Assay Detail
Binding
CHEMBL4844511
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Inhibition of equine serum BuChE using butyrylthiocholine as substrate incubated for 5 mins followed by substrate addition and measured after 5 mins by spectrophotometric based Ellman's method
22
Total Activities
22
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
Discovery of 1-(phenylsulfonyl)-1H-indole-based multifunctional ligands targeting cholinesterases and 5-HT<sub>6</sub> receptor with anti-aggregation properties against amyloid-beta and tau.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 6.51 | 8.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4848231 | — | — | 1 | 8.66 |
| CHEMBL4877482 | — | — | 1 | 8.39 |
| CHEMBL4874513 | — | — | 1 | 8.03 |
| CHEMBL95 | TACRINE | 4.0 | 1 | 7.82 |
| CHEMBL4850051 | — | — | 1 | 7.73 |
| CHEMBL4850546 | — | — | 1 | 7.61 |
| CHEMBL4871964 | — | — | 1 | 6.41 |
| CHEMBL4845823 | — | — | 1 | 6.34 |
| CHEMBL4878361 | — | — | 1 | 6.28 |
| CHEMBL4878383 | — | — | 1 | 6.23 |
| CHEMBL4866788 | — | — | 1 | 6.15 |
| CHEMBL4850488 | — | — | 1 | 6.05 |
| CHEMBL4847532 | — | — | 1 | 5.97 |
| CHEMBL4864206 | — | — | 1 | 5.97 |
| CHEMBL4852099 | — | — | 1 | 5.88 |
| CHEMBL4847373 | — | — | 1 | 5.78 |
| CHEMBL502 | DONEPEZIL | 4.0 | 1 | 5.74 |
| CHEMBL4863218 | — | — | 1 | 5.70 |
| CHEMBL4868597 | — | — | 1 | 5.68 |
| CHEMBL4854972 | — | — | 1 | 5.67 |
| CHEMBL636 | RIVASTIGMINE | 4.0 | 1 | 5.66 |
| CHEMBL4851595 | — | — | 1 | 5.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4848231 | — | IC50 | = | 2.17 | nM | 8.66 |
| CHEMBL4877482 | — | IC50 | = | 4.07 | nM | 8.39 |
| CHEMBL4874513 | — | IC50 | = | 9.39 | nM | 8.03 |
| CHEMBL95 | TACRINE | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4850051 | — | IC50 | = | 18.76 | nM | 7.73 |
| CHEMBL4850546 | — | IC50 | = | 24.39 | nM | 7.61 |
| CHEMBL4871964 | — | IC50 | = | 393.7 | nM | 6.41 |
| CHEMBL4845823 | — | IC50 | = | 454.5 | nM | 6.34 |
| CHEMBL4878361 | — | IC50 | = | 527.9 | nM | 6.28 |
| CHEMBL4878383 | — | IC50 | = | 585.7 | nM | 6.23 |
| CHEMBL4866788 | — | IC50 | = | 701.4 | nM | 6.15 |
| CHEMBL4850488 | — | IC50 | = | 887.4 | nM | 6.05 |
| CHEMBL4847532 | — | IC50 | = | 1075.0 | nM | 5.97 |
| CHEMBL4864206 | — | IC50 | = | 1067.0 | nM | 5.97 |
| CHEMBL4852099 | — | IC50 | = | 1304.0 | nM | 5.88 |
| CHEMBL4847373 | — | IC50 | = | 1661.0 | nM | 5.78 |
| CHEMBL502 | DONEPEZIL | IC50 | = | 1830.0 | nM | 5.74 |
| CHEMBL4863218 | — | IC50 | = | 1991.0 | nM | 5.70 |
| CHEMBL4868597 | — | IC50 | = | 2071.0 | nM | 5.68 |
| CHEMBL4854972 | — | IC50 | = | 2118.0 | nM | 5.67 |
| CHEMBL636 | RIVASTIGMINE | IC50 | = | 2195.0 | nM | 5.66 |
| CHEMBL4851595 | — | IC50 | = | 4263.0 | nM | 5.37 |