Assay Detail
Binding
CHEMBL4362640
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Inhibition of recombinant human aromatase expressed in baculovirus infected insect cells using O-benzyl fluorescein benzyl ester as substrate in presence of NADPH generating system by fluorescence based analysis
38
Total Activities
21
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis, molecular docking, and QSAR study of bis-sulfonamide derivatives as potential aromatase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 6.27 | 8.72 |
| pIC50 | 17 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1444 | LETROZOLE | 4.0 | 1 | 8.72 |
| CHEMBL4460718 | — | — | 2 | 7.30 |
| CHEMBL4590541 | — | — | 2 | 7.22 |
| CHEMBL4449929 | — | — | 2 | 6.89 |
| CHEMBL4444996 | — | — | 2 | 6.80 |
| CHEMBL4462178 | — | — | 2 | 6.68 |
| CHEMBL4567479 | — | — | 2 | 6.55 |
| CHEMBL4570681 | — | — | 2 | 6.43 |
| CHEMBL4556427 | — | — | 2 | 6.37 |
| CHEMBL4543747 | — | — | 2 | 6.28 |
| CHEMBL4527809 | — | — | 2 | 6.18 |
| CHEMBL4446561 | — | — | 2 | 6.11 |
| CHEMBL2299368 | — | — | 1 | 6.10 |
| CHEMBL4536389 | — | — | 2 | 5.66 |
| CHEMBL4439561 | — | — | 2 | 5.56 |
| CHEMBL4436270 | — | — | 2 | 5.50 |
| CHEMBL4448018 | — | — | 2 | 5.48 |
| CHEMBL4555477 | — | — | 2 | 5.43 |
| CHEMBL2299369 | — | — | 1 | 5.26 |
| CHEMBL4531367 | — | — | 2 | 4.94 |
| CHEMBL4585518 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1444 | LETROZOLE | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4460718 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4590541 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4449929 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4444996 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4462178 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4567479 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4570681 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4556427 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL4543747 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL4527809 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL4446561 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL2299368 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL4536389 | — | IC50 | = | 2190.0 | nM | 5.66 |
| CHEMBL4439561 | — | IC50 | = | 2750.0 | nM | 5.56 |
| CHEMBL4436270 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL4448018 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL4555477 | — | IC50 | = | 3670.0 | nM | 5.43 |
| CHEMBL2299369 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL4531367 | — | IC50 | = | 11600.0 | nM | 4.94 |
| CHEMBL4436270 | — | pIC50 | = | -0.505 | — | - |
| CHEMBL4462178 | — | pIC50 | = | 0.678 | — | - |
| CHEMBL4531367 | — | pIC50 | = | -1.064 | — | - |
| CHEMBL4556427 | — | pIC50 | = | 0.367 | — | - |
| CHEMBL4536389 | — | pIC50 | = | -0.34 | — | - |
| CHEMBL4460718 | — | pIC50 | = | 1.301 | — | - |
| CHEMBL4590541 | — | pIC50 | = | 1.222 | — | - |
| CHEMBL4444996 | — | pIC50 | = | 0.796 | — | - |
| CHEMBL4567479 | — | pIC50 | = | 0.553 | — | - |
| CHEMBL4449929 | — | pIC50 | = | 0.886 | — | - |
| CHEMBL4570681 | — | pIC50 | = | 0.432 | — | - |
| CHEMBL4555477 | — | pIC50 | = | -0.565 | — | - |
| CHEMBL4439561 | — | pIC50 | = | -0.439 | — | - |
| CHEMBL4448018 | — | pIC50 | = | -0.519 | — | - |
| CHEMBL4527809 | — | pIC50 | = | 0.18 | — | - |
| CHEMBL4543747 | — | pIC50 | = | 0.276 | — | - |
| CHEMBL4446561 | — | pIC50 | = | 0.108 | — | - |
| CHEMBL4585518 | — | IC50 | > | 12500.0 | nM | - |