Assay Detail
Binding
CHEMBL988317
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Inhibition of aromatase activity in human JEG3 cells
25
Total Activities
25
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
Chiral aromatase and dual aromatase-steroid sulfatase inhibitors from the letrozole template: synthesis, absolute configuration, and in vitro activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 7.69 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL453736 | — | — | 1 | 9.22 |
| CHEMBL1444 | LETROZOLE | 4.0 | 1 | 9.05 |
| CHEMBL519436 | — | — | 1 | 8.86 |
| CHEMBL481091 | — | — | 1 | 8.74 |
| CHEMBL100749 | rac-VOROZOLE | — | 1 | 8.59 |
| CHEMBL518761 | — | — | 1 | 8.52 |
| CHEMBL479559 | — | — | 1 | 8.49 |
| CHEMBL481092 | — | — | 1 | 8.49 |
| CHEMBL500976 | — | — | 1 | 8.47 |
| CHEMBL479385 | — | — | 1 | 8.26 |
| CHEMBL519937 | — | — | 1 | 8.14 |
| CHEMBL480451 | — | — | 1 | 8.00 |
| CHEMBL479551 | — | — | 1 | 7.92 |
| CHEMBL479366 | — | — | 1 | 7.89 |
| CHEMBL480321 | — | — | 1 | 7.84 |
| CHEMBL479928 | — | — | 1 | 7.37 |
| CHEMBL224060 | VOROZOLE | 2.0 | 1 | 7.36 |
| CHEMBL479737 | — | — | 1 | 7.00 |
| CHEMBL480515 | — | — | 1 | 6.77 |
| CHEMBL480514 | — | — | 1 | 6.75 |
| CHEMBL480516 | — | — | 1 | 6.67 |
| CHEMBL286738 | IROSUSTAT | 2.0 | 1 | 6.52 |
| CHEMBL480718 | — | — | 1 | 6.17 |
| CHEMBL455832 | — | — | 1 | 5.61 |
| CHEMBL479942 | — | — | 1 | 5.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL453736 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL1444 | LETROZOLE | IC50 | = | 0.89 | nM | 9.05 |
| CHEMBL519436 | — | IC50 | = | 1.38 | nM | 8.86 |
| CHEMBL481091 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL100749 | rac-VOROZOLE | IC50 | = | 2.59 | nM | 8.59 |
| CHEMBL518761 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL479559 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL481092 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL500976 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL479385 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL519937 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL480451 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL479551 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL479366 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL480321 | — | IC50 | = | 14.3 | nM | 7.84 |
| CHEMBL479928 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL224060 | VOROZOLE | IC50 | = | 44.2 | nM | 7.36 |
| CHEMBL479737 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL480515 | — | IC50 | = | 169.0 | nM | 6.77 |
| CHEMBL480514 | — | IC50 | = | 178.0 | nM | 6.75 |
| CHEMBL480516 | — | IC50 | = | 215.0 | nM | 6.67 |
| CHEMBL286738 | IROSUSTAT | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL480718 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL455832 | — | IC50 | = | 2457.0 | nM | 5.61 |
| CHEMBL479942 | — | IC50 | = | 3044.0 | nM | 5.52 |