Assay Detail
Binding
CHEMBL5326431
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Binding affinity to ERalpha (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 | 6.86 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5433532 | — | — | 1 | 7.60 |
| CHEMBL5394879 | — | — | 1 | 7.46 |
| CHEMBL5398866 | — | — | 1 | 7.44 |
| CHEMBL5420394 | — | — | 1 | 7.42 |
| CHEMBL5433442 | — | — | 1 | 7.26 |
| CHEMBL5421409 | — | — | 1 | 7.26 |
| CHEMBL5419649 | — | — | 1 | 7.26 |
| CHEMBL5423258 | — | — | 1 | 7.21 |
| CHEMBL5411799 | — | — | 1 | 7.17 |
| CHEMBL5426251 | — | — | 1 | 7.16 |
| CHEMBL5404699 | — | — | 1 | 7.14 |
| CHEMBL5408038 | — | — | 1 | 7.14 |
| CHEMBL5400803 | — | — | 1 | 7.14 |
| CHEMBL4800654 | — | — | 1 | 7.12 |
| CHEMBL5404063 | — | — | 1 | 7.12 |
| CHEMBL5394007 | — | — | 1 | 7.11 |
| CHEMBL5394546 | — | — | 1 | 7.11 |
| CHEMBL5412790 | — | — | 1 | 7.08 |
| CHEMBL5427513 | — | — | 1 | 7.08 |
| CHEMBL5423781 | — | — | 1 | 7.04 |
| CHEMBL5403786 | — | — | 1 | 7.03 |
| CHEMBL5410004 | — | — | 1 | 7.00 |
| CHEMBL5436925 | — | — | 1 | 7.00 |
| CHEMBL5435743 | — | — | 1 | 7.00 |
| CHEMBL5400203 | — | — | 1 | 6.96 |
| CHEMBL5405944 | — | — | 1 | 6.92 |
| CHEMBL5401146 | — | — | 1 | 6.85 |
| CHEMBL5407335 | — | — | 1 | 6.80 |
| CHEMBL5398724 | — | — | 1 | 6.77 |
| CHEMBL5399056 | — | — | 1 | 6.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5433532 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL5394879 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL5398866 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL5420394 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL5433442 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL5421409 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL5419649 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL5423258 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL5411799 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL5426251 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL5404699 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL5408038 | — | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL5400803 | — | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL4800654 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL5404063 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL5394007 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL5394546 | — | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL5412790 | — | Ki | = | 84.0 | nM | 7.08 |
| CHEMBL5427513 | — | Ki | = | 84.0 | nM | 7.08 |
| CHEMBL5423781 | — | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL5403786 | — | Ki | = | 93.0 | nM | 7.03 |
| CHEMBL5410004 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL5436925 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL5435743 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL5400203 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL5405944 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL5401146 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL5407335 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL5398724 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL5399056 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL5413340 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL5426947 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL5426175 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL5414572 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL5428681 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL5414261 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL5423408 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL5414659 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL5418690 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL5417452 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL5403080 | — | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL5432102 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL5396802 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL5436713 | — | Ki | = | 520.0 | nM | 6.28 |
| CHEMBL5402392 | — | Ki | = | 670.0 | nM | 6.17 |
| CHEMBL5422315 | — | Ki | = | 780.0 | nM | 6.11 |
| CHEMBL5424929 | — | Ki | = | 970.0 | nM | 6.01 |
| CHEMBL5437007 | — | Ki | = | 1560.0 | nM | 5.81 |