Assay Detail
Binding
CHEMBL867524
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Binding affinity to ERalpha
14
Total Activities
13
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Novel chromene-derived selective estrogen receptor modulators useful for alleviating hot flushes and vaginal dryness.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| RBA | 8 | - | - |
| IC50 | 6 | 8.49 | 9.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL207324 | — | — | 1 | 9.21 |
| CHEMBL81 | RALOXIFENE | 4.0 | 2 | 8.74 |
| CHEMBL691 | ETHINYL ESTRADIOL | 4.0 | 1 | 8.70 |
| CHEMBL208085 | — | — | 1 | 7.29 |
| CHEMBL210648 | — | — | 1 | - |
| CHEMBL381489 | — | — | 1 | - |
| CHEMBL207362 | — | — | 1 | - |
| CHEMBL209090 | — | — | 1 | - |
| CHEMBL209014 | — | — | 1 | - |
| CHEMBL206680 | — | — | 1 | - |
| CHEMBL379415 | — | — | 1 | - |
| CHEMBL426322 | — | — | 1 | - |
| CHEMBL210699 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL207324 | — | IC50 | = | 0.61 | nM | 9.21 |
| CHEMBL81 | RALOXIFENE | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL691 | ETHINYL ESTRADIOL | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL208085 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL210648 | — | RBA | = | 61.0 | % | - |
| CHEMBL381489 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL207362 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL81 | RALOXIFENE | RBA | = | 64.0 | % | - |
| CHEMBL209090 | — | RBA | = | 6.4 | % | - |
| CHEMBL209014 | — | RBA | = | 13.0 | % | - |
| CHEMBL206680 | — | RBA | = | 55.0 | % | - |
| CHEMBL379415 | — | RBA | = | 340.0 | % | - |
| CHEMBL426322 | — | RBA | = | 35.0 | % | - |
| CHEMBL210699 | — | RBA | = | 31.0 | % | - |