Assay Detail
Binding
CHEMBL679114
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In vitro binding affinity to endothelin A receptor in rat heart ventricles
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Potent nonpeptide endothelin antagonists: synthesis and structure-activity relationships of pyrazole-5-carboxylic acids.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 7.92 | 9.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL86965 | — | — | 1 | 9.09 |
| CHEMBL313044 | — | — | 1 | 8.96 |
| CHEMBL313153 | — | — | 1 | 8.96 |
| CHEMBL88011 | — | — | 1 | 8.89 |
| CHEMBL312979 | — | — | 1 | 8.89 |
| CHEMBL315936 | — | — | 1 | 8.60 |
| CHEMBL312854 | — | — | 1 | 8.60 |
| CHEMBL314974 | — | — | 1 | 8.47 |
| CHEMBL87070 | — | — | 1 | 8.44 |
| CHEMBL314454 | — | — | 1 | 8.33 |
| CHEMBL315805 | — | — | 1 | 8.31 |
| CHEMBL315638 | — | — | 1 | 8.21 |
| CHEMBL315087 | — | — | 1 | 7.96 |
| CHEMBL314206 | — | — | 1 | 7.83 |
| CHEMBL315752 | — | — | 1 | 7.82 |
| CHEMBL315622 | — | — | 1 | 7.77 |
| CHEMBL314357 | — | — | 1 | 7.75 |
| CHEMBL26474 | — | — | 1 | 7.75 |
| CHEMBL314973 | — | — | 1 | 7.69 |
| CHEMBL316187 | — | — | 1 | 7.55 |
| CHEMBL87801 | — | — | 1 | 7.55 |
| CHEMBL313920 | — | — | 1 | 7.47 |
| CHEMBL315280 | — | — | 1 | 7.23 |
| CHEMBL86821 | — | — | 1 | 7.16 |
| CHEMBL88019 | — | — | 1 | 7.10 |
| CHEMBL86505 | — | — | 1 | 7.05 |
| CHEMBL315175 | — | — | 1 | 6.65 |
| CHEMBL315788 | — | — | 1 | 5.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL86965 | — | IC50 | = | 0.81 | nM | 9.09 |
| CHEMBL313044 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL313153 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL88011 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL312979 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL315936 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL312854 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL314974 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL87070 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL314454 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL315805 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL315638 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL315087 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL314206 | — | IC50 | = | 14.9 | nM | 7.83 |
| CHEMBL315752 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL315622 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL314357 | — | IC50 | = | 17.8 | nM | 7.75 |
| CHEMBL26474 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL314973 | — | IC50 | = | 20.5 | nM | 7.69 |
| CHEMBL316187 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL87801 | — | IC50 | = | 28.3 | nM | 7.55 |
| CHEMBL313920 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL315280 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL86821 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL88019 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL86505 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL315175 | — | IC50 | = | 226.0 | nM | 6.65 |
| CHEMBL315788 | — | IC50 | = | 2300.0 | nM | 5.64 |