Assay Detail
Binding
CHEMBL5541253
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Inhibition of human recombinant CES2 activity assessed as fluorescence of the AP product using Benz-AP as substrate
18
Total Activities
18
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
Tight-Binding Small-Molecule Carboxylesterase 2 Inhibitors Reduce Intracellular Irinotecan Activation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.08 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5567105 | — | — | 1 | 7.75 |
| CHEMBL5593400 | — | — | 1 | 7.42 |
| CHEMBL5567018 | — | — | 1 | 7.37 |
| CHEMBL5574747 | — | — | 1 | 7.23 |
| CHEMBL5569141 | — | — | 1 | 7.21 |
| CHEMBL5575498 | — | — | 1 | 7.18 |
| CHEMBL5572109 | — | — | 1 | 7.17 |
| CHEMBL5569484 | — | — | 1 | 7.16 |
| CHEMBL5565903 | — | — | 1 | 6.90 |
| CHEMBL5573951 | — | — | 1 | 6.76 |
| CHEMBL5572084 | — | — | 1 | 6.75 |
| CHEMBL5572424 | — | — | 1 | 6.75 |
| CHEMBL4095302 | — | — | 1 | 6.72 |
| CHEMBL5569676 | — | — | 1 | 6.71 |
| CHEMBL5568952 | — | — | 1 | - |
| CHEMBL5574138 | — | — | 1 | - |
| CHEMBL5573291 | — | — | 1 | - |
| CHEMBL5594347 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5567105 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5593400 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5567018 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL5574747 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL5569141 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL5575498 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL5572109 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL5569484 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL5565903 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL5573951 | — | IC50 | = | 172.0 | nM | 6.76 |
| CHEMBL5572084 | — | IC50 | = | 177.0 | nM | 6.75 |
| CHEMBL5572424 | — | IC50 | = | 178.0 | nM | 6.75 |
| CHEMBL4095302 | — | IC50 | = | 189.0 | nM | 6.72 |
| CHEMBL5569676 | — | IC50 | = | 193.0 | nM | 6.71 |
| CHEMBL5568952 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL5574138 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL5573291 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL5594347 | — | IC50 | - | — | - |