Membrane Transporter/Ion Channel

(S)-6-Methylnicotine is a nicotinic acetylcholine receptor ( nAChR ) agonist that exhibits agonistic activity on isolated guinea pig ileum.

Hydrohydrastinine is a selective α4β2 nicotinic acetylcholine receptor antagonist with an IC 50 of 2.6 μM and a K i of 17 μM.

nAChR antagonist 3 is a selective α7 nAChR antagonist with an IC 50 of 0.86 μM.

RGH-857 is an orally active, selective, potent nicotinic α7 positive allosteric modulator.

Spinosyn L is a selective nicotinic acetylcholine receptors ( nAChR ) agonist.

SKF-96365 is a TRPC channel antagonist and store-operated calcium entry ( SOCE ) inhibitor.

Nav1.2-IN-2 is a Nav1.2 inhibitor with a human IC 50 of 0.18 μM.

CAD204520 dihydrochloride, a SERCA inhibitor ( IC 50 = 0.34 μM), targets mutated over wild type NOTCH1 proteins in T-cell acute lymphoblastic leukemia (T-ALL) and mantle cell lymphoma (MCL).

TRPA1 agonist-3 is a selective and orally active TRPA1 agonist, with EC 50 values of 50.05 μM and 314.04 μM for human and mouse TRPA1, respectively.

Indazapyroxamet is an orally active insect TRPV channel (Nan/Iav subunit) modulator and insecticide.

ADM 12 is a highly selective transient receptor potential ankyrin 1 ( TRPA1 ) channel antagonist.

TRPM3-IN-1 (compound 124) is an inhibitor of TRPM3 with an IC 50 value <1 µM.

AM-0883 is a TRPC6 (Transient receptor potential canonical 6) agonist ( hTRPC6 EC 50 = 46 nM).

AMG-8562 is a selective, orally active transient receptor potential vanilloid 1 ( TRPV1 ) modulator that inhibits the activation of rat TRPV1 by Capsaicin, Anandamide and N-arachidonyldopamine, with IC 50 values of 1.75, 9.29 and 3.87 nM, respectively.

ZA18 is a selective TRPM2 channel inhibitor, with an IC 50 value of 6.2 μM.

TRPC3 agonist-1 (compound 4n) is a selective and competitive TRPC3 channel agonist.

Trpvicin is a potent and subtype-selective TRPV3 inhibitor with IC 50 s of 0.41 and 0.22 μM for hTRPV3-WT and hTRPV3-G573S mutant, respectively.

L-R4W2 acetate is a potent antagonist of vanilloid receptor 1 (VR1, TRPV1 ), with an IC 50 of 0.1 μM.

HKC54 is a selective TRPV2 antagonist with an IC 50 of 0.4 μM.

FP802 is an orally active potent TwinF interface inhibitor that disrupts and detoxifies the NMDAR/TRPM4 death complex.

FP802 dihydrochloride is an orally active potent TwinF interface inhibitor that disrupts and detoxifies the NMDAR/TRPM4 death complex.

PSFL2915 is a selective, orally active P2X receptor inhibitor with oral effectiveness, with an IC 50 of 0.319 μM for human P2X3, 0.261 μM for rat P2X2/3, and 13.3 μM for human P2X2.

PSB-10211 is a P2X2 receptor antagonist with an IC 50 of 0.086 μM against rat P2X2 receptors.

VU6080824 (hydrochloride), a derivative of ML-133, is an inward-rectifier potassium channel (K ir 2.1) inhibitor with an IC 50 of 0.35 μM.