Assay Detail
Binding
CHEMBL4676155
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of fluormone ES2 green reagent from human GST-tagged ERalpha LBD (282 to 595 residues) expressed in baculovirus infected insect cells incubated for 1 hrs by TR-FRET Lanthascreen assay
36
Total Activities
36
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 AZD9833, a Potent and Orally Bioavailable Selective Estrogen Receptor Degrader and Antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 8.39 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4759688 | — | — | 1 | 9.10 |
| CHEMBL4756497 | — | — | 1 | 9.00 |
| CHEMBL4757886 | — | — | 1 | 8.90 |
| CHEMBL4782483 | — | — | 1 | 8.90 |
| CHEMBL4779715 | — | — | 1 | 8.70 |
| CHEMBL4758424 | — | — | 1 | 8.70 |
| CHEMBL4756831 | — | — | 1 | 8.70 |
| CHEMBL4751770 | — | — | 1 | 8.70 |
| CHEMBL4763079 | — | — | 1 | 8.60 |
| CHEMBL4650365 | CAMIZESTRANT | 3.0 | 1 | 8.60 |
| CHEMBL4780809 | — | — | 1 | 8.60 |
| CHEMBL4743256 | — | — | 1 | 8.60 |
| CHEMBL4795387 | — | — | 1 | 8.50 |
| CHEMBL4753585 | — | — | 1 | 8.50 |
| CHEMBL4785486 | — | — | 1 | 8.50 |
| CHEMBL4797729 | — | — | 1 | 8.50 |
| CHEMBL4752903 | — | — | 1 | 8.50 |
| CHEMBL4777960 | — | — | 1 | 8.40 |
| CHEMBL4749269 | — | — | 1 | 8.40 |
| CHEMBL4754747 | — | — | 1 | 8.40 |
| CHEMBL4792482 | — | — | 1 | 8.30 |
| CHEMBL4744329 | — | — | 1 | 8.30 |
| CHEMBL4759597 | — | — | 1 | 8.30 |
| CHEMBL4790076 | — | — | 1 | 8.20 |
| CHEMBL4759607 | — | — | 1 | 8.20 |
| CHEMBL4751971 | — | — | 1 | 8.20 |
| CHEMBL4742862 | — | — | 1 | 8.10 |
| CHEMBL4750007 | — | — | 1 | 8.10 |
| CHEMBL4792890 | — | — | 1 | 8.10 |
| CHEMBL4780994 | — | — | 1 | 8.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4759688 | — | IC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL4756497 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4782483 | — | IC50 | = | 1.259 | nM | 8.90 |
| CHEMBL4757886 | — | IC50 | = | 1.259 | nM | 8.90 |
| CHEMBL4779715 | — | IC50 | = | 1.995 | nM | 8.70 |
| CHEMBL4758424 | — | IC50 | = | 1.995 | nM | 8.70 |
| CHEMBL4756831 | — | IC50 | = | 1.995 | nM | 8.70 |
| CHEMBL4751770 | — | IC50 | = | 1.995 | nM | 8.70 |
| CHEMBL4780809 | — | IC50 | = | 2.512 | nM | 8.60 |
| CHEMBL4743256 | — | IC50 | = | 2.512 | nM | 8.60 |
| CHEMBL4650365 | CAMIZESTRANT | IC50 | = | 2.512 | nM | 8.60 |
| CHEMBL4763079 | — | IC50 | = | 2.512 | nM | 8.60 |
| CHEMBL4752903 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL4797729 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL4785486 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL4795387 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL4753585 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL4754747 | — | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL4749269 | — | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL4777960 | — | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL4792482 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL4744329 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL4759597 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL4790076 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL4759607 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL4751971 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL4750007 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL4756084 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL4780994 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL4792890 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL4742862 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL4779640 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4752435 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4762458 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4787725 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4797178 | — | IC50 | = | 39.81 | nM | 7.40 |