Romifidine is a drug that is used in veterinary medicine as a sedative mainly in large animals such as horses. It acts as an agonist at the α2 adrenergic receptor subtype.

Vinclozolin is a common dicarboximide fungicide used to control diseases, such as blights, rots and molds in vineyards.

Conessine is a steroidal alkaloid isolated from Holarrhena floribunda that has anti-malarial activity and interacts with the histamine H3 receptor.

Bendiocarb is a carbamate insecticide and is one of the 12 insecticides recommended by the World Health Organization for use in malaria control in Africa.

Bromacil is a substituted uracil herbicide used worldwide. It is not readily biodegradable and therefore has consequences to the environment.

Oxadiargyl is a protoporphyrinogen oxidase inhibitor and is used as a herbicide in China.

Doxorubicinol is the primary circulating metabolite of doxorubicin which may be used as an antineoplastic.

Isoxaflutole is a preemergence herbicide that has been marketed as a substitute for atrazine.

Vamidothion is a polar organophosphorus pesticide.

Cyclanilide is a plant growth regulator that is registered for use in cotton at different stages of growth.

RS 42358-197 is the S-isomer of the novel 5-HT3 receptor antagonist RS-42358.

Deltamethrin is globally used in crop protection and control of malaria and other vector-borne diseases and is easily degradable.

Trandolaprilat is a non-sulfhydryl angiotensin-converting enzyme inhibitor.

Rubrofusarin is an orange polyketide pigment that is a common intermediate in many different fungal biosynthetic pathways.

Crufomate is an insecticide used extensively for the control of cattle grubs, cattle lice, and hornflies.

Metacetamol is an isomer of paracetamol and it similarly exhibits polymorphism.

Prodiamine is a herbicide.

Bromofos is a pesticide.

Disulfoton is an organophosphate insecticide.

Butamifos is an anti-tubulin herbicide.

Cyphenothrin is a synthetic pyrethroid insecticide. It is effective against cockroaches that have developed resistance to organophosphorous and carbamate insecticides.

Buthiazide, also known as Butizide, is a 3-isobutyl analog of hydrochlorothiazide.

Prallethrin is a pyrethroid insecticide. Prallethrin 1.6% w/w liquid vaporizer is a repellent insecticide which is generally used for the control of mosquitoes in the household.

Imiprothrin is a synthetic pyrethroid insecticide. It is an ingredient in some commercial and consumer insecticide products for indoor use.[2] It has low acute toxicity to humans,[2] but to insects it acts as a neurotoxin causing paralysis.

Bromobutide is a herbicide.

Flumioxazin is an herbicide registered for use in soybean and peanut.

Procymidone is a dicarboximide fungicide mainly used for vineyard protection but also for different crops.

Perindoprilat is a non-sulfhydryl angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity.

Escitalopram is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class.

Cadusafos is an organophosphorous-nematicide soil insecticide.

Azamethiphos is an organothiophosphate insecticide. It is a veterinary drug used in Atlantic salmon fish farming to control parasites.

Sulfabromomethazine, also known as Bromosulfamethazine, NSC 5874, SN 3517, is a long-acting derivative of sulfamezathine that is used in the poultry, swine and cattle industries for the treatment of coccidiosis.

Resmethrin is a synthetic pyrethroid insecticide used against a variety of insects.

Tetrantoin is an anticonvulsant of the hydantoin group.

Disperse Red 1 is an azo dye that contributes to the toxicity and pollution of wastewater.

Triflusulfuron-methyl is a triazinylsulfonylurea herbicide.

Propetamphos is an organophosphate pesticide.

Drazoxolon is a lipid-soluble fungicide.

Sakuranetin is flavonoid phytoalexin that serves as a plant antibiotic and exists in Prunus and several other plant species.

Oxyclozanide is a salicylanilide anthelmintic. It is used in the treatment and control of fascioliasis in ruminants mainly domestic animals such as cattle, sheep, and goats.

Dioxabenzofos is a pesticide that causes rreversible ataxia in chicken, mice, and sheep.

Quinalphos is an organophosphate pesticide.

Metoxuron is a phenylurea herbicide.

Norflurazon is an excellent weed controlling agent being practiced in the agricultural lands.

Etrimfos is an organophosphorus pesticide.

Dimethenamid is a chloroacetamide herbicide.

Dipropetryn is a triazine herbicide.

