Assay Detail
Binding
CHEMBL4257759
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate pretreated for 4.5 mins followed by substrate addition and measured after 2.5 mins by Ellman's method
20
Total Activities
20
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
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 | 20 | 6.53 | 9.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4291154 | — | — | 1 | 9.34 |
| CHEMBL32823 | — | — | 1 | 9.14 |
| CHEMBL4287748 | — | — | 1 | 8.75 |
| CHEMBL95 | TACRINE | 4.0 | 1 | 8.57 |
| CHEMBL4283298 | — | — | 1 | 8.29 |
| CHEMBL4289232 | — | — | 1 | 8.06 |
| CHEMBL4293086 | — | — | 1 | 6.99 |
| CHEMBL4276885 | — | — | 1 | 6.69 |
| CHEMBL4279836 | — | — | 1 | 6.58 |
| CHEMBL4285270 | — | — | 1 | 6.49 |
| CHEMBL4292521 | — | — | 1 | 6.46 |
| CHEMBL3121480 | — | — | 1 | 6.07 |
| CHEMBL4281409 | — | — | 1 | 5.37 |
| CHEMBL3121475 | — | — | 1 | 5.19 |
| CHEMBL3121476 | — | — | 1 | 5.13 |
| CHEMBL4280937 | — | — | 1 | 5.10 |
| CHEMBL3121477 | — | — | 1 | 4.97 |
| CHEMBL4292032 | — | — | 1 | 4.88 |
| CHEMBL382846 | — | — | 1 | 4.41 |
| CHEMBL4284343 | — | — | 1 | 4.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4291154 | — | IC50 | = | 0.4571 | nM | 9.34 |
| CHEMBL32823 | — | IC50 | = | 0.7244 | nM | 9.14 |
| CHEMBL4287748 | — | IC50 | = | 1.778 | nM | 8.75 |
| CHEMBL95 | TACRINE | IC50 | = | 2.692 | nM | 8.57 |
| CHEMBL4283298 | — | IC50 | = | 5.129 | nM | 8.29 |
| CHEMBL4289232 | — | IC50 | = | 8.71 | nM | 8.06 |
| CHEMBL4293086 | — | IC50 | = | 102.33 | nM | 6.99 |
| CHEMBL4276885 | — | IC50 | = | 204.17 | nM | 6.69 |
| CHEMBL4279836 | — | IC50 | = | 263.03 | nM | 6.58 |
| CHEMBL4285270 | — | IC50 | = | 323.59 | nM | 6.49 |
| CHEMBL4292521 | — | IC50 | = | 346.74 | nM | 6.46 |
| CHEMBL3121480 | — | IC50 | = | 851.14 | nM | 6.07 |
| CHEMBL4281409 | — | IC50 | = | 4265.8 | nM | 5.37 |
| CHEMBL3121475 | — | IC50 | = | 6456.54 | nM | 5.19 |
| CHEMBL3121476 | — | IC50 | = | 7413.1 | nM | 5.13 |
| CHEMBL4280937 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL3121477 | — | IC50 | = | 10715.19 | nM | 4.97 |
| CHEMBL4292032 | — | IC50 | = | 13182.57 | nM | 4.88 |
| CHEMBL382846 | — | IC50 | = | 38904.51 | nM | 4.41 |
| CHEMBL4284343 | — | IC50 | = | 85113.8 | nM | 4.07 |