Assay Detail
Binding
CHEMBL5657594
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Inhibition of human neutrophil elastase using MeOSuc-AAPV-MCA as substrate measured at 60 mins interval for up to several hrs by fluorescence assay
27
Total Activities
27
Compounds Tested
1
Activity Types
2
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Freezing the Bioactive Conformation to Boost Potency: The Identification of BAY 85-8501, a Selective and Potent Inhibitor of Human Neutrophil Elastase for Pulmonary Diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 8.04 | 10.62 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| EFO_ID | EFO_ID | - | — | EFO:0003818 |
| EFO_TERM | EFO_TERM | - | — | lung disease |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5661917 | — | — | 1 | 10.62 |
| CHEMBL3617973 | — | — | 1 | 10.19 |
| CHEMBL5661855 | — | — | 1 | 9.60 |
| CHEMBL3617972 | — | — | 1 | 9.27 |
| CHEMBL5661860 | — | — | 1 | 9.22 |
| CHEMBL5661868 | — | — | 1 | 9.00 |
| CHEMBL5661928 | — | — | 1 | 9.00 |
| CHEMBL5661871 | — | — | 1 | 8.80 |
| CHEMBL5661863 | — | — | 1 | 8.68 |
| CHEMBL3617969 | — | — | 1 | 8.46 |
| CHEMBL1738716 | — | — | 1 | 8.37 |
| CHEMBL5661856 | — | — | 1 | 8.33 |
| CHEMBL5661846 | — | — | 1 | 8.30 |
| CHEMBL5661879 | — | — | 1 | 7.89 |
| CHEMBL5661897 | — | — | 1 | 7.70 |
| CHEMBL3617968 | BAY-678 | — | 1 | 7.70 |
| CHEMBL5661905 | — | — | 1 | 7.70 |
| CHEMBL5661882 | — | — | 1 | 7.60 |
| CHEMBL5661864 | — | — | 1 | 7.57 |
| CHEMBL5661832 | — | — | 1 | 7.40 |
| CHEMBL5661875 | — | — | 1 | 7.30 |
| CHEMBL5661851 | — | — | 1 | 7.16 |
| CHEMBL5661893 | — | — | 1 | 6.70 |
| CHEMBL5661839 | — | — | 1 | 6.70 |
| CHEMBL5661903 | — | — | 1 | 6.70 |
| CHEMBL5275929 | — | — | 1 | 6.05 |
| CHEMBL5661854 | — | — | 1 | 5.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5661917 | — | IC50 | = | 0.024 | nM | 10.62 |
| CHEMBL3617973 | — | IC50 | = | 0.065 | nM | 10.19 |
| CHEMBL5661855 | — | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL3617972 | — | IC50 | = | 0.54 | nM | 9.27 |
| CHEMBL5661860 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL5661868 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5661928 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5661871 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5661863 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3617969 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL1738716 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL5661856 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL5661846 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5661879 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5661897 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3617968 | BAY-678 | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5661905 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5661882 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5661864 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL5661832 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5661875 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5661851 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL5661893 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL5661839 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL5661903 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL5275929 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL5661854 | — | IC50 | = | 7000.0 | nM | 5.16 |