- Guide to PHARMACOLOGY
Synonyms: CHF 5074 | CHF5074
Compound class: Synthetic organic
Comment: CHF-5074 is a gamma-secretase modulator (GSM). These are small molecules (<600 Da) causing a product shift from Abeta42 toward shorter and less toxic Abeta fragments. Classical non-steroidal anti-inflammatory drugs (NSAIDs) constituted the first class of GSMs. This compound has advanced to phase I trials
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Ross J, Sharma S, Winston J, Nunez M, Bottini G, Franceschi M, Scarpini E, Frigerio E, Fiorentini F, Fernandez M et al.. (2013)
CHF5074 reduces biomarkers of neuroinflammation in patients with mild cognitive impairment: a 12-week, double-blind, placebo-controlled study.
Curr Alzheimer Res, 10 (7): 742-53. [PMID:23968157]
2. Xin Z, Peng H, Zhang A, Talreja T, Kumaravel G, Xu L, Rohde E, Jung MY, Shackett MN, Kocisko D et al.. (2011)
Discovery of 4-aminomethylphenylacetic acids as γ-secretase modulators via a scaffold design approach.
Bioorg Med Chem Lett, 21 (24): 7277-80. [PMID:22061640]