GW 842166X is a cannabinoid receptor 2 (CB2) agonist potentially for the treatment of inflammatory pain.

Oxipurinol is a xanthine oxidase inhibitor potentially for the treatment of heart failure and gout.

ZD-0947, also known as AZD-0947, is a K(ATP) channel activator potentially for the treatment of overactive bladder (OAB).

Pyridoxyl phosphate is a purinergic P2 receptor antagonist potentially for the treatment of tardive dyskinesia

NGX-267 is a muscarinic M1 agonist potentially for the treatment of Xerostomia, Alzheimer's disease and cognitive

Siramesine Fumarate is a sigma receptor agonist potentially for the treatment of generalized anxiety disorder

Sodium taurocholate is a GPBAR1 protein agonist potentially for the treatment of type 2 diabetes and obesity in rats.

Celgosivir is an α-glucosidase inhibitor potentially for the treatment of dengue fever.

Equol is a drug is potentially for the treatment of acute thyroid disease and inhibits proliferation of human gastric carcinoma cells. Equol (racemic) is a mixture of S-equol and R-equol.

Ferroquine is a hemozoin inhibitor potentially for the treatment of malaria.

Secoisolarisiresinol diglucoside (SDG) is potentially for the treatment of oxidative stress.

Phenylethyl isothiocyanate is an HDAC inhibitor potentially for the treatment of benign prostatic hypertrophy.

FdCyd is a DNA methyltransferase (DNMT) inhibitor potentially for the treatment of solid tumours.

P-1075, also known as PNU-83757 and U-83757, is a K-ATP channel agonist potentially for the treatment of erectile dysfunction, alopecia and arrhythmia.

N-Acetylmannosamine, also known as ManNAc, DEX M-74, N-acetyl-D-mannosamine, is a drug potentially for the treatment of hereditary inclusion body myopathy

Sodium pyruvate is a antioxidant potentially for the treatment of chronic obstructive pulmonary disease

Alpha-Lipoic Acid Choline Ester, also known as alpha-LACE, EV-06 or UNR844, is a drug candidate potentially for the treatment of presbyopia. Alpha-LACE was designed to permeate biological membranes with the incorporation of the cationic choline head grou

Sipatrigine is a multiple channels blocker potentially for the treatment of stroke. It has been shown to blocks multiple cardiac ion channels, cause triangulation of the ventricular action potential,and could have therapeutic potential for major depression and bipolar depression through antagonism of the two-pore-domain K+ channel TREK-1.

An alpha2-adrenoceptor antagonist potentially for the treatment of schizophrenia.

GW-870086 is a glucocorticoid receptor agonist potentially for the treatment of asthma and atopic dermatitis.

Apratastat, also known as TMI-005 and XMT-1191, is a matrix metalloproteinase/tumour necrosis factor-α convertase inhibitor.

Fluasterone, also known as HE2500, is an NF-κB activation inhibitor potentially for the treatment of metabolic syndrome.

Tocladesine is a cyclic adenosine monophosphate (cAMP) receptor agonist potentially for the treatment of colorectal cancer.

Examorelin, also known as Hexarelin, is a growth hormone-releasing factor (GHRF) agonist potentially for the treatment of cardiac diseases.

Asimadoline HCl is a κ-opioid receptor agonist potentially for the treatment of pruritus. Asimadoline has also been shown to be used in the treatment of irritable bowel syndrome.

REC-2615 (HCl) is a α1B-adrenoceptor antagonist potentially for the treatment of female sexual dysfunction.

Tributyrin, also known as NSC661583, is a histone deacetylase (HDAC) inhibitor potentially for the treatment of solid tumors.

ɑ-Tocopherolquinone, also known as Vitamin E Quinone (D-form), is a mitochondrial membrane transport protein that has been in phase II clinical trials for the treatment of inherited mitochondrial respiratory chain diseases, however this research has been discontinued. It has also been used for the treatment of Frederich's ataxia and MEILAS syndrome.

Withanolide B is a withanolide that has been found in W. somnifera. Unlike withanolide A, it does not increase glucose uptake in L6 myotubes. In in silico docking studies, withanolide B was identified as a neuronal nitric oxide synthase (nNOS) inhibitor that also inhibited inducible NOS (iNOS) and endothelial NOS and as a ligand for the PARP1 catalytic domain.

CAY10499 is a potent and selective monoglyceride lipase inhibitor exhibiting an IC50 of 90 nM for the recombinant enzyme.

ZK-756326 is a potent, selective and non-peptide CCR8 chemokine receptor agonist. ZK 756326 inhibited the binding of the CCR8 ligand I-309 (CCL1), with an IC(50) value of 1.8 muM. ZK 756326 was a full agonist of CCR8, dose-responsively eliciting an increase in intracellular calcium and cross-desensitizing the response of the receptor to CCL1.

IR-825 is a near-infrared dye (NIR). IR-825, after encapsulated into nanoparticles may be useful for cancer photothermal and photodynamic therapy. IR-825 nanoparticles showed pH-dependent fluorescence emission and excellent near-infrared (NIR) irradiation of cancer cells targeted in vitro to provide cytotoxicity. IR-825 nanoparticles showed efficient tumor homing together with rapid renal excretion behaviors, as revealed by MR imaging and confirmed by biodistribution measurement. Notably, when irradiated with an 808 nm laser, tumors on mice with IR-825 nanoparticle injection are completely eliminated without recurrence within 60 days, demonstrating the high efficacy of photothermal therapy.

C16, also known as GW-506033X or PKR Inhibitor. C16 binds the ATP-binding site of PKR and blocks autophosphorylation with an IC50 value of 186-210 nM. GW-506033X protects human neuroblastoma cells against cell damage triggered by tunicamycin-mediated endoplasmic reticulum stress. PKR inhibitor C16 prevents apoptosis and IL-1β production in an acute excitotoxic rat model with a neuroinflammatory component. PKR inhibitor C16 binds efficiently with human microtubule affinity-regulating kinase 4.

