Assay Detail
Binding
CHEMBL2399380
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Antagonist activity at human GTS-tagged FXR after 20 mins by TR-FRET assay
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 |
Publication
Development of time resolved fluorescence resonance energy transfer-based assay for FXR antagonist discovery.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 5.41 | 6.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6067487 | IVERMECTIN | 4.0 | 1 | 6.58 |
| CHEMBL1358 | FULVESTRANT | 4.0 | 1 | 6.10 |
| CHEMBL282489 | — | — | 1 | 5.88 |
| CHEMBL45281 | — | — | 1 | 5.56 |
| CHEMBL998 | LORATADINE | 4.0 | 1 | 5.51 |
| CHEMBL104 | CLOTRIMAZOLE | 4.0 | 1 | 5.49 |
| CHEMBL306764 | — | — | 1 | 5.49 |
| CHEMBL409450 | 6BIO | — | 1 | 5.47 |
| CHEMBL21241 | GW7647 | — | 1 | 5.31 |
| CHEMBL1480 | FELODIPINE | 4.0 | 1 | 5.30 |
| CHEMBL1221 | SULCONAZOLE | 4.0 | 1 | 5.16 |
| CHEMBL1624 | LEVOTHYROXINE | 4.0 | 1 | 5.11 |
| CHEMBL109037 | — | — | 1 | 5.10 |
| CHEMBL1428 | NIMODIPINE | 4.0 | 1 | 5.05 |
| CHEMBL1256761 | — | — | 1 | 5.01 |
| CHEMBL81 | RALOXIFENE | 4.0 | 1 | 4.94 |
| CHEMBL2107430 | FLUTRIMAZOLE | 2.0 | 1 | 4.86 |
| CHEMBL410683 | GUGGULSTERONE | — | 1 | - |
| CHEMBL1478 | LITHOCHOLIC ACID | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6067487 | IVERMECTIN | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL1358 | FULVESTRANT | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL282489 | — | IC50 | = | 1310.0 | nM | 5.88 |
| CHEMBL45281 | — | IC50 | = | 2770.0 | nM | 5.56 |
| CHEMBL998 | LORATADINE | IC50 | = | 3070.0 | nM | 5.51 |
| CHEMBL104 | CLOTRIMAZOLE | IC50 | = | 3240.0 | nM | 5.49 |
| CHEMBL306764 | — | IC50 | = | 3220.0 | nM | 5.49 |
| CHEMBL409450 | 6BIO | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL21241 | GW7647 | IC50 | = | 4910.0 | nM | 5.31 |
| CHEMBL1480 | FELODIPINE | IC50 | = | 4960.0 | nM | 5.30 |
| CHEMBL1221 | SULCONAZOLE | IC50 | = | 6880.0 | nM | 5.16 |
| CHEMBL1624 | LEVOTHYROXINE | IC50 | = | 7860.0 | nM | 5.11 |
| CHEMBL109037 | — | IC50 | = | 7920.0 | nM | 5.10 |
| CHEMBL1428 | NIMODIPINE | IC50 | = | 8960.0 | nM | 5.05 |
| CHEMBL1256761 | — | IC50 | = | 9750.0 | nM | 5.01 |
| CHEMBL81 | RALOXIFENE | IC50 | = | 11560.0 | nM | 4.94 |
| CHEMBL2107430 | FLUTRIMAZOLE | IC50 | = | 13800.0 | nM | 4.86 |
| CHEMBL410683 | GUGGULSTERONE | IC50 | - | — | - | |
| CHEMBL1478 | LITHOCHOLIC ACID | IC50 | - | — | - |