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.

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.

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.

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.

AF64394 is a potent, selective GPR3 inverse agonist with pIC50 of 7.3, displays >100-fold selectivity over GPR6 and GPR12.

RO5203648 is a high-affinity, selective partial agonist of TAAR1 (trace amine-associated receptor 1) that represents an innovative pharmacological approach for investigating neuropsychiatric disorders.

ML311 is a potent and selective inhibitor of the Mcl-1/Bim interaction.

MSBN is a highly selective fluorogenic probe for thiols, selectively imaging thiols in live cells and specifically label protein thiols with a turn-on signal to determine diverse reversible protein thiol modifications.

BRD6688 is a selective HDAC2 inhibitor. It acts by enhancing the learning and memory processes.

Creatine riboside is the strongest classifier of lung cancer status in all and stage I-II cases, important for early detection, and also associated with worse prognosis in stage I-II lung cancer.

NRF2 inhibitor AEM1 is a specific small molecule inhibitor of Nrf2 transcriptional activity in cancer cells, shows no activity against a panel of >100 kinases (including isoforms of PI3K, AKT, and PKC).

JCP174 is an inhibitor of a depalmitoylase that enhances Toxoplasma host-cell invasion by targeting TgPPT1.

PH-064 (also known as BIM-46187) functions as a potent inhibitor targeting the heterotrimeric G-protein signaling complex.

CE3F4 is a potent, noncompetitive EPAC1 inhibitor that blocks EPAC1-induced Rap1 activation both in cell-free systems and in intact cells and did not influence protein kinase A holoenzyme activity.

VPC 23019 is an aryl amide-based S1P receptor modulator that demonstrates receptor subtype selectivity. It functions as a competitive antagonist at S1P1 (pKi=7.86) and S1P3 (pKi=5.93), while acting as an agonist at S1P4 (pEC50=6.58) and S1P5 (pEC50=7.07) receptors.

ML298 demonstrates potent and selective inhibition of phospholipase D2 (PLD2), exhibiting an IC50 of 355 nM while showing minimal activity against PLD1 (IC50 >20 μM), representing >53-fold selectivity.

Atglistatin is a potent and selective inhibitor of adipose triglyceride lipase (ATGL), effectively suppressing lipolysis activity. In vitro studies demonstrate its inhibitory effect with a half-maximal inhibitory concentration (IC50) of 0.7 μM.

The small molecule ML336 demonstrates specific antiviral activity against the TC-83 strain of Venezuelan equine encephalitis virus (VEEV) by functioning as a potent inhibitor.

GSK 2830371 is a selective inhibitor of the WiP1 phosphatase that demonstrates potent antitumor activity in both lymphoma and neuroblastoma preclinical models by suppressing malignant cell proliferation.

5F-203 (NSC-703786) exhibits its anticancer properties through a multimodal mechanism of action. As a DNA-damaging agent, it creates stable adducts while arresting cell cycle progression. The compound's ability to strongly activate AhR signaling results in marked CYP1A1 induction. Additional effects include ROS generation and concurrent activation of multiple stress-responsive kinase pathways (JNK, ERK, and p38), collectively contributing to its cytotoxic profile.

Mps1-IN-3 is a selective and highly potent Mps1 kinase inhibitor with IC50 of 50 nM.

Nisoxetine acts as a highly selective and potent noradrenaline transporter (NET) antagonist, exhibiting a binding affinity (Kd) of 0.76 nM. In addition to its antidepressant properties, nisoxetine functions as a local anesthetic by inhibiting voltage-gated sodium channels. This dual pharmacological activity makes it a compound of interest for both neurological and pain management research.

Kobe0065 is a novel and effective small-molecule compound inhibiting Ras–Raf interaction by SBDD; exhibits potent activity to competitively inhibit the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46 ± 13 μM.