGEAEGFPATV
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BDBM269445 |
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n/a |
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Name | BDBM269445 |
Synonyms: | (E)-3-(4-((6-hydroxy-2- (2-methylpyridin-3- yl)benzo[b]thiophen-3- yl)oxy)phenyl)acrylic acid | US10058534, 100 |
Type | Small organic molecule |
Emp. Form. | C23H17NO4S |
Mol. Mass. | 403.45 |
SMILES | Cc1ncccc1-c1sc2cc(O)ccc2c1Oc1ccc(\C=C\C(O)=O)cc1 |
Structure |
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