Assay Detail
Binding
CHEMBL677404
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebellum |
| 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 | 24 | 5.18 | 7.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL26474 | — | — | 1 | 7.47 |
| CHEMBL281865 | — | — | 1 | 7.40 |
| CHEMBL3144607 | — | — | 1 | 6.00 |
| CHEMBL281677 | — | — | 1 | 5.66 |
| CHEMBL3144605 | — | — | 1 | 5.62 |
| CHEMBL3144732 | — | — | 1 | 5.50 |
| CHEMBL3144737 | — | — | 1 | 5.48 |
| CHEMBL3144735 | — | — | 1 | 5.27 |
| CHEMBL3144803 | — | — | 1 | 5.08 |
| CHEMBL3144799 | — | — | 1 | 5.04 |
| CHEMBL3144599 | — | — | 1 | 4.96 |
| CHEMBL3144733 | — | — | 1 | 4.92 |
| CHEMBL3144806 | — | — | 1 | 4.85 |
| CHEMBL3144850 | — | — | 1 | 4.82 |
| CHEMBL3144602 | — | — | 1 | 4.77 |
| CHEMBL3144604 | — | — | 1 | 4.66 |
| CHEMBL3144728 | — | — | 1 | 4.62 |
| CHEMBL3144845 | — | — | 1 | 4.62 |
| CHEMBL3144600 | — | — | 1 | 4.60 |
| CHEMBL3144800 | — | — | 1 | 4.54 |
| CHEMBL3144729 | — | — | 1 | 4.48 |
| CHEMBL3144606 | — | — | 1 | 4.44 |
| CHEMBL3144736 | — | — | 1 | 4.41 |
| CHEMBL283037 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL26474 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL281865 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3144607 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL281677 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL3144605 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL3144732 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL3144737 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL3144735 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL3144803 | — | IC50 | = | 8400.0 | nM | 5.08 |
| CHEMBL3144799 | — | IC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL3144599 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL3144733 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL3144806 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL3144850 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL3144602 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL3144604 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL3144728 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL3144845 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL3144600 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL3144800 | — | IC50 | = | 29000.0 | nM | 4.54 |
| CHEMBL3144729 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL3144606 | — | IC50 | = | 36000.0 | nM | 4.44 |
| CHEMBL3144736 | — | IC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL283037 | — | IC50 | > | 25000.0 | nM | - |