Thiohydantoin, also known as 2-Thiohydantoin and NSC 11772, is a potent inhibitors of mutant IDH1. Thiohydantoin can decrease the cellular concentration of D2HG, reduce the levels of histone methylation, and suppress the proliferation of stem-like cancer cells in BT142 glioma with IDH1 R132H mutation. Somatic mutations of isocitrate dehydrogenase 1 (IDH1) at R132 are frequently found in certain cancers such as glioma. With losing the activity of wild-type IDH1, the R132H and R132C mutant proteins can reduce α-ketoglutaric acid (α-KG) to d-2-hydroxyglutaric acid (D2HG).

AR-R17779 is a selective alpha7 nicotinic agonist (Ki values are 190 and 16000 nM for rat α7 and α4β2 receptors respectively). AR-R17779 improves learning and memory in rats. Treatment with AR-R17779 significantly reduced atherosclerotic plaque area and improved survival of mice. Treatment with AR-R17779 also suppressed abdominal aortic aneurysm formation. Quantitative RT-PCR of the aorta revealed that mRNA expression levels of interleukin-1β, interleukin-6 and NOX2 were significantly decreased in AR-R17779-treated mice compared with Ang II+HFD mice. AR-R17779 treatment also reduced blood pressure and serum lipid levels.

JT010 is a potent agonist of TRPA1 with an EC50 of 0.65 nM.

TNCA, also known as Lycoperodine-1, is a high-affinity CaSR ligand (CaSRL) with co-agonist activity. .

P-3298, also known as P32/98, Isoleucine-thiazolidide, is a DPP-4 inhibitor potentially for the treatment of type 2 diabetes. P32/98 decreased non-fasting morning blood glucose more effectively in ZR with iIGT than in ZR with mIGT. Compared with study entry, P32/98 improved DNP of blood glucose in ZR with mIGT and nearly normalized DNP in ZR with iIGT. P32/98 significantly reduced triglycerides and non-esterified fatty acids. Intestinal growth was comparable between inhibitor- and placebo-treated fatty rats.

LP533401 is an inhibitor of tryptophan hydroxylase 1, which regulates serotonin production in the gut. LP533401 has an anabolic effect in bone. Inhibiting GDS biosynthesis could become a new anabolic treatment for osteoporosis.

MitoPQ, also known as MitoParaquat, is a redox cycler. MitoParaquat (MitoPQ) that comprises a triphenylphosphonium lipophilic cation conjugated to the redox cycler paraquat. MitoPQ accumulates selectively in the mitochondrial matrix driven by the membrane potential. Within the matrix, MitoPQ produces superoxide by redox cycling at the flavin site of complex I, selectively increasing superoxide production within mitochondria. MitoPQ increased mitochondrial superoxide in isolated mitochondria and cells in culture ~a thousand-fold more effectively than untargeted paraquat. MitoPQ was also more toxic than paraquat in the isolated perfused heart and in Drosophila in vivo. MitoPQ enables the selective generation of superoxide within mitochondria and is a useful tool to investigate the many roles of mitochondrial superoxide in pathology and redox signaling in cells and in vivo.

MC-976 is an Vitamin D3 derivative.

Y-26763 is Kir6 (KATP) channel opener and active metabolite of Y-27152. Y-26763 protects the canine heart from a stunning injury through opening of the KATP channels. Y-26763 protects the working rat myocardium from ischemia/reperfusion injury through opening of KATP channels. Y-26763 activated K(ATP) channels in a reversible manner with a similar activity to diazoxide. Y-26763-induced inhibition of insulin release is dependent upon the activation of K(ATP) channels in human beta-cells.

PF-06279794, also known as PF-794, is a potent, selective and ATP-competitive TNIK inhibitor.

GSK124576A is a bioactive chemical.

ZCZ011 is a positive allosteric modulator of the cannabinoid CB1 receptor. ZCZ011 potentiated binding of [(3)H]CP55,940 to the CB1 receptor as well as enhancing AEA-stimulated [(35)S]GTPγS binding in mouse brain membranes and β-arrestin recruitment and ERK phosphorylation in hCB1 cells. In the whole animal, ZCZ011 is brain penetrant, increased the potency of these orthosteric agonists in mouse behavioral assays indicative of cannabimimetic activity, including antinociception, hypothermia, catalepsy, locomotor activity, and in the drug discrimination paradigm. ZCZ011 acts as a CB1 PAM and provide the first proof of principle that CB1 PAMs offer a promising strategy to treat neuropathic and inflammatory pain with minimal or no cannabimimetic side effects.

H-89 is a specific adenylyl cyclase inhibitor (DDA) and a cyclic AMP-dependent protein kinase inhibitor. H-89 blocks the action of equine growth hormone on in vitro maturation of equine oocytes. H-89 decreases the gain of excitation-contraction coupling and attenuates calcium sparks in the absence of beta-adrenergic stimulation. H-89 potentiates adipogenesis in 3T3-L1 cells by activating insulin signaling independently of protein kinase A.

KN-92 is an inactive analog of the CaM kinase II inhibitor KN 93.

BAY-588 is an inactive control probe for BAY-876 (catalog no. SML1774). BAY-876 is a potent, highly selective, cell-permeable inhibitor of glucose transporter GLUT1.

JIB-04 Z-isomer, also known as NSC 693627, is an isomer of JIB-04. JIB-04 is a Jumonji histone demethylase inhibitor. JIB-04 selectively blocks cancer cell growth in vitro and diminishes tumor growth in H358 and A549 mouse xenograft models in vivo. JIB-04 can prolong survival in a mouse model of breast cancer.

SLM6031434 is SphK2-selective inhibitor.

DCG04 is a multivalent ligand for the mannose-6-phosphate receptor for endolysosomal targeting of an activity-based probe. DCG-04 is an activity-based probe for cysteine cathepsins, enabled fluorescent readout of its receptor-targeting properties.

CAY10575 is a benzimidazole analog IKK-ε inhibitor that inhibits IKK-ε with an IC50 value of ~15.8 μM.

