Assay Detail
Binding
CHEMBL677262
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Affinity against ET A receptor
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Design and synthesis of nonpeptidal endothelin receptor antagonists based on the structure of a cyclic pentapeptide
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 4.90 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL314691 | BQ-123 | 2.0 | 1 | 7.75 |
| CHEMBL86581 | — | — | 1 | 5.16 |
| CHEMBL86489 | — | — | 1 | 4.85 |
| CHEMBL314915 | — | — | 1 | 4.77 |
| CHEMBL421349 | — | — | 1 | 4.55 |
| CHEMBL314364 | — | — | 1 | 4.48 |
| CHEMBL313184 | — | — | 1 | 4.39 |
| CHEMBL315096 | — | — | 1 | 4.10 |
| CHEMBL316247 | — | — | 1 | 4.08 |
| CHEMBL87859 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL314691 | BQ-123 | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL86581 | — | Ki | = | 7000.0 | nM | 5.16 |
| CHEMBL86489 | — | Ki | = | 14000.0 | nM | 4.85 |
| CHEMBL314915 | — | Ki | = | 17000.0 | nM | 4.77 |
| CHEMBL421349 | — | Ki | = | 28000.0 | nM | 4.55 |
| CHEMBL314364 | — | Ki | = | 33000.0 | nM | 4.48 |
| CHEMBL313184 | — | Ki | = | 41000.0 | nM | 4.39 |
| CHEMBL315096 | — | Ki | = | 80000.0 | nM | 4.10 |
| CHEMBL316247 | — | Ki | = | 83000.0 | nM | 4.08 |
| CHEMBL87859 | — | Ki | = | 109000.0 | nM | - |