Assay Detail
Binding
CHEMBL831155
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Inhibition of [3H]17-beta-estradiol binding to human estrogen receptor alpha expressed in Escherichia coli
70
Total Activities
70
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
ERbeta ligands. 3. Exploiting two binding orientations of the 2-phenylnaphthalene scaffold to achieve ERbeta selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 70 | 6.85 | 8.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | 4.0 | 1 | 8.49 |
| CHEMBL195311 | — | — | 1 | 8.00 |
| CHEMBL192621 | — | — | 1 | 7.99 |
| CHEMBL363425 | — | — | 1 | 7.68 |
| CHEMBL193726 | — | — | 1 | 7.66 |
| CHEMBL192386 | — | — | 1 | 7.66 |
| CHEMBL195878 | — | — | 1 | 7.62 |
| CHEMBL363634 | — | — | 1 | 7.58 |
| CHEMBL195289 | — | — | 1 | 7.57 |
| CHEMBL363367 | — | — | 1 | 7.52 |
| CHEMBL192260 | — | — | 1 | 7.46 |
| CHEMBL191710 | — | — | 1 | 7.44 |
| CHEMBL191300 | — | — | 1 | 7.40 |
| CHEMBL195389 | — | — | 1 | 7.40 |
| CHEMBL193146 | — | — | 1 | 7.40 |
| CHEMBL192876 | — | — | 1 | 7.37 |
| CHEMBL426641 | — | — | 1 | 7.35 |
| CHEMBL192390 | — | — | 1 | 7.26 |
| CHEMBL447837 | — | — | 1 | 7.24 |
| CHEMBL192901 | — | — | 1 | 7.14 |
| CHEMBL191759 | — | — | 1 | 7.14 |
| CHEMBL192782 | — | — | 1 | 7.11 |
| CHEMBL194762 | — | — | 1 | 7.08 |
| CHEMBL193727 | — | — | 1 | 7.04 |
| CHEMBL364092 | — | — | 1 | 7.04 |
| CHEMBL191716 | — | — | 1 | 7.04 |
| CHEMBL192000 | — | — | 1 | 7.02 |
| CHEMBL192218 