Assay Detail
Binding
CHEMBL679119
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In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
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
Nonpeptide endothelin antagonists: from lower affinity pyrazol-5-ols to higher affinity pyrazole-5-carboxylic acids.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 5.58 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL26474 | — | — | 1 | 7.75 |
| CHEMBL281865 | — | — | 1 | 7.55 |
| CHEMBL3144737 | — | — | 1 | 6.96 |
| CHEMBL3144607 | — | — | 1 | 6.85 |
| CHEMBL3144732 | — | — | 1 | 6.38 |
| CHEMBL281677 | — | — | 1 | 6.35 |
| CHEMBL3144605 | — | — | 1 | 6.22 |
| CHEMBL3144735 | — | — | 1 | 5.89 |
| CHEMBL3144599 | — | — | 1 | 5.82 |
| CHEMBL3144606 | — | — | 1 | 5.77 |
| CHEMBL3144729 | — | — | 1 | 5.75 |
| CHEMBL3144806 | — | — | 1 | 5.72 |
| CHEMBL3144799 | — | — | 1 | 5.68 |
| CHEMBL3144850 | — | — | 1 | 5.51 |
| CHEMBL3144800 | — | — | 1 | 5.46 |
| CHEMBL3144733 | — | — | 1 | 5.42 |
| CHEMBL3144600 | — | — | 1 | 5.42 |
| CHEMBL3144604 | — | — | 1 | 5.37 |
| CHEMBL3144602 | — | — | 1 | 5.25 |
| CHEMBL3144728 | — | — | 1 | 5.12 |
| CHEMBL3144803 | — | — | 1 | 5.00 |
| CHEMBL3144845 | — | — | 1 | 5.00 |
| CHEMBL3144846 | — | — | 1 | 4.70 |
| CHEMBL283037 | — | — | 1 | 4.40 |
| CHEMBL3144603 | — | — | 1 | 4.40 |
| CHEMBL3144736 | — | — | 1 | 4.32 |
| CHEMBL444545 | — | — | 1 | 4.19 |
| CHEMBL3144831 | — | — | 1 | 4.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL26474 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL281865 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3144737 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3144607 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3144732 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL281677 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL3144605 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3144735 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3144599 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3144606 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL3144729 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL3144806 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL3144799 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL3144850 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL3144800 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL3144733 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL3144600 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL3144604 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL3144602 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL3144728 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL3144803 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3144845 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3144846 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL283037 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL3144603 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL3144736 | — | IC50 | = | 48000.0 | nM | 4.32 |
| CHEMBL444545 | — | IC50 | = | 64000.0 | nM | 4.19 |
| CHEMBL3144831 | — | IC50 | = | 98000.0 | nM | 4.01 |