Ginsenoside Rg1 is one of the major active components of ginseng. Ginsenoside Rg1 displays promising effects by reducing cerebral Aβ levels. Ginsenoside Rg1 also reduces NF-κB nuclear translocation.

BDTX-189 is a potent, orally active and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations, includes EGFR/HER2 exon 20 insertion mutants. BDTX-189 shows KDs of 0.2, 0.76, 13 and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. Anticancer activity.

SYP-5 is a novel HIF-1 inhibitor, suppresses tumor cells invasion and angiogenesis.

Nifurtimox is a 5-nitrofuran and is used to treat diseases caused by trypanosomes including Chagas disease and sleeping sickness. It is given by mouth and not by injection. Nifurtimox is now in a Phase II clinical trial for the treatment of pediatric neuroblastoma and medulloblastoma. Nifurtimox decreased cell viability in a concentration-dependent manner. Nifurtimox also suppressed basal and TrkB-mediated Akt phosphorylation, and the cytotoxicity of nifurtimox was attenuated by a tyrosine hydroxylase inhibitor (alpha-methyl-tyrosine). Nifurtimox killed catecholaminergic, but not cholinergic, autonomic neurons in culture. In vivo xenograft models showed inhibition of tumor growth with a histologic decrease in proliferation and increase in apoptosis. These results suggest that nifurtimox induces cell death in neuroblastoma . Therefore, further studies are warranted to develop nifurtimox as a promising new treatment for neuroblastoma.

DS-6930 (DS 6930, DS6930) is a novel potent, selective PPARγ agonist with EC50 of 41 nM, Emax-68%; significantly recruits several cofactors, such as RIP140 and PGC1, in cofactor recruitment assays; demonstrateshigh PPARγ agonist potency with robust plasma glucose reduction, maintains diminished PPARγ-related adverse effects upon toxicological evaluation in vivo, and demonstrated no hepatotoxicity.

8-Hydroxy-efavirenz is the primary metabolite of the antiretroviral drug Efavirenz, stimulates the glycolytic flux in cultured rat astrocytes.

AZD9977 is a first-in-class, potent, selective, mineralocorticoid receptor (MR) modulator with IC50 of 0.37. 0.08 and 0.08 uM for human, mouse and rat MR, respectively.

Daidzin is a potent, selective aldehyde dehydrogenase 2 (ALDH2,IC50 = 80 nM) inhibitor, which has antiallergic anti-oxidant, anti-carcinogenic, antithrombotic,and anti-atherosclerotic activities

Cimicoxib, aslo known as UR-8880, is a non-steroidal anti-inflammatory drug (NSAID) used in veterinary medicine to treat dogs for pain and inflammation associated with osteoarthritis and for the management of pain and inflammation associated with surgery. It acts as a COX-2 inhibitor.

BAR501 is a potent and selective agonist of GPBAR1 with an EC50 of 1 μM.

KL201 a circadian clock modulator, is a isoform-selective cryptochrome 1 (CRY1) stabilizer. KL201 has no stabilizing effect on CRY2. KL201 lengthens the period of circadian rhythms in cells and tissues.

Darusentan is a potent inhibitor of endothelin signaling and function in both large and small arteries.

DASA-58 is a highly specific small molecule PKM2 activator. DASA-58 inhibits LPS-induced Hif-1a and IL-1b, as well as the expression of a range of other Hif-1a-dependent genes.

Dasotraline(SEP-225289) is a triple reuptake inhibitor that blocks dopamine, norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respectively.

Datelliptium chloride is a DNA-intercalating agent derived from ellipticine, with anti-tumor activities.

DC260126, a small-molecule antagonist of GPR40.

Decursin is an anticancer agent, with potential anti-inflammatory activity.

YKL-05-099 is a salt-inducible kinase (SIK) probe; inhibits SIK2 with an IC50 of 40 nM.

Vericiguat (BAY 1021189) is a novel potent, selective, orally available soluble guanylate cyclase (sGC) stimulator (MEC=0.3 uM), stimulating sGC NO-independently and in synergy with NO.

SRX3207 is an orally active and first-in-class dual Syk/PI3K inhibitor. SRX3207 possesses anti-tumor activity.

UAMC-3203 is a novel potent, drug-like ferroptosis inhibitor with IC50 of 12 nM, inhibit erastin-induced ferroptotic cell death more potently than Ferrostatin-1.

AC-262536 is a selective androgen receptor modulator (SARM, Ki = 5.01 nM). It is also a partial agonist of the androgen receptor (EC50 = 1.58 nM in a luciferase assay).

25-Hydroxycholesterol is a metabolite of cholesterol that is produced and secreted by macrophages in response to Toll-like receptor (TLR) activation. 25-hydroxycholesterol is a potent (EC50≈65 nM) and selective suppressor of IgA production by B cells.

DOTATATE acetate, a DOTA-conjugated peptide, and can be labelled with radionuclides for positron emission tomography (PET) imaging and peptide receptor radionuclide therapy (PRRT).

Indophagolin is a potent, indoline-containing autophagy inhibitor (IC50=140 nM). Indophagolin antagonizes the purinergic receptor P2X4 as well as P2X1 and P2X3 with IC50s of 2.71, 2.40 and 3.49 μM, respectively. Indophagolin also antagonizes the Gq-protein-coupled P2Y4, P2Y6, and P2Y11 receptors (IC50s =3.4~15.4 μM). Indophagolin has a strong antagonistic effect on serotonin receptor 5-HT6 (IC50=1.0 μM) and a moderate effect on receptors 5-HT1B, 5-HT2B, 5-HT4e, and 5-HT7.

TPT-172, also known as R33 (described in Mecozzi et al' s paper), is a thiophene thiourea derivative with molecule weight 172 in free base form. There is no formal name yet, we temporally call this molecule as TPT-172.

MLN-4760 is a potent and selective human ACE2 inhibitor (IC50, 0.44 nM), with excellent selectivity (>5000-fold) versus related enzymes including human testicular ACE (IC50, >100 μM) and bovine carboxypeptidase A (CPDA; IC50, 27 μM).

AM095 is a potent LPA1 receptor antagonist with IC50 values of 0.98 and 0.73 μM for recombinant human or mouse LPA1 respectively.

CNX-500 is a probe consisting of a covalent Btk inhibitor (CC-292) chemically linked to biotin. CNX-500 retains inhibitory activity against Btk (IC50 of 0.5 nM) and the ability to form a covalent bond with Btk. CNX-500 has low inhibitory effects on kinase epidermal growth factor receptor, and upstream Src-family kinases including Syk and Lyn.

Regorafenib hydrochloride (BAY73-4506) is a potent, orally active multikinase inhibitor that potently inhibits endothelial cell kinases in biochemical and cellular kinase phosphorylation assays with nanomolar range (IC50=3-200 nM).