GSK650394 was synthesized by the CVU Medicinal Chemistry Department at GlaxoSmithKline as an inhibitor of serum- and glucocorticoid-regulated kinases, SGK1 and SGK2. It was shown, that GSK650394 possessed antiproliferative properties against the human prostate carcinoma cell line LNCaP.

Delsoline is a Nicotinic receptor antagonist, ganglion blocker; exhibits weak affinity at brain α-bungarotoxin-sensitive nicotinic acetylcholine receptors.

NPS-2143 is a novel potent and selective antagonist of Ca(2+) receptor with IC50 of 43 nM. Blockage of CaSR with NPS-2143 has being shown to prevent the development of pulmonary hypertension and right ventricular hypertrophy in animal models of pulmonary hypertension. The use of calcilytics, antagonists of CaSR, may be a novel therapeutic approach for PAH patients. Calcilytic drugs have been researched as potential treatments for osteoporosis, and as the first such compound developed, NPS-2143 is still widely used in research into the CaSR receptor as well as design of newer calcilytic agents. When administered together with an antiresorptive agent (estradiol), NPS 2143 causes an increase in trabecular bone volume and bone mineral density in osteopenic rats.

BAY-36-7620 is a potent and selective antagonist at mGlu1receptors and inhibits >60% of mGlu1a receptor constitutive activity (IC50 = 0.38 uM). BAY-36-7620 is thus the first described mGlu1 receptor inverse agonist. It impairs classical conditioning and associated synaptic plasticity in hippocampal neurons. BAY-36-7620 exhibits neuroprotective and anticonvulsive effects in vivo following systemic administration.

R-1485 is a lead candidate identified from Roche Pharmaceuticals research programme for the treatment of Alzheimer's disease. Selective and high affinity 5-HT6 antagonist; displays low hERG inhibition. Exhibits >100 fold selectivity against a panel of 50 targets including other 5-HT receptor subtypes. R-1485 is currently in Phase I trials at Roche for the treatment of Alzheimer’s type dementia. This compound showed a pKi value of 9.3 when it was tested for inhibition of [3H]-LSD binding to human 5-HT6 receptors expressed in HEK293 cells. In addition, it was also found that in rats this agent has good BBB permeability.