Leupeptin hemisulfate is a reversible, competitive serine/cysteine protease inhibitor, which has been shown to inhibit cathepsins B, H, L, and S, calpain, and trypsin. Leupeptin hemisulfate is an orally active, antioxidant and anti-inflammatory agent.

Apremilast(CC10004) is a novel small molecule inhibitor of PDE4 with an IC50 value of 74 nM.

PSB-06126 is a selective nucleoside triphosphate diphosphohydrolase (NTPDase) inhibitor, with the Ki values of 0.33 μM for rat NTPDase 1, 19.1 μM for NTPDase 2 and 2.22 μM for NTPDase 3, respectively.

HSD-016 (HSD016) is a potent, selective, and efficacious 11β-HSD1 inhibitor with IC50 of 149 and 530 nM for mouse and human 11β-HSD1, respectively.

Razuprotafib is a potent protein tyrosine phosphatase β (HPTPβ) inhibitor..

Plecanatide, an analogue of Uroguanylin, is an orally active guanylate cyclase-C (GC-C) receptor agonist. Plecanatide activates GC-C receptors to stimulate cGMP synthesis with an EC50 of 190 nM in T84 cells assay. Plecanatide shows anti-inflammatory activity in models of murine colitis.

CDC25B-IN-2 is a potent cdc25B inhibitor.

MAGL-IN-4 is an orally active, selective and reversible monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 6.2 nM. MAGL-IN-4 can penetrate the blood-brain barrier (BBB). MAGL-IN-4 enhances endocannabinoid signaling mostly by the increase in the level of 2-AG via selective MAGL inhibition in the brain.

SID 26681509 is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 inhibits in vitro propagation of malaria parasite Plasmodium falciparum and inhibits Leishmania major with IC50s of 15.4 μM and 12.5 μM, respectively. SID 26681509 shows no inhibitory activity against cathepsin G.

Cerivastatin is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally active HMG-CoA reductase inhibitor, with a Ki of 1.3 nM/L. Cerivastatin reduces low-density lipoprotein cholesterol levels. Cerivastatin also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, and has anti-cancer effect.

BAY-678 is a cell-permeable inhibitor of human neutrophil elastase (HNE).

ARP-100 is a potent and selective matrix metalloproteinase MMP-2 inhibitor (IC50=12 nM). ARP-100 interacts with S1＇ pocket of MMP-2 and shows anti-invasive properties in an in vitro model of invasion on matrigel. ARP-100 shows the less inhibitory activity towards MMP-1 (>50 μM), MMP-3 (4.5 μM), MMP-7 (>50 μM), and MMP-9 (0.2 μM).

4-Hydroxynonenal (4-HNE) is an α,β unsaturated hydroxyalkenal and an oxidative/nitrosative stress biomarker. 4-Hydroxynonenal is a substrate and an inhibitor of acetaldehyde dehydrogenase 2 (ALDH2). 4-Hydroxynonenal can modulate a number of signaling processes mainly through forming covalent adducts with nucleophilic functional groups in proteins, nucleic acids, and membrane lipids. 4-Hydroxynonenal plays an important role in cancer through mitochondria.

Enzalutamide carboxylic acid (MDV3100 carboxylic acid) is an inactive metabolite of Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist.

ABX-1431 (ABX1431) is a highly potent, selective, orally available, CNS-penetrant monoacylglycerol lipase (MGLL) with IC50 of 14 nM (hMGLL).

THP104c is a mitochondrial fission inhibitor.

MCI-INI-3 is a potent, selective, competitive inhibitor of ALDH1A3 (Ki=0.55 uM), shows poor inhibitory effect on the structurally related isoform ALDH1A1 (>140-fold selectivity).MCI-INI-3 also displays on inhibition against six isoforms of ALDH (ALDH16A1, ALDH7A1, ALDH9A1, ALDH2, ALDH1B1, ALDH18A1).MCI-INI-3 demonstrates selective binding to ALDH1A3 in glioma stem cell lysates, inhibits ALDH activity and affects RA synthesis in cells.

AC1-IN-38 is a potent, selective inhibitor of adenylyl cyclase type 1 (AC1) with IC50 of 0.54 uM.AC1-IN-38 shows selectivity over a closely related isoform AC8, and no activity against AC2/5 and other common neurological targets.AC1-IN-38 displayed modest antiallodynic effects in a mouse model of inflammatory pain.

SGK1-IN-4 (compound 17a) is a highly selective, orally active SGK1 inhibitor. SGK1-IN-4 can be used for osteoarthritis research.

MCUF-651 (MCUF651) is a small molecule guanylyl cyclase A receptor (GC-A) positive allosteric modulator (PAM), potentiate ANP-mediated cGMP with EC50 of 0.45 uM (Emax=82%) in HEK293 GC-A cells.MCUF-651 enhanced ANP-mediated cGMP generation in human cardiac, renal, and fat cells and inhibited cardiomyocyte hypertrophy in vitro.MCUF-651 binds to GC-A (Kd=397 nM) and selectively enhances the binding of ANP to GC-A ( MCUF-651+ANP, Kd=0.06 nM).MCUF-651 is orally bioavailable in mice and enhances the ability of endogenous ANP and BNP to generate GC-A-mediated cGMP ex vivo.

BAY-747 (BAY747) is a novel potent, selective, brain-penetrant soluble guanylate cyclase (sGC) stimulator.

BMS-820132 (BMS 820132) is potent, selective, partial glucokinase (GK) activator with AC50 of 29 nM.

N-Desmethyl Pimavanserin (AC-279) is the active metabolite of Pimavanserin. Pimavanserin is a selective inverse agonist of the 5-HT2A receptor with pIC50 and pKd of 8.73 and 9.3, respectively.

Enasidenib (Idhifa, AG-221) mesylate is an orally available, selective and potent inhibitor of mutant isocitrate dehydrogenase 2 (IDH2).

Simvastatin sodium is a lactone prodrug, can be hydrolysed to active hydroxy-acid by non-specific carboxyesterases or non-enzymatic processes. Simvastatin sodium shows a inhibition of HMG-CoA reductase with a Ki value of 0.12 nM.

INU-101 (INU101) is a highly potent, selective, orally acitve 11β-HSD1 inhibitor with IC50 of 26.2 nM, 37 nM and 0.6 nM for mice, rats, and human 11β-HSD1, respectively.

ASP3662 is a potent, selective, CNS-penetrable and orally active inhibitor of 11β-HSD1 with Ki of 5.3, 2.6 and 23 nM for human, mouse and rat 11β-HSD1, does not inhibit human 11β-HSD2 at 30 uM.

Abiraterone decanoate is a potent Abiraterone prodrug. Abiraterone decanoate provide a controlled release of Abiraterone and long-acting CYP17 inhibition with intramuscular (IM) delivery.

POMHEX, a racemic mixture and a cell-permeable pivaloyloxymethyl (POM) prodrug of HEX, is a potent, ENO2-specific of enolase. POMHEX exhibits low-nanomolar potency against ENO1-deleted cells in vitro and is capable of eradicating ENO1-deleted xenografted tumours in vivo. POMHEX is a potent glycolysis.

2-MPPA (GPI-5693) is an orally active and selective glutamate carboxypeptidase II (GCP II; PSMA) inhibitor with an IC50 of 90 nM.