Assay Detail
Binding
CHEMBL4730252
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at full length human ERbeta receptor assessed as transcriptional activity incubated for 22 to 24 hrs by cell based luciferase reporter gene assay
13
Total Activities
13
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
Synthesis and evaluation of 17α-triazolyl and 9α-cyano derivatives of estradiol.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 13 | 8.50 | 10.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | 4.0 | 1 | 10.66 |
| CHEMBL4782490 | — | — | 1 | 10.54 |
| CHEMBL691 | ETHINYL ESTRADIOL | 4.0 | 1 | 9.80 |
| CHEMBL1405 | ESTRONE | 4.0 | 1 | 9.30 |
| CHEMBL4761096 | — | — | 1 | 9.09 |
| CHEMBL4785948 | — | — | 1 | 8.68 |
| CHEMBL4778702 | — | — | 1 | 8.13 |
| CHEMBL4744639 | — | — | 1 | 8.05 |
| CHEMBL4751119 | — | — | 1 | 7.85 |
| CHEMBL4745013 | — | — | 1 | 7.80 |
| CHEMBL4752614 | — | — | 1 | 7.68 |
| CHEMBL4741481 | — | — | 1 | 6.62 |
| CHEMBL4754151 | — | — | 1 | 6.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | EC50 | = | 0.022 | nM | 10.66 |
| CHEMBL4782490 | — | EC50 | = | 0.029 | nM | 10.54 |
| CHEMBL691 | ETHINYL ESTRADIOL | EC50 | = | 0.16 | nM | 9.80 |
| CHEMBL1405 | ESTRONE | EC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4761096 | — | EC50 | = | 0.81 | nM | 9.09 |
| CHEMBL4785948 | — | EC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4778702 | — | EC50 | = | 7.4 | nM | 8.13 |
| CHEMBL4744639 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4751119 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4745013 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4752614 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4741481 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4754151 | — | EC50 | = | 490.0 | nM | 6.31 |