Assay Detail
Binding
CHEMBL5118295
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Inhibition of aromatase in human JEG-3 cells using Androst-4-ene-3,17-dione as substrate incubated for 1 hr and measured by BCA assay
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | JEG-3 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
4th generation nonsteroidal aromatase inhibitors: An iterative SAR-guided design, synthesis, and biological evaluation towards picomolar dual binding inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 9.06 | 11.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4639677 | — | — | 1 | 11.00 |
| CHEMBL4632445 | — | — | 1 | 11.00 |
| CHEMBL5203413 | — | — | 1 | 10.05 |
| CHEMBL197650 | — | — | 1 | 9.96 |
| CHEMBL198291 | — | — | 1 | 9.82 |
| CHEMBL5175340 | — | — | 1 | 9.41 |
| CHEMBL5184004 | — | — | 1 | 9.34 |
| CHEMBL382902 | — | — | 1 | 9.33 |
| CHEMBL5177269 | — | — | 1 | 9.29 |
| CHEMBL5174567 | — | — | 1 | 9.28 |
| CHEMBL202226 | — | — | 1 | 9.25 |
| CHEMBL1444 | LETROZOLE | 4.0 | 1 | 9.15 |
| CHEMBL5179009 | — | — | 1 | 9.14 |
| CHEMBL4634777 | — | — | 1 | 9.11 |
| CHEMBL446706 | — | — | 1 | 9.10 |
| CHEMBL5197552 | — | — | 1 | 8.99 |
| CHEMBL5186519 | — | — | 1 | 8.70 |
| CHEMBL5205534 | — | — | 1 | 8.56 |
| CHEMBL5173597 | — | — | 1 | 8.39 |
| CHEMBL5178202 | — | — | 1 | 8.25 |
| CHEMBL2179110 | — | — | 1 | 7.93 |
| CHEMBL5204674 | — | — | 1 | 7.68 |
| CHEMBL5175025 | — | — | 1 | 7.52 |
| CHEMBL1200374 | EXEMESTANE | 4.0 | 1 | 7.30 |
| CHEMBL5185187 | — | — | 1 | - |
| CHEMBL5177518 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4639677 | — | IC50 | = | 0.01 | nM | 11.00 |
| CHEMBL4632445 | — | IC50 | = | 0.01 | nM | 11.00 |
| CHEMBL5203413 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL197650 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL198291 | — | IC50 | = | 0.15 | nM | 9.82 |
| CHEMBL5175340 | — | IC50 | = | 0.39 | nM | 9.41 |
| CHEMBL5184004 | — | IC50 | = | 0.46 | nM | 9.34 |
| CHEMBL382902 | — | IC50 | = | 0.47 | nM | 9.33 |
| CHEMBL5177269 | — | IC50 | = | 0.51 | nM | 9.29 |
| CHEMBL5174567 | — | IC50 | = | 0.53 | nM | 9.28 |
| CHEMBL202226 | — | IC50 | = | 0.56 | nM | 9.25 |
| CHEMBL1444 | LETROZOLE | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5179009 | — | IC50 | = | 0.72 | nM | 9.14 |
| CHEMBL4634777 | — | IC50 | = | 0.77 | nM | 9.11 |
| CHEMBL446706 | — | IC50 | = | 0.79 | nM | 9.10 |
| CHEMBL5197552 | — | IC50 | = | 1.03 | nM | 8.99 |
| CHEMBL5186519 | — | IC50 | = | 2.01 | nM | 8.70 |
| CHEMBL5205534 | — | IC50 | = | 2.76 | nM | 8.56 |
| CHEMBL5173597 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL5178202 | — | IC50 | = | 5.67 | nM | 8.25 |
| CHEMBL2179110 | — | IC50 | = | 11.8 | nM | 7.93 |
| CHEMBL5204674 | — | IC50 | = | 21.05 | nM | 7.68 |
| CHEMBL5175025 | — | IC50 | = | 30.25 | nM | 7.52 |
| CHEMBL1200374 | EXEMESTANE | IC50 | = | 50.1 | nM | 7.30 |
| CHEMBL5185187 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5177518 | — | IC50 | > | 1000.0 | nM | - |