Assay Detail
Binding
CHEMBL5326432
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Binding affinity to ERbeta (unknown origin) assessed as inhibition constant
48
Total Activities
48
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
Structure-guided identification of novel dual-targeting estrogen receptor α degraders with aromatase inhibitory activity for the treatment of endocrine-resistant breast cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 48 | 5.61 | 7.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5418690 | — | — | 1 | 7.64 |
| CHEMBL5432102 | — | — | 1 | 7.05 |
| CHEMBL5428681 | — | — | 1 | 6.41 |
| CHEMBL5398866 | — | — | 1 | 6.31 |
| CHEMBL5414572 | — | — | 1 | 6.30 |
| CHEMBL5394879 | — | — | 1 | 6.23 |
| CHEMBL5435743 | — | — | 1 | 6.12 |
| CHEMBL5400803 | — | — | 1 | 6.07 |
| CHEMBL5405944 | — | — | 1 | 6.05 |
| CHEMBL5423408 | — | — | 1 | 6.02 |
| CHEMBL5399056 | — | — | 1 | 5.92 |
| CHEMBL5396802 | — | — | 1 | 5.89 |
| CHEMBL5414659 | — | — | 1 | 5.88 |
| CHEMBL4800654 | — | — | 1 | 5.87 |
| CHEMBL5424929 | — | — | 1 | 5.85 |
| CHEMBL5427513 | — | — | 1 | 5.84 |
| CHEMBL5401146 | — | — | 1 | 5.68 |
| CHEMBL5423258 | — | — | 1 | 5.68 |
| CHEMBL5426175 | — | — | 1 | 5.65 |
| CHEMBL5403786 | — | — | 1 | 5.64 |
| CHEMBL5426251 | — | — | 1 | 5.59 |
| CHEMBL5404063 | — | — | 1 | 5.54 |
| CHEMBL5398724 | — | — | 1 | 5.54 |
| CHEMBL5404699 | — | — | 1 | 5.45 |
| CHEMBL5423781 | — | — | 1 | 5.45 |
| CHEMBL5394007 | — | — | 1 | 5.43 |
| CHEMBL5436713 | — | — | 1 | 5.36 |
| CHEMBL5394546 | — | — | 1 | 5.33 |
| CHEMBL5421409 | — | — | 1 | 5.28 |
| CHEMBL5411799 | — | — | 1 | 5.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5418690 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL5432102 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL5428681 | — | Ki | = | 390.0 | nM | 6.41 |
| CHEMBL5398866 | — | Ki | = | 490.0 | nM | 6.31 |
| CHEMBL5414572 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL5394879 | — | Ki | = | 590.0 | nM | 6.23 |
| CHEMBL5435743 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL5400803 | — | Ki | = | 850.0 | nM | 6.07 |
| CHEMBL5405944 | — | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL5423408 | — | Ki | = | 960.0 | nM | 6.02 |
| CHEMBL5399056 | — | Ki | = | 1210.0 | nM | 5.92 |
| CHEMBL5396802 | — | Ki | = | 1280.0 | nM | 5.89 |
| CHEMBL5414659 | — | Ki | = | 1330.0 | nM | 5.88 |
| CHEMBL4800654 | — | Ki | = | 1360.0 | nM | 5.87 |
| CHEMBL5424929 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL5427513 | — | Ki | = | 1460.0 | nM | 5.84 |
| CHEMBL5401146 | — | Ki | = | 2070.0 | nM | 5.68 |
| CHEMBL5423258 | — | Ki | = | 2070.0 | nM | 5.68 |
| CHEMBL5426175 | — | Ki | = | 2250.0 | nM | 5.65 |
| CHEMBL5403786 | — | Ki | = | 2310.0 | nM | 5.64 |
| CHEMBL5426251 | — | Ki | = | 2540.0 | nM | 5.59 |
| CHEMBL5404063 | — | Ki | = | 2910.0 | nM | 5.54 |
| CHEMBL5398724 | — | Ki | = | 2910.0 | nM | 5.54 |
| CHEMBL5423781 | — | Ki | = | 3570.0 | nM | 5.45 |
| CHEMBL5404699 | — | Ki | = | 3570.0 | nM | 5.45 |
| CHEMBL5394007 | — | Ki | = | 3740.0 | nM | 5.43 |
| CHEMBL5436713 | — | Ki | = | 4370.0 | nM | 5.36 |
| CHEMBL5394546 | — | Ki | = | 4630.0 | nM | 5.33 |
| CHEMBL5421409 | — | Ki | = | 5240.0 | nM | 5.28 |
| CHEMBL5411799 | — | Ki | = | 6050.0 | nM | 5.22 |
| CHEMBL5412790 | — | Ki | = | 6050.0 | nM | 5.22 |
| CHEMBL5433442 | — | Ki | = | 6050.0 | nM | 5.22 |
| CHEMBL5410004 | — | Ki | = | 6550.0 | nM | 5.18 |
| CHEMBL5400203 | — | Ki | = | 7860.0 | nM | 5.11 |
| CHEMBL5419649 | — | Ki | = | 8730.0 | nM | 5.06 |
| CHEMBL5408038 | — | Ki | = | 9830.0 | nM | 5.01 |
| CHEMBL5403080 | — | Ki | = | 19650.0 | nM | 4.71 |
| CHEMBL5426947 | — | Ki | = | 19650.0 | nM | 4.71 |
| CHEMBL5413340 | — | Ki | = | 19650.0 | nM | 4.71 |
| CHEMBL5437007 | — | Ki | = | 26200.0 | nM | 4.58 |
| CHEMBL5422315 | — | Ki | = | 39300.0 | nM | 4.41 |
| CHEMBL5414261 | — | Ki | > | 78000.0 | nM | - |
| CHEMBL5433532 | — | Ki | > | 78000.0 | nM | - |
| CHEMBL5407335 | — | Ki | > | 78000.0 | nM | - |
| CHEMBL5420394 | — | Ki | > | 78000.0 | nM | - |
| CHEMBL5436925 | — | Ki | > | 78000.0 | nM | - |
| CHEMBL5417452 | — | Ki | > | 78000.0 | nM | - |
| CHEMBL5402392 | — | Ki | > | 78000.0 | nM | - |