Assay Detail
Binding
CHEMBL674886
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Binding affinity against human leukocyte elastase (HLE) enzyme
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Nonpeptidic inhibitors of human leukocyte elastase. 3. Design, synthesis, X-ray crystallographic analysis, and structure-activity relationships for a series of orally active 3-amino-6-phenylpyridin-2-one trifluoromethyl ketones.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 42 | 7.81 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL307315 | — | — | 1 | 9.15 |
| CHEMBL431864 | — | — | 1 | 8.85 |
| CHEMBL282694 | — | — | 1 | 8.74 |
| CHEMBL354883 | — | — | 1 | 8.60 |
| CHEMBL55210 | — | — | 1 | 8.51 |
| CHEMBL113187 | — | — | 1 | 8.39 |
| CHEMBL11391 | — | — | 1 | 8.35 |
| CHEMBL333835 | — | — | 1 | 8.32 |
| CHEMBL280916 | — | — | 1 | 8.24 |
| CHEMBL304354 | — | — | 1 | 8.22 |
| CHEMBL113110 | — | — | 1 | 8.16 |
| CHEMBL113358 | — | — | 1 | 8.15 |
| CHEMBL275043 | — | — | 1 | 8.10 |
| CHEMBL303165 | — | — | 1 | 8.08 |
| CHEMBL113905 | — | — | 1 | 8.06 |
| CHEMBL325870 | — | — | 1 | 8.06 |
| CHEMBL111955 | — | — | 1 | 8.03 |
| CHEMBL114868 | — | — | 1 | 8.03 |
| CHEMBL113725 | — | — | 1 | 7.89 |
| CHEMBL109306 | — | — | 1 | 7.89 |
| CHEMBL324983 | — | — | 1 | 7.82 |
| CHEMBL113014 | — | — | 1 | 7.82 |
| CHEMBL326238 | — | — | 1 | 7.82 |
| CHEMBL113148 | — | — | 1 | 7.82 |
| CHEMBL278222 | — | — | 1 | 7.80 |
| CHEMBL279250 | — | — | 1 | 7.75 |
| CHEMBL324343 | — | — | 1 | 7.75 |
| CHEMBL424620 | — | — | 1 | 7.64 |
| CHEMBL66520 | — | — | 1 | 7.58 |
| CHEMBL325713 | — | — | 1 | 7.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL307315 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL431864 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL282694 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL354883 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL55210 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL113187 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL11391 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL333835 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL280916 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL304354 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL113110 | — | Ki | = | 6.9 | nM | 8.16 |
| CHEMBL113358 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL275043 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL303165 | — | Ki | = | 8.4 | nM | 8.08 |
| CHEMBL325870 | — | Ki | = | 8.7 | nM | 8.06 |
| CHEMBL113905 | — | Ki | = | 8.8 | nM | 8.06 |
| CHEMBL111955 | — | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL114868 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL113725 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL109306 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL113148 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL113014 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL324983 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL326238 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL278222 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL279250 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL324343 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL424620 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL66520 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL325713 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL113129 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL113409 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL112410 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL325503 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL112924 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL418841 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL13923 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL109396 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL112335 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL323443 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL14516 | — | Ki | = | 469.0 | nM | 6.33 |
| CHEMBL68841 | — | Ki | = | 480.0 | nM | 6.32 |