Basmisanil is a highly selective inverse agonist/negative allosteric modulator of α5 subunit-containing GABAA receptors which is under development by Roche for the treatment of cognitive impairment associated with Down syndrome.

BAY-8002 is a novel potent, selective, orally available monocarboxylate transporter 1 (MCT1) inhibitor (Kd=7.9 nM).

Brevianamide F , also known as cyclo-(L-Trp-L-Pro), belongs to a class of naturally occurring 2,5-diketopiperazines.

KL-11743 is a potent, orally active, and glucose-competitive inhibitor of the class I glucose transporters, with IC50s of 115, 137, 90, and 68 nM for GLUT1, GLUT2, GLUT3, and GLUT4, respectively. KL-11743 specifically blocks glucose metabolism. KL-11743 can synergize with electron transport inhibitors to induce cell death.

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.

Xestospongin C ((-)-Xestospongin C) is a selective, reversible inositol 1,4,5-trisphosphate receptor (IP3R) inhibitor. Xestospongin C acts as an inhibitor of the sarcoplasmic/endoplasmic reticulum Ca2+ ATPase (SERCA) pump of internal stores. Xestospongin C blocks IP3-induced Ca2+ release from cerebellar microsomes with an IC50 of 358 nM. Xestospongin C is a valuable tool for investigating the structure and function of IP3Rs and Ca2+ signaling in neuronal and nonneuronal cells.

HSK16149 is a novel ligand of voltage-gated calcium channel (VGCC) α 2 δ subunit.

Clemizole is a H1 histamine receptor antagonist.Recently, researchers have identified that clemizole hydrochloride can inhibit NS4B's RNA binding and hepatitis C virus (HCV) replication.

Clevidipine(Clevidipine) is a short-acting dihydropyridine calcium channel antagonist (IC50= 7.1 nM, V(H) = -40 mV ) under development for treatment of perioperative hypertension.

WAY-213613 (WAY213613) is a potent, non-substrate inhibitor of EAAT2 (GLT-1) with IC50 of 85 nM, displays > 44-fold selectivity over EAAT1 and EAAT3; also exhibits no activity towards ionotropic and metabotropic glutamate receptors.

A2793 is an efficient TWIK-related acid-sensitive K+ channel (TASK)-1 inhibitor, with an IC50 of 6.8 μM.

Caroverine hydrochloride is a potent, competitive and reversible antagonist of NMDA and AMPA glutamate receptor. Caroverine hydrochloride is also an antioxidant and calcium-blocking agent that exhibits vasorelaxant action. Caroverine hydrochloride can be used for the research of inner ear tinnitus.

Cilnidipine(FRC8653) is a dual L- and N-type calcium channel blocker and displays antihypertensive, sympatholytic and neuroprotective activity.

Eliprodil is a non-competitive NMDA receptor antagonist that acts at the polyamine modulatory site.

GLPG-1837(ABBV-974) is a novel cystic fibrosis transmembrane conductance regulator CFTR potentiator.