Application | Comment | Organism |
---|---|---|
drug development | the enzyme is a target for development of drugs for use in therapy of Alzheimer's diesease | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
2-[(1-[2-[(6-chloro-1,2,3,4-tetrahydroacridin-9-yl)amino]ethyl]piperidin-4-yl)methyl]-5,6-dimethoxy-2,3-dihydro-1H-inden-1-one | - |
Homo sapiens | |
2-[(1-[3-[(6-chloro-1,2,3,4-tetrahydroacridin-9-yl)amino]propyl]piperidin-4-yl)methyl]-5,6-dimethoxy-2,3-dihydro-1H-inden-1-one | - |
Homo sapiens | |
3-[5-(4-chlorophenyl)-3,4-dihydro-2H-pyrano[3,2-c]quinolin-9-yl]-N-[4-[(6-chloro-1,2,3,4-tetrahydroacridin-9-yl)amino]butyl]propanamide | - |
Homo sapiens | |
3-[5-(4-chlorophenyl)-3,4-dihydro-2H-pyrano[3,2-c]quinolin-9-yl]-N-[5-[(6-chloro-1,2,3,4-tetrahydroacridin-9-yl)amino]pentyl]propanamide | - |
Homo sapiens | |
3-[5-(4-chlorophenyl)-3,4-dihydro-2H-pyrano[3,2-c]quinolin-9-yl]-N-[6-[(6-chloro-1,2,3,4-tetrahydroacridin-9-yl)amino]hexyl]propanamide | - |
Homo sapiens | |
3-[5-(4-chlorophenyl)-3,4-dihydro-2H-pyrano[3,2-c]quinolin-9-yl]-N-[7-[(6-chloro-1,2,3,4-tetrahydroacridin-9-yl)amino]heptyl]propanamide | - |
Homo sapiens | |
3-[5-(4-chlorophenyl)-3,4-dihydro-2H-pyrano[3,2-c]quinolin-9-yl]-N-[8-[(6-chloro-1,2,3,4-tetrahydroacridin-9-yl)amino]octyl]propanamide | - |
Homo sapiens | |
5,6-dimethoxy-2-([1-[2-(1,2,3,4-tetrahydroacridin-9-ylamino)ethyl]piperidin-4-yl]methyl)-2,3-dihydro-1H-inden-1-one | - |
Homo sapiens | |
5,6-dimethoxy-2-([1-[3-(1,2,3,4-tetrahydroacridin-9-ylamino)propyl]piperidin-4-yl]methyl)-2,3-dihydro-1H-inden-1-one | - |
Homo sapiens | |
5-(4-chlorophenyl)-N-[10-[(6-chloro-1,2,3,4-tetrahydroacridin-9-yl)amino]decyl]-3,4-dihydro-2H-pyrano[3,2-c]quinoline-9-carboxamide | - |
Homo sapiens | |
5-(4-chlorophenyl)-N-[6-[(6-chloro-1,2,3,4-tetrahydroacridin-9-yl)amino]hexyl]-3,4-dihydro-2H-pyrano[3,2-c]quinoline-9-carboxamide | - |
Homo sapiens | |
5-(4-chlorophenyl)-N-[7-[(6-chloro-1,2,3,4-tetrahydroacridin-9-yl)amino]heptyl]-3,4-dihydro-2H-pyrano[3,2-c]quinoline-9-carboxamide | - |
Homo sapiens | |
5-(4-chlorophenyl)-N-[8-[(6-chloro-1,2,3,4-tetrahydroacridin-9-yl)amino]octyl]-3,4-dihydro-2H-pyrano[3,2-c]quinoline-9-carboxamide | - |
Homo sapiens | |
5-(4-chlorophenyl)-N-[9-[(6-chloro-1,2,3,4-tetrahydroacridin-9-yl)amino]nonyl]-3,4-dihydro-2H-pyrano[3,2-c]quinoline-9-carboxamide | - |
Homo sapiens | |
6-chloro-N-(2-[4-[(5,6-dimethoxy-2,3-dihydro-1H-inden-2-yl)methyl]piperidin-1-yl]ethyl)-1,2,3,4-tetrahydroacridin-9-amine | - |
Homo sapiens | |
6-chloro-N-(3-[4-[(5,6-dimethoxy-2,3-dihydro-1H-inden-2-yl)methyl]piperidin-1-yl]propyl)-1,2,3,4-tetrahydroacridin-9-amine | - |
Homo sapiens | |
6-chlorotacrine | - |
Homo sapiens | |
donepizil | - |
Homo sapiens | |
additional information | development and synthesis of two families of dual binding site acetylcholinesterase inhibitors consisting of a tacrine or 6-chlorotacrine unit as the active site interacting moiety, either the 5,6-dimethoxy-2-[(4-piperidinyl)methyl]-1-indanone fragment of donepezil (or the indane derivative thereof) or a 5-phenylpyrano[3,2-c]quinoline system, reminiscent to the tryciclic core of propidium, as the peripheral site interacting unit, and a linker of suitable length as to allow the simultaneous binding at both sites. These hybrid compounds are all potent and selective inhibitors of human AChE, and are able to interfere in vitro both formation and aggregation of the beta-amyloid peptide, the latter effects endowing these compounds with the potential to modify Alzheimers disease progression. No inhibition by propidium iodide. In hibitor molecular dynamics simulations, overview | Homo sapiens | |
