Assay Detail
Binding
CHEMBL677603
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibition of human leukocyte elastase mediated hydrolysis of the synthetic substrate MeO-Suc-Ala-Ala-Pro-Val-pNA
39
Total Activities
39
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. 5. Design, synthesis, and X-ray crystallography of a series of orally active 5-aminopyrimidin-6-one-containing trifluoromethyl ketones.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 39 | 7.72 | 9.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL11099 | — | — | 1 | 9.68 |
| CHEMBL442524 | — | — | 1 | 9.02 |
| CHEMBL274123 | — | — | 1 | 8.80 |
| CHEMBL11398 | — | — | 1 | 8.44 |
| CHEMBL11113 | — | — | 1 | 8.31 |
| CHEMBL11391 | — | — | 1 | 8.25 |
| CHEMBL269181 | — | — | 1 | 8.21 |
| CHEMBL11403 | — | — | 1 | 8.18 |
| CHEMBL267093 | — | — | 1 | 8.11 |
| CHEMBL11098 | — | — | 1 | 8.09 |
| CHEMBL11335 | — | — | 1 | 8.09 |
| CHEMBL11347 | — | — | 1 | 8.05 |
| CHEMBL10975 | — | — | 1 | 7.96 |
| CHEMBL274618 | — | — | 1 | 7.82 |
| CHEMBL10869 | — | — | 1 | 7.80 |
| CHEMBL418707 | — | — | 1 | 7.77 |
| CHEMBL11246 | — | — | 1 | 7.75 |
| CHEMBL275558 | — | — | 1 | 7.70 |
| CHEMBL276680 | — | — | 1 | 7.66 |
| CHEMBL276174 | — | — | 1 | 7.64 |
| CHEMBL11144 | — | — | 1 | 7.64 |
| CHEMBL415972 | — | — | 1 | 7.58 |
| CHEMBL274674 | — | — | 1 | 7.57 |
| CHEMBL11032 | — | — | 1 | 7.48 |
| CHEMBL11336 | — | — | 1 | 7.40 |
| CHEMBL273449 | — | — | 1 | 7.40 |
| CHEMBL11383 | — | — | 1 | 7.38 |
| CHEMBL273981 | — | — | 1 | 7.38 |
| CHEMBL274780 | — | — | 1 | 7.37 |
| CHEMBL274567 | — | — | 1 | 7.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL11099 | — | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL442524 | — | Ki | = | 0.96 | nM | 9.02 |
| CHEMBL274123 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL11398 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL11113 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL11391 | — | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL269181 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL11403 | — | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL267093 | — | Ki | = | 7.7 | nM | 8.11 |
| CHEMBL11098 | — | Ki | = | 8.2 | nM | 8.09 |
| CHEMBL11335 | — | Ki | = | 8.1 | nM | 8.09 |
| CHEMBL11347 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL10975 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL274618 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL10869 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL418707 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL11246 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL275558 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL276680 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL276174 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL11144 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL415972 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL274674 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL11032 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL11336 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL273449 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL11383 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL273981 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL274780 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL274567 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL275455 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL11084 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL11428 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL11070 | — | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL11264 | — | Ki | = | 94.0 | nM | 7.03 |
| CHEMBL428848 | — | Ki | = | 101.0 | nM | 7.00 |
| CHEMBL10867 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL11334 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL262956 | — | Ki | = | 270.0 | nM | 6.57 |