Reaction Details |
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Target | Estrogen receptor |
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Ligand | BDBM50517555 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1869253 (CHEMBL4370319) |
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IC50 | 1.6±n/a nM |
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Citation | Scott, JS; Bailey, A; Buttar, D; Carbajo, RJ; Curwen, J; Davey, PRJ; Davies, RDM; Degorce, SL; Donald, C; Gangl, E; Greenwood, R; Groombridge, SD; Johnson, T; Lamont, S; Lawson, M; Lister, A; Morrow, CJ; Moss, TA; Pink, JH; Polanski, R Tricyclic Indazoles-A Novel Class of Selective Estrogen Receptor Degrader Antagonists. J Med Chem62:1593-1608 (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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BDBM50517555 |
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n/a |
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Name | BDBM50517555 |
Synonyms: | CHEMBL4515724 |
Type | Small organic molecule |
Emp. Form. | C24H26FN3O2 |
Mol. Mass. | 407.4805 |
SMILES | C[C@@H]1Cc2c(ccc3[nH]ncc23)[C@H](N1CC(C)(C)F)c1ccc(\C=C\C(O)=O)cc1 |r| |
Structure |
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