Assay Detail
Binding
CHEMBL2185145
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human placental aromatase using [3H]-1beta-androstenedione as substrate after 16 hrs by [3H]-water method
22
Total Activities
11
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
Novel aromatase inhibitors by structure-guided design.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Inhibition | 11 | - | - |
| IC50 | 11 | 6.79 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1444 | LETROZOLE | 4.0 | 2 | 8.00 |
| CHEMBL2179110 | — | — | 2 | 7.93 |
| CHEMBL2179114 | — | — | 2 | 7.70 |
| CHEMBL132530 | FORMESTANE | 2.0 | 2 | 7.31 |
| CHEMBL1200374 | EXEMESTANE | 4.0 | 2 | 7.30 |
| CHEMBL2179111 | — | — | 2 | 7.08 |
| CHEMBL2179109 | — | — | 2 | 6.95 |
| CHEMBL2179112 | — | — | 2 | 6.74 |
| CHEMBL2179113 | — | — | 2 | 5.66 |
| CHEMBL2179107 | — | — | 2 | 5.28 |
| CHEMBL2179108 | — | — | 2 | 4.74 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1444 | LETROZOLE | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL2179110 | — | IC50 | = | 11.8 | nM | 7.93 |
| CHEMBL2179114 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL132530 | FORMESTANE | IC50 | = | 48.6 | nM | 7.31 |
| CHEMBL1200374 | EXEMESTANE | IC50 | = | 50.1 | nM | 7.30 |
| CHEMBL2179111 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL2179109 | — | IC50 | = | 112.3 | nM | 6.95 |
| CHEMBL2179112 | — | IC50 | = | 181.1 | nM | 6.74 |
| CHEMBL2179113 | — | IC50 | = | 2180.0 | nM | 5.66 |
| CHEMBL2179107 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL2179108 | — | IC50 | = | 18100.0 | nM | 4.74 |
| CHEMBL1444 | LETROZOLE | Inhibition | - | % | - | |
| CHEMBL132530 | FORMESTANE | Inhibition | - | % | - | |
| CHEMBL1200374 | EXEMESTANE | Inhibition | - | % | - | |
| CHEMBL2179114 | — | Inhibition | - | % | - | |
| CHEMBL2179113 | — | Inhibition | - | % | - | |
| CHEMBL2179112 | — | Inhibition | - | % | - | |
| CHEMBL2179111 | — | Inhibition | - | % | - | |
| CHEMBL2179110 | — | Inhibition | - | % | - | |
| CHEMBL2179109 | — | Inhibition | - | % | - | |
| CHEMBL2179108 | — | Inhibition | - | % | - | |
| CHEMBL2179107 | — | Inhibition | - | % | - |