Assay Detail
Binding
CHEMBL4821399
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Inhibition of porcine liver carboxylesterase using 4-NPA as substrate preincubated for 10 mins followed by substrate addition by spectrophotometric analysis
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Sus scrofa |
| Tissue | Liver |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel potent bifunctional carboxylesterase inhibitors based on a polyfluoroalkyl-2-imino-1,3-dione scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 7.11 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4854298 | — | — | 1 | 8.30 |
| CHEMBL4868014 | — | — | 1 | 8.29 |
| CHEMBL4853742 | — | — | 1 | 8.21 |
| CHEMBL4853637 | — | — | 1 | 8.14 |
| CHEMBL4858186 | — | — | 1 | 8.14 |
| CHEMBL4849361 | — | — | 1 | 8.13 |
| CHEMBL4855838 | — | — | 1 | 8.12 |
| CHEMBL4855755 | — | — | 1 | 7.88 |
| CHEMBL4868687 | — | — | 1 | 7.56 |
| CHEMBL4847987 | — | — | 1 | 7.38 |
| CHEMBL4856140 | — | — | 1 | 7.33 |
| CHEMBL4872772 | — | — | 1 | 7.33 |
| CHEMBL4849436 | — | — | 1 | 7.26 |
| CHEMBL4848799 | — | — | 1 | 7.05 |
| CHEMBL4879228 | — | — | 1 | 6.99 |
| CHEMBL4849604 | — | — | 1 | 6.99 |
| CHEMBL4853013 | — | — | 1 | 6.79 |
| CHEMBL4870030 | — | — | 1 | 5.80 |
| CHEMBL1231178 | — | — | 1 | 5.75 |
| CHEMBL4849511 | — | — | 1 | 5.49 |
| CHEMBL4878259 | — | — | 1 | 5.26 |
| CHEMBL4872814 | — | — | 1 | 4.25 |
| CHEMBL153 | TROLOX | — | 1 | - |
| CHEMBL196 | ASCORBIC ACID | 4.0 | 1 | - |
| CHEMBL280998 | CATECHOL | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4854298 | — | IC50 | = | 4.95 | nM | 8.30 |
| CHEMBL4868014 | — | IC50 | = | 5.14 | nM | 8.29 |
| CHEMBL4853742 | — | IC50 | = | 6.14 | nM | 8.21 |
| CHEMBL4853637 | — | IC50 | = | 7.27 | nM | 8.14 |
| CHEMBL4858186 | — | IC50 | = | 7.16 | nM | 8.14 |
| CHEMBL4849361 | — | IC50 | = | 7.41 | nM | 8.13 |
| CHEMBL4855838 | — | IC50 | = | 7.65 | nM | 8.12 |
| CHEMBL4855755 | — | IC50 | = | 13.1 | nM | 7.88 |
| CHEMBL4868687 | — | IC50 | = | 27.8 | nM | 7.56 |
| CHEMBL4847987 | — | IC50 | = | 41.6 | nM | 7.38 |
| CHEMBL4856140 | — | IC50 | = | 47.1 | nM | 7.33 |
| CHEMBL4872772 | — | IC50 | = | 46.7 | nM | 7.33 |
| CHEMBL4849436 | — | IC50 | = | 55.5 | nM | 7.26 |
| CHEMBL4848799 | — | IC50 | = | 89.3 | nM | 7.05 |
| CHEMBL4879228 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL4849604 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL4853013 | — | IC50 | = | 164.0 | nM | 6.79 |
| CHEMBL4870030 | — | IC50 | = | 1570.0 | nM | 5.80 |
| CHEMBL1231178 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4849511 | — | IC50 | = | 3230.0 | nM | 5.49 |
| CHEMBL4878259 | — | IC50 | = | 5540.0 | nM | 5.26 |
| CHEMBL4872814 | — | IC50 | = | 56600.0 | nM | 4.25 |
| CHEMBL153 | TROLOX | IC50 | - | — | - | |
| CHEMBL196 | ASCORBIC ACID | IC50 | - | — | - | |
| CHEMBL280998 | CATECHOL | IC50 | - | — | - |