Assay Detail
Binding
CHEMBL1067556
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Inhibition of aromatase in human JEG3 cells by scintillation spectrometry
40
Total Activities
40
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
Highly potent first examples of dual aromatase-steroid sulfatase inhibitors based on a biphenyl template.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 40 | 8.08 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL597416 | — | — | 1 | 10.00 |
| CHEMBL597808 | — | — | 1 | 9.82 |
| CHEMBL597606 | — | — | 1 | 9.70 |
| CHEMBL592852 | — | — | 1 | 9.70 |
| CHEMBL589974 | — | — | 1 | 9.66 |
| CHEMBL599864 | — | — | 1 | 9.66 |
| CHEMBL604716 | — | — | 1 | 9.52 |
| CHEMBL599239 | — | — | 1 | 9.46 |
| CHEMBL598224 | — | — | 1 | 9.30 |
| CHEMBL596779 | — | — | 1 | 9.30 |
| CHEMBL592131 | — | — | 1 | 9.30 |
| CHEMBL598223 | — | — | 1 | 9.10 |
| CHEMBL1444 | LETROZOLE | 4.0 | 1 | 9.05 |
| CHEMBL1399 | ANASTROZOLE | 4.0 | 1 | 8.82 |
| CHEMBL589738 | — | — | 1 | 8.77 |
| CHEMBL598212 | — | — | 1 | 8.72 |
| CHEMBL598199 | — | — | 1 | 8.70 |
| CHEMBL599238 | — | — | 1 | 8.62 |
| CHEMBL608153 | — | — | 1 | 8.34 |
| CHEMBL605418 | — | — | 1 | 8.22 |
| CHEMBL589247 | — | — | 1 | 7.84 |
| CHEMBL597403 | — | — | 1 | 7.76 |
| CHEMBL599456 | — | — | 1 | 7.72 |
| CHEMBL598846 | — | — | 1 | 7.62 |
| CHEMBL599455 | — | — | 1 | 7.53 |
| CHEMBL609333 | — | — | 1 | 7.28 |
| CHEMBL598009 | — | — | 1 | 7.16 |
| CHEMBL609332 | — | — | 1 | 7.13 |
| CHEMBL598628 | — | — | 1 | 7.10 |
| CHEMBL601840 | — | — | 1 | 6.95 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL597416 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL597808 | — | IC50 | = | 0.15 | nM | 9.82 |
| CHEMBL592852 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL597606 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL589974 | — | IC50 | = | 0.22 | nM | 9.66 |
| CHEMBL599864 | — | IC50 | = | 0.22 | nM | 9.66 |
| CHEMBL604716 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL599239 | — | IC50 | = | 0.35 | nM | 9.46 |
| CHEMBL598224 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL596779 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL592131 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL598223 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL1444 | LETROZOLE | IC50 | = | 0.89 | nM | 9.05 |
| CHEMBL1399 | ANASTROZOLE | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL589738 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL598212 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL598199 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL599238 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL608153 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL605418 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL589247 | — | IC50 | = | 14.4 | nM | 7.84 |
| CHEMBL597403 | — | IC50 | = | 17.5 | nM | 7.76 |
| CHEMBL599456 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL598846 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL599455 | — | IC50 | = | 29.3 | nM | 7.53 |
| CHEMBL609333 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL598009 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL609332 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL598628 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL601840 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL599442 | — | IC50 | = | 146.0 | nM | 6.84 |
| CHEMBL592376 | — | IC50 | = | 176.0 | nM | 6.75 |
| CHEMBL598847 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL598629 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL598627 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL609618 | — | IC50 | = | 284.0 | nM | 6.55 |
| CHEMBL286738 | IROSUSTAT | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL598020 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL598211 | — | IC50 | = | 571.0 | nM | 6.24 |
| CHEMBL607855 | — | IC50 | = | 920.0 | nM | 6.04 |