Assay Detail
Functional
CHEMBL758986
Review assay metadata, readout intent, target linkage, and publication context from the same page.
in vitro agonist activity against peroxisome proliferator activated receptor-gamma (PPAR-gamma), using alkaline phosphatase activity transactivator assay
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Peroxisome proliferator-activated receptor gamma (CHEMBL235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 3. Structure-activity relationship and optimization of the N-aryl substituent.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 43 | 7.59 | 9.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2112870 | — | — | 1 | 9.55 |
| CHEMBL147770 | — | — | 1 | 9.52 |
| CHEMBL107367 | FARGLITAZAR | 2.0 | 1 | 9.47 |
| CHEMBL148668 | — | — | 1 | 9.24 |
| CHEMBL106666 | GW7845 | — | 1 | 9.15 |
| CHEMBL148300 | — | — | 1 | 9.04 |
| CHEMBL414442 | — | — | 1 | 9.04 |
| CHEMBL148596 | — | — | 1 | 8.85 |
| CHEMBL148384 | — | — | 1 | 8.83 |
| CHEMBL2112871 | — | — | 1 | 8.54 |
| CHEMBL146821 | — | — | 1 | 8.11 |
| CHEMBL149780 | — | — | 1 | 8.08 |
| CHEMBL150232 | — | — | 1 | 8.07 |
| CHEMBL347788 | — | — | 1 | 8.05 |
| CHEMBL146355 | — | — | 1 | 8.03 |
| CHEMBL146637 | — | — | 1 | 7.93 |
| CHEMBL345541 | — | — | 1 | 7.92 |
| CHEMBL2112020 | — | — | 1 | 7.82 |
| CHEMBL150215 | — | — | 1 | 7.78 |
| CHEMBL145824 | — | — | 1 | 7.76 |
| CHEMBL149714 | — | — | 1 | 7.74 |
| CHEMBL146217 | — | — | 1 | 7.62 |
| CHEMBL146530 | — | — | 1 | 7.61 |
| CHEMBL147419 | — | — | 1 | 7.49 |
| CHEMBL149381 | — | — | 1 | 7.49 |
| CHEMBL421781 | — | — | 1 | 7.42 |
| CHEMBL147021 | — | — | 1 | 7.42 |
| CHEMBL146579 | — | — | 1 | 7.40 |
| CHEMBL146584 | — | — | 1 | 7.34 |
| CHEMBL146562 | — | — | 1 | 7.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2112870 | — | EC50 | = | 0.2818 | nM | 9.55 |
| CHEMBL147770 | — | EC50 | = | 0.302 | nM | 9.52 |
| CHEMBL107367 | FARGLITAZAR | EC50 | = | 0.3388 | nM | 9.47 |
| CHEMBL148668 | — | EC50 | = | 0.5754 | nM | 9.24 |
| CHEMBL106666 | GW7845 | EC50 | = | 0.7079 | nM | 9.15 |
| CHEMBL148300 | — | EC50 | = | 0.912 | nM | 9.04 |
| CHEMBL414442 | — | EC50 | = | 0.912 | nM | 9.04 |
| CHEMBL148596 | — | EC50 | = | 1.413 | nM | 8.85 |
| CHEMBL148384 | — | EC50 | = | 1.479 | nM | 8.83 |
| CHEMBL2112871 | — | EC50 | = | 2.884 | nM | 8.54 |
| CHEMBL146821 | — | EC50 | = | 7.762 | nM | 8.11 |
| CHEMBL149780 | — | EC50 | = | 8.318 | nM | 8.08 |
| CHEMBL150232 | — | EC50 | = | 8.511 | nM | 8.07 |
| CHEMBL347788 | — | EC50 | = | 8.913 | nM | 8.05 |
| CHEMBL146355 | — | EC50 | = | 9.333 | nM | 8.03 |
| CHEMBL146637 | — | EC50 | = | 11.75 | nM | 7.93 |
| CHEMBL345541 | — | EC50 | = | 12.02 | nM | 7.92 |
| CHEMBL2112020 | — | EC50 | = | 15.14 | nM | 7.82 |
| CHEMBL150215 | — | EC50 | = | 16.6 | nM | 7.78 |
| CHEMBL145824 | — | EC50 | = | 17.38 | nM | 7.76 |
| CHEMBL149714 | — | EC50 | = | 18.2 | nM | 7.74 |
| CHEMBL146217 | — | EC50 | = | 23.99 | nM | 7.62 |
| CHEMBL146530 | — | EC50 | = | 24.55 | nM | 7.61 |
| CHEMBL147419 | — | EC50 | = | 32.36 | nM | 7.49 |
| CHEMBL149381 | — | EC50 | = | 32.36 | nM | 7.49 |
| CHEMBL421781 | — | EC50 | = | 38.02 | nM | 7.42 |
| CHEMBL147021 | — | EC50 | = | 38.02 | nM | 7.42 |
| CHEMBL146579 | — | EC50 | = | 39.81 | nM | 7.40 |
| CHEMBL146584 | — | EC50 | = | 45.71 | nM | 7.34 |
| CHEMBL146562 | — | EC50 | = | 63.1 | nM | 7.20 |
| CHEMBL146258 | — | EC50 | = | 89.13 | nM | 7.05 |
| CHEMBL145886 | — | EC50 | = | 117.49 | nM | 6.93 |
| CHEMBL145938 | — | EC50 | = | 208.93 | nM | 6.68 |
| CHEMBL359333 | — | EC50 | = | 229.09 | nM | 6.64 |
| CHEMBL359150 | — | EC50 | = | 407.38 | nM | 6.39 |
| CHEMBL344776 | — | EC50 | = | 416.87 | nM | 6.38 |
| CHEMBL146687 | — | EC50 | = | 562.34 | nM | 6.25 |
| CHEMBL147282 | — | EC50 | = | 758.58 | nM | 6.12 |
| CHEMBL342990 | — | EC50 | = | 4073.8 | nM | 5.39 |
| CHEMBL356353 | — | EC50 | = | 4897.79 | nM | 5.31 |
| CHEMBL149147 | — | EC50 | = | 7585.78 | nM | 5.12 |
| CHEMBL149309 | — | EC50 | = | 9332.54 | nM | 5.03 |
| CHEMBL2112021 | — | EC50 | < | 10000.0 | nM | - |