Assay Detail
Functional
CHEMBL2185144
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Cytotoxicity against human MCF7a cells expressing Tet-off-3betaHSD1-Arom assessed as inhibition of TST-stimulated cell proliferation measured after 10 days
14
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | MCF7a |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Novel aromatase inhibitors by structure-guided design.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 8 | 8.80 | 10.52 |
| Inhibition | 6 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2179110 | — | — | 2 | 10.52 |
| CHEMBL2179114 | — | — | 2 | 9.52 |
| CHEMBL2179109 | — | — | 2 | 8.77 |
| CHEMBL2179111 | — | — | 2 | 8.47 |
| CHEMBL2179112 | — | — | 2 | 8.27 |
| CHEMBL1200374 | EXEMESTANE | 4.0 | 1 | 8.25 |
| CHEMBL2179113 | — | — | 2 | 7.80 |
| CHEMBL1444 | LETROZOLE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2179110 | — | EC50 | = | 0.03 | nM | 10.52 |
| CHEMBL2179114 | — | EC50 | = | 0.3 | nM | 9.52 |
| CHEMBL2179109 | — | EC50 | = | 1.7 | nM | 8.77 |
| CHEMBL2179111 | — | EC50 | = | 3.4 | nM | 8.47 |
| CHEMBL2179112 | — | EC50 | = | 5.4 | nM | 8.27 |
| CHEMBL1200374 | EXEMESTANE | EC50 | = | 5.6 | nM | 8.25 |
| CHEMBL2179113 | — | EC50 | = | 15.7 | nM | 7.80 |
| CHEMBL1444 | LETROZOLE | EC50 | = | 0.004 | nM | - |
| CHEMBL2179114 | — | Inhibition | - | % | - | |
| CHEMBL2179113 | — | Inhibition | - | % | - | |
| CHEMBL2179112 | — | Inhibition | - | % | - | |
| CHEMBL2179111 | — | Inhibition | - | % | - | |
| CHEMBL2179110 | — | Inhibition | - | % | - | |
| CHEMBL2179109 | — | Inhibition | - | % | - |