Novel Pan-TEAD and Subtype-Selective Inhibitors from Phenotypic Screen

A dataset from figshare describes compounds identified as inhibitors of YAP-TEAD-dependent transcription. The data, authored by Timo Heinrich and last updated in May 2026, includes results from a TEAD-reporter-based cellular screen, thermal shift assays, and in vivo xenograft studies. Derivatives with varied selectivity profiles and optimized physicochemical properties were generated.

Use Cases

• Training ML models for compound potency prediction based on structural modifications described.
• Analyzing structure-activity relationships for TEAD subtype selectivity mentioned in the optimization process.
• Benchmarking in vivo antitumor activity of novel inhibitors against lung cancer xenografts.

Strengths

• Includes data from multiple assay types: cellular screens, thermal shift assays, and in vivo studies.
• Describes compounds with diverse selectivity profiles, including pan-TEAD and TEAD3-sparing inhibitors.
• Reports monotherapeutic antitumor activity in lung cancer xenograft models.

Limitations

• Dataset size is only 7.5 KB, indicating a very limited scope.
• Column-level documentation is absent; field semantics must be inferred after download.
• Row count is unknown, which may limit suitability assessment.

Provenance

Source

figshare

Collection Method

Phenotypic screening and subsequent medicinal chemistry optimization, as described.

Freshness

Last updated 2026-05-27 15:11:10; freshness should be verified.