Assay Detail
Functional
CHEMBL650274
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro antagonist activity against angiotensin II receptor type 1 in rabbit aorta using [125I]-Sar, Ile AII.
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Oryctolagus cuniculus |
| Tissue | Aorta |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Type-1 angiotensin II receptor (CHEMBL3948) ↗| Type | SINGLE PROTEIN |
| Organism | Oryctolagus cuniculus |
Publication
Non-peptide angiotensin II receptor antagonists. 1. Design, synthesis, and biological activity of N-substituted indoles and dihydroindoles.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 7.06 | 9.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL7550 | L-158809 | — | 1 | 9.27 |
| CHEMBL337086 | — | — | 1 | 9.10 |
| CHEMBL135775 | — | — | 1 | 9.00 |
| CHEMBL132408 | — | — | 1 | 8.30 |
| CHEMBL334660 | — | — | 1 | 8.06 |
| CHEMBL135999 | — | — | 1 | 7.82 |
| CHEMBL442963 | — | — | 1 | 7.75 |
| CHEMBL335535 | — | — | 1 | 7.75 |
| CHEMBL133653 | — | — | 1 | 7.70 |
| CHEMBL134151 | — | — | 1 | 7.32 |
| CHEMBL191 | LOSARTAN | 4.0 | 1 | 7.27 |
| CHEMBL338505 | — | — | 1 | 7.09 |
| CHEMBL134901 | — | — | 1 | 7.04 |
| CHEMBL334775 | — | — | 1 | 6.92 |
| CHEMBL131676 | — | — | 1 | 6.80 |
| CHEMBL134567 | — | — | 1 | 6.77 |
| CHEMBL135521 | — | — | 1 | 6.77 |
| CHEMBL334622 | — | — | 1 | 6.64 |
| CHEMBL341407 | — | — | 1 | 6.62 |
| CHEMBL335323 | — | — | 1 | 6.60 |
| CHEMBL278656 | — | — | 1 | 6.50 |
| CHEMBL135792 | — | — | 1 | 6.46 |
| CHEMBL335228 | — | — | 1 | 6.21 |
| CHEMBL135522 | — | — | 1 | 6.17 |
| CHEMBL133654 | — | — | 1 | 6.11 |
| CHEMBL134433 | — | — | 1 | 5.96 |
| CHEMBL134307 | — | — | 1 | 5.80 |
| CHEMBL335680 | — | — | 1 | 5.48 |
| CHEMBL335179 | — | — | 1 | 5.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL7550 | L-158809 | IC50 | = | 0.54 | nM | 9.27 |
| CHEMBL337086 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL135775 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL132408 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL334660 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL135999 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL442963 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL335535 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL133653 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL134151 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL191 | LOSARTAN | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL338505 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL134901 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL334775 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL131676 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL134567 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL135521 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL334622 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL341407 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL335323 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL278656 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL135792 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL335228 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL135522 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL133654 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL134433 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL134307 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL335680 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL335179 | — | IC50 | = | 4600.0 | nM | 5.34 |