H3B-120 is a competitive, selective and allosteric inhibitor of carbamoyl phosphate synthetase 1 (CPS1) with IC50 of 1.5 μM and Ki of 1.4 μM. H3B-120 exhibits anti-tumor activity.

KS176 is a potent and selective inhibitor of the breast cancer resistance protein (BCRP) multidrug transporter (IC50 values are 0.59 and 1.39 μM in Pheo A and Hoechst 33342 assays respectively). Displays no inhibitory activity against P-gp or MRP1.

BI 1265162 is a potent ENaC inhibitor, inhibits Na+ transport with IC50 3 nM and 8 nM in M1 and NCI-H441 cells, respectively.BI 1265162 dose-dependently inhibited Na+ transport and decreased water resorption in cell line models.BI 1265162 reduced liquid absorption in rat lungs and increased MCC in sheep, with no effects on renal function in the animal models.BI 1265162 alone and in combination with CF transmembrane conductance regulator (CFTR) modulators decreased water transport and increased MCC in both normal and CF airway human epithelial models.

NV-6297 (NV6297) is a potent, selective mTORC1 pathway signaling inhibitor without inhibition on mTORC2, inhibits S6K1 phosphorylation (pS6K1 T389) in MCF7 cells with IC50 of 120 nM, directly and selectively targets GLUT-1.

LTGO-33 is a potent, selective inhibitor of voltage-gated sodium channel NaV1.8 with IC50 of 44 nM (hNaV1.8), 600-fold selectivity against NaV1.1-NaV1.7 and NaV1.9.

Iclepertin (BI-425809) is a potent, selective and orally active glycine transporter 1 (GlyT1) inhibitor. Iclepertin is inactive against GlyT2. Iclepertin can be used for Alzheimer disease and schizophrenia research.

BAY-876 is the first highly selective GLUT1 inhibitor with IC50 of 0.002 uM. show good metabolic stability in vitro and high oral bioavailability in vivo.

Ancistrotecine B (Compound 2) is a Nav1.7 channel inhibitor (IC50: 0.73 μM). Ancistrotecine B relieves inflammatory pain in mice.

Guvacine hydrobromide, an alkaloid found in the nut of Areca catechu, is a potent GABA uptakp inhibitor. Guvacine hydrobromide inhibits rat GAT-1, rat GAT-2 and rat GAT-3 with IC50 values of 39 μM, 58 μM and 378 μM, respectively.

Arecaidine hydrobromide, a pyridine alkaloid, is a potent GABA uptake inhibitor. Arecaidine hydrobromide is a substrate of H+-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits L-proline uptake.

KC289 is a specific small-molecule agonist of PIEZO1 channel and Yoda1 analogue with EC50 of 150 nM in in calcium assays.

slCeMM1 is a potent, highly selective inhibitor of lactate transporter SLC16A3 (MCT4), inhibits intracellular lactate accumulation in SLC16A3 dependent cells (IC50=91 nM).

VPC01091.4 is a non-phosphorylatable FTY720 analogue and novel TRPM7 inhibitor, inhibits IM7 in a dose-dependent manner with IC50 of 0.665 uM.

Trpvicin is a potent and subtype-selective inhibitor of TRPV3 with IC50 of 0.41 and 0.22 uM for hTRPV3-WT and hTRPV3-G573S mutant, respectively.

Triphenylphosphine oxide (TPPO) is a selective and potent inhibitor of TRPM5 with IC50 of 12 and 30 uM for human and murine TRPM5 heterologously expressed in HEK293 cells.

SAR7334 (SAR-7334 ) is a highly potent and selective inhibitor of TRPC6 channel, reduces TRPC6-mediated Ca2+ influx with IC50 of 9.5 nM.

M085 (TRPC3/6/7 activator 4o) is a potent and selective TRPC3/6/7 activator with EC50 of 4.66 uM, also activates hTRPC6 with EC50 of 3.8 uM.

Libvatrep (SAF312) is a potent, selective non-competitive inhibitor/antagonist of the transient receptor potential cation channel subfamily V member 1 (TRPV1), shows potential for treatment of ocular surface pain.

KS0365 (KS 0365) is a potent and selective activator of transient receptor potential vanilloid 3 (TRPV3) channel with EC50 of 5.08 uM.

JNc-463 is a small-molecule that could increase the TRPV4-eNOS interaction, enhances vasodilation and exert antihypertensive effects in mice.

GDC-6599 is a potent, selective transient receptor potential ankyrin 1 (TRPA1) antagonist with IC50 of 5.3 nM (hTRPA1), exhibits TRPA1 cell potency (IC50=20 nM) in the Ca2+ influx assay in CHO cells.

AZ465 (AZ-465) is a potent selective TRPA1 inhibitor, potently inhibitor Zn2+ (100 μM)- and O-chlorobenzylidene malononitrile (CS) (10 nM)-induced TRPA1 activation with IC50 of 85 nM and 20 nM, respectively.

AMG2504 (AMG 2504) is a selective small molecule TRPA1 inhibitor, inhibits AITC-induced increase in intracellular calcium mediated by TRPA1 in CHO cells with IC50 of 35 nM.

AAL-149 is a non-phosphorylatable FTY720 analogue and novel TRPM7 inhibitor, inhibits IM7 in a dose-dependent manner with IC50 of 1.081 uM, shows potent anti-inflammatory effects in vivo.

XPC-7224 is a potent, selective NaV1.6 inhibitor with IC50 of 78 nM and 130 nM for human and mouse NaV1.6, respectively, interacts with the inactivated state of the channel.

XPC-5462 is a potent, selective dual inhibitor of NaV1.6 and NaV1.2 with IC50 of 10.9 nM and 10.3 nM, respectively.

UTX-143 is a potent, selective sodium-hydrogen exchange subtype 5 (NHE5) inhibitor with IC50 of 3.11 uM, 80-fold selective over NHE1.

BW-031 iodide is a potent cationic sodium channel inhibitor, inhibited Nav 1.7 (IC50=9.5 uM) and Nav 1.1 channels with approximately sixfold greater potency than QX-314.

BW-031 chloride is a potent cationic sodium channel inhibitor, inhibited Nav 1.7 (IC50=9.5 uM) and Nav 1.1 channels with approximately sixfold greater potency than QX-314.

Benzocaine is a local anesthetic.