Compound class:
Synthetic organic
Comment: AGI-5198 is a selective inhibitor of R132H mutated metabolic enzyme, isocitrate dehydrogenase 1 (IDH1) [2]. R132H is a mutation found in multiple human cancers which is responsible for the generation of the oncometabolite R-2-hydroxyglutarate (R-2HG). Inhibition of R132H IDH1 is being examined for antineoplastic activity. This corresponds to example 165 in a patent from Agios [1] who also filed on ivosidenib (but both with binned activity values). This has a Probe Portal entry SGC AGI-5198.
![]() 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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Bioactivity Comments |
AGI-5198 inhibits R132H IDH1 with an IC50 of 70nM, but 13000 nM Ki against wild-type IDH1 enzyme and inactive against IDH2 (selected mutants and wild-type enzyme) [2]. In cellular in vitro assays and in vivo, AGI-5198 inhibits proliferation of IDH1-mutant, but not IDH1-wild-type glioma cells. |
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