| Reaction Details |
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 | Report a problem with these data |
| Target | Estrogen receptor |
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| Ligand | BDBM50090462 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_2118286 (CHEMBL4827352) |
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| IC50 | 5.3±n/a nM |
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| Citation |  Liang, J; Zbieg, JR; Blake, RA; Chang, JH; Daly, S; DiPasquale, AG; Friedman, LS; Gelzleichter, T; Gill, M; Giltnane, JM; Goodacre, S; Guan, J; Hartman, SJ; Ingalla, ER; Kategaya, L; Kiefer, JR; Kleinheinz, T; Labadie, SS; Lai, T; Li, J; Liao, J; Liu, Z; Mody, V; McLean, N; Metcalfe, C; Nannini, MA; Oeh, J; O'Rourke, MG; Ortwine, DF; Ran, Y; Ray, NC; Roussel, F; Sambrone, A; Sampath, D; Schutt, LK; Vinogradova, M; Wai, J; Wang, T; Wertz, IE; White, JR; Yeap, SK; Young, A; Zhang, B; Zheng, X; Zhou, W; Zhong, Y; Wang, X GDC-9545 (Giredestrant): A Potent and Orally Bioavailable Selective Estrogen Receptor Antagonist and Degrader with an Exceptional Preclinical Profile for ER+ Breast Cancer. J Med Chem64:11841-11856 (2021) [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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| BDBM50090462 |
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| n/a |
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| Name | BDBM50090462 |
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| Synonyms: | CHEMBL3581693 | US20240043442, Example GDC-0810 |
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| Type | Small organic molecule |
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| Emp. Form. | C26H20ClFN2O2 |
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| Mol. Mass. | 446.901 |
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| SMILES | CC\C(=C(\c1ccc(\C=C\C(O)=O)cc1)c1ccc2[nH]ncc2c1)c1ccc(F)cc1Cl |
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| Structure | 
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