PI-828 is a potent inhibitor of phosphatidylinositol 3-kinase.

TCN-201 is a selective antagonist of NMDA receptors containing the NR2A subunit. TCN 201 selectively blocks GluN2A-containing NMDARs in a GluN1 co-agonist dependent but non-competitive manner.

GSK2837808A is a potent, selective lactate dehydrogenase A (LDHA) inhibitor (IC50 values are 1.9 and 14 nM for LDHA and LDHB respectively).

LY255582 is a phenylpiperidine non-selective opioid antagonist. It has been shown to reduce ethanol consumption in experiments carried out on rats. It has also been shown to reduce food and water consumption in rats. LY255582 inhibits the diet-associated increases in mesolimbic dopamine levels and reduces the consumption of highly-palatable food intake.

RO10-5824 is a D4-selective partial agonist. RO10-5824 is a potent candidate for the management of cocaine use disorders. The identification of effective medications for the management of cocaine use disorders remains an unmet public health challenge. In view of the prominent role of dopaminergic mechanisms in cocaine's abuse-related effects, research has focused on the development of subtype-selective dopamine D1-4 receptor antagonists.

ML-030, also known as CID-11757146, is a potent and selective PDE4 inhibitor. ML-030 inhibits PDE4 in a cell-based cyclic nucleotide-gated cation channel biosensor assay with an EC50 value of 18.7 nM.

PF-04628935 is is a potent antagonist/inverse agonist of the ghrelin receptor, growth hormone secretagogue receptor 1a (GHS-R1a) with an IC50 of 4.6 nM. Ghrelin and GSHR are involved in regulation of food intake and long-term energy homeostasis; GSHR ligands are of interest for obesity and other metabolic disorders. PF-04628935 is orally bioavailable and brain penetrant.

PZ-II-029 is a α6β3γ2-selective GABAA channel modulator.

NF-1819 is a Potent and selective irreversible MAGL inhibitor.

nor-NOHA is a potent, selective, competitive, and high affinity inhibitor of arginase. nor-NOHA inhibits arginase from rat liver (IC50 = 2 μM) and mouse macrophages (IC50 = 50 μM).

MDK-4111 is a potent and selective GPR120 receptor agonist. MDK-4111 has CAS#1234844-11-1. The last 4 digit of its CAS# is used for naming.

GSK656, also known as GSK3036656 and GSK070, is a potent Mtb LeuRS inhibitor. GSK656 shows potent inhibition of Mtb LeuRS (IC50 = 0.20 μM) and in vitro antitubercular activity (Mtb H37Rv MIC = 0.08 μM). Additionally, it is highly selective for the Mtb LeuRS enzyme with IC50 of >300 μM and 132 μM for human mitochondrial LeuRS and human cytoplasmic LeuRS, respectively. In addition, it exhibits remarkable PK profiles and efficacy against Mtb in mouse TB infection models with superior tolerability over initial leads. GSK656 has been progressed to clinical development for the treatment of tuberculosis.

TAN-420C, also known as Dihydroherbimycin C, is an antibiotic. TAN 420C is a minor analogue of the herbimycin complex, isolated from Streptomyces hygroscopicus. TAN 420C is known to exhibit antitumour activity.

AR-420626 is a FFA3 agonist. FFA3 is a promising target for the treatment of neurogenic diarrheal disorders by suppressing nAChR-mediated neural pathways.

OXSI-2 is an Syk Inhibitor. OXSI-2 blocks nigericin-induced inflammasome signaling and pyroptosis independent of potassium efflux. OXSI-2 inhibits inflammasome assembly, caspase-1 activation, IL-1β processing and release, mitochondrial ROS generation, and pyroptotic cell death. Using a novel live cell potassium sensor we show that Syk inhibition with OXSI-2 has no effect on potassium efflux kinetics and that blockade of potassium efflux with extracellular potassium alters Syk phosphorylation.

N-Formyl-Met-Leu-Phe, also known as fMLF, is a potent neutrophil chemoattractant and the reference agonist for the G protein-coupled N-formylpeptide receptor (FPR).

PU-02 is a potent and selective 5-HT3 receptor antagonist. PU02 displays IC(50) values of ~1 μM at 5-HT(3)Rs and substantially lower activities at other Cys-loop receptors. In an elaborate mutagenesis study of the 5-HT(3)A receptor guided by a homology model, PU02 is demonstrated to act through a transmembrane intersubunit site situated in the upper three helical turns of TM2 and TM3 in the (+)-subunit and TM1 and TM2 in the (-)-subunit.

Atorvastatin lactone, also known as Atorvastatin Related Compound H, is a prodrug form of atorvastatin, an HMG-CoA reductase inhibitor used to lower blood cholesterol levels. It hydrolyzes rapidly to the acid form of atorvastatin in human serum.

CP-74006 is a selective D5D inhibitor. CP-74006 potently blocks the Delta5D activity with an IC(50) value of 20 nM and simplifies the metabolism of [1-(14)C]-alpha-linolenate (C18:3, cis-9,12,15) by accumulating (14)C-eicosatetraenoic acid (C20:4, cis-8,11,14,17) as the major (14)C-eicosatrienoic acid (C20:3, cis-11,14,17) and (14)C-docosatetraenoic acid (C22:4, cis-10,13,16,19) as the minor metabolites through Delta6 desaturation and elongation.

Anthralin, also known as Dithranol, is a hepsin activity inhibitor used for treatment of psoriasis Inhibition of hepsin activity suppresses the invasive growth of the tumor. Anthralin exerts a direct effect on keratinocytes and leukocytes. Anthralin significantly prolonged the prophase of mitotic keratinocytes in subtoxic doses and suppressed the expression of keratin 6 mRNA in the immediately suprabasal layer of psoriatic epidermis in vivo. Anthralin also inhibits the transformation of lymphocytes and the release of reactive oxygen species from activated leukocytes, in vitro.

