PD123319 is a potent, selective AT2 angiotensin II receptor antagonist with IC50 of 34 nM.PD123319 had been in phase I clinical trials by Pfizer for the treatment of hypertension. However, this research has been discontinued.

CP 226269 is a selective dopamine D4 agonist. This compound was developed by Pfizer for Neuroscience research. CP226269 showed a significant enhancement in the 5-trial inhibitory avoidance model.

PF-04479745 (PF-4479745) is a selective serotonin 5HT2C agonist. PF-4479745 displayed robust pharmacology in a preclinical canine model of stress urinary incontinence (SUI) and no measurable functional agonism at the key selectivity targets 5-HT2A and 5-HT2B in relevant tissue-based assay systems.

CP 135807 is a selective 5-HT1D receptor agonist. Preclinical development for migraine was proposed but no development report released. This compound is used for neuroscience research.

PF 4800567 is a drug developed by Pfizer which acts as a selective potent inhibitor of CK1epsilon (IC(50) = 32 nM) with greater than 20-fold selectivity over CK1delta, and has mainly been used in the study of the casein kinase 1 enzymes in the regulation of circadian rhythm, as well as showing potential neuroprotective effects. PF 4800567 was found in animal studies to enhance responses to certain drugs of abuse such as methamphetamine and fentanyl, which suggests a role for CK1-ε in negative regulation of sensitivity to stimulant and opioid drugs.

PD 144418 oxalate is a remarkably potent and selective sigma1 receptor ligand having potential antipsychotic properties. PD 144418 oxalate displayed an apparent affinity (Ki) of 0.08 nM for sigma1 sites in guinea pig brain membranes and a Ki of 1377 nM for sigma2 sites in rodent neuronal NG108-15 cell membranes. PD 144418 oxalate was classified as sigma1 receptor antagonist based upon several assays, including the ability to attenuate mescaline-induced scratching in mice. PD 144418 oxalate attenuates cocaine-induced hyperactivity in mice. It showed potential antipsychotic activity, but no antidepressant or anxiolytic actions.

PF-4981517 is a potent and selective inhibitor of CYP3A4 (P450) with IC50 of 0.03 uM, exhibits >500-fold selectivity over CYP3A5 and CYP3A7. PF-4981517 is a very useful tool for understanding the relative roles of CYP3A4 versus CYP3A5 and the impact of CYP3A5 genetic polymorphism on a compound's pharmacokinetics.

MCOPPB trihydrochloride (MCOPPB) is a nonpeptide agonist of the NOP receptor, an anxiolytic agent. MCOPPB has a high affinity for the human NOP receptor (pKi = 10.07 +/- 0.01) and selectivity for the NOP receptor over other members of the opioid receptor family: 12-, 270- and >1000-fold more selective for the NOP receptor than for the micro-, kappa-, and delta-receptor, respectively. In an ex vivo binding study, MCOPPB (10 mg/kg, p.o.) inhibited signaling through the NOP receptor in the mouse brain, suggesting that it penetrated into the brain after it was orally administered. MCOPPB - a compound with few adverse effects on the central nervous system - is a potential therapeutic agent for the treatment of anxiety.

PF 3644022 is potent, ATP-competitive inhibitor of mitogen-activated protein kinase (MAPK)-activated protein kinase-2 (MK2) (IC50 = 5.2 nM; Ki = 3 nM). Inhibits tumor necrosis factor α (TNFα) production in U937 monocytic cells and peripheral blood mononuclear cells (PBMCs) (IC50 = 160 nM). PF-3644022 is orally efficacious at inhibiting TNFalpha production in LPS-challenged rats and blocking paw swelling in the chronic SCW-arthritis model.

PF-03246799 (PF-3246799) is a potent 5-HT2C receptor agonist. PF-3246799 had minimal activation at either the 5-HT2A or 5-HT2B receptors, combined with robust efficacy in a preclinical canine model of SUI and attractive pharmacokinetic and safety properties. It is a candidate for clinical development for the treatment of SUI.