Assay Detail
Functional
CHEMBL648847
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro antagonistic activity for angiotensin II receptor, type 1 by displacing 125I[Sar, ILe8 ]AII radioligand in rabbit aorta membrane without using bovine serum albumin (BSA)
91
Total Activities
91
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Oryctolagus cuniculus |
| Tissue | Aorta |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Type-1 angiotensin II receptor (CHEMBL3948) ↗| Type | SINGLE PROTEIN |
| Organism | Oryctolagus cuniculus |
Publication
Triazolinones as nonpeptide angiotensin II antagonists. 1. Synthesis and evaluation of potent 2,4,5-trisubstituted triazolinones.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 91 | 7.80 | 9.13 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL419483 | — | — | 1 | 9.13 |
| CHEMBL87074 | — | — | 1 | 9.07 |
| CHEMBL313371 | — | — | 1 | 9.05 |
| CHEMBL312913 | — | — | 1 | 9.03 |
| CHEMBL19018 | — | — | 1 | 8.92 |
| CHEMBL431411 | — | — | 1 | 8.85 |
| CHEMBL87964 | — | — | 1 | 8.74 |
| CHEMBL86314 | — | — | 1 | 8.74 |
| CHEMBL87513 | — | — | 1 | 8.70 |
| CHEMBL19202 | — | — | 1 | 8.68 |
| CHEMBL18287 | — | — | 1 | 8.62 |
| CHEMBL87778 | — | — | 1 | 8.54 |
| CHEMBL87239 | — | — | 1 | 8.54 |
| CHEMBL83194 | — | — | 1 | 8.51 |
| CHEMBL313025 | — | — | 1 | 8.49 |
| CHEMBL87057 | — | — | 1 | 8.49 |
| CHEMBL315776 | — | — | 1 | 8.44 |
| CHEMBL83180 | — | — | 1 | 8.39 |
| CHEMBL422593 | — | — | 1 | 8.34 |
| CHEMBL85545 | — | — | 1 | 8.31 |
| CHEMBL84627 | — | — | 1 | 8.30 |
| CHEMBL314042 | — | — | 1 | 8.25 |
| CHEMBL316052 | — | — | 1 | 8.24 |
| CHEMBL278741 | — | — | 1 | 8.24 |
| CHEMBL907 | CARBOXYLIC ACID METABOLITE | — | 1 | 8.22 |
| CHEMBL83248 | — | — | 1 | 8.18 |
| CHEMBL313435 | — | — | 1 | 8.13 |
| CHEMBL313579 | — | — | 1 | 8.11 |
| CHEMBL87985 | — | — | 1 | 8.11 |
| CHEMBL82797 | — | — | 1 | 8.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL419483 | — | IC50 | = | 0.74 | nM | 9.13 |
| CHEMBL87074 | — | IC50 | = | 0.85 | nM | 9.07 |
| CHEMBL313371 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL312913 | — | IC50 | = | 0.93 | nM | 9.03 |
| CHEMBL19018 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL431411 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL87964 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL86314 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL87513 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL19202 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL18287 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL87778 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL87239 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL83194 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL87057 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL313025 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL315776 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL83180 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL422593 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL85545 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL84627 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL314042 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL316052 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL278741 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL907 | CARBOXYLIC ACID METABOLITE | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL83248 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL313435 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL313579 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL87985 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL82797 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL87392 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL86084 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL313696 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL314447 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL87363 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL312921 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL313222 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL407827 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL87341 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL87129 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL87942 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL87798 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL87330 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL86255 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL86906 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL87669 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL314810 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL315077 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL314179 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL85541 | — | IC50 | = | 17.0 | nM | 7.77 |