BAY-6672 is a potent and selective human Prostaglandin F (FP) receptor antagonist with an IC50 value of 11 nM.

BAY 1214784 is an orally available, potent, and selective hGnRH-R antagonist. BAY 1214784 effectively lowered plasma luteinizing hormone levels by up to 49%, at the same time being associated with low pharmacokinetic variability and good tolerability.

SPR519 is a potent dual inhibitor of PI3Kα and mTOR kinases with IC50 (PI3Kalpha) = 30 nM and IC50 (mTOR) = 10 nM. SPR519 exhibits an EC50 of low sub-micromolar range among various tested cancer cell lines such as A2780 (0.23 μM), PC3 (0.48 μM), and SKOV3 (0.50 μM).

SCO-267 is an allosteric GPR40 full agonist. SCO-267 can be used for the research of chronic diseases including diabetes.

OP-5244 is a potent and orally bioavailable CD73 inhibitor.

ropsacitinib, also known as PF-06826647 and Tyk2-IN-8, is an orally administered, tyrosine kinase 2 (TYK2) inhibitor, that is in development with Pfizer for the treatment of plaque psoriasis and inflammatory bowel disease.

SSK1 is a senolytic prodrug, which was designed from gemcitabine, by chem. modifying gemcitabin to incorporate a site cleavable by SA-β-gal following delivery of the prodrug in vivo, to release the active parent drug gemcitabine. SSK1 can be used to reduce one or more symptoms associated with a Senescence-associated disease or disorder in a subject. SSK1 is specifically activated by β-gal and eliminates mouse and human senescent cells independently of senescence inducers and cell types. In aged mice, SSK1 effectively cleared senescent cells in different tissues, decreased the senescence- and age-associated gene signatures, attenuated low-grade local and systemic inflammation, and restored physical function.

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.

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.

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).