Assay Detail
Binding
CHEMBL4308796
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 measured after 20 mins by TR-FRET Lanthascreen assay
7
Total Activities
7
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
Building Bridges in a Series of Estrogen Receptor Degraders: An Application of Metathesis in Medicinal Chemistry.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 9.07 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4447306 | — | — | 1 | 9.40 |
| CHEMBL4587197 | — | — | 1 | 9.20 |
| CHEMBL3623004 | AZD-9496 | 1.0 | 1 | 9.10 |
| CHEMBL4452972 | — | — | 1 | 9.10 |
| CHEMBL4528514 | — | — | 1 | 9.00 |
| CHEMBL4591926 | — | — | 1 | 9.00 |
| CHEMBL4516412 | — | — | 1 | 8.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4447306 | — | IC50 | = | 0.3981 | nM | 9.40 |
| CHEMBL4587197 | — | IC50 | = | 0.631 | nM | 9.20 |
| CHEMBL3623004 | AZD-9496 | IC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL4452972 | — | IC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL4528514 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4591926 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4516412 | — | IC50 | = | 1.995 | nM | 8.70 |