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Updated: Jun 22, 2026

Quantitative PCR-based Assay to Measure Sonic Hedgehog Signaling in Cellular Model of Ciliogenesis
Published on: January 31, 2025
Potent agonists of the Hedgehog signaling pathway
Shirley A Brunton1, John H A Stibbard, Lee L Rubin
1Evotec, 114 Milton Park, Abingdon, Oxfordshire OX14 4SA, UK. shirley.brunton@evotec.com
Abstract:
A family of biaryl substituted 1,4-diaminocyclohexanamides of 3-chlorobenzothiophene-2-carboxylic acid is reported as picomolar modulators of Hedgehog protein function. SAR for the 1,4-diaminocyclohexane group is shown to be exquisitely sensitive to substitution on the 4-amino group, and SAR for the 3-chlorobenzothiophene group is highly specific. Preliminary SAR studies of the biaryl substituent led to a picomolar compound with in vivo activity.
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