Assay Detail
Binding
CHEMBL1011777
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Inhibition of human aromatase-mediated conversion of [1beta3H]androstenedione to estrone by liquid scintillation counting in presence of NADPH
89
Total Activities
88
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
Fast three dimensional pharmacophore virtual screening of new potent non-steroid aromatase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 89 | 6.25 | 8.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL224665 | — | — | 1 | 8.64 |
| CHEMBL513615 | — | — | 1 | 8.28 |
| CHEMBL1444 | LETROZOLE | 4.0 | 1 | 8.21 |
| CHEMBL459503 | — | — | 1 | 7.60 |
| CHEMBL459502 | — | — | 1 | 7.60 |
| CHEMBL159073 | — | — | 1 | 7.40 |
| CHEMBL421149 | — | — | 1 | 7.37 |
| CHEMBL213588 | — | — | 1 | 7.35 |
| CHEMBL509750 | — | — | 1 | 7.32 |
| CHEMBL522917 | — | — | 1 | 7.31 |
| CHEMBL437731 | — | — | 1 | 7.29 |
| CHEMBL522733 | — | — | 1 | 7.26 |
| CHEMBL209731 | — | — | 1 | 7.16 |
| CHEMBL213587 | — | — | 1 | 7.15 |
| CHEMBL223874 | — | — | 1 | 7.13 |
| CHEMBL495567 | — | — | 1 | 7.12 |
| CHEMBL212473 | — | — | 1 | 7.10 |
| CHEMBL421829 | — | — | 1 | 7.05 |
| CHEMBL495565 | — | — | 1 | 7.02 |
| CHEMBL525379 | — | — | 1 | 7.02 |
| CHEMBL158984 | — | — | 1 | 7.00 |
| CHEMBL224787 | — | — | 1 | 6.97 |
| CHEMBL225079 | — | — | 1 | 6.96 |
| CHEMBL224228 | — | — | 2 | 6.84 |
| CHEMBL225499 | — | — | 1 | 6.82 |
| CHEMBL375046 | — | — | 1 | 6.78 |
| CHEMBL53068 | — | — | 1 | 6.77 |
| CHEMBL496777 | — | — | 1 | 6.72 |
| CHEMBL188664 | — | — | 1 | 6.68 |
| CHEMBL496375 | — | — | 1 | 6.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL224665 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL513615 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL1444 | LETROZOLE | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL459503 | — | IC50 | = | 24.9 | nM | 7.60 |
| CHEMBL459502 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL159073 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL421149 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL213588 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL509750 | — | IC50 | = | 47.7 | nM | 7.32 |
| CHEMBL522917 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL437731 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL522733 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL209731 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL213587 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL223874 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL495567 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL212473 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL421829 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL495565 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL525379 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL158984 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL224787 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL225079 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL224228 | — | IC50 | = | 144.0 | nM | 6.84 |
| CHEMBL225499 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL375046 | — | IC50 | = | 168.0 | nM | 6.78 |
| CHEMBL53068 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL496777 | — | IC50 | = | 190.3 | nM | 6.72 |
| CHEMBL188664 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL496375 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL53290 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL161230 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL225472 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL185950 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL376786 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL54803 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL350922 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL377766 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL212168 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL293122 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL186079 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL363493 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL158635 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL184749 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL451201 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL224649 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL57513 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL225178 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL192306 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL78322 | — | IC50 | = | 940.0 | nM | 6.03 |