Assay Detail
Functional
CHEMBL883721
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro effective concentration against human peroxisome proliferator activated receptor gamma/Gal4 in cell-based transactivation assay
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Peroxisome proliferator-activated receptor gamma (CHEMBL235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis of new carbo- and heterocyclic analogues of 8-HETE and evaluation of their activity towards the PPARs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 26 | 6.35 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 8.40 |
| CHEMBL2113104 | — | — | 1 | 7.55 |
| CHEMBL2113105 | — | — | 1 | 6.47 |
| CHEMBL373318 | — | — | 1 | 6.26 |
| CHEMBL383607 | — | — | 1 | 6.21 |
| CHEMBL194698 | — | — | 1 | 6.19 |
| CHEMBL2113108 | — | — | 1 | 5.92 |
| CHEMBL198170 | — | — | 1 | 5.87 |
| CHEMBL197684 | — | — | 1 | 5.85 |
| CHEMBL2113107 | — | — | 1 | 5.82 |
| CHEMBL2113106 | — | — | 1 | 5.81 |
| CHEMBL2113109 | — | — | 1 | 5.80 |
| CHEMBL197268 | — | — | 1 | - |
| CHEMBL196260 | — | — | 1 | - |
| CHEMBL196261 | — | — | 1 | - |
| CHEMBL198034 | — | — | 1 | - |
| CHEMBL198166 | — | — | 1 | - |
| CHEMBL198163 | — | — | 1 | - |
| CHEMBL370374 | — | — | 1 | - |
| CHEMBL198708 | — | — | 1 | - |
| CHEMBL199125 | — | — | 1 | - |
| CHEMBL199121 | — | — | 1 | - |
| CHEMBL196139 | — | — | 1 | - |
| CHEMBL295416 | PIRINIXIC ACID | 2.0 | 1 | - |
| CHEMBL196227 | — | — | 1 | - |
| CHEMBL199172 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL121 | ROSIGLITAZONE | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2113104 | — | EC50 | = | 28.0 | nM | 7.55 |
| CHEMBL2113105 | — | EC50 | = | 340.0 | nM | 6.47 |
| CHEMBL373318 | — | EC50 | = | 549.0 | nM | 6.26 |
| CHEMBL383607 | — | EC50 | = | 617.0 | nM | 6.21 |
| CHEMBL194698 | — | EC50 | = | 642.0 | nM | 6.19 |
| CHEMBL2113108 | — | EC50 | = | 1195.0 | nM | 5.92 |
| CHEMBL198170 | — | EC50 | = | 1356.0 | nM | 5.87 |
| CHEMBL197684 | — | EC50 | = | 1413.0 | nM | 5.85 |
| CHEMBL2113107 | — | EC50 | = | 1503.0 | nM | 5.82 |
| CHEMBL2113106 | — | EC50 | = | 1546.0 | nM | 5.81 |
| CHEMBL2113109 | — | EC50 | = | 1566.0 | nM | 5.80 |
| CHEMBL197268 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL196260 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL196261 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL198034 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL198166 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL198163 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL370374 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL198708 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL199125 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL199121 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL196139 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL295416 | PIRINIXIC ACID | EC50 | > | 10000.0 | nM | - |
| CHEMBL196227 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL199172 | — | EC50 | > | 10000.0 | nM | - |