Fig. 1.

Focused screening for opsin-stabilizing compounds. (A) Single-point thermofluor screening at 47 μM compound and 1.4 μM protein concentration. Hits are above the threshold of 54.6 °C (green line). (B) FSEC-TS hit validation at 0.26 µM human opsin N2C N282C in the absence and presence of 10 µM compound concentration (triplicate). Stabilization by the S but not the R enantiomer of RS1 suggests stereoselective binding to opsin. (C) Pharmacotrafficking assay demonstrating cell surface trafficking of disease-mutated opsin P23H at EC₅₀ values (duplicate) of 1.0 µM (9-cis retinal), 2.4 µM (RS2), 16.7 µM (RS4), and 20 µM (RS3).