Assay Detail
Binding
CHEMBL4815504
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Inhibition of rat cortex homogenate acetylcholinesterase using acetylthiocholine iodide as substrate incubated for 20 mins by Ellman's method
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cortex |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Kinetics-Driven Drug Design Strategy for Next-Generation Acetylcholinesterase Inhibitors to Clinical Candidate.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 7.57 | 9.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4859647 | — | — | 1 | 9.07 |
| CHEMBL4846450 | — | — | 1 | 9.02 |
| CHEMBL502 | DONEPEZIL | 4.0 | 1 | 8.70 |
| CHEMBL4857100 | — | — | 1 | 8.70 |
| CHEMBL4857791 | — | — | 1 | 8.57 |
| CHEMBL4853698 | — | — | 1 | 8.52 |
| CHEMBL4867751 | — | — | 1 | 8.46 |
| CHEMBL4860655 | — | — | 1 | 8.45 |
| CHEMBL4856312 | — | — | 1 | 8.43 |
| CHEMBL4860419 | — | — | 1 | 8.40 |
| CHEMBL4846622 | — | — | 1 | 8.36 |
| CHEMBL4867225 | — | — | 1 | 8.34 |
| CHEMBL4848806 | — | — | 1 | 8.27 |
| CHEMBL4864695 | — | — | 1 | 8.23 |
| CHEMBL4851135 | — | — | 1 | 8.20 |
| CHEMBL4877719 | — | — | 1 | 8.08 |
| CHEMBL4863392 | — | — | 1 | 7.93 |
| CHEMBL4864886 | — | — | 1 | 7.85 |
| CHEMBL4860777 | — | — | 1 | 7.74 |
| CHEMBL4873794 | — | — | 1 | 7.65 |
| CHEMBL4854986 | — | — | 1 | 7.60 |
| CHEMBL4871360 | — | — | 1 | 7.55 |
| CHEMBL4877366 | — | — | 1 | 7.35 |
| CHEMBL4851673 | — | — | 1 | 7.23 |
| CHEMBL4846857 | — | — | 1 | 7.22 |
| CHEMBL4857091 | — | — | 1 | 7.18 |
| CHEMBL4868720 | — | — | 1 | 7.17 |
| CHEMBL4856424 | — | — | 1 | 7.12 |
| CHEMBL4867651 | — | — | 1 | 6.79 |
| CHEMBL4869273 | — | — | 1 | 6.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4859647 | — | IC50 | = | 0.86 | nM | 9.07 |
| CHEMBL4846450 | — | IC50 | = | 0.96 | nM | 9.02 |
| CHEMBL4857100 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL502 | DONEPEZIL | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4857791 | — | IC50 | = | 2.67 | nM | 8.57 |
| CHEMBL4853698 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4867751 | — | IC50 | = | 3.44 | nM | 8.46 |
| CHEMBL4860655 | — | IC50 | = | 3.52 | nM | 8.45 |
| CHEMBL4856312 | — | IC50 | = | 3.71 | nM | 8.43 |
| CHEMBL4860419 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4846622 | — | IC50 | = | 4.33 | nM | 8.36 |
| CHEMBL4867225 | — | IC50 | = | 4.59 | nM | 8.34 |
| CHEMBL4848806 | — | IC50 | = | 5.39 | nM | 8.27 |
| CHEMBL4864695 | — | IC50 | = | 5.87 | nM | 8.23 |
| CHEMBL4851135 | — | IC50 | = | 6.29 | nM | 8.20 |
| CHEMBL4877719 | — | IC50 | = | 8.33 | nM | 8.08 |
| CHEMBL4863392 | — | IC50 | = | 11.7 | nM | 7.93 |
| CHEMBL4864886 | — | IC50 | = | 14.1 | nM | 7.85 |
| CHEMBL4860777 | — | IC50 | = | 18.3 | nM | 7.74 |
| CHEMBL4873794 | — | IC50 | = | 22.5 | nM | 7.65 |
| CHEMBL4854986 | — | IC50 | = | 25.3 | nM | 7.60 |
| CHEMBL4871360 | — | IC50 | = | 28.3 | nM | 7.55 |
| CHEMBL4877366 | — | IC50 | = | 44.9 | nM | 7.35 |
| CHEMBL4851673 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL4846857 | — | IC50 | = | 60.5 | nM | 7.22 |
| CHEMBL4857091 | — | IC50 | = | 66.7 | nM | 7.18 |
| CHEMBL4868720 | — | IC50 | = | 67.3 | nM | 7.17 |
| CHEMBL4856424 | — | IC50 | = | 75.7 | nM | 7.12 |
| CHEMBL4867651 | — | IC50 | = | 163.0 | nM | 6.79 |
| CHEMBL4869273 | — | IC50 | = | 176.0 | nM | 6.75 |
| CHEMBL4876130 | — | IC50 | = | 181.0 | nM | 6.74 |
| CHEMBL4877089 | — | IC50 | = | 226.0 | nM | 6.65 |
| CHEMBL4863729 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL4856120 | — | IC50 | = | 306.0 | nM | 6.51 |
| CHEMBL4871843 | — | IC50 | = | 348.0 | nM | 6.46 |
| CHEMBL4850869 | — | IC50 | = | 404.0 | nM | 6.39 |
| CHEMBL4860492 | — | IC50 | = | 646.0 | nM | 6.19 |
| CHEMBL4869023 | — | IC50 | = | 1640.0 | nM | 5.79 |
| CHEMBL4858969 | — | IC50 | = | 8780.0 | nM | 5.06 |