Novel non-MPEP site metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs)

Novel selective agonist of TLR8

Sphingosine kinase (SphK) inhibitor, having modest SphK2-selectivity

Novel Promoter of Neuronal Branching Via Transcellular Activation of the Focal Adhesion Kinase (FAK) and the ERK1/2 Signaling Pathway In Vitro

Novel inhibitor of geranylgeranyl diphosphate synthase (GGDPS)

Novel Potent HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI)

Inhibitor of the catalytic activity of VRV-PL-VIIIa, strongly inhibiting the hemolysis of red blood cells and VRV-PL-VIIIa-induced myotoxicity and lung hemorrhage in mice

Corrector of F508del-cystic fibrosis transmembrane conductance regulator (CFTR) mutant

Competitive S1P1/3 antagonist, increasing capillary permeability as measured by Evans blue dye leakage in mouse lung tissue

Novel Androgen Receptor Antagonist, inhibiting the LNCaP cell line as well as cell lines with wild-type androgen receptor

S1P1/S1P3 receptor agonist

Novel potent and selective inhibitor of ERα-dependent cell growth and gene expression, preventing the interaction between ERα-LBD and SRC-3 fusion proteins in a dose-dependent manner

Potent Antiandrogen, Targeting the BF3 Site of the Androgen Receptor and Inhibiting Enzalutamide-Resistant Prostate Cancer

Novel potent and highly selective type-II inhibitor of p38α/β, targeting an inactive state of the kinases induced by a unique folded P-loop conformation

Novel potassium-competitive acid blocker

Novel potent VEGFR2 modulator, exhibiting increased antiangiogenic potency than voacangine against VEGF-induced VEGFR2 phosphorylation without cytotoxic effects, resulting in significant tumor cell death in a mouse xenograft model

Novel and selective desensitizer of

Fluorescent cyclin-dependent kinase inhibitor, blocking the proliferation of human breast cancer cells

Natural inhibitor of ST2 (IL1RL1)

Endogenous cannabinoid receptor mixed agonist/antagonist, being a full agonist at GPR55 and CB2 and partial agonist/antagonist at CB1

Natural antimicrobial, antioxidant, and anti-inflammator agent

Natural inhibitor of 3C-like protease (3CLpro), targeting SARS-CoV-2 3CLpro, SARS-CoV 3CLpro and MERS-CoV 3CLpro

Novel antagonist against hypocretin (orexin) receptor 2, significantly preventing acute morphine-conditioned place preference (CPP) and stress-induced reinstatement of extinguished morphine-CPP in mouse models of opioid reward and relapse

Selective long-acting beta2-adrenergic agonist (LABA) with inherent 24-hour activity for once daily treatment of COPD and asthma

Broad spectrum antibiotic, inhibiting adenylyl cyclase type 5 (AC5) and protecting against chronic coronary artery occlusion (CAO)

Clopidogrel analog as an antiplatelet agent

Natural protein kinase C (PKC) activator and HSP90 inhibitor, sensitizing human acute myeloid leukemia cells to tyrosine kinase inhibitor-induced myeloid differentiation via activation of PKC and upregulation of Lyn

The first sub-micromolar inhibitor of the VHL-HIF1α interaction

Novel Inhibitor of the Pro-Angiogenic Activity of the Zinc Finger Transcription Factor Vezf1

Novel anti-vesiculoviral agent, inhibiting transcription initiation of vesiculoviruses