Assay Detail
Binding
CHEMBL4344571
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human PPARalpha expressed in nonhuman mammalian cells assessed as increase in receptor transcriptional activity incubated for 22 to 24 hrs by luciferase reporter gene assay
30
Total Activities
30
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 alpha (CHEMBL239) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Evolution of a 4-Benzyloxy-benzylamino Chemotype to Provide Efficacious, Potent, and Isoform Selective PPARα Agonists as Leads for Retinal Disorders.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 30 | 6.37 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL219586 | GW590735 | 2.0 | 1 | 7.82 |
| CHEMBL4455560 | — | — | 1 | 7.75 |
| CHEMBL4550448 | — | — | 1 | 7.57 |
| CHEMBL4455529 | — | — | 1 | 7.54 |
| CHEMBL4437601 | — | — | 1 | 7.51 |
| CHEMBL4463341 | — | — | 1 | 7.43 |
| CHEMBL4592059 | — | — | 1 | 7.40 |
| CHEMBL4448658 | — | — | 1 | 7.28 |
| CHEMBL4540905 | — | — | 1 | 7.25 |
| CHEMBL4465958 | — | — | 1 | 7.17 |
| CHEMBL4468359 | — | — | 1 | 6.44 |
| CHEMBL4466987 | — | — | 1 | 6.27 |
| CHEMBL4454550 | — | — | 1 | 6.24 |
| CHEMBL4561177 | — | — | 1 | 6.13 |
| CHEMBL4564731 | — | — | 1 | 6.11 |
| CHEMBL4468237 | — | — | 1 | 6.09 |
| CHEMBL4245047 | — | — | 1 | 6.08 |
| CHEMBL4448919 | — | — | 1 | 6.05 |
| CHEMBL4591150 | — | — | 1 | 6.03 |
| CHEMBL4443452 | — | — | 1 | 6.02 |
| CHEMBL4448458 | — | — | 1 | 6.01 |
| CHEMBL4476782 | — | — | 1 | 5.95 |
| CHEMBL4458366 | — | — | 1 | 5.93 |
| CHEMBL4473188 | — | — | 1 | 5.84 |
| CHEMBL4471493 | — | — | 1 | 5.84 |
| CHEMBL4513352 | — | — | 1 | 5.79 |
| CHEMBL4237449 | — | — | 1 | 5.35 |
| CHEMBL4467075 | — | — | 1 | 5.07 |
| CHEMBL4240680 | — | — | 1 | 4.60 |
| CHEMBL4465679 | — | — | 1 | 4.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL219586 | GW590735 | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4455560 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4550448 | — | EC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4455529 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4437601 | — | EC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4463341 | — | EC50 | = | 37.0 | nM | 7.43 |
| CHEMBL4592059 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4448658 | — | EC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4540905 | — | EC50 | = | 56.0 | nM | 7.25 |
| CHEMBL4465958 | — | EC50 | = | 67.0 | nM | 7.17 |
| CHEMBL4468359 | — | EC50 | = | 360.0 | nM | 6.44 |
| CHEMBL4466987 | — | EC50 | = | 540.0 | nM | 6.27 |
| CHEMBL4454550 | — | EC50 | = | 580.0 | nM | 6.24 |
| CHEMBL4561177 | — | EC50 | = | 740.0 | nM | 6.13 |
| CHEMBL4564731 | — | EC50 | = | 770.0 | nM | 6.11 |
| CHEMBL4468237 | — | EC50 | = | 810.0 | nM | 6.09 |
| CHEMBL4245047 | — | EC50 | = | 830.0 | nM | 6.08 |
| CHEMBL4448919 | — | EC50 | = | 900.0 | nM | 6.05 |
| CHEMBL4591150 | — | EC50 | = | 930.0 | nM | 6.03 |
| CHEMBL4443452 | — | EC50 | = | 960.0 | nM | 6.02 |
| CHEMBL4448458 | — | EC50 | = | 970.0 | nM | 6.01 |
| CHEMBL4476782 | — | EC50 | = | 1120.0 | nM | 5.95 |
| CHEMBL4458366 | — | EC50 | = | 1180.0 | nM | 5.93 |
| CHEMBL4473188 | — | EC50 | = | 1450.0 | nM | 5.84 |
| CHEMBL4471493 | — | EC50 | = | 1450.0 | nM | 5.84 |
| CHEMBL4513352 | — | EC50 | = | 1610.0 | nM | 5.79 |
| CHEMBL4237449 | — | EC50 | = | 4430.0 | nM | 5.35 |
| CHEMBL4467075 | — | EC50 | = | 8520.0 | nM | 5.07 |
| CHEMBL4240680 | — | EC50 | = | 25300.0 | nM | 4.60 |
| CHEMBL4465679 | — | EC50 | = | 25600.0 | nM | 4.59 |