Pyrcoumin is a competitive inhibitor of dCTP pyrophosphatase 1 (dCTPP1, IC50=3.3 uM), inhibits Wnt signaling with IC50 of 8.4 uM in SuperTOPFlash reporter gene assays.

QP5038 is a potent inhibitor of glutaminyl-peptide cyclotransferase-like protein (QPCTL) with IC50 of 3.8 nM, shows promising in vitro and in vivo anti-tumor efficacies.

R805 is a small molecule modulator of gp130 receptor pro-inflammatory signaling, targets a signaling tyrosine 814 (Y814) within gp130, modulates gp130 Y814 upstream of the SRC and MAPK circuit, elicits a protective effect on tissues after injury.

RA 5557 is a brain-penetrant, selective, oral UGT8 inhibitor, inhibits galactosylceramide biosynthesis.

RBS-10 is a small molecule that shows preferential cytotoxicity against cells pan-resistant to degraders, acts as a prodrug bioactivated by the oxidoreductase enzyme NQO1.

RECTAS is a small molecule splice modulator that corrects aberrant splicing of familial dysautonomia (FD), promotes exon 20 inclusion of IKBKAP pre-mRNA and expression of IKAP.

RF03176 is a selective AQP9 inhibitor with IC50 of 1.3 uM (inhibition of CHO-AQP9 cell water permeability).

RG100204 is a novel selective, small molecule inhibitor of the neutral solute channel Aquaporin 9 (AQP9), inhibits AQP9 water permeability (IC50=110 nM) and AQP9 glycerol permeability (IC50=76 nM).

Ro 48-8071 is a potent 2,3-oxidosqualene cyclase (OSC) inhibitor with IC50 of 6.5 nM.

RPE65-61 ((±)-RPE65-61) is a selective, non-retinoid and uncompetitive inhibitor of RPE65 (a key enzyme in the visual cycle), inhibits the retinol isomerase activity of RPE65 in vitro with IC50 of 80 nM.

RPI-194 is a novel troponin activator that binds to cardiac/slow skeletal muscle troponin, binds to cardiac troponin with KD of 24 uM, stabilizing the activated complex between troponin C and the switch region of troponin I.

RTI-263 (SerPheLysAsn-NH2) is a potent, selective tetrapeptide neuropeptide S receptor (NPSR, GPR154) biased agonist with EC50 of 3.02 nM for hNPSR calcium mobilization.

RU-NT-206 is a small molecule inhibitor targeting the P-stalk binding pocket of ricin toxin A subunit (RTA) with IC50 of 7 uM, inhibits catalytic activity and protects cells against ricin and Stx2 holotoxins.

RX-105 (RX105) is a small molecule inhibitor of protein interaction with glycosaminoglycans (SMIGs) with anti-inflammatory properties, binds directly to glycosaminoglycans (GAGs).

RX-207 (RX207) is a small molecule inhibitor of protein binding to glycosaminoglycans (SMIGs), inhibits protein binding to glycosaminoglycans (GAGs), inhibits inflammatory neutrophil adhesion and activity in vitro and in vivo.

S-181 (S 181) is a specific small-molecule activator (modulator) of β-glucocerebrosidase (GCase) with AC50 of 1.49 uM and a maximum activation of 780%.

S202 is a potent, selective and brain-penetrant small molecule inhibitor of ceramide galactosyltransferase (CGT) with IC50 of 15 nM in the cell-lysate assays and 3.6 nM in intact-cell assays.

S9-A13 is a highly potent and specific inhibitor of SLC26A9, potently inhibits SLC26A9-mediated Cl−/I− and Cl−/SCN− exchange activities with IC50 of 90.9 and 171.5 nM, respectively.S9-A13 does not inhibit other members of the SLC26 family and has no effects on Cl− channels such as CFTR, TMEM16A, or VRAC.S9-A13 (0-1 uM ) inhibits SLC26A9 currents in a dose-dependent manner in HEK293 cells, but shows little effects on CFTR currents in HEK293 cells at the highest concentration (5 uM).S9-A13 has a minor effect on ion transport in human airway epithelial cells and mouse trachea, despite clear expression of SLC26A9 in the apical membrane of ciliated cells.

SACLAC is an α-chloroamide ceramide analog that binds irreversibly to acid ceramidase (ASAH1), significantly reduces the viability of AML cells (EC50=3 uM) across 30 human AML cell lines.

SAN4825 is a selective small-molecule inhibitor of cardiac ADP-ribosyl cyclase (ADPR cyclase) with IC50 of 0.13 uM.

SAR439883 (SAR 439883) is a novel potent, selective, orally active PKR inhibitor with IC50 of 0.68/0.69 uM against hPKR/mPKR, respectively.

SB1501 (SB 1501) is a bioactive compound that reduces fat accumulation by elevating mitochondrial biogenesis and fatty acid oxidation via the PGC-1α-UCP1 pathway, shows anti-obesity effects in vivo.