Assay Detail
Binding
CHEMBL645647
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In vitro inhibition of angiotensin I converting enzyme in rabbit lung with hippuryl-histidyl-leucine as substrate
34
Total Activities
34
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
(Phosphinyloxy)acyl amino acid inhibitors of angiotensin converting enzyme (ACE). 1. Discovery of (S)-1-[6-amino-2-[[hydroxy(4-phenylbutyl)phosphinyl]oxy]-1-oxohexyl]-L -proline a novel orally active inhibitor of ACE.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 7.24 | 8.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL577 | ENALAPRILAT ANHYDROUS | 4.0 | 1 | 8.37 |
| CHEMBL66683 | — | — | 1 | 8.21 |
| CHEMBL417408 | — | — | 1 | 8.05 |
| CHEMBL67253 | — | — | 1 | 7.92 |
| CHEMBL302996 | — | — | 1 | 7.85 |
| CHEMBL68472 | — | — | 1 | 7.72 |
| CHEMBL67156 | — | — | 1 | 7.72 |
| CHEMBL1560 | CAPTOPRIL | 4.0 | 1 | 7.64 |
| CHEMBL63671 | — | — | 1 | 7.62 |
| CHEMBL67125 | — | — | 1 | 7.57 |
| CHEMBL63302 | — | — | 1 | 7.51 |
| CHEMBL422051 | — | — | 1 | 7.51 |
| CHEMBL303606 | — | — | 1 | 7.50 |
| CHEMBL36503 | CERONAPRIL | 2.0 | 1 | 7.44 |
| CHEMBL302477 | — | — | 1 | 7.42 |
| CHEMBL63881 | — | — | 1 | 7.40 |
| CHEMBL68112 | — | — | 1 | 7.38 |
| CHEMBL67102 | — | — | 1 | 7.26 |
| CHEMBL63517 | — | — | 1 | 7.23 |
| CHEMBL308917 | — | — | 1 | 7.21 |
| CHEMBL431773 | — | — | 1 | 7.07 |
| CHEMBL305443 | — | — | 1 | 7.03 |
| CHEMBL302896 | — | — | 1 | 7.02 |
| CHEMBL67904 | — | — | 1 | 7.02 |
| CHEMBL413771 | — | — | 1 | 6.96 |
| CHEMBL291625 | — | — | 1 | 6.82 |
| CHEMBL66313 | — | — | 1 | 6.75 |
| CHEMBL302871 | — | — | 1 | 6.75 |
| CHEMBL66754 | — | — | 1 | 6.72 |
| CHEMBL422405 | — | — | 1 | 6.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL577 | ENALAPRILAT ANHYDROUS | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL66683 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL417408 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL67253 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL302996 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL68472 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL67156 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1560 | CAPTOPRIL | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL63671 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL67125 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL63302 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL422051 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL303606 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL36503 | CERONAPRIL | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL302477 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL63881 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL68112 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL67102 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL63517 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL308917 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL431773 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL305443 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL302896 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL67904 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL413771 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL291625 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL66313 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL302871 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL66754 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL422405 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL63958 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL68181 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL66946 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL63447 | — | IC50 | = | 3800.0 | nM | 5.42 |