Assay Detail
Binding
CHEMBL829540
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory concentration against human ER alpha expressed in Escherichia coli was determined using [3H]17-beta-estradiol as radio ligand
107
Total Activities
107
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
Design and synthesis of aryl diphenolic azoles as potent and selective estrogen receptor-beta ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 107 | 6.30 | 8.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | 4.0 | 1 | 8.49 |
| CHEMBL188051 | — | — | 1 | 8.22 |
| CHEMBL187105 | — | — | 1 | 8.10 |
| CHEMBL186598 | — | — | 1 | 7.89 |
| CHEMBL189200 | — | — | 1 | 7.66 |
| CHEMBL360410 | — | — | 1 | 7.62 |
| CHEMBL187219 | — | — | 1 | 7.62 |
| CHEMBL361078 | — | — | 1 | 7.52 |
| CHEMBL362307 | — | — | 1 | 7.48 |
| CHEMBL189077 | — | — | 1 | 7.46 |
| CHEMBL187311 | — | — | 1 | 7.36 |
| CHEMBL187915 | — | — | 1 | 7.33 |
| CHEMBL187393 | — | — | 1 | 7.31 |
| CHEMBL435090 | — | — | 1 | 7.30 |
| CHEMBL186597 | — | — | 1 | 7.19 |
| CHEMBL187087 | — | — | 1 | 7.09 |
| CHEMBL189356 | — | — | 1 | 7.01 |
| CHEMBL185918 | — | — | 1 | 6.93 |
| CHEMBL188391 | — | — | 1 | 6.86 |
| CHEMBL189658 | — | — | 1 | 6.86 |
| CHEMBL183367 | — | — | 1 | 6.82 |
| CHEMBL188528 | — | — | 1 | 6.81 |
| CHEMBL188189 | — | — | 1 | 6.79 |
| CHEMBL183368 | — | — | 1 | 6.79 |
| CHEMBL367588 | — | — | 1 | 6.75 |
| CHEMBL189080 | — | — | 1 | 6.74 |
| CHEMBL189287 | — | — | 1 | 6.72 |
| CHEMBL361272 | — | — | 1 | 6.71 |
| CHEMBL360189 | — | — | 1 | 6.68 |
| CHEMBL188846 | — | — | 1 | 6.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL188051 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL187105 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL186598 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL189200 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL360410 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL187219 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL361078 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL362307 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL189077 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL187311 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL187915 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL187393 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL435090 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL186597 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL187087 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL189356 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL185918 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL188391 | — | IC50 | = | 139.0 | nM | 6.86 |
| CHEMBL189658 | — | IC50 | = | 138.0 | nM | 6.86 |
| CHEMBL183367 | — | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL188528 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL183368 | — | IC50 | = | 163.0 | nM | 6.79 |
| CHEMBL188189 | — | IC50 | = | 161.0 | nM | 6.79 |
| CHEMBL367588 | — | IC50 | = | 176.0 | nM | 6.75 |
| CHEMBL189080 | — | IC50 | = | 183.0 | nM | 6.74 |
| CHEMBL189287 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL361272 | — | IC50 | = | 196.0 | nM | 6.71 |
| CHEMBL360189 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL188846 | — | IC50 | = | 227.0 | nM | 6.64 |
| CHEMBL188517 | — | IC50 | = | 249.0 | nM | 6.60 |
| CHEMBL185890 | — | IC50 | = | 264.0 | nM | 6.58 |
| CHEMBL187207 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL360651 | — | IC50 | = | 273.0 | nM | 6.56 |
| CHEMBL188458 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL362355 | — | IC50 | = | 373.0 | nM | 6.43 |
| CHEMBL186643 | — | IC50 | = | 376.0 | nM | 6.42 |
| CHEMBL188957 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL44 | GENISTEIN | IC50 | = | 395.0 | nM | 6.40 |
| CHEMBL186513 | — | IC50 | = | 411.0 | nM | 6.39 |
| CHEMBL186945 | — | IC50 | = | 431.0 | nM | 6.37 |
| CHEMBL189556 | — | IC50 | = | 434.0 | nM | 6.36 |
| CHEMBL363955 | — | IC50 | = | 447.0 | nM | 6.35 |
| CHEMBL362356 | — | IC50 | = | 464.0 | nM | 6.33 |
| CHEMBL188299 | — | IC50 | = | 463.0 | nM | 6.33 |
| CHEMBL187937 | — | IC50 | = | 481.0 | nM | 6.32 |
| CHEMBL189822 | — | IC50 | = | 475.0 | nM | 6.32 |
| CHEMBL363963 | — | IC50 | = | 474.0 | nM | 6.32 |
| CHEMBL184003 | — | IC50 | = | 498.0 | nM | 6.30 |
| CHEMBL188246 | — | IC50 | = | 511.0 | nM | 6.29 |