Naroparcil [LF 90055], the lead compound in a series of orally-active antithrombotics, is an analogue of LF 1351, a compound shown to have antithrombotic action. Antithrombotic activity of naroparcil is dependent on modification in the plasma GAG profile which inactivates thrombin via heparin cofactor II (HCII).

Nadoxolol is a beta-adrenergic blocking agent and an antihypertensive drug.

Oxindanac, a non-steroidal anti-inflammatory drug, and is a weak cyclooxygenase inhibitor possessed antipyretic activity. This drug is used as a veterinary inflammatory drug. In addition, oxindanac was studied in phase III clinical trials for the treatment of rheumatic disorders. However, this study was discontinued.

Olaquindox, a potent antibacterial agent, is used as an effective feed additive in the livestock industry. Olaquindox could potentially expose a human to the risk of biological hazards due to its genotoxicity and cytotoxicity. However, the potential mechanism of toxicity is still unknown. Recently was provided experiments to explore the molecular mechanism of p21 on olaquindox-induced mitochondrial apoptosis. It was shown, that olaquindox promoted the production of ROS, suppressed the protein expression p21 in a p53-independent way and phosphorylated p21. This experiment provided new insights into the molecular mechanism of olaquindox and shed light on the role of p21.

Phenylthilone is an anticonvulsant, hypnotic and spasmolytic agent.

AVN-944 is an IMPDH (inosine 5-monophosphate dehydrogenase) inhibitor which is now being tested in phase I of clinical trials for the treatment of hematologic malignancies and solid tumors and in phase II for pancreatic cancer (in combination with gemcitabine). The drug showed good inhibition of IMPDH isoforms I and II with Ki=6-10 nM.

Bristol-Myers Squibb developed BMS-184476 for the potential treatment of solid tumors. BMS-184476 participated in phase II clinical trials for patients with non-small-cell lung cancer, breast, and ovarian cancers. However, that development has been discontinued.

Fananserin is a potential antipsychotic compound with a high affinity for both D4 and 5-HT2A receptors, and negligible affinity for D2 receptors. Fananserin has been researched for the treatment of schizophrenia. Fananserin was the first selective D4/5-HT2A antagonist to undergo clinical trials for schizophrenia. It has a high affinity for D4 (Ki 2.9 nM) and 5-HT2A (Ki 0.37 nM) receptors and is over 100-fold selective versus H1, a1 adrenergic, 5-HT1A and D2 dopamine receptors. Development of this compound was halted following phase II clinical trials due to lack of efficacy.