Assay Detail
Binding
CHEMBL641387
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Inhibition of acetylcholinesterase activity in rat cerebral cortex homogenate, in the presence of a specific butyrylcholinesterase (BChE) inhibitor; ethopropazine
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebral cortex |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Heterodimeric tacrine-based acetylcholinesterase inhibitors: investigating ligand-peripheral site interactions.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 7.15 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL555320 | — | — | 1 | 8.82 |
| CHEMBL557225 | — | — | 1 | 8.11 |
| CHEMBL542236 | — | — | 1 | 8.06 |
| CHEMBL545539 | — | — | 1 | 8.00 |
| CHEMBL542234 | — | — | 1 | 7.89 |
| CHEMBL543906 | — | — | 1 | 7.87 |
| CHEMBL544369 | — | — | 1 | 7.41 |
| CHEMBL539811 | — | — | 1 | 7.35 |
| CHEMBL541853 | — | — | 1 | 7.33 |
| CHEMBL542732 | — | — | 1 | 7.28 |
| CHEMBL542477 | — | — | 1 | 7.15 |
| CHEMBL543667 | — | — | 1 | 7.08 |
| CHEMBL544605 | — | — | 1 | 7.05 |
| CHEMBL545774 | — | — | 1 | 6.88 |
| CHEMBL540837 | — | — | 1 | 6.83 |
| CHEMBL544143 | — | — | 1 | 6.75 |
| CHEMBL544603 | — | — | 1 | 6.75 |
| CHEMBL1677 | TACRINE HYDROCHLORIDE | 4.0 | 1 | 6.65 |
| CHEMBL542482 | — | — | 1 | 6.58 |
| CHEMBL538533 | — | — | 1 | 6.58 |
| CHEMBL540830 | — | — | 1 | 6.50 |
| CHEMBL58146 | QUINOLIN-4-AMINE | — | 1 | 4.29 |
| CHEMBL284348 | DALFAMPRIDINE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL555320 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL557225 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL542236 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL545539 | — | IC50 | = | 10.1 | nM | 8.00 |
| CHEMBL542234 | — | IC50 | = | 12.8 | nM | 7.89 |
| CHEMBL543906 | — | IC50 | = | 13.6 | nM | 7.87 |
| CHEMBL544369 | — | IC50 | = | 38.7 | nM | 7.41 |
| CHEMBL539811 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL541853 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL542732 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL542477 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL543667 | — | IC50 | = | 83.6 | nM | 7.08 |
| CHEMBL544605 | — | IC50 | = | 89.4 | nM | 7.05 |
| CHEMBL545774 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL540837 | — | IC50 | = | 147.0 | nM | 6.83 |
| CHEMBL544143 | — | IC50 | = | 176.0 | nM | 6.75 |
| CHEMBL544603 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL1677 | TACRINE HYDROCHLORIDE | IC50 | = | 223.0 | nM | 6.65 |
| CHEMBL542482 | — | IC50 | = | 261.0 | nM | 6.58 |
| CHEMBL538533 | — | IC50 | = | 264.0 | nM | 6.58 |
| CHEMBL540830 | — | IC50 | = | 319.0 | nM | 6.50 |
| CHEMBL58146 | QUINOLIN-4-AMINE | IC50 | = | 50700.0 | nM | 4.29 |
| CHEMBL284348 | DALFAMPRIDINE | IC50 | > | 500000.0 | nM | - |