Development of MENA EVH1 inhibitors to prevent cancer metastasis

National Center For Advancing Translational Sciences

Investigators

Abstract

An HTRF assay was developed by collaborators at Albert Einstein School of Medicine and adapted to 1536-well format for HTS by NCATS. We have screened over 50,000 compounds in house and applied machine learning approaches to identify novel chemical space for inhibitors of MENA-PTP1B interactions. We've identified several initial hits that are being reordered or remade to validate their activity. Using the covalent fragment library, we also identified 63 potential covalent warheads which can be leveraged for covalent inhibitors. Characterization of hits is ongoing.