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.

Fitusiran (ALN-AT3SC), an small interfering RNA, specifically targets antithrombin (AT) messenger RNA to lower production of AT in the liver. Fitusiran increases thrombin generation and has the potential for the research of the hemophilia.