Tilfrinib is a potent and selective breast tumor kinase (Brk) inhibitor (IC50 = 3.15 nM). Tilfrinib has >1000-fold selectivity for Brk over a panel of other kinases and inhibits proliferation of breast cancer cells in vitro.

GW590735 is a potent and selective agonist of PPARα with an EC50 value of 4 nM for the expression a GAL4-responsive reporter gene and at least 500-fold selectivity versus PPARγ and PPARδ. GW590735 significantly increased HDL cholesterol, decreased LDL and VLDL cholesterol, and significantly reduced triglycerides. Maximal increases in HDL cholesterol were 37%, 53%, and 84% with fenofibrate, torcetrapib, and GW590735, respectively.

Gly-Pro-Glu, also known as GPE, is a neuroprotective agent and the N-terminal tripeptide of IGF-1. Gly-Pro-Glu is neuroprotective after central administration in animal models of neurodegenerative processes, such as Huntington’s, Parkinson’s, Alzheimer’s diseases, and varies acute brain injury animal models. GPE mimics insulin-like growth factor I effects on the somatostatin system through a mechanism independent of β-amyloid clearance that involves modulation of calcium and glycogen synthase kinase 3β signaling.

SQ109 is a drug undergoing development for treatment of tuberculosis. SQ109 showed activity against both drug susceptible and Multi-drug-resistant tuberculosis bacteria, including Extensively drug-resistant tuberculosis strains. In preclinical studies SQ109 enhanced the activity of anti-tubercular drugs isoniazid and rifampin and reduced by >30% the time required to cure mice of experimental TB. SQ109 is being developed by OOO Infectex in Russia and by Sequella Inc internationally. I

Y-29794 Tosylate is an orally active, potent and specific non-peptide prolyl endopeptidase (PPCE) inhibitor. Y-29794 selectively and competitively inhibited rat brain PPCE (Ki = 0.95 nM) in a reversible manner. Ex vivo study demonstrated that Y-29794 could penetrate into brain to exhibit dose-dependent and long-lasting inhibition. Furthermore, Y-29794 could potentiate the effect of TRH on the release of ACh in the rat hippocampus. Y-29794 prevents the progression of A beta-like deposition in the hippocampus of the SAM.

MK-7622 is a cholinesterase inhibitor under evaluation for the treatment of Alzheimer's disease. No studies have been published on this compound in the peer-reviewed literature or other publicly available documents. In October 2013, Merck began a Phase 2 trial in the United States to evaluate the compound's tolerability and efficacy as a symptomatic adjunct to donepezil therapy in patients with probable AD as diagnosed by two conventional diagnostic criteria, the NINCDS-ADRDA and DSM-IV.

UNIL088 is a water-soluble prodrug of cyclosporine A (CsA) designed for topical ocular delivery. The pro-moiety is grafted via an ester function to CsA and the solubilizing group is a phosphate ion. UNIL-088 can be rapidly hydrolysed under physiological conditions, and can retain a long shelf-life in aqueous media. UNIL-088 is more stable at pH 5 than at pH 7 with conversion rate constant of 3.2 x 10(-3) and 26.0 x 10(-3)days(-1), respectively.

ML192, also known as MLS000526305 and CID1434953, is a selective ligands for GPR55. The orphan G protein coupled receptor, ML192 (CID1434953) with 1080 nM potency for GPR55 and >45-fold antagonist and agonist selectivity against GPR35, CB1 and CB2. GPR55 has gained notoriety because of its putative identification as a cannabinoid receptor subtype. The significance of this assignment should not be underestimated given the importance of cannabinoids to drug abuse and the potential utility of cannabinoid ligands in treating behavioral disorders leading to conditions such as obesity.

GSK-7975A is an potent and orally active inhibitors of ORAI1 (calcium release-activated calcium modulator ). GSK-7975A prevents Cytosolic Calcium-Associated Injury of Human Pancreatic Acinar Cells and Acute Pancreatitis in 3 Mouse Models. GSK-7975A inhibited toxin-induced activation of ORAI1 and/or activation of Ca(2+) currents after Ca(2+) release, in a concentration-dependent manner, in mouse and human pancreatic acinar cells (inhibition >90% of the levels observed in control cells). ORAI1 inhibitors might be developed for the treatment of patients with pancreatitis.

ST247 is a PPAR β/δ selective inverse agonist. ST247 IC50 = 19 nm vs. GSK0660 IC50 = 210 nM.

