Assay Detail
Binding
CHEMBL3365756
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Inhibition of human recombinant NEP using Suc-Ala-Ala-Phe-AMC as substrate after 30 mins by fluorimetry
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
New orally active dual enkephalinase inhibitors (DENKIs) for central and peripheral pain treatment.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 8.26 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL51715 | — | — | 1 | 9.15 |
| CHEMBL298827 | (S)-THIORPHAN | — | 1 | 8.82 |
| CHEMBL3298934 | — | — | 1 | 8.82 |
| CHEMBL3298935 | — | — | 1 | 8.70 |
| CHEMBL3298860 | — | — | 1 | 8.60 |
| CHEMBL3298859 | — | — | 1 | 8.54 |
| CHEMBL3298940 | — | — | 1 | 8.46 |
| CHEMBL3298937 | — | — | 1 | 8.09 |
| CHEMBL3298941 | — | — | 1 | 7.75 |
| CHEMBL3298936 | — | — | 1 | 7.62 |
| CHEMBL3298938 | — | — | 1 | 7.36 |
| CHEMBL3298939 | — | — | 1 | 7.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL51715 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL298827 | (S)-THIORPHAN | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL3298934 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL3298935 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL3298860 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL3298859 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL3298940 | — | Ki | = | 3.45 | nM | 8.46 |
| CHEMBL3298937 | — | Ki | = | 8.2 | nM | 8.09 |
| CHEMBL3298941 | — | Ki | = | 17.9 | nM | 7.75 |
| CHEMBL3298936 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL3298938 | — | Ki | = | 44.1 | nM | 7.36 |
| CHEMBL3298939 | — | Ki | = | 59.0 | nM | 7.23 |