Apomorphine Hydrochloride, also known as APL-130277 and TAK-251, is a dopamine D2 agonist used for the treatment of Parkinson's disease. Apomorphine also promotes intraneuronal amyloid-β (Aβ) degradation and improves memory function in an Alzheimer's disease model. Protein levels of two types of serine-phosphorylated insulin receptor substrate-1 (IRS-1), pS616 and pS636/639, significantly decreased following Apomorphine treatment in the 13-month-old 3xTg-AD mice brain, suggesting improved brain insulin resistance.

Benzethonium Chloride, also known as Hyamine, is synthetic quaternary ammonium salt that has surfactant, antiseptic, and anti-infective properties. Benzethonium Chloride is commonly used as a topical antimicrobial agent. Benzethonium chloride exhibited concentration-dependent inhibitions of HERG channel currents with IC(50) values of 4nM and 17nM, respectively, which were also voltage-dependent and use-dependent. Benzethonium Chloride shifted the channel activation I-V curves in a hyperpolarized direction for 10-15mV and accelerated channel activation and inactivation processes by 2-fold.

Bisacodyl, also known as Dulcolax, is a stimulant laxative drug. Oral bisacodyl is an effective and well-tolerated treatment for patients with chronic constipation. It improves bowel function, constipation-related symptoms, and disease-related quality of life.

Butamben, also known as Butoform, is a local anesthetic. Blockade of voltage-gated channel expressed in the peripheral sensory neurons has been suggested as a mechanism of action. Butaben effects on another sensory neuronal channel family, transient receptor potential (TRP) have remained unclear. Butamben attenuated acute animal pain behaviors in a TRPA1- or TRPV4-dependent manner. Butamben inhibits the total barium current through expressed calcium channel types in PC12 cells, including Cav1.2/L-type channels.

Chlortetracycline hydrochloride, also known as Aureomycin, is a broad-spectrum antibiotic used in veterinary medicine for pulmonary or digestive infections. Chlortetracycline and its metal complexes are toxic to bacteria when they are biologically available. Chlortetracycline and copper plus Chlortetracycline supplementation increased both the prevalence and gene copy numbers of tetA, while decreasing both the prevalence and gene copies of tetB.

Cinchonidine is an cinchona alkaloid with antimalarial activity. Cinchonidine adsorbed onto a platinum metal catalyst leads to rate acceleration and induces strong stereocontrol in the asymmetric hydrogenation of trifluoroacetophenone. In the hydrogenation of the heteroaromatic ring of cinchonidine in toluene, the diastereomeric excess of the (S)-hexahydrocinchonidine increased upon increasing Pt{111}/Pt{100} ratio, but this distinct shape selectivity was observed only after the oxidative removal of PAA at 473 K. The use of the as-prepared nanoparticles inverted the major diastereomer to R, and this isomer was formed also in acetic acid.

Denatonium, also known as Bitrex, is a bitterant (or bitter agonist). Denatonium activates bitter taste receptors on many cell types and plays important roles in chemical release, ciliary beating and smooth muscle relaxation through intracellular Ca(2+)-dependent pathways. Denatonium significantly effects cellular morphology, decreases cell proliferation and reduces the number of cells in S phase in a dose-dependent manner. Denatonium causes large amplitude swelling of mitochondria, which was confirmed by the loss of mitochondrial membrane potential, the down-regulation of Bcl-2 protein and the subsequent enhancement of the mitochondrial release of cytochrome c and Smac/DIABLO after denatonium treatment.

Dehydrocholic acid is a semisynthetic bile acid synthesized from cholic acid. Dehydrocholic acid caused a dramatic decrease of phospholipid, cholesterol and bilirubin concentration but had little effect on bile acids concentration. Bile flow, expressed as the ratio of bile flow to bile acid excretion, was increased after dehydrocholic acid administration. It was speculated that the hydroxy keto metabolites are hydrocholeretics. The proportion of cholesterol to lecithin and bile acids did not change significantly after dehydrocholic acid administration.

Domiphen bromide is a quaternary antiseptic used as an antifungal agent. Domiphen bromide has potent activity on blockade of human ether-a-go-go related gene (HERG) channels. Domiphen bromide inhibited HERG channel currents in a dose-dependent manner with IC50 values of 9nM. Block of HERG channel by domiphen bromide was voltage-dependent and use-dependent. Domiphen bromide caused substantial negative shift of the activation curves, accelerated activated process, but had no effects on the deactivation and reactivation processes.

Ergoloid Mesylates, also known as dihydroergotoxine mesylate, is a mixture of three dihydrogenated ergot alkaloids (dihydroergocristine, dihydroergocornine, and alpha- and beta-dihydroergocryptine). Ergoloid mesylates is used as a treatment for dementia and Alzheimer disease. Ergoloid Mesylates stimulates dopaminergic and serotonergic receptors and blocks alpha-adrenoreceptors. Ergoloid Mesylates binds to the GABAA receptor Cl- channel, producing a reaction at the benzodiazepine site.

Ethopabate is a folate metabolism inhibitor used in the prophylaxis and treatment of coccidiosis in chickens.

Hematein, also known as Haematein, is an oxidized derivative of Hematoxylin (Haematoxylin) used in staining the staining of cell nuclei in animal tissue. Hematein also can be used in the staining of myelin sheaths and nerve fibers.

Iodoquinol is one of the halogenated 8-quinolinols that's widely used as an intestinal antiseptic, especially as an antiamebic agent. Iodoquinol is also used topically in other infections and may cause central nervous system and eye damage.

Isoxsuprine is a beta 2-adrenergic agonist and NR2B subtype-selective N-methyl-D-aspartate (NMDA) receptor antagonist used for the treatment of pre-term labor and dysmenorrhea. Isoxsuprine affects the vascular smooth muscle and results in peripheral vascular dilation. Isoxsuprine also relaxes the uterine smooth muscles. Isoxsuprine elevated the blood flow volume in the umbilical arteries. Veterinary treatment of cows with isoxsuprine may temporarily lead to low levels of isoxsuprine in the hair of their newborn calves, which promotes growth.

