Compound class:
Synthetic organic
Comment: This Amgen BACE1 inhibitor for Alzheimer's disease, AMG-8718, had a balanced profile of potency, hERG binding affinity, and Pgp recognition. It also produced robust and sustained reductions of CSF and brain Aβ levels in a rat pharmacodynamic model [1]. However, retinal thinning was observed in a 1-month toxicity study in the rat and further studies suggested this to be an off-target effect where, in the rat, AMG-8718 impairs phagolysosomal function, leading to photoreceptor dysfunction and ultimately loss of photoreceptors [2]. The compound is example 288 in [3] from over 1000 analogues, but only binned activity data is provided. While the PubChem Bioassay data and other sources link to this structure note that MMDB and PubMed link their PDB structure to a different tautomeric representation as PubChem CID 86580376.
Ligand Activity Visualisation ChartsThese 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. ✖ |
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