Assay Detail
Functional
CHEMBL774081
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Ability to antagonize endothelin -1 (ET-1) stimulated vasoconstriction in vitro in rabbit femoral artery
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Oryctolagus cuniculus |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
Design of a potent combined pseudopeptide endothelin-A/endothelin-B receptor antagonist, Ac-DBhg16-Leu-Asp-Ile-[NMe]Ile-Trp21 (PD 156252): examination of its pharmacokinetic and spectral properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 3 | 6.90 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1790519 | — | — | 1 | 7.30 |
| CHEMBL262993 | — | — | 1 | 6.80 |
| CHEMBL328942 | — | — | 1 | 6.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1790519 | — | Kd | = | 50.12 | nM | 7.30 |
| CHEMBL262993 | — | Kd | = | 158.49 | nM | 6.80 |
| CHEMBL328942 | — | Kd | = | 251.19 | nM | 6.60 |