Paromomycin sulfate is an aminoglycoside antimicrobial agent derived from Streptomyces sp. AG-P 1441. Paromomycin likely induced resistance as confirmed by the expression of pathogenesis-related genes: PR-1, β-1,3-glucanase, chitinase, PR-4, peroxidase, and PR-10, which enhanced plant defense against P. capsici in chili pepper.

Phenoxybenzamine hydrochloride is an α-1 adrenergic receptor antagonist used to treat hypertension and as a peripheral vasodilator. Phenoxybenzamine reduced neuronal death in rat hippocampal slice cultures following exposure to oxygen glucose deprivation. Phenoxybenzamine treated TBI (traumatic brain injury) animals also showed a significant improvement in both learning and memory compared to saline treated controls. At 32 h post-TBI phenoxybenzamine treated animals had significantly lower expression of pro-inflammatory signaling proteins CCL2, IL1β, and MyD88, suggesting that phenoxybenzamine may exert a neuroprotective effect by reducing neuroinflammation after TBI.

Phthalylsulfathiazole is a broad spectrum antimicrobial agent. Phthalylsulfathiazole is used in the treatment of dysentery, colitis, and gastroenteritis.

Pramoxine, also known as Pramocaine, is a topical anesthetic. Pramoxine decreases the permeability of the neuronal membrane to sodium ions by reversibly binding to and inhibiting voltage-gated sodium channels. This results in stabilization of the membrane and, thereby inhibiting the ionic fluxes required for membrane depolarization, hence resulting in the failure to initiate a propagated action potential and subsequent conduction blockade.

Tramiprosate, also known as homotaurine, is a gamma-Aminobutyric acid (GABA) receptor agonist and a glycosaminoglycan mimetic used in the treatment of Alzheimer's disease.

Aklomide is a Coccidiostat (for Poultry).

Nitrophenide is a bioactive chemical.

Phenazepam is the benzodiazepine that exhibit anticonvulsive, anxiolytic, sedative and hypnotic effects in humans and experimental animals. Phenazepam is an agonist of the γ-Aminobutyric acid A (GABAA)-benzodiazepine receptor chloride channel complex.

PHA 767491 hydrochloride is a potent and selective ATP-competitive dual inhibitor cdc7/cdk9. PHA-767491 blocks DNA synthesis and affects the phosphorylation of the replicative DNA helicase at Cdc7-dependent phosphorylation sites.

PF9601N is a selective and potent monoamine oxidase B inhibitor that exhibit anti-Parkinsonian effects in several models of PD.

PF-514273 is a highly selective CB1 antagonist. The Ki for binding to CB1 and CB2 receptors is 1 nM and 10 mM, respectively. PF-514273 inhibits food intake and weight gain in rodents.

PF-5081090 is a potent inhibitor of LpxC, a metalloenzyme required for the synthesis of lipid A, an essential component of the outer membrane of Gram-negative bacteria. The IC50 for enzyme inhibition is 1.1 nM and the minimal inhibitory concentration (MIC) for inhibiting growth of Pseudomonas aeruginosa growth is 0.008 mg/mL.

PF-4800567 hydrochloride is a casein kinase 1e (CK1e) selective inhibitor (IC50 = 32 nM) that is 20 fold selective for the CK1e isoform over CK1d. PF-4800567 blockes CK1e-mediated PER3 nuclear translocation, but does not effect the circadian clock in animal studies.

PF-3774076 is a CNS penetrant, potent, selective, partial agonist at the human α1A adrenoceptor. PF-3774076 is selective over α1B and α1D adrenoceptors.

PF-06748962 is a potent and selective lactam-based prostaglandin EP3 receptor antagonist.

PF-06745268 is an orally available, brain penetrant, potent and selective γ-secretase modulator. PF-06745268 induces robust and sustained reduction of brain amyloid-β42 (Aβ42) in rats.

A286982 is an inhibitor that blocks the integrin-ligand interaction between leukocyte function-associated antigen-1 (LFA-1) and intercellular adhesion molecule-1.

PF-06663195 is a potent inhibitor of β-site amyloid precursor protein (APP) Cleaving Enzyme 1 (BACE1, β-Secretase 1).

PF-06463922 acetate is a potent, selective brain-penetrable inhibitor of both anaplastic lymphoma kinase (ALK) and c-ros Oncogene 1 (ROS1) with strong activity against all known ALK and ROS1 mutants identified in patients with crizotinib-resistant disease. PF-06463922 is in clinical trials for the treatment of non–small cell lung cancer (NSCLC).

PF-06456384 trihydrochloride is a highly potent and selective inhibitor against voltage-gated sodium channel NaV1.7 (SCN9A; IC50 = 0.01, <0.1, 75 nM against human, mouse, rat Nav1.7, respectively, by conventional patch clamp; human Nav1.7 IC50 = 0.58 nM by PatchExpress electrophysiology) with >300-fold selectivity over other human NaVs (IC50 = 3 nM/NaV1.2, 5.8 nM/NaV1.6, 75 nM/NaV1.7, 314 nM/NaV1.1, 1.45 μM/NaV1.4, 2.59 μM/NaV1.5, 6.44 μM/NaV1.3, 26 μM/NaV1.8).

PF-06422913 is an orally active, potent and selective metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator.

PF-06284674 is a cell permeable, potent and selective M2 isoform of pyruvate kinase (PKM2) activator.

PF-05236216 hydrochloride is a brain penetrant, potent and selective inhibitor of casein kinase 1 delta/epsilon (CK1δ/ε) that modulates circadian rhythms in mice.

PF-04753299 is a potent and selective inhibitor of LpxC (UDP-3-O-(R-3-hydroxymyristol)-N-acetylglucosamine deacetylase) that is effective in a murine of gram-negative bacteria infection model.

