MG-6267 is the first dual inhibitor of AChE and microRNA-15b biogenesis, protecting SH-SY5Y neuroblastoma cells from amyloid-beta (Aβ)-induced cytotoxicity

TGP-377 specifically and potently enhances VEGFA expression by targeting of a non-coding microRNA (pre-miR-377) that regulates its expression.

GSK789 is a potent, cell-permeable and highly selective inhibitor of the first bromodomains (BD1) with greater than 1000-fold selectivity for the BD1 domains over the BD2s.

ETX0282(ETX-0282,ETX 0282) is an orally available β-Lactamase inhibitor with a broad spectrum of activity against class A, C and D serine β-lactamases.

LEI-401 is a first-in-class, selective, and CNS-active NAPE-PLD (N-acylphosphatidylethanolamine phospholipase D) inhibitor, with an IC50 of 27 nM. LEI-401 modulates emotional behavior in mice.

MS117 is a first-in-class and cell-active irreversible protein arginine methyltransferase 6 (PRMT6) covalent inhibitor, with an IC50 of 18 nM.

JCN037 (JGK037) is non-covalent and BBB-penetrant EGFR tyrosine kinase inhibitor, with IC50 values of 2.49 nM, 3.95 nM, 4.48 nM for EGFR, p-wtEGFR and pEGFRvⅢ, respectively.

RO7185876 is a potent and selective gamma secretase modulator as a potential treatment for Alzheimer's disease.

RK-582 is an orally efficacious spiroindolinone-based tankyrase inhibitor for the treatment of colon cancer. It exhibits a markedly improved robust tumor growth inhibition in a COLO-320DM mouse xenograft model when orally administered.

UCSF4226 is a selective and inverse agonists of melatonin receptor 1 (MT2) with EC50 of 6.3 nM, and shows 91-fold selectivity for human MT2 over human MT1.

UCSF3384 is a selective and inverse agonists of melatonin receptor 1 (MT1) with EC50 of 21 nM, and shows 31-fold selectivity for human MT1 over human MT2.

UCSF7447 is a selective and inverse agonists of melatonin receptor 1 (MT1) with EC50 of 41 nM, and shows 53-fold selectivity for human MT1 over human MT2.

JA2-5 (NSC99667) is a potent dose-dependent inhibitor of PARG with IC50 of 1.0 mM.

JA2-4 (NSC99657) is a potent dose-dependent inhibitor of PARG with IC50 of 0.9 mM

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.

Samidorphan, also known as ALKS-33 and RDC-0313, is an opioid modulator with μ-antagonist properties. It is under development by Alkermes for the treatment of major depressive disorder and possibly other psychiatric conditions.

GNF2133 is a selective DYRK1A inhibitor with an IC50 value of 6 nM.

BMS-986260 is a potent, selective, and orally bioavailable TGFβR1 inhibitor (IC50=1.6 nM). BMS-986260 demonstrated functional activity in multiple TGFβ-dependent cellular assays, excellent kinome selectivity, favorable pharmacokinetic properties, and curative in vivo efficacy in combination with anti-PD-1 antibody in murine colorectal cancer (CRC) models.

ASP4132(ASP-4132,ASP 4132) is a potent adenosine monophosphate-activated protein kinase (AMPK) activator with EC50 of 18 nM, which shows moderately aqueous solublity and oral activity.

I-BET469 is a bromodomain and extraterminal (BET) inhibitor with pIC50 of 7.9 against BRD4 and is projected to have a low human efficacious dose.

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.