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.

Triptorelin is a synthetic decapeptide agonist analog of luteinizing hormone releasing hormone (LHRH), shows greater potency than endogenous LHRH, triptorelin reversibly represses gonadotropin secretion..

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].

A potent, selective and orally active blocker of voltage-gated potassium channels Kv7 (KCNQ) that blocks KCNQ1, KCNQ2 and KCNQ2+KCNQ3 with Kd of 0.78, 0.7 and 0.6 uM, respectively.

BLT-1 is an irreversible Scavenger receptor class B member I (SR-BI) inhibitor that blocks SR-BI-mediated selective lipid uptake and bidirectional cholesterol flux with an IC50 of 50 nM; significantly inhibits baicalin-induced cholesterol efflux in THP-1 macrophages.

TH1020 is a novel Toll-Like Receptor 5 (TLR5)/Flagellin Complex Inhibitor with promising activity (IC50 =0.85±0.12?μm) and specificity. TH1020 was shown to repress the expression of downstream TNF-α signaling pathways mediated by the TLR5/flagellin complex formation. Based on molecular docking simulation, TH1020 is suggested to compete with flagellin and disrupt its association with TLR5. TH1020 provides a much-needed molecular probe for studying this important protein-protein interaction and a lead compound for identifying novel therapeutics targeting TLR5.

Amlexanox, also known as AA-673 and CHX 3673, is an anti-inflammatory antiallergic immunomodulator used to treat recurrent aphthous ulcers (canker sores), and (in Japan) several inflammatory conditions. Amlexanox inhibits the synthesis and release of inflammatory mediators, including leukotrienes and histamine, from mast cells, neutrophils, and mononuclear cells. Amlexanox also acts as a leukotriene D4 antagonist and a phosphodiesterase inhibitor. Amlexanox decreases the time ulcers take to heal as well as the pain associated with the ulcers.

ETC-206 (ETC-1907206) is a novel potent, selective MNK1/2 inhibitor with IC50 of 64/86 nM, inhibits eIF4E phosphorylation inhibition in HeLa cell line with IC50 of 321 nM.

Nitazoxanide is a synthetic nitrothiazolyl-salicylamide derivative and an antiprotozoal agent. (IC50 for canine influenza virus ranges from 0.17 to 0.21 μM).

Centhaquine (Centhaquin; PMZ-2010) is a novel agent has the potential for treatment of  haemorrhagic shock. Centhaquine (Centhaquin; PMZ-2010) can augment cardiac output, reduce systemic vascular resistance in haemorrhagic models.

Abexinostat (CRA 024781) is a novel pan-HDAC inhibitor mostly targeting HDAC1 with Ki of 7 nM.

FLT3-IN-1(SKLB4771) is a novel potent and selective Flt3 inhibitor with IC50 of 10 nM; against FLT3-ITD-expressing MV4-11 cells with IC50 of 6 nM.

VLX600 is a cell-permeable anticancer agent. It acts by reducing mitochondrial oxidative phosphorylation in tumor cells.

LY-3381916, also known as IDO1-IN-5, is a potent, selective and brain penetrated DO1 inhibitor. LY3381916 specifically targets and binds to IDO1, a cytosolic enzyme responsible for the oxidation of the amino acid tryptophan into the immunosuppressive metabolite kynurenine. By inhibiting IDO1 and decreasing kynurenine in tumor cells, LY3381916 restores and promotes the proliferation and activation of various immune cells, including dendritic cells (DCs), natural killer (NK) cells, and T lymphocytes, and causes a reduction in tumor-associated regulatory T cells (Tregs).

CADD522 is a potent inhibitor of runt-related transcription factor-2 (RUNX2)-DNA binding with an IC50 of 10 nM. CADD522 treatment resulted in significant growth inhibition, clonogenic survival, tumorsphere formation, and invasion of breast cancer cells. CADD522 negatively regulated transcription of RUNX2 target genes such as matrix metalloproteinase-13, vascular endothelial growth factor and glucose transporter-1, but upregulated RUNX2 expression by increasing RUNX2 stability. CADD522 reduced RUNX2-mediated increases in glucose uptake and decreased the level of CBF-β and RUNX2 phosphorylation at the S451 residue.

Torezolid (TR-701; tedizolid) is a novel oxazolidinone for gram-positive infections.