Devazepide is a potent, and orally active CCK1 (CCK-A) receptor antagonist that displays appetite-stimulant effects. It blocks the anorectic response to CCK-8 and increases food intake in rats following systemic and i.c.v administration.

A potent inhibitor of tumor promoting phorbol ester TPA/PMA and inhibitor of Ca2+/calmodulin dependent EF-2 phosphorylation

Amastatin HCl is an aminopeptidase inhibitor that also induces vasoconstriction.

Phenylacetylglutamine is used as biomarker for metabolic age.

ER-464195-01 is a specific, orally active inhibitor that inhibits Calreticulin (CRT) binding to integrin α subunits (ITGAs) with IC50 of 0.17, 0.36, and 0.23 uM in the interaction between CRT and ITGA α4, αL, and αM/α2/α5.

AGF347 (AGF-347) is a small molecule inhibitor targeting mitochondrial C1 metabolism at SHMT2 (in vitro Ki=2.19 uM), also directly targers the purine biosynthetic enzymes GARFTase (Ki=3.13 uM) and AICARFTase (Ki=3.72 uM), and SHMT1 (Ki=2.91 uM).

A small molecule inhibitor of diacylglycerol kinase (DGK) with IC50 of 2.8 uM, inhibits the phosphorylation of OAG to OAPA with IC50 of 3.8 uM in intact platelets.

LBL1 is a first-in-class pyrroloquinazoline small molecule that selectively targets the coiled-coil domain of lamin A (binding affinity Kd = 5.11 μM), demonstrating potent anticancer effects through nuclear lamina disruption.

GNE-049 (GNE049) is a potent, selective, orally available inhibitor of CBP/p300 bromodomain with biochemical IC50 of 1.1/2.3 nM, respectively.

Varoglutamstat (PQ912) is a potent glutaminyl cyclase (QC) inhibitor with Ki values of 20-65 nM for human, rat, and mouse QC activity.

WQ-2101 (WQ2101, PKUMDL-WQ-2101) is a specific, allosteric inhibitor of PHGDH with IC50 of 34.8 uM (WT PHGDH), shows dramatically reduced potenecy for mutants R134A (IC50 =141 uM) and K57AT59A (IC50=128 uM).

ZLD1039 is a novel, orally active EZH2 inhibitor demonstrating high selectivity and potency. It effectively suppresses PRC2 enzymatic activity across wild-type EZH2 (IC50 = 5.6 nM) and mutant forms (Y641F: 15 nM; A677G: 4.0 nM), while exhibiting significant anti-tumor and anti-metastatic effects in breast cancer models.

LY305 is a potent non-steroidal SARM exhibiting high androgen receptor binding affinity (Ki = 2.03 nM) and strong agonist activity in C2C12 cells (EC50 = 0.499 nM), demonstrating its selective modulation capabilities.

NNK is a procarcinogen, a major tobacco-specific toxicant that inhibits the expression of lysyl oxidase, a tumor suppressor.

Tradipitant (VLY-686) is a selective neurokinin-1 (NK-1) receptor antagonist with potential therapeutic applications.

SKI-178 is a potent, specific, non-lipid SphK1 inhibitor with Ki of 1.33 uM, displays no significant activity for SphK2 (IC50>25 uM).

SW-100 (SW100) is a potent, selective, brain penetrable HDAC6 inhibitor with IC50 of 2.3 nM, displays >1,000-fold selectivity over all other class I, II, and IV HDAC isoforms.

Adaphostin is a novel activator of Fas-mediated death pathway in Bcr/Abl-positive leukaemia.

VU-29 (DPAP) is a potent, selective and allosteric potentiator of rat mGlu5 receptor with EC50 of 9 nM, displays >50-fold selectivity over mGlu1 and mGlu2 receptor (EC50=557 nM and 1.51 uM).

AGI-001 is an orally bioavailable, competitive antagonist of 5-HT1A/1B receptors with reversible binding properties. This compound also functions as a partial agonist at β-adrenergic receptors, making it a valuable pharmacological tool for investigating neurological disorders.

LASV inhibitor 3.3 (LAMP1 inhibitor 3.3) is a specific inhibitor of Lassa fever virus (LASV, IC50=1.8 uM), inhibits LASV GP-mediated infection and cross-links to the LASV receptor, LAMP1, in cells; does not inhibits the GP-mediated infection of LCMV, LuJo

HOIPIN-1 (JTP-0819958, HOIP inhibitor-1) is a chemical inhibitor of linear ubiquitin chain assembly complex (LUBAC, IC50=2.8 uM), specifically generates Met1-linked linear ubiquitin chains through the ubiquitin ligase activity in HOIP, and activates the N

UCF-101 is a selective inhibitor of the pro-apoptotic mitochondrial serine protease Omi/HtrA2 involved in the cellular response to thermal and oxidative stress.

JR-AB2-011 is a potent and selective inhibitor of mTORC2 kinase activity. It markedly reduces mTORC2 signaling and IC50 while enhancing apoptotic levels in GBM cells.

NSC 370284 is a small molecule that directly binds to and inhibits STAT3/5, significantly and selectively suppresses the viability of AML cells with high level of TET1 expression both in vitro and in vivo.

DB818 (DB-818, DB 818) is a small molecule inhibitor of HOXA9/DNA interaction through binding as minor groove DNA ligand on the HOXA9 cognate sequence.

SR31527 is a novel allosteric Kinesin-like protein KIFC1 inhibitor that inhibits microtubule-stimulated KIFC1 ATPase activity with IC50 of 6.6 uM, binds directly to KIFC1 with Kd of 25.4 nM.

NPD8733 (NPD-8733) is a small-molecule ligand of valosin-containing protein (VCP)/p97, binds to the D1 domain of VCP/p97.

SC-57461A is a highly potent, orally bioavailable nonpeptide compound that selectively inhibits Leukotriene A4 (LTA4) hydrolase. It demonstrates strong activity with IC50 values of 2.5 nM (human), 3 nM (mouse), and 23 nM (rat) for recombinant LTA4 hydrolase.

Gboxin is a compound that disrupts oxidative phosphorylation, making it a promising therapeutic agent specifically for glioblastoma treatment.