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Poster
148

An AMI-MS assay enables biochemical profiling of novel hydrolase inhibitors

Authors

S Northall1; D Slade2
1 AstraZeneca, UK;  2 AstraZeneca Discovery Biology, Cambridge, UK, UK

Discussion

Authors

S Northall1; D Slade2
1 AstraZeneca, UK;  2 AstraZeneca Discovery Biology, Cambridge, UK, UK

Discussion

Acoustic mist ionization - mass spectrometry (AMI-MS) enables high throughput analysis of liquid samples. An AMI-MS assay was chosen as an orthogonal enzymatic assay to a primary TR-FRET probe displacement screen in an HTS campaign to identify inhibitors of a challenging hydrolase target. The assay enables readout of enzymatic activity by direct measurement of reaction products.



In parallel to the primary assay, this functional assay has been used to validate compounds from HTS and DEL hit finding campaigns. It is currently used in a screening cascade for the first time in a live project to drive the DMTA cycle.