Assay Detail
Binding
CHEMBL651097
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro binding affinity against angiotensin II (AT2) receptor to competitively block the specific binding of [125I]- [Sar1,Ile8] AII to a rat mid brain AT2 receptor preparation
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Triazolinone biphenylsulfonamides as angiotensin II receptor antagonists with high affinity for both the AT1 and AT2 subtypes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 41 | 7.76 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL276674 | — | — | 1 | 9.00 |
| CHEMBL341828 | — | — | 1 | 8.85 |
| CHEMBL334300 | — | — | 1 | 8.80 |
| CHEMBL96075 | — | — | 1 | 8.80 |
| CHEMBL275552 | — | — | 1 | 8.68 |
| CHEMBL341934 | — | — | 1 | 8.64 |
| CHEMBL343142 | — | — | 1 | 8.64 |
| CHEMBL338101 | — | — | 1 | 8.62 |
| CHEMBL93907 | — | — | 1 | 8.60 |
| CHEMBL344597 | — | — | 1 | 8.54 |
| CHEMBL138690 | — | — | 1 | 8.47 |
| CHEMBL139325 | — | — | 1 | 8.39 |
| CHEMBL343309 | — | — | 1 | 8.36 |
| CHEMBL337118 | — | — | 1 | 8.36 |
| CHEMBL139452 | — | — | 1 | 8.32 |
| CHEMBL435792 | — | — | 1 | 8.25 |
| CHEMBL140708 | — | — | 1 | 8.19 |
| CHEMBL139041 | — | — | 1 | 8.18 |
| CHEMBL265797 | — | — | 1 | 7.92 |
| CHEMBL136465 | — | — | 1 | 7.89 |
| CHEMBL140619 | — | — | 1 | 7.82 |
| CHEMBL292150 | — | — | 1 | 7.77 |
| CHEMBL341783 | — | — | 1 | 7.77 |
| CHEMBL139582 | — | — | 1 | 7.54 |
| CHEMBL344467 | — | — | 1 | 7.47 |
| CHEMBL316300 | — | — | 1 | 7.44 |
| CHEMBL344387 | — | — | 1 | 7.24 |
| CHEMBL344811 | — | — | 1 | 7.24 |
| CHEMBL342605 | — | — | 1 | 7.00 |
| CHEMBL342492 | — | — | 1 | 6.97 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL276674 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL341828 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL96075 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL334300 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL275552 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL341934 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL343142 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL338101 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL93907 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL344597 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL138690 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL139325 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL343309 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL337118 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL139452 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL435792 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL140708 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL139041 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL265797 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL136465 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL140619 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL341783 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL292150 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL139582 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL344467 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL316300 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL344387 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL344811 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL342605 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL342492 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL341986 | — | IC50 | = | 134.0 | nM | 6.87 |
| CHEMBL343719 | — | IC50 | = | 142.0 | nM | 6.85 |
| CHEMBL293501 | — | IC50 | = | 173.0 | nM | 6.76 |
| CHEMBL344466 | — | IC50 | = | 185.0 | nM | 6.73 |
| CHEMBL341715 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL337588 | — | IC50 | = | 201.0 | nM | 6.70 |
| CHEMBL141592 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL279629 | L-159913 | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL138654 | — | IC50 | = | 306.0 | nM | 6.51 |
| CHEMBL342843 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL343634 | — | IC50 | > | 10.0 | nM | - |