Lanicemine (free base) is a low-trapping NMDA receptor antagonist. Lanicemine is used the management of severe and treatment-resistant depression. Lanicemine was originally developed as a neuroprotective agent, but was redeveloped as an antidepressant.

RL648_81 is a novel potent and selective activator of KCNQ2/3 channels.

TH1020 is a novel Toll-Like Receptor 5 (TLR5)/Flagellin Complex Inhibitor with promising activity (IC50 =0.85±0.12?μm) and specificity. TH1020 was shown to repress the expression of downstream TNF-α signaling pathways mediated by the TLR5/flagellin complex formation. Based on molecular docking simulation, TH1020 is suggested to compete with flagellin and disrupt its association with TLR5. TH1020 provides a much-needed molecular probe for studying this important protein-protein interaction and a lead compound for identifying novel therapeutics targeting TLR5.

Neoseptin-3 is a novel specific agonist of the mouse TLR4 (mTLR4)/myeloid differentiation factor 2 (MD-2) complex.

GSK984 is a negative control probe for GSK983 (GLXC-08449).

Rbin-2 is a novel cell penetrant, potent, selective and reversible inhibitor of Midasin, inhibiting eukaryotic ribosome biogenesis and directly targeting AAA+ ATPase Midasin.

HPB is a selective inhibitor of HDAC6 deacetylase.

ORM-3819 is a novel selective and potent inhibitor of PDE III, promoting cardiac contractility through Ca(2+) sensitization.

LY 116467 is a dopamine agonist. LY116467 increases serum corticosterone concentration in rats at a dose of 3 mg/kg.

LY 215840 is a potent 5-hydroxytryptamine (5-HT)2 receptor antagonist. It has anti-hypertensive and muscle relaxant effects in animal studies.

LY 255283 is a a specific leukotriene B4 (LTB4) receptor antagonist. It inhibits the production of LTB(4) in human peripheral blood polymorphonuclear leukocytes (PMNL) and in monocytes activated by calcium ionophore A23187.

LY-301664 is a bio-active chemical.

RI(dl)-2 is a selective inhibitor of Rad51-mediated D-loop formation.

Targapremir-210 is a novel inhibitor of microRNA-210, reprograming an oncogenic hypoxic circuit.

Mavacoxib is a veterinary drug used to treat pain and inflammation in dogs with degenerative joint disease. It acts as a COX-2 inhibitor.

Meclofenamate sodium is a potent nonsteroidal antiinflammatory agent, specifically inhibits chemotactic factor-induced human polymorphonuclear leukocyte functions: chemotaxis, degranulation, and generation of superoxide anion radicals. These effects of MSM were found to be dependent upon the concentrations of drug not bound to albumin (free drug), and were caused by its ability to interfere at both a receptor and post-receptor (i.e., a step distal to mobilization of polymorphonuclear leukocyte intracellular Ca2+) level.

Metaproterenol, also known as Th-152 and Orciprenaline, is used for asthmatic children with therapeutic serum theophylline concentrations. In the recommended doses, metaproterenol can improve pulmonary function in asthmatic children who have abnormal pulmonary function while being maintained on theophylline.

Methiocarb is a carbamate pesticide which is used as a bird repellent, insecticide, acaricide and molluscicide. Methiocarb inhibits reversibly acetylcholinesterase activity resulting in a cholinergic stimulation making methiocarb a potent neurotoxin.

Methyldopa is a centrally acting antihypertensive agent. It is metabolized to alpha-methylnorepinephrine in the brain, and this compound activates central alpha-2 adrenergic receptors. Being a selective agonist for α2 adrenergic receptors, psychoactive drug is used as a sympatholytic or antihypertensive.

Aromatic diamine used in the plastics industry as curing agent for epoxy resins and urethane rubbers. It is a curing agent in polyurethane production. It causes bladder, liver, lung, and other neoplasms.

Aminocarb Aminocarb is an carbamate insecticide widely used to protect cotton fields, crop fields, and forests from insect infestation. It helps in the control of aphids, soil mollusks, lepidopterous larvae, and other types of chewing insects.

MMPX is a selective inhibitor of Ca2±calmodulin-dependent phosphodiesterase I (PDE1).

MK-912 is a potent new selective alpha 2-adrenergic receptor antagonist that is active orally, to study the effect of short-term, selective alpha 2-blockade on fasting plasma glucose (FPG) and pancreatic islet function in non-insulin-dependent diabetes (NIDDM).

Morantel tartrate is an Antinematodal agent and anthelmintic used mainly for livestock.

Muraglitazar is a Peroxime Proliferator Activated (PPAR) Agonist that has glucose- and lipid-lowering activities. It is used for the treatment of Type-2 Diabetes Mellitus, Mixed Dyslipidemia, Atherosclerosis, and Metabolic Syndrome (Dual (alpha and gamma). Muraglitazar improves glycaemic control by enhancing insulin sensitivity and β cell function in T2DM (Type 2 Diabetes Mellitus) subjects, improves multiple cardiovascular risk factors, reduces muscle, visceral and hepatic fat content in T2DM subjects.

Naftalofos is an insecticide and an anthelmintic. Naftalofos represents an effective therapeutic alternative for incorporation into worm control programmes.

(S)-Warfarin is a more potent enantiomer of Warfarin as a vitamin K antagonist, anticoagulant.

