Efficacious compounds which were confirmed safe in rodents at doses up to 30 mg/kg were progressed to safety, PK and efficacy studies in dogs.
The most efficacious compounds that induce muscle hypertrophy or endurance are hampered by severe side effects and are classified as doping.
Recent animal genetic models point to the potential validity of several neuropeptide receptors as targets for drug discovery, though the need for safe, efficacious compounds cannot be underestimated.
The two most efficacious compounds identified inhibit activation of the LPA3 receptor by 200 nM LPA with IC50 values of 752 nM and 2992 nM.
We believe that the top-ranked molecules with anti-cancer activity are clearly amenable to chemical modifications for creating potent, safe and efficacious compounds with the feasibility of generating new chemical entities after pre-clinical and clinical studies.
In an effort to develop safe and efficacious compounds for the treatment of metabolic disorders, novel thiophene substituted oxazole containing α-alkoxy-phenylpropanoic acid derivatives are designed as highly potent PPARα/γ dual agonists.