UBP-310 is a potent and selective GLUK5 kainate receptor antagonist (IC50 = 130 nM). UBP-310also blocks recombinant homomeric GLUK7 receptors.

PF-04937319 is a glucokinase activator which is under development for the treatment of type 2 diametes mellitus. Glucose-phosphorylating enzyme, glucokinase (GK) plays a major role in glucose homeostasis primarily through its regulatory actions in pancreatic β-cells and liver hepatocytes. Conversion of glucose to glucose-6-phosphate by GK promotes glycogen synthesis in liver hepatocytes, and insulin release in the pancreatic β-cells.

OL-135 is a CNS penetrant, highly potent and selective reversible inhibitor of FAAH. OL-135 exhibits analgesic pharmacology in various animal models without the motor impairment associated with direct CB1 agonism.

XMD8-85, also known as ERK5-IN-1, exhibits potent inhibition of ERK5 and LRRK2.

PF-06442609 is a potent, metabolic stable γ-secretase modulators (GSMs) for Alzheimer's disease (AD). PF-06442609 displayed a favorable rodent pharmacokinetic profile, and robust reductions of brain Aβ42 and Aβ40 were observed in a guinea pig time-course experiment. F-06442609 is suitable for rodent model of AD.

VU0483605 is a potent and selective positive allosteric modulator (PAM) of mGluR1, displaying EC50 values of 0.39 and 0.36 μM at human and rat receptors, respectively, and no activity as a mGlu4 PAM (EC50 >10 μM).

PF05020182 is novel potent and selective Kv7.2/4 potassium channel opener. PF-05020182 (2) significantly inhibits convulsions in the MES assay at doses tested, consistent with in vitro activity measure. The physiochemical properties, in vitro and in vivo activities of PF-05020182 support further development as an adjunctive treatment of refractory epilepsy. Facilitating activation, or delaying inactivation, of the native Kv7 channel reduces neuronal excitability, which may be beneficial in controlling spontaneous electrical activity during epileptic seizures.

P7C3A20-analog, as known as defluoro-P7C3-A20, is a structural analogue of P7C3-A20. Compared to P7C3-A20 structure, P7C3-A20 analog has no fluorine atom in the 1,3-diaminopropane-bridge. P7C3-A20 analog was synthesized by mistake during a process to make P7C3-A20. The bioactivity of P7C3-A20 analog is unknown. P7C3-A20 analog may be used for research to compare with P7C3-A20. P7C3-A20 is a proneurogenic, neuroprotective agent. P7C3-A20 displayed increased activity and an improved toxicity profile compared to P7C3. P7C3-A20 demonstrated greater proneurogenic efficacy than a wide spectrum of currently marketed antidepressant drugs. P7C3-A20 showed neuroprotective properties in rodent models of Parkinson's disease, amyotrophic lateral sclerosis, traumatic brain injury and age-related cognitive decline.

BMS-582949 is a potent and selective P38 mitogen-activated protein kinase (P38 MAPK) inhibitor. BMS-582949 is currently under Phase II clinical trials for the treatment of inflammatory diseases. One clinical study showed that, in stable atherosclerosis, 12 weeks of treatment with BMS-582949 did not reduce arterial inflammation or hs-CRP compared to placebo, whereas intensification of statin therapy significantly decreased arterial inflammation. p38α MAP kinase plays a crucial role in regulating the biosynthesis of many inflammatory cytokines including TNFα and IL-1β.

Salmeterol is a long-acting beta2-adrenergic receptor agonist drug used in the maintenance and prevention of asthma symptoms and maintenance of chronic obstructive pulmonary disease (COPD) symptoms. Symptoms include shortness of breath, wheezing, coughing and chest tightness. Salmeterol is also used to prevent breathing difficulties during exercise (exercise induced bronchospasm). It is marketed as Serevent in the US.

CGP-7930 is a positive allosteric modulator at the GABAB receptor. It has anxiolytic effects in animal studies, and has a synergistic effect with GABAB agonists such as baclofen and GHB, as well as reducing self-administration of ethanol and cocaine.

GS-39783 is a novel positive allosteric modulators of the GABA(B) receptor, which is a compound used in scientific research which acts as a positive allosteric modulator at the GABAB receptor. It has been shown to produce anxiolytic effects in animal studies, and reduces self-administration of ethanol, cocaine and nicotine.

