Cudetaxestat (BLD-0409) is a potent and orally active autotaxin (ATX) inhibitor.

ATX inhibitor 7 is a autotaxin inhibitor and shows good oral exposure.

Arofylline is a PDE4 inhibitor as a potential treatment for asthma.

Andolast is an anti-allergic agent for the treatment of bronchial asthma, chronic obstructive pulmonary disease (COPD). Andolast inhibits dose dependently guinea-pig lung cAMP-phosphodiesterase with an IC50 of 50 mM.

Mufemilast is a phosphodiesterase 4 (PDE4) inhibitor.

Safusidenib is a novel IDH1 inhibitor for the treatment of IDH1-mutated tumors.

IDO1-IN-12 is a potent and orally available IDO1 inhibitor.

IDO1-IN-11 is an IDO1 inhibitor with an IC50 value of 0.6 nM.

FXIa-IN-7 is a selective and orally bioavailable factor XIa inhibitor with an IC50 value of 0.4 nM.

FXIa-IN-6 is a potent FXIa inhibitor with selectivity against most of the relevant serine proteases (Ki = 0.3 nM).

D-(-)-3-Phosphoglyceric acid (3-Phospho-D-glyceric acid) disodium is an important intermediate in the enzyme-catalysed process of glycolysis. D-(-)-3-Phosphoglyceric acid disodium competitively inhibits yeast enolase.

ARG1-IN-1 is a human arginase 1 inhibitor with an IC50 of 29 nM.

Alacepril (Cetapril) is an orally active angiotensin converting enzyme (ACE) inhibitor with long lasting antihypertensive effect.

Fasidotril is a dual inhibitor of neprilysin and angiotensin-converting enzyme (ACE) for the potential treatment of hypertension and congestive heart failure (CHF).

Motugivatrep is the potent antagonist of transient receptor potential type 1 (TRPV1). Motugivatrep has a wide range of usefulness in treating drugs, urine tabletops, and respiratory diseases (extracted from patent WO2007010383A1).

TRPV4 antagonist 3 is a TRPV4 antagonist (pIC50 = 8.4).

TRPA1-IN-1 is a potent, selective, and orally bioavailable TRPA1 small molecule antagonist.

Oleoyl Serotonin is a TRPV1 antagonist with IC50 value of 2.57 μM for human TRPV1.

S-Bioallethrin is a pyrethroid insecticide. S-Bioallethrin disrupts nerve function by modifying the gating kinetics of transitions between the conducting and nonconducting states of voltage-gated sodium channels.

Bliretrigine is a sodium channel blocker. Bliretrigine has the effect of relieving pain.

SGLT1/2-IN-2 demonstrates potent dual inhibitory activities (IC50 = 96 nM for SGLT1 and IC50 = 1.3 nM for SGLT2).

Cibenzoline is a potent inhibitor of KATP channel with directly affecting the pore-forming Kir6.2 subunit rather than the SUR1 subunit. Cibenzoline is a class Ia antiarrhythmic drug. Cibenzoline has little anticholinergic activity. Cibenzoline markedly attenuate LVPG which has a close relationship with myocardial contractility decreasing. Cibenzoline has the potential for the research of hypertrophic obstructive cardiomyopathy.

Alloisolithocholic acid (AILCA) activates large-conductance calcium-activated potassium (BK) channels with an EC50 value of 44.21 μM in Xenopus oocytes.

S-(+)-Mecamylamine (hydrochloride) is a neuronal nicotinic receptor modulator with antidepressant activity.

UBP301 is a potent and selective antagonist of kainate receptor with IC50 and KD of 164 μM and 5.94 μM, respectively. UBP301 has ∼30-fold selectivity of kainate receptor over AMPA receptor. UBP301 is the derivative of willardiine.

Onfasprodil is negative allosteric modulator of NR2B. Onfasprodil in combination with GABA receptor regulator has the potential for the research of Alzheimer's disease (extracted from patent CN111481543A).

GluN2B receptor modulator-1 is a selective GluN2B negative allosteric modulator with an IC50 value of 31 nM.

Aptiganel hydrochloride (Cerestat) is a non-competitive NMDA receptor antagonist with neuroprotective effect.

Arbaclofen placarbil is a novel transported prodrug of the active R-isomer of baclofen. Baclofen is a racemic GABAB receptor agonist

Adipiplon (NG2-73) is a selective GABAA receptor positive allosteric modulator. Adipiplon is particularly useful in the treatment of a variety of central nervous system (CNS) disorders.