LJ570 is the first PPARα/γ Dual Agonist Able To Bind to Canonical and Alternative Sites of PPARγ and To Inhibit Its Cdk5-Mediated Phosphorylation. LJ570 is a potent partial agonist of both PPARα and γ subtypes. LJ570 inhibited the Cdk5-mediated phosphorylation of PPARγ at serine 273 that is currently considered the mechanism by which some PPARγ partial agonists exert antidiabetic effects similar to thiazolidinediones, without showing their typical side effects. LJ570 may be useful for treatment of dyslipidemic type 2 diabetes.

O(6)-Benzylguanine is an MGMT inhibitor that prevents the repair of DNA damage induced by chemotherapeutics. It allows apoptosis and other mechanisms of cell death to occur.

Lyn-IN-1 is a potent and selective dual Bcr-Abl/Lyn inhibitor..

A potent PI3K inhibitor with IC50 3 nM, does not inhibit PI4K activity.

Mianserin is a psychoactive drug of the tetracyclic antidepressant (TeCA) therapeutic family. It is classified as a noradrenergic and specific serotonergic antidepressant (NaSSA) and has antidepressant, anxiolytic (anti-anxiety), hypnotic (sedating), antiemetic (nausea and vomiting-attenuating), orexigenic (appetite-stimulating), and antihistamine effects.

Mianserin hydrochloride is a tetracyclic compound with antidepressant effects. It may cause drowsiness and hematological problems. Its mechanism of therapeutic action is not well understood, although it apparently blocks alpha-adrenergic, histamine H1, and some types of serotonin receptors.

Prolyl Endopeptidase Inhibitor 1 (Boc-Pro-prolinal) is a potent prolyl endopeptidase (PEP; PE) inhibitor, with a Ki value of 15 nM. Prolyl Endopeptidase Inhibitor 1 has anti-amnesic effect.

CGP-42112 (CGP42112A) is a highly potent, selective Angiotensin-II subtype 2 receptor(AT2 receptor) agonist with Ki of 0.24 nM.

A neuropeptide derived from the same precursor polypeptide as neurotensin, and with similar but subtly distinct expression and effects..

A potent melanocortin MC3 and MC4 receptor antagonist with IC50 of 0.23 nM and 0.06 nM, respectively.

Super-TDU is an inhibitory peptide targeting YAP-TEADs interaction.

A potent, selective, and orally bioavailable ghrelin receptor (GHSR) inverse agonist with binding pKi of 8.36.

KN-92 is an inactive derivative of KN-93. KN-93 is a selective inhibitor of Ca2+/calmodulin-dependent kinase II (CaMKII), competitively blocking CaM binding to the kinase (Ki = 370 nM).

HS-173 is a potent PI3Kα inhibitor with IC50 of 0.8 nM.

Tipifarnib S enantiomer is a potent and selective inhibitor of FTase (farnesyltransferase).

A novel, potent, and selective inhibitor of Late sodium current (late INa) for treatment of long QT-3 syndrome (LQT-3), hypertrophic cardiomyopathy (HCM), and ventricular tachycardia–ventricular fibrillation (VT–VF).

UU-T03 is the ethyl ester derivative of UU-T02, which is a potent, selective inhibitor of β-catenin/Tcf4 interaction with Ki of 1.36 uM; exhibits growth inhibition of SW480 cells with IC50 of 10.77 uM; downregulates the transcription of AXIN2, LGR5, cyclin D1, and c-Myc in dose-dependent manners in SW480 cells.

Tamoxifen(ICI-46474) is an antagonist of the estrogen receptor in breast tissue via its active metabolite, hydroxytamoxifen.

GSK3039294 is a Serum amyloid P component inhibitor.

Gemcabene (PD-72953, PD72953) is a first-in-class lipid-lowering agent and activator of PARP.

Fasudil, a Rho-kinase inhibitor, has been shown to reduce portal venous pressure in cirrhotic rats.

LCH 7749944 (GNF-PF-2356) is a novel and potent PAK4 with IC50 of 14.93 uM, shows weak activity against other PAK family members.

CDPPB is a potent, selective, brain penetrant positive allosteric modulator of mGlu5 receptor with EC50 of 10 nM and 20 nM for human and rat mGluR5, respectively.

Blasticidin S hydrochloride is a nucleoside antibiotic isolated from Streptomyces griseochromogenes. Blasticidin S is a potent inhibitor of protein synthesis in both prokaryotic and eukaryotic cells.

ADX-102 (Reproxalap, NS-2) is a novel small molecule immunomodulator that covalently binds aldehydes including malondialdehyde and 4-hydroxynonenal, which have been shown to mediate inflammatory pain; DX-102 is a promising agent for the treatment of dry eye disease.

MDI-2268 (MDI2268) is a small-molecule, in vivo-active inhibitor of plasminogen activator inhibitor type-1 (PAI-1), demonstrates excellent pharmacokinetics, potent activity against vitronectin-bound PAI-1 in vivo, and efficacy in murine model of venous thrombosis.

Tafluprost(AFP-168) is an anti-glaucoma prostaglandin (PG) analog.A number of 17-phenyl trinor PGF2α derivatives have been approved for the treatment of glaucoma.1,2,3,4 Of these, the ones wherein the 13,14-double bond has been hydrogenated retain relatively good potency.

CC-90011 is a potent and orally active LSD1 inhibitor. CC-90011 binds to and inhibits LSD1, a demethylase that suppresses the expression of target genes by converting the di- and mono-methylated forms of lysine at position 4 of histone H3 (H3K4) to mono- and unmethylated H3K4, respectively. CC-90011 exhibits potent on-target induction of cellular differentiation in acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cell lines, and antitumor efficacy in patient-derived xenograft (PDX) SCLC models.

Difluprednate(Durezol) is a corticosteroid, approved difluprednate for the treatment of post-operative ocular inflammation and pain.

Osilodrostat is an inhibitor of aldosterone synthase and aromatase, for treating Cushing’s disease.