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β-NETA (α-NETA) is a stable, noncompetitive, slowly reversible choline acetyltransferase (ChAT) inhibitor with an IC50 of 9 μM and is a potent chemokine-like receptor-1 (CMKLR1) antagonist. β-NETA has anti-cancer activity[1][2]. β-NETA weakly inhibits cholinesterase (IC50=84 µM) and acetylcholinesterase (IC50=300 µM).

Rivastigmine tartrate (SDZ-ENA 713) is a carbamate-derived reversible CHOLINESTERASE INHIBITOR that is selective for the CENTRAL NERVOUS SYSTEM and is used for the treatment of DEMENTIA in ALZHEIMER DISEASE and PARKINSON DISEASE.

Rivastigmine (Exelon) is a Cholinesterase Inhibitor, used for therapy of Alzheimer disease.

ChE/GSK-3β-IN-1 (compound 18o) is a potent dual inhibitor of ChE/GSK-3β. It effectively inhibits acetylcholinesterase (AChE) with an IC50 of 1.7 μM, butyrylcholinesterase (BChE) with an IC50 of 5.3 μM, and GSK-3β with an IC50 of 5.7 μM. Additionally, ChE/GSK-3β-IN-1 prevents the self-aggregation of Aβ1-42 and is applicable in Alzheimer's disease (AD) research.

ChE/Aβ1-42-IN-1 (compound 28) is a potent aggregation inhibitor of ChE and Aβ1-42 with excellent BBB permeability, exhibiting IC50 values of 0.062 μM for AChE, 0.767 μM for BuChE, and 1.227 μM for Aβ1-42 aggregation. ChE/Aβ1-42-IN-1 is a potent multi-targeted anti-Alzheimer's disease agent [1].

hBChE-IN-2 is a butyrylcholinesterase (BChE) inhibitor and cannabinoid receptor 2 (CB2R) agonist with neuroprotective activity for the study of Alzheimer's disease-like neurological disorders.

BChE/HDAC6-IN-2 is a selective and potent dual inhibitor of BChE and HDAC6 with neuroprotective and reactive oxygen species (ROS) scavenging activity. BChE/HDAC6-IN-2 is a metal ion co-agonist that inhibits tau phosphorylation and can be used in the study of immune and neurological diseases.

AChE-IN-27 is a small molecule used for high-throughput assays.

AChE-IN-23 (compound 3h) is an acetylcholinesterase (AChE) inhibitor with an IC50 value of 48.3 μM [1].

ACHE Inhibitor 12 inhibited acetylcholinesterase with an IC50 value of 0.38 µM.

AChE-IN-29, a 3-OH pyrrolidine derivative, acts as a cholinesterase (ChE) inhibitor with potent activity against human acetylcholinesterase (hAChE), electric eel acetylcholinesterase (eeAChE), and equine butyrylcholinesterase (eqBChE), exhibiting IC50 values of 0.25 μM, 0.23 μM, and 0.72 μM, respectively. It is utilized in Alzheimer's disease research [1].

BuChE-IN-TM-10 (TM-10) is a potent inhibitor of butyrylcholinesterase (BuChE) with an IC50 of 8.9 nM. It effectively inhibits and disaggregates self-induced Aβ aggregation, exhibits significant antioxidant activity, and demonstrates substantial penetration through the blood-brain barrier (BBB), holding promise as a potential treatment for Alzheimer's disease.

AChE/BChE-IN-21 is an antagonist of the histamine H3 receptor, a calcium channel blocker, and an acetylcholinesterase inhibitor. It exhibits neuroprotective activities against H2O2 and Aβ1-40, and can restore cognitive functions in AD mice.

AChE/BChE-IN-25 (Compound 6e) is an orally active inhibitor of hAChE and eqBChE, with IC50 values of 7.9 nM and 0.79 nM, respectively. This compound exhibits antioxidant activity, effective in scavenging free radicals with an IC50 of 22.91 μM. AChE/BChE-IN-25 demonstrates neuroprotective effects by reducing mitochondrial and cellular oxidative stress in a Drosophila Alzheimer's model and improves spatial and cognitive memory impairments induced by Scopolamine in mouse models.

