Almorexant(ACT078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively.IC50 value: 1.3/0.7 nM(OX1/OX2 receptor) [1] [2]Target: Dual OX!/OX2 receptorin vitro: [(3)H]Almorexant bound to a single saturable site on hOX(1) and hOX(2) with high affinity (K(d) of 1.3 and 0.17 nM, respectively. In Schild analyses using the [(3)H]inositol phosphates assay, almorexant acted as a competitive antagonist at hOX(1) and as a noncompetitive-like antagonist at hOX(2). In binding kinetic analyses, [(3)H]almorexant had fast association and dissociation rates at hOX(1), whereas it had a fast association rate and a remarkably slow dissociation rate at hOX(2) [1]. in vivo: During the 12-h dark period after dosing, ALM(Almorexant) exacerbated cataplexy in TG mice and increased nonrapid eye movement sleep with heightened sleep/wake fragmentation in both genotypes. ALM showed greater hypnotic potency in WT mice than in TG mice. The 100 mg/kg dose conferred maximal promotion of cataplexy in TG mice and maximal promotion of REM sleep in WT mice. In TG mice, ALM (30 mg/ kg) paradoxically induced a transient increase in active wakefulness [3]. Almorexant 200 mg showed significantly less 'Drug Liking' than both zolpidem doses (p < 0.01), and almorexant 400 mg had smaller effects than zolpidem 20 mg (p < 0.05), while almorexant 1,000 mg was not different from either zolpidem dose [4].

AA-115 (APG 115) is a potent and orally active MDM2 inhibitor with Ki <1 nM, potently inhibits SJSA-1 cell growth with IC50 of 60 nM.

A potent, specific inhibitor of HCV NS5B polymerase and HCV replication (IC50=1.28 uM, replicon assay).

Hydrazinocurcumin is a synthetic curcumin derivative that inhibits the proliferation of bovine aortic endothelial cells (BAECs) with IC50 of 520 nM without cytotoxicity, inhibits STAT3 phosphorylation and downregulates an array of STAT3 downstream targets.

Pateamine A (Pateamine) is a potent small molecule inhibitor of eukaryotic translation that stimulates eIF4AI/II and eIF4AIII activity, but not eIF4E, eIF2α, and elF4B.

Tubulysin B is a cytotoxic agent, used as the cytotoxic component in antibody-drug conjugates.

Tipranavir is a nonpeptidic protease inhibitor. Tipranavir has the ability to inhibit the replication of viruses that are resistant to other protease inhibitors and it recommended for patients who are resistant to other treatments. Resistance to tipranavir itself seems to require multiple mutations. Tipranavir was approved by the Food and Drug Administration (FDA) on June 22, 2005, and was approved for pediatric use on June 24, 2008. Like lopinavir and atazanavir, it is very potent and is effective in salvage therapy for patients with some drug resistance.

A highly potent agonist of σ1 receptor with Ki of 0.8 nM.

Melagatran is a synthetic, small-peptide direct thrombin inhibitor with anticoagulant activity.

Hi 76-0079 (NNC0076-0079) is a specfic, small molecule inhibitor of hormone-sensitive lipase (HSL) with IC50 of 0.11 uM. Hi 76-0079 does not affect ATGL or other lipases (IC50>50 uM). Hi 76-0079 inhibits lipolysis in vivo.

Culmerciclib maleate is a cyclin dependent kinase (CDK) inhibitor, and has antineoplastic activity.

BAY 1251152 (VIP152 ) is the first potent, selective, orally available PTEFb/CDK9 inhibitor with biochemical IC50 of 9 nM and MOLM13 cell IC50 of 29 nM, displays> 50-fold selectivity against other CDKs.

A synthetic curcuminoid that selectively inhibits STAT3 phosphorylation, transcription, and DNA binding without affecting the expression of other active STATs.

Serlopitant (VPD-737, MK-0594) is a potent, selective substance P/neurokinin 1 (NK1) receptor for treating chronic pruritus..

