Reaction Details |
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Target | Estrogen receptor |
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Ligand | BDBM50517560 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1869253 (CHEMBL4370319) |
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IC50 | 0.316228±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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BDBM50517560 |
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n/a |
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Name | BDBM50517560 |
Synonyms: | CHEMBL4583286 |
Type | Small organic molecule |
Emp. Form. | C24H24F3N3O3 |
Mol. Mass. | 459.4609 |
SMILES | COc1cc(\C=C\C(O)=O)cc(F)c1[C@H]1N(CC(C)(F)F)[C@H](C)Cc2c1ccc1[nH]ncc21 |r| |
Structure |
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