Flusilazole is an organosilicon fungicide which is used to control fungal infections on a variety of fruit and vegetable crops. It is moderately toxic to animals and has been shown to produce birth defects and embryotoxicity at high doses.

Pyridaben is a pyridazinone derivative, is a new acaricide and insecticide for control of mites and some insects such as white flies, aphids and thrips. It acts as a complex I inhibitor.

Chlorfenvinphos is an organophosphorous compound that possesses acaricidal and insecticidal properties.

Sarcophine is a natural cembranoid from the Red Sea soft coral Sarcophyton glaucum.

Sari 59-801 is a novel, orally effective hypoglycemic compound.

Thiobencarb is a thiocarbamate cholinesterase inhibitor that is used as a pre-emergence herbicide.

Cetrorelix acetate is a synthetic decapeptide with gonadotropin-releasing hormone (GnRH) antagonistic activity used in infertility treatment.

Sulcotrione is a triketone herbicide used to control dicotyledonous weeds in maize culture.

Menbutone is an oxobutyric acid derivative and acts as a choleretic.

Viridicatumtoxin is a fungus-derived tetracycline-like antibiotic.

Flunixin is a nonsteroidal anti-inflammatory drug (NSAID), analgesic, and antipyretic used in horses, cattle and pigs.

Desmedipham is a carbamate herbicide.

Schisantherin B is one bioactive of lignans isolated from Schisandra chinensis (Turcz.) Baill which has been commonly used as a traditional herbal medicine for thousands of years.

Diacetoxyscirpenol is a mycotoxin from the group of type A trichothecenes. It is a secondary metabolite product of fungi of the genus Fusarium.

Sclerotiorin is a compound isolated from the fermented broth of Penicillium frequentans that exhibited potent inhibition against human polymorphonuclear leukocytes 5-lipoxygenase and human platelet aggregation.

FGTI-2734 is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor. It can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors.

MDR-652 is a nonpungent transient receptor potential vanilloid 1 (TRPV1) agonist discovered to be a strong topical analgesic.

Succinylacetone is an inhibitor of δ-aminolevulinic acid dehydratase

Ciclopirox olamine is a synthetic, broad-spectrum antifungal agent with additional antibacterial, anti-inflammatory and also recently antitumor activities.

Pimprinine is an alkaloid. It is a potent inhibitor of MAO (monoamine oxidase). More recently, pimprinine showed promising anticonvulsant activity in electric seizure threshold.

(-)-Cotinine is a major metabolite of nicotine in humans, it is a minor alkaloid found in tobacco plants.

LUF6283 is a partial agonist of hydroxycarboxylic acid receptor 2

VH 032 Linker 3 is a derivative of the proteolysis-targeting chimera technology (PROTAC) for PROTAC research and development; by incorporating an E3 ligase ligand and a short alkyl linker, it is ready for conjugation to a target protein ligand.

VH 032 Linker 6 is a derivative of the proteolysis-targeting chimera technology (PROTAC) for PROTAC research and development; by incorporating an E3 ligase ligand and a PEG2 linker with terminal alkyne, it is ready for conjugation to a target protein ligand

VH032-linker 5 is a derivative of the proteolysis-targeting chimera technology (PROTAC) for PROTAC research and development; by incorporating an E3 ligase ligand and an alkyl C4 linker with terminal carboxylic acid, it is ready for conjugation to a target protein ligand.

CMS121 is a substituted quinoline that has neuroprotective, anti-inflammatory, antioxidative, and renoprotective activities.

Diflapolin is a potent dual soluble epoxide hydrolase (sEH)/5-lipoxygenase-activating protein (FLAP) inhibitor

L-778123 is an inhibitor of FPTase and GGPTase-I, which was developed in part because it can completely inhibit Ki-Ras prenylation. The combination of L-778,123 and radiotherapy at dose level 1 showed acceptable toxicity in patients with locally advanced pancreatic cancer. Radiosensitization of a patient-derived pancreatic cancer cell line was observed.

Nepodin, also know as Musizin; is a naphthol that has been found in Rumex and has diverse biological activities

Quazinone, is a phosphodiesterase 3 (PDE3) inhibitor and novel cardiotonic agent with vasodilating properties.

ST 045849 is an O-GlcNAc transferase (OGT) inhibitor, it can reduce proliferation and viability of prostate cancer cells in vitro.

