Assay Detail
Binding
CHEMBL682952
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Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Lung |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
IRL 2500: A potent ETB selective endothelin antagonist
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 6.49 | 10.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL437472 | ENDOTHELIN | 2.0 | 1 | 10.40 |
| CHEMBL405377 | — | — | 1 | 7.02 |
| CHEMBL412065 | — | — | 1 | 6.60 |
| CHEMBL72410 | — | — | 1 | 6.36 |
| CHEMBL427778 | — | — | 1 | 6.21 |
| CHEMBL412003 | — | — | 1 | 5.89 |
| CHEMBL407559 | — | — | 1 | 5.70 |
| CHEMBL413604 | — | — | 1 | 5.30 |
| CHEMBL439759 | — | — | 1 | 4.96 |
| CHEMBL411399 | — | — | 1 | - |
| CHEMBL412002 | — | — | 1 | - |
| CHEMBL216772 | — | — | 1 | - |
| CHEMBL405753 | — | — | 1 | - |
| CHEMBL405796 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL437472 | ENDOTHELIN | Ki | = | 0.04 | nM | 10.40 |
| CHEMBL405377 | — | Ki | = | 96.0 | nM | 7.02 |
| CHEMBL412065 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL72410 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL427778 | — | Ki | = | 620.0 | nM | 6.21 |
| CHEMBL412003 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL407559 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL413604 | — | Ki | = | 5000.0 | nM | 5.30 |
| CHEMBL439759 | — | Ki | = | 11000.0 | nM | 4.96 |
| CHEMBL411399 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL412002 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL216772 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL405753 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL405796 | — | Ki | > | 10000.0 | nM | - |