Assay Detail
Binding
CHEMBL4368706
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist actvity in pFA-GAL4-DBD fused PPARgamma LBD (unknown origin) transfected in HEK293T cells assessed as inhibition of rosiglitazone-induced PPARgamma transactivation incubated for 24 hrs by luciferase reporter gene assay
35
Total Activities
35
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 gamma (CHEMBL235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure optimization of a new class of PPARγ antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 5.23 | 5.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4463449 | — | — | 1 | 5.72 |
| CHEMBL4561516 | — | — | 1 | 5.64 |
| CHEMBL4577891 | — | — | 1 | 5.60 |
| CHEMBL4460559 | — | — | 1 | 5.58 |
| CHEMBL4564535 | — | — | 1 | 5.50 |
| CHEMBL4438749 | — | — | 1 | 5.46 |
| CHEMBL4450797 | — | — | 1 | 5.41 |
| CHEMBL4469210 | — | — | 1 | 5.41 |
| CHEMBL4539507 | — | — | 1 | 5.38 |
| CHEMBL3397721 | — | — | 1 | 5.37 |
| CHEMBL4557705 | — | — | 1 | 5.33 |
| CHEMBL4467078 | — | — | 1 | 5.33 |
| CHEMBL4440578 | — | — | 1 | 5.30 |
| CHEMBL4579845 | — | — | 1 | 5.24 |
| CHEMBL4516607 | — | — | 1 | 5.21 |
| CHEMBL4448302 | — | — | 1 | 5.21 |
| CHEMBL4460064 | — | — | 1 | 5.14 |
| CHEMBL4546295 | — | — | 1 | 5.12 |
| CHEMBL4436200 | — | — | 1 | 5.08 |
| CHEMBL4558793 | — | — | 1 | 5.03 |
| CHEMBL4533671 | — | — | 1 | 5.02 |
| CHEMBL4550568 | — | — | 1 | 5.02 |
| CHEMBL4532632 | — | — | 1 | 4.96 |
| CHEMBL4440852 | — | — | 1 | 4.88 |
| CHEMBL4528757 | — | — | 1 | 4.82 |
| CHEMBL4438177 | — | — | 1 | 4.80 |
| CHEMBL4465395 | — | — | 1 | 4.62 |
| CHEMBL4438636 | — | — | 1 | - |
| CHEMBL4458082 | — | — | 1 | - |
| CHEMBL4467971 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4463449 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4561516 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL4577891 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4460559 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL4564535 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL4438749 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL4450797 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL4469210 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL4539507 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL3397721 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL4557705 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL4467078 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL4440578 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL4579845 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL4448302 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL4516607 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL4460064 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL4546295 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL4436200 | — | IC50 | = | 8400.0 | nM | 5.08 |
| CHEMBL4558793 | — | IC50 | = | 9400.0 | nM | 5.03 |
| CHEMBL4533671 | — | IC50 | = | 9600.0 | nM | 5.02 |
| CHEMBL4550568 | — | IC50 | = | 9500.0 | nM | 5.02 |
| CHEMBL4532632 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL4440852 | — | IC50 | = | 13100.0 | nM | 4.88 |
| CHEMBL4528757 | — | IC50 | = | 15100.0 | nM | 4.82 |
| CHEMBL4438177 | — | IC50 | = | 15800.0 | nM | 4.80 |
| CHEMBL4465395 | — | IC50 | = | 23900.0 | nM | 4.62 |
| CHEMBL4438636 | — | IC50 | - | — | - | |
| CHEMBL4458082 | — | IC50 | - | — | - | |
| CHEMBL4467971 | — | IC50 | - | — | - | |
| CHEMBL4435190 | — | IC50 | - | — | - | |
| CHEMBL4450373 | — | IC50 | - | — | - | |
| CHEMBL4572326 | — | IC50 | - | — | - | |
| CHEMBL4572658 | — | IC50 | - | — | - | |
| CHEMBL4536044 | — | IC50 | - | — | - |