Assay Detail
Binding
CHEMBL1060019
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Inhibition of pig kidney NEP by fluorimetry
9
Total Activities
9
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
Synthesis and enzymatic evaluation of novel partially fluorinated thiol dual ACE/NEP inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.86 | 8.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL10247 | THIORPHAN | -1.0 | 1 | 8.21 |
| CHEMBL173287 | — | — | 1 | 7.39 |
| CHEMBL367174 | — | — | 1 | 7.30 |
| CHEMBL540674 | — | — | 1 | 7.10 |
| CHEMBL551145 | — | — | 1 | 6.64 |
| CHEMBL560685 | — | — | 1 | 6.52 |
| CHEMBL560409 | — | — | 1 | 6.37 |
| CHEMBL551622 | — | — | 1 | 6.24 |
| CHEMBL558146 | — | — | 1 | 5.94 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL10247 | THIORPHAN | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL173287 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL367174 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL540674 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL551145 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL560685 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL560409 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL551622 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL558146 | — | IC50 | = | 1150.0 | nM | 5.94 |