PF-04671536 is a highly potent and selective inhibitor of phosphodiesterase 8B (PDE8B) phosphodiesterase 8A (PDE8A). In primary human pancreatic islets, PF-04671536 increases insulin secretion in a glucose-dependent manner.

PF-04445597 is a potent, orally bioavailable inhibitor of cholesteryl ester transfer protein (CETP).

PF-04279405 is a potent and selective glucokinase activator.

PE 154 are known to associate with β-amyloid plaques, and histological co-localization of AChE and Ab peptides is well established in Alzheimer’s disease. PE-154 is a fluorescent inhibitor of both AChE and BChE with IC50 values of 280 pM and 16 nM. PE-154 stains Aβ plaques in both rodent and human tissue samples, and does not cross react with phospho-tau.

AC-186 is reported as a selective nonsteroidal estrogen receptor agonist.

PD-85639 is a voltage-gated sodium (Na+) channel blocker (75% in 10 min & >95% in 25 min blockage of Na+ current by 25 μM PD85,639; whole-cell patch clamp using primary rat brain neurons) that is shown to target rat brain Nav1.2 with simultaneous high- and low-affinity modes of binding (EC50 = 56 nM/40% & 20 μM/60% at pH 9.0, 5 nM/28% & 3 μM/72% at pH 7.4, against 2 nM [3H]-PD85,639 for binding rat brain synaptosomes; EC50 = 17 nM/39% & 10 μM/61% using at pH 9.0 using rat brain synaptosome membranes) and a fast kinetic (t1/2 = 1.2 at 4°C, <0.5 min at 25°C), competitive against the local anesthetic Na+ channel blockers tetracaine, bupivacaine, and mepivacaine, as well as Na+ channel activators veratridine and batrachotoxin (K1 = 0.26 μM against 5 nM [3H]-BTX for binding rat neocrotical membranes).

PBOX-6 belongs to a group of tubulin-targeting pyrrolo-1,5-benzoxazepine (PBOX) compounds that potently induce apoptosis in a wide spectrum of cancer cells, including those originating from the four main types of leukemia and those exhibiting multi-drug resistance (IC50 = 2.28 μM/HL60-MDR1, 2.86 μM/HL60-BCG2, 1.91 μM/HL60; IC50 = 4.71 μM/A2780-ADR, 4.10 μM/A2780). PBOX-6 inhibits the assembly of purified tubulin in cell-free assays and causes microtubule depolymerization in MCF-7 cells by binding a tubulin site distinct from those targeted by vinblastine and colchicine. When administered via intratumoral injection (7.5 mg/kg/day) in vivo, PBOX-6 is reported to significantly inhibit tumour growth in a murine model of neuroblastoma and a CML model of the imatinib-resistant T315I mutants.

Panepoxydone is a fungal metabolite that inhibits NF-κB transcription factor by preventing IκB phosphorylation, thus inhibiting the release of NF-κB from the IκB : NF-κB complex and its translocation into the nucleus. Panepoxydone also has antimalarial, cytotoxic activities and anti-parasitic activity against Trypanosoma cruzi.

AC-90179 is a high selective 5-hydroxytryptamine2A receptor inverse agonist. It is an atypical antipsychotic pharmaceutical. It has been shown to alleviate hallucinogen-induced vasocontriction and possible other harmful physical symptoms.

p38 MAP Kinase Inhibitor IV is an ATP-competitive inhibitor of p38α/β MAPK with IC50 values of 130 nM for p38α and 550 nM for p38β. It is much less active with ≤23% inhibition at 1 μM against p38γ/σ, ERK1/2, and JNK1/2/3. Shown to be more effective than SB 203580 in inhibiting LPS-induced IL-1β release from hPBMC (100% vs. 50% inhibition with 100 μM inhibitor). A recent study showed that p38 MAP Kinase Inhibitor IV could consistently and significantly enhance reprogramming and iPS cell generation from somatic cells.

ACT-462206 is an orally active, potent, brain-penetrant dual orexin 1/orexin 2 receptor antagonist.

AFDX384 is potent M2/M4 selective antagonist.

AGN193109 is a retinoic acid receptor (RAR) antagonist.

AH13205 is an EP2 prostanoid receptor agonist.

AL-8810 is a prostaglandin F2α receptor antagonist

ARC-239 is an α2-adrenergic receptor agonist.

AR-C118925XX is a bioactive chemical.

AZ12216052 is a mGluR II and III activator.

UMB-68 is a GHB receptor ligand. UMB68 showed no affinity (IC(50) >100 microM) at GABA(A) or GABA(B) receptors. In vivo studies showed that, at behaviorally active doses, rats trained to discriminate GHB did not recognize the novel ligands as GHB. Thus, UMB68 is a selective GHB receptor ligand in binding assays, will not undergo metabolism to GABA-active compounds, and does not show the same effects as GHB in vivo. These data suggest that, although UMB68 binds to the GHB receptor, it does not have the observed GABA receptor-mediated effects of GHB in vivo and could provide a novel tool for studying the pharmacology of the GHB receptor in the absence of complicating GABAergic effects.

BIBF-1202 is the carboxylate metabolite of BIBF 1120, which is an oral triple angiokinase inhibitor targeting VEGFR, PDGFR, FGFR.

BRD9539 is an inhibitor of euchromatin histone methyltransferase 2 (EHMT2), also known as G9a, with an IC50 value of 6.3 μM.

m-Aminoacetanilide is a bioactive chemical.

CP-775146 is a selective, high affinity PPARα agonist. CP-775146 exhibits hypolipidemic activity in vivo.

CP 99994 dihydrochloride is a high affinity NK1 antagonist (Ki = 0.145 nM in vitro). CP 99994 dihydrochloride also displays high ex vivo binding potency in gerbil striatum (IC50 = 36.8 nM).

CV-1808 is an adenosine A2 receptor agonist that acts as a coronary vasodilator, antihypertensive and antipsychotic following systemic administration in vivo.

DQP-1105 is a negative allosteric modulator of the GluN2C/D NMDA receptor inhibiting receptor function more potently when glutamate is present .

