Assay Detail
Binding
CHEMBL3825918
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Agonist activity at C-terminal Gal4-tagged human FXR (187 to 472 residues) expressed in HEK-293 cells co-expressing pFRluc by mammalian one hybrid assay
28
Total Activities
28
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
Novel substituted isoxazole FXR agonists with cyclopropyl, hydroxycyclobutyl and hydroxyazetidinyl linkers: Understanding and improving key determinants of pharmacological properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 28 | 7.21 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3822755 | — | — | 1 | 8.40 |
| CHEMBL3822798 | — | — | 1 | 8.22 |
| CHEMBL3824163 | — | — | 1 | 7.85 |
| CHEMBL3824337 | — | — | 1 | 7.85 |
| CHEMBL3822859 | — | — | 1 | 7.82 |
| CHEMBL3822901 | — | — | 1 | 7.60 |
| CHEMBL3824162 | — | — | 1 | 7.54 |
| CHEMBL3822597 | — | — | 1 | 7.47 |
| CHEMBL318457 | — | — | 1 | 7.46 |
| CHEMBL3823213 | — | — | 1 | 7.36 |
| CHEMBL3823077 | — | — | 1 | 7.36 |
| CHEMBL3822464 | — | — | 1 | 7.33 |
| CHEMBL3822477 | — | — | 1 | 7.30 |
| CHEMBL3823070 | — | — | 1 | 7.24 |
| CHEMBL3823938 | — | — | 1 | 7.20 |
| CHEMBL3822803 | — | — | 1 | 7.12 |
| CHEMBL3823564 | — | — | 1 | 7.07 |
| CHEMBL3824077 | — | — | 1 | 7.05 |
| CHEMBL3823491 | — | — | 1 | 7.04 |
| CHEMBL3823637 | — | — | 1 | 6.99 |
| CHEMBL3824207 | — | — | 1 | 6.96 |
| CHEMBL3823312 | — | — | 1 | 6.96 |
| CHEMBL3822773 | PX-102 | 2.0 | 1 | 6.73 |
| CHEMBL3822935 | — | — | 1 | 6.68 |
| CHEMBL3823688 | — | — | 1 | 6.66 |
| CHEMBL3823467 | — | — | 1 | 6.42 |
| CHEMBL3823517 | — | — | 1 | 6.26 |
| CHEMBL3822953 | — | — | 1 | 5.86 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3822755 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3822798 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3824163 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3824337 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3822859 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3822901 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3824162 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3822597 | — | EC50 | = | 34.0 | nM | 7.47 |
| CHEMBL318457 | — | EC50 | = | 35.0 | nM | 7.46 |
| CHEMBL3823213 | — | EC50 | = | 44.0 | nM | 7.36 |
| CHEMBL3823077 | — | EC50 | = | 44.0 | nM | 7.36 |
| CHEMBL3822464 | — | EC50 | = | 47.0 | nM | 7.33 |
| CHEMBL3822477 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3823070 | — | EC50 | = | 57.0 | nM | 7.24 |
| CHEMBL3823938 | — | EC50 | = | 63.0 | nM | 7.20 |
| CHEMBL3822803 | — | EC50 | = | 76.0 | nM | 7.12 |
| CHEMBL3823564 | — | EC50 | = | 86.0 | nM | 7.07 |
| CHEMBL3824077 | — | EC50 | = | 90.0 | nM | 7.05 |
| CHEMBL3823491 | — | EC50 | = | 92.0 | nM | 7.04 |
| CHEMBL3823637 | — | EC50 | = | 102.0 | nM | 6.99 |
| CHEMBL3824207 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3823312 | — | EC50 | = | 111.0 | nM | 6.96 |
| CHEMBL3822773 | PX-102 | EC50 | = | 186.0 | nM | 6.73 |
| CHEMBL3822935 | — | EC50 | = | 209.0 | nM | 6.68 |
| CHEMBL3823688 | — | EC50 | = | 220.0 | nM | 6.66 |
| CHEMBL3823467 | — | EC50 | = | 377.0 | nM | 6.42 |
| CHEMBL3823517 | — | EC50 | = | 552.0 | nM | 6.26 |
| CHEMBL3822953 | — | EC50 | = | 1372.0 | nM | 5.86 |