Navuridine, also known as 3’-Azido-2’,3’-dideoxyuridine, is a dideoxyuridine inhibitor of HIV reverse transcriptase that is related to zidovudine. Navuridine exhibits a relatively short half-life and incomplete oral bioavailability and has not been developed into a clinical drug.

Naxagolide is a sustained release formulation of a naphthoxazine compound with selective D-2 dopamine receptor agonism. It is a dopamine agonist and an Antiparkinsonian.

NBI-27914 is a Corticotropin-Releasing Factor Antagonist of the CRF1 and CRF2 recepetors (Corticotropin-releasing factor).

Netropsin is a basic polypeptide isolated from Streptomyces netropsis. It is cytotoxic and its strong, specific binding to A-T areas of DNA is useful to genetics research. Netropsin is a polyamide with antibiotic and antiviral activity. It has been shown that Netropsin is active both against Gram-positive bacteria and Gram-negative bacteria.

Nitromifene Citrate A non-steroidal estrogen antagonist (as the 1:1 citrate) most commonly used as a research tool in animal studies.

Olaquindox is used in prevention of swine dysentary. It is also a growth promoting additive in pig feed.

Omigapil maleate is a drug that was developed by Novartis and tested in clinical trials for its ability to help treat Parkinson's disease (PD) and amyotrophic lateral sclerosis (ALS). The development for PD and ALS have been terminated due to lack of benefit, but Santhera Pharmaceuticals bought the compound for development for the treatment of congenital muscular dystrophy (CMD).

MNI-caged-L-Glutamate is a photo sensitive probe, releasing glutamate when photolysed with wavelength between 300 - 380 nm.

MR2034 is a kappa-Opioid receptor agonist, stimulating hypothalamic-pituitary-adrenal axis.

Oxantel Pamoate is an anthelmintic used to treat Trichuris trichiura infection.

Oxfenicine, also known as UK-25842, is a carnitine palmitoyltransferase I (CPT-1) inhibitor involved in fatty acid metabolism in the heart. In animal studies oxfenicine acts as a cardioprotective agent during ischemia. Oxfenicine produces changes in myocardial substrate utilisation and is attributed to the protection of ischemic stressed myocardium by shifting the cardiac metabolism with reduction of FFA (Free Fatty Acid) utilisation. This may be favourable in circumstances with limited oxygen supply.

Papaverine Hydrochloride, USP, is the hydrochloride of an alkaloid obtained from opium or prepared synthetically. It belongs to the benzylisoquinoline group of alkaloids. It does not contain a phenanthrene group as do morphine and codeine. The most characteristic effect of papaverine is relaxation of the tonus of all smooth muscle, especially when it has been spasmodically contracted. Papaverine Hydrochloride apparently acts directly on the muscle itself. This relaxation is noted in the vascular system and bronchial musculature and in the gastrointestinal, biliary and urinary tracts.

PD 109488 is a metabolite of quinapril. PD 109488, otherwise known as Quinapril Diketopiperazine, is a derivative of Quinapril that acts as an ACE inhibitor. Inhibition of ACE prevents the conversion of signaling peptide angiotensin I into angiotensin II, which acts as a potent vasoconstrictor. Reduced levels of angiotensin II also reduces the amount of aldosterone that is expressed due to RAAS signaling.

PD 135158 is a Selective cholecystokinin type B (CCKB)/gastrin receptor agonist. In studies, PD- 135158 stimulates lipase release from isolated rat pancreatic acini dose dependently in a biphasic manner, with identical efficacy but lower potency compared to cholecystokinin octapeptide (CCK-8). PD 135158 is classified into Anti-Anxiety Agents, Central Nervous System Agents, Central Nervous System Depressants, Psychotropic Drugs, and Tranquilizing Agents.

(S)-alpha-Fluoromethylhistidine HCl is a potent irreversible histidine decarboxylase (HDC) inhibitor and glutathione S-transferase inhibitor. a-FMH was demonstrated to be an effective inhibitor of GST at micromolar concentration, suggesting that off-target effects of a-FMH may limit physiological drug metabolism and elimination by GST-dependent mechanisms.

Oxantel is a fumarate reductase inhibitor; Anthelmintic.

Nitrocefin is an antibiotic, being sensitive to hydrolysis by all lactamases produced by gram-positive and gram-negative bacteria.

NB-64 is a novel human immunodeficiency virus type 1 (HIV-1) entry inhibitor, interferring with the gp41 six-helix bundle formation and blocking virus fusion.

Tiaprost is a prostaglandin F2 alpha analogue as an estrus-synchronizing agent.

MEK Inhibitor I is a selective and potent inhibitor of MEK.

TrxR-IN-D9, also known as D9, is a novel inhibitor of thioredoxin reductase (TrxR).

PD-176252 is a non-peptide gastrin-releasing peptide receptor (GRP-R, BB2) and neuromedin B receptor (NMB-R, BB1) antagonist (Ki values are 0.17 and 1.0 nM for BB1 and BB2 respectively). It inhibits proliferation of rat C6 glioma cells (IC50 = 2 μM) and inhibits NCI-H1299 xenograft proliferation in nude mice (IC50 = 5 μM).

NCL00017509 is a potent and reversible NIMA related kinase 2 (Nek2) inhibitor.

