CJ-033466 is experimental drug, which acts as selective 5-HT4 serotonin receptor partial agonist. It was originally synthesized at Pfizer Laboratories, and it was specifically exemplified in Pfizer patent applications (WO2003035649 and WO2004026869). In animal tests, it stimulated gastrointestinal motility with 30 times the potency of cisapride. CJ-033,466 does not affect D2 and other 5-HT receptors, and it is a potential therapy for gastroparesis patients.

PF-06380101 is a novel cytotoxic Dolastatin 10 analogue; with excellent potencies in tumor cell proliferation assays and differential ADME properties when compared to other synthetic auristatin analogues that are used in the preparation of ADCs.

CP-809101 is a potent, functionally selective 5-HT(2C) agonist that displays approximately 100% efficacy in vitro. CP-809101 has a pharmacological profile similar to that of the atypical antipsychotics with low extrapyramidal symptom liability. CP-809101 was active in novel object recognition, an animal model of cognitive function. It had promising results in animal models of obesity and psychosis.

CP-91149 is a selective glycogen phosphorylase (GP) inhibitor in the presence of glucose, 5- to 10-fold less potent in the absence of glucose. It may be useful in the treatment of type 2 diabetes. In vivo, oral injection of CP-91149 to diabetic ob/ob mice at 25–50 mg/kg led in rapid (3 h) glucose lowering by 100–120 mg/dl without producing hypoglycemia. In addition, upon treatment with CP-91149, A549 non-small cell lung carcinoma (NSCLC) cells accumulated glycogen with associated growth retardation. Treated normal skin fibroblasts also accumulated glycogen with G1-cell cycle arrest that was associated with inhibition of cyclin E-CDK2 activity

CP-640186 is a potent inhibitor of mammalian ACCs and can reduce body weight and improve insulin sensitivity in test animals. CP-640186 has recently been shown to be a potent inhibitor of isoforms of mammalian ACCs with IC50 values of about 55 nM. This is currently the only reported potent inhibitor of mammalian ACCs. In cell cultures as well as in animal models, CP-640186 can reduce tissue malonyl-CoA levels, inhibit fatty acid biosynthesis, and stimulate fatty acid oxidation. Most importantly, CP-640186 can reduce body fat mass and body weight, and improve insulin sensitivity, validating ACCs as targets for antiobesity and antidiabetes drugs.CP-640186 potently inhibited HepG2 cell fatty acid and TG synthesis. CP-640186 also stimulated fatty acid oxidation in C2C12 cells (ACC2) and in rat epitrochlearis muscle strips with EC50s of 57 nm and 1.3 uM. In rats, CP-640186 lowered hepatic, soleus muscle, quadriceps muscle, and cardiac muscle malonyl-CoA with ED50s of 55, 6, 15, and 8 mg/kg. Consequently, CP-640186 inhibited fatty acid synthesis in rats, CD1 mice, and ob/ob mice with ED50s of 13, 11, and 4 mg/kg, and stimulated rat whole body fatty acid oxidation with an ED50 of approximately 30 mg/kg.

CP-673,451 is a potent inhibitor of platelet-derived growth factor beta-receptor (PDGFR-beta) kinase- and PDGF-BB-stimulated autophosphorylation of PDGFR-beta in cells. CP 673451 in a sponge implant model where a surgical sponge was soaked with PDGFBB to initiate angiogenesis, CP 673451 inhibited 75% of PDGF-BB-stimulated angiogenesis at a dose of 3 mg/kg for 5 days. CP 673451 did not inhibit angiogenesis induced by either VEGF or bFGF in the sponge. CP 673451 also inhibited tumour growth in H460 human lung carcinoma, Colo205 and LS174T human colon carcinomas and U87MG human glioblastoma multiforme xenograft models. CP-673,451 has not been studied in clinical trials due to issues with toxicity in preclinical studies.

PF-750 is a covalent irreversible inhibitor of FAAH, discovered by Pfizer.

PF-998425 is a selective non-steroidal androgen receptor antagonist. It is rapidly metabolized systemically, and demonstrated efficacy for treatment of androgenic alopecia in preclinical model.

CP-868388 is a potent PPAR-alpha agonist The orally administered CP-868388 is well tolerated. It has been very useful in acute preclinical models for treating dyslipidemia.

cis-(-)-Sertraline (aka 1R,4R-sertraline) is the therapeutically inactive enantiomer of Sertraline. Sertraline has four stereoisomers: (1R,4R), (1S,4S), (1R,4S), and (1S,4R), of which the (1S,4S) isomer is the active therapeutic compound. Sertraline is sold under the brand name Zoloft (and others) as an anti-depressant acting as a selective serotonin reuptake inhibitor. The bio-activity of sertraline is restricted to (1S,4S), and (1R,4R), where (1S,4S) is most potent.