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.

Isonaringin shows anti-Alzheimer’s activity by inhibiting AChE.

GCPII-IN-1 is a glutamate carboxypeptidase II (GCPII, or PSMA) inhibitor scaffold with a Ki of 44.3 nM.

Cathepsin L-IN-2 (Z-Phe-Phe-FMK) is a potent and irreversible cathepsin L and cathepsin B inhibitor.

Indoluidin E selectively inhibits DHODH and suppresses cancer cell growth.

DHODH-IN-18 is a human DHODH inhibitor (IC50 = 0.2 nM).

Ascochlorin A is a novel and potent hDHODH inhibitor (KD = 3.29 μM) for treatment of triple-negative breast cancer.

Indole-3-acetaldehyde inhibits Escherichia coli O157:H7 biofilm formation.

Ganoderlactone D shows inhibitory effects of yeast α-Glucosidase with IC50 values of 41.7 μM.

IDO-IN-14 is an IDO inhibitor with an IC50 value of 0.6928 nM.

IDO-IN-15 is an IDO1 inhibitor (IC50 < 0.51 nM).

D-Cl-amidine hydrochloride is a potent and highly selective PAD1 inhibitor. D-Cl-amidine is well-torelated with no significant toxicity.

(E)-Dehydrodiconiferyl alcohol behaves as good hCA IX and hCA XII dual inhibitors. And (E)-Dehydrodiconiferyl alcohol suppresses the NF-κB nuclear translocation in connective tissue of healing area.

ABP 25 is an activity-based probe for cathepsin K imaging with excellent potency and selectivity.

4-Hydroxytryptamine creatinine sulfate, a tryptamine derivative, is a neurotransmitter agonist.

ADAM8-IN-1 is a potent ADAM8 inhibitor with an IC50 value of 73 nM.

(S)-Salsolidine is a weak monoamine oxidase (MAO) inhibitor (Ki=63 μM). The R enantiomer of Salsolidine is more potent than the S form (Ki=26 μM).

(+)-Cinchonaminone shows monoamine oxidase (MAO) inhibitory activity.

28-O-β-D-Glucopyranosyl pomolic acid is a urokinase plasminogen activator inhibitor with IC50 at 37.82 μM.