Assay Detail
Binding
CHEMBL4257760
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of electric eel AChE using acetylthiocholine iodide as substrate pretreated for 4.5 mins followed by substrate addition and measured after 2.5 mins by Ellman's method
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Electrophorus electricus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel bipharmacophoric inhibitors of the cholinesterases with affinity to the muscarinic receptors M<sub>1</sub> and M<sub>2</sub>.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.94 | 10.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL32823 | — | — | 1 | 10.48 |
| CHEMBL4287748 | — | — | 1 | 9.81 |
| CHEMBL4279836 | — | — | 1 | 9.40 |
| CHEMBL4289232 | — | — | 1 | 9.25 |
| CHEMBL4291154 | — | — | 1 | 9.00 |
| CHEMBL4283298 | — | — | 1 | 8.76 |
| CHEMBL95 | TACRINE | 4.0 | 1 | 7.60 |
| CHEMBL4293086 | — | — | 1 | 6.50 |
| CHEMBL4285270 | — | — | 1 | 6.44 |
| CHEMBL4292521 | — | — | 1 | 6.10 |
| CHEMBL4276885 | — | — | 1 | 6.04 |
| CHEMBL3121480 | — | — | 1 | 5.98 |
| CHEMBL3121477 | — | — | 1 | 5.62 |
| CHEMBL4281409 | — | — | 1 | 5.26 |
| CHEMBL3121476 | — | — | 1 | 4.89 |
| CHEMBL3121475 | — | — | 1 | 4.83 |
| CHEMBL4292032 | — | — | 1 | 4.80 |
| CHEMBL4280937 | — | — | 1 | 4.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL32823 | — | IC50 | = | 0.03311 | nM | 10.48 |
| CHEMBL4287748 | — | IC50 | = | 0.1549 | nM | 9.81 |
| CHEMBL4279836 | — | IC50 | = | 0.3981 | nM | 9.40 |
| CHEMBL4289232 | — | IC50 | = | 0.5623 | nM | 9.25 |
| CHEMBL4291154 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4283298 | — | IC50 | = | 1.738 | nM | 8.76 |
| CHEMBL95 | TACRINE | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL4293086 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL4285270 | — | IC50 | = | 363.08 | nM | 6.44 |
| CHEMBL4292521 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL4276885 | — | IC50 | = | 912.01 | nM | 6.04 |
| CHEMBL3121480 | — | IC50 | = | 1047.13 | nM | 5.98 |
| CHEMBL3121477 | — | IC50 | = | 2398.83 | nM | 5.62 |
| CHEMBL4281409 | — | IC50 | = | 5495.41 | nM | 5.26 |
| CHEMBL3121476 | — | IC50 | = | 12882.5 | nM | 4.89 |
| CHEMBL3121475 | — | IC50 | = | 14791.08 | nM | 4.83 |
| CHEMBL4292032 | — | IC50 | = | 15848.93 | nM | 4.80 |
| CHEMBL4280937 | — | IC50 | = | 67608.3 | nM | 4.17 |