Assay Detail
Binding
CHEMBL682954
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to Endothelin A receptor
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Discovery of IRL 3461: a novel and potent endothelin antagonist with balanced ETA/ETB affinity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 26 | 7.81 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL308102 | — | — | 1 | 9.05 |
| CHEMBL311854 | — | — | 1 | 8.74 |
| CHEMBL310039 | — | — | 1 | 8.72 |
| CHEMBL72348 | — | — | 1 | 8.66 |
| CHEMBL310920 | — | — | 1 | 8.64 |
| CHEMBL306950 | — | — | 1 | 8.54 |
| CHEMBL307384 | — | — | 1 | 8.51 |
| CHEMBL307471 | — | — | 1 | 8.41 |
| CHEMBL73373 | — | — | 1 | 8.28 |
| CHEMBL307045 | — | — | 1 | 8.28 |
| CHEMBL308269 | — | — | 1 | 8.27 |
| CHEMBL73835 | — | — | 1 | 8.26 |
| CHEMBL72924 | — | — | 1 | 8.22 |
| CHEMBL73042 | — | — | 1 | 8.16 |
| CHEMBL72217 | — | — | 1 | 8.10 |
| CHEMBL72358 | — | — | 1 | 8.07 |
| CHEMBL263301 | — | — | 1 | 8.04 |
| CHEMBL73000 | — | — | 1 | 8.00 |
| CHEMBL433106 | — | — | 1 | 7.35 |
| CHEMBL305462 | — | — | 1 | 7.27 |
| CHEMBL307470 | — | — | 1 | 7.06 |
| CHEMBL73697 | — | — | 1 | 6.89 |
| CHEMBL70686 | — | — | 1 | 6.60 |
| CHEMBL72410 | — | — | 1 | 6.36 |
| CHEMBL70310 | — | — | 1 | 5.64 |
| CHEMBL439759 | — | — | 1 | 4.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL308102 | — | Ki | = | 0.89 | nM | 9.05 |
| CHEMBL311854 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL310039 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL72348 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL310920 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL306950 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL307384 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL307471 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL73373 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL307045 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL308269 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL73835 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL72924 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL73042 | — | Ki | = | 6.9 | nM | 8.16 |
| CHEMBL72217 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL72358 | — | Ki | = | 8.6 | nM | 8.07 |
| CHEMBL263301 | — | Ki | = | 9.1 | nM | 8.04 |
| CHEMBL73000 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL433106 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL305462 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL307470 | — | Ki | = | 87.0 | nM | 7.06 |
| CHEMBL73697 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL70686 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL72410 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL70310 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL439759 | — | Ki | = | 11000.0 | nM | 4.96 |