Assay Detail
Binding
CHEMBL5148482
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Agonist activity at Gal4-fused human FXR in HEK293 cells incubated for 15 min by luciferase reporter assay
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of BMS-986339, a Pharmacologically Differentiated Farnesoid X Receptor Agonist for the Treatment of Nonalcoholic Steatohepatitis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 33 | 6.96 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5181899 | — | — | 1 | 7.60 |
| CHEMBL5202191 | — | — | 1 | 7.60 |
| CHEMBL5187016 | — | — | 1 | 7.57 |
| CHEMBL5170740 | — | — | 1 | 7.54 |
| CHEMBL5182534 | — | — | 1 | 7.47 |
| CHEMBL5177647 | — | — | 1 | 7.39 |
| CHEMBL5189418 | — | — | 1 | 7.36 |
| CHEMBL5190243 | — | — | 1 | 7.35 |
| CHEMBL4862974 | — | — | 1 | 7.28 |
| CHEMBL5169696 | — | — | 1 | 7.24 |
| CHEMBL5174333 | — | — | 1 | 7.23 |
| CHEMBL5190997 | — | — | 1 | 7.18 |
| CHEMBL5172239 | — | — | 1 | 7.16 |
| CHEMBL5174082 | — | — | 1 | 7.04 |
| CHEMBL5180682 | — | — | 1 | 7.03 |
| CHEMBL5178176 | — | — | 1 | 7.02 |
| CHEMBL5182204 | — | — | 1 | 6.98 |
| CHEMBL5173549 | — | — | 1 | 6.96 |
| CHEMBL5203086 | — | — | 1 | 6.96 |
| CHEMBL5199184 | — | — | 1 | 6.94 |
| CHEMBL5184707 | — | — | 1 | 6.93 |
| CHEMBL5196639 | — | — | 1 | 6.85 |
| CHEMBL5184419 | — | — | 1 | 6.83 |
| CHEMBL5205123 | — | — | 1 | 6.82 |
| CHEMBL5178315 | — | — | 1 | 6.82 |
| CHEMBL5189617 | — | — | 1 | 6.77 |
| CHEMBL5194619 | — | — | 1 | 6.64 |
| CHEMBL5208567 | — | — | 1 | 6.63 |
| CHEMBL5191475 | — | — | 1 | 6.52 |
| CHEMBL5204574 | — | — | 1 | 6.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5181899 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5202191 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5187016 | — | EC50 | = | 27.0 | nM | 7.57 |
| CHEMBL5170740 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5182534 | — | EC50 | = | 34.0 | nM | 7.47 |
| CHEMBL5177647 | — | EC50 | = | 41.0 | nM | 7.39 |
| CHEMBL5189418 | — | EC50 | = | 44.0 | nM | 7.36 |
| CHEMBL5190243 | — | EC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4862974 | — | EC50 | = | 53.0 | nM | 7.28 |
| CHEMBL5169696 | — | EC50 | = | 57.0 | nM | 7.24 |
| CHEMBL5174333 | — | EC50 | = | 59.0 | nM | 7.23 |
| CHEMBL5190997 | — | EC50 | = | 66.0 | nM | 7.18 |
| CHEMBL5172239 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL5174082 | — | EC50 | = | 92.0 | nM | 7.04 |
| CHEMBL5180682 | — | EC50 | = | 93.0 | nM | 7.03 |
| CHEMBL5178176 | — | EC50 | = | 95.0 | nM | 7.02 |
| CHEMBL5182204 | — | EC50 | = | 104.0 | nM | 6.98 |
| CHEMBL5173549 | — | EC50 | = | 111.0 | nM | 6.96 |
| CHEMBL5203086 | — | EC50 | = | 111.0 | nM | 6.96 |
| CHEMBL5199184 | — | EC50 | = | 114.0 | nM | 6.94 |
| CHEMBL5184707 | — | EC50 | = | 118.0 | nM | 6.93 |
| CHEMBL5196639 | — | EC50 | = | 142.0 | nM | 6.85 |
| CHEMBL5184419 | — | EC50 | = | 149.0 | nM | 6.83 |
| CHEMBL5205123 | — | EC50 | = | 152.0 | nM | 6.82 |
| CHEMBL5178315 | — | EC50 | = | 152.0 | nM | 6.82 |
| CHEMBL5189617 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL5194619 | — | EC50 | = | 228.0 | nM | 6.64 |
| CHEMBL5208567 | — | EC50 | = | 232.0 | nM | 6.63 |
| CHEMBL5191475 | — | EC50 | = | 299.0 | nM | 6.52 |
| CHEMBL5204574 | — | EC50 | = | 538.0 | nM | 6.27 |
| CHEMBL5201654 | — | EC50 | = | 919.0 | nM | 6.04 |
| CHEMBL5204648 | — | EC50 | = | 1092.0 | nM | 5.96 |
| CHEMBL5205416 | — | EC50 | = | 1638.0 | nM | 5.79 |