Assay Detail
Functional
CHEMBL768975
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Ability to inhibit histamine phase of platelet activating factor (PAF)-induced bronchoconstriction in vivo in pulmonary function assays in Guinea pigs dosing orally 5 hours prior was determined
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Oryctolagus cuniculus |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
Synthesis, structure-activity relationships, and pharmacological evaluation of pyrrolo[3,2,1-ij]quinoline derivatives: potent histamine and platelet activating factor antagonism and 5-lipoxygenase inhibitory properties. Potential therapeutic application in asthma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 5.27 | 7.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL349811 | TULOPAFANT | 2.0 | 1 | 7.44 |
| CHEMBL161815 | — | — | 1 | 4.70 |
| CHEMBL350987 | — | — | 1 | 4.51 |
| CHEMBL349081 | — | — | 1 | 4.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL349811 | TULOPAFANT | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL161815 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL350987 | — | IC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL349081 | — | IC50 | = | 36000.0 | nM | 4.44 |