Assay Detail
Binding
CHEMBL860989
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Displacement of [3H]estrone from ER alpha
42
Total Activities
42
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 | 42 | 5.03 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | 4.0 | 1 | 8.00 |
| CHEMBL1405 | ESTRONE | 4.0 | 1 | 7.54 |
| CHEMBL380359 | — | — | 1 | 6.92 |
| CHEMBL206814 | — | — | 1 | 6.75 |
| CHEMBL379889 | — | — | 1 | 5.76 |
| CHEMBL44 | GENISTEIN | 2.0 | 1 | 5.71 |
| CHEMBL205920 | — | — | 1 | 5.65 |
| CHEMBL208324 | — | — | 1 | 5.58 |
| CHEMBL206137 | — | — | 1 | 5.54 |
| CHEMBL207101 | — | — | 1 | 5.51 |
| CHEMBL203283 | — | — | 1 | 5.36 |
| CHEMBL206499 | — | — | 1 | 5.27 |
| CHEMBL206131 | — | — | 1 | 5.20 |
| CHEMBL377083 | — | — | 1 | 5.13 |
| CHEMBL206336 | — | — | 1 | 5.02 |
| CHEMBL203442 | — | — | 1 | 4.97 |
| CHEMBL205398 | — | — | 1 | 4.96 |
| CHEMBL206349 | — | — | 1 | 4.95 |
| CHEMBL203351 | — | — | 1 | 4.88 |
| CHEMBL381720 | — | — | 1 | 4.82 |
| CHEMBL206286 | — | — | 1 | 4.81 |
| CHEMBL202894 | — | — | 1 | 4.71 |
| CHEMBL379213 | — | — | 1 | 4.59 |
| CHEMBL203724 | — | — | 1 | 4.56 |
| CHEMBL205577 | — | — | 1 | 4.48 |
| CHEMBL379252 | — | — | 1 | 4.46 |
| CHEMBL382698 | — | — | 1 | 4.36 |
| CHEMBL206764 | — | — | 1 | 4.36 |
| CHEMBL202738 | — | — | 1 | 4.36 |
| CHEMBL425231 | — | — | 1 | 4.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1405 | ESTRONE | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL380359 | — | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL206814 | — | IC50 | = | 178.0 | nM | 6.75 |
| CHEMBL379889 | — | IC50 | = | 1753.0 | nM | 5.76 |
| CHEMBL44 | GENISTEIN | IC50 | = | 1973.0 | nM | 5.71 |
| CHEMBL205920 | — | IC50 | = | 2260.0 | nM | 5.65 |
| CHEMBL208324 | — | IC50 | = | 2636.0 | nM | 5.58 |
| CHEMBL206137 | — | IC50 | = | 2854.0 | nM | 5.54 |
| CHEMBL207101 | — | IC50 | = | 3080.0 | nM | 5.51 |
| CHEMBL203283 | — | IC50 | = | 4382.0 | nM | 5.36 |
| CHEMBL206499 | — | IC50 | = | 5365.0 | nM | 5.27 |
| CHEMBL206131 | — | IC50 | = | 6247.0 | nM | 5.20 |
| CHEMBL377083 | — | IC50 | = | 7485.0 | nM | 5.13 |
| CHEMBL206336 | — | IC50 | = | 9635.0 | nM | 5.02 |
| CHEMBL203442 | — | IC50 | = | 10649.0 | nM | 4.97 |
| CHEMBL205398 | — | IC50 | = | 11097.0 | nM | 4.96 |
| CHEMBL206349 | — | IC50 | = | 11111.0 | nM | 4.95 |
| CHEMBL203351 | — | IC50 | = | 13240.0 | nM | 4.88 |
| CHEMBL381720 | — | IC50 | = | 15297.0 | nM | 4.82 |
| CHEMBL206286 | — | IC50 | = | 15521.0 | nM | 4.81 |
| CHEMBL202894 | — | IC50 | = | 19437.0 | nM | 4.71 |
| CHEMBL379213 | — | IC50 | = | 25956.0 | nM | 4.59 |
| CHEMBL203724 | — | IC50 | = | 27569.0 | nM | 4.56 |
| CHEMBL205577 | — | IC50 | = | 33248.0 | nM | 4.48 |
| CHEMBL379252 | — | IC50 | = | 34626.0 | nM | 4.46 |
| CHEMBL382698 | — | IC50 | = | 43968.0 | nM | 4.36 |
| CHEMBL206764 | — | IC50 | = | 44175.0 | nM | 4.36 |
| CHEMBL202738 | — | IC50 | = | 43814.0 | nM | 4.36 |
| CHEMBL425231 | — | IC50 | = | 48473.0 | nM | 4.32 |
| CHEMBL203370 | — | IC50 | = | 53640.0 | nM | 4.27 |
| CHEMBL203330 | — | IC50 | = | 55015.0 | nM | 4.26 |
| CHEMBL202996 | THIOGENISTEIN | IC50 | = | 55883.0 | nM | 4.25 |
| CHEMBL206426 | — | IC50 | = | 66860.0 | nM | 4.17 |
| CHEMBL206773 | — | IC50 | = | 70277.0 | nM | 4.15 |
| CHEMBL203122 | — | IC50 | = | 70399.0 | nM | 4.15 |
| CHEMBL378572 | — | IC50 | = | 75588.0 | nM | 4.12 |
| CHEMBL205137 | — | IC50 | = | 81324.0 | nM | 4.09 |
| CHEMBL206648 | — | IC50 | = | 97982.0 | nM | 4.01 |
| CHEMBL425941 | — | IC50 | = | 101544.0 | nM | - |
| CHEMBL377293 | — | IC50 | - | — | - | |
| CHEMBL382786 | — | IC50 | - | — | - |