Assay Detail
Binding
CHEMBL4880802
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Estrogen ERalpha at 10 µM in the Eurofins-Panlabs radioligand binding assay (Eurofins_assay_226010)
25
Total Activities
23
Compounds Tested
3
Activity Types
14
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Profiling data from Eurofins-Panlabs
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Inhibition | 23 | - | - |
| IC50 | 1 | 5.60 | 5.60 |
| Ki | 1 | 6.14 | 6.14 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Assay protocol publication | Assay protocol publication | - | — | PMID: 8512933 |
| Detection method | Detection method | - | — | Radioligand Binding |
| Incubation temperature | Incubation temperature | - | — | 25 °C |
| Incubation time | Incubation time | - | — | 2 h |
| Ligand | Ligand | - | — | [3H] Estradiol |
| Ligand Bmax | Ligand Bmax | 1400.0 | pM/ mg protein | — |
| Ligand concentration | Ligand concentration | 0.5 | nM | — |
| Ligand Kd | Ligand Kd | 0.2 | nM | — |
| Ligand specific binding | Ligand specific binding | 85.0 | % | — |
| Non-specific ligand with concentration | Non-specific ligand with concentration | - | — | 1 µM Diethylstilbestrol |
| Reference compound | Reference compound | - | — | Diethylstilbestrol |
| reference compound IC50 | reference compound IC50 | 0.77 | nM | — |
| reference compound Ki | reference compound Ki | 0.22 | nM | — |
| Source of protein | Source of protein | - | — | Human recombinant insect Sf9 cells |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4514203 | BAY-390 | — | 3 | 6.14 |
| CHEMBL4551635 | BAY-069 | — | 1 | - |
| CHEMBL4585243 | BAY-7598 | — | 1 | - |
| CHEMBL4521594 | BAY-1797 | — | 1 | - |
| CHEMBL4537788 | BAY-784 | — | 1 | - |
| CHEMBL4630644 | BAY-386 | — | 1 | - |
| CHEMBL4098877 | MLi-2 | — | 1 | - |
| CHEMBL1800685 | PPTN | — | 1 | - |
| CHEMBL2204538 | THPP-1 | — | 1 | - |
| CHEMBL3582478 | MSD-CYP11B2 | — | 1 | - |
| CHEMBL4088216 | TP-030-1 | — | 1 | - |
| CHEMBL4549667 | TP-030-2 | — | 1 | - |
| CHEMBL4593677 | BAY-474 | — | 1 | - |
| CHEMBL4643852 | BAY-6672 | — | 1 | - |
| CHEMBL1800285 | MSD-M1PAM | — | 1 | - |
| CHEMBL4802045 | BAY-091 | — | 1 | - |
| CHEMBL2048623 | — | — | 1 | - |
| CHEMBL5079207 | — | — | 1 | - |
| CHEMBL5084426 | — | — | 1 | - |
| CHEMBL5410211 | — | — | 1 | - |
| CHEMBL4594444 | PECAVAPTAN | 2.0 | 1 | - |
| CHEMBL5465173 | — | — | 1 | - |
| CHEMBL4097778 | TP-030n | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4514203 | BAY-390 | Ki | = | 720.0 | nM | 6.14 |
| CHEMBL4514203 | BAY-390 | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4585243 | BAY-7598 | Inhibition | = | 2.0 | % | - |
| CHEMBL4521594 | BAY-1797 | Inhibition | = | 5.0 | % | - |
| CHEMBL4537788 | BAY-784 | Inhibition | = | 21.0 | % | - |
| CHEMBL4630644 | BAY-386 | Inhibition | = | -1.0 | % | - |
| CHEMBL4098877 | MLi-2 | Inhibition | = | 8.0 | % | - |
| CHEMBL1800685 | PPTN | Inhibition | = | 12.0 | % | - |
| CHEMBL2204538 | THPP-1 | Inhibition | = | -1.0 | % | - |
| CHEMBL3582478 | MSD-CYP11B2 | Inhibition | = | 1.0 | % | - |
| CHEMBL4088216 | TP-030-1 | Inhibition | = | 36.0 | % | - |
| CHEMBL4549667 | TP-030-2 | Inhibition | = | 10.0 | % | - |
| CHEMBL4097778 | TP-030n | Inhibition | = | 5.0 | % | - |
| CHEMBL4593677 | BAY-474 | Inhibition | = | 2.0 | % | - |
| CHEMBL4643852 | BAY-6672 | Inhibition | = | 1.0 | % | - |
| CHEMBL4514203 | BAY-390 | Inhibition | = | 75.0 | % | - |
| CHEMBL1800285 | MSD-M1PAM | Inhibition | = | -1.0 | % | - |
| CHEMBL4802045 | BAY-091 | Inhibition | = | 10.0 | % | - |
| CHEMBL2048623 | — | Inhibition | = | 3.0 | % | - |
| CHEMBL5079207 | — | Inhibition | = | 7.0 | % | - |
| CHEMBL5084426 | — | Inhibition | = | 10.0 | % | - |
| CHEMBL5410211 | — | Inhibition | = | 6.2 | % | - |
| CHEMBL4594444 | PECAVAPTAN | Inhibition | = | 8.0 | % | - |
| CHEMBL5465173 | — | Inhibition | = | 4.0 | % | - |
| CHEMBL4551635 | BAY-069 | Inhibition | = | 6.0 | % | - |