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.

RU 28318, potassium salt is a potent and selective antagonist for the mineralocorticoid receptor (MR). RU 28318, potassium salt inhibits aldosterone production and secretion, and selectively decreases ex-vivo MR binding in the hippocampus of adrenalectomised rats. It also decreases blood pressure in female rats following central administration in vivo.

SIB-1757 is a highly selective antagonist for the mGlu5 metabotropic glutamate receptor subtype. SIB-1757 displays an IC50 value of 0.4 μM at hmGlu5 compared with > 30 μM at hmGlu1b, hmGlu2, hmGlu4, hmGlu6, hmGlu7 and hmGlu8.

SIB-1893 is a highly selective non-competitive antagonist for the metabotropic glutamate mGlu5 receptor subtype; displays an IC50 value of 0.3 μM at hmGlu5, compared with > 100 μM at hmGlu1b, hmGlu2, hmGlu6, hmGlu7 and hmGlu8. It positive allosteric modulator at mGlu4 receptors.

SKF-75670 hydrobromide is a atypical D1DR (dopamine receptor) agonist. It displays antagonist activity in vitro and agonist activity in vivo.

SKF-81297 HBr is a selective dopamine D1 receptor agonist, which stimulates motor behaviour of MPTP-lesioned monkeys.

SKF-83959 HBr is a dopamine D1-like receptor partial agonist (Ki values are 1.18, 7.56, 920 and 399 nM for rat D1, D5, D2 and D3 receptors respectively). SKF-83959 HBr may act as an antagonist in vivo, producing anti-Parkinsonian effects and antagonizing the behavioral effects of cocaine.

SM19712 is a nonpeptide endothelin converting enzyme inhibitor.

SM 21 is a novel sigma(2) antagonist.

SNAP5089 is a subtype-selective α1A-adrenoceptor antagonist that displays > 600-fold selectivity over other adrenoceptors (Kivalues are 0.35, 220, 370, 540, 800 and 1200 nM for α1A, α1B, α2C, α1D, α2B and α2A subtypes respectively and 540 nM for L-type Ca2+ channels).

SQ-29548 is a highly selective TP receptor antagonist which binds to the human recombinant TP receptor with a Ki of 4.1 nM. SQ-29548 inhibits the aggregation of washed human platelets induced by U-46619 with an IC50 of 0.06 μM.

SSR 146977 is a new potent nonpeptide tachykinin NK3 receptor antagonist.

TG6-129 is an antagonist of the EP2 receptor, suppressing PGE2-induced elevation of cAMP in cells expressing EP2 with an IC50 value of 1.6 μM. It is without effect on EP4, DP1, IP, and β2-adrenergic receptors. TG6-129 reduces the expression of COX-2, IL-1β, IL-12, IL-23, IL-6, and TNF-α induced by the EP2-selective agonist butaprost in P388D1 macrophages.

U69593 is a a selective KOR-1 (κ1-opioid receptor) agonist. U-69593 is known to inhibit cocaine sensitization in meso-limbic dopamine neurons by normalizing basal overflow of dopamine.

VRT-532 is a CFTR modulator for the treatment of cystic fibrosis.

VU0285683 is a negative allosteric modulator of mGlu5 receptors. VU0285683 acts as a full antagonist and blocks the glutamate response to mGlu5 (IC50 = 24.4 nM). VU0285683 is selective for mGlu5 over mGlu1, mGlu3 and mGlu4.

DCPIB is a novel Inhibitor of Volume-Regulated Anion Channels, Distinctly Modulating K2P Channels.

VU0424465 is a potent mGlu5 positive allosteric modulator and agonist

WB 4101 hydrochloride is a α1A-adrenergic selective antagonist.

WIN 64338 hydrochloride is a potent, non-peptide, competitive bradykinin B2 receptor antagonist.WIN 64338 inhibits [3H]-bradykinin binding on guinea pig trachea with nanomolar affinity but is not active in the rabbit aorta (the classical bradykinin B1 preparation).

XAP044 is a potent and selective mGlu7 antagonist (IC50 = 88 nM). It inhibits lateral amygdala long term potentiation (LTP) in brain slices from wild type mice. XAP044 displays no effects on the LTP of mGlu7 deficient mice.

YM976 is an orally active PDE4 inhibitor (IC50 = 2.2 nM). YM976 has low emetogenic activity, suggested to be due to poor brain penetration.

