Assay Detail
Binding
CHEMBL5657598
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Inhibition of rat neutrophil elastase using MeOSuc-AAPV-MCA as substrate measured at 60 mins interval for up to several hrs by fluorescence assay
10
Total Activities
10
Compounds Tested
1
Activity Types
2
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 0 — Uncurated / Unknown |
| 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 | 10 | 6.88 | 7.82 |
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 |
|---|---|---|---|---|
| CHEMBL5661928 | — | — | 1 | 7.82 |
| CHEMBL5661863 | — | — | 1 | 7.37 |
| CHEMBL3617969 | — | — | 1 | 7.36 |
| CHEMBL5661868 | — | — | 1 | 7.31 |
| CHEMBL5661846 | — | — | 1 | 6.90 |
| CHEMBL5661864 | — | — | 1 | 6.72 |
| CHEMBL5661882 | — | — | 1 | 6.63 |
| CHEMBL1738716 | — | — | 1 | 6.56 |
| CHEMBL3617968 | BAY-678 | — | 1 | 6.10 |
| CHEMBL5661856 | — | — | 1 | 5.99 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5661928 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5661863 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL3617969 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL5661868 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL5661846 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL5661864 | — | IC50 | = | 192.0 | nM | 6.72 |
| CHEMBL5661882 | — | IC50 | = | 233.0 | nM | 6.63 |
| CHEMBL1738716 | — | IC50 | = | 276.0 | nM | 6.56 |
| CHEMBL3617968 | BAY-678 | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL5661856 | — | IC50 | = | 1018.0 | nM | 5.99 |