Assay Detail
Binding
CHEMBL677612
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In vitro inhibitory activity against human neutrophil elastase (HNE) catalyzed hydrolysis of the synthetic substrate MeO-Suc-Ala- Ala-Pro-Val-pN
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Peptidyl alpha-ketoheterocyclic inhibitors of human neutrophil elastase. 2. Effect of varying the heterocyclic ring on in vitro potency.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 6.86 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL165759 | — | — | 1 | 9.40 |
| CHEMBL354832 | — | — | 1 | 9.26 |
| CHEMBL166401 | — | — | 1 | 9.22 |
| CHEMBL171288 | — | — | 1 | 8.92 |
| CHEMBL169887 | — | — | 1 | 8.80 |
| CHEMBL354883 | — | — | 1 | 8.80 |
| CHEMBL424550 | — | — | 1 | 8.74 |
| CHEMBL108783 | — | — | 1 | 8.52 |
| CHEMBL353441 | — | — | 1 | 7.60 |
| CHEMBL352305 | — | — | 1 | 7.55 |
| CHEMBL165525 | — | — | 1 | 7.39 |
| CHEMBL169268 | — | — | 1 | 7.31 |
| CHEMBL169842 | — | — | 1 | 6.57 |
| CHEMBL355464 | — | — | 1 | 6.48 |
| CHEMBL171086 | — | — | 1 | 6.39 |
| CHEMBL167824 | — | — | 1 | 5.47 |
| CHEMBL168120 | — | — | 1 | 5.37 |
| CHEMBL168761 | — | — | 1 | 5.25 |
| CHEMBL355477 | — | — | 1 | 5.10 |
| CHEMBL169076 | — | — | 1 | 4.92 |
| CHEMBL166859 | — | — | 1 | 4.68 |
| CHEMBL168834 | — | — | 1 | 4.66 |
| CHEMBL169750 | — | — | 1 | 4.10 |
| CHEMBL166598 | — | — | 1 | 4.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL165759 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL354832 | — | Ki | = | 0.55 | nM | 9.26 |
| CHEMBL166401 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL171288 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL169887 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL354883 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL424550 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL108783 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL353441 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL352305 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL165525 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL169268 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL169842 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL355464 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL171086 | — | Ki | = | 410.0 | nM | 6.39 |
| CHEMBL167824 | — | Ki | = | 3400.0 | nM | 5.47 |
| CHEMBL168120 | — | Ki | = | 4300.0 | nM | 5.37 |
| CHEMBL168761 | — | Ki | = | 5600.0 | nM | 5.25 |
| CHEMBL355477 | — | Ki | = | 8000.0 | nM | 5.10 |
| CHEMBL169076 | — | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL166859 | — | Ki | = | 21000.0 | nM | 4.68 |
| CHEMBL168834 | — | Ki | = | 22000.0 | nM | 4.66 |
| CHEMBL169750 | — | Ki | = | 80000.0 | nM | 4.10 |
| CHEMBL166598 | — | Ki | = | 87000.0 | nM | 4.06 |