Assay Detail
Binding
CHEMBL652353
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]-Sar1-Ile8-A II from rat adrenal Angiotensin-1 (AT-1) receptor
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Type-1 angiotensin II receptor B (CHEMBL263) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and SAR studies of novel triazolopyrimidine derivatives as potent, orally active angiotensin II receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 43 | 7.42 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL77959 | — | — | 1 | 9.00 |
| CHEMBL191 | LOSARTAN | 4.0 | 1 | 8.44 |
| CHEMBL80773 | — | — | 1 | 8.30 |
| CHEMBL77783 | — | — | 1 | 8.30 |
| CHEMBL80446 | — | — | 1 | 8.22 |
| CHEMBL78021 | — | — | 1 | 8.10 |
| CHEMBL80380 | — | — | 1 | 8.05 |
| CHEMBL311657 | — | — | 1 | 8.00 |
| CHEMBL77036 | — | — | 1 | 8.00 |
| CHEMBL432153 | — | — | 1 | 8.00 |
| CHEMBL419089 | — | — | 1 | 8.00 |
| CHEMBL79879 | — | — | 1 | 7.96 |
| CHEMBL312632 | — | — | 1 | 7.92 |
| CHEMBL309384 | — | — | 1 | 7.92 |
| CHEMBL309458 | — | — | 1 | 7.82 |
| CHEMBL80688 | — | — | 1 | 7.64 |
| CHEMBL312104 | RIPISARTAN | 2.0 | 1 | 7.62 |
| CHEMBL76900 | — | — | 1 | 7.57 |
| CHEMBL76149 | — | — | 1 | 7.57 |
| CHEMBL80218 | — | — | 1 | 7.52 |
| CHEMBL80967 | — | — | 1 | 7.50 |
| CHEMBL79171 | — | — | 1 | 7.50 |
| CHEMBL76787 | — | — | 1 | 7.46 |
| CHEMBL419835 | — | — | 1 | 7.46 |
| CHEMBL80167 | — | — | 1 | 7.39 |
| CHEMBL420028 | — | — | 1 | 7.34 |
| CHEMBL310678 | — | — | 1 | 7.30 |
| CHEMBL76421 | — | — | 1 | 7.28 |
| CHEMBL76079 | — | — | 1 | 7.09 |
| CHEMBL311825 | — | — | 1 | 7.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL77959 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL191 | LOSARTAN | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL77783 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL80773 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL80446 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL78021 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL80380 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL311657 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL77036 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL432153 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL419089 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL79879 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL312632 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL309384 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL309458 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL80688 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL312104 | RIPISARTAN | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL76900 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL76149 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL80218 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL79171 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL80967 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL76787 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL419835 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL80167 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL420028 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL310678 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL76421 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL76079 | — | Ki | = | 82.0 | nM | 7.09 |
| CHEMBL311825 | — | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL80161 | — | Ki | = | 99.0 | nM | 7.00 |
| CHEMBL78532 | — | Ki | = | 106.0 | nM | 6.97 |
| CHEMBL78433 | — | Ki | = | 111.0 | nM | 6.96 |
| CHEMBL80219 | — | Ki | = | 127.0 | nM | 6.90 |
| CHEMBL76359 | — | Ki | = | 139.0 | nM | 6.86 |
| CHEMBL78399 | — | Ki | = | 147.0 | nM | 6.83 |
| CHEMBL76866 | — | Ki | = | 174.0 | nM | 6.76 |
| CHEMBL80854 | — | Ki | = | 175.0 | nM | 6.76 |
| CHEMBL77384 | — | Ki | = | 185.0 | nM | 6.73 |
| CHEMBL78342 | — | Ki | = | 225.0 | nM | 6.65 |
| CHEMBL76775 | — | Ki | = | 622.0 | nM | 6.21 |
| CHEMBL308138 | — | Ki | = | 659.0 | nM | 6.18 |
| CHEMBL421141 | — | Ki | = | 9000.0 | nM | 5.05 |