Assay Detail
Binding
CHEMBL861175
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Anticholinesterase activity against human plasma BChE
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Plasma |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 6.71 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL381926 | — | — | 1 | 8.70 |
| CHEMBL204895 | — | — | 1 | 8.52 |
| CHEMBL205340 | — | — | 1 | 8.40 |
| CHEMBL205231 | — | — | 1 | 8.40 |
| CHEMBL433041 | EPTASTIGMINE | 2.0 | 1 | 8.30 |
| CHEMBL206642 | — | — | 1 | 7.89 |
| CHEMBL204732 | — | — | 1 | 7.82 |
| CHEMBL94 | PHYSOSTIGMINE | 3.0 | 1 | 7.80 |
| CHEMBL382207 | — | — | 1 | 7.77 |
| CHEMBL380830 | — | — | 1 | 7.64 |
| CHEMBL205826 | — | — | 1 | 7.64 |
| CHEMBL377283 | — | — | 1 | 7.55 |
| CHEMBL636 | RIVASTIGMINE | 4.0 | 1 | 7.43 |
| CHEMBL206237 | — | — | 1 | 7.40 |
| CHEMBL95 | TACRINE | 4.0 | 1 | 7.33 |
| CHEMBL129837 | 4-ISOPROPYLPHENSERINE | — | 1 | 7.30 |
| CHEMBL205321 | — | — | 1 | 7.27 |
| CHEMBL205940 | — | — | 1 | 7.25 |
| CHEMBL205967 | — | — | 1 | 6.92 |
| CHEMBL494887 | TETRAISOPROPYL PYROPHOSPHORAMIDE | — | 1 | 6.01 |
| CHEMBL381782 | — | — | 1 | 5.93 |
| CHEMBL205895 | — | — | 1 | 5.81 |
| CHEMBL54727 | — | — | 1 | 5.81 |
| CHEMBL130458 | TOLSERINE | — | 1 | 5.71 |
| CHEMBL382351 | — | — | 1 | 5.60 |
| CHEMBL502 | DONEPEZIL | 4.0 | 1 | 5.38 |
| CHEMBL383013 | — | — | 1 | 5.29 |
| CHEMBL205335 | — | — | 1 | 5.29 |
| CHEMBL659 | GALANTAMINE | 4.0 | 1 | 5.14 |
| CHEMBL426674 | — | — | 1 | 4.94 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL381926 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL204895 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL205340 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL205231 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL433041 | EPTASTIGMINE | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL206642 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL204732 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL94 | PHYSOSTIGMINE | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL382207 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL380830 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL205826 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL377283 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL636 | RIVASTIGMINE | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL206237 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL95 | TACRINE | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL129837 | 4-ISOPROPYLPHENSERINE | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL205321 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL205940 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL205967 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL494887 | TETRAISOPROPYL PYROPHOSPHORAMIDE | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL381782 | — | IC50 | = | 1180.0 | nM | 5.93 |
| CHEMBL205895 | — | IC50 | = | 1560.0 | nM | 5.81 |
| CHEMBL54727 | — | IC50 | = | 1560.0 | nM | 5.81 |
| CHEMBL130458 | TOLSERINE | IC50 | = | 1950.0 | nM | 5.71 |
| CHEMBL382351 | — | IC50 | = | 2490.0 | nM | 5.60 |
| CHEMBL502 | DONEPEZIL | IC50 | = | 4150.0 | nM | 5.38 |
| CHEMBL383013 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL205335 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL659 | GALANTAMINE | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL426674 | — | IC50 | = | 11400.0 | nM | 4.94 |
| CHEMBL206093 | — | IC50 | = | 36400.0 | nM | 4.44 |
| CHEMBL464538 | — | IC50 | = | 48000.0 | nM | 4.32 |
| CHEMBL378404 | — | IC50 | = | 52000.0 | nM | 4.28 |
| CHEMBL395280 | HUPERZINE A | IC50 | > | 10000.0 | nM | - |