Targeting TEAD with small-molecule inhibitors is an emerging therapeutic strategy for YAP/TAZ-dependent human cancers with Hippo pathway alterations. Bridgene Biosciences Inc. identified three hits with the Isobaric Mass Tagged Affinity Characterization (IMTAC) screening platform that covalently bound to TEAD1 with the binding site being cysteine 359, which led to the BGI-9004 compound.