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Smurf1-IN-1 is an orally active and selective inhibitor of specific E3 ubiquitin protein ligase 1 (SMURF1) with an IC50 of 92 nM. Smurf1-IN-1 has significant efficacy in rats model of pulmonary hypertension[1]. | [References]
[1] Shaw DE, et.al. Design and Synthesis of Inhibitors of the E3 Ligase SMAD Specific E3 Ubiquitin Protein Ligase 1 as a Treatment for Lung Remodeling in Pulmonary Arterial Hypertension. J Med Chem. 2023 Jun 22;66(12):8130-8139. DOI:10.1021/acs.jmedchem.3c00229 |
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