PF-06439015 is a potent and selective inihibitor that overcomes clinical ALK (receptor tyrosine kinase anaplastic lymphoma kinase) mutations resistant to Crizotinib. PF-06439015 is potent across a broad panel of ALK mutant cell lines with an IC50 of 6.6 nM for tumor growth inhibition in a crizotinib-resistant cell line (H3122-L1196M).

CP 99994 dihydrochloride have shown the compound to be a potent, selective and competitive NK-1 receptor antagonist. In preclinical studies, CP 99994 decreased cough number, peak abdominal activity, and peak tracheal pressure, without affecting baseline respiration. But in clinical trial administration of CP 99994 over 2 h does not significantly inhibit hypertonic saline-induced bronchoconstriction or cough in subjects with mild asthma. CP 99994 significantly suppressed acute postoperative pain at 90 min after surgery.

SD-06 (SD0006) is a potent, selective and orally available inhibitor of p38 kinase. In vitro, SD0006 was selective for p38alpha kinase over 50 other kinases screened (including p38gamma and p38delta with modest selectivity over p38beta). Crystal structures with p38alpha show binding at the ATP site with additional residue interactions outside the ATP pocket unique to p38alpha that can confer advantages over other ATP competitive inhibitors. Direct correlation between inhibition of p38alpha activity and that of lipopolysaccharide-stimulated TNFalpha release was established in cellular models and in vivo, including a phase 1 clinical trial. Potency (IC(50)) for inhibiting tumor necrosis factor-alpha (TNFalpha) release, in vitro and in vivo, was <200 nmol/l. In vivo, SD0006 was effective in the rat streptococcal-cell-wall-induced arthritis model, with dramatic protective effects on paw joint integrity and bone density as shown by radiographic analysis. In the murine collagen-induced arthritis model, equivalence was demonstrated to anti-TNFalpha treatment. SD0006 also demonstrated good oral anti-inflammatory efficacy with excellent cross-species correlation between the rat, cynomolgus monkey, and human. SD0006 suppressed expression of multiple proinflammatory proteins at both the transcriptional and translational levels. These properties suggest SD0006 could provide broader therapeutic efficacy than cytokine-targeted monotherapeutics.

PF-8380 is a potent autotaxin inhibitor with an IC(50) of 2.8 nM in isolated enzyme assay and 101 nM in human whole blood. Inhibition of ATX by PF-8380 led to decreased invasion and enhanced radiosensitization of GBM cells.

PF-514273 is a drug developed by Pfizer, which acts as an extremely selective antagonist for the CB1 receptor, with approximately 10,000x selectivity over the closely related CB2 receptor. Pfizer was developing PF 514273 in phase I clinical studies for the treatment of obesity in the US. However, these studies were discontinued.

PHA-543613 was discovered by Pfizer and has been under development primarily as a potential treatment of schizophrenia. PHA-543613 acts as an agonist to the Neuronal acetylcholine receptor protein alpha-7 subunit. A single human trial was conducted in healthy human volunteers, but the compound has been studied extensively in rat models for schizophrenia as well as Parkinson's disease and Alzheimer's disease.

N-(1-amino-3,3-dimethyl-1-oxobutan-2-yl)-1-(4-fluorobenzyl)-1H-indazole-3-carboxamide [ADB-FUBINACA] is a synthetic cannabinoid, a Schedule I drug. ADB-FUBINACA acts as a high potency agonist of cannabinoid CB1 receptor. The compound considered to be a component of illicit smoking mixtures "spice".

AB‐FUBINACA is a synthetic cannabinoid and it is a very potent agonist for the cannabinoid (CB1) receptor. AB-FUBINACA is designated as a Schedule I controlled substance in the United States.

N-((1S)-1-(Aminocarbonyl)-2-methylpropyl)-1-(5-fluoropentyl)-1H-indazole-3-carboxamide (5F-AB-PINACA) is an indazole-based synthetic cannabinoid developed by Pfizer in 2009 as an analgesic medication. In January 2015, AB-PINACA became a controlled substance in the USA and 5F-ABPINACA will be prohibited based on the analog law. 5F-AB-PINACA has been sold online as a designer drug.