Reaction Details |
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Target | Estrogen receptor |
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Ligand | BDBM50523049 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1888881 (CHEMBL4390558) |
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IC50 | 0.030000±n/a nM |
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Citation | Labadie, SS; Li, J; Blake, RA; Chang, JH; Goodacre, S; Hartman, SJ; Liang, W; Kiefer, JR; Kleinheinz, T; Lai, T; Liao, J; Ortwine, DF; Mody, V; Ray, NC; Roussel, F; Vinogradova, M; Yeap, SK; Zhang, B; Zheng, X; Zbieg, JR; Liang, J; Wang, X Discovery of a C-8 hydroxychromene as a potent degrader of estrogen receptor alpha with improved rat oral exposure over GDC-0927. Bioorg Med Chem Lett29:2090-2093 (2019) [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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BDBM50523049 |
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n/a |
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Name | BDBM50523049 |
Synonyms: | CHEMBL4441471 |
Type | Small organic molecule |
Emp. Form. | C28H26ClF2NO3 |
Mol. Mass. | 497.961 |
SMILES | CC1=C([C@@H](Oc2ccc(O)c(Cl)c12)c1ccc(OCCN2CC(CF)C2)cc1)c1ccc(F)cc1 |r,t:1| |
Structure |
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