Assay Detail
Binding
CHEMBL4677799
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human neutrophil elastase using N-methylsuccinyl-Ala-Ala-Pro-Val-7-amino-4-methylcoumarin as substrate measured for every 30 sec for 10 mins by fluorescence based assay
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Exploration of nitrogen heterocycle scaffolds for the development of potent human neutrophil elastase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 6.71 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4761049 | — | — | 1 | 8.00 |
| CHEMBL4747003 | — | — | 1 | 7.85 |
| CHEMBL4765112 | — | — | 1 | 7.80 |
| CHEMBL4744044 | — | — | 1 | 7.68 |
| CHEMBL4783748 | — | — | 1 | 7.64 |
| CHEMBL4797962 | — | — | 1 | 7.48 |
| CHEMBL4749406 | — | — | 1 | 7.47 |
| CHEMBL4793337 | — | — | 1 | 7.30 |
| CHEMBL76688 | SIVELESTAT | 3.0 | 1 | 7.30 |
| CHEMBL4791155 | — | — | 1 | 7.25 |
| CHEMBL4765083 | — | — | 1 | 7.16 |
| CHEMBL4753315 | — | — | 1 | 7.10 |
| CHEMBL4777121 | — | — | 1 | 7.06 |
| CHEMBL4790048 | — | — | 1 | 7.05 |
| CHEMBL4749925 | — | — | 1 | 7.01 |
| CHEMBL4758569 | — | — | 1 | 6.85 |
| CHEMBL4792286 | — | — | 1 | 6.80 |
| CHEMBL4740453 | — | — | 1 | 6.74 |
| CHEMBL4749095 | — | — | 1 | 6.71 |
| CHEMBL4751776 | — | — | 1 | 6.48 |
| CHEMBL4750483 | — | — | 1 | 6.38 |
| CHEMBL4792553 | — | — | 1 | 6.12 |
| CHEMBL4752637 | — | — | 1 | 6.01 |
| CHEMBL4790493 | — | — | 1 | 5.96 |
| CHEMBL4787564 | — | — | 1 | 5.82 |
| CHEMBL4784285 | — | — | 1 | 5.82 |
| CHEMBL4740321 | — | — | 1 | 5.70 |
| CHEMBL4786666 | — | — | 1 | 5.10 |
| CHEMBL4783275 | — | — | 1 | 5.00 |
| CHEMBL4780137 | — | — | 1 | 4.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4761049 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4747003 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4765112 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4744044 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4783748 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4797962 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4749406 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4793337 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL76688 | SIVELESTAT | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4791155 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL4765083 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL4753315 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL4777121 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL4790048 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL4749925 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL4758569 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4792286 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4740453 | — | IC50 | = | 183.0 | nM | 6.74 |
| CHEMBL4749095 | — | IC50 | = | 194.0 | nM | 6.71 |
| CHEMBL4751776 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL4750483 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL4792553 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL4752637 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL4790493 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4787564 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4784285 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4740321 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4786666 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL4783275 | — | IC50 | = | 9900.0 | nM | 5.00 |
| CHEMBL4780137 | — | IC50 | = | 25200.0 | nM | 4.60 |
| CHEMBL4753872 | — | IC50 | - | — | - | |
| CHEMBL4744938 | — | IC50 | - | — | - | |
| CHEMBL4795722 | — | IC50 | - | — | - | |
| CHEMBL4779092 | — | IC50 | - | — | - | |
| CHEMBL4789363 | — | IC50 | - | — | - | |
| CHEMBL4761477 | — | IC50 | - | — | - | |
| CHEMBL4778211 | — | IC50 | - | — | - | |
| CHEMBL4782325 | — | IC50 | - | — | - | |
| CHEMBL4745191 | — | IC50 | - | — | - |