FK-888 is a selective, high affinity tachykinin NK1 receptor antagonist (Ki = 0.69 nM) that displays 320-fold selectivity for human over rat NK1 receptors. FK-888 inhibits substance P-induced contraction of isolated guinea pig trachea (IC50 = 32 nM) and inhibits substance P-induced airway constriction in vivo.

m-Phenylenediacetic acid is a bioactive chemical.

GR 89696 fumarate is a highly potent and selective κ-opioid agonist (IC50 = 0.04 nM) that may be selective for the putative κ2 receptor. It is anti-nociceptive and neuroprotective in vivo.

GSK4716 is a selective agonist at estrogen-related receptors ERRβ and ERRγ. GSK4716 displays selectivity over ERRα and the classical estrogen receptors.

GSK-264220A is an endothelial lipase and lipoprotein lipase inhibitor (IC50 values are 0.13 and 0.10 μM respectively).

GSK575594A is a GPR55-selective agonist.

GW 583340 dihydrochloride is a potent dual EGFR/ErbB2 tyrosine kinase inhibitor (IC50 values are 0.01 and 0.014 μM respectively). GW 583340 dihydrochloride selectively inhibits growth of human tumor cells overexpressing EGFR and ErbB2 (IC50 values are 0.11 μM for inhibition of HN5, N87 and BT474 tumor cell lines vs. > 30 μM for inhibition of non-tumor cell line HFF).

GW 9578 is a potent agonist of PPARα that activates the murine and human receptors with EC50 values of 0.005 and 0.05 μM. GW 9578 is a potent lipid lowering agent that may reduce insulin resistance.

GW542573X is an activator of small-conductance Ca2±activated K+ channels (KCa2).

GYKI53655 Hydrochloride is a non-competitive AMPA and kainate receptor antagonist. GYKI53655 Hydrochloride exhibits anticonvulsant activity. GYKI53655 Hydrochloride also blocks GluK3 homomeric receptors (IC50 = 63 μM) and GluK2b(R)/GluK3 heteroreceptors (IC50 = 32 μM) at high concentrations.

HX 531 is an antagonist of retinoid X receptors.

IBC 293 is a highly selective agonist for GPR109B (HM74), human orphan G-protein-coupled receptor expressed in adipocytes. IBC 293 is selective for GPR109B over niacin receptor GPR109A (HM74A).

ICI 192605 is a potent thromboxane A2 receptor (TP receptor) antagonist.

JWH015 is a selective CB2 agonist (Ki values are 13.8 and 383 nM as measured at human cloned CB2 and CB1 receptors expressed in CHO cells).

KF 17837S is an adenosine A(2a) receptor antagonists, which is potential therapeutic and neuroprotective effects in Parkinson's disease.

KH064 is a orally active inhibitor of sPLA2-IIA.

L-152,804 is a potent, selective non-peptide neuropeptide Y Y5 receptor antagonist (Ki = 26 nM for hY5). L-152,804 displays > 300-fold selectivity over hY1, hY2, and hY4 receptors.

L-162,313 is a non-peptide AT1 receptor agonist.

L-168,049 is a non-peptidyl human glucagon receptor antagonist.

L-371,257 is a potent, high affinity human oxytocin (OT) receptor antagonist (Ki = 4.6 nM) that displays > 800-fold selectivity over human arginine vasopressin receptors V1a and V2. L-371,257 antagonizes oxytocin-induced contractions in isolated rat uterine tissue (pA2 = 8.44) and in anesthetised rats following intravenous and intraduodenal administration.

L-659,699, also known as hymeglusin, is a fungal β-lactone antibiotic that inhibits HMG-CoA synthase (IC50 = 0.12 μM) by covalently modifying the active Cys129 residue of the enzyme.

L659989 is a PAF receptor antagonist.

L690330 is a potent inhibitor of inositol monophophatase. L690330 induces autophagy in COS-7 cells independently of mTOR inhibition.

L-703,606 is a potent, selective antagonist to the human NK1 receptor.

L-741,626 is a selective D2 receptor antagonist.

L-750,667 TriHydrochloride is a selective D4 dopamine receptor antagonist.

L-759,633 is high affinity, selective CB2 receptor agonist (Ki values are 6.4 and 1043 nM for CB2 and CB1 receptors respectively). L-759,633 potently inhibits forskolin-stimulated cAMP production via CB2 receptors expressed in CHO cells (EC50 = 8.1 nM).

L-765,314 is a drug which acts as a potent and selective antagonist for the Alpha-1 adrenergic receptor subtype α1B. It has mainly been used to investigate the role of α1B receptors in the regulation of blood pressure.

L838417 is a GABAA receptor modulator.

LG100268 is a potent and selective rexinoid and retinoid-X receptor (RXR) agonist. LG100268 binds to the α, β and γ RXR receptors with an IC50 = 3-4 nM and has no activity at the RAR retinoic acid receptors.

LP-44 is a high affinity 5-HT7 receptor agonist (Ki = 0.22 nM) that displays selectivity over 5-HT1A and 5-HT2A receptors (200- and > 1000-fold respectively). LP-44 dnduces relaxation of substance P-stimulated guinea pig ileum (EC50 = 2.56 μM).

LSN2463359 is a novel positive allosteric modulators of the mGlu? receptor.

LY-165163 is a selective 5-HT1A and 5-HT1D serotonin receptor antagonists.

LY2087101 is an allosteric potentiator of α7, α4β2 and α4β4 nAChRs. LY2087101 displays selectivity against α3β4 nAChRs.

LY 334370 hydrochloride is a selective 5-HT1F receptor agonist (Ki values are 1.87, 16.4, > 100 (IC50)). LY 334370 hydrochloride displays antimigraine effects.

LY456236 HCl is a selective mGlu1 receptor antagonist (IC50 values are 143 nM and > 10 μM for mGlu1 and mGlu5 receptors respectively). LY456236 HCl reduces hyperalgesic behavior induced by formalin in both mouse and rat with ED50 values of 28 and 16.3 mg/kg respectively.

