Potent inhibitor of PfDHODH, showing greater than 4,000-fold selectivity for the malarial enzyme

Novel VEGFR inhibitor, also a moderate inhibitor of BET proteins with an IC 50 value of 4.6 μM for BRD4(1)

Inhibitor of Mer Kinase, also inhibiting EGFR

Orally active, nonsteroidal tamoxifen derivative and a ligand for the estrogen receptors (ERs), steroid receptor members of the nuclear receptor superfamily of transcription factors

Novel agonist at the adenosine A1 receptor

Potent TrkA kinase inhibitor

Novel potent RET kinase inhibitor

Potent and selective full agonist for peroixisome proliferator-activated receptor-alpha

Novel selective and soluble inhibitor of tumor necrosis factor-alpha converting enzyme (TACE)

Novel inhibitor of CDK

Inhibotor of active Vaccinia-Related Kinases (VRK)

Novel agonist for retinoid X receptor

Novel Selective and Nonpeptidomimetic Proteasome Inhibitor As an Antimalarial, specifically inhibiting the proteasome activity in P. falciparum

Potent inhibitor of adipocyte differentiation and weak partial agonist of

Negative allosteric modulator of human P2X7 and a positive allosteric modulator of rat P2X7

Potent inhibitor of cabonic anhydrase 2 (CA2)

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

Acyl-CoA, inhibiting cholesterol acyltransferase

Novel inhibitor of the activation of nuclear factor (NF)-κB signaling in bone marrow-derived dendritic cells, significantly inhibiting LPS-induced IL-12p40 and TNF-α gene expression, IκBα degradation, and NF-κB DNA binding activity in BMDCs, attenuating c

Inhibitor of vasoconstrictor responses to sympathetic nerve stimulation, potentiating the actions of adrenaline and noradrenaline, increasing the blood glucose concentration and decreasing the appetite

First-In-Class Antagonist against the Adrenomedullin-2 (AM2) Receptor

Novel broad-spectrum inhibitor of coronavirus and enterovirus replication, targeting the main protease (Mpro or 3CLpro)

Novel potent histamine H3 receptor antagonist

Novel hepatitis B surface antigen (HBsAg) inhibitor for the treatment of hepatitis B virus infection

Next-generation NSAID-like γ-secretase modulator (GSM) with improved in vitro potency and brain penetration, effectively lowering Aβ42 production in cells and in amyloid precursor protein transgenic mice

Negative control as an inactive IDH1 inhibitor

Novel potent transrepression-selective liver X receptor modulator with anti-inflammatory activity

Potent inhibitor of bacterial type IIA topoisomerases

Selective inhibitor of iE-DAP-stimulated IL-8 release via the NOD1 signaling pathway

Novel potent inhibitor of bacterial type IIA topoisomerases