Assay Detail
Binding
CHEMBL4138592
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of Fluormone ES2 Green from full-length untagged human ERalpha expressed in insect cells after 2 hrs by fluorescence polarization assay
13
Total Activities
13
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
Design and synthesis of novel selective estrogen receptor degradation inducers based on the diphenylheptane skeleton.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 7.51 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4176843 | — | — | 1 | 8.62 |
| CHEMBL4161714 | — | — | 1 | 8.31 |
| CHEMBL4168979 | — | — | 1 | 8.31 |
| CHEMBL489 | AFIMOXIFENE | 3.0 | 1 | 8.25 |
| CHEMBL2403356 | — | — | 1 | 8.14 |
| CHEMBL4165107 | — | — | 1 | 7.70 |
| CHEMBL4176665 | — | — | 1 | 7.40 |
| CHEMBL4163000 | — | — | 1 | 7.11 |
| CHEMBL4173705 | — | — | 1 | 7.11 |
| CHEMBL4165384 | — | — | 1 | 7.06 |
| CHEMBL4173298 | — | — | 1 | 6.78 |
| CHEMBL4103516 | — | — | 1 | 6.50 |
| CHEMBL4175592 | — | — | 1 | 6.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4176843 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4161714 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL4168979 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL489 | AFIMOXIFENE | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL2403356 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL4165107 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4176665 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4163000 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL4173705 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL4165384 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL4173298 | — | IC50 | = | 168.0 | nM | 6.78 |
| CHEMBL4103516 | — | IC50 | = | 313.0 | nM | 6.50 |
| CHEMBL4175592 | — | IC50 | = | 400.0 | nM | 6.40 |