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TargetEstrogen receptor
LigandBDBM50517560
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1869253 (CHEMBL4370319)
IC50 0.316228±n/a nM
Citation Scott, JSBailey, AButtar, DCarbajo, RJCurwen, JDavey, PRJDavies, RDMDegorce, SLDonald, CGangl, EGreenwood, RGroombridge, SDJohnson, TLamont, SLawson, MLister, AMorrow, CJMoss, TAPink, JHPolanski, R Tricyclic Indazoles-A Novel Class of Selective Estrogen Receptor Degrader Antagonists. J Med Chem62:1593-1608 (2019) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Estrogen receptor
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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50517560
n/a
NameBDBM50517560
Synonyms:CHEMBL4583286
TypeSmall organic molecule
Emp. Form.C24H24F3N3O3
Mol. Mass.459.4609
SMILESCOc1cc(\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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