Assay Detail
Binding
CHEMBL4731980
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of fluorescent labelled fluormone ES2 from human recombinant GST tagged ER alpha LBD ( 282 to 595 residues) expressed in baculovirus infected insect cells incubate for 20 mins measured after 1 hr by TR-FRET Lanthascreen assay
12
Total Activities
12
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
Addition of Fluorine and a Late-Stage Functionalization (LSF) of the Oral SERD AZD9833.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 8.38 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4789498 | — | — | 1 | 9.30 |
| CHEMBL4777139 | — | — | 1 | 9.00 |
| CHEMBL4754652 | — | — | 1 | 8.90 |
| CHEMBL4749445 | — | — | 1 | 8.80 |
| CHEMBL4789223 | — | — | 1 | 8.70 |
| CHEMBL4799234 | — | — | 1 | 8.70 |
| CHEMBL4650365 | CAMIZESTRANT | 3.0 | 1 | 8.60 |
| CHEMBL4780699 | — | — | 1 | 8.60 |
| CHEMBL4754747 | — | — | 1 | 8.40 |
| CHEMBL4745941 | — | — | 1 | 7.80 |
| CHEMBL4746365 | — | — | 1 | 7.40 |
| CHEMBL4757584 | — | — | 1 | 6.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4789498 | — | IC50 | = | 0.5012 | nM | 9.30 |
| CHEMBL4777139 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4754652 | — | IC50 | = | 1.259 | nM | 8.90 |
| CHEMBL4749445 | — | IC50 | = | 1.585 | nM | 8.80 |
| CHEMBL4789223 | — | IC50 | = | 1.995 | nM | 8.70 |
| CHEMBL4799234 | — | IC50 | = | 1.995 | nM | 8.70 |
| CHEMBL4650365 | CAMIZESTRANT | IC50 | = | 2.512 | nM | 8.60 |
| CHEMBL4780699 | — | IC50 | = | 2.512 | nM | 8.60 |
| CHEMBL4754747 | — | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL4745941 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL4746365 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL4757584 | — | IC50 | = | 501.19 | nM | 6.30 |