ML169 is a novel, selective and brain penetrant M1 positive allosteric modulator (PAM).

ML218 HCl is a selective inhibitor of T-type calcium channels (IC50 values are 270 and 310 nM for Cav3.3 and Cav3.2 respectively in a patch EP assay). ML218 HCl decreases burst activity in STN neurons; reduces cataleptic behaviour in an in vivo rat model of Parkinson's disease.

MM11253 is a potent and selective RARγ antagonist with an IC50 of 44 nM. MM11253 has lower inhibition of RARα, RARβ and RXRα. MM11253 blocks the growth inhibitory effects of RARγ-selective agonists.

MRS1191 is a selective A3 adenosine receptor antagonist.

MRS1220 is a potent and highly selective antagonist at the human A3 adenosine receptor (Ki values are 0.65, 305, and 52 nM at hA3, rA1 and rA2A respectively. MRS1220 displays an IC50 value > 1 μM for inhibition of binding to rat A3 receptors.

MRS 2219 is a selective potentiator of ATP-evoked responses at rat P2X1 receptors (EC50 = 5.9 μM).

MRS 2693 trisodium salt is a selective P2Y6 agonist (EC50 = 0.015 μM at the hP2Y6 receptor). MRS 2693 trisodium salt displays no activity at other P2Y subtypes.

MRS2905 is a bioactive chemical.

MRS 4062 triethylammonium salt is a selective P2Y4 receptor agonist (EC50 values are 23, 640, and 740 nM for hP2Y4, hP2Y2 and hP2Y6 respectively).

MRS5698 is a high affinity and selective A3 adenosine receptor agonist (Ki ~ 3 nM) protects against chronic neuropathic pain. MRS5698 displays >1000-fold selectivity over A1 and A2A adenosine receptors. MRS5698 reverses mechanoallodynia in several neuropathic pain models in vivo.

NE58018 is a bioactive chemical.

NE58043 is a bioactive chemical.

NF449 is a potent purinergic receptor antagonist that displays high selectivity for P2X1 (IC50 values are 0.28, 0.69, 120, 1820, 47000 and > 300000 nM for rP2X1, rP2X1+5, rP2X2+3, rP2X3, rP2X2 and P2X4 receptors respectively). NF449 provides antithrombotic protection in vivo. NF449 also acts as a Gsα-selective antagonist.

NGB2904 is a potent and selective dopamine D3 receptor antagonist (Ki values are 1.4, 217, 223, 642, > 5000, > 10000 and > 10000 nM for D3, D2, 5-HT2, α1, D4, D1 and D5 receptors respectively). NGB2904 potently antagonizes quinpirole-stimulated mitogenesis (IC50 = 6.8 nM)

NGD 94-1 is a high affinity D4 receptor ligand. NGD 94-1 is selective over D1, D2, D3 and D5 receptors. NGD 94-1 displays antagonist activity at the human D4.2 receptor (Ki = 3.6 nM in transfected CHO cells) and exhibits agonist activity at the D4.4 receptor in HEK 293 cells.

NNC052090 is a GABA uptake inhibitor that displays moderate selectivity for BGT-1 (mGAT-2) transporters (Ki values are 1.4, 15, 19 and 41 μM for hBGT-1, hGAT-3, hGAT-1 and hGAT-2 respectively). NNC052090 inhibits sound-induced tonic and clonic convulsions in DBA/2 mice. NNC052090 also displays affinity at α1- and D2-receptors (IC50 values are 266 and 1632 nM respectively).

NNC269100 is a somatostatin sst4 receptor agonist that displays > 100-fold selectivity over sst2 receptors (Ki values are 6 and 621 nM for sst4 and sst2 receptors respectively). NNC269100 potently inhibits forskolin-induced cAMP accumulation (EC50 = 26 nM).

NPS2390 is a group I mGlu antagonist. It displays noncompetitive antagonist activity at both mGlu1 and mGlu5 receptors. NPS2390 is thought to act on a site separate from the glutamate binding pocket.

NS1738 is a α7 positive allosteric modulator.

NS3763 is a noncompetitive antagonist of GLUK5 receptor. NS3763 displays selectivity for inhibition of domoate-induced increase in intracellular calcium mediated through the GLU(K5) subtype (IC(50) = 1.6 microM) of kainate receptors compared with the GLU(K6) subtype (IC(50) > 30 microM). NS3763 inhibits the GLU(K5)-mediated response in a noncompetitive manner. NS3763 selectively inhibits l-glutamate- and domoate-evoked currents through GLU(K5) receptors in HEK293 cells.

m-Methylphenylacetonitrile is a bioactive chemical.

PD-156707 is an endothelin A receptor-selective antagonist.

PD 168368 is a competitive antagonist of neuromedin B (NMB) receptors (Kis = 15-45 nM for rat and human receptors expressed in various cell lines). It blocks the elevation of intracellular calcium and release of inositol phosphate induced by NMB in cells expressing NMB receptors.

PF-04859989 HCl is a brain-penetrable irreversible inhibitor of kynurenine amino transferase II (KAT II), the enzyme responsible for most of the brain synthesis of kynurenic acid. PF-04859989 HCl has been implicated in several psychiatric and neurological disorders, including schizophrenia and bipolar disorder.

PF0998425 is a bioactive chemical.

PSB1115 is a highly selective, water-soluble, human A2B adenosine receptor antagonist. PSB1115 has Ki values are 53.4, > 10000 and > 10000 nM at human A2B, A1 and A3 receptors respectively. It produces potent analgesic effects in vivo.

PSB603 is a adenosine A(2B) receptor antagonist which suppresses tumor growth and metastasis by inhibiting induction of regulatory T cells.

Ro67-7476 is a positive allosteric modulator of mGlu1 receptors. It potentiates glutamate-induced calcium release (EC50 = 60.1 nM at rat mGluR1a). Ro67-7476 displays no activity at human mGlu1 receptors.