Assay Detail
Functional
CHEMBL860992
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ER beta-mediated transactivation of ERE in HeLa cell luciferase assay
47
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| 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 |
|---|---|---|---|
| EC50 | 47 | 6.21 | 9.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | 4.0 | 1 | 9.08 |
| CHEMBL208324 | — | — | 1 | 7.89 |
| CHEMBL202996 | THIOGENISTEIN | — | 1 | 7.85 |
| CHEMBL207101 | — | — | 1 | 7.70 |
| CHEMBL1405 | ESTRONE | 4.0 | 1 | 7.58 |
| CHEMBL205920 | — | — | 1 | 7.28 |
| CHEMBL203351 | — | — | 1 | 7.21 |
| CHEMBL44 | GENISTEIN | 2.0 | 1 | 7.14 |
| CHEMBL205398 | — | — | 1 | 7.12 |
| CHEMBL203283 | — | — | 1 | 6.96 |
| CHEMBL206764 | — | — | 1 | 6.93 |
| CHEMBL206336 | — | — | 1 | 6.87 |
| CHEMBL206137 | — | — | 1 | 6.80 |
| CHEMBL203724 | — | — | 1 | 6.76 |
| CHEMBL377083 | — | — | 1 | 6.72 |
| CHEMBL379889 | — | — | 1 | 6.65 |
| CHEMBL206131 | — | — | 1 | 6.60 |
| CHEMBL206648 | — | — | 1 | 6.45 |
| CHEMBL205395 | — | — | 1 | 6.23 |
| CHEMBL382698 | — | — | 1 | 6.14 |
| CHEMBL205249 | — | — | 1 | 6.12 |
| CHEMBL202738 | — | — | 1 | 6.04 |
| CHEMBL203370 | — | — | 1 | 6.02 |
| CHEMBL203330 | — | — | 1 | 5.93 |
| CHEMBL202894 | — | — | 1 | 5.90 |
| CHEMBL379252 | — | — | 1 | 5.90 |
| CHEMBL206773 | — | — | 1 | 5.88 |
| CHEMBL205577 | — | — | 1 | 5.80 |
| CHEMBL206287 | — | — | 1 | 5.79 |
| CHEMBL378572 | — | — | 1 | 5.76 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | EC50 | = | 0.84 | nM | 9.08 |
| CHEMBL208324 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL202996 | THIOGENISTEIN | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL207101 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1405 | ESTRONE | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL205920 | — | EC50 | = | 53.0 | nM | 7.28 |
| CHEMBL203351 | — | EC50 | = | 62.0 | nM | 7.21 |
| CHEMBL44 | GENISTEIN | EC50 | = | 73.0 | nM | 7.14 |
| CHEMBL205398 | — | EC50 | = | 76.0 | nM | 7.12 |
| CHEMBL203283 | — | EC50 | = | 111.0 | nM | 6.96 |
| CHEMBL206764 | — | EC50 | = | 117.0 | nM | 6.93 |
| CHEMBL206336 | — | EC50 | = | 136.0 | nM | 6.87 |
| CHEMBL206137 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL203724 | — | EC50 | = | 173.0 | nM | 6.76 |
| CHEMBL377083 | — | EC50 | = | 190.0 | nM | 6.72 |
| CHEMBL379889 | — | EC50 | = | 222.0 | nM | 6.65 |
| CHEMBL206131 | — | EC50 | = | 251.0 | nM | 6.60 |
| CHEMBL206648 | — | EC50 | = | 358.0 | nM | 6.45 |
| CHEMBL205395 | — | EC50 | = | 593.0 | nM | 6.23 |
| CHEMBL382698 | — | EC50 | = | 729.0 | nM | 6.14 |
| CHEMBL205249 | — | EC50 | = | 750.0 | nM | 6.12 |
| CHEMBL202738 | — | EC50 | = | 904.0 | nM | 6.04 |
| CHEMBL203370 | — | EC50 | = | 961.0 | nM | 6.02 |
| CHEMBL203330 | — | EC50 | = | 1181.0 | nM | 5.93 |
| CHEMBL379252 | — | EC50 | = | 1254.0 | nM | 5.90 |
| CHEMBL202894 | — | EC50 | = | 1261.0 | nM | 5.90 |
| CHEMBL206773 | — | EC50 | = | 1313.0 | nM | 5.88 |
| CHEMBL205577 | — | EC50 | = | 1583.0 | nM | 5.80 |
| CHEMBL206287 | — | EC50 | = | 1638.0 | nM | 5.79 |
| CHEMBL378572 | — | EC50 | = | 1721.0 | nM | 5.76 |
| CHEMBL206702 | — | EC50 | = | 1966.0 | nM | 5.71 |
| CHEMBL206349 | — | EC50 | = | 1985.0 | nM | 5.70 |
| CHEMBL206286 | — | EC50 | = | 2064.0 | nM | 5.68 |
| CHEMBL378807 | — | EC50 | = | 3804.0 | nM | 5.42 |
| CHEMBL206772 | — | EC50 | = | 3843.0 | nM | 5.42 |
| CHEMBL380359 | — | EC50 | = | 4457.0 | nM | 5.35 |
| CHEMBL205717 | — | EC50 | = | 7579.0 | nM | 5.12 |
| CHEMBL379213 | — | EC50 | = | 8506.0 | nM | 5.07 |
| CHEMBL426115 | — | EC50 | = | 8506.0 | nM | 5.07 |
| CHEMBL208451 | — | EC50 | = | 8776.0 | nM | 5.06 |
| CHEMBL381720 | — | EC50 | = | 8870.0 | nM | 5.05 |
| CHEMBL205137 | — | EC50 | = | 9406.0 | nM | 5.03 |
| CHEMBL206426 | — | EC50 | = | 9763.0 | nM | 5.01 |
| CHEMBL382240 | — | EC50 | = | 11342.0 | nM | 4.95 |
| CHEMBL425941 | — | EC50 | = | 11685.0 | nM | 4.93 |
| CHEMBL382786 | — | EC50 | - | — | - | |
| CHEMBL377293 | — | EC50 | - | — | - |