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Literature summary extracted from

  • Saxena, A.; Fedorko, J.M.; Vinayaka, C.R.; Medhekar, R.; Radic, Z.; Taylor, P.; Lockridge, O.; Doctor, B.P.
    Aromatic amino-acid residues at the active and peripheral anionic sites control the binding of E2020 (Aricept) to cholinesterases (2003), Eur. J. Biochem., 270, 4447-4458.
    View publication on PubMed

Protein Variants

EC Number Protein Variants Comment Organism
3.1.1.7 D74N altered Ki for E2020 Mus musculus
3.1.1.7 F295L altered Ki for E2020 Mus musculus
3.1.1.7 F297I altered Ki for E2020 Mus musculus
3.1.1.7 W286A altered Ki for E2020 Mus musculus
3.1.1.7 W86A altered Ki for E2020 Mus musculus
3.1.1.7 Y124Q altered Ki for E2020 Mus musculus
3.1.1.7 Y337A altered Ki for E2020 Mus musculus
3.1.1.7 Y337F altered Ki for E2020 Mus musculus
3.1.1.7 Y72N altered Ki for E2020 Mus musculus
3.1.1.7 Y72N/Y124N/W286R altered Ki for E2020 Mus musculus
3.1.1.8 A277W mutation does not affect binding of E2020 Homo sapiens
3.1.1.8 A328F altered Ki for E2020 Homo sapiens
3.1.1.8 A328Y Ki for E2020 similar to wild-type enzyme Homo sapiens
3.1.1.8 D70G altered Ki for E2020 Homo sapiens
3.1.1.8 Q119Y altered Ki for E2020 Homo sapiens
3.1.1.8 Q119Y/V288F/A328Y altered Ki for E2020 Homo sapiens
3.1.1.8 V288F Ki for E2020 similar to wild-type enzyme Homo sapiens
3.1.1.8 W82A altered Ki for E2020 Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.1.1.7 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride E2020, acetylcholinesterase inhibitor used in treatment of Alzheimer's diaease, inhibition kinetics Mus musculus
3.1.1.7 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride E2020, acetylcholinesterase inhibitor used in treatment of Alzheimer's diaease, interacts with the active site and the peripheral anionic site of the enzyme Tetronarce californica
3.1.1.8 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride E2020, acetylcholinesterase inhibitor used in treatment of Alzheimer's disease, interacts with the active site and the peripheral anionic site of the enzyme Equus caballus
3.1.1.8 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride E2020, acetylcholinesterase inhibitor used in treatment of Alzheimer's diaease, inhibition kinetics Homo sapiens
3.1.1.8 7(R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride
-
 Equus caballus

Organism

EC Number Organism UniProt Comment Textmining
3.1.1.7 Mus musculus
-
-
-
3.1.1.7 Tetronarce californica
-
-
-
3.1.1.8 Equus caballus
-
-
-
3.1.1.8 Homo sapiens
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.1.1.7 acetylthiocholine + H2O
-
 Tetronarce californica thiocholine + acetate
-
 ?
3.1.1.7 butyrylthiocholine + H2O
-
 Mus musculus thiocholine + butyrate
-
 ?
3.1.1.8 butyrylthiocholine + H2O
-
 Homo sapiens thiocholine + butyrate
-
 ?
3.1.1.8 butyrylthiocholine + H2O
-
 Equus caballus thiocholine + butyrate
-
 ?

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.1.1.7 0.0000004
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, Y337A mutant Mus musculus
3.1.1.7 0.0000005
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, Y337F mutant Mus musculus
3.1.1.7 0.0000022
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, wild-type enzyme Mus musculus
3.1.1.7 0.0000031
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C Tetronarce californica
3.1.1.7 0.00002
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, Y124Q mutant Mus musculus
3.1.1.7 0.00002
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, Y72N mutant Mus musculus
3.1.1.7 0.000027
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, F295L mutant Mus musculus
3.1.1.7 0.00007
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, F297I mutant Mus musculus
3.1.1.7 0.00069
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, W86A mutant Mus musculus
3.1.1.7 0.0032
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, W286A mutant Mus musculus
3.1.1.7 0.0051
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, D74N mutant Mus musculus
3.1.1.7 0.0087
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, Y72N/Y124N/W286R mutant Mus musculus
3.1.1.8 0.00064
-
 7(R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C Equus caballus
3.1.1.8 0.0008
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, Q119Y/V288F/A328Y mutant Homo sapiens
3.1.1.8 0.00111
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, wild-type enzyme Homo sapiens
3.1.1.8 0.0024
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, A277W mutant Homo sapiens
3.1.1.8 0.0035
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, V288F mutant Homo sapiens
3.1.1.8 0.0039
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, A328Y mutant Homo sapiens
3.1.1.8 0.0129
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, Q119Y mutant Homo sapiens
3.1.1.8 0.0228
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, A328F mutant Homo sapiens
3.1.1.8 0.03
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, D70G mutant Homo sapiens
3.1.1.8 0.12
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, W82A mutant Homo sapiens