Assay Detail
Binding
CHEMBL4716146
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Inhibition of recombinant human aromatase incubated for 30 mins using fluorometric substrate 7-methoxy-4-trifluoromethylcoumarin in presence of NADPH cofactor mix by fluorometric assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis of Triphenylethylene Bisphenols as Aromatase Inhibitors That Also Modulate Estrogen Receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.30 | 8.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4777271 | — | — | 1 | 8.32 |
| CHEMBL4755831 | — | — | 1 | 8.28 |
| CHEMBL4745681 | — | — | 1 | 7.75 |
| CHEMBL4760286 | — | — | 1 | 7.44 |
| CHEMBL4778401 | — | — | 1 | 7.22 |
| CHEMBL4780337 | — | — | 1 | 7.22 |
| CHEMBL4753594 | — | — | 1 | 7.03 |
| CHEMBL4750835 | — | — | 1 | 6.98 |
| CHEMBL4797578 | — | — | 1 | 6.86 |
| CHEMBL4761359 | — | — | 1 | 6.36 |
| CHEMBL4764457 | — | — | 1 | 5.53 |
| CHEMBL4753984 | — | — | 1 | 5.52 |
| CHEMBL4749692 | — | — | 1 | 4.90 |
| CHEMBL4763409 | — | — | 1 | 4.89 |
| CHEMBL4752568 | — | — | 1 | 4.85 |
| CHEMBL4747849 | — | — | 1 | 4.82 |
| CHEMBL4743255 | — | — | 1 | 4.76 |
| CHEMBL149791 | — | — | 1 | 4.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4777271 | — | IC50 | = | 4.77 | nM | 8.32 |
| CHEMBL4755831 | — | IC50 | = | 5.24 | nM | 8.28 |
| CHEMBL4745681 | — | IC50 | = | 17.7 | nM | 7.75 |
| CHEMBL4760286 | — | IC50 | = | 36.3 | nM | 7.44 |
| CHEMBL4778401 | — | IC50 | = | 60.4 | nM | 7.22 |
| CHEMBL4780337 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4753594 | — | IC50 | = | 94.4 | nM | 7.03 |
| CHEMBL4750835 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL4797578 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL4761359 | — | IC50 | = | 439.0 | nM | 6.36 |
| CHEMBL4764457 | — | IC50 | = | 2980.0 | nM | 5.53 |
| CHEMBL4753984 | — | IC50 | = | 3030.0 | nM | 5.52 |
| CHEMBL4749692 | — | IC50 | = | 12500.0 | nM | 4.90 |
| CHEMBL4763409 | — | IC50 | = | 12800.0 | nM | 4.89 |
| CHEMBL4752568 | — | IC50 | = | 14200.0 | nM | 4.85 |
| CHEMBL4747849 | — | IC50 | = | 15200.0 | nM | 4.82 |
| CHEMBL4743255 | — | IC50 | = | 17200.0 | nM | 4.76 |
| CHEMBL149791 | — | IC50 | = | 24900.0 | nM | 4.60 |