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.

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

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.

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.

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.

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

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

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.

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.

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.

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.

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

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

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.

SLM6031434 is SphK2-selective inhibitor.

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.

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

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.

GSK124576A is a bioactive chemical.

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.

MC-976 is an Vitamin D3 derivative.

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.

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.

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

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.

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).

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.

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.

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

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.