| Reaction Details |
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 | Report a problem with these data |
| Target | Estrogen receptor |
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| Ligand | BDBM368200 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1736208 (CHEMBL4151744) |
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| IC50 | 0.300000±n/a nM |
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| Citation |  Nagasawa, J; Govek, S; Kahraman, M; Lai, A; Bonnefous, C; Douglas, K; Sensintaffar, J; Lu, N; Lee, K; Aparicio, A; Kaufman, J; Qian, J; Shao, G; Prudente, R; Joseph, JD; Darimont, B; Brigham, D; Maheu, K; Heyman, R; Rix, PJ; Hager, JH; Smith, ND Identification of an Orally Bioavailable Chromene-Based Selective Estrogen Receptor Degrader (SERD) That Demonstrates Robust Activity in a Model of Tamoxifen-Resistant Breast Cancer. J Med Chem61:7917-7928 (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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| BDBM368200 |
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| n/a |
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| Name | BDBM368200 |
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| Synonyms: | 3-(3-Hydroxyphenyl)-4-methyl-2-(4-(2-(3-methylazetidin-1-yl)ethoxy)phenyl)-2H-chromen-6-ol | US10227334, Example 4 |
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| Type | Small organic molecule |
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| Emp. Form. | C28H29NO4 |
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| Mol. Mass. | 443.5342 |
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| SMILES | CC1CN(CCOc2ccc(cc2)C2Oc3ccc(O)cc3C(C)=C2c2cccc(O)c2)C1 |c:25| |
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| Structure | 
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