SCH486757 was invented as a selective nociceptin/orphanin FQ peptide (NOP) receptor agonist. SCH486757 participated in phase II clinical trial for the treatment of cough, however, this study was discontinued.

Gepotidacin (formerly GSK2140944) is a novel, first-in-class, triazaacenaphthylene antibacterial that selectively inhibits bacterial DNA gyrase and topoisomerase IV by a unique mechanism, one that is not utilized by any currently approved human therapeutic agent. As a consequence of its novel mode of action, gepotidacin is active in vitro against target pathogens carrying resistance determinants to established antibacterials, including fluoroquinolones. Gepotidacin has demonstrated in vitro activity against key pathogens, including drug-resistant strains, associated with a range of conventional and biothreat infections. GlaxoSmithKline is developing Gepotidacin for the treatment of gonorrhoea and skin and soft tissue infections.

LANOPEPDEN is an inhibitor of peptide deformylase, a bacterial enzyme required for protein maturation. It was in development for the treatment of complicated bacterial skin infection and hospitalized community-acquired pneumonia.

GSK-1004723 is a dual histamine H(1) and H(3) receptor antagonist with a long duration of action that has been investigated for the treatment of allergic rhinitis. GSK-1004723 was designed for intranasal administration as a suspension or solution. Clinical trials (phase 1 and 2) showed that GSK-1004723 is well tolerated and demonstrates clinically significant attenuation of symptoms (tested in an environmental allergen challenge chamber). However, attenuation of symptoms was less than seen for treatment with cetirizine (a commonly used over-the-counter antihistamine).

Recilisib (also known as EX-RAD or ON-01210) is a radioprotectant, which means that this compound can protect cells from harmful effects of ionizing radiation. Unlike other radioprotectors, recilisib is not a free-radical scavenger or responsible for cell cycle arrest. Recilisib was suggested to have a different radiation protection mechanism involving DNA repair pathways. This compound has been studied as prophylactic (use prior to radiation exposure) and therapeutic (after exposure to radiation) drug. In studies with healthy volunteers, recilisib was rapidly absorbed and well-tolerated, with only mild adverse events. Phase I clinical trials have been completed.

O-Desmethyl tramadol (O-Desmethyltramadol, O-DSMT) is a metabolite of tramadol. O-Desmethyltramadol is an opioid analgesic and the main active metabolite of tramadol. (+)-O-Desmethyltramadol is the most important metabolite of tramadol produced in the liver after tramadol is consumed. This metabolite is considerably more potent as a μ-opioid agonist than the parent compound. O-desmethyl tramadol, inhibits 5-hydroxytryptamine type 2C receptors expressed in xenopus oocytes. O-desmethyl tramadol inhibits functions of M(1) receptors but has little effect on those of M(3) receptors. O-desmethyl tramadol has been widely used clinically and has analgesic activity.

SB-705498 is a selective vanilloid receptor-1 (VR1/TRPV1) antagonist developed by GlaxoSmithKline. The drug was tested in phase II of clinical trials for the treatment of pain (dental, rectal, in migraine) and rhinitis/cough. The development of the drug has been terminated by unknown reason (SB-705498 is no longer in GSK pipeline).