Assay Detail
Binding
CHEMBL3877081
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of fluormone-labeled ES2 from recombinant full length human ERalpha ligand binding domain expressed in insect cells after 2 hrs by TR-FRET assay
4
Total Activities
4
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
Rational Design of a Boron-Modified Triphenylethylene (GLL398) as an Oral Selective Estrogen Receptor Downregulator.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 8.87 | 9.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | 4.0 | 1 | 9.39 |
| CHEMBL489 | AFIMOXIFENE | 3.0 | 1 | 9.28 |
| CHEMBL3885342 | — | — | 1 | 8.94 |
| CHEMBL3581633 | — | — | 1 | 7.86 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | IC50 | = | 0.41 | nM | 9.39 |
| CHEMBL489 | AFIMOXIFENE | IC50 | = | 0.53 | nM | 9.28 |
| CHEMBL3885342 | — | IC50 | = | 1.14 | nM | 8.94 |
| CHEMBL3581633 | — | IC50 | = | 13.8 | nM | 7.86 |