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.

MAO-B-IN-2 is a selective and competitive inhibitor of MAO-B and BChE with IC50 values of 0.51 and 7.00 μM, respectively.

Mulberrofuran G protects ischemic injury-induced cell death via inhibition of NOX4-mediated ROS generation and ER stress. Mulberrofuran G shows moderate inhibiting activity of hepatitis B virus (HBV) DNA replication with the

Okadaic acid, a marine toxin, is an inhibitor of protein phosphatases (PP), including PP1 (IC50=15-50 nM), PP2A (IC50=0.1-0.3 nM), PP3 (IC50=3.7-4 nM), PP4 (IC50=0.1 nM), PP5 (IC50=3.5 nM), with a significantly higher affinity for PP2A. Okadaic acid increase of phosphorylation of a number of proteins by inhibiting PP, and acts a tumor promoter.

PTP1B-IN-14 is a selective PTP1B inhibitor (IC50 = 0.72 μM) targeting the allosteric site.

PTP1B-IN-13 is a selective PTP1B inhibitor targeting the allosteric site with an IC50 value of 1.59 μM.

PDE4-IN-3 is a novel and orally active PDE4 inhibitor with potent inhibitory affinity (IC50 = 4.2 nM).

N-Desmethyl Sildenafil (Desmethylsildenafil) is a major metabolite of Sildenafil. Sildenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor.

PCSK9-IN-2 is a novel small molecule inhibitor of PCSK9-LDLR protein–protein interaction (PPI) with an IC50 value of 7.57 μM.

Chikusetsusaponin Ib has anti-Alzheimer's disease activity and is a potent AChE inhibitor.

Cyclopenin ((±)-Isocyclopenine) is a racemate.

Cyclanoline (chloride) shows cholinesterase inhibitory activity.