SCH-50911 is a selective GABAB antagonist developed by Schering-Plough Corporation. Its main applications are in pharmacology research. SCH-50911 also acts as an anticonvulsant under normal conditions, and so counteracts both the depressant and pro-convulsant effects of GHB overdose. This pharmacological profile makes SCH-50911 a promising candidate as a GHB antidote for human use, and might also make it useful for treating overdoses of other GABAB agonists such as Baclofen.

Nemiralisib, also known as GSK-2269557, is a potent and selective PI3Kδ inhibitor. GSK-2269557 is is currently in clinical trials for the treatment of respiratory diseases such as asthma and COPD. GSK-2269557 is highly selective for PI3Kδ over the closely related isoforms and are active in a disease relevant brown Norway rat acute OVA model of Th2-driven lung inflammation. PI3Kδ is highly enriched in leukocytes, making it an attractive target for the treatment of inflammatory conditions, such as asthma,6 chronic obstructive pulmonary disease (COPD), and autoimmune diseases.

CHF-5074, also known as CSP-1103, is a γ-secretase modulator. CHF-5074 reduces Aβ42 and Aβ40 secretion, with an IC50 of 3.6 and 18.4 μM respectively. CHF5074 reduces brain beta-Amyloid pathology in a transgenic mouse model of Alzheimer's Disease without causing peripheral toxicity. CHF5074 is a non-steroidal anti-inflammatory derivative holding disease-modifying potential for the treatment of Alzheimer's disease.

WWL70 is a potent inhibitor of α/β-hydrolase domain 6 (ABHD6) (IC50 = 70 nM), an enzyme which catalyzes the hydrolysis of 2-arachidonylglycerol.

T-1095 is a potent and selective inhibitor of Na±glucose cotransporters (SGLTs). T-1095 may be a useful antidiabetic drug. Long-term treatment with T-1095 causes sustained improvement in hyperglycemia and prevents diabetic neuropathy in Goto-Kakizaki Rats. Chronic administration of T-1095 (0.1% w w(-1) pellet chow, for 12 weeks) decreased blood glucose and haemoglobin A(1C) levels, and improved glucose intolerance in db/db mice. The age-related decrease in plasma insulin levels was markedly inhibited and there was a 2.5 fold increase of insulin content in the pancreas of T-1095-treated db/db mice. T-1095 improved the metabolic abnormalities and inhibit the development of diabetic complications in db/db mice.

Duvoglustat, also known as AT2220, 1-Deoxynojirimycin, Moranoline, deoxynojirimycin or DNJ, is a potent and selective alpha-glucosidase inhibitor, most commonly found in mulberry leaves. Duvoglustat is used to suppress the elevation of postprandial hyperglycemia. Duvoglustat acts as an antihyperglycemic agent by slowing the rate of carbohydrate degradation to monosaccharides. Duvoglustat inhibits glucose absorption by suppressing intestinal glucose transport. Duvoglustat accelerates glucose utilization by regulating hepatic glucose metabolism enzymes. Duvoglustat directly regulates expression of hepatic enzymes involved in glucose metabolism.

AB05831, also known as 2-Acetamido-1,2-dideoxynojirimycin, is a highly potent and specific inhibitor of beta-hexosaminidase. N-Acetyl-3-hexosaminidase (HEX) is a member of lysosomal hydrolases, which catalyzes hydrolysis of terminal, non-reducing N-acetyl-|3-D-glucosamine (GlcNAc) andN-acetyl-(3-D-galactosamine (GalNAc) residues in glycoproteins, gan-gliosides, and glycosaminoglycans (GAGs). HEX, released by chondrocytes into the extracellular compartment, promotes cartilage matrix degradation. Osteoarthritis patients have increased HEX activity in synovial fluid.

U-73343 is a negative control (or inactive analogue) of U73122, which is a putative phospholipase C inhibitor. U73343 was found to inhibit TxA2 formation; it therefore partially inhibited the rise in [Ca2+]i evoked by low concentrations of thrombin, by thapsigargin or by collagen. U73343 had a greater effect than aspirin on the action of collagen, indicating an action on the TxA2-independent component of the signal, via PLC gamma-U73343 lowered TxA2 production by inhibiting the activation of cPLA2, probably at a tyrosine phosphorylation step. U73343 seems to inhibit only the tyrosine kinases involved in the activation of PLC gamma and the generation of TxA2.