A chemical probe is a tool molecule that selectively binds to a target and is used to elucidate its biological function, helping bridge together chemical biology and drug discovery. TATA binding protein (TBP) associated factor 1 (TAF1) and TAF-1-like (TAF1L) are multidomain proteins that have been implicated with oncology and neurodegenerative diseases. The biological role of these proteins and their bromodomain regions within disease is still unknown with further target validation required. Herein we report the discovery of GSK9742, a potent, selective and cell penetrant TAF1/TAF1L bromodomain chemical probe and accompanying negative control GSK5121 for pre-clinical target validation.

Design of GSK9742, a chemical probe for the TAF1/TAF1L bromodomains

2019 Fall National Meeting

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