Assay Detail
Binding
CHEMBL1787217
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Inhibition of Equine serum BChE using butyrylthiocholine iodide as a substrate after 20 mins by Ellman's assay
45
Total Activities
45
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
Quinolizidinyl derivatives of bi- and tricyclic systems as potent inhibitors of acetyl- and butyrylcholinesterase with potential in Alzheimer's disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 45 | 5.82 | 6.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1782718 | — | — | 1 | 6.82 |
| CHEMBL251940 | PERICIAZINE | 2.0 | 1 | 6.64 |
| CHEMBL1782742 | — | — | 1 | 6.47 |
| CHEMBL1782719 | — | — | 1 | 6.39 |
| CHEMBL1782733 | — | — | 1 | 6.37 |
| CHEMBL1782735 | — | — | 1 | 6.33 |
| CHEMBL1782709 | — | — | 1 | 6.29 |
| CHEMBL1782724 | — | — | 1 | 6.20 |
| CHEMBL1782743 | — | — | 1 | 6.16 |
| CHEMBL1206 | ETHOPROPAZINE | 4.0 | 1 | 6.14 |
| CHEMBL1782737 | — | — | 1 | 6.13 |
| CHEMBL1782736 | — | — | 1 | 6.12 |
| CHEMBL1782730 | — | — | 1 | 6.08 |
| CHEMBL1782739 | — | — | 1 | 6.07 |
| CHEMBL1782741 | — | — | 1 | 6.06 |
| CHEMBL1782714 | — | — | 1 | 6.06 |
| CHEMBL1782738 | — | — | 1 | 6.05 |
| CHEMBL1782721 | — | — | 1 | 6.03 |
| CHEMBL1782720 | — | — | 1 | 6.02 |
| CHEMBL1782713 | — | — | 1 | 5.96 |
| CHEMBL1782725 | — | — | 1 | 5.96 |
| CHEMBL1782734 | — | — | 1 | 5.92 |
| CHEMBL1782715 | — | — | 1 | 5.85 |
| CHEMBL1201342 | METHIXENE | 4.0 | 1 | 5.80 |
| CHEMBL1782723 | — | — | 1 | 5.70 |
| CHEMBL1782712 | — | — | 1 | 5.70 |
| CHEMBL1782708 | LUPINYLPHENOTHIAZINE | — | 1 | 5.70 |
| CHEMBL1782711 | — | — | 1 | 5.66 |
| CHEMBL1782717 | — | — | 1 | 5.66 |
| CHEMBL1782716 | — | — | 1 | 5.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1782718 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL251940 | PERICIAZINE | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL1782742 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL1782719 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL1782733 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL1782735 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL1782709 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL1782724 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL1782743 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL1206 | ETHOPROPAZINE | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL1782737 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL1782736 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL1782730 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL1782739 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL1782714 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL1782741 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL1782738 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL1782721 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL1782720 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL1782713 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1782725 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1782734 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL1782715 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL1201342 | METHIXENE | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL1782723 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL1782712 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL1782708 | LUPINYLPHENOTHIAZINE | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL1782711 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL1782717 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL1782716 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL1782731 | HOMOLUPINANOYLPHENOTHIAZINE | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL609132 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL1782729 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL1782728 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL1782710 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL1782722 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL1782747 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL7568 | QUINACRINE | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL1782744 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL1782732 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL1782746 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL1782727 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL1782748 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL570 | TRIFLUPROMAZINE | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL1782726 | — | IC50 | = | 8100.0 | nM | 5.09 |