MB-0223 is a novel potent and selective STING agonist.

GSK 2239633A, is a potent CCR4 antagonist.

(±)-Liquiritigenin is a flavonoid that has anticancer activity.

LH1307 is an inhibitor of the interaction between programmed cell death 1 (PD-1) and its ligand PD-L1.

YE-120 is an agonist of G protein-coupled receptor 35 (GPR35).

RJR 2429 (dihydrochloride) is a nicotinic acetylcholine receptor (AChR) agonist that displays selectivity for α4β2

Pyropheophorbide-a methyl ester (MPPa) is a PDT photosensitizer, and is also a semisynthetic natural product derived from chlorophyll a. The absorption peak of MPPa in organic solvent and in cells was at 667 and 674 nm, respectively. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide reduction assay showed that MPPa had no dark cytotoxicity.

Chlorin E6 is a natural molecule and a promising photosensitizer. Chlorin E6 usually can be made from Live chlorella and other green plants . Chlorin E6 is an attractive photodynamic therapy (PDT) drug candidate because of (1) its high absorption in the red spectral region , and (2) its low cost to make compared to other porphyrin-based PDT drugs . Chlorin E6 exhibits advantageous photophysical properties for PDT such as having long lifetimes in their photoexcited triplet states and high molar absorption in the red region of the visible spectrum. Moreover, a 664-nm laser light can penetrate tissue deeper that the 630-nm laser light used for Photofrin. Chlorin E6 is also an important starting material for making PDT drug Talaporfin sodium (mono-L-aspartyl chlorin e6, NPe6).

TPT-172, also known as R33 (described in Mecozzi et al' s paper), is a thiophene thiourea derivative with molecule weight 172 in free base form. There is no formal name yet, we temporally call this molecule as TPT-172.

TPT-197 is a thiophene thiourea derivative with molecule weight 197 in free base form. There is no formal name yet, we temporally call this molecule as TPT-197. Please also see similar products: TPT-197; TPT-260; TPT-172.

ML3403 is a potent and selective p38 MAP kinase inhibitor. ML3403 has potent anti-inflammatory activity in airway smooth muscle.

ML-314 is a brain penetrant nonpeptidic β-arrestin biased ggonist of the neurotensin NTR1 receptor, which exhibits full agonist behavior against NTR1 (EC50 = 2.0 μM) in the primary assay and selectivity against NTR2. The effect of ML314 is blocked by the NTR1 antagonist SR142948A in a dose-dependent manner. Unlike peptide-based NTR1 agonists, ML314 has no significant response in a Ca2+ mobilization assay and is thus a biased agonist that activates the β-arrestin pathway rather than the traditional Gq coupled pathway. This bias has distinct biochemical and functional consequences that may lead to physiological advantages. ML314 displays good brain penetration in rodents, and studies examining its in vivo properties are underway.

Oliceridine, also known as TRV130, is a μ- opioid receptor agonist, that is currently under evaluation in human clinical trials for the treatment of acute severe pain. It is a functionally selective μ-opioid receptor agonist developed by Trevena Inc. TRV130 elicits robust G protein signaling, with potency and efficacy similar to morphine, but with far less β-arrestin 2 recruitment and receptor internalization, it displays less adverse effects than morphine. (http://en.wikipedia.org/wiki/TRV130).

MCOPPB is a drug which acts as a potent and selective agonist for the nociceptin receptor, with a pKi of 10.07 and much weaker activity at other opioid receptors. It has only moderate affinity for the mu opioid receptor, weak affinity for the kappa opioid receptor and negligible binding at the delta opioid receptor. In animal studies, MCOPPB produces potent anxiolytic effects, with no inhibition of memory or motor function, and only slight sedative side effects which do not appear until much higher doses than the effective anxiolytic dose range. (http://en.wikipedia.org/wiki/MCOPPB)

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.

Idalopirdine, also known as Lu AE58054 or Iladopirdine, is a potent and selective 5-HT6 receptor antagonist under development by Lundbeck as an augmentation therapy for the treatment of cognitive deficits associated with Alzheimer's disease and schizophrenia. It is in phase III clinical trials. Lu AE58054 displayed high affinity to the human 5-HT(6) receptor (5-HT(6)R) with a Ki of 0.83 nm. Lu AE58054 demonstrated >50-fold selectivity for more than 70 targets examined. Lu AE58054 is a selective antagonist of 5-HT(6)Rs with good oral bioavailability and robust efficacy in a rat model of cognitive impairment in schizophrenia. Lu AE58054 may be useful for the pharmacotherapy of cognitive dysfunction in disease states such as schizophrenia and Alzheimer's disease.

