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Your search for gamma secretase returned 20 results

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Ligand: (R)-flurbiprofen
Comments: gamma-secretase modulator (GSM) that blocks gamma-secretase cleavage of amyloid-beta protein precursor (AbetaPP
Bioactivity comments: Mechanism of action thought to be gamma secretase modulation but no quantitiative data reported.
Ligand: MK-0752
Comments: gamma-secretase and Notch pathway inhibitor that was originally intended for the treatment of Alzheimer
Bioactivity comments: gamma-secretase-mediated Notch receptor cleavage in vitro . Since gamma-secretase is a protein complex
Ligand: begacestat
Comments: gamma-secretase inhibitor (GSI) for Alzheimer's Disease that selectively inhibits cleavage of APP over
Bioactivity comments: gamma-secretase function, and displaces a tritiated analog of GSI-953 from enriched gamma-secretase
Ligand: nirogacestat
Comments: gamma-secretase inhibitor. It is a reversible, non-competitive, and orally bioactive agent. It was proposed
Clinical use: gamma-secretase inhibitor to reach the clinic and was the first approved treatment for desmoid
Bioactivity comments: gamma-secretase activity with an IC50 of 1.2nM , measured as a reduction of Abeta
Ligand: DAPT
Synonyms: gamma-Secretase Inhibitor IX
Comments: gamma-secretase inhibitor that is used experimentally to inhibit NOTCH pathway signalling. Chemically it is a modified
Bioactivity comments: gamma-secretase inhibitor IN973 from the enzyme complex in human THP-1 cells in vitro
Ligand: crenigacestat
Comments: gamma-secretase/NOTCH pathway inhibitor that was developed for anti-tumour potential . Structurally, it is a modified
Bioactivity comments: gamma-secretase-madiated cleavage of NOTCH1 in MDA-MB-231 cancer cells with an IC50
Ligand: semagacestat
Comments: gamma-secretase inhibitor that was developed by Eli Lilly as a potential treatment for Alzheimer
Bioactivity comments: Shows potent Inhibition of gamma secretase-mediated amyloid beta (1 to 40) production in vitro
Detailed family introduction: Notch receptors
Detailed family introduction: ...gamma-secretase proteinase plays a pivotal role in Notch cleavage. As a result, gamma-secretase...
Ligand: RO4929097
Comments: gamma-secretase, was originally developed for Alzheimer's disease but based on its ability to inhibit
Bioactivity comments: RO4929097 strongly inhibits gamma-secretase enzyme activity.
Ligand: CHF-5074
Comments: gamma-secretase modulator (GSM). These are small molecules (<600 Da) causing a product shift from
Bioactivity comments: Note as a GSM the potency of gamma secretase inhibition is low

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