Lp-PLA2-IN-9 (compound 17), a tetracyclic pyrimidinone compound, is a potent Lp-PLA2 inhibitor with a pIC50 of 10.1 for rhLp-PLA2. Lp-PLA2-IN-9 has the potential for neurodegenerative related diseases research.

Lp-PLA2-IN-11 is a potent inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). Lp-PLA2 previously known as platelet- activating factor acetylhydrolase (PAF-AH), is a phospholipase A2 enzyme involved in hydrolysis of lipoprotein lipids or phospholipids. Lp-PLA2-IN-11 has the potential for the research of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease (extracted from patent WO2014114249A1, compound E145).

PACOCF3 (Palmityltrifluoromet​hylketone) is a selective phospholipase A2 inhibitor with an IC50 of 3.8 μM. PACOCF3 alters Ca2+ signaling in renal tubular cells.

Vinaxanthone (SM-345431) is a potent and selective semaphorin3A inhibitor. Vinaxanthone exhibits semaphorin3A inhibiting activity with an IC50 of 0.1-0.2 μM. Vinaxanthone shows selective inhibitory activity against phospholipase C (PLC) from rat brain, mutine colon 26 Adenocarcinoma and murine fibroblasts NIH3T3 with IC50s being 5.4, 9.3 and 44 μM, respectively.

Lp-PLA2-IN-10 is a potent inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). Lp-PLA2 previously known as platelet- activating factor acetylhydrolase (PAF-AH), is a phospholipase A2 enzyme involved in hydrolysis of lipoprotein lipids or phospholipids. Lp-PLA2-IN-10 has the potential for the research of neurodegenerative-related diseases such as Alzheimer's disease (AD), glaucoma, age-related macular degeneration (AMD), or cardiovascular diseases including atherosclerosis (extracted from patent WO2022001881A1, compound 4).

PDE4-IN-8 (Example 5) is a potent PDE4 inhibitor with an IC50 of 0.93 nM for PDE4B2.PDE4-IN-8 has little effect on IL13 (IC50=4.04 nM), IL4 (IC50=36.33 nM), IFNy (IC50=2394 nM).

PF-07038124 is a PDE4 inhibitor with an IC50 of 0.5 nM for PDE4B2. PF-07038124 shows inhibitory activities against IL-13, IL4, and IFNγ (IC50=125, 4.1 1.06 nM, respectively).

PDE4-IN-5 (compound 33a) is a potent and selective PDE4 inhibitor (IC50=3.1 nM). PDE4-IN-5 has favorable skin permeability and a well-characterized binding mechanism. Anti-psoriasis effect.

Ro 3-1314 (9a,12a-Octadecadiynoic acid) is a plant lipoxygenase inhibitor. Ro 3-1314 is a linoleic acid metabolism inhibitor. Ro 3-1314 stimulates the antigen-induced contraction of guinea-pig tracheal spirals and the immunological release of slow reacting substance of anaphylaxis (SRS-A) from actively sensitized guinea-pig lung fragments.

AGI-12026 is brain-penetrant dual inhibitor of mutant IDH1 and 2. AGI-12026 shows partial inhibition of the IDH1-R132H homodimer as allosteric modulators. AGI-12026 has the potential for research of glioma.

IDO1-IN-15 is a potent IDO1 inhibitor (IC50=127 nM). IDO1-IN-15 has comparable potency against IDO1 enzyme in vitro with Epacadostat.

IDO1-IN-14 (compound 4a) is a potent IDO1 inhibitor with an IC50 of 396.9 nM. IDO1-IN-14 has cellular IDO1 inhibition (HeLa EC50=3393 nM).

IDO1-IN-13 (compound 27a) is a potent IDO1 inhibitor with an IC50 of 61.6 nM. IDO1-IN-13 has cellular IDO1 inhibition (HeLa EC50= 30 nM). IDO1-IN-13 decreases 51% of the kyn/trp ratio in SK-OV-3 xenograft tumor tissues.

S-2E is an orally active and noncompetitive HMG-CoA reductase and acetyl-CoA carboxylase inhibitor. S-2E has an anti-hyperlipidemic action. S-2E has the potential for familial hypercholesterolemia and mixed hyperlipidemia research.

