VU 0238429 is positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5), with an EC50 of 1.16 μM.

A potent, orally-active MEK1/2 inhibitor with IC50 of 10-100 nM.

A potent glutaminyl cyclase (QC) inhibitor with Ki of 60 nM.

A novel potent, irreversible Myeloperoxidase (MPO) inhibitor with IC50 of 44 nM.

A potent, selective and competitive NK1 receptor antagonist with IC50 of 2.3 nM.

QStatin is a novel, potent, and selective Vibrio quorum sensing (QS) inhibitor, shows pan-QS inhibitor activity in diverse Vibrio species.

HA14-1 is a nonpeptidic ligand of a Bcl-2 surface pocket with IC50 of~9 μM.

BTZO-1 is a cardioprotective agent and Macrophage migration inhibitory factor (MIF) activator, binds to MIF with Kd of 68.6 nM, regulates ARE-mediated gene expression.

A potent and selective inhibitor of PDGFR with IC50 of about 0.4 uM both in vitro and in cells.

Cavosonstat is a potent, orally bioavailable inhibitor of S-nitrosoglutathione reductase (GSNOR) and CFTR modulator.

Mca-PL is a fluorogenic peptide that has been used as a building block in the synthesis of Mca-PLGL-Dpa-AR-NH2, a fluorogenic substrate for matrix metalloproteinase-2 (MMP-2) and MMP-7.

Tegobuvir (GS-9190; GS 333126) is a non-nucleoside nonstructural protein (NS)5B polymerase inhibitor.

4E2RCat is an inhibitor of eIF4E-eIF4G interaction with an IC50 of 13.5 μM.

HSP70-IN-1 is a heat shock protein (HSP) inhibitor; inhibits the growth of Kasumi-1 cells with an IC50 of 2.3 μM.

A potent, functionally selective TSH receptor (TSHR) positive allosteric modulator with EC50 of 11.6 uM (β-Arr 1 translocation).

HMN-214(IVX214) is a potent PLK1 inhibitor an average IC50 of 0.12 μM.

Vatalanib (PTK787) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM, less potent against VEGFR1/Flt-1, 18-fold against VEGFR3/Flt-4. Phase 1/2.

ARA-290 (Cibinetide) is a non-erythropoietic erythropoietin (EPO) derivative.

SC-236 (SC58236) is a potent, selective, orally active inhibitor of COX-2 with IC50 of 10 nM.

AA26-9 is a potent and broad spectrum serine hydrolase inhibitor.

AEE788 is a potent inhibitor of EGFR and HER2/ErbB2 with IC50 of 2 nM and 6 nM, less potent to VEGFR2/KDR, c-Abl, c-Src, and Flt-1, does not inhibit Ins-R, IGF-1R, PKCα and CDK1. Phase 1/2.

A first-in-class analogue of unacylated ghrelin, and unacylated ghrelin receptor agonist.

Filastatin is a long-lasting inhibitor of Candida albicans filamentation. Filastatin inhibits adhesion by multiple pathogenic Candida species with an IC50 of ~3 μM in the GFP-based adhesion assay. Filastatin inhibits fungal adhesion to polystyrene and human cells, the yeast-to-hyphal morphological transition, induction of the hyphal-specific HWP1 promoter. Filastatin has potent antifungal effect.

A cytotoxic agent used in antibody-drug conjugates

TAK-981 is a first in class and selective inhibitor of the SUMOylation enzymatic cascade, with potential immune-activating and antineoplastic activities[1].

SB-633825 is a potent and ATP-competitive inhibitor of TIE2, LOK (STK10) and BRK with IC50s of 3.5 nM, 66 nM, 150 nM, respectively. SB-633825 can inhibit cancer cell growth and angiogenesis.

LR-90 is an advanced glycation end product (AGE) inhibitor, inhibits inflammatory responses in human monocytes. LR-90 is also used in the research of diabetic animal model.

RP-64477 is a potent inhibitor of the cholesterol esterifying enzyme Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT).

A potent inhibitor of MLL1/WDR5 protein-protein interaction with IC50 of 0.9 nM.

Velneperit, also known as S-2367, is potent and selective neuropeptide Y Y5-receptor antagonist under evaluating for treatment of obesity.