MS-PPOH is a potent and selective cytochrome P450 (CYP) epoxygenase inhibitor. MS-PPOH inhibits CYP2C8 and CYP2C9 with IC50s of 15 and 11 µM, respectively.

ONO-RS-082 is an inhibitor of phospholipase A (PLA). ONO-RS-082 inhibits PLA2 with the IC50 of 1.0 μM, but does not inhibit PLC even at 100 μM.

PCSK9-IN-3 is a novel, highly potent, and orally bioavailable next-generation tricyclic peptide PCSK9 inhibitor.

PDE4-IN-4 is a dual M3 (pIC50 = 10.2) antagonist-PDE4 (pIC50 = 8.8) inhibitor for the inhaled treatment of pulmonary diseases.

ROC-0929 (compound 13a) is a potent and selective inhibitor of secreted phospholipases A2 (sPLA2s) with an IC50 of 80 nM, specially targeting hGX. ROC-0929 inhibits the phosphorylation of ERK1/2 and p-38. Secreted phospholipases A2 (sPLA2s) are a family of disulfide-rich, Ca2+-dependent enzymes that hydrolyze the sn-2 position of glycero-phospholipids to release a fatty acid and a lysophospholipid. ROC-0929 has the potential for researching inflammation related diseases.

Sphinganine 1-phosphate (D-erythro-Dihydrosphingosine 1-phosphate) is a polar sphingolipid metabolite that regulates cell migration, differentiation, survival and complex physiological processes.

SSR69071 is a potent, orally active and selective inhibitor of neutrophil elastase. SSR69071 reduces myocardial infarct size following ischemia-reperfusion injury. SSR69071 displays a higher affinity for human elastase (Ki=0.0168 nM) than for rat (Ki=3 nM), mouse (Ki=1.8 nM), and rabbit (Ki= 58 nM) elastases.

trans-urocanic acid (trans-UCA), a natural epidermal constituent, inhibits human natural killer cell (NK) activity in vitro. trans-urocanic acid is active in regulating an immune function.

WNK-IN-11 D3 is an orally active, selective and potent With-No-Lysine (WNK) kinase inhibitor. WNK-IN-11 D3 is effective at regulating cardiovascular homeostasis.

Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces. Actinonin inhibits aminopeptidase M, aminopeptidase N and leucine aminopeptidase. Actinonin is a potent reversible peptide deformylase (PDF) inhibitor with a Ki of 0.28 nM. Actinonin also inhibits MMP-1, MMP-3, MMP-8, MMP-9, and hmeprin α with Ki values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin is an apoptosis inducer. Actinonin has antiproliferative and antitumor activities.

Etilevodopa (L-Dopa ethyl ester), an ethyl-ester prodrug of Levodopa, is rapidly hydrolyzed to Levodopa and ethanol by nonspecific esterases in the gastrointestinal tract. Etilevodopa is used for the treatment of Parkinson disease (PD). Levodopa is the direct precursor of dopamine and is a suitable prodrug as it facilitates CNS penetration and delivers dopamine.

Halopemide is a potent phospholipase D (PLD) inhibitor, with IC50s of 220 and 310 nM for human PLD1 and PLD2, respectively. Halopemid is a dopamine receptors antagonist, and acts a psychotropic agent.

N-Desmethyl Clomipramine hydrochloride (Desmethylclomipramine hydrochloride) is a primary plasma N-desmethyl metabolite of Clomipramine. Clomipramine is a tricyclic antidepressant.

MJ33 is an active-site-directed, specific, competitive, and reversible phospholipase A2 (PLA2) inhibitor. MJ33 blocks the calcium-independent phospholipase A2 (iPLA2) activity of Prdx6. MJ33 has a critical effect on inflammatory brain damage.

Streptolysin O, a group A streptococcal toxin, is a well-characterized oxygen-labile prototype of a cholesterol-binding bacterial exotoxin. Streptolysin O causes both lysis of cells and cardiotoxicity. Streptolysin O is widely used for the controlled permeabilization of cell membranes. Streptolysin O exists in two forms, a reduced active state and an oxidized reversibly inactive state .

L-Methionine sulfoxide (H-Met(O)-OH), a metabolite of Methionine, induces M1/classical macrophage polarization, and modulates oxidative stress and purinergic signaling parameters.

Obidoxime dichloride is a non-full spectrum oxime agent and can be used as an antidote for organophosphate nerve agent poisoning. Obidoxime dichloride reactivates sarin-inhibited acetylcholinesterase (AChE) and reduces acute toxicity of sarin-evaluated.

U-73122 is an inhibitor of phospholipase C, phospholipase A2, and 5-LO (5-lipoxygenase).

Bay 60-7550 is a potent PDE2 inhibitor with IC50 values of 2.0 nM (bovine) and 4.7 nM (human); 50-fold more selective for PDE2 compared to PDE1 and greater than 100-fold selective compared to PDE5, PDE3B, PDE4B, PDE7B, PDE8A, PDE9A, PDE10A, and PDE11A.

D609 is a selective competitive phosphatidyl choline-specific phospholipase C (PC-PLC) inhibitor (Ki = 6.4 μM); antiviral and antitumor agent.

Merimepodib(VX-497) is a novel noncompetitive inhibitor of IMPDH (Inosine monophosphate dehydrogenase).

β-Secretase Inhibitor III is an extremely selective BACE1 inhibitor (Ki = 0.13 nM).

β-Secretase Inhibitor I is an extremely potent β-secretase inhibitor with reduced cardiovascular and liver toxicity.

Liarozole Dihydrochloride is identified as a modest inhibitor of P450 with IC50 of 2.2–6.0 μM and 260 nM for CYP26 and rat CYP17 respectively.

Millmerranone A shows the acetylcholinesterase inhibitory property.

Phenylpyropene C (S14-95), a JAK/STAT pathway inhibitor, can inhibit IFN-γ mediated expression of the reporter gene (IC50=5.4~10.8 μM). Phenylpyropene C also is an inhibitor of acyl-CoA, with an IC50 of 16.0 μM.

MeDTC (S-Methyl-N,N-diethylthiocarbamate Sulfone), a Disulfiram metabolite, is a potent, irreversible aldehyde dehydrogenase (ALDH) inhibitor.

Plantainoside D shows ACE inhibitory activity with IC50 2.17 mM. And plantainoside D is a promising IKK-β inhibitor.

p-Hydroxyphenethyl trans-ferulate has anti-hyperglycemic（yeast α-glucosidase，IC50 19.24 ± 1.73 µmol L-1）, antioxidant, and anti-inflammatory activities. p-Hydroxyphenethyl trans-ferulate shows inhibiting cancer preve

Ladostigil (TV-3326) hemitartrate is a dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), with an IC50 of 37.1 and 31.8 μM for MAO-B and AChE, reapectively. Ladostigil hemitartrate could increase cholinergic transmission, prevent the formation of ROS or their actions and be used for the research of depression and Alzheimer's disease.