Assay Detail
Binding
CHEMBL4689737
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at recombinant GST-tagged FXR LBD (unknown origin) assessed as inhibition of GW4064-induced Fluorecein-SRC2-2 coactivator peptide recruitment by LanthaScreen TR-FRET co-regulator assay
8
Total Activities
8
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 of Orally Active and Nonsteroidal Farnesoid X Receptor (FXR) Antagonist with Propensity for Accumulation and Responsiveness in Ileum.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.40 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4552760 | — | — | 1 | 8.15 |
| CHEMBL4797745 | — | — | 1 | 8.11 |
| CHEMBL4783205 | — | — | 1 | 7.48 |
| CHEMBL4453417 | — | — | 1 | 7.46 |
| CHEMBL4785930 | — | — | 1 | 7.20 |
| CHEMBL4783777 | — | — | 1 | 7.19 |
| CHEMBL4778665 | — | — | 1 | 6.85 |
| CHEMBL4749439 | — | — | 1 | 6.74 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4552760 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4797745 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL4783205 | — | IC50 | = | 32.9 | nM | 7.48 |
| CHEMBL4453417 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4785930 | — | IC50 | = | 62.6 | nM | 7.20 |
| CHEMBL4783777 | — | IC50 | = | 64.5 | nM | 7.19 |
| CHEMBL4778665 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4749439 | — | IC50 | = | 183.1 | nM | 6.74 |