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TargetEstrogen receptor [Y537S]
LigandBDBM443440
Substrate/Competitorn/a
Ki 8.55±n/a nM
Citation Bastian, JACohen, JDRubio, ASall, DJMcMahon, JA Selective estrogen receptor degraders US Patent US11634426 Publication Date 4/25/2023
More Info.:Get all data from this article,  Assay Method
 
Estrogen receptor [Y537S]
Name:Estrogen receptor [Y537S]
Synonyms:ESR | ESR1 | ESR1_HUMAN | Estrogen receptor (Y537S) | Estrogen receptor alpha Y537S | NR3A1
Type:Enzyme Catalytic Domain
Mol. Mass.:66154.35
Organism:Homo sapiens (Human)
Description:P03372[Y537S]
Residue:595
Sequence:
MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAY
EFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPF
LQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAK
ETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQAC
RLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKR
SKKNSLALSLTADQMVSALLDAEPPILYSEYDPTRPFSEASMMGLLTNLADRELVHMINW
AKRVPGFVDLTLHDQVHLLECAWLEILMIGLVWRSMEHPGKLLFAPNLLLDRNQGKCVEG
MVEIFDMLLATSSRFRMMNLQGEEFVCLKSIILLNSGVYTFLSSTLKSLEEKDHIHRVLD
KITDTLIHLMAKAGLTLQQQHQRLAQLLLILSHIRHMSNKGMEHLYSMKCKNVVPLSDLL
LEMLDAHRLHAPTSRGGASVEETDQSHLATAGSTSSHSLQKYYITGEAEGFPATV
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM443440
n/a
NameBDBM443440
Synonyms:US10654866, Example 7 | US11634426, Example 7
TypeSmall organic molecule
Emp. Form.C29H27FN2O3
Mol. Mass.470.5347
SMILESCc1ccc-2c(OC(c3ccc(OCCN4CC(CF)C4)cc3)c3c-2cnc2cc(O)ccc32)c1
Structure
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