PF-03716556 is a novel, potent, and selective acid pump antagonist for the treatment of gastroesophageal reflux disease. PF-03716556 inhibits the porcine, canine, and human recombinant gastric H+,K+-ATPase in a competitive manner without any biologically relevant activity against other tested receptors, ion channels, and enzymes, including the Na+,K+-ATPase. PF-03716556 inhibits gastric acid secretion in a dose-dependent manner in Ghosh-Schild rats and Heidenhain pouch dogs, producing full efficacy on treatment day 1. PF-03716556 is used for the treatment of gastroesophageal reflux disease.

PD 176252 is a competitive antagonist of neuromedin-B preferring (BB1) and gastrin-releasing peptide preferring (BB2) receptors. PD176252 inhibited tumor growtn in preclinical model of lung cancer, and exhibited synergy with EGFR inhibitor in the model of head and neck cancer. PD176252 demonstrated anxiolytic properties in preclinical models.

The synthetic retinoid AGN-193109 is a potent pan retinoic acid receptor (RAR) antagonist. It has been shown to block the antiproliferative effect of retinoids in cultured human cervical cancer cells. AGN-193109 is a potent RAR antagonist and a potential antidote of retinoid intoxication in vivo. In addition to potential clinical applications in the prevention and treatment of retinoid toxicity, AGN-193109 should provide a powerful experimental tool for the elucidation of retinoid biology.

BIO-5192 is a highly selective and potent (KD of <10 pM) inhibitor of integrin alpha 4 beta 1. The high affinity for integrin alpha 4 beta 1 results from an extremely slow dissociation rate of the inhibitor from the integrin/inhibitor complex, with a dissociation half-life of >12 h for both the unactivated and activated integrin. Preclinical trials in multiple sclerosis in USA were underway, but no recent development of BIO-5192 or its pegylated form has been reported; it appears that development has been discontinued.

BIIE-0246 is a highly potent, high affinity antagonist selective for the Y2 receptor subtype. BIIE-0246 is a drug used in scientific research, it was one of the first non-peptide Y2-selective antagonists developed, and remains among the most widely used tools for studying this receptor. It has been used to demonstrate a role for the Y2 subtype as a presynaptic autoreceptor limiting further neuropeptide Y release, as well as modulating dopamine and acetylcholine release. Blockade of central neuropeptide Y (NPY) Y2 receptors by BIIE-0246 has being shown to reduce ethanol self-administration in rats.

BIBO-3304 is a subtype selective nonpeptide antagonist with subnanomolar affinity for the Y1 receptor subtype that significantly inhibits food intake induced by application of NPY or by fasting. BIBO-3304 is a NPY Y1 receptor antagonist (IC50 values are 0.38 and 0.72 nM at human and rat receptors respectively) that displays > 2600-fold selectivity over Y2, Y4 and Y5 receptors.

BGC 20761 is an orally active, tryptamine analogue that is being developed by BTG as a procognitive antipsychotic for the treatment of schizophrenia. Preclinical development is underway in the US. This serotonin6 and serotonin2A receptor antagonist has nootropic properties with a balance of serotonergic and dopaminergic antagonist activity; BGC 20761 has moderate to low affinity for dopamine2, serotonin2C, histamine1, muscarinic M1-5, and α1 adrenergic receptors, indicating a potentially low propensity to cause serious adverse events.