Idronoxil, also known as Phenoxodiol, is a synthetic flavonoid derivative. Phenoxodiol activates the mitochondrial caspase system, inhibits X-linked inhibitor of apoptosis (XIAP), and disrupts FLICE inhibitory protein (FLIP) expression, resulting in tumor cell apoptosis. This agent also inhibits DNA topoisomerase II by stabilizing the cleavable complex, thereby preventing DNA replication and resulting in tumor cell death.

CK-2127107(CK-107, Reldesemtiv) is a novel orally active fast skeletal troponin activator, selectively activates fast skeletal myofibrils with EC50 of 3.4 uM.

LY3325656 is a novel GPR142 agonist and is the first GPR142 agonist molecule advancing to phase 1 clinic trials for the treatment of Type 2 diabetes.

Taniborbactam (VNRX-5133) is a boronic-acid-containing pan-spectrum β-lactamase inhibitor against the class A, C, and D serine β-lactamases (SBLs).

DBPR112 is a potent EGFR mutation inhibitor against EGFRL858R/T790M double mutations with IC50 of 48 nM and also exhibits 10-fold potency better than Osimertinib, against EGFR and HER2 exon 20 insertion mutations.

M8891 is a methionine aminopeptidase-2 (MetAP-2) selective inhibitor with Ki and IC50 of 4.33 nM and 54 nM, respectively.

BAY-298 is a potent, and selective antagonists of the luteinizing hormone receptor with IC50 of 96 nM, 23 nM and 78 nM against human, rat, and cynomolgus monkey LH receptors.

VUF16839 is a high-affinity non-imidazole histamine H3 receptor agonist with pKi of 8.5 and pEC50 of 9.5, which shows weak activity on CYP enzymes and good metabolic stability.

DS54360155 is an orally potent analgesic without μ-opioid receptor agonist activity.

AGX51 is a small-molecule Id antagonist and inhibits the Id1-E47 interaction, leading to ubiquitin-mediated degradation of Ids, cell growth arrest, and reduced viability.

GS-6207 (GS6207, GS-CA1) is a potent, selective inhibitor of HIV-1 capsid function with potency and potential to be clinically effective against a broad range of HIV-1 strains..

3AC is an inhibitor of SH2 domain-containing inositol-5’-phosphatase 1 (SHP-1). It is selective for SHP-1 over SHP-2 and phosphatase and tensin homolog (PTEN). 3α-Aminocholestane induces hyperactivation of the tyrosine kinase SYK in patient-derived Ph+ acute lymphoblastic leukemia (ALL) cells and selectively induces cytotoxicity in these cells over mature B cell lymphoma cells. It reduces leukemia burden and increases survival in a tyrosine kinase inhibitor-resistant patient-derived Ph+ ALL mouse xenograft model when administered at a dose of 50 mg/kg. 3α-Aminocholestane reduces cell viability of OPM2 multiple myeloma (MM) cells in a concentration-dependent manner and of RPMI8226 MM cells when used at concentrations greater than or equal to 12.5 μM. It halts the cell cycle at the G0/G1 or G2/M stages in the highly proliferative OPM2 or less proliferative RPMI8226 cell lines, respectively. It induces apoptosis via activation of caspase-3, caspase-9, and poly(ADP-ribose) polymerase (PARP) in OPM2 cells but not in RPMI8226 cells. 3α-Aminocholestane reduces tumor burden and increases survival in an OPM2 mouse xenograft model.

Nimbolide is a natural inhibitor of pancreatic cancer growth and metastasis through ROS-mediated apoptosis. It inhibits epithelial-to-mesenchymal transition.

OP-3633 is a potent steroidal glucocorticoid receptor (GR) antagonist with IC50 of 29 nM and shows excellent selectivity against GR over progesterone receptors (PR) and androgen receptors (AR).

UDM-001651 is a potent , selective and orally active Protease-Activated Receptor 4 (PAR4) Antagonist with in Vivo Antithrombotic Efficacy (IC50 = 2.4 nM). UDM-001651 was evaluated in a monkey thrombosis model and shown to have robust antithrombotic efficacy and no prolongation of kidney bleeding time. This combination of excellent efficacy and safety margin strongly validates PAR4 antagonism as a promising antithrombotic mechanism.

VU6003586 is a novel allosteric modulators of mGlu5 with EC50 of 174 nM.