Assay Detail
Binding
CHEMBL3124385
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human serum BChE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition measured after 5 mins by Ellman's method
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
1,2,3,4-Tetrahydrobenzo[h][1,6]naphthyridines as a new family of potent peripheral-to-midgorge-site inhibitors of acetylcholinesterase: synthesis, pharmacological evaluation and mechanistic studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 5.94 | 7.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL95 | TACRINE | 4.0 | 1 | 7.34 |
| CHEMBL3122167 | — | — | 1 | 6.04 |
| CHEMBL3122168 | — | — | 1 | 5.86 |
| CHEMBL3122169 | — | — | 1 | 5.59 |
| CHEMBL345124 | PROPIDIUM | — | 1 | 4.88 |
| CHEMBL3122150 | — | — | 1 | - |
| CHEMBL3122145 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL95 | TACRINE | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL3122167 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL3122168 | — | IC50 | = | 1370.0 | nM | 5.86 |
| CHEMBL3122169 | — | IC50 | = | 2590.0 | nM | 5.59 |
| CHEMBL345124 | PROPIDIUM | IC50 | = | 13200.0 | nM | 4.88 |
| CHEMBL3122150 | — | IC50 | - | — | - | |
| CHEMBL3122145 | — | IC50 | - | — | - |