Reaction Details |
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Target | Estrogen receptor |
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Ligand | BDBM50090462 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1497878 (CHEMBL3582785) |
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IC50 | 6.1±n/a nM |
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Citation | Lai, A; Kahraman, M; Govek, S; Nagasawa, J; Bonnefous, C; Julien, J; Douglas, K; Sensintaffar, J; Lu, N; Lee, KJ; Aparicio, A; Kaufman, J; Qian, J; Shao, G; Prudente, R; Moon, MJ; Joseph, JD; Darimont, B; Brigham, D; Grillot, K; Heyman, R; Rix, PJ; Hager, JH; Smith, ND Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts. J Med Chem58:4888-904 (2015) [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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BDBM50090462 |
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n/a |
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Name | BDBM50090462 |
Synonyms: | CHEMBL3581693 |
Type | Small organic molecule |
Emp. Form. | C26H20ClFN2O2 |
Mol. Mass. | 446.901 |
SMILES | CC\C(=C(\c1ccc(\C=C\C(O)=O)cc1)c1ccc2[nH]ncc2c1)c1ccc(F)cc1Cl |
Structure |
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