| Reaction Details |
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 | Report a problem with these data |
| Target | Estrogen receptor |
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| Ligand | BDBM368203 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1736208 (CHEMBL4151744) |
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| IC50 | 0.100000±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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| BDBM368203 |
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| n/a |
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| Name | BDBM368203 |
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| Synonyms: | US10227334, Example (S)-3-(3-Hydroxyphenyl)-4-methyl-2-(4-((S)-2-((R)-3-methylpyrrolidin-1- yl)propoxy)phenyl)-2H-chromen-6-ol |
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| Type | Small organic molecule |
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| Emp. Form. | C30H33NO4 |
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| Mol. Mass. | 471.5873 |
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| SMILES | C[C@@H](COc1ccc(cc1)[C@@H]1Oc2ccc(O)cc2C(C)=C1c1cccc(O)c1)N1CC[C@@H](C)C1 |c:22| |
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| Structure | 
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