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.

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.

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.

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

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.

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.

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.

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.

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.

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.

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.

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.

BAM15 is a potent and selective mitochondrial uncoupler or protonophore. Chemical mitochondrial uncouplers are lipophilic weak acids that transport protons into the mitochondrial matrix via a pathway that is independent of ATP synthase, thereby uncoupling nutrient oxidation from ATP production. These uncouplers have potential for the treatment of diseases such as obesity, Parkinson’s disease, and aging.

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.

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).

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.

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

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.

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.

CTP354, also known as C-21191, a novel deuterated subtype-selective GABA(A) modulator. CTP may be potentially useful for treatment of neuropathic pain, spasticity and anxiety disorders. GABAA receptors are found in the nervous system and, when activated, reduce the transmission of certain nerve signals. Several classes of widely used drugs target GABAA receptors, including benzodiazepines, but do not have the receptor subtype selectivity of CTP-354.

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

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

PF-06260414 is a selective androgen receptor modulator, or SARM, which is developed to treat muscle weakening. Testosterone’s anabolic properties help develop muscle mass, and its androgenic activity is associated with reproduction. Improving muscle mass would improve quality of life and may even prolong survival in certain patient populations.

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.

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.

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.

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.

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.

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

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.

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.

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.

2-Phospho-L-ascorbic acid trisodium salt is a stable ascorbic acid derivative used in cell culture. In combination with FGF-2, it maintains differentiation potential in bone marrow-derived mesenchymal stem cells (MSC) through increased expression of HGF. L-Ascorbic acid 2-phosphate may be used in cell differentiation and tissue engineering applications. 2-Phospho-L-ascorbic acid trisodium salt also exhibits synergistic protection of hMSCs under oxidative stress in combination with N-acetylcysteine. Asc-2P is used in studies of gene repression, such as the repression of dihydrotestosterone-induced dickkopf-1 expression. AA2P has been shown to increase myogenin gene expression and promote differentiation in L6 muscle cells.

MI-192 is an inhibitor of histone deacetylases (HDACs) that preferentially inhibits HDAC2 (IC50 = 30 nM) and HDAC3 (IC50 = 16 nM) over HDAC1, 4, 6, 7, and 8 (IC50s = 4.8, 5, >10, 4.1, and >10 μM, respectively).

Prostratin is a protein kinase C activator found in the bark of the mamala tree of Samoa, Homalanthus nutans (Euphorbiaceae). While prostratin was originally isolated and identified as a new phorbol from species of the genus Pimelea (Thymelaceae) in Australia, the antiviral activity of prostratin was discovered during research on the traditional knowledge of Samoan healers in Falealupo village by ethnobotanist Paul Alan Cox and a team at the U.S. National Cancer Institute. Samoan healers use the mamala tree to treat hepatitis. Research indicated that prostratin has potential to be useful in the treatment of HIV as it could flush viral reservoirs in latently infected CD4+ T-cells. As a modulator of Protein Kinase C, it has been shown to exhibit promising therapeutic potential against other diseases such as cancer and Alzheimer's disease. In 2015, study showed that orally administrated prostratin repressed human pancreatic tumor. (Source: https://en.wikipedia.org/wiki/Prostratin). (Last update: 4/1/2016).

DY-268 is a trisubstituted-pyrazol carboamide based compound that acts as a potent FXR antagonist (IC50 = 7.5 nM). It does not display any FXR agonistic activity and cytotoxicity.

Cytosporone B is the first naturally occurring agonist for nuclear orphan receptor Nur77. The molecule binds with high affinity (IC50=0.278 nM) to the ligand-binding domain of Nur77 and stimulates Nur77-dependent activities. Nur77 is also involved in glucose homeostasis, where it induces genes involved in gluconeogenesis. Csn-B physically binds to Nur77 and activates its transactivational activity and translocation to mitochondria to induce apoptosis. It inhibits cancer cell proliferation and tumor growth.

Aphidicolin is a tetracyclic diterpene antibiotic isolated from the fungus, Cephalosporum aphidicola with antiviral and antimitotic properties. Aphidicolin is a reversible inhibitor of eukaryotic nuclear DNA replication. It blocks the cell cycle at early S phase. It is a specific inhibitor of DNA polymerase A,D in eukaryotic cells and in some viruses (vaccinia and herpesviruses) and an apoptosis inducer in HeLa cells. Natural aphidicolin is a secondary metabolite of the fungus Nigrospora oryzae.

MSC 2032964A is a potent and selective ASK1 inhibitor (IC50 = 93 nM). It blocks LPS-induced ASK1 and p38 phosphorylation in cultured mouse astrocytes and suppresses neuroinflammation in a mouse EAE model. MSC 2032964A is orally bioavailable and brain penetrant.

Abafungin is a broad-spectrum antifungal agent.

Alatrofloxacin Mesylate is the parental prodrug of Trovafloxacin, a broad-spectrum antibiotic.

AM 114 is a proteasome inhibitor. It is an inhibitor of chymotrypsin-like activity of the 20S proteasome. Also, AM-114 displays anticancer activity, inhibits cell growth in human colon cancer HCT116 p53+/+ cells.

AM-1235 is a drug that acts as a potent and is selective agonist for the cannabinoid receptor CB1.

AM-1248 is a drug that acts as a moderately potent agonist for both the cannabinoid receptors CB1 and CB2.

AM-2232 is a drug that acts as a potent but unselective agonist for the cannabinoid receptors.

AM-2233 is a highly potent full agonist for the cannabinoid receptors. It was developed as a selective radioligand for the cannabinoid receptors and has been used as its 131I derivative for mapping the distribution of the CB1 receptor in the brain. AM-2233 was found to fully substitute for THC in rats, with a potency lower than that of JWH-018 but higher than WIN 55,212-2.

AMG 009 is an orally active, small molecule CRTH2 (chemoattractant receptor-homologous molecule expressed on Th2 cells) and DP (D prostanoid) dual antagonist, which was in preclinical development in the US for the treatment of asthma and allergic rhinitis.

Anecortave Acetate is an angiostatic steroid used for proteomics research.

AR-9281 is a soluble epoxide hydrolase (s-EH) inhibitor potentially for the treatment of hypertension and type 2 diabetes.

Arundic Acidis is an astrocyte modulating agent, in acute ischemic stroke. It is a therapeutic agent for the treatment of neurodegenerative diseases including Alzheimer’s disease and Parkinson’s disease.

Avridine is a potent synthetic adjuvant that can induce arthritis. It is an immunomodulator and interferon-inducing agent.

AZ-11645373 is a potent and selective human P2X7 antagonist that is completely without effect at all other P2X subtypes. It also inhibits BzATP-mediated calcium influx and inhibits ATP-mediated IL-1β release.

AZD5423 is a nonsteroidal glucocorticoid by AstraZeneca used to treat respiratory diseases and in particular chronic obstructive pulmonary disease.

Barban is a selective herbicide for wild oats.

Bentazepam is a thienodiazepine which is a benzodiazepine analog. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. Peak plasma rates are achieved in around 2,5 hours after oral administration.

BIIE-0246 is a potent, selective and competitive non-peptide antagonist for the neuropeptide Y Y2 receptor. BIIE-0246 displays > 650-fold selectivity over Y1, Y4 and Y5 receptors.

Bucinnazine Hydrochloride, also known as AP-237 HCl, is an analgesic.

Carbenicillin disodium salt is a penicillin-derived, β-lactam antibiotic which inhibits the synthesis of peptidoglycan, a key component of the bacterial cell wall. Unlike most β-lactams, carbenicillin disodium is limited to primarily gram negative bacteria including Pseudomonas aeruginosa and common enteric species. In plants Carbenicillin was investigated for its effects on morphology and growth of Beta vulgaris, Capsicum annuum and Glehnia littoralis roots. Carbenicillin was noted to inhibit root elongation while promoting root branching in contrast to Ampicillin.

CGP-54626 is a selective antagonist of the GABAB receptor with an IC50 value of 4 nM.1 It can be used to investigate the role of GABAB receptors in neurological signaling.

CGP-77675 is a potent and selective Src family kinase (SFK) inhibitor. CGP-77675 inhibited phosphorylation of peptide substrates and autophosphorylation of purified Src (IC50: 5-20 and 40 nM, respectively). The dual inhibition of Src and GSK-3 signaling by CGP 77675 and CHIR 99021 was found to maintain mouse embryonic stem cell (mESC) self-renewal and pluripotency marker expression as efficiently as the dual inhibition of MAPK and GSK-3 by PD 0325901 and CHIR 99021.

Cianopramine hydrochloride is a bio-active chemical.

Climbazole is a potent inducer and inhibitor of P450-dependent drug metabolizing enzymes, which is also used as antifungal and antidandruff agent.

Clinafloxacin is an antimicrobial antibiotic that displays broad-spectrum antibacterial activity against Gram-positive, Gram-negative, and anaerobic pathogens by inhibiting the bacterial regulatory enzyme DNA gyrase (IC50 = 0.92 μg/ml) as well as topoisomerase IV (IC50 = 1.62 μg/ml).

Clorindione is a long acting oral anticoagulant.

Clorsulon is antihelminthic compound that is a potent fasciolicide. Clorsulon targets phosphoglycerate mutase and phosphoglycerate kinase. Clorsulon also discriminates between highly similar host and parasite enzymes.

CP 100356 is a high affinity P-glycoprotein (P-gp) inhibitor (Ki values are 58 and 94 nM for mouse Pgp1a and Pgp1b isoforms). Inhibits calcein-AM uptake in MDR1-transfected MDCKII cells (IC50 = 0.5 μM) and prazosin transport in BCRP-transfected MDCKII cells (IC50 = 1.5 μM). CP 100356 modulates multidrug resistance.

CP-55940 is a non-selective cannabinoid receptor agonist with Ki values of 0.58 and 0.69 nM for human recombinant CB1 and CB2, respectively.

CP-471474 is a broad spectrum Matrix Metalloprotease inhibitor (IC50 values are 0.7, 0.9, 13, 16 and 1170 nM for MMP-2, MMP-13, MMP-9, MMP-3 and MMP-1 respectively).

Cycloguanil is a dihydrofolate reductase inhibitor, and is a metabolite of the antimalarial drug proguanil; its formation in vivo has been thought to be primarily responsible for the antimalarial activity of proguanil. However, more recent work has indicated that, while proguanil is synergistic with the drug atovaquone (as in the combination Malarone), cycloguanil is in fact antagonistic to the effects of atovaquone, suggesting that, unlike cycloguanil, proguanil may have an alternative mechanism of antimalarial action besides dihydrofolate reductase inhibition.

Cyclopenthiazide is a thiazide diuretic used in the treatment of heart failure and hypertension. It increases the excretion of sodium and potassium ions and decrease the excretion of calcium ions and uric acid so they are contraindicated in patients with hyponatraemia, hypokalaemia, hypercalcaemia and hyperuricaemia.

Darglitazone, also known as CP-86,325-2, is PPAR-gamma agonist. Darglitazone restores acute inflammatory responses to cerebral hypoxia-ischemia in the diabetic ob/ob mouse. Darglitazone enhanced adipogenesis and caused cancellous bone loss by increasing bone resorption and decreasing bone formation in mice. In addition, darglitazone induced cortical bone loss on the endocortical surface but increased bone formation on the periosteal surface.

Devazepide is a potent, and orally active CCK1 (CCK-A) receptor antagonist that displays appetite-stimulant effects. It blocks the anorectic response to CCK-8 and increases food intake in rats following systemic and i.c.v administration.

Dexibuprofen, also known as S-ibuoprofen, is a non-steroidal anti-inflammatory drug. It is the active dextrorotatory enantiomer of ibuprofen. Most ibuprofen formulations contain a racemic mixture of both isomers. Dexibuprofen acts as cyclooxygenase inhibitor.

Anandamide, also known as N-arachidonoylethanolamine or AEA, is a fatty acid neurotransmitter derived from the non-oxidative metabolism of eicosatetraenoic acid (arachidonic acid) an essential ω-6 polyunsaturated fatty acid. The name is taken from the Sanskrit word ananda, which means "joy, bliss, delight", and amide. It is synthesized from N-arachidonoyl phosphatidylethanolamine by multiple pathways. It is degraded primarily by the fatty acid amide hydrolase (FAAH) enzyme, which converts anandamid.

Enrofloxacin is a fluoroquinolone antibiotic sold by the Bayer Corporation. It is a bactericidal agent. The bactericidal activity of enrofloxacin is concentration-dependent, with susceptible bacteria cell death occurring within 20–30 minutes of exposure. Enrofloxacin has demonstrated a significant post-antibiotic effect for both Gram-negative and Gram-positive bacteria and is active in both stationary and growth phases of bacterial replication.

Famphur is an organic thiophosphate and an organothiophosphate insecticide. It has a role as an EC 3.1.1.7 (acetylcholinesterase) inhibitor, an agrochemical, and an anthelminthic drug. Use of famphur as an insecticide is restricted.

Febantel is an oral anthelmintic. It is a prodrug metabolised in vivo to fenbendazole. Febantel is used for the treatment and control of gastro-intestinal roundworms, lung worms and tapeworms.

Fenclonine acts as a selective and irreversible inhibitor of tryptophan hydroxylase, which is a rate-limiting enzyme in the biosynthesis of serotonin. It has been used experimentally to treat carcinoid syndrome.

Fentrazamide is a herbicide.

Florfenicol is a fluorinated synthetic analog of thiamphenicol , mainly used in veterinary medicine. It is used for the treatment of bovine respiratory disease (BRD) associated with Mannheimia (Pasteurella) haemolytica, Pasteurella multocida, and Haemophilus somnus, for treatment of bovine interdigital phlegmon.

Flubenzimine is a bio-active chemical. Detailed information has not been published.

Fuberidazole is a chemical compound used in fungicides.

Gaboxadol, also known as THIP, OV-101; Lu-02-030; MK-0928; Lu-02030, is a GABA agonist. It is an inhibitor of GABA uptake systems. Gaboxadol can also be a non-opioid analgesic and a novel type of hypnotic.

BH3I-2' is a cell-permeable BH3 mimetic which induces apoptosis by specifically preventing BH3 domain-mediated interactions between pro-apoptotic and anti-apoptotic members of the Bcl-2 family, thereby blocking the interaction between Bak BH3 and Bcl-x by targeting the Bcl-x binding pocket.

Denopamine is a ?1-Adrenoceptor agonist.

PF-4479745 ia a potent and selective 5-HT2C receptor agonist.

Lasalocid A is a cationic ionophore antibiotic.

Dehydroleucodin is an inducer of cell cycle arrest, senescence and apoptosis, inhibiting tumor growth in a preclinical melanoma model.

PD-144418 Oxalate is a novel selective sigma ligand.

VU0409106 is a potent and selective inhibitor of mGlu5.

Icaridin, also known as picaridin andKBR 3023, is an insect repellent. It has broad efficacy against various insects and is almost colorless and odorless.

nor-Binaltorphimine dihydrochloride is a long-acting potent and highly selective kappa opioid receptor antagonist.

Ionox 330 is an alkylphenol compound used as antioxdiant.

Iopromide is a low osmolar, non-ionic contrast agent for intravascular use. Iopromide is a molecule used as a contrast medium.

SM16 is a novel Type I TGF-β signaling inhibitor.

Thiolutin, also known as Acetopyrrothin aand NSC-3927, is an antibiotic and anti-angiogenic agent, acting as a zinc chelator that inhibits the Rpn11 and other JAMM metalloproteases.

AM4113 is a cannabinoid receptor 1 (CB1)-selective antagonist.

Levobunolol Hydrochloride is a non-cardioselective adrenergic beta-receptor antagonist with anti-glaucoma activity.

GSK2578999A is a betulin derivative as antitumor agent.

Iodophenpropit Dihydrobromide is a potent and selective H3 antagonist.

Agmatine Sulfate is a neurotransmitter and neuromodulator, inhibiting N-methyl-D-aspartate (NMDA), nicotinic acetylcholine receptors nitric oxide synthase, calcium channels and certain serotonin receptors, activating imidazoline receptors.

NNC63-0532 is a potent and selective non-peptide agonist of the NOP receptors.

Lanatoside C is an anticancer agent, acting through protein kinase C-delta (PKCdelta) to cause apoptosis of human hepatocellular carcinoma cells.

cis-ABCD is a potent, competitive and selective inhibitor of glutamate uptake.

DPO is a quorum sensing (QS) autoinducer, binding to and activating a transcription factor, VqmA.

GW405833, also klnown as L-768242, is a cannabinoid-2 (CB(2)) receptor-selective agonist. It displays anti-nociceptive activity in models of neuropathic and inflammatory pain.