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.

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

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

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.

VHL ligand 2 hydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Me hydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader.

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.

BAY 80-6946(Copanlisib) is a potent and highly selective reversible PI3K inhibitor for PI3Kα/β with IC50 of 0.469 nM/3.72 nM.

STING agonist 4 is an amidobenzimidazole (ABZI)-based compound that functions as a STING agonist with Kd of 1.6 nM (binding of endogenous full-length STING, THP-1 cell lysates); caused dose-dependent phosphorylation of IRF3 and STING that was inhibited by the TBK1 inhibitor BX795, induced dose-dependent secretion of IFN-β with EC50 of 3.1 uM in PBMCs (18-fold more potent than cGAMP); promotes production of IFN-γ-induced protein 10 (IP-10), IL-6 and TNFα by a mechanism that is dependent on STING-mediated activation of TBK1; unlike cGAMP and DMXAA, compound 2 efficiently activates STING function while maintaining an open STING confirmation.