Assay Detail
Binding
CHEMBL3369130
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Inhibition of human AChE
29
Total Activities
15
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
Amine substitution of quinazolinones leads to selective nanomolar AChE inhibitors with 'inverted' binding mode.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 6.10 | 7.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3323035 | — | — | 1 | 7.47 |
| CHEMBL95 | TACRINE | 4.0 | 2 | 7.15 |
| CHEMBL3323036 | — | — | 2 | 6.85 |
| CHEMBL3323039 | — | — | 2 | 6.70 |
| CHEMBL3323042 | — | — | 2 | 6.67 |
| CHEMBL3323059 | — | — | 2 | 6.65 |
| CHEMBL3323046 | — | — | 2 | 6.27 |
| CHEMBL3323043 | — | — | 2 | 6.17 |
| CHEMBL3323065 | — | — | 2 | 6.09 |
| CHEMBL3323053 | — | — | 2 | 5.97 |
| CHEMBL3323056 | — | — | 2 | 5.92 |
| CHEMBL3323062 | — | — | 2 | 5.82 |
| CHEMBL3323049 | — | — | 2 | 5.38 |
| CHEMBL3323068 | — | — | 2 | 4.92 |
| CHEMBL3323051 | — | — | 2 | 4.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3323035 | — | IC50 | = | 33.9 | nM | 7.47 |
| CHEMBL95 | TACRINE | IC50 | = | 71.5 | nM | 7.15 |
| CHEMBL95 | TACRINE | IC50 | = | 71.61 | nM | 7.14 |
| CHEMBL3323036 | — | IC50 | = | 142.0 | nM | 6.85 |
| CHEMBL3323036 | — | IC50 | = | 142.89 | nM | 6.84 |
| CHEMBL3323039 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3323039 | — | IC50 | = | 200.91 | nM | 6.70 |
| CHEMBL3323042 | — | IC50 | = | 216.0 | nM | 6.67 |
| CHEMBL3323042 | — | IC50 | = | 216.77 | nM | 6.66 |
| CHEMBL3323059 | — | IC50 | = | 224.91 | nM | 6.65 |
| CHEMBL3323059 | — | IC50 | = | 225.0 | nM | 6.65 |
| CHEMBL3323046 | — | IC50 | = | 534.56 | nM | 6.27 |
| CHEMBL3323046 | — | IC50 | = | 535.0 | nM | 6.27 |
| CHEMBL3323043 | — | IC50 | = | 669.88 | nM | 6.17 |
| CHEMBL3323043 | — | IC50 | = | 669.0 | nM | 6.17 |
| CHEMBL3323065 | — | IC50 | = | 820.35 | nM | 6.09 |
| CHEMBL3323065 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL3323053 | — | IC50 | = | 1081.43 | nM | 5.97 |
| CHEMBL3323053 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3323056 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3323056 | — | IC50 | = | 1244.51 | nM | 5.91 |
| CHEMBL3323062 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3323062 | — | IC50 | = | 1531.09 | nM | 5.82 |
| CHEMBL3323049 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL3323049 | — | IC50 | = | 4178.3 | nM | 5.38 |
| CHEMBL3323068 | — | IC50 | = | 12100.0 | nM | 4.92 |
| CHEMBL3323068 | — | IC50 | = | 12078.14 | nM | 4.92 |
| CHEMBL3323051 | — | IC50 | = | 56500.0 | nM | 4.25 |
| CHEMBL3323051 | — | IC50 | = | 56493.7 | nM | 4.25 |