PSB-KK-1415 is a selective GPR18 agonist with EC50 of 19.1 nM (hGPR18) in β-arrestin recruitment assays, shows no activity against GPR55.

PT91 is a small-molecule GPR27 (SREB1) agonist with pEC50 of 6.15 (human GPR27) in β-arrestin 2 recruitment-based firefly luciferase complementation assay, Emax=100%.

PTI-125 (Simufilam, Sumifilam) is a small molecule targeting scaffolding protein filamin A (FLNA), preferentially binds altered FLNA and restores its native conformation.

PXS-4748 (PXS4748) is a potent, selective and irreversible pan-lysyl oxidase (pan-LOX) inhibitor with IC50 of 2.0 uM and 3.2/0.6/1.4/0.2 uM for bovine (aorta) LOX and rh LOXL1/2/3/4, respectively.

PXS-5129A is the pro-drug form of PXS-5120A, a potent, selective, irreversible inhibitor of Lysyl oxidase-like 2 (LOXL2).

PXS-5505 dihydrochloride monohydrate is an orally available, small-molecule, irreversible inhibitor of all lysyl oxidases (pan-LOX) family members, with potential antifibrotic activity.

PXS-6302 (PXS6302) is a potent, irreversible pan-lysyl oxidase (pan-LOX) inhibitor with IC50 of 3.7 uM and 3.4/0.4/1.5/0.3 uM for bovine (aorta) LOX and rh LOXL1/2/3/4, respectively.

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.