Assay Detail
Binding
CHEMBL671392
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Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Sus scrofa |
| Tissue | Lung |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
IRL 2500: A potent ETB selective endothelin antagonist
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 8.08 | 10.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL427778 | — | — | 1 | 10.11 |
| CHEMBL405377 | — | — | 1 | 9.60 |
| CHEMBL412003 | — | — | 1 | 9.04 |
| CHEMBL412065 | — | — | 1 | 9.00 |
| CHEMBL72410 | — | — | 1 | 9.00 |
| CHEMBL407559 | — | — | 1 | 8.28 |
| CHEMBL405796 | — | — | 1 | 8.23 |
| CHEMBL413604 | — | — | 1 | 7.96 |
| CHEMBL418898 | — | — | 1 | 7.80 |
| CHEMBL439759 | — | — | 1 | 7.44 |
| CHEMBL411399 | — | — | 1 | 6.75 |
| CHEMBL412002 | — | — | 1 | 6.58 |
| CHEMBL405753 | — | — | 1 | 5.28 |
| CHEMBL437472 | ENDOTHELIN | 2.0 | 1 | - |
| CHEMBL216772 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL427778 | — | Ki | = | 0.077 | nM | 10.11 |
| CHEMBL405377 | — | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL412003 | — | Ki | = | 0.91 | nM | 9.04 |
| CHEMBL412065 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL72410 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL407559 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL405796 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL413604 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL418898 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL439759 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL411399 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL412002 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL405753 | — | Ki | = | 5200.0 | nM | 5.28 |
| CHEMBL437472 | ENDOTHELIN | Ki | = | 0.008 | nM | - |
| CHEMBL216772 | — | Ki | > | 10000.0 | nM | - |