Cyclo(L-Pro-L-Val) is a diketopiperazine that has been found in the marine sponge T. ignis, the bacterium B. pumilus, and the fungus A. fumigatus, among others.

MX1013 is a dipeptide pan-caspase inhibitor that inhibits caspase-1

YW1128 is an inhibitor of Wnt/β-catenin signaling with an IC50 value of 4.1 nM in a reporter assay.

Suc-YVAD-pNA is a colorimetric substrate for caspase-1/interleukin-1β-converting enzyme (ICE) and caspase-4.

Ecabet is an antiulcerative and gastroprotective agent.

Z-Phe-Tyr(tBu)-diazomethylketone is an inhibitor of cathepsin L

Questiomycin A is a phenoxazine and a chromophore that has been found in Streptomyces and has antibacterial and anticancer activities.

STING agonist C11 is an agonist of the stimulator of interferon genes (STING) pathway.

YW1159 is an inhibitor of Wnt signaling with an IC50 value of 1.2 nM in a reporter assay.

AT-127 is a novel potent, selective nociceptin/orphanin FQ receptor (NOP receptor) agonist with Ki of 1.18 nM.

BAY 61-3606 is a potent, ATP-competitive, reversible, and highly selective inhibitor of Syk tyrosine kinase with Ki of 7.5 nM, displays no inhibitory effect against Btk, Fyn, Itk, Lyn, and Src.

A highly potent, subtype-selective melanin concentrating hormone receptor 1 (MCHR1) inhibitor with Ki of 17 nM, without inhibitory activity for MCHR2 at 10 uM.

The first small molecule ligand for the VEGF-A receptor neuropilin 1 (NRP1).

GNE-616 (GNE616) is a highly potent, metabolically stable, subtype selective inhibitor of Nav1.7 with Ki of 0.79 nM (hNav1.7).

A potent, specific, orally active melanin concentrating hormone receptor 1 (MCHR1) inhibitor with kI of 3.8 nM, >100-fold selectivity over a battery of GPCRs, ion channels and enzymes.

GX-674 is a potent, selective Nav1.7 inhibitor with IC50 of 0.1 nM.

JTE-852 is a novel potent, selective, ATP-competitive Syk kinase inhibitor with IC50 of 1.25/1.28 nM for human/rat Syk, respectively.

PF-05198007 is a potent, state-dependent, subtype selective Nav1.7 inhibitor with IC50 of 9 nM, no significant activity against Nav1.5 (IC50>10 uM).

SR-14150 is a potent NOP/μ-opioid partial agonist with Ki of 1.39 nM and 29.9 nM, respectively.

SR-16507 is a potent full agonist of ORL1 receptor (NOP receptor) and partial agonist of mu-opioid receptor with Ki of 5.22 nM and 1.07 nM, respectively.

MCL0129 is a selective, potent melanocortin-4 receptor (MC4R) antagonist with Ki of 7.9 nM, without affinity for MC1 and MC3.

LSP4–2022 is a novel potent, selective, brain-penetrant mGluR4 agonist with EC50 of 0.11 uM in cell-based assays.