Assay Detail
Binding
CHEMBL1249049
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Inhibition of human AChE by Ellmans test
106
Total Activities
81
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel carbamates as orally active acetylcholinesterase inhibitors found to improve scopolamine-induced cognition impairment: pharmacophore-based virtual screening, synthesis, and pharmacology.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| logIC50 | 60 | - | - |
| IC50 | 46 | 6.73 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1243360 | — | — | 1 | 8.15 |
| CHEMBL1243329 | — | — | 1 | 8.09 |
| CHEMBL340391 | ETHYLPHENSERINE | — | 2 | 8.00 |
| CHEMBL130270 | — | — | 2 | 7.82 |
| CHEMBL1243359 | — | — | 1 | 7.76 |
| CHEMBL433041 | EPTASTIGMINE | 2.0 | 1 | 7.66 |
| CHEMBL74926 | PHENSERINE | — | 2 | 7.66 |
| CHEMBL337675 | — | — | 2 | 7.58 |
| CHEMBL11833 | — | — | 1 | 7.52 |
| CHEMBL1240668 | — | — | 1 | 7.50 |
| CHEMBL130458 | TOLSERINE | — | 2 | 7.40 |
| CHEMBL1243012 | — | — | 2 | 7.40 |
| CHEMBL1241427 | — | — | 2 | 7.25 |
| CHEMBL94 | PHYSOSTIGMINE | 3.0 | 2 | 7.25 |
| CHEMBL131210 | — | — | 2 | 7.11 |
| CHEMBL502 | DONEPEZIL | 4.0 | 1 | 7.05 |
| CHEMBL205340 | — | — | 2 | 7.03 |
| CHEMBL295462 | — | — | 1 | 7.00 |
| CHEMBL129837 | 4-ISOPROPYLPHENSERINE | — | 2 | 6.96 |
| CHEMBL519475 | — | — | 1 | 6.90 |
| CHEMBL1243298 | QUILOSTIGMINE | 2.0 | 1 | 6.83 |
| CHEMBL1243076 | — | — | 2 | 6.79 |
| CHEMBL1243111 | — | — | 2 | 6.61 |
| CHEMBL131825 | — | — | 2 | 6.54 |
| CHEMBL1243203 | — | — | 2 | 6.48 |
| CHEMBL1241457 | — | — | 2 | 6.41 |
| CHEMBL335167 | — | — | 2 | 6.16 |
| CHEMBL132285 | — | — | 2 | 6.11 |
| CHEMBL95 | TACRINE | 4.0 | 1 | 6.10 |
| CHEMBL1243140 | — | — | 2 | 6.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1243360 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1243329 | — | IC50 | = | 8.11 | nM | 8.09 |
| CHEMBL340391 | ETHYLPHENSERINE | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL130270 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1243359 | — | IC50 | = | 17.3 | nM | 7.76 |
| CHEMBL74926 | PHENSERINE | IC50 | = | 22.1 | nM | 7.66 |
| CHEMBL433041 | EPTASTIGMINE | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL337675 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL11833 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1240668 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL1243012 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL130458 | TOLSERINE | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL1241427 | — | IC50 | = | 56.7 | nM | 7.25 |
| CHEMBL94 | PHYSOSTIGMINE | IC50 | = | 56.7 | nM | 7.25 |
| CHEMBL131210 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL502 | DONEPEZIL | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL205340 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL295462 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL129837 | 4-ISOPROPYLPHENSERINE | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL519475 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL1243298 | QUILOSTIGMINE | IC50 | = | 148.0 | nM | 6.83 |
| CHEMBL1243076 | — | IC50 | = | 160.8 | nM | 6.79 |
| CHEMBL1243111 | — | IC50 | = | 245.3 | nM | 6.61 |
| CHEMBL131825 | — | IC50 | = | 285.0 | nM | 6.54 |
| CHEMBL1243203 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL1241457 | — | IC50 | = | 387.5 | nM | 6.41 |
| CHEMBL335167 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL132285 | — | IC50 | = | 780.4 | nM | 6.11 |
| CHEMBL95 | TACRINE | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL1243140 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL74257 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL1243170 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL1243388 | — | IC50 | = | 3310.0 | nM | 5.48 |
| CHEMBL1243234 | — | IC50 | = | 3560.0 | nM | 5.45 |
| CHEMBL636 | RIVASTIGMINE | IC50 | = | 4150.0 | nM | 5.38 |
| CHEMBL1243268 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL1243269 | — | IC50 | = | 9887.0 | nM | 5.00 |
| CHEMBL1243297 | — | IC50 | = | 41130.0 | nM | 4.39 |
| CHEMBL1241427 | — | logIC50 | = | 1.754 | — | - |
| CHEMBL54014 | — | logIC50 | = | 2.0 | — | - |
| CHEMBL130956 | — | logIC50 | = | 2.15 | — | - |
| CHEMBL1243076 | — | logIC50 | = | 2.206 | — | - |
| CHEMBL205340 | — | logIC50 | = | 1.973 | — | - |
| CHEMBL1242953 | — | IC50 | - | — | - | |
| CHEMBL1242952 | — | IC50 | - | — | - | |
| CHEMBL1242928 | — | IC50 | - | — | - | |
| CHEMBL1242927 | — | IC50 | - | — | - | |
| CHEMBL1242926 | — | IC50 | - | — | - | |
| CHEMBL1243361 | — | IC50 | - | — | - | |
| CHEMBL1243389 | — | IC50 | - | — | - |