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.

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.

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

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.

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.

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.

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

Yhhu-3792 is a novel small molecule that enhances the self-renewal capability of neural stem cells (NSCs) in vitro and in vivo via activating the Notch signaling pathway.

UU-T02 is a novel potent, selective small-molecule inhibitor of β-catenin/Tcf4 interaction with Ki of 1.36 uM.

Prodigiosin is a natural red pigment produced by numerous bacterial species, has exhibited promising anticancer activity.

BI 1467335 (PXS-4728A, PXS-4728) is a potent, selective, orally active SSAO/VAP-1 (AOC3) inhibitor with IC50 of 5 nM; displays >500-fold selective for VAP-1/SSAO over all the related human amine oxidases; diminishes leukocyte rolling and adherence induced by CXCL1/KC, also inhibits the migration of neutrophils to the lungs in response to LPS, Klebsiella pneumoniae lung infection and CLP induced sepsis.

Cetrorelix acetate is a synthetic decapeptide with gonadotropin-releasing hormone (GnRH) antagonistic activity used in infertility treatment.

Aviptadil (INN) is an analog of vasoactive intestinal polypeptide (VIP) for the treatment of erectile dysfunction,showed potent activity against COVID-19(SARS-COV-2).

TLX agonist 1 (ccrp2) is an orphan nuclear receptor tailless (TLX, NR2E1) modulator (EC50=1μM; Kd= 650 nM). TLX agonist 1 potentiates TLX transcriptional repressive activity.

4-IPP (4-Iodo-6-phenylpyrimidine) is a specific suicide substrate and irreversible inhibitor of macrophage migration inhibitory factor (MIF).

Omadacycline is novel, aminomethyl tetracycline antibiotic being developed for the treatment of community-acquired bacterial infections.

ML406 is a small molecule Mtb bioA (DAPA synthase) enzyme inhibitor (IC50=30 nM) that shows anti-tubercular activity, dispalys >100-fold selectivity over bioD.

NS5806 is a potent potassium current activator, increases KV4.3/KChIP2 peak current amplitudes with an EC50 of 5.3 μM. NS5806 slows KV4.3 and KV4.2 current dacay in channel complexes containing KChIP2[1].