Potent neurotensin receptor agonist (IC₅₀ of 0.15 nM for inhibition of ¹²⁵I-neurotensin binding to neonatal mouse brain and an EC₅₀ of 1.9 nM in contracting the guinea-pig ileum).

Highly potent and long-lasting hypothermic and analgesic effects in the mouse.

Potent and highly selective farnesyltransferase (FTase) inhibitor (IC₅₀=1.4 nM).

>3000-fold more potent at blocking H-Ras (IC₅₀, 10 nM) than Rap1A processing.

Blocks bipolar spindle formation and chromosome alignment.

Potent, orally active dual MDR1 (P-gp)/BCRP inhibitor.

Inhibits MDR1-mediated Calcein-AM transport and BCRP-mediated Prazosin transport (IC₅₀=0.5 and 1.5 µM, respectively).

Potent, selective and orally active inhibitor of RORγt (IC₅₀ of <30 nM towards human RORγt).

Inhibits Th17 cell differentiation from human naive CD4⁺ T cells with an IC₅₀ of 24 nM.

For the research of psoriasis with low risk of thymic aberrations.

Potent and orally active STAT6 inhibitor (IC₅₀=1.9 nM) and shows a good CYP3A4 inhibition profile.

Inhibits in vitro Th2 differentiation (IC₅₀=2.4 nM) and inhibits production of IL-4 (IC₅₀=2.4 nM).

Suppresses eosinophil infiltration in an antigen-induced mouse asthmatic model.

First-in-class orally active aminomethylcycline antibacterial.

Inhibits bacterial protein synthesis by binding to the 30S ribosomal subunit.

Possesses broad-spectrum antibacterial activity against aerobic and anaerobic Gram-positive and Gram-negative bacteria, as well as atypical bacteria.