Reaction Details |
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Target | Estrogen receptor [Y537S] |
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Ligand | BDBM443448 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ERalpha (Wild Type), ERalpha (Y537ERalpha (Wild Type), ERalph (Y537S Mutant) and ERbeta Competition Binding Assay |
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Ki | 46.0±n/a nM |
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Citation | Bastian, JA; Cohen, JD; Rubio, A; Sall, DJ; McMahon, JA Selective estrogen receptor degraders US Patent US11117902 Publication Date 9/14/2021 |
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More Info.: | Get all data from this article, Assay Method |
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Estrogen receptor [Y537S] |
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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
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BDBM443448 |
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n/a |
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Name | BDBM443448 |
Synonyms: | US10654866, Example 6B | US11117902, Example 6A | US11634426, Example 6B |
Type | Small organic molecule |
Emp. Form. | C28H24F2N2O3 |
Mol. Mass. | 474.4986 |
SMILES | Oc1ccc2c3[C@@H](Oc4c(F)cccc4-c3cnc2c1)c1ccc(OCCN2CC(CF)C2)cc1 |r| |
Structure |
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