Assay Detail
Binding
CHEMBL3888432
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Cell-Based Assay: PheG Assay: Two ß-glucuronidase activity assays were employed to examine the potency of inhibitors both in vitro and in cell-based studies. An absorbance assay based on the conversion of p-nitrophenyl glucuronide (PNPG) to p-nitrophenol (PNP) (Szasz (1967) Clin Chem 13:752-759), which absorbs at 410 nm, was employed as the primary in vitro assay. A secondary assay involving the conversion of phenolphthalein glucuronide (PheG) to phenolphthalein (Phe), which absorbs at 540 nm, was also employed. Id. Both assays were validated in vitro and in living cells, and the wavelengths monitored did not overlap with absorbance characteristics of putative inhibitors.
17
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Selective β-glucuronidase inhibitors as a treatment for side effects of camptothecin antineoplastic agents
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.52 | 9.01 |
| EC50 | 8 | 6.90 | 8.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3980115 | — | — | 2 | 9.01 |
| CHEMBL3903683 | — | — | 2 | 7.54 |
| CHEMBL1236932 | — | — | 2 | 7.48 |
| CHEMBL2335167 | — | — | 2 | 7.00 |
| CHEMBL1236933 | — | — | 2 | 6.66 |
| CHEMBL3922222 | — | — | 2 | 6.14 |
| CHEMBL3916758 | — | — | 2 | 6.04 |
| CHEMBL3938333 | — | — | 2 | 5.97 |
| CHEMBL3925625 | — | — | 1 | 5.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3980115 | — | IC50 | = | 0.984 | nM | 9.01 |
| CHEMBL3980115 | — | EC50 | = | 3.41 | nM | 8.47 |
| CHEMBL3903683 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL1236932 | — | EC50 | = | 33.2 | nM | 7.48 |
| CHEMBL2335167 | — | EC50 | = | 99.9 | nM | 7.00 |
| CHEMBL2335167 | — | IC50 | = | 212.6 | nM | 6.67 |
| CHEMBL1236933 | — | EC50 | = | 221.2 | nM | 6.66 |
| CHEMBL3903683 | — | IC50 | = | 277.3 | nM | 6.56 |
| CHEMBL1236932 | — | IC50 | = | 377.8 | nM | 6.42 |
| CHEMBL1236933 | — | IC50 | = | 600.8 | nM | 6.22 |
| CHEMBL3922222 | — | IC50 | = | 721.7 | nM | 6.14 |
| CHEMBL3922222 | — | EC50 | = | 793.1 | nM | 6.10 |
| CHEMBL3916758 | — | EC50 | = | 913.3 | nM | 6.04 |
| CHEMBL3938333 | — | IC50 | = | 1067.2 | nM | 5.97 |
| CHEMBL3916758 | — | IC50 | = | 1266.4 | nM | 5.90 |
| CHEMBL3938333 | — | EC50 | = | 1302.5 | nM | 5.88 |
| CHEMBL3925625 | — | IC50 | = | 1688.9 | nM | 5.77 |