AChE/BuChE-IN-6 (Compound 11f) is an inhibitor of AChE and BuChE, with IC50 values of 1.24 and 1.85 μg/mL, respectively. It exhibits strong DPPH radical scavenging activity (IC50 = 3.15 μg/mL). In vivo toxicity studies demonstrate that AChE/BuChE-IN-6 is safe, showing no significant differences in blood and biochemical parameters compared to controls, and no abnormalities in liver and kidney tissues. This compound shows potential for Alzheimer's disease research.

BChE-IN-39 (Compound 7c) selectively inhibits butyrylcholinesterase (BChE) with an IC50 of 0.08 μM, while showing an IC50 of 3.98 μM for acetylcholinesterase (AChE) inhibition. Additionally, BChE-IN-39 downregulates GSK-3β expression, thereby inhibiting the excessive phosphorylation of tau protein.

AChE/hCA I-IN-1 (Compound L3) is an inhibitor of acetylcholinesterase (AChE) and carbonic anhydrase (CA), effectively inhibiting AChE, hCA I, and hCA II with IC50 values of 302 nM, 265 nM, and 283 nM, respectively.

hAChE/hBuChE/GSK-3β-IN-1 (Compound 6c) is a multi-target compound designed for Alzheimer's treatment capable of crossing the blood-brain barrier. It inhibits hAChE with an IC50 of 28.88 nM, hBuChE with an IC50 of 131.90 nM, and GSK-3β with an IC50 of 51.42 nM. Additionally, it acts as an inhibitor of tau protein and Aβ protein aggregation.

BChE-IN-38 (compound 13) is a potent BChE inhibitor, with Ki values of 62.05, 28.78, 14.09, and 1.15 nM for hCAI, hCAII, AChE, and BChE, respectively. BChE-IN-38 also demonstrates cytotoxic activity.

hAChE/hBuChE-IN-1 (compound C2) acts as a dual inhibitor of cholinesterases, exhibiting IC50 values of 514 nM for hAChE and 358 nM for hBuChE. It is orally active and capable of enhancing cognitive function and spatial memory.

AChE/MAO-B-IN-7 (VAV-8) is a compound that acts as a dual inhibitor of acetylcholinesterase (AChE) and MAO-B, with the ability to cross the blood-brain barrier. It also inhibits the aggregation of Aβ42, making it a valuable compound for Alzheimer's disease (AD) research.

hAChE-IN-10 (Compound ET11) is an inhibitor of human acetylcholinesterase (AChE) with an IC50 of 6.34 nM. This compound is capable of scavenging free radicals and exhibits antioxidant activity. Additionally, hAChE-IN-10 demonstrates metal-chelating properties, inhibiting Cu2+-induced Aβ1-42 aggregation, reducing amyloid plaque formation, and offering neuroprotective effects. It also ameliorates cognitive impairment in mice induced by Scopolamine.

BuChE-IN-16 (Compound 6a) is an orally active, blood-brain barrier-permeable, and selective BuChE inhibitor with an IC50 of 0.33 μM. It exhibits anti-inflammatory and neuroprotective effects, improves cognitive function in Alzheimer's disease (AD) zebrafish models, and alleviates scopolamine-induced memory impairment in mice. BuChE-IN-16 is applicable for Alzheimer's disease research.

AChE-IN-81 (compound 22) is a reversible, selective inhibitor of AChE with an 80.0% inhibition rate and an IC50 of 3.7 μM. It binds to AChE with an affinity (Kd) of 5.37 μM. AChE-IN-81 effectively reduces apoptosis in zebrafish brain cells and shows potential neuroprotective activity in an H2O2-induced SH-SY5Y cell damage model.