Protein Variants | Comment | Organism |
---|---|---|
A277W | mutation does not affect binding of E2020 | Homo sapiens |
A328F | altered Ki for E2020 | Homo sapiens |
A328Y | Ki for E2020 similar to wild-type enzyme | Homo sapiens |
D70G | altered Ki for E2020 | Homo sapiens |
Q119Y | altered Ki for E2020 | Homo sapiens |
Q119Y/V288F/A328Y | altered Ki for E2020 | Homo sapiens |
V288F | Ki for E2020 similar to wild-type enzyme | Homo sapiens |
W82A | altered Ki for E2020 | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(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 | |
(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 | |
7(R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride | - |
Equus caballus |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Equus caballus | - |
- |
- |
Homo sapiens | - |
- |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
butyrylthiocholine + H2O | - |
Homo sapiens | thiocholine + butyrate | - |
? | |
butyrylthiocholine + H2O | - |
Equus caballus | thiocholine + butyrate | - |
? |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.00064 | - |
7(R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride | pH 8, 25°C | Equus caballus | |
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 | |
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 | |
0.0024 | - |
(R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride | pH 8, 25°C, A277W mutant | Homo sapiens | |
0.0035 | - |
(R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride | pH 8, 25°C, V288F mutant | Homo sapiens | |
0.0039 | - |
(R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride | pH 8, 25°C, A328Y mutant | Homo sapiens | |
0.0129 | - |
(R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride | pH 8, 25°C, Q119Y mutant | Homo sapiens | |
0.0228 | - |
(R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride | pH 8, 25°C, A328F mutant | Homo sapiens | |
0.03 | - |
(R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride | pH 8, 25°C, D70G mutant | Homo sapiens | |
0.12 | - |
(R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride | pH 8, 25°C, W82A mutant | Homo sapiens |