Assay Detail
Binding
CHEMBL965675
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Inhibition of rat AChE
10
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Exploiting protein fluctuations at the active-site gorge of human cholinesterases: further optimization of the design strategy to develop extremely potent inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.70 | 8.82 |
| Ki | 1 | 7.71 | 7.71 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL258928 | — | — | 1 | 8.82 |
| CHEMBL32823 | — | — | 1 | 8.82 |
| CHEMBL76658 | — | — | 1 | 8.06 |
| CHEMBL484705 | — | — | 1 | 8.06 |
| CHEMBL519154 | — | — | 2 | 7.71 |
| CHEMBL179732 | — | — | 1 | 7.55 |
| CHEMBL395280 | HUPERZINE A | 2.0 | 2 | 6.94 |
| CHEMBL483090 | — | — | 1 | 6.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL258928 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL32823 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL76658 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL484705 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL519154 | — | Ki | = | 19.6 | nM | 7.71 |
| CHEMBL179732 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL519154 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL395280 | HUPERZINE A | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL395280 | HUPERZINE A | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL483090 | — | IC50 | = | 151.0 | nM | 6.82 |