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.

CDKI-73 is a potent CDK9 inhibitor with Ki of 4 nM, shows cytotoxicity against a broad CLL samples with mean LD50 of 80 nM.

Pyr10 is a pyrazole derivative and a selective TRP cation 3 (TRPC3) inhibitor. Pyr10 inhibits Ca2+ influx in carbachol-stimulated TRPC3-transfected HEK293 cells with an IC50 of 0.72 μM (IC50 of 13.08 μM for store operated Ca2+ entry in BRL-2H3 cells). Pyr10 has the ability to distinguish between receptor-operated TRPC3 and native stromal interaction molecule 1 (STIM1)/Orai1 channels[1].

S29434 (S 29434) is a highly potent, selective, cell-active inhibitor of Quinone reductase 2 (QR2) with IC50 of 5-16 nM, shows good selectivity for QR2 over QR1.

FTBMT is a novel selective GPR52 agonist of GPR52, increases intracellular cAMP levels in CHO cells expressing human, mouse, or rat GPR52, with pEC50 of 7.03, 6.85, and 6.87M, respectively.

N-Succinimidyl S-acetylthioacetate (SATA), a protein modification agent, introduces thiol-groups into protein molecules. N-Succinimidyl S-acetylthioacetate adds sulfhydryl groups to proteins and other amine-containing molecules in a protected form.

MCP110 is a potent Ras/Raf-1 interaction inhibitor.

TCN-201 is a selective antagonist of NMDA receptors containing the NR2A subunit. TCN 201 selectively blocks GluN2A-containing NMDARs in a GluN1 co-agonist dependent but non-competitive manner.

AMG-Tie2-1 is a highly potent, non-selective inhibitor of Tie-2 (IC50 <1 nM).

AZD-26 is an inhibitor of AKT. AZD-26 inhibits the phosphorylation of Thr308 on AKT in BT474 cells with an IC50 of 422 nM.

Bayer-18 is a selective TYK2 inhibitor, with an IC50 of 18.7nM on TYK2 as measured by TYK2 HTRF assays.

BGG463 can inhibit c-ABL-T334I, BCR-ABL and BCR-ABL-T315I variants with a 50% inhibitory concentration (IC50) of 0.25 μM, 0.09 μM and 0.590 μM, respectively.

BIX 02565 is a novel ribosomal S6 kinase 2 (RSK2) inhibitor with an IC50 of 1.1 nM.

CFI-400437 is potent against PLK4 (IC50 = 0.6 nM) and selective against other members of the PLK family (>10 uM).

Mubritinib is a potent inhibitor of the human epidermal growth factor receptor 2 (HER2) tyrosine kinase.

SD169 is an orally available, ATP-competitive, isoenzyme-selective Mitogen-Activated Protein Kinase (MAPK) inhibitor.

RET-IN-1 is a RET kinase inhibitor extracted from patent WO2018071447A1, Compound Example 552, has IC50s of 1 nM, 7 nM, and 101 nM for RET (WT), RET (V804M) , and RET (G810R), respectively .

A potent PIKfyve inhibitor that inhibits autophagy by impairing lysosomal maturation, potently and reversibly inhibits autophagosome-lysosome fusion by activating RAB5A.