Assay Detail
Binding
CHEMBL980782
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Displacement of [3H]2AD-5075 from GST-tagged human PPARgamma receptor expressed in Escherichia coli BL21
19
Total Activities
19
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
Highly functionalized 7-azaindoles as selective PPAR gamma modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.96 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL460072 | — | — | 1 | 9.00 |
| CHEMBL452051 | — | — | 1 | 9.00 |
| CHEMBL460073 | — | — | 1 | 8.70 |
| CHEMBL462378 | — | — | 1 | 8.70 |
| CHEMBL461944 | — | — | 1 | 8.52 |
| CHEMBL518499 | — | — | 1 | 8.52 |
| CHEMBL509236 | — | — | 1 | 8.40 |
| CHEMBL455127 | — | — | 1 | 8.30 |
| CHEMBL507477 | — | — | 1 | 8.00 |
| CHEMBL461378 | — | — | 1 | 7.82 |
| CHEMBL510180 | — | — | 1 | 7.80 |
| CHEMBL517436 | — | — | 1 | 7.66 |
| CHEMBL461379 | — | — | 1 | 7.64 |
| CHEMBL452054 | — | — | 1 | 7.60 |
| CHEMBL509369 | — | — | 1 | 7.27 |
| CHEMBL455126 | — | — | 1 | 7.18 |
| CHEMBL455130 | — | — | 1 | 6.97 |
| CHEMBL452299 | — | — | 1 | 6.14 |
| CHEMBL459466 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL460072 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL452051 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL460073 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL462378 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL461944 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL518499 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL509236 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL455127 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL507477 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL461378 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL510180 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL517436 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL461379 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL452054 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL509369 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL455126 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL455130 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL452299 | — | IC50 | = | 726.0 | nM | 6.14 |
| CHEMBL459466 | — | IC50 | < | 1.0 | nM | - |