Assay Detail
Binding
CHEMBL4023601
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Transactivation of human GAL4-fused PPARalpha LBD expressed in African green monkey COS7 cells co-expressing 5Gal4 pGL3 TK Luc after overnight incubation by luciferase reporter gene assay
32
Total Activities
32
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
Design, Synthesis, and Evaluation of a Novel Series of Indole Sulfonamide Peroxisome Proliferator Activated Receptor (PPAR) α/γ/δ Triple Activators: Discovery of Lanifibranor, a New Antifibrotic Clinical Candidate.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 32 | 6.01 | 6.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4103575 | — | — | 1 | 6.80 |
| CHEMBL4074391 | — | — | 1 | 6.58 |
| CHEMBL4093146 | — | — | 1 | 6.52 |
| CHEMBL4083589 | — | — | 1 | 6.39 |
| CHEMBL4072395 | — | — | 1 | 6.38 |
| CHEMBL4060007 | — | — | 1 | 6.12 |
| CHEMBL4101596 | — | — | 1 | 6.10 |
| CHEMBL4062472 | — | — | 1 | 6.04 |
| CHEMBL4094877 | — | — | 1 | 6.02 |
| CHEMBL4081907 | — | — | 1 | 5.93 |
| CHEMBL4079308 | — | — | 1 | 5.92 |
| CHEMBL4104907 | — | — | 1 | 5.90 |
| CHEMBL4073181 | — | — | 1 | 5.90 |
| CHEMBL4095821 | — | — | 1 | 5.89 |
| CHEMBL4091374 | LANIFIBRANOR | 3.0 | 1 | 5.81 |
| CHEMBL4066889 | — | — | 1 | 5.79 |
| CHEMBL4098415 | — | — | 1 | 5.71 |
| CHEMBL4087052 | — | — | 1 | 5.63 |
| CHEMBL4067479 | — | — | 1 | 5.62 |
| CHEMBL4071373 | — | — | 1 | 5.56 |
| CHEMBL4062724 | — | — | 1 | 5.55 |
| CHEMBL4068482 | — | — | 1 | - |
| CHEMBL4089775 | — | — | 1 | - |
| CHEMBL4087194 | — | — | 1 | - |
| CHEMBL4065772 | — | — | 1 | - |
| CHEMBL4090691 | — | — | 1 | - |
| CHEMBL4072143 | — | — | 1 | - |
| CHEMBL4093864 | — | — | 1 | - |
| CHEMBL4095891 | — | — | 1 | - |
| CHEMBL4075456 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4103575 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4074391 | — | EC50 | = | 260.0 | nM | 6.58 |
| CHEMBL4093146 | — | EC50 | = | 305.0 | nM | 6.52 |
| CHEMBL4083589 | — | EC50 | = | 410.0 | nM | 6.39 |
| CHEMBL4072395 | — | EC50 | = | 419.0 | nM | 6.38 |
| CHEMBL4060007 | — | EC50 | = | 764.0 | nM | 6.12 |
| CHEMBL4101596 | — | EC50 | = | 790.0 | nM | 6.10 |
| CHEMBL4062472 | — | EC50 | = | 901.0 | nM | 6.04 |
| CHEMBL4094877 | — | EC50 | = | 956.0 | nM | 6.02 |
| CHEMBL4081907 | — | EC50 | = | 1164.0 | nM | 5.93 |
| CHEMBL4079308 | — | EC50 | = | 1198.0 | nM | 5.92 |
| CHEMBL4104907 | — | EC50 | = | 1263.0 | nM | 5.90 |
| CHEMBL4073181 | — | EC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL4095821 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4091374 | LANIFIBRANOR | EC50 | = | 1537.0 | nM | 5.81 |
| CHEMBL4066889 | — | EC50 | = | 1620.0 | nM | 5.79 |
| CHEMBL4098415 | — | EC50 | = | 1963.0 | nM | 5.71 |
| CHEMBL4087052 | — | EC50 | = | 2360.0 | nM | 5.63 |
| CHEMBL4067479 | — | EC50 | = | 2421.0 | nM | 5.62 |
| CHEMBL4071373 | — | EC50 | = | 2756.0 | nM | 5.56 |
| CHEMBL4062724 | — | EC50 | = | 2824.0 | nM | 5.55 |
| CHEMBL4068482 | — | EC50 | - | — | - | |
| CHEMBL4089775 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL4087194 | — | EC50 | - | — | - | |
| CHEMBL4065772 | — | EC50 | - | — | - | |
| CHEMBL4090691 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL4072143 | — | EC50 | - | — | - | |
| CHEMBL4093864 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL4095891 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL4075456 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL4088168 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL4063529 | — | EC50 | - | — | - |