Assay Detail
Binding
CHEMBL3385304
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inverse agonist activity at human recombinant N-terminally 6xHis-tagged RORgamma ligand binding domain (unknown origin) expressed in Escherichia coli incubated for 1 hr by FRET assay
4
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORβ and RORγt.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 7.37 | 7.90 |
| pIC50 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3105674 | — | — | 1 | 7.90 |
| CHEMBL3105681 | — | — | 1 | 7.70 |
| CHEMBL62136 | T091317 | — | 1 | 6.50 |
| CHEMBL38 | TRETINOIN | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3105674 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL3105681 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL62136 | T091317 | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL38 | TRETINOIN | pIC50 | - | — | - |