Assay Detail
Functional
CHEMBL984568
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at estrogen receptor alpha expressed in human HEC1 cells assessed as inhibition of 1 nM estradiol-induced transcriptional activity after 24 hrs by luciferase reporter gene assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | HEC-1 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Gag polyprotein (CHEMBL5824) ↗| Type | SINGLE PROTEIN |
| Organism | Avian erythroblastosis virus (strain ES4) |
Publication
Synthesis and biological evaluation of guanylhydrazone coactivator binding inhibitors for the estrogen receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 5.55 | 6.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL458496 | — | — | 1 | 6.05 |
| CHEMBL456392 | — | — | 1 | 5.92 |
| CHEMBL456598 | — | — | 1 | 5.89 |
| CHEMBL448651 | — | — | 1 | 5.85 |
| CHEMBL460174 | — | — | 1 | 5.85 |
| CHEMBL456393 | — | — | 1 | 5.82 |
| CHEMBL456106 | — | — | 1 | 5.70 |
| CHEMBL456600 | — | — | 1 | 5.51 |
| CHEMBL456594 | — | — | 1 | 5.48 |
| CHEMBL512206 | — | — | 1 | 5.46 |
| CHEMBL456179 | — | — | 1 | 5.41 |
| CHEMBL33663 | — | — | 1 | 5.12 |
| CHEMBL285853 | — | — | 1 | 5.12 |
| CHEMBL456599 | — | — | 1 | 5.11 |
| CHEMBL458495 | — | — | 1 | 4.92 |
| CHEMBL459968 | — | — | 1 | - |
| CHEMBL508968 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL458496 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL456392 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL456598 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL448651 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL460174 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL456393 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL456106 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL456600 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL456594 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL512206 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL456179 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL33663 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL285853 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL456599 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL458495 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL459968 | — | IC50 | >= | 50000.0 | nM | - |
| CHEMBL508968 | — | IC50 | >= | 50000.0 | nM | - |