Assay Detail
Functional
CHEMBL5653637
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human ETB receptor transfected in CHO cell membrane assessed as inhibition of 125I-labelled ET-3 binding to receptor incubated for 3 hrs by competition binding assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Pharmacology of endothelin receptor antagonists ABT-627, ABT-546, A-182086 and A-192621: in vitro studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 7.57 | 9.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL111277 | — | — | 1 | 9.55 |
| CHEMBL332794 | A-192621 | — | 1 | 8.34 |
| CHEMBL111612 | ABT-546 | — | 1 | 4.81 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL111277 | — | IC50 | = | 0.28 | nM | 9.55 |
| CHEMBL332794 | A-192621 | IC50 | = | 4.54 | nM | 8.34 |
| CHEMBL111612 | ABT-546 | IC50 | = | 15400.0 | nM | 4.81 |