JNJ-54175446 is a potent and selective brain penetrant P2X7 receptor antagonist, with pIC50s of 8.46 and 8.81 for hP2X7 receptor and rP2X7 receptor, respectively.

Camlipixant (BLU-5937) a potent, selective, non-competitive and orally active P2X3 homotrimeric receptor antagonist with an IC50 of 25 nM against hP2X3 homotrimeric. Camlipixant shows potent anti-tussive effect and no taste alteration. Camlipixant can be used for the research of unexplained, refractory chronic cough.

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

Tetramethylglycerol (Tetramethylglycoluril) is a small molecule that acts on GABA Receptor, with anti-anxiety activity.

Azumolene (EU4093 free base), a Dantrolene analog, is a muscle relaxant. Azumolene is a ryanodine receptor (RyR) modulator and inhibits the calcium-release through ryanodine receptor. Azumolene can be used for malignant hyperthermia research.

GNE-131 is a novel NaV1.7 inhibitor with IC50 0.003uM,improving metabolic stability,efficacy in mouse IEM model at C-plasma <2.8uM.

DL-AP7 is a competitive antagonist of the ionotropic glutamate receptor, NMDA.

NS8593 hydrochloride is a potent and selective small conductance Ca2+-activated K+ channels (SK channels) inhibitor. NS8593 hydrochloride reversibly inhibits SK3-mediated currents with a Kd value of 77 nM. NS8593 hydrochloride inhibits all the SK1-3 subtypes Ca2+-dependently (Kds of 0.42, 0.60, and 0.73 μM, respectively, at 0.5 μM Ca2+), and does not affect the Ca2+-activated K+ channels of intermediate and large conductance (hIK and hBK channels, respectively).

α-Conotoxin MII is a highly potent and selective competitive antagonist for α3β2 subunit-containing nicotinic receptors (IC50 = 0.5 - 3.5 nM at α3β2 expressed in Xenopus oocytes). Also potently blocks β3-containing neuronal nicotinic receptors. Displays > 200-fold selectivity for α3β2 over α2β2, α4β2 and α3β4.

DPO-1 is a potent inhibitor of the voltage-gated potassium channel subtype Kv1.5 and a blocker of ultrarapid delayed rectifier potassium current. DPO-1 prevents atrial arrhythmia.

KM91104, a cell-permeable V-ATPase inhibitor, specifically targets the a3-b2 subunits of V-ATPase.

VB-124 is a potent and selective MCT4 inhibitor. VB124 might redirect glycolytic carbon flux into mitochondrial pyruvate oxidation. VB 124 bolcks lactate import (IC50=8.6nM), and export (IC50=19nM) in MDA-MB-231 cells that are engineers to express MCT4 as the only major plasma membrane lactate transporter.

NBI921352 is a Nav1.6 inhibitor with an IC50 value of 3.765 μM.

DNQX is a elective non-NMDA antagonist

AZD0095 is a selective and orally active MCT4 inhibitor (IC50: 1.3 nM). AZD0095 effectively inhibits the tumor growth in NCI-H358 xenograft in combination with Cediranib.

GSK3395879 (GSK-3395879) is a novel potent, selective, orally bioavailable antagonist of TRPV4 with IC50 of 1 nM (hTRPV4); exhibits little or no activity against a broad panel of TRP channels (IC50 > 10µM for TRPA1, TRPV1, TRPM2, TRPM4, TRPM8, TRPC3, TRPC4, TRPC5, TRPC6); demonstrates the ability to inhibit TRPV4-mediated pulmonary edema in an in vivo rat model.

GSK3527497 (GSK-3527497) is a potent, selective TRPV4 inhibitor with IC50 of 12 nM (hTRPV4).GSK3527497 is a pre-clinical candidate for treatment of diseases resulting from TRPV4 activation.

SG094 is a potent TPC2 inhibitor with antiproliferative effects. SG-094 can be used for the research of cancer.