Glucokinase activator 3 is a potent and full Glucokinase (GK) activator with an AC50 of 38 nM. Glucokinase activator 3 has the potential for the research of type 2 diabetes.

Alvelestat (tosylate) is an orally bioavailable, affinity and selective inhibitor of neutrophil elastase (NE) with a pIC50 value of 7.9 nM, a Ki value of 9.4 nM and a Kd value of 9.5 nM.

Cathepsin G Inhibitor I is a potent, selective, reversible, competitive, non-peptide inhibitor of cathepsin G.

Cathepsin K inhibitor 2 is a potent inhibitor of cathepsin K. Cathepsin K, Cat K is a cysteine protease expressed under the control of CTSK gene and closely related to osteoporosis, whose main function is to hydrolyze collagen. Cathepsin K inhibitor 2 has the potential for the research of osteoarthfitis (extracted from patent WO2021147882A1, compound 78).

Carbonic anhydrase inhibitor 12 is a potent CA II inhibitor, also has inhibitory activity in CA I (Kis of 1.72 and 271 nM in CA II and CA I, respectively). Carbonic anhydrase inhibitor 12 has potent anticancer activity against different cancer cell lines.

Carbonic anhydrase inhibitor 9 is a potent carbonic anhydrase (CA) inhibitor with Kis of 56.4 and 56.9 nM for hCA II and IX, respectively. Antiproliferative activity.

Carbonic anhydrase inhibitor 11 (compound VI) is a potent, selective carbonic anhydrase inhibitor. Carbonic anhydrase inhibitor 11 shows Ki values of 40, 39, 200 and 900 nM against CA II, IX, and XII, respectively.

Human carbonic anhydrase II-IN-24 (Compound R-13) is a potent human carbonic anhydrase (hCA) inhibitor with Kis of 60.7, 320.7, 2298, and 35.2 nM for hCA I, II, IV and IX, respectively.

Human carbonic anhydrase II-IN-1 (Compound S-13) is a potent human carbonic anhydrase II (hCA II) inhibitor with a Ki of 4.4 nM. Human carbonic anhydrase II-IN-1 also inhibits other hCAs isoforms I, IV and IX, with Ki values of 9.2 nM, 480.2 nM and 14.7 nM, respectively. Human carbonic anhydrase II-IN-1 can be used for glaucoma research.

AD013 is a dual inhibitor of cACE/NEP. AD013 is synthesized based on the previously reported C-domain selective ACE inhibitor lisinopril-tryptophan. AD013 has the potential for providing the potent antihypertensive and cardioprotective benefits.

AD012 is a dual inhibitor of cACE/NEP. AD012 is synthesized based on the previously reported C-domain selective ACE inhibitor lisinopril-tryptophan. AD012 has the potential for providing the potent antihypertensive and cardioprotective benefits.

AD011 is a dual inhibitor of cACE/NEP. AD011 is synthesized based on the previously reported C-domain selective ACE inhibitor lisinopril-tryptophan. AD011 has the potential for providing the potent antihypertensive and cardioprotective benefits.

Aldose reductase-IN-2 (Compound 5f) is a potent inhibitor of aldose reductase (AR). Aldose reductase-IN-2 has antioxidation capacity. Aldose reductase-IN-2 is a promising anti-diabetic complications agent.

Aldose reductase-IN-3 (Compound 5) is a potent and moderately selective inhibitor of aldose reductase (AR) with an IC50 of 3.99 μM. Aldose reductase has recently emerged as a molecular target that is involved in various inflammatory diseases, including sepsis. Aldose reductase-IN-3 has the potential for the research of sepsis.

ALDH1A1-IN-2 is a potent inhibitor of aldehyde dehydrogenase 1a1 (aldh1a1). Aldehyde dehydrogenases (ALDH) constitute a family of enzymes that play a critical role in oxidizing various cytotoxic xenogenic and biogenic aldehydes. ALDH1A1-IN-2 has the potential for the research of cancer, inflammation, or obesity (extracted from patent WO2019089626A1, compound 295).

Guanylyl imidodiphosphate (Gpp(NH)p) lithium, a non-hydrolyzable GTP analogue, increases adenylate cyclase activity.