Vilazodone (EMD 68843) is a combined serotonin specific reuptake inhibitor (SSRI) and 5-HT1A receptor partial agonist currently under clinical evaluation.

Voltage-independent, selective CFTR chloride channel blocker (Ki = 300 nM) that alters channel gating.

VU0463271 is a potent KCC2 antagonist, with an IC50 of 61 nM.

VX-661 is a second F508del CFTR corrector and is believed to help CFTR protein reach the cell surface.

VX-809 is a CFTR modulator with EC50 of 0.1 μM.

WZB117 is an irreversible inhibitor of glucose transporter 1 (Glut1) that blocks glucose transport in diverse cancer cells (IC50 = ~0.6 µM), reducing extracellular lactate and intracellular ATP levels.

YHO-13177 is a potent and specific inhibitor of BCRP; potentiated the cytotoxicity of SN-38 in cancer cells and no effect on P-glycoprotein–mediated paclitaxel resistance in MDR1-transduced human leukemia K562 cells.

YM-58483 is the first selective and potent inhibitor of CRAC channels and subsequent Ca2+ signals.

Zatebradine hydrochloride is a bradycardic agent that creates use-dependent inhibition of hyperpolarization-activated current (If) in sinoatrial node cells (EC50 = 480 nM) and Purkinje fibres.

Zatebradine(UL-FS49) is a potent HCN channels antagonist, which decreased the heartbeat in a reversible manner; 92% inhibition of the hHCN1-mediated current at 10 uM.

ZK 200775 is a competitive GluR (AMPA)/kainate antagonist.

α5IA is a selective inverse agonist for Α5 subtype of GABAA receptor with a higher intrinsic activity at the A5 subtype than other drugs.

KPT-251 is a selective inhibitor of nuclear export (SINE).

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.

A-887826 is a potent, selective, oral bioavailable and voltage-dependent Na(v)1.8 sodium channel blocker with an IC50 of 11 nM . A-887826 attenuates neuropathic tactile allodynia in vivo.