Mazindol was developed as an appetite suppressant. It exists in a dynamic equilibrium between three isomers (the keto and the R and S–ol forms, respectively) with the R or S–ol being the only relevant forms at physiologic pH. Both S- and R-mazindol supposed to target human serotonin and dopamine transporters. R-mazindol is the biologically relevant enantiomer.

Mazindol was developed as an appetite suppressant. It exists in a dynamic equilibrium between three isomers (the keto and the R and S–ol forms, respectively) with the R or S–ol being the only relevant forms at physiologic pH. Both S- and R-mazindol supposed to target human serotonin and dopamine transporters. R-mazindol is the biologically relevant enantiomer.

(–)-Blebbistatin is the active enantiomer of (±)-Blebbistatin that accounts for the inhibitory activity towards ATPase and myosin II-dependent cellular processes. It is of great interest because it is specific for certain myosin isoforms: (–)-Blebbistatin potently inhibit the actomyosin ATPase activities of expressed nonmuscle myosin IIA, nonmuscle myosin IIB, rabbit skeletal muscle myosin II, and D. discoideum myosin II, but does not inhibit smooth muscle myosin II, nor myosins from classes I, V or X. Blebbistatin binds within the apex of the myosin cleft at the opposite end of the ‘phosphate tube’ from MgADP–vanadate.

Pseudopelletierine is the main alkaloid derived from the root-bark of the pomegranate tree (Punica granatum). Pseudopelletierine is used as an enzyme substrate.

Cyanidin is a natural anthocyanidin present in fruits and vegetables, attenuates the development of several diseases, including asthma, diabetes, atherosclerosis, and cancer, through its anti-inflammatory effects. Its mechanism of action is still undefined, but it was revealed that cyanidin specifically recognizes an IL-17A binding site in the IL-17A receptor subunit (IL-17RA) and inhibits the IL-17A/IL-17RA interaction and thus can be used as a drug for the treatment of IL-17A-dependent inflammatory diseases and cancer. In addition, cyanidin was capable of inhibiting osteoclast formation and thus might have therapeutic potential for osteolytic diseases.

Reserpic acid, a derivative of the antihypertensive drug reserpine, can inhibit norepinephrine uptake although it is much less effective than reserpine itself. Recently was shown, that reserpic acid possessed a strong binding to the pancreatic lipase, a major target for controlling the obesity.

Racemic phenibut (beta-phenyl-gamma-aminobutyric acid or 4-amino-3-phenylbutyric acid) is a neuropsychotropic drug that was discovered and introduced into clinical practice in Russia in the 1960s. In pharmacological tests of locomotor activity, antidepressant and pain effects, S-phenibut was inactive. In contrast, R-phenibut turned out to be two times more potent than racemic phenibut in most of the tests. Racemic phenibut and R-phenibut demonstrated an affinity for GABAB receptors, in contrast, S-phenibut was not able to bind receptors. Pharmacological activity of racemic phenibut relies on R-phenibut and this correlates to the binding affinity of enantiomers of phenibut to the GABAB receptor. Both S- and R-phenibut bind to the α2-δ subunit of voltage-dependent calcium channels and exert gabapentin-like anti-nociceptive effects. In addition S-isomer was found to be a substrate of gamma-aminobutyric acid aminotransferase, however, the R-isomer is a competitive inhibitor.