Assay Detail
Binding
CHEMBL4256759
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Partial agonist activity at human PPARgamma LBD expressed HEK293T cells after 12 to 14 hrs by dual-glo luciferase reporter gene assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor gamma (CHEMBL235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Boosting Anti-Inflammatory Potency of Zafirlukast by Designed Polypharmacology.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 10 | 6.31 | 6.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4280282 | — | — | 1 | 6.85 |
| CHEMBL4289768 | — | — | 1 | 6.70 |
| CHEMBL48435 | — | — | 1 | 6.64 |
| CHEMBL4279086 | — | — | 1 | 6.52 |
| CHEMBL4294239 | — | — | 1 | 6.46 |
| CHEMBL4290919 | — | — | 1 | 6.43 |
| CHEMBL4288574 | — | — | 1 | 6.17 |
| CHEMBL4286347 | — | — | 1 | 6.13 |
| CHEMBL603 | ZAFIRLUKAST | 4.0 | 1 | 5.61 |
| CHEMBL431348 | — | — | 1 | 5.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4280282 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4289768 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL48435 | — | EC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4279086 | — | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4294239 | — | EC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4290919 | — | EC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4288574 | — | EC50 | = | 670.0 | nM | 6.17 |
| CHEMBL4286347 | — | EC50 | = | 740.0 | nM | 6.13 |
| CHEMBL603 | ZAFIRLUKAST | EC50 | = | 2440.0 | nM | 5.61 |
| CHEMBL431348 | — | EC50 | = | 2490.0 | nM | 5.60 |