YS121 is a dual inhibitor of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase.

ZK93423 is a potent benzodiazepine receptor agonist (IC50 = 1 nM). ZK93423 is non-selective between α1-, α2-, α3- and α5-subunit containing GABAA receptors (Ki values are 4.1, 4.2, 6 and 4.5 nM for inhibition of [3H]Ro15-1788 binding to human recombinant α1β3γ2, α2β3γ2, α3β3γ2 and α5β3γ2 receptors respectively).

ZK93426 is a potent, selective and competitive benzodiazepine receptor antagonist (IC50 values are 0.4 and 0.7 nM for inhibition of [3H]-flunitrazepam binding to rat cerebellum and hippocampus respectively)

C620-0696 is a novel potent inhibitor of bromodomain PHD-finger transcription factor (BPTF).

COH34 S-dioxide is an oxidized analog of COH34

CRBN-6-5-5-VHL is a novel cell-permeable, potent and selective cereblon degrader.

NPE-caged-HPTS is a caged fluorescent pH indicator, rapidly releasing the fluorophore HPTS (pKa 7.25) upon two-photon excitation (>3000 s-1).

MRK-740 is a novel potent (IC50: 80?±?16?nM), selective and cell-active PRDM9 inhibitor, specifically and directly inhibiting H3K4 methylation at endogenous PRDM9 target loci.

Niclosamide-olamine is a Insect Attractant, Repellent and Chemosterilant.

Nafcillin sodium is an antibacterial chemical.

Oxacillin (trade name Bactocill) is a narrow-spectrum beta-lactam antibiotic of the penicillin class developed by Beecham. It was patented in 1960 and approved for medical use in 1962. Oxacillin is a penicillinase-resistant β-lactam. It is similar to methicillin, and has replaced methicillin in clinical use.

Levothyroxine sodium is a thyroid hormone.

Garcinoic Acid is a natural and selective agonist of pregnane X receptor.

Nevirapine-d3 is deuterized nevirapine, reducing P450 metabolite formation, impacting on phase II metabolism and hepatocyte protein expression.

MS4 is a novel glucocorticoid receptor (GR) agonist with anti-inflammatory activity and displaying reduced impact on islets.

Pramiverin HCl is a bioactive chemical.

Acepromazine maleate, also known as Sch-10649, is a dopamine D1/2 receptor and 5-HT1A/2A receptor antagonist used to prevent nausea and induce sedation. Acepromazine maleate is discontinued.

L-Alaninol , also known as 2-Aminopropanol, is an amino acid derivative that inhibits melanoma proliferation and increases cytrochrome C reductase and tau-glutamyl transpeptidase.

Alloxan Monohydrate is a glucose analog used to induce diabetes by destroying beta-cells.

Alternariol is a mycotoxin, topoisomerase I and II inhibitor and potential ER agonist found in Alternaria.

Alyssin is a sulforaphane homolog and antioxidant. It induces phase II enzymes and increases Nrf2 levels in adenocarcinoma cells. It is has been shown to decrease the metabolism of polycyclic aromatic hydrocarbons, supressing the risk of carcinogenesis in vitro.

Amastatin HCl is an aminopeptidase inhibitor that also induces vasoconstriction.

Amisulpride is an antagonist 5-HT7 receptor and dopamine D2 and D3 receptors. It modulates beta 2- arresting signaling and increases neurite outgrowth.

Amitraz, also known as Mitaban and Taktic, is an alpha-adrenergic receptor agonist and MAO inhibitor used as an insecticide in prevention of flea and tick infections. It prevents prostaglandin synthesis and may inhibit beta-cell insulin release.

Amphotericin B binds ergosterol and induces membrane pore formations, increasing ROS and suppressing fungal growth. It also increases expression of IL-1-beta, TNF-alpha, BDNF and GDNF and protects against prion-induced neurodegeneration.

Ampicillin Trihydrate is a transpeptidase inhibitor that prevents bacterial cell wall formation. It is effective against gram negative and gram positive bacteria.

Amprolium HCl is coccidiostat and thiamine transporter inhibitor. It inhibits thiamine transporters in species of Eimera, preventing carbohydrate synthesis.