N-(2-[4-[(5,6-dimethoxy-2,3-dihydro-1H-inden-2-yl)methyl]piperidin-1-yl]ethyl)-1,2,3,4-tetrahydroacridin-9-amine | - |
Homo sapiens | |
N-(3-[4-[(5,6-dimethoxy-2,3-dihydro-1H-inden-2-yl)methyl]piperidin-1-yl]propyl)-1,2,3,4-tetrahydroacridin-9-amine | - |
Homo sapiens | |
tacrine | - |
Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Synonyms | Comment | Organism |
---|---|---|
AChE | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00000027 | - |
- |
Homo sapiens | 2-[(1-[3-[(6-chloro-1,2,3,4-tetrahydroacridin-9-yl)amino]propyl]piperidin-4-yl)methyl]-5,6-dimethoxy-2,3-dihydro-1H-inden-1-one | |
0.00000067 | - |
- |
Homo sapiens | 2-[(1-[2-[(6-chloro-1,2,3,4-tetrahydroacridin-9-yl)amino]ethyl]piperidin-4-yl)methyl]-5,6-dimethoxy-2,3-dihydro-1H-inden-1-one | |
0.00000088 | - |
- |
Homo sapiens | 5,6-dimethoxy-2-([1-[3-(1,2,3,4-tetrahydroacridin-9-ylamino)propyl]piperidin-4-yl]methyl)-2,3-dihydro-1H-inden-1-one | |
0.00000106 | - |
- |
Homo sapiens | 6-chloro-N-(3-[4-[(5,6-dimethoxy-2,3-dihydro-1H-inden-2-yl)methyl]piperidin-1-yl]propyl)-1,2,3,4-tetrahydroacridin-9-amine | |
0.00000192 | - |
- |
Homo sapiens | 5-(4-chlorophenyl)-N-[6-[(6-chloro-1,2,3,4-tetrahydroacridin-9-yl)amino]hexyl]-3,4-dihydro-2H-pyrano[3,2-c]quinoline-9-carboxamide | |
0.00000216 | - |
- |
Homo sapiens | N-(3-[4-[(5,6-dimethoxy-2,3-dihydro-1H-inden-2-yl)methyl]piperidin-1-yl]propyl)-1,2,3,4-tetrahydroacridin-9-amine | |
0.0000026 | - |
- |
Homo sapiens | 6-chloro-N-(2-[4-[(5,6-dimethoxy-2,3-dihydro-1H-inden-2-yl)methyl]piperidin-1-yl]ethyl)-1,2,3,4-tetrahydroacridin-9-amine | |
0.000004 | - |
- |
Homo sapiens | 5,6-dimethoxy-2-([1-[2-(1,2,3,4-tetrahydroacridin-9-ylamino)ethyl]piperidin-4-yl]methyl)-2,3-dihydro-1H-inden-1-one | |
0.00000513 | - |
- |
Homo sapiens | N-(2-[4-[(5,6-dimethoxy-2,3-dihydro-1H-inden-2-yl)methyl]piperidin-1-yl]ethyl)-1,2,3,4-tetrahydroacridin-9-amine | |
0.0000073 | - |
- |
Homo sapiens | 5-(4-chlorophenyl)-N-[8-[(6-chloro-1,2,3,4-tetrahydroacridin-9-yl)amino]octyl]-3,4-dihydro-2H-pyrano[3,2-c]quinoline-9-carboxamide | |
0.0000083 | - |
- |
Homo sapiens | 6-chlorotacrine | |
0.0000096 | - |
- |
Homo sapiens | 3-[5-(4-chlorophenyl)-3,4-dihydro-2H-pyrano[3,2-c]quinolin-9-yl]-N-[5-[(6-chloro-1,2,3,4-tetrahydroacridin-9-yl)amino]pentyl]propanamide | |
0.0000111 | - |
- |
Homo sapiens | 3-[5-(4-chlorophenyl)-3,4-dihydro-2H-pyrano[3,2-c]quinolin-9-yl]-N-[6-[(6-chloro-1,2,3,4-tetrahydroacridin-9-yl)amino]hexyl]propanamide | |
0.0000116 | - |
- |
Homo sapiens | donepizil | |
0.000014 | - |
- |
Homo sapiens | 3-[5-(4-chlorophenyl)-3,4-dihydro-2H-pyrano[3,2-c]quinolin-9-yl]-N-[8-[(6-chloro-1,2,3,4-tetrahydroacridin-9-yl)amino]octyl]propanamide | |
0.0000144 | - |
- |
Homo sapiens | 3-[5-(4-chlorophenyl)-3,4-dihydro-2H-pyrano[3,2-c]quinolin-9-yl]-N-[7-[(6-chloro-1,2,3,4-tetrahydroacridin-9-yl)amino]heptyl]propanamide | |
0.0000166 | - |
- |
Homo sapiens | 3-[5-(4-chlorophenyl)-3,4-dihydro-2H-pyrano[3,2-c]quinolin-9-yl]-N-[4-[(6-chloro-1,2,3,4-tetrahydroacridin-9-yl)amino]butyl]propanamide | |
0.0000183 | - |
- |
Homo sapiens | 5-(4-chlorophenyl)-N-[7-[(6-chloro-1,2,3,4-tetrahydroacridin-9-yl)amino]heptyl]-3,4-dihydro-2H-pyrano[3,2-c]quinoline-9-carboxamide | |
0.0000249 | - |
- |
Homo sapiens | 5-(4-chlorophenyl)-N-[9-[(6-chloro-1,2,3,4-tetrahydroacridin-9-yl)amino]nonyl]-3,4-dihydro-2H-pyrano[3,2-c]quinoline-9-carboxamide | |
0.00005 | - |
- |
Homo sapiens | 5-(4-chlorophenyl)-N-[10-[(6-chloro-1,2,3,4-tetrahydroacridin-9-yl)amino]decyl]-3,4-dihydro-2H-pyrano[3,2-c]quinoline-9-carboxamide | |
0.000205 | - |
- |
Homo sapiens | tacrine |