Assay Detail
Binding
CHEMBL1114856
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human PPARdelta ligand binding domain expressed in human 293T cells co-transfected with Gal4-DBD by luciferase transactivation assay
136
Total Activities
136
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | 293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor delta (CHEMBL3979) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Novel bisaryl substituted thiazoles and oxazoles as highly potent and selective peroxisome proliferator-activated receptor delta agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 136 | 7.08 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1080365 | — | — | 1 | 9.00 |
| CHEMBL1075895 | — | — | 1 | 9.00 |
| CHEMBL1075732 | — | — | 1 | 9.00 |
| CHEMBL1075723 | — | — | 1 | 8.70 |
| CHEMBL1075894 | — | — | 1 | 8.70 |
| CHEMBL1080368 | — | — | 1 | 8.52 |
| CHEMBL1075836 | — | — | 1 | 8.52 |
| CHEMBL1081917 | — | — | 1 | 8.52 |
| CHEMBL1075683 | — | — | 1 | 8.40 |
| CHEMBL38943 | GW501516 | 2.0 | 1 | 8.30 |
| CHEMBL1075724 | — | — | 1 | 8.22 |
| CHEMBL1080172 | — | — | 1 | 8.22 |
| CHEMBL1080349 | — | — | 1 | 8.15 |
| CHEMBL1080173 | — | — | 1 | 8.15 |
| CHEMBL1082118 | — | — | 1 | 8.10 |
| CHEMBL1079752 | — | — | 1 | 8.10 |
| CHEMBL1079505 | — | — | 1 | 8.10 |
| CHEMBL1080822 | — | — | 1 | 8.05 |
| CHEMBL1076162 | — | — | 1 | 8.05 |
| CHEMBL1080109 | — | — | 1 | 8.05 |
| CHEMBL1081601 | — | — | 1 | 8.00 |
| CHEMBL1082114 | — | — | 1 | 8.00 |
| CHEMBL1082137 | — | — | 1 | 8.00 |
| CHEMBL1079910 | — | — | 1 | 8.00 |
| CHEMBL1079911 | — | — | 1 | 8.00 |
| CHEMBL1075682 | — | — | 1 | 8.00 |
| CHEMBL210469 | — | — | 1 | 8.00 |
| CHEMBL1081546 | — | — | 1 | 7.96 |
| CHEMBL1080823 | — | — | 1 | 7.96 |
| CHEMBL279053 | L-165461 | — | 1 | 7.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1080365 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1075732 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1075895 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1075894 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1075723 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1075836 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1081917 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1080368 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1075683 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL38943 | GW501516 | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1075724 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1080172 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1080173 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1080349 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1082118 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1079505 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1079752 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1080822 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1076162 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1080109 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1079910 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1079911 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1082137 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1081601 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1075682 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL210469 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1082114 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1081546 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1080823 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL279053 | L-165461 | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1075703 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1080184 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1079983 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1079965 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1081962 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1076163 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1075835 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1075725 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1079826 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1081763 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1079449 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1081224 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL1080188 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL1081046 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1080143 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1080369 | — | EC50 | = | 31.0 | nM | 7.51 |
| CHEMBL1079925 | — | EC50 | = | 32.0 | nM | 7.50 |
| CHEMBL1079984 | — | EC50 | = | 34.0 | nM | 7.47 |
| CHEMBL1080108 | — | EC50 | = | 35.0 | nM | 7.46 |
| CHEMBL1081749 | — | EC50 | = | 40.0 | nM | 7.40 |