Assay Detail
Functional
CHEMBL943100
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Agonist activity at rat PPARalpha in rat H4IIE cells assessed as gene induction
58
Total Activities
58
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Cell Type | H4IIE |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Peroxisome proliferator-activated receptor alpha (CHEMBL2129) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Design and synthesis of indane-ureido-thioisobutyric acids: A novel class of PPARalpha agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 58 | 6.47 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL249865 | — | — | 1 | 8.70 |
| CHEMBL427710 | — | — | 1 | 7.64 |
| CHEMBL250036 | — | — | 1 | 7.50 |
| CHEMBL401315 | — | — | 1 | 7.48 |
| CHEMBL250041 | — | — | 1 | 7.34 |
| CHEMBL443585 | — | — | 1 | 7.02 |
| CHEMBL249868 | — | — | 1 | 6.98 |
| CHEMBL398684 | — | — | 1 | 6.93 |
| CHEMBL398722 | — | — | 1 | 6.85 |
| CHEMBL248857 | — | — | 1 | 6.84 |
| CHEMBL250894 | — | — | 1 | 6.80 |
| CHEMBL398700 | — | — | 1 | 6.80 |
| CHEMBL249869 | — | — | 1 | 6.80 |
| CHEMBL398723 | — | — | 1 | 6.78 |
| CHEMBL278590 | GSK-9578 | — | 1 | 6.78 |
| CHEMBL249866 | — | — | 1 | 6.78 |
| CHEMBL251422 | — | — | 1 | 6.77 |
| CHEMBL250042 | — | — | 1 | 6.75 |
| CHEMBL399089 | — | — | 1 | 6.71 |
| CHEMBL251062 | — | — | 1 | 6.68 |
| CHEMBL249871 | — | — | 1 | 6.66 |
| CHEMBL251063 | — | — | 1 | 6.64 |
| CHEMBL249870 | — | — | 1 | 6.60 |
| CHEMBL251240 | — | — | 1 | 6.60 |
| CHEMBL251239 | — | — | 1 | 6.60 |
| CHEMBL250896 | — | — | 1 | 6.58 |
| CHEMBL251421 | — | — | 1 | 6.53 |
| CHEMBL251064 | — | — | 1 | 6.41 |
| CHEMBL251065 | — | — | 1 | 6.37 |
| CHEMBL249867 | — | — | 1 | 6.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL249865 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL427710 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL250036 | — | EC50 | = | 32.0 | nM | 7.50 |
| CHEMBL401315 | — | EC50 | = | 33.0 | nM | 7.48 |
| CHEMBL250041 | — | EC50 | = | 46.0 | nM | 7.34 |
| CHEMBL443585 | — | EC50 | = | 96.0 | nM | 7.02 |
| CHEMBL249868 | — | EC50 | = | 105.0 | nM | 6.98 |
| CHEMBL398684 | — | EC50 | = | 117.0 | nM | 6.93 |
| CHEMBL398722 | — | EC50 | = | 141.0 | nM | 6.85 |
| CHEMBL248857 | — | EC50 | = | 146.0 | nM | 6.84 |
| CHEMBL250894 | — | EC50 | = | 158.0 | nM | 6.80 |
| CHEMBL398700 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL249869 | — | EC50 | = | 159.0 | nM | 6.80 |
| CHEMBL278590 | GSK-9578 | EC50 | = | 166.0 | nM | 6.78 |
| CHEMBL398723 | — | EC50 | = | 166.0 | nM | 6.78 |
| CHEMBL249866 | — | EC50 | = | 165.0 | nM | 6.78 |
| CHEMBL251422 | — | EC50 | = | 169.0 | nM | 6.77 |
| CHEMBL250042 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL399089 | — | EC50 | = | 195.0 | nM | 6.71 |
| CHEMBL251062 | — | EC50 | = | 210.0 | nM | 6.68 |
| CHEMBL249871 | — | EC50 | = | 219.0 | nM | 6.66 |
| CHEMBL251063 | — | EC50 | = | 229.0 | nM | 6.64 |
| CHEMBL249870 | — | EC50 | = | 249.0 | nM | 6.60 |
| CHEMBL251240 | — | EC50 | = | 252.0 | nM | 6.60 |
| CHEMBL251239 | — | EC50 | = | 252.0 | nM | 6.60 |
| CHEMBL250896 | — | EC50 | = | 260.0 | nM | 6.58 |
| CHEMBL251421 | — | EC50 | = | 294.0 | nM | 6.53 |
| CHEMBL251064 | — | EC50 | = | 386.0 | nM | 6.41 |
| CHEMBL251065 | — | EC50 | = | 425.0 | nM | 6.37 |
| CHEMBL249867 | — | EC50 | = | 561.0 | nM | 6.25 |
| CHEMBL249872 | — | EC50 | = | 598.0 | nM | 6.22 |
| CHEMBL398936 | — | EC50 | = | 707.0 | nM | 6.15 |
| CHEMBL250887 | — | EC50 | = | 910.0 | nM | 6.04 |
| CHEMBL398737 | — | EC50 | = | 1030.0 | nM | 5.99 |
| CHEMBL400094 | — | EC50 | = | 1110.0 | nM | 5.96 |
| CHEMBL250888 | — | EC50 | = | 1110.0 | nM | 5.96 |
| CHEMBL401116 | — | EC50 | = | 1270.0 | nM | 5.90 |
| CHEMBL251419 | — | EC50 | = | 1960.0 | nM | 5.71 |
| CHEMBL248854 | — | EC50 | = | 2090.0 | nM | 5.68 |
| CHEMBL250044 | — | EC50 | = | 2340.0 | nM | 5.63 |
| CHEMBL251420 | — | EC50 | = | 2670.0 | nM | 5.57 |
| CHEMBL248855 | — | EC50 | = | 2730.0 | nM | 5.56 |
| CHEMBL249864 | — | EC50 | = | 2850.0 | nM | 5.54 |
| CHEMBL400093 | — | EC50 | = | 4990.0 | nM | 5.30 |
| CHEMBL398448 | — | EC50 | = | 6390.0 | nM | 5.19 |
| CHEMBL251238 | — | EC50 | = | 7540.0 | nM | 5.12 |
| CHEMBL251237 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL400269 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL398447 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL248856 | — | EC50 | > | 13000.0 | nM | - |