Assay Detail
Binding
CHEMBL5355282
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Inhibition of human AChE using acetylthiocholine as substrate preincubated for 5 mins followed by substrate addition and measured after 2 mins by Perkin elmer based spectrophotometer analysis
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel slow-binding reversible acetylcholinesterase inhibitors based on uracil moieties for possible treatment of myasthenia gravis and protection from organophosphate poisoning.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 8.88 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5417346 | — | — | 1 | 10.00 |
| CHEMBL5419243 | — | — | 1 | 9.70 |
| CHEMBL5440753 | — | — | 1 | 9.40 |
| CHEMBL5426103 | — | — | 1 | 9.30 |
| CHEMBL5434553 | — | — | 1 | 9.22 |
| CHEMBL5417632 | — | — | 1 | 9.00 |
| CHEMBL5418455 | — | — | 1 | 8.70 |
| CHEMBL5396497 | — | — | 1 | 8.15 |
| CHEMBL812 | PYRIDOSTIGMINE BROMIDE | 4.0 | 1 | 6.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5417346 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL5419243 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL5440753 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL5426103 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL5434553 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL5417632 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5418455 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5396497 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL812 | PYRIDOSTIGMINE BROMIDE | IC50 | = | 350.0 | nM | 6.46 |