Assay Detail
Binding
CHEMBL644736
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In vitro inhibition of Angiotensin I converting enzyme activity at pH 8.5 in rabbit lung
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Oryctolagus cuniculus |
| Tissue | Lung |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Angiotensin-converting enzyme (CHEMBL4074) ↗| Type | SINGLE PROTEIN |
| Organism | Oryctolagus cuniculus |
Publication
Angiotensin-converting enzyme inhibitors: new orally active 1,4-thiazepine-2,5-diones, 1,4-thiazine-2,5-diones, and 1,4-benzothiazepine-2,5-diones possessing antihypertensive activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.77 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL353788 | — | — | 1 | 8.30 |
| CHEMBL352295 | — | — | 1 | 7.77 |
| CHEMBL2051970 | PIVOPRIL | 2.0 | 1 | 7.77 |
| CHEMBL1560 | CAPTOPRIL | 4.0 | 1 | 7.77 |
| CHEMBL167373 | — | — | 1 | 7.75 |
| CHEMBL351870 | — | — | 1 | 7.60 |
| CHEMBL166718 | — | — | 1 | 7.58 |
| CHEMBL164655 | — | — | 1 | 7.35 |
| CHEMBL353962 | — | — | 1 | 7.24 |
| CHEMBL350725 | — | — | 1 | 7.24 |
| CHEMBL424202 | — | — | 1 | 6.55 |
| CHEMBL351370 | — | — | 1 | 6.42 |
| CHEMBL441491 | — | — | 1 | 5.72 |
| CHEMBL165105 | — | — | 1 | 5.32 |
| CHEMBL351872 | — | — | 1 | 5.17 |
| CHEMBL167485 | — | — | 1 | 4.82 |
| CHEMBL424390 | — | — | 1 | 4.68 |
| CHEMBL165318 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL353788 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL352295 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL2051970 | PIVOPRIL | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1560 | CAPTOPRIL | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL167373 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL351870 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL166718 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL164655 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL353962 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL350725 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL424202 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL351370 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL441491 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL165105 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL351872 | — | IC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL167485 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL424390 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL165318 | — | IC50 | > | 100000.0 | nM | - |