Figure 1.

Dose–response curves for the ten most potent screening hits as well as for the positive control HTS06792. Shown is t_½ of cell shrinking, indicating that water permeability was measured in calcein-loaded, mAQP3-expressing CHO cells. Screening hits were repurchased before analysis to confirm hit identity. Supplier product codes are indicated above each substance. Compounds MWP00821 and S04288 were not sufficiently soluble in DMSO and were thus tested at lower concentrations than the other compounds. AQP3 inhibition could be confirmed for five hit compounds. In addition, JM00015 showed AQP3 inhibition at the highest tested concentration and at lower efficacy than expected.