Inhibitor of Phosphodiesterase (PDE)-2

Potent and selective inhibitor for gelatinases, matrix metalloproteinase 2 (MMP2) and matrix metalloproteinase 9 (MPP9)

Selective water-soluble gelatinase inhibitor

Novel potent and highly specific IRAK4 inhibitor

Novel degrader of steroid receptor co-activator 1 (SRC-1)

Tricyclic antidepressant (TCA), acting as a serotonin–norepinephrine reuptake inhibitor (SNRI) and also having other activities including antihistamine, antiadrenergic, antiserotonergic, anticholinergic, and sodium channel-blocking effects

Cyanogen Bromide adduct of (R)-SCH-12679, a D1 antagonist

Novel HMG-CoA reductase inhibitor and nitric oxide donor

Novel NO-donor, suppressing inflammatory and nociceptive responses

Novel blocker of the interaction between FGF1 and FGFRD2 to inhibit cell proliferation, showing potent antiproliferent with less cytotoxicity.

Beclin 1 mimetic, selectively binding to Bcl-xL and inducing autophagy, showing potent cytotoxicity in PC-3, PC-3a and DU145 prostate cancer cells

Analogue of γ-hydroxybutyric acid (GHB), acting as a substrate for both the monocarboxylate transporter subtype 1 (MCT1) and subtype 4 (MCT4)

Novel GPR139 receptor agonist

Novel SIRT1 inhibitor, inducing cell death in adult T-cell leukaemia cells

Novel potent inhibitor of IRAK1/4 and FLT3

Novel AMA1-RON2 Inhibitor

Novel allosteric Eya2 phosphatase inhibitor, specifically targeting migration, invadopodia formation, and invasion of lung cancer cells

TSHR neutral antagonist, inhibiting stimulated signaling but not basal signaling

Novel Agonist for Human Resolvin D1 Receptor DRV1 with Pro-Resolving Functions

Novel inhibitor of ovarian cancer metastasis, adhesion, invasion and proliferation

Potent pan KDM Inhibitor, inhibiting KDM2A, KDM7A, KDM7B, KDM4A, KDM4C, and KDM5A

Less active trans-isomer of NCB-0846, acting as the negative control for NCB-0846, showing 13-fold weaker TNIK enzyme-inhibitory activity

First-in-class, potent, and selective Lactate dehydrogenase inhibitor

First-in-class, potent, and selective Lactate dehydrogenase inhibitor

Novel inhibitor of methionine aminopeptidase 2 (MetAP2)

M. tuberculosis Dihydrofolate Reductase Inhibitor

Novel bacterial type II topoisomerase inhibitor with activity against gram-negative bacteria and in vivo efficacy

Potent and selective 5-HT2A receptor agonist

Potent agonist of the human 5-HT2A and 5-HT2C receptors

Novel CD4-mimetic HIV-1 entry inhibitor