A potent inwardly rectifying K+ channel Kir7.1 inhibitor with IC50 of 5.6 uM in T1+ flux assays.

BL-1249 is a nonsteroidal anti-inflammatory drug (NSAID) and a potassium channel activator. BL-1249 exhibits more selective for the bladder (EC50 of 1.26 μM) than vascular tissue (EC50 of 21.0 μM). BL-1249 extracellular application activates all TREK subfamily members but has no effect on other K2P subfamilies. BL-1249 potently activates K2P2.1 (TREK-1) and K2P10.1 (TREK-2) with EC50 values of 5.5 μM and 8.0 μM, respectively

A potent Kir7.1 inhibitor with IC50 of 2.0 uM, induces long-lasting uterine contractility similar to those observed with VU590..

A potent, highly selective glycine transporter 1 (GlyT2) inhibitor with IC50 of 16 nM with negligible affinity for GlyT1..

A potent, selective CRAC channel Orai1 blocker with IC50 of 3 uM.

A potent, selective glycine transporter 1 (GlyT1) inhibitor with IC50 of 100 nM.

A potent, selective inhibitor of the Na+/citrate transporter NaCT (SLC13A5) that shows inhibition of citrate uptake in the HEKNaCT cells with IC50 of 0.41 uM.

CLP257 (CLP-257) is a potent, selective K+-Cl- cotransporter KCC2 activator with EC50 of 616 nM; displays selectivity for KCC2 over other KCC family members, NKCC1 and GABAA receptors, and a panel of 55 other receptors; restores impaired Cl(-) transport i

A potent, selective renal outer medullary potassium channel (ROMK, Kir1.1) inhibitor with IC50 of 0.24 uM in T1+ flux assays.

A potent, selective, and oral renal outer medullary potassium channel (ROMK) inhibitor with IC50 of 68 nM.

A selective renal outer medullary potassium channel (ROMK, Kir1.1) inhibitor with IC50 of 8 uM in T1+ flux assays, does not inhibit Kir7.1 at 100 uM.

A selective, potent peptidyl blocker of the big conductance Ca2+-activated K+ channel (BKCa, KCa1.1, MaxiK) with IC50 of 0.25 nM.

A selective, potent peptidyl blocker of the big conductance Ca2+-activated K+ channel (BKCa, KCa1.1, MaxiK).

A small molecule corrector of ΔF508-CFTR with IC50 of 6.0 uM..

A small molecule positive allosteric modulator of both proton and vanilloid activation of TRPV1 (EC50=21.3 uM).

A-1048400(A 1048400) is a novel potent, selective, orally active N-type and T-type calcium channel blocker with IC50 of 1.4 and 1.2 uM, respectively.

A-317567 (A317567) is a novel potent acid sensing ion channel (ASIC) blocker with IC50 of 2-30 uM.

A-740003 is potent, selective and competitive P2X7 receptor antagonist (IC50 values are 18 and 40 nM for rat and human receptors respectively).

A-803467 is a selective NaV1.8 channel blocker with IC50 of 8 nM.

A-804598 is a novel, competitive, and selective P2X7 receptor antagonist with IC50 of 10 nM, 9 nM and 11 nM in rat, mouse and human P2X7 receptors respectively.

A-867744 is a positive allosteric modulator of α7 nAChRs (IC50 values are 0.98 and 1.12 μM for human and rat α7 receptor ACh-evoked currents respectively, in X.

ABT-639 is a novel, peripherally acting, selective T-type Ca2+ channel blocker. ABT-639 blocks recombinant human T-type (Cav3.2) Ca2+ channels in a voltage-dependent fashion (IC50 = 2 μM) and attenuates LVA currents in rat DRG neurons (IC50 = 8 μM).