Assay Detail
Binding
CHEMBL2345137
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Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate after 10 mins by Ellman method
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Equus caballus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and biological evaluation of 1,3,4-thiadiazole analogues as novel AChE and BuChE inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 4.91 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54126 | NEOSTIGMINE BROMIDE | 2.0 | 1 | 7.16 |
| CHEMBL396226 | — | — | 1 | 6.54 |
| CHEMBL2337265 | — | — | 1 | 5.67 |
| CHEMBL2337271 | DONEPEZIL HYDROCHLORIDE MONOHYDRATE | — | 1 | 5.12 |
| CHEMBL2337272 | — | — | 1 | 4.77 |
| CHEMBL2337276 | — | — | 1 | 4.72 |
| CHEMBL2337278 | — | — | 1 | 4.58 |
| CHEMBL243254 | — | — | 1 | 4.57 |
| CHEMBL2337280 | — | — | 1 | 4.56 |
| CHEMBL2337269 | — | — | 1 | 4.49 |
| CHEMBL2337268 | — | — | 1 | 4.24 |
| CHEMBL2337263 | — | — | 1 | 4.20 |
| CHEMBL2337267 | — | — | 1 | 4.07 |
| CHEMBL2337261 | — | — | 1 | 4.02 |
| CHEMBL2337279 | — | — | 1 | - |
| CHEMBL2337270 | — | — | 1 | - |
| CHEMBL2337273 | — | — | 1 | - |
| CHEMBL2337274 | — | — | 1 | - |
| CHEMBL2337275 | — | — | 1 | - |
| CHEMBL2337277 | — | — | 1 | - |
| CHEMBL2337262 | — | — | 1 | - |
| CHEMBL2337264 | — | — | 1 | - |
| CHEMBL2337266 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54126 | NEOSTIGMINE BROMIDE | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL396226 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL2337265 | — | IC50 | = | 2160.0 | nM | 5.67 |
| CHEMBL2337271 | DONEPEZIL HYDROCHLORIDE MONOHYDRATE | IC50 | = | 7520.0 | nM | 5.12 |
| CHEMBL2337272 | — | IC50 | = | 17020.0 | nM | 4.77 |
| CHEMBL2337276 | — | IC50 | = | 19060.0 | nM | 4.72 |
| CHEMBL2337278 | — | IC50 | = | 26490.0 | nM | 4.58 |
| CHEMBL243254 | — | IC50 | = | 26740.0 | nM | 4.57 |
| CHEMBL2337280 | — | IC50 | = | 27320.0 | nM | 4.56 |
| CHEMBL2337269 | — | IC50 | = | 32140.0 | nM | 4.49 |
| CHEMBL2337268 | — | IC50 | = | 57320.0 | nM | 4.24 |
| CHEMBL2337263 | — | IC50 | = | 63280.0 | nM | 4.20 |
| CHEMBL2337267 | — | IC50 | = | 84320.0 | nM | 4.07 |
| CHEMBL2337261 | — | IC50 | = | 96340.0 | nM | 4.02 |
| CHEMBL2337279 | — | IC50 | = | 212380.0 | nM | - |
| CHEMBL2337270 | — | IC50 | = | 147620.0 | nM | - |
| CHEMBL2337273 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL2337274 | — | IC50 | = | 196240.0 | nM | - |
| CHEMBL2337275 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL2337277 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL2337262 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL2337264 | — | IC50 | = | 196210.0 | nM | - |
| CHEMBL2337266 | — | IC50 | = | 112410.0 | nM | - |