Assay Detail
Binding
CHEMBL917586
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Inhibition of porcine liver carboxylesterase using [14C]GS-7340 substrate
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Sus scrofa |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Cathepsin A is the major hydrolase catalyzing the intracellular hydrolysis of the antiretroviral nucleotide phosphonoamidate prodrugs GS-7340 and GS-9131.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 7.30 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1025 | ISOFLUROPHATE | 4.0 | 1 | 7.30 |
| CHEMBL24983 | — | — | 1 | - |
| CHEMBL374508 | E-64 | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1025 | ISOFLUROPHATE | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL24983 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL374508 | E-64 | IC50 | > | 300000.0 | nM | - |