Assay Detail
Binding
CHEMBL648760
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Inhibition of [125I]angiotensin-II binding to the angiotensin II receptor type 1 in rat uterine membranes
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Membrane |
| 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 structure-activity relationships of nonpeptide, potent triazolone-based angiotensin II receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 43 | 7.52 | 8.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL313371 | — | — | 1 | 8.51 |
| CHEMBL304329 | — | — | 1 | 8.44 |
| CHEMBL66173 | — | — | 1 | 8.36 |
| CHEMBL87778 | — | — | 1 | 8.29 |
| CHEMBL70029 | — | — | 1 | 8.25 |
| CHEMBL87942 | — | — | 1 | 8.10 |
| CHEMBL68760 | — | — | 1 | 8.06 |
| CHEMBL67764 | — | — | 1 | 8.05 |
| CHEMBL68719 | — | — | 1 | 8.01 |
| CHEMBL87964 | — | — | 1 | 8.00 |
| CHEMBL304134 | — | — | 1 | 7.92 |
| CHEMBL302261 | — | — | 1 | 7.92 |
| CHEMBL303683 | — | — | 1 | 7.82 |
| CHEMBL87669 | — | — | 1 | 7.82 |
| CHEMBL82797 | — | — | 1 | 7.82 |
| CHEMBL422593 | — | — | 1 | 7.80 |
| CHEMBL307310 | — | — | 1 | 7.80 |
| CHEMBL68731 | — | — | 1 | 7.77 |
| CHEMBL313222 | — | — | 1 | 7.75 |
| CHEMBL306882 | — | — | 1 | 7.75 |
| CHEMBL87985 | — | — | 1 | 7.70 |
| CHEMBL412664 | — | — | 1 | 7.68 |
| CHEMBL86084 | — | — | 1 | 7.66 |
| CHEMBL304600 | — | — | 1 | 7.66 |
| CHEMBL302478 | — | — | 1 | 7.60 |
| CHEMBL307752 | — | — | 1 | 7.52 |
| CHEMBL71613 | — | — | 1 | 7.46 |
| CHEMBL191 | LOSARTAN | 4.0 | 1 | 7.44 |
| CHEMBL308416 | — | — | 1 | 7.44 |
| CHEMBL69508 | — | — | 1 | 7.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL313371 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL304329 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL66173 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL87778 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL70029 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL87942 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL68760 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL67764 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL68719 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL87964 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL304134 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL302261 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL303683 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL82797 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL87669 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL422593 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL307310 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL68731 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL313222 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL306882 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL87985 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL412664 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL304600 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL86084 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL302478 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL307752 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL71613 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL191 | LOSARTAN | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL308416 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL69508 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL69296 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL308239 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL87184 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL85876 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL68582 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL68919 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL68275 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL67515 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL86986 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL443005 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL65905 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL71518 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL306328 | — | IC50 | = | 5800.0 | nM | 5.24 |