Assay Detail
Binding
CHEMBL5538267
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Antagonist activity against human FXR transfected in HEK293T cells co-transfected with pCDNA-hFXR and pRL-TK incubated for 24 hrs by dual-luciferase reporter assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of 4-aminophenylacetamide derivatives as intestine-specific farnesoid X receptor antagonists for the potential treatment of nonalcoholic steatohepatitis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 5.17 | 6.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5568904 | — | — | 1 | 6.05 |
| CHEMBL5567170 | — | — | 1 | 5.86 |
| CHEMBL5595315 | — | — | 1 | 5.57 |
| CHEMBL5571821 | — | — | 1 | 5.54 |
| CHEMBL5569389 | — | — | 1 | 5.45 |
| CHEMBL5564082 | — | — | 1 | 5.43 |
| CHEMBL5570505 | — | — | 1 | 5.37 |
| CHEMBL5574125 | — | — | 1 | 5.30 |
| CHEMBL5567095 | — | — | 1 | 5.29 |
| CHEMBL5571011 | — | — | 1 | 5.24 |
| CHEMBL5574735 | — | — | 1 | 5.20 |
| CHEMBL5568984 | — | — | 1 | 5.18 |
| CHEMBL5566799 | — | — | 1 | 5.18 |
| CHEMBL5563884 | — | — | 1 | 5.16 |
| CHEMBL5569132 | — | — | 1 | 5.14 |
| CHEMBL5565546 | — | — | 1 | 5.06 |
| CHEMBL5571410 | — | — | 1 | 5.03 |
| CHEMBL5570321 | — | — | 1 | 4.94 |
| CHEMBL5591721 | — | — | 1 | 4.87 |
| CHEMBL5595380 | — | — | 1 | 4.83 |
| CHEMBL5566319 | — | — | 1 | 4.83 |
| CHEMBL272427 | TAURURSODIOL | 4.0 | 1 | 4.17 |
| CHEMBL410683 | GUGGULSTERONE | — | 1 | 4.13 |
| CHEMBL5563435 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5568904 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL5567170 | — | IC50 | = | 1370.0 | nM | 5.86 |
| CHEMBL5595315 | — | IC50 | = | 2670.0 | nM | 5.57 |
| CHEMBL5571821 | — | IC50 | = | 2850.0 | nM | 5.54 |
| CHEMBL5569389 | — | IC50 | = | 3570.0 | nM | 5.45 |
| CHEMBL5564082 | — | IC50 | = | 3710.0 | nM | 5.43 |
| CHEMBL5570505 | — | IC50 | = | 4270.0 | nM | 5.37 |
| CHEMBL5574125 | — | IC50 | = | 4990.0 | nM | 5.30 |
| CHEMBL5567095 | — | IC50 | = | 5170.0 | nM | 5.29 |
| CHEMBL5571011 | — | IC50 | = | 5820.0 | nM | 5.24 |
| CHEMBL5574735 | — | IC50 | = | 6270.0 | nM | 5.20 |
| CHEMBL5568984 | — | IC50 | = | 6640.0 | nM | 5.18 |
| CHEMBL5566799 | — | IC50 | = | 6650.0 | nM | 5.18 |
| CHEMBL5563884 | — | IC50 | = | 6930.0 | nM | 5.16 |
| CHEMBL5569132 | — | IC50 | = | 7310.0 | nM | 5.14 |
| CHEMBL5565546 | — | IC50 | = | 8770.0 | nM | 5.06 |
| CHEMBL5571410 | — | IC50 | = | 9240.0 | nM | 5.03 |
| CHEMBL5570321 | — | IC50 | = | 11600.0 | nM | 4.94 |
| CHEMBL5591721 | — | IC50 | = | 13460.0 | nM | 4.87 |
| CHEMBL5595380 | — | IC50 | = | 14650.0 | nM | 4.83 |
| CHEMBL5566319 | — | IC50 | = | 14840.0 | nM | 4.83 |
| CHEMBL272427 | TAURURSODIOL | IC50 | = | 68220.0 | nM | 4.17 |
| CHEMBL410683 | GUGGULSTERONE | IC50 | = | 74360.0 | nM | 4.13 |
| CHEMBL5563435 | — | IC50 | - | — | - |