Assay Detail
Binding
CHEMBL5621144
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Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured after 20 mins by DTNB reagent based Ellman's method
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Equus caballus |
| Tissue | Serum |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Sulfur-fluoride exchange (SuFEx)-enabled lead discovery of AChE inhibitors by fragment linking strategies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 5.36 | 7.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL636 | RIVASTIGMINE | 4.0 | 1 | 7.28 |
| CHEMBL5624584 | — | — | 1 | 5.48 |
| CHEMBL5630661 | — | — | 1 | 5.30 |
| CHEMBL5630544 | — | — | 1 | 5.10 |
| CHEMBL502 | DONEPEZIL | 4.0 | 1 | 5.01 |
| CHEMBL5624445 | — | — | 1 | 4.97 |
| CHEMBL5630831 | — | — | 1 | 4.92 |
| CHEMBL5624533 | — | — | 1 | 4.85 |
| CHEMBL5629983 | — | — | 1 | - |
| CHEMBL5630220 | — | — | 1 | - |
| CHEMBL5625068 | — | — | 1 | - |
| CHEMBL5624473 | — | — | 1 | - |
| CHEMBL5624757 | — | — | 1 | - |
| CHEMBL5630049 | — | — | 1 | - |
| CHEMBL5630704 | — | — | 1 | - |
| CHEMBL5624457 | — | — | 1 | - |
| CHEMBL5630674 | — | — | 1 | - |
| CHEMBL5624597 | — | — | 1 | - |
| CHEMBL5629892 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL636 | RIVASTIGMINE | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL5624584 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL5630661 | — | IC50 | = | 5030.0 | nM | 5.30 |
| CHEMBL5630544 | — | IC50 | = | 7980.0 | nM | 5.10 |
| CHEMBL502 | DONEPEZIL | IC50 | = | 9830.0 | nM | 5.01 |
| CHEMBL5624445 | — | IC50 | = | 10690.0 | nM | 4.97 |
| CHEMBL5630831 | — | IC50 | = | 11970.0 | nM | 4.92 |
| CHEMBL5624533 | — | IC50 | = | 14020.0 | nM | 4.85 |
| CHEMBL5629983 | — | IC50 | - | — | - | |
| CHEMBL5630220 | — | IC50 | - | — | - | |
| CHEMBL5625068 | — | IC50 | - | — | - | |
| CHEMBL5624473 | — | IC50 | - | — | - | |
| CHEMBL5624757 | — | IC50 | - | — | - | |
| CHEMBL5630049 | — | IC50 | - | — | - | |
| CHEMBL5630704 | — | IC50 | - | — | - | |
| CHEMBL5624457 | — | IC50 | - | — | - | |
| CHEMBL5630674 | — | IC50 | - | — | - | |
| CHEMBL5624597 | — | IC50 | - | — | - | |
| CHEMBL5629892 | — | IC50 | - | — | - |