Assay Detail
Binding
CHEMBL3082114
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Inhibition of carboxylesterase in Fischer 344 Rattus norvegicus (rat) liver microsomes using p-nitrophenyl acetate as substrate incubated for 5 min prior to substrate addition measured for 2 min by spectrophotometric analysis
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Liver |
| Subcellular | Microsomes |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis of new carboxylesterase inhibitors and evaluation of potency and water solubility.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.07 | 8.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL467451 | — | — | 1 | 8.20 |
| CHEMBL467450 | — | — | 1 | 7.99 |
| CHEMBL460807 | — | — | 1 | 7.61 |
| CHEMBL89506 | — | — | 1 | 7.43 |
| CHEMBL440542 | — | — | 1 | 7.26 |
| CHEMBL270374 | — | — | 1 | 6.94 |
| CHEMBL460809 | — | — | 1 | 6.79 |
| CHEMBL270375 | — | — | 1 | 6.79 |
| CHEMBL449775 | — | — | 1 | 5.89 |
| CHEMBL2268509 | — | — | 1 | 5.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL467451 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL467450 | — | IC50 | = | 10.3 | nM | 7.99 |
| CHEMBL460807 | — | IC50 | = | 24.5 | nM | 7.61 |
| CHEMBL89506 | — | IC50 | = | 37.2 | nM | 7.43 |
| CHEMBL440542 | — | IC50 | = | 54.6 | nM | 7.26 |
| CHEMBL270374 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL460809 | — | IC50 | = | 162.0 | nM | 6.79 |
| CHEMBL270375 | — | IC50 | = | 164.0 | nM | 6.79 |
| CHEMBL449775 | — | IC50 | = | 1290.0 | nM | 5.89 |
| CHEMBL2268509 | — | IC50 | = | 1500.0 | nM | 5.82 |