Assay Detail
Binding
CHEMBL4702899
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Agonist activity at human FXR expressed in HEK293 cells measured after 18 hrs by steady-glo luciferase reporter gene assay
39
Total Activities
39
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 and Optimization of Non-bile Acid FXR Agonists as Preclinical Candidates for the Treatment of Nonalcoholic Steatohepatitis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 39 | 7.31 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4751757 | — | — | 1 | 9.40 |
| CHEMBL4781153 | — | — | 1 | 9.30 |
| CHEMBL4794704 | — | — | 1 | 9.15 |
| CHEMBL4780363 | — | — | 1 | 9.00 |
| CHEMBL4763830 | — | — | 1 | 8.89 |
| CHEMBL4749142 | — | — | 1 | 8.82 |
| CHEMBL4791413 | — | — | 1 | 8.55 |
| CHEMBL3746388 | TERN-101 | 2.0 | 1 | 8.40 |
| CHEMBL4776080 | — | — | 1 | 8.37 |
| CHEMBL4741830 | — | — | 1 | 8.28 |
| CHEMBL4751890 | — | — | 1 | 8.24 |
| CHEMBL4753329 | — | — | 1 | 8.12 |
| CHEMBL4747855 | — | — | 1 | 8.06 |
| CHEMBL4778278 | — | — | 1 | 7.96 |
| CHEMBL318457 | — | — | 1 | 7.92 |
| CHEMBL4756996 | — | — | 1 | 7.70 |
| CHEMBL4743486 | — | — | 1 | 7.46 |
| CHEMBL4763935 | — | — | 1 | 7.43 |
| CHEMBL4779832 | — | — | 1 | 7.33 |
| CHEMBL4747240 | — | — | 1 | 7.22 |
| CHEMBL4800066 | — | — | 1 | 7.19 |
| CHEMBL4800163 | — | — | 1 | 7.02 |
| CHEMBL4786636 | — | — | 1 | 7.00 |
| CHEMBL4757540 | — | — | 1 | 6.85 |
| CHEMBL4742812 | — | — | 1 | 6.85 |
| CHEMBL4745499 | — | — | 1 | 6.75 |
| CHEMBL4751112 | — | — | 1 | 6.75 |
| CHEMBL4746270 | — | — | 1 | 6.64 |
| CHEMBL4791913 | — | — | 1 | 6.57 |
| CHEMBL4763612 | — | — | 1 | 6.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4751757 | — | EC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4781153 | — | EC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4794704 | — | EC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4780363 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4763830 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4749142 | — | EC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4791413 | — | EC50 | = | 2.8 | nM | 8.55 |
| CHEMBL3746388 | TERN-101 | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4776080 | — | EC50 | = | 4.3 | nM | 8.37 |
| CHEMBL4741830 | — | EC50 | = | 5.2 | nM | 8.28 |
| CHEMBL4751890 | — | EC50 | = | 5.8 | nM | 8.24 |
| CHEMBL4753329 | — | EC50 | = | 7.6 | nM | 8.12 |
| CHEMBL4747855 | — | EC50 | = | 8.7 | nM | 8.06 |
| CHEMBL4778278 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL318457 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4756996 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4743486 | — | EC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4763935 | — | EC50 | = | 37.0 | nM | 7.43 |
| CHEMBL4779832 | — | EC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4747240 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4800066 | — | EC50 | = | 65.0 | nM | 7.19 |
| CHEMBL4800163 | — | EC50 | = | 96.0 | nM | 7.02 |
| CHEMBL4786636 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4757540 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4742812 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4745499 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4751112 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4746270 | — | EC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4791913 | — | EC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4763612 | — | EC50 | = | 330.0 | nM | 6.48 |
| CHEMBL4745008 | — | EC50 | = | 440.0 | nM | 6.36 |
| CHEMBL566315 | OBETICHOLIC ACID | EC50 | = | 710.0 | nM | 6.15 |
| CHEMBL4778910 | — | EC50 | = | 740.0 | nM | 6.13 |
| CHEMBL4753607 | — | EC50 | = | 770.0 | nM | 6.11 |
| CHEMBL4777088 | — | EC50 | = | 910.0 | nM | 6.04 |
| CHEMBL4743594 | — | EC50 | = | 1240.0 | nM | 5.91 |
| CHEMBL4760686 | — | EC50 | = | 2730.0 | nM | 5.56 |
| CHEMBL4778597 | — | EC50 | = | 16770.0 | nM | 4.78 |
| CHEMBL4750348 | — | EC50 | = | 44660.0 | nM | 4.35 |