Assay Detail
Functional
CHEMBL663217
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Antagonism of Cysteinyl leukotriene receptor 1 from guinea pig lung membranes
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Tissue | Lung |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Development of 2,2-dimethylchromanol cysteinyl LT1 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 8.53 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL300701 | — | — | 1 | 9.15 |
| CHEMBL21333 | PRANLUKAST | 4.0 | 1 | 9.10 |
| CHEMBL332680 | — | — | 1 | 8.70 |
| CHEMBL603 | ZAFIRLUKAST | 4.0 | 1 | 8.70 |
| CHEMBL120200 | — | — | 1 | 8.40 |
| CHEMBL119214 | — | — | 1 | 8.40 |
| CHEMBL331884 | — | — | 1 | 8.30 |
| CHEMBL331747 | — | — | 1 | 8.15 |
| CHEMBL442150 | — | — | 1 | 7.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL300701 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL21333 | PRANLUKAST | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL332680 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL603 | ZAFIRLUKAST | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL120200 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL119214 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL331884 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL331747 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL442150 | — | Ki | = | 14.0 | nM | 7.85 |