PD-198306 is a cell-permeable amino-benzamide compound that acts as a potent and non-ATP-competitive inhibitor of MEK1/2 (IC50 = 8 nM) with an excellent selectivity over ERK, c-Src, Cdk's, and PI 3-Kγ (IC50 >1.0 μM).

Pencycuron, also known as Monceren, is a phenylurea fungicide.

Periciazine is a drug that belongs to the phenothiazine class of typical antipsychotics. Periciazine is used to treat short-term severe anxiety or tension and in the maintenance treatment of psychotic disorders such as schizophrenia.

5-BDBD is a selective inhibitor of P2X4.

LP117 is a novel drug-specific modulator of ABCB1-mediated drug transport.

CPT is a potent adenosine A1 receptor antagonist.

Fenirofibrate is a metabolite of Fenofibrate.

Sulfidefluor-7 AM is a novel hydrogen sulphide (H2S) fluorescent probe.

Rauwolscine hydrochloride is an alpha2-Adrenergic antagonist and partial agonist at 5-HT1A receptors.

Desmosterol is an endogenous agonist of RORgamma; Intermediate in the synthesis of cholesterol.

L-670596 is a potent and selective thromboxane A2/prostaglandin endoperoxide receptor antagonist, also showing ALDH1A1 specific inhibitory activity.

Propachlor is a specific ALDH1A1 inhibitor. It is sometimes used as an herbicide.

PBI-51 is a competitive Inhibitor of Abscisic Acid-Regulated Gene Expression.

Levoglucosenone is a cytotoxic, against human hepatocarcinoma cell lines.

PHA-543613 acts as a potent and selective agonist for the α7 subtype of neural nicotinic acetylcholine receptors, with a high level of brain penetration and good oral bioavailability. It is under development as a possible treatment for cognitive deficits in schizophrenia.

PDP-EA is an FAAH activator, enhancing amidohydrolase activity of FAAH.

Phenthoate is an organothiophosphate insecticide. It is used against Lepidoptera, jassids, aphids, soft scales, mosquitoes, blowflies, houseflies, and ked.

Physostigmine salicylate is a reversible cholinesterase inhibitor, a parasympathomimetic alkaloid. It also can cross the blood-brain barrier and is used when central nervous system effects are desired, as in the treatment of severe anticholinergic toxicity.

Piromidic acid is antibacterial against mainly gram negative organisms. It is used for urinary tract and intestinal infections.

Sulfaclozine is an antiprotozoal.

HHQ is an antagonist of PqsR.

rac-CCT-250863 is a potent Nek2 inhibitor. exhibiting selectivity for Nek2 over PLK1, MPS1, Cdk2 and Aurora A.

Fenpyroximate is an acaricide and insecticide, blocking the mitochondrial electron transport in complex I.

PNU-142633 selective, high affinity 5-HT1D receptor antagonist and is an experimental drug candidate for the treatment of migraine.

Glibornuride is a blocker of adenosine 5'-triphosphate (ATP)-sensitive K+ channels (KATP channels).

H2DCFDA is a fluorescent cell permeabl ROS indicator.

Procaterol is an intermediate-acting β2 adrenoreceptor agonist used for the treatment of asthma.

Propanidid, also known as Sombrevin, is a short-acting phenylacetate general anesthetic.

Propoxur is a carbamate insecticide. Propoxur is a non-systemic insecticide with a fast knockdown and long residual effect used against turf, forestry, and household pests and fleas.

Danofloxacin is a fluoroquinolone antibiotic used in veterinary medicine.

Pyrazoloacridine is an investigational nucleic acid binding agent that inhibits the activity of topoisomerases 1 and 2. Pyrazoloacridine was a phase II clinical study to determine the efficacy and toxicities of PZA in patients with metastatic breast cancer (MBC)Pyrazoloacridine appears to intercalate into DNA and inhibit RNA synthesis, DNA synthesis, and the activities of topoisomerases I and II, thereby causing cytotoxicity.

Talniflumate is a novel potent and selective inhibitor of core mucin-synthesizing enzyme GCNT3 (core 2b-1,6 N-acetylglucosaminyltrans-ferase).

Propranolol Hydrochloride is a non-cardioselective beta-adrenergic antagonist. It has been shown to be active against disorders including cardiac infarcations, arrhythmias, hypertension, and hyperthyroidism.

Quinaprilat is the active metabolite of quinapril, an angiotensin-converting enzyme inhibitor (ACE inhibitor) used in the treatment of hypertension and congestive heart failure.

FSB is a highly fluorescent amyloid-specific dye.

A-350619 hydrochloride is an activator of soluble guanylyl cyclase (sGC).

Cyclo-L-Trp-L-Trp is a broad spectrum antifungal, inducing a high degree of acetylation of histones.

2-DG is an inhibitor of glycolysis via its actions on hexokinase, the rate limiting step of glycolysis.

Aminotadalafil is an analog of Tadalafil as a phosphodiesterase type 5 (PDE-5) inhibitor.

Ro 24-7429 is a Tat antagonist. Ro 24-7429 blocks the action of the HIV tat protein and is an analog of Ro 5-3335.

TBMP is a novel inhibitor of the viral envelope protein hemagglutinin (HA)-mediated entry.

2-Hydroxysaclofen is a GABA-B antagonist.

