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

Potent inhibitor of acetylcholine transport

Apoptosis inducer, inhibiting Leiomyosarcoma and Malignant peripheral nerve sheath tumor growth

Natural insect ryanodine receptor (RyR) antagonist

Natural Reversible Plant Growth Inhibitor

Novel blocker of atrial potassium channels

Natural anti-inflammatory and antioxidant agent, inhibiting both iNOS expression and NO release in the LPS-induced J774.A1 macrophage cell line, enhancing protein expression levels of PARP-1 and p53, and attenuating intracellular ROS and stress (oxidative

Natural Janus-Faced Modulator of Voltage-Gated Sodium Ion Channels, acting on the channel as either an agonist or antagonist depending on the nature of the electrophysiological stimulation protocol