Chikusetsusaponin Ib has anti-Alzheimer's disease activity and is a potent AChE inhibitor.

Millmerranone A shows the acetylcholinesterase inhibitory property.

Paecilomide is a pyridone alkaloid and acetylcholinesterase inhibitor.

Dual AChE-MAO B-IN-1 (compound 15) is an orally bioavailable CNS-permeant potent inhibitor of both human AChE (IC50=550 nM) and MAO B (IC50=8.2 nM). Dual AChE-MAO B-IN-1 behaves as a safe and metabolically stable neuroprotective agent, devoid of cytochrome liability.

AChE-IN-4 shows the acetylcholine esterase inhibition (AChEI) with an IC50 value of 24.1 μM.

AChE-IN-5 (compound 5) exhibits strong in vitro bioactivity against AChE/5-HT1A/SERT and exhibits good BBB permeability. AChE-IN-5 shows IC50 value 2.29 nM against AChE, EC50 58.6 nM against 5-HT1A and IC50 value against SERT. Orally active.

Dual AChE-MAO B-IN-2 is a potent AChE and MAO B dual inhibitor with IC50s of 0.12 µM and 0.01 µM for b>AChE and MAO B, respectively. Dual AChE-MAO B-IN-2 has the potential for the research of Alzheimer’s disease.

Bis(7)-tacrine dihydrochloride is a dimeric AChE inhibitor derived from tacrine. Bis(7)-tacrine dihydrochloride prevents glutamate-induced neuronal apoptosis by blocking NMDA receptors. Bis(7)-tacrine dihydrochloride is a potent GABAAreceptor antagonist. Bis(7)-tacrine dihydrochloride has the potential for the research of Alzheimer's disease .

sEH/AChE-IN-1 (Compound 12a) is a dual inhibitor of the enzymes soluble epoxide hydrolase (sEH) and acetylcholinesterase (AChE). sEH/AChE-IN-1 provides cumulative effects against neuroinflammation and memory impairment. sEH/AChE-IN-1 has the potential for the research of Alzheimer's disease (AD).

sEH/AChE-IN-2 (Compound 12b) is a dual inhibitor of the enzymes soluble epoxide hydrolase (sEH) and acetylcholinesterase (AChE). sEH/AChE-IN-2 provides cumulative effects against neuroinflammation and memory impairment. sEH/AChE-IN-2 has the potential for the research of Alzheimer's disease (AD).

AChE-IN-7 (Compound 16) is a selective and potent inhibitor of acetylcholinesterase (eeAChE IC50 = 0.045 μM; eeBuChE IC50 = 19.68 μM). AChE-IN-7 is safe in vivo and in vitro, and shows good overall pharmacokinetic performance and high bioavailability (F = 55.5%). AChE-IN-7 also has high BBB permeability.

AChE-IN-6 (Compound 12a) is an optimal multifunctional ligand with significant inhibition of AChE (EeAChE, IC50 = 0.20 μM; HuAChE, IC50 = 37.02 nM) and anti-Aβ activity (IC50 = 1.92 μM for self-induced Aβ1-42 aggregation; IC50 = 1.80 μM for disaggregation of Aβ1-42 fibrils; IC50 = 2.18 μM for Cu2+-induced Aβ1-42 aggregation; IC50 = 1.17 μM for disaggregation of Cu2+-induced Aβ1-42 fibrils). AChE-IN-6 has the potential for the research of Alzheimer's disease.

ZLWH-23 is a selective AChE inhibitor (IC50=0.27 μM) with GSK-3β inhibitory property (IC50=6.78 μM). ZLWH-23 possesses selectivity for AChE over BChE (IC50=20.82 μM) and for GSK-3β over multi-kinases. ZLWH-23 has the potential for the research of Alzheimer's disease.

Cytidine 5′-diphosphoethanolamine is an intermediate compound in the synthesis of phosphatidylethanolamine. Cytidine 5′-diphosphoethanolamine is a stimulant of Ach synthesis.

AChE/BuChE-IN-1 (Compound 1), a chrysin derivative, is a selective butyrylcholinesterase (BuChE) inhibitor with an IC50 of 0.48 μM. AChE/BuChE-IN-1 inhibits acetylcholinesterase (AChE) with an IC50 of 7.16 μM. AChE/BuChE-IN-1 shows strong scavenging ·OH activities with a IC50 of 0.1674 μM. AChE/BuChE-IN-1 inhibits reactive oxygen species (ROS), Aβ1-42 aggregation (self-, Cu2+-induced, AChE-induced). AChE/BuChE-IN-1 has high BBB permeability and bioavailability and low cell toxicity. AChE/BuChE-IN-1 has the potential for Alzheimer' disease (AD) research.

ChE/Aβ1-42-IN-1 (compound 28) is a potent ChE and Aβ1-42 aggregation inhibitor with IC50s of 0.062, 0.767 and 1.227 µM for AChE, BuChE and Aβ1-42 aggregation, respectively. ChE/β1-42-IN-1 shows excellent BBB penetration. ChE/Aβ1-42-IN-1 is a potent multi-targeted anti-Alzheimer's agent.

AChE-IN-8 (Compound 19) is a potent inhibitor of AChE with an IC50 of 1.95 μM. AChE-IN-8 has the potential for the research of Alzheimer's disease.

AChE-IN-11 (compound 5C) is a good multifunctional agent (AChE IC50 = 7.9 μM, MAO-B IC50 = 9.9 μM, BACE1 IC50 = 8.3 μM). AChE-IN-11 displays a mixed-type AChE inhibition, which can bind to the CAS and PAS of AChE. AChE-IN-11 also exhibits good antioxidant activity (ORAC = 2.5 eq) and neuroprotective effects. AChE-IN-11 is a selective metal ions chelator. AChE-IN-11 has the potential for the research of AD.

Y13g is the potent inhibitor of both AChE and IL-6. Interleukin-6 (IL-6) and acetylcholinesterase (AChE) are two important targets implicated in progression of Alzheimer's Disease (AD). Y13g reverses the STZ-induced memory deficit, and shows histopathology similarly as in normal animals.

hAChE/Aβ1-42-IN-1 (Compound 16) is a potent inhibitor of hAChE and Aβ1-42 aggregation. hAChE/Aβ1-42-IN-1 shows acceptable relative safety upon hepG2 cell line and excellent BBB penetration with wide safety margin. hAChE/Aβ1-42-IN-1 has the potential for the research of Alzheimer disease (AD).

K203 is a potent reactivator of tabun-inhibited AChE. K203 is a crucial antidote used for the organophosphate intoxication.

VP15 hydrochloride (VP-15 HCl) is a BBB-penetrant, orally active, multitarget directed ligand against acetylcholine and monoamine oxidase enzymes with IC50 of 0.04 and 0.37 uM for AChE and MAO-B, respectively, >600-fold selectivity over BuChE.