Assay Detail
Binding
CHEMBL5522907
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Agonist activity at GST-tagged human FXR LBD using SRCI coactivator peptide by Alphascreen 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 |
Publication
Discovery and Optimization of Novel Nonbile Acid FXR Agonists as Preclinical Candidates for the Treatment of Inflammatory Bowel Disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 35 | 6.14 | 6.97 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3746388 | TERN-101 | 2.0 | 1 | 6.97 |
| CHEMBL5555964 | — | — | 1 | 6.72 |
| CHEMBL5556964 | — | — | 1 | 6.61 |
| CHEMBL5560140 | — | — | 1 | 6.60 |
| CHEMBL5559957 | — | — | 1 | 6.56 |
| CHEMBL5560772 | — | — | 1 | 6.46 |
| CHEMBL5567573 | — | — | 1 | 6.42 |
| CHEMBL5563110 | — | — | 1 | 6.38 |
| CHEMBL5561797 | — | — | 1 | 6.34 |
| CHEMBL5559067 | — | — | 1 | 6.33 |
| CHEMBL5564635 | — | — | 1 | 6.33 |
| CHEMBL5558528 | — | — | 1 | 6.31 |
| CHEMBL5561445 | — | — | 1 | 6.28 |
| CHEMBL5556116 | — | — | 1 | 6.27 |
| CHEMBL5564138 | — | — | 1 | 6.20 |
| CHEMBL5568192 | — | — | 1 | 6.18 |
| CHEMBL5561496 | — | — | 1 | 6.17 |
| CHEMBL5560179 | — | — | 1 | 6.15 |
| CHEMBL5563946 | — | — | 1 | 6.14 |
| CHEMBL5568180 | — | — | 1 | 6.10 |
| CHEMBL5561027 | — | — | 1 | 6.08 |
| CHEMBL5565429 | — | — | 1 | 6.04 |
| CHEMBL5557131 | — | — | 1 | 6.04 |
| CHEMBL5555480 | — | — | 1 | 6.03 |
| CHEMBL5561278 | — | — | 1 | 6.02 |
| CHEMBL5542969 | — | — | 1 | 5.98 |
| CHEMBL5549875 | — | — | 1 | 5.97 |
| CHEMBL5564776 | — | — | 1 | 5.95 |
| CHEMBL5558779 | — | — | 1 | 5.94 |
| CHEMBL5561500 | — | — | 1 | 5.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3746388 | TERN-101 | EC50 | = | 106.0 | nM | 6.97 |
| CHEMBL5555964 | — | EC50 | = | 188.9 | nM | 6.72 |
| CHEMBL5556964 | — | EC50 | = | 247.8 | nM | 6.61 |
| CHEMBL5560140 | — | EC50 | = | 253.3 | nM | 6.60 |
| CHEMBL5559957 | — | EC50 | = | 274.3 | nM | 6.56 |
| CHEMBL5560772 | — | EC50 | = | 350.8 | nM | 6.46 |
| CHEMBL5567573 | — | EC50 | = | 377.5 | nM | 6.42 |
| CHEMBL5563110 | — | EC50 | = | 415.0 | nM | 6.38 |
| CHEMBL5561797 | — | EC50 | = | 459.1 | nM | 6.34 |
| CHEMBL5559067 | — | EC50 | = | 471.3 | nM | 6.33 |
| CHEMBL5564635 | — | EC50 | = | 464.5 | nM | 6.33 |
| CHEMBL5558528 | — | EC50 | = | 491.5 | nM | 6.31 |
| CHEMBL5561445 | — | EC50 | = | 522.2 | nM | 6.28 |
| CHEMBL5556116 | — | EC50 | = | 540.4 | nM | 6.27 |
| CHEMBL5564138 | — | EC50 | = | 636.6 | nM | 6.20 |
| CHEMBL5568192 | — | EC50 | = | 663.8 | nM | 6.18 |
| CHEMBL5561496 | — | EC50 | = | 671.6 | nM | 6.17 |
| CHEMBL5560179 | — | EC50 | = | 704.1 | nM | 6.15 |
| CHEMBL5563946 | — | EC50 | = | 718.8 | nM | 6.14 |
| CHEMBL5568180 | — | EC50 | = | 787.9 | nM | 6.10 |
| CHEMBL5561027 | — | EC50 | = | 839.5 | nM | 6.08 |
| CHEMBL5565429 | — | EC50 | = | 911.2 | nM | 6.04 |
| CHEMBL5557131 | — | EC50 | = | 923.2 | nM | 6.04 |
| CHEMBL5555480 | — | EC50 | = | 940.4 | nM | 6.03 |
| CHEMBL5561278 | — | EC50 | = | 961.8 | nM | 6.02 |
| CHEMBL5542969 | — | EC50 | = | 1040.5 | nM | 5.98 |
| CHEMBL5549875 | — | EC50 | = | 1067.8 | nM | 5.97 |
| CHEMBL5564776 | — | EC50 | = | 1110.7 | nM | 5.95 |
| CHEMBL5558779 | — | EC50 | = | 1154.0 | nM | 5.94 |
| CHEMBL5561500 | — | EC50 | = | 1765.0 | nM | 5.75 |
| CHEMBL5563833 | — | EC50 | = | 1968.0 | nM | 5.71 |
| CHEMBL5557829 | — | EC50 | = | 1934.5 | nM | 5.71 |
| CHEMBL5555199 | — | EC50 | = | 2524.5 | nM | 5.60 |
| CHEMBL5558721 | — | EC50 | = | 3645.5 | nM | 5.44 |
| CHEMBL5561681 | — | EC50 | = | 8443.5 | nM | 5.07 |