Anabasine HCl is used as an insecticide and as a clinical biomarker for tobacco smoke exposure. It is also a depolarizing NMJ blocker, nAChr antagonist, aromatase inhibitor, and teratogen found in species of Nicotiana.

Anisodamine is an inhibitor of alpha-1 adrenergic receptors and mAChRs isolated from Chinese solanacea plant.

Antipain HCl is a protease inhibitor found in Actinomycetes.

Arvanil is a CB1 and TRPV1 agonist. It increases lung tidal volume, diaphragm activity, mean arterial blood pressure and inhibits lymphocyte proliferation.

Atropine is a mAChR antagonist found in Solanaceae used to initiate mydriasis. It decreases thermal pain, inhibits histamine-induced increases in thromboxane A2, and acts as a positive inotrope.

Azithromycin dihydrate is a protein translation inhibitor used for it's antibacterial properties. It is also known to inhibit the epithelila-to-mesenchymal transition and suppresses LPS-stimulated production of pro-inflammatory cytokines in macrophages.

O(6)-Benzylguanine is an MGMT inhibitor that prevents the repair of DNA damage induced by chemotherapeutics. It allows apoptosis and other mechanisms of cell death to occur.

Berteroin is an erucin homolog and potential antioxidant. It is present in cruciferous vegetables, including Chinese cabbage, rucola salad leaves, and mustard oil. It decreases expression of androgen receptors in prostate cancer cells. It also decreases the release of pro-inflammatory cytokines in LPS-stimulated macrophages.

Ubenimex, also known as NK 421 and Bestatin, is a CD13 inhibitor. Ubenimex attenuates acquired sorafenib resistance in renal cell carcinoma by inhibiting Akt signaling in a lipophagy associated mechanism. Ubenimex synergistically enhances the effects of anticancer drugs in hepatocellular carcinoma. Ubenimex inhibits cell proliferation, migration and invasion by inhibiting the expression of APN and inducing autophagic cell death in prostate cancer cells.

Biopterin is an endogenous pterin coenzyme required for production of neutrotransmitters and release of NO

Bupivacaine is a BK/SK, Kv1, Kv3, TASK-2 K Channel and voltage-gated Na channel blocker used as an anesthetic. It maybe neurotoxic at high does, inducing apoptosis in neuroblastoma cells.

Butein is found in Rhuteic verniciflua and Butea monosperma. It induces cell cycle arrest and apoptosis in lung cancer cells, inhibits vessel spouting from aortic rings, and prevents hepatic stellate cell activation.

Cerulomycin A is a toxin that inhibits growth of Entamoeba. It may prevent proliferation of cancer cells, and suppresses immune responses.

Canrenone is a metabolite of spironolactone, Na/K ATPase partial agonist and aldosterone and androgen receptor antagonist used as a diuretic.

Carbadox is a livestock anitbiotic and growth promoter. It is particularly effective in treating swine dysentery and enteritis. However, its use has been prohibited in the UK following reports of carcinogenicity and mutagenicity.

Cefaclor monohydrate is a penicillin binding protein inhibitor that prevents peptidoglycan synthesis and bacterial cell wall formation. It also enhances phagocytosis, bacterial activity of granulocytes and macrophages, and slows gastric emptying and intestinal transit.

Cefoperazone is a penicillin binding protein inhibitor and mammalian mRNA splicing inhibitor that prevents peptidoglycan synthesis and bacterial cell wall formation.

Cefotaxime Acid is a penicillin binding protein inhibitor that prevents peptidoglycan synthesis and bacterial cell wall formation. It is mostly resistant to β-lactamase activity.

Ceftiofur sodium is a penicillin binding protein inhibitor that prevents synthesis of bacterial cell walls. It also decreases LPS-induced expression of pro-inflammatory cytokines in endotoxemia models.

Cheirolin is an antioxidant and sulfonyl analog of sulforaphane. It induces phase II enzyme activity and expression.

Chlormadinone acetate is a synthetic steroid hormone and antagonist at androgen and estrogen receptors used to treat BPH and polycystic ovary syndrome. It also promotes osteoblast differentiation and Ca deposition in bone marrow stem cells.

Chromium picolinate is used to prevent chromium deficiency and to decrease serum glucose and insuline levels. It also decreases plasma lipid levels and platelet aggregation and improves myocardial contractility.

Chymostatin is a protease inhibitor used in research models.