Assay Detail
Binding
CHEMBL752982
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Inhibition of neutral endopeptidase (NEP).
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis of constrained thiorphan analogs as inhibitors of neutral endopeptidase
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 8.71 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL63123 | — | — | 1 | 9.70 |
| CHEMBL294536 | — | — | 1 | 9.52 |
| CHEMBL304233 | — | — | 1 | 9.40 |
| CHEMBL294760 | — | — | 1 | 9.30 |
| CHEMBL62535 | — | — | 1 | 9.22 |
| CHEMBL65610 | — | — | 1 | 9.22 |
| CHEMBL61512 | (R)-THIORPHAN | — | 1 | 8.80 |
| CHEMBL298827 | (S)-THIORPHAN | — | 1 | 8.72 |
| CHEMBL433492 | — | — | 1 | 8.70 |
| CHEMBL63096 | — | — | 1 | 8.40 |
| CHEMBL62957 | — | — | 1 | 8.30 |
| CHEMBL64661 | — | — | 1 | 8.15 |
| CHEMBL431957 | — | — | 1 | 8.00 |
| CHEMBL61840 | — | — | 1 | 7.85 |
| CHEMBL293477 | — | — | 1 | 7.35 |
| CHEMBL64847 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL63123 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL294536 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL304233 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL294760 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL62535 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL65610 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL61512 | (R)-THIORPHAN | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL298827 | (S)-THIORPHAN | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL433492 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL63096 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL62957 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL64661 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL431957 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL61840 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL293477 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL64847 | — | Ki | > | 300.0 | nM | - |