(+)-Bicuculline is a competitive antagonist of GABAA receptors with IC50 of 2 μM, also blocks Ca(2+)-activated potassium channels.

(-)-MK 801 Maleate is the enantiomer of (+)-MK-801; (+)-MK-801 is a highly potent and selective non-competitive NMDA glutamate receptor antagonist .

GAT1508 (GAT-1508) is a potent, specific activator for brain-expressed GIRK1/2 channels (EC50=75 nM), specifically activates the brain GIRK1/2 over the cardiac GIRK1/4; GAT1508 is an allosteric modulator of channel–phosphatidylinositol 4,5-bisphosphate interactions. GAT1508 effectively extinguished conditioned fear in rodents and lacked cardiac and behavioral side effects, suggesting its potential for use in pharmacotherapy for post-traumatic stress disorder.

TRPC6-PAM-C20 is a selective TRPC6 positive allosteric modulator. TRPC6-PAM-C20 selectively activates TRPC6 over other TRP channels and also activates TRPA1. TRPC6-PAM-C20 induces transient increase in intracellular Ca2+ in HEK cells expressing TRPC6 (EC50=2.37 μM).

ML213 is a novel potent, selective KCNQ2 (Kv7.2) and KCNQ4 (Kv7.4) activator with EC50 of 230 and 510 nM, respectively. ML213 displays >80-fold selectivity over other related potassium channels (KCNQ1/3/5). ML213 causes significant hyperpolarization in mesenteric artery smooth muscle cells, shows potent vasorelaxant effects in different blood vessels.

FM04 is a potent P-glycoprotein (P-gp) inhibitor (EC50=83 nM). FM04 inhibits P-gp in 2 mechanism: (1)FM04 binds to Q1193, followed by interacting with the functionally critical residues H1195 and T1226; or (2)FM04 binds to I1115 (a functionally critical residue itself), disrupting the R262-Q1081-Q1118 interaction pocket and uncoupling ICL2-NBD2 interaction and thereby inhibiting P-gp.

ORM‐11372 is a potent and highly selective NCX 1.1 inhibitor, inhibits human NCX 1.1 reverse and forward currents with IC50 of 5 and 6 nM respectively.ORM‐11372 weakly inhibits human cardiac sodium 1.5 (I Na) and hERG KV11.1 currents (I hERG) with IC50 of 23.2 and 10.0 uM.ORM‐11372 decreased both the outward and inward currents of hiPSC‐CMs with IC50 of 4.8 and 5.6 nM respectively, reduced the magnitude of outward I NCX (the reverse mode) in rat primary ventricular CMs with IC50 of 11.3 nM.ORM‐11372 concentration‐dependently inhibited the calcium efflux signa with an IC50 of 142 and 164 nM for experimental conditions increasing intracellular calcium and eliciting NCX forward mode activity, repectively.ORM‐11372 induced positive inotropic effects of 18 ± 6% and 35 ± 8% in anaesthetized rats with myocardial infarctions and in healthy rabbits respectively with no other haemodynamic effects.

AM-0466 is a potent and selective NaV1.7 Inhibitor (Nav 1.7 IC50 = 21 nM; Nav 1.5 IC50 =>30.0 uM. PXR = 22% @10 uM; CYP 2C9 IC50 = 4.6 uM; CYP3A4 TDI IC50 =>50.0 uM.).

UR-MB108 (Compound 57) is a potent, selective ABCG2 (BCRP) inhibitor with an IC50 of 79 nM. UR-MB108 is stable in blood plasma.

Tenapanor is an inhibitor of the Na+/H+ exchanger NHE3 with IC50 values of 5 and 10 nM against human and Rat NHE3, respectively.

Enavogliflozin (DWP-16001), an antidiabetic agent, is an orally active, best-in-class and selective sodium-glucose cotransporter-2 (SGLT-2) inhibitor.

AnCoA4 (AnCoA-4, AnCoA 4) is a potent Orai1 channel inhibitor that inhibits store-operated calcium (SOC) with EC50 of 0.88 uM.