Assay Detail
Binding
CHEMBL860987
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Displacement of [3H]estrone from ER beta
51
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Synthesis and characterization of 3-arylquinazolinone and 3-arylquinazolinethione derivatives as selective estrogen receptor beta modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 51 | 5.70 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | 4.0 | 1 | 7.96 |
| CHEMBL380359 | — | — | 1 | 7.62 |
| CHEMBL1405 | ESTRONE | 4.0 | 1 | 7.51 |
| CHEMBL208324 | — | — | 1 | 7.33 |
| CHEMBL44 | GENISTEIN | 2.0 | 1 | 7.21 |
| CHEMBL379889 | — | — | 1 | 7.10 |
| CHEMBL207101 | — | — | 1 | 6.99 |
| CHEMBL205920 | — | — | 1 | 6.81 |
| CHEMBL205398 | — | — | 1 | 6.75 |
| CHEMBL206814 | — | — | 1 | 6.60 |
| CHEMBL377083 | — | — | 1 | 6.59 |
| CHEMBL206131 | — | — | 1 | 6.58 |
| CHEMBL203351 | — | — | 1 | 6.58 |
| CHEMBL206336 | — | — | 1 | 6.50 |
| CHEMBL203283 | — | — | 1 | 6.38 |
| CHEMBL203724 | — | — | 1 | 6.29 |
| CHEMBL206764 | — | — | 1 | 6.19 |
| CHEMBL206137 | — | — | 1 | 6.18 |
| CHEMBL381720 | — | — | 1 | 5.89 |
| CHEMBL202996 | THIOGENISTEIN | — | 1 | 5.87 |
| CHEMBL382698 | — | — | 1 | 5.64 |
| CHEMBL206499 | — | — | 1 | 5.49 |
| CHEMBL206648 | — | — | 1 | 5.45 |
| CHEMBL202738 | — | — | 1 | 5.42 |
| CHEMBL206287 | — | — | 1 | 5.40 |
| CHEMBL205395 | — | — | 1 | 5.39 |
| CHEMBL202894 | — | — | 1 | 5.24 |
| CHEMBL206349 | — | — | 1 | 5.16 |
| CHEMBL203442 | — | — | 1 | 5.14 |
| CHEMBL203330 | — | — | 1 | 5.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL380359 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL1405 | ESTRONE | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL208324 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL44 | GENISTEIN | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL379889 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL207101 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL205920 | — | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL205398 | — | IC50 | = | 179.0 | nM | 6.75 |
| CHEMBL206814 | — | IC50 | = | 249.0 | nM | 6.60 |
| CHEMBL377083 | — | IC50 | = | 256.0 | nM | 6.59 |
| CHEMBL206131 | — | IC50 | = | 263.0 | nM | 6.58 |
| CHEMBL203351 | — | IC50 | = | 265.0 | nM | 6.58 |
| CHEMBL206336 | — | IC50 | = | 317.0 | nM | 6.50 |
| CHEMBL203283 | — | IC50 | = | 422.0 | nM | 6.38 |
| CHEMBL203724 | — | IC50 | = | 515.0 | nM | 6.29 |
| CHEMBL206764 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL206137 | — | IC50 | = | 658.0 | nM | 6.18 |
| CHEMBL381720 | — | IC50 | = | 1275.0 | nM | 5.89 |
| CHEMBL202996 | THIOGENISTEIN | IC50 | = | 1340.0 | nM | 5.87 |
| CHEMBL382698 | — | IC50 | = | 2302.0 | nM | 5.64 |
| CHEMBL206499 | — | IC50 | = | 3224.0 | nM | 5.49 |
| CHEMBL206648 | — | IC50 | = | 3531.0 | nM | 5.45 |
| CHEMBL202738 | — | IC50 | = | 3842.0 | nM | 5.42 |
| CHEMBL206287 | — | IC50 | = | 3970.0 | nM | 5.40 |
| CHEMBL205395 | — | IC50 | = | 4081.0 | nM | 5.39 |
| CHEMBL202894 | — | IC50 | = | 5752.0 | nM | 5.24 |
| CHEMBL206349 | — | IC50 | = | 6994.0 | nM | 5.16 |
| CHEMBL203442 | — | IC50 | = | 7305.0 | nM | 5.14 |
| CHEMBL203330 | — | IC50 | = | 7211.0 | nM | 5.14 |
| CHEMBL379252 | — | IC50 | = | 7487.0 | nM | 5.13 |
| CHEMBL206286 | — | IC50 | = | 8242.0 | nM | 5.08 |
| CHEMBL203370 | — | IC50 | = | 8609.0 | nM | 5.07 |
| CHEMBL206773 | — | IC50 | = | 9379.0 | nM | 5.03 |
| CHEMBL205137 | — | IC50 | = | 9536.0 | nM | 5.02 |
| CHEMBL379213 | — | IC50 | = | 9525.0 | nM | 5.02 |
| CHEMBL205577 | — | IC50 | = | 11371.0 | nM | 4.94 |
| CHEMBL378807 | — | IC50 | = | 11979.0 | nM | 4.92 |
| CHEMBL206702 | — | IC50 | = | 12298.0 | nM | 4.91 |
| CHEMBL208451 | — | IC50 | = | 13426.0 | nM | 4.87 |
| CHEMBL205249 | — | IC50 | = | 17004.0 | nM | 4.77 |
| CHEMBL378572 | — | IC50 | = | 18472.0 | nM | 4.73 |
| CHEMBL425941 | — | IC50 | = | 30661.0 | nM | 4.51 |
| CHEMBL202733 | — | IC50 | = | 44265.0 | nM | 4.35 |
| CHEMBL203122 | — | IC50 | = | 48086.0 | nM | 4.32 |
| CHEMBL206426 | — | IC50 | = | 51696.0 | nM | 4.29 |
| CHEMBL206772 | — | IC50 | = | 72848.0 | nM | 4.14 |
| CHEMBL205717 | — | IC50 | = | 73677.0 | nM | 4.13 |
| CHEMBL425231 | — | IC50 | = | 440553.0 | nM | - |
| CHEMBL377293 | — | IC50 | - | — | - |