GSK3987 functions as a dual agonist for both LXRα and LXRβ nuclear receptors, demonstrating potent activation with EC50 values of 50 nM (LXRα-SRC1) and 40 nM (LXRβ-SRC1). This compound effectively upregulates key metabolic regulators ABCA1 and SREBP-1c, while simultaneously promoting cholesterol efflux from cells and stimulating intracellular triglyceride deposition.

L82-G17 is a selective, uncompetitive inhibitor that specifically targets DNA ligase I (Lig I). This compound uniquely blocks the final stage of the ligation process by interfering with phosphodiester bond formation. Due to its specific mechanism of action, L82-G17 serves as a valuable molecular probe for studying ligase catalytic activity.

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

SSAA09E3 is a potent viral entry inhibitor that effectively blocks SARS-CoV infection. In cellular assays, it demonstrates inhibitory activity against SARS/HIV pseudotyped viruses in 293T cells (EC50 = 9.7 μM) and shows even greater potency against authentic SARS-CoV in Vero cells (EC50 = 0.15 μM).

STING-IN-2 (C-170) is a covalent-binding small molecule that potently suppresses STING activity. It demonstrates effective inhibition against both murine (mmSTING) and human (hsSTING) variants, making it a valuable tool for investigating autoinflammatory disorders.

PKZ18 is a novel antibiotic that effectively suppresses bacterial growth, exhibiting MIC values ranging from 32 to 64 μg/mL against a broad spectrum of Gram-positive bacteria. Its mechanism involves the selective inhibition of glycyl-tRNA synthetase mRNA transcription and translation in vivo. PKZ18 specifically targets stem I specifier loops in Gram-positive bacteria, disrupting T-box-mediated transcriptional read-through of downstream genes. By interfering with codon-anticodon recognition, it blocks essential tRNA binding and demonstrates a high barrier to resistance development.

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.

Novel mucolipin 1 (ML1) agonist, inducing lysosomal Ca2+ release, ameliorating muscular dystrophies and activating TFEB to correct lysosomal insufficiency in mdx mice

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.

VPC-80051 (VPC80051) is the first small molecule inhibitor of hnRNP A1 splicing activity, targets RNA-binding domain (RBD) of hnRNP A1.

RG7834 (RO 7020322) is a highly selective and orally bioavailable HBV inhibitor, potently inhibits HBV antigens (both HBsAg and HBeAg) and HBV DNA, with IC50s of 2.8, 2.6, and 3.2 nM, respectively, in dHepaRG Cells.

CVT-11127 functions as a potent inhibitor of stearoyl-CoA desaturase (SCD), demonstrating significant biological activity. This compound triggers apoptotic pathways and effectively halts cell cycle progression at the G1/S transition phase. Due to these mechanisms of action, CVT-11127 shows promise as a candidate for lung cancer research.

NS13001 is a highly selective and orally bioavailable allosteric positive modulator targeting small-conductance calcium-activated potassium (SK) channels. It exhibits potent activity, with EC50 values of 1.8 μM for SK2 and 0.14 μM for SK3, demonstrating greater potency toward SK3. Due to its pharmacological profile, NS13001 has emerged as a promising candidate for treating spinocerebellar ataxia type 2 (SCA2) and may also have therapeutic potential in other forms of cerebellar ataxia.

GNE-140 racemate consists of equal parts (R)-GNE-140 and (S)-GNE-140 enantiomers, functioning as a potent inhibitor of lactate dehydrogenase A (LDHA).

AA 41612 is a potent, synthetic melanopsin antagonist with IC50 of 15.8 nM, attenuates melanopsin photocurrent in a dose-dependent manner.

KLH45 is a selective inhibitor of DDHD2 (DDHD domain containing 2).

WWL229 is a selective, distinct Carboxylesterase Ces3 inhibitor with IC50 of 1.94 uM, but not Ces1f, ABHD6, other serine hydrolases.

NCGC00262650 demonstrates potent inhibition of the AMA1-RON2 protein interaction, effectively preventing merozoite invasion of erythrocytes.

BAY-549 (Azaindole 1) is an orally bioavailable, ATP-competitive inhibitor demonstrating potent inhibition of both ROCK isoforms, with IC50 values of 0.6 nM (ROCK-1) and 1.1 nM (ROCK-2) in human enzymes.

ML-226 is an inhibitor of α/β hydrolase domain-containing protein 11 (ABHD11) that inhibits ABHD11 in vitro and in situ.

BMS-986188 functions as a selective positive allosteric modulator for the δ-opioid receptor, demonstrating potent activity with an EC50 of 50 nM.

NCGC607 is a a small-molecule noninhibitory chaperone of glucocerebrosidase.

Metarrestin (ML246) is a specific inhibitor of perinuclear compartment (PNC), disrupts PNCs in PC3M-GFP-PTB cells with IC50 of 0.39 uM, specifically binds eEF1A2.