FOY 251 is a metabolite of Camostat and a pollen protease inhibitor for prevention and control of allergy.

Gemcitabine elaidate is a lipophilic, unsaturated fatty acid ester derivative of gemcitabine (dFdC), an antimetabolite deoxynucleoside analogue, with potential antineoplastic activity.

BIA is a potential TMBIM6 antagonist, prevents TMBIM6 binding to mTORC2, decreases mTORC2 activity, and also regulates TMBIM6-leaky Ca2+, further suppressing tumor formation and progression in cancer xenograft models.It is a potential anticancer agent that prevents the binding between mTORC2 and TMBIM6.

N-Methyl-N,N-bis(2-pyridylethyl)amine is used as a reagent in the preparation of copper pyridylmethylethylenediamine dicyanamido polymeric complexes.

TGR-1202 is an orally available, next generation PI3Kdelta inhibitor, inhibits PI3Kδ activity in enzyme and cell based assays with IC50 and EC50 values of 22.2 and 24.3 nM respectively.

ZT-12-037-01 is a potent, selective, ATP-competitive STK19 inhibitor with IC50 of 20.04 nM measured as percentage of NRAS phosphorylation; shows similar IC50 of 23.96 and 27.94 nM for STK19WTWT STK19D89N respectively; displays extremely high kinase selectivity using KINOMEscan against a panel of 468 diverse kinases using an in vitro ATP-site competition binding assay at 1 uM; efficiently inhibits phosphorylation of NRAS in a dose- and time-dependent manner, inhibits NRAS activity in a dose-dependent manner but does not affect the levels of H3K9 methylation; effectively inhibits NRAS signaling, including the MEK-ERK and PI3K pathways in SK-MEL-2 and WM2032 cells (with NRASQ61R), but the inhibition was much less effective in A375 or UACC62 cells (with NRASWT), effectively inhibits cell growth and induces apoptosis of SK-MEL-2 and WM2032 melanoma cells.

ALZ-801 is a potent and orally available small-molecule β-amyloid (Aβ) anti-oligomer and aggregation inhibitor, valine-conjugated prodrug of Tramiprosate with substantially improved PK properties and gastrointestinal tolerability compared with the parent compound. ALZ-801 is an advanced and markedly improved candidate for the treatment of alzheimer’s disease.

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

Asciminib (ABL-001) is a potent and selective allosteric ABL1 inhibitor with IC50 of 0.25 nM in BCR–ABL1-transformed BaF3 cells.

RCGD423 is a gp130 modulator, which prevents articular cartilage degeneration and promotes repair.

A small molecule inhibitor of trans-translation that has broad-spectrum antibiotic activity.

CX546 is an AMPA receptor potentiator and GluR activator, binds specifically to the agonist bound non-desensitized receptor.

TH-257 (TH257) is a potent, selective, allosteric inhibitor of LIMK1 and LIMK2 with IC50 of 84 nM for LIMK1 and 39 nM for LIMK2 in a RapidFire MS assay.

AZD-7325 is a potent, α2/3 functionally selective, partial GABAA receptor modulator with pKi of 9.51.

BTZ043 racemate is a decaprenylphosphoryl-β-D-ribose 2-epimerase (DprE1) inhibitor acting as a new antimycobacterial agent that kill Mycobacterium tuberculosis.

CCT007093 is a potent PPM1D (WIP1) inhibitor with IC50 of 8.4 μM.

WHI-P97 is a rationally designed potent inhibitor of JAK-3.

A highly potent sigma receptor agonist with Ki of 1.7 nM and 25.2 nM for σ1 and σ2, respectively.

CID 1375606 is a surrogate agonist of orphan G protein-coupled receptor GPR27.

AKOS B018304 is an arylalkylidene derivative, with polar substitution at para-position.

URB937 is a potent fatty acid amide hydrolase (FAAH) inhibitor (IC50 = 26.8 nM, in vitro) that does not penetrate the blood-brain barrier, thus preventing arachidonoyl ethanolamidedeactivation only in peripheral tissues.

GNE-8324 is a potent and selective NMDA receptor PAM.

VU 0465350 is a potent, specific BMP receptor activin receptor-like kinase 3 (ALK3) antaognist with Ki of 92.3 nM; shows no activity for ALK2/4/5, also shows affinity for TGFBR2, VEGFR2 and AMPK; blocks SMAD phosphorylation in vitro and in vivo, and enhances liver regeneration after partial hepatectomy.

MI-2-2 is a potent inhibitor of the menin-MLL interaction that binds to menin with low nanomolar affinity (Kd=22 nM); inhibits the interaction of menin with MLL-AF9 in HEK293 cells in a dose-dependent manner with 4-fold potentcy improvement over MI-2; suppresses growth of MLL-AF9–transformed BMCs; causes MV4:11 cells growth inhibition of with GI50 of 3 uM.

Iguratimod is one of a series of 4H-1-benzopyran-4-ones which has potent anti-inflammatory, analgesic and antipyretic activity.

Israpafant (Y24180) is a specific antagonist of PAF receptor that inhibits PAF-induced rabbit platelet aggregation in vitro (IC50=3.84 nM), with little effect on adenosine diphosphate- or arachidonic acid-induced aggregation.

ML-9 is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity. ML-9 inhibits inhibits MLCK, PKA and PKC activity with Ki values of 4, 32 and 54 μM, respectively. ML-9 induces autophagy by stimulating autophagosome formation and inhibiting their degradation.

HJC0197 is a potent Epac1 (exchange protein directly activated by cAMP 1) and Epac2 (IC50=5.9 μM for Epac2) antagonist. HJC0197 selectively blocks cAMP-induced Epac activation. HJC0197 inhibits Epac1-mediated Rap1-GDP exchange activity at 25 μM in the presence of equal concentration of cAMP.

AT-007 is an orally active central nervous system (CNS) penetrant Aldose Reductase inhibitor for treatment of Galactosemia with an IC50 value of 100 pM. AT-007 reduces toxic galactitol levels and prevents disease complications in GALT deficiency rats.

UBCS039 is the first synthetic, specific Sirtuin 6 (SIRT6) activator, inducing autophagy in human tumor cells, with an EC50 of 38 μM.