Target family: Acetylcholine turnover (type: enzyme)
Target: acetylcholinesterase (Yt blood group)

Ligand: tacrine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1993)
Primary target: yes
Median affinity: 7.5 pKi
Reference (Journal): Exploiting protein fluctuations at the active-site gorge of human cholinesterases: further optimization of the design strategy to develop extremely potent inhibitors.
Published in: J Med Chem

Ligand: AChE reactivator 2 (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity: 5.639999866485596 pIC50
Reference (Journal): Structure-Based Optimization of Nonquaternary Reactivators of Acetylcholinesterase Inhibited by Organophosphorus Nerve Agents.
Published in: J Med Chem

Ligand: BW284C51 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 7.7 pIC50
Reference (Journal): Cholinesterases: new roles in brain function and in Alzheimer's disease.
Published in: Neurochem Res

Ligand: compound 2f [Jiang et al., 2018] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.1899995803833 pIC50
Reference (Journal): Dual GSK-3β/AChE Inhibitors as a New Strategy for Multitargeting Anti-Alzheimer's Disease Drug Discovery.
Published in: ACS Med Chem Lett

Ligand: donecopride (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.800000190734863 pIC50
Reference (Journal): Design of donecopride, a dual serotonin subtype 4 receptor agonist/acetylcholinesterase inhibitor with potential interest for Alzheimer's disease treatment.
Published in: Proc Natl Acad Sci USA

Ligand: donepezil (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1996)
Primary target: yes
Median affinity:  pIC50
Reference (Journal): QSAR analyses of the substituted indanone and benzylpiperidine rings of a series of indanone-benzylpiperidine inhibitors of acetylcholinesterase.
Published in: J Med Chem

Ligand: donepezil (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1996)
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine.
Published in: J Med Chem

Ligand: donepezil (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1996)
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Acetylcholinesterase protection and the anti-diisopropylfluorophosphate efficacy of E2020.
Published in: Eur J Pharmacol

Ligand: echothiophate (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1960)
Primary target: no
Median affinity:  -

Ligand: edrophonium (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1951)
Primary target: no
Median affinity: 6.699999809265137 pKi
Reference (Journal): Synthesis and study of thiocarbonate derivatives of choline as potential inhibitors of acetylcholinesterase.
Published in: J Med Chem

Ligand: galantamine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2001)
Primary target: no
Median affinity: 6.300000190734863 pIC50
Reference (Journal): Quaternary salts of E2020 analogues as acetylcholinesterase inhibitors for the reversal of neuromuscular block.
Published in: Bioorg Med Chem Lett

Ligand: neostigmine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA
Primary target: no
Median affinity: 7.349999904632568 pIC50
Reference (Journal): Synthesis and screening for acetylcholinesterase inhibitor activity of some novel 2-butyl-1,3-diaza-spiro[4,4]non-1-en-4-ones: derivatives of irbesartan key intermediate.
Published in: Bioorg Med Chem

Ligand: physostigmine (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine.
Published in: J Med Chem

Ligand: pralidoxime (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1964)
Primary target: yes
Median affinity: 3.0999999046325684 pIC50
Reference (Journal): Mono-oxime bisquaternary acetylcholinesterase reactivators with prop-1,3-diyl linkage-Preparation, in vitro screening and molecular docking.
Published in: Bioorg Med Chem

Ligand: pyridostigmine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1955)
Primary target: no
Median affinity: 6.440000057220459 pIC50
Reference (Journal): Long-acting anticholinesterases for myasthenia gravis: synthesis and activities of quaternary phenylcarbamates of neostigmine, pyridostigmine and physostigmine.
Published in: Bioorg Med Chem

Ligand: rivastigmine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2000), EMA (1998)
Primary target: yes
Median affinity: 5.400000095367432 pIC50
Reference (Journal): Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine.
Published in: J Med Chem