Assay Detail
Binding
CHEMBL4730248
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Displacement of fluormone from GST-tagged ERbeta receptor LBD (unknown origin) measured after 60 mins by TR-FRET competitive binding assay
14
Total Activities
14
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 | 14 | 7.85 | 9.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | 4.0 | 1 | 9.68 |
| CHEMBL4782490 | — | — | 1 | 9.57 |
| CHEMBL691 | ETHINYL ESTRADIOL | 4.0 | 1 | 9.43 |
| CHEMBL4761096 | — | — | 1 | 9.19 |
| CHEMBL1405 | ESTRONE | 4.0 | 1 | 9.03 |
| CHEMBL4785948 | — | — | 1 | 8.22 |
| CHEMBL4752614 | — | — | 1 | 7.92 |
| CHEMBL4778702 | — | — | 1 | 7.82 |
| CHEMBL4745013 | — | — | 1 | 7.30 |
| CHEMBL4751119 | — | — | 1 | 7.29 |
| CHEMBL4744639 | — | — | 1 | 7.11 |
| CHEMBL4741481 | — | — | 1 | 6.44 |
| CHEMBL4754151 | — | — | 1 | 5.55 |
| CHEMBL4747395 | — | — | 1 | 5.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | EC50 | = | 0.21 | nM | 9.68 |
| CHEMBL4782490 | — | EC50 | = | 0.27 | nM | 9.57 |
| CHEMBL691 | ETHINYL ESTRADIOL | EC50 | = | 0.37 | nM | 9.43 |
| CHEMBL4761096 | — | EC50 | = | 0.65 | nM | 9.19 |
| CHEMBL1405 | ESTRONE | EC50 | = | 0.94 | nM | 9.03 |
| CHEMBL4785948 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4752614 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4778702 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4745013 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4751119 | — | EC50 | = | 51.0 | nM | 7.29 |
| CHEMBL4744639 | — | EC50 | = | 78.0 | nM | 7.11 |
| CHEMBL4741481 | — | EC50 | = | 360.0 | nM | 6.44 |
| CHEMBL4754151 | — | EC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL4747395 | — | EC50 | = | 4400.0 | nM | 5.36 |