Suprafenacine is a novel cell permeable selective inhibitor of cancer cell proliferation, binding microtubules at the colchicine-binding site and inhibiting polymerization, leading to G2/M cell cycle arrest and cell death via a mitochondria-mediated apoptotic pathway.

SB 224289 is a selective 5-HT1B receptor antagonist (pKi = 8.2). SB 224289 displays > 60-fold selectivity over 5-HT1D, 5-HT1A, 5-HT1E, 5-HT1F, 5-HT2A and 5-HT2C receptors in radioligand binding and functional assays. SB 224289 is a centrally active following oral administration in vivo.

Myoseverin is an inducer of the reversible fission of multinucleated myotubes into mononucleated fragments, affecting the expression of a variety of growth factor, immunomodulatory, extracellular matrix-remodeling, and stress response genes, consistent with the activation of pathways involved in wound healing and tissue regeneration.

Triclabendazole is an anthelmintic and fasciolicidal, binding to beta-tubulin and preventing the polymerization of the microtubules of which they are part. Studies in vitro and/or in infected animals suggest that triclabendazole and its active metabolites (sulfoxide and sulfone) are absorbed by the tegument of the immature and mature worms, leading to a decrease of the resting membrane potential, inhibition of tubulin function as well as protein and enzyme synthesis. These metabolic disturbances are associated with inhibition of motility, disruption of the surface as well as ultrastructure that includes inhibition of spermatogenesis and vitelline cells.

Pyrabactin is a plant growth inhibitor, acting as a seed-selective abscisic acid (ABA) agonist; Novel PYL agonist.

SCH-23390 is a potent dopamine receptor antagonist (Ki values are 0.2 nM and 0.3 nM at D1 and D5 receptor sub-types, respectively). SCH-23390 is also an agonist at 5-HT1C and 5-HT2C receptors in vitro (Ki values are 6.3 nM and 9.3 nM respectively). It blocks quinpirole-induced Kir3 (GIRK) currents (EC50 = 268 nM) independently of receptors.

HA-1004 is an inhibitor of PKA, cGKI, PKC, MYLK, and calcium channel protein.

Sofalcone is an oral gastroprotective, gastrointestinal medication. It is a synthetic analog of sophoradin.

BMS-770767 is a novel inhibitor of 11-betahydroxysteroid dehydrogenase type I (11?-HSD1).

CP-944629 is a novel, potent, and selective p38alpha inhibitor.

MHY908 is a novel inhibitor of melanogenesis, potently inhibiting mushroom tyrosinase activity in a dose-dependent manner.

Sulfamonmethoxine is a competitive inhibitor of dihydropteroate synthetase, blocking the synthesis of folic acid.

Sudoxicam is a nonsteroidal anti-inflammatory drugs (NSAIDs) from the enol-carboxamide class.

Sulbactam pivoxil, also known as CP-47904 and Pivsulbactam, is an irreversible inhibitor of β-lactamase; it binds to the enzyme and does not allow it to degrade the antibiotic.

GNE-140 racemic is a novel potent lactate dehydrogenase (LDHA) inhibitor. In MIA PaCa-2 human pancreatic cells, LDHA inhibition rapidly affected global metabolism, although cell death only occurred after 2 d of continuous LDHA inhibition. Pancreatic cell lines that utilize oxidative phosphorylation (OXPHOS) rather than glycolysis were inherently resistant to GNE-140, but could be resensitized to GNE-140 with the OXPHOS inhibitor phenformin. Acquired resistance to GNE-140 was driven by activation of the AMPK-mTOR-S6K signaling pathway, which led to increased OXPHOS, and inhibitors targeting this pathway could prevent resistance.

HUN85199, also known as B-Raf inhibitor 1 dihydrochloride, is a novel potent and selective B-Raf inhibitor. HUN85199 has CAS#1191385-19-9, was first reported in Journal of Medicinal Chemistry (2009), 52(20), 6189-6192. It has no code name. For the convenience of scientific communication, we name it as HUN85199 by using CAS# ahdn inchi key as proposed by Hodoodo Chemical Nomenclature (see https://hodoodo.com/hodoodo-chemical-nomenclature).

FKGK11 is a novel potent inhibitor of GVIA iPLA2 with little or no inhibition against GIVA cPLA2 (XI(50) = 0.0073 and >0.91, respectively).

CP-24879 hydrochloride is a D5D/D6D dual-inhibitor, showing beneficial effects against increased intracellular lipid accumulation and inflammatory injury in hepatocytes.

Z-LLNle-CHO, also known as gamma-Secretase Inhibitor I, is a cell permeable inhibitor of gamma-secretase, inducing apoptosis of human glioblastoma tumor-initiating cells by proteasome inhibition and mitotic arrest response.

AZ-PFKFB3-67 is a novel potent and selective PFKFB3 inhibitor.

Tebuconazole is a triazole fungicide used agriculturally to treat plant pathogenic fungi. Though the U.S. Food and Drug Administration considers this fungicide to be safe for humans, it may still pose a risk. It is listed as a possible carcinogen in the United States Environmental Protection Agency Office of Pesticide Programs carcinogen list with a rating of C (possible carcinogen). Its acute toxicity is moderate. According to the World Health Organization toxicity classification, it is listed as III, which means slightly hazardous.

Thiolactomycin is a novel reversible dual inhibitor of D-Aspartate oxidase (DDO) and D-amino acid oxidase (DAO).

Proxyfan Oxalate is a potent histamine H3 receptor ligand, acting as a protean agonist with activity ranges from full agonist to inverse agonist depending on system used. also displaying partial agonist effects on cAMP inhibition and MAPK activity, neutral antagonist activity on histamine release and partial inverse agonism of [3H]-arachidonic acid release.

MAFP is an irreversible inhibitor of Ca(2+)-independent phospholipase A2 (iPLA2).

Tomelukast, also known as LY171883, is a leukotriene inhibitor. Tomelukast showed protective effects in traumatic shock. LY-171883 stimulates the activity of BK(Ca) channels in a manner unlikely to be linked to its blockade of leukotriene receptors or stimulation of peroxisome proliferator-activated receptors. The stimulatory effects on these channels may, at least in part, contribute to the underlying cellular mechanisms by which LY-171883 affects neuronal or neuroendocrine function.

TMI-1 is a novel orally active inhibitor of ADAM17 (TACE) and MMP, inducing tumor apoptosis in a breast cancer.

Triadimefon is an azole fungicide.

SKF1 is a suppressor of the ability of FK506 to inhibit cell growth in the presence of high levels of NaCl, inducing cell death in low salt conditions, interacting directly with yeast mitochodria.

Triadimenol is a flammable white to gray solid with phenolartigem odor which is practically insoluble in water. It decomposes when heated above 150 ° C. The compound is present in several isomeric front forms, the technical product to 78 to 88% of the diastereoisomer A is (RS + SR). The compound is stable to hydrolysis at pH values ??of 4, 7 and 9 and is subject to a small extent of photolysis. Triadimenol is a systemic fungicide with a broad spectrum. It inhibits the ergosterol - and gibberellin - biosynthesis , and thus the rate of cell division.

Triflumuron is an insecticide belonging to the group of so-called insect growth regulators. It inhibits the synthesis of chitin by the insect larvae, causing the die. This operation is similar to that of, inter alia, flufenoxuron , lufenuron and novaluron ; triflumuron belongs to the same group of benzoylureas. It is a product of Bayer CropScience ; Alsystin brand. It is applied to apples, pears, peaches, nectarines and mushrooms, as well as in the storage of cereals.

KUN79359, also known as PKC? inhibitor, is a potent and selective inhibitor of PKC? isozymes. KUN79359 has no formal name, and has CAS#257879-35-9. For the convenience of scientific communication, it is named as KUN79359. The name was generated based on Hodoodo chemical nomenclature.

Vibunazole is an antifungal agent

Way 100135 is a serotonergic drug of the phenylpiperazine family which is used in scientific research. It acts as potent 5-HT1A receptor antagonist, and was originally believed to be highly selective, but further studies have demonstrated that it also acts as a partial agonist of the 5-HT1D receptor (pKi = 7.58; virtually the same affinity for 5-HT1A), and to a much lesser extent, of the 5-HT1B receptor (pKi = 5.82). These findings may have prompted the development of the related compound WAY-100,635, another purportedly selective and even more potent 5-HT1A antagonist, which was synthesized shortly thereafter.

Xylazine is an analogue of clonidine and an agonist at the α2 class of adrenergic receptor. It is used for sedation, anesthesia, muscle relaxation, and analgesia in animals such as horses, cattle and other non-human mammals. Veterinarians also use xylazine as an emetic, especially in cats.

Zeranol is a non-steroidal estrogen agonist. It is a mycotoxin, derived from fungi in the Fusarium family, and may be found as a contaminant in fungus-infected crops. It is 3-4x more potent as an estrogen agonist than the related compound zearalenone. Zeranol increases cancer cell proliferation in already existing breast cancer. There are mixed results to whether zeranol has anticancer or carcinogenic properties in non cancer containing breast cells depending on dose. Overall evidence points to zeranol being a risk factor and promoter for cancer. However, dietary exposure from the use of zeranol-containing implants in cattle is insignificant.

Zoniporide: a potent and selective inhibitor of the human sodium-hydrogen exchanger isoform 1 (NHE-1). Zoniporide preserves left ventricular compliance during ventricular fibrillation and minimizes postresuscitation myocardial dysfunction through benefits on energy metabolism. Zoniporide produces clinical, electrophysiologic, and microscopic evidence of peripheral sensory axonopathy and establishes the importance of careful preclinical evaluation of neurological function.

Zopolrestat is a aldose reductase inhibitor potentially for the treatment of diabetic nephropathy and diabetes.

GYKI-23107 is an antiarrhythmic agent with local anaesthetic activity. GYKI-23107 was effective against chemically (aconitine and ouabain) induced arrhythmias after both parenteral and oral administration. GYKI-23107 and mexiletine produced similar elevation of the fibrillation threshold in anaesthetized cats. After oral pretreatment, GYKI-23107 showed protective effects against coronary ligation-induced arrhythmia in conscious rats. The circulatory side-effects of GYKI-23107 in anaesthetized and conscious dogs and cats were milder then those of mexiletine.

CRANAD-2 is a difluoroboron-derivatized curcumins as near-infrared probe for in vivo detection of amyloid-beta deposits. Upon interacting with Abeta aggregates, CRANAD-2 undergoes a range of changes, which include a 70-fold fluorescence intensity increase, a 90 nm blue shift (from 805 to 715 nm), and a large increase in quantum yield. Moreover, this probe also shows a high affinity for Abeta aggregates (K(d) = 38.0 nM), a reasonable log P value (log P = 3), considerable stability in serum, and a weak interaction with albumin. After intravenous injection of this probe, 19-month-old Tg2576 mice exhibited significantly higher relative signal than that of the control mice over the same period of time.

L-655708, also known as FG-8094, is a nootropic drug. L-655708 acts as a subtype-selective inverse agonist at the α5 subtype of the benzodiazepine binding site on the GABAA receptor. A radiolabelled form of L-655708 was used to map the distribution of the GABAA α5 subtype in the brain. L-655708 was indeed found to produce improved cognitive performance in animal studies, without producing the side effect of convulsions which is produced by non-selective inverse agonists like DMCM.

Procarbazine is an antineoplastic chemotherapy drug for the treatment of Hodgkin's lymphoma and certain brain cancers (such as glioblastoma multiforme). It is a member of a group of medicines called alkylating agents. The drug is metabolized and activated in the liver. It also inhibits MAO thus increasing the effects of sympathomimetics, TCAs, and tyramine. It gained FDA Approved in July 1969. It is on the World Health Organization's List of Essential Medicines, a list of the most important medication needed in a basic health system.

MSBN is a highly selective fluorogenic probe for thiols, selectively imaging thiols in live cells and specifically label protein thiols with a turn-on signal to determine diverse reversible protein thiol modifications.

MDL-72274 HCl is selective and potent inhibitors of SSAO for treatment of Parkinson diseases. MDL-72974 is a potent (IC50 = 10(-9) M) inhibitor of both MAO-B and SSAO, with 190-fold lower affinity for MAO-A. In clinical studies, oral doses as low as 100 micrograms produced substantial inhibition of platelet MAO-B. One or 4 mg MDL-72274 HCl given daily for 28 days to 40 Parkinson's patients treated with L-dopa produced statistically significant reductions in the Unified Parkinson's Disease Rating Scale. MAO-B inhibitors, such as MDL 72974A and L-deprenyl, offer the potential of being neuroprotective in Parkinson's Disease and other neurogenerative disorders.

27-Hydroxycholesterol, also known as 27-HC, is an endogenous oxysterol with multiple biological functions, including activity as a selective estrogen receptor modulator (SERM) (a mixed, tissue-specific agonist-antagonist of the estrogen receptor (ER)) and as an agonist of the liver X receptor (LXR). It is a metabolite of cholesterol that is produced by the enzyme CYP27A1. 27-Hydroxycholesterol suppresses lipid accumulation by down-regulating lipogenic and adipogenic gene expression in 3T3-L1 cells. 27-Hydroxycholesterol stimulates cell proliferation and resistance to docetaxel-induced apoptosis in prostate epithelial cells.

RO 46-8443 is the first non-peptide endothelin ETB receptor selective antagonist. RO 46-8443 displays up to 2000-fold selectivity for ETB receptors both in terms of binding inhibitory potency and functional inhibition. The observed parallel rightward shift of concentration-response curves with different antagonist concentrations is consistent with a competitive binding mode. Since R0 46-8443 selectively inhibits ETB receptor mediated responses, it is a valuable tool for clarifying the role of ETB receptors in pathology.

ABT-046 is a potent, safe, and orally efficacious inhibitor of acyl-CoA:diacylglycerol acyltransferase 1. Oral administration of ABT-046 at doses ≥0.03 mg/kg significantly reduced postprandial triglycerides in mice following an oral lipid challenge. Further assessment in both acute and chronic safety pharmacology and toxicology studies demonstrated a clean profile up to high plasma levels.

LAS101057 is a Potent, Selective, and Orally Efficacious A2B Adenosine Receptor Antagonist. (last updated: 6/30/2016). LAS101057 inhibits agonist-induced IL-6 production in human fibroblasts and is active in an ovalbumin (OVA)-sensitized mouse model after oral administration, reducing airway hyperresponsiveness to methacholine, Th2 cytokine production, and OVA-specific IgE levels.

PF-06767832 is a high quality M1 selective PAM (M1 PAM EC50 = 60 nM; M2-M5 PAM EC50 > 10 microM; CNS MPO = 4.9). PF-06767832 has well aligned physicochemical properties, good brain penetration and pharmacokinetic properties. Extensive safety profiling suggested that despite being devoid of mAChR M2/M3 subtype activity, compound 38 still carries gastrointestinal and cardiovascular side effects. These data provide strong evidence that M1 activation contributes to the cholinergic liabilities that were previously attributed to activation of the M2 and M3 receptors.

Necrostatin-2, also known as Nec-2, is a necroptosis inhibitor.

INCB3284 is a potent, selective, and orally bioavailable hCCR2 Antagonist. INCB3284 exhibited an IC50 of 3.7 nM in antagonism of monocyte chemoattractant protein-1 binding to hCCR2, an IC50 of 4.7 nM in antagonism of chemotaxis activity, an IC50 of 84 μM in inhibition of the hERG potassium current, a free fraction of 58% in protein binding, high selectivity over other chemokine receptors and G-protein-coupled receptors, and acceptable oral bioavailability in rodents and primates. In human clinical trials, INCB3284 exhibited a pharmacokinetic profile suitable for once-a-day dosing (T 1/2 = 15 h).

ZD-9379 is a NMDA receptor antagonist potentially for the treatment of pain and stroke. ZD9379 is also a glycine site antagonist, ZD9379 which reduces number of spreading depressions and infarct size in rats with permanent middle cerebral artery occlusion. ZD9379 reduces number of spreading depressions and infarct size in rats with permanent middle cerebral artery occlusion.

5alpha-THDOC is a positive allosteric modulator of GABAA receptors.

MOPS-Na is a novel stabilizer as buffer for the native structure of BSA against thermal denaturation.

Nequinate is an anticoccidial agent, preventing coccidiosis and developing immunity against five different species of Eimeria.

X-alpha-Gal is a substrate for alpha-galactosidase, differentiating alpha-galactosidase-positive strains of yeast.

Rabeprazole is an inhibitor of H(+)-K(+)-exchanging atpase in gastric parietal cells.

Ceftiofur Hydrochloride is a broad-spectrum, third-generation cephalosporin antibiotic, binding to and inactivating penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall.

Pentamidine is an antiprotozoal and antifungal agent, interacting directly with the pathogen genome by binding to AT-rich regions of duplex DNA and the minor groove of DNA, thereby interfering with DNA replication.

Salbutamol Sulfate is a short-acting beta-2 adrenergic agonist.

Quinocetone is an animal growth promoter; Antimicrobial agent.

Nortropine Hydrochloride is a secondary metabolite of tropine derivative drugs, such as atropine and benztropine.

Isoxepac, also known as Olopatadine USP Related Compound C, is a non-steroidal anti-antiphlogistic agent and analgesic.

NPPB is a voltage-dependent cystic fibrosis transmembrane conductance regulator (CFTR) channel blocker.

(-)-Isoproterenol hydrochloride is an agonist of beta-adrenergic receptor. (-)-Isoproterenol hydrochloride is also used in the treatment of bradycardia; bronchodilator.

CGP12177A is a partial agonist of ?3-adrenoceptors and antagonist of ?1- and ?2-adrenoceptor.

CAY10471, also known as TM30089, is a potent and selective long-lasting antagonist of CRTH2. Cat#527092 is a + rotation. isomer (note sure it is a R-isomer or S-isomer).

AT2 Agonist C21 is the first potent and selective agonist of angiotensin AT2 receptors, preventing endothelial inflammation and leukocyte adhesion in vitro and in vivo. AT2 Agonist C21 prevents cognitive decline after permanent stroke in aged animals-A randomized double- blind pre-clinical study. AT2 Agonist C21 attenuates pulmonary inflammation in a model of acute lung injury. AT2 Agonist C21 attenuates the Progression of Lung Fibrosis and Pulmonary Hypertension in an Experimental Model of Bleomycin-Induced Lung Injury.

Olodanrigan, also known as EMA401, is a novel orally available and highly selective angiotensin II type 2 receptor (AT2R) antagonist.

Forodesine is a transition-state analog inhibitor of purine nucleoside phosphorylase.

Sinafloxacin Mesylate is a quinolone antibiotic potentially for the treatment of bacterial infections. There is a strong interaction between sinafloxacin and BSA. From thermodynamic coordination it can be judged that the binding force between sinafloxacin and BSA is mainly electro-static force. The effect of sinafloxacin on the conformation of BSA was analyzed by synchronous fluorescence spectrometry and three-dimensional fluorescence spectrometry. The emission maximum of tyrosine residues does not show a significant shift, while the small blue shift of tryptophan residues indicates that the hydrophobicity of microenvironment was increased. In addition, in the plasma, there are some metal ions, which can participate in many important vital actions and affect the reactions of the drugs with the serum albumins.

Kukoamine B Mesylate is potentially for the treatment of sepsis. Kukoamines are a series of bioactive phytochemicals conjugated by a polyamine backbone and phenolic moieties. Treatment with KuB prior to H2O2 exposure effectively increased the cell viability, and restored the mitochondria membrane potential (MMP). Furthermore, KuB enhanced the antioxidant enzyme activities of superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GSH-Px) and decreased the malondialdehyde (MDA) content. Moreover, KuB minimized the ROS formation and inhibited mitochondria-apoptotic pathway, MAPKs (p-p38, p-JNK, p-ERK) pathways, but activated PI3K-AKT pathway.

NCDM-32B is a novel potent and selective KDM4 inhibitor, impairing viability and transforming phenotypes of basal breast cancer.

NMIA, also known as N-Methylisatoic Anhydride, is an RNA SHAPE reagent.

P18IN011 is a novel p18(INK4C) inhibitor.

SB-505124 HCl is an inhibitor of activin receptor-like kinase (ALK) 5.

Naltriben is a highly selective δ2 opioid receptor antagonist.Naltriben (NTB) has been used to differentiate the subtypes of delta opioid receptors, delta1 and delta2. NTB displaced the specific binding of [3H]DAMGO with Ki value of 19.79 +/- 1.12 nM in rat cortex membranes. Specific binding of [3H]diprenorphine ([3H]DIP) was inhibited by NTB with Ki value of 82.75 +/- 6.32 nM in the presence of DAMGO and DPDPE. Naltriben enhanced the MAPK/ERK signaling pathway, but not the PI3k/Akt pathway. Therefore, potentiated TRPM7 activity contributes to the devastating migratory and invasive characteristics of GBM.

NRC-2694 is an epidermal growth factor receptor (EGFR) antagonist potentially for the treatment of solid tumors.

BCI hydrochloride is an allosteric inhibitor of Dusp6, acting within the phosphatase domain to prevent the catalytic stimulation of phosphatase activity induced by ERK2 substrate binding.

U-69593 is a selective kappa opioid receptor agonist.

(-)-MDO-NPA HCl is an orally effective long-acting agent active at central dopamine receptors, and analogous aporphines.

RP-106 is a selective, potent, ATP-competitive inhibitor of CDK1/cyclin B, CDK5/p25, and GSK-3.

SC-53116 HCl is a psychoactive agent, increasing in production of serotonin in central nervous system tissue.

Amperozide HCl is a 5-HT2/D2 antagonist, inhibiting nomifensine-induced hyperlocomotion and human FAAH.

A3 HCl is an inhibitor of PKA, PKC, and casein kinase I and II, and MLCK.

PPDA is a subtype-selective NMDA receptor antagonist that preferentially binds to NR2C/NR2D-containing receptors.

FPL-55712 is a CysLT1 leukotriene receptor antagonist.

Spiperone HCl is a 5-HT2A serotonin and selective D2-like dopamine receptor antagonist.

MitoB is a novel exomarker of mitochondrial hydrogen peroxide.

Etilevodopa HCl is a prodrug of levodopa with greater gastric solubility and significant brain penetration.

gamma-DGG is a broad spectrum glutamate receptor antagonist.

ONO-8130 is an orally available EP1 receptor antagonist.

IWP-12 is a potent inhibitor of Porcupine (PORCN), a membrane-bound O-acyltransferase (MBOAT).

1,3-Dicaffeoylquinic acid is an inhibitor of taste receptors.

ENMD-1068 HBr is a novel antagonist of Proteinase-Activated Receptor 2 (PAR-2).

Adaphostin is a novel activator of Fas-mediated death pathway in Bcr/Abl-positive leukaemia.

CAY10404 is one of the most selective inhibitors of COX-2 over COX-1.

Undecylprodigiosin is a classical cytotoxic immunosuppressant, suppressing immune functions and inhibiting DNA synthesis.

Spongouridine is a deamination metabolite of Cytarabine (GLXC-07791).

Lupulon, also known as Lupulone, is a beta-acid that has been found in the hop plant, H. lupulus, and has diverse biological activities, including antibacterial, antioxidant, and anticarcinogenic properties. Lupulone is active against B. subtilis and S. aureus as well as T. b. brucei and L. m. mexicana. It scavenges 2,2-diphenyl-1-picrylhydrazyl (DPPH) radicals and reduces proliferation, migration, and capillary tube formation in human umbilical vein endothelial cells (HUVECs). Lupulone also activates the extrinsic apoptotic death pathway in SW480 and SW620 colon cancer cells.

Histapyrrodine hydrochloride is a bioactive chemical.

Indole-3-propionic acid, also known as IPA and SHP-622, is a beta-amyloid protein neurotoxicity inhibitor potentially for the treatment of Friedreich's ataxia. The administration of IPA significantly decreased the level of 4-hydroxy-2-nonenal, a marker of lipid peroxidation, in ischemic hippocampal homogenates compared with that in the vehicle-treated ischemic groups at various times after ischemia/reperfusion. In addition, immunostaining for 8-hydroxy-2'-deoxyguanosine showed DNA damage in pyramidal neurons in the ischemic CA1 was significantly lower in the IPA-treated ischemic groups than in the vehicle-treated ischemic groups. IPA may be used as a pharmacological agent to protect against iron-induced oxidative damage to membranes and, potentially, against carcinogenesis.

Bepafant, also known as WEB-2170 and STY-2108, is a platelet activating factor (PAF) antagonist potentially for the treatment of asthma. Bepafant triggered apoptosis in NB4, KG1, and NB4-MR4 cells where PTEN was expressed, but not in THP1 and U937 cells where PTEN was absent. Bepafant may produce significant anti-inflammatory effects.

SR-33805 is a calcium channel antagonist potentially for the treatment of atherosclerosis and heart failure. SR-33805 restored the MI-altered cell shortening without affecting the Ca(2+) transient amplitude, suggesting an increase of myofilament Ca(2+) sensitivity in MI myocytes. A SR33805-induced sensitization of myofilament activation was found to be associated with a slight increase in myosin light chain-2 phosphorylation and a more significant decrease on troponin I (TnI) phosphorylation. Decreased TnI phosphorylation was related to inhibition of protein kinase A activity by SR-33805.

Espindolol is a β-adrenoceptor antagonist potentially for the treatment of cachexia related to cancer.

Pinocembrin, also known as DL-0108, is an androgen receptor ligand potentially for the treatment of acute stroke.

AIM-102 is nonsteroidal, immune modulating, anti-inflammatory drug potentially for the treatment of allergic asthma

Idremcinal is a motilin receptor agonist potentially for the treatment of gastritis

Tesofensine, also known as NS-2330, is a serotonin–noradrenaline–dopamine reuptake inhibitor potentially for the treatment of obesity.