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TargetEstrogen receptor
LigandBDBM269399
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1674615 (CHEMBL4024644)
IC50 1.000000±n/a nM
Citation Tria, GSAbrams, TBaird, JBurks, HEFirestone, BGaither, LAHamann, LGHe, GKirby, CAKim, SLombardo, FMacchi, KJMcDonnell, DPMishina, YNorris, JDNunez, JSpringer, CSun, YThomsen, NMWang, CWang, JYu, BTiong-Yip, CLPeukert, S Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer. J Med Chem61:2837-2864 (2018) [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:
BDBM269399
n/a
NameBDBM269399
Synonyms:US10058534, 54
TypeSmall organic molecule
Emp. Form.C24H18N4O3S
Mol. Mass.442.49
SMILESCn1nnnc1\C=C\c1ccc(Oc2c(sc3cc(O)ccc23)-c2ccc(O)cc2)cc1
Structure
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