Assay Detail
Binding
CHEMBL1828368
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Inhibition of aromatase using 7-methoxy-4-trifluoromethyl coumarin as substrate after 30 mins by fluorescence-based colorimetric analysis
68
Total Activities
68
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Synthesis and structure-activity relationship of 1- and 2-substituted-1,2,3-triazole letrozole-based analogues as aromatase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 68 | 5.37 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL29482 | — | — | 1 | 8.40 |
| CHEMBL349822 | — | — | 1 | 8.15 |
| CHEMBL224789 | — | — | 1 | 8.10 |
| CHEMBL1444 | LETROZOLE | 4.0 | 1 | 8.10 |
| CHEMBL336638 | — | — | 1 | 7.70 |
| CHEMBL1824769 | — | — | 1 | 7.00 |
| CHEMBL14192 | BENZYLIMIDAZOLE | — | 1 | 6.82 |
| CHEMBL1825020 | — | — | 1 | 6.82 |
| CHEMBL1825024 | — | — | 1 | 5.96 |
| CHEMBL1825045 | — | — | 1 | 5.87 |
| CHEMBL1825047 | — | — | 1 | 5.64 |
| CHEMBL1825036 | — | — | 1 | 5.63 |
| CHEMBL1825046 | — | — | 1 | 5.56 |
| CHEMBL1825027 | — | — | 1 | 5.51 |
| CHEMBL1825030 | — | — | 1 | 5.47 |
| CHEMBL1825032 | — | — | 1 | 5.41 |
| CHEMBL1825021 | — | — | 1 | 5.39 |
| CHEMBL1825035 | — | — | 1 | 5.38 |
| CHEMBL1825025 | — | — | 1 | 5.36 |
| CHEMBL1824755 | — | — | 1 | 5.34 |
| CHEMBL1824742 | — | — | 1 | 5.33 |
| CHEMBL1824750 | — | — | 1 | 5.33 |
| CHEMBL1825044 | — | — | 1 | 5.30 |
| CHEMBL1824743 | — | — | 1 | 5.29 |
| CHEMBL1825026 | — | — | 1 | 5.28 |
| CHEMBL1825034 | — | — | 1 | 5.25 |
| CHEMBL1825031 | — | — | 1 | 5.21 |
| CHEMBL1825041 | — | — | 1 | 5.19 |
| CHEMBL1825039 | — | — | 1 | 5.13 |
| CHEMBL1824751 | — | — | 1 | 5.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL29482 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL349822 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1444 | LETROZOLE | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL224789 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL336638 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1824769 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL14192 | BENZYLIMIDAZOLE | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL1825020 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL1825024 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1825045 | — | IC50 | = | 1360.0 | nM | 5.87 |
| CHEMBL1825047 | — | IC50 | = | 2270.0 | nM | 5.64 |
| CHEMBL1825036 | — | IC50 | = | 2340.0 | nM | 5.63 |
| CHEMBL1825046 | — | IC50 | = | 2780.0 | nM | 5.56 |
| CHEMBL1825027 | — | IC50 | = | 3070.0 | nM | 5.51 |
| CHEMBL1825030 | — | IC50 | = | 3380.0 | nM | 5.47 |
| CHEMBL1825032 | — | IC50 | = | 3910.0 | nM | 5.41 |
| CHEMBL1825021 | — | IC50 | = | 4110.0 | nM | 5.39 |
| CHEMBL1825035 | — | IC50 | = | 4170.0 | nM | 5.38 |
| CHEMBL1825025 | — | IC50 | = | 4370.0 | nM | 5.36 |
| CHEMBL1824755 | — | IC50 | = | 4580.0 | nM | 5.34 |
| CHEMBL1824742 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL1824750 | — | IC50 | = | 4640.0 | nM | 5.33 |
| CHEMBL1825044 | — | IC50 | = | 5040.0 | nM | 5.30 |
| CHEMBL1824743 | — | IC50 | = | 5070.0 | nM | 5.29 |
| CHEMBL1825026 | — | IC50 | = | 5260.0 | nM | 5.28 |
| CHEMBL1825034 | — | IC50 | = | 5620.0 | nM | 5.25 |
| CHEMBL1825031 | — | IC50 | = | 6090.0 | nM | 5.21 |
| CHEMBL1825041 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL1825039 | — | IC50 | = | 7470.0 | nM | 5.13 |
| CHEMBL1824751 | — | IC50 | = | 7730.0 | nM | 5.11 |
| CHEMBL1825042 | — | IC50 | = | 7980.0 | nM | 5.10 |
| CHEMBL1825028 | — | IC50 | = | 7880.0 | nM | 5.10 |
| CHEMBL1825033 | — | IC50 | = | 9160.0 | nM | 5.04 |
| CHEMBL1825040 | — | IC50 | = | 9530.0 | nM | 5.02 |
| CHEMBL1825043 | — | IC50 | = | 9770.0 | nM | 5.01 |
| CHEMBL1824747 | — | IC50 | = | 10330.0 | nM | 4.99 |
| CHEMBL272339 | — | IC50 | = | 10600.0 | nM | 4.97 |
| CHEMBL1824744 | — | IC50 | = | 10600.0 | nM | 4.97 |
| CHEMBL1825029 | — | IC50 | = | 10700.0 | nM | 4.97 |
| CHEMBL1825049 | — | IC50 | = | 10700.0 | nM | 4.97 |
| CHEMBL1824752 | — | IC50 | = | 10950.0 | nM | 4.96 |
| CHEMBL1824748 | — | IC50 | = | 10970.0 | nM | 4.96 |
| CHEMBL1824756 | — | IC50 | = | 10960.0 | nM | 4.96 |
| CHEMBL1825037 | — | IC50 | = | 11570.0 | nM | 4.94 |
| CHEMBL1824765 | — | IC50 | = | 11610.0 | nM | 4.93 |
| CHEMBL1825018 | — | IC50 | = | 11880.0 | nM | 4.92 |
| CHEMBL1825023 | — | IC50 | = | 12010.0 | nM | 4.92 |
| CHEMBL1824753 | — | IC50 | = | 12160.0 | nM | 4.92 |
| CHEMBL1825017 | — | IC50 | = | 12200.0 | nM | 4.91 |
| CHEMBL1825038 | — | IC50 | = | 12630.0 | nM | 4.90 |