FzM1

Description: FzM1, a negative allosteric modulator (NAM) of the Frizzled receptor FZD4, diminishes WNT5A-dependent WNT responsive element (WRE) activity (log EC50inh=-6.2) by binding to an allosteric site on intracellular loop 3 (ICL3) of FZD4. This interaction changes the receptor's conformation and inhibits the WNT/beta-catenin signaling pathway. Target: Wnt/beta-catenin. Smiles: Oc1cc(NC(=O)Nc2ccc3ccccc3c2)cc(c1)-c1cccs1. References: Riccio G, et al. A Negative Allosteric Modulator of WNT Receptor Frizzled 4 Switches into an Allosteric Agonist. Biochemistry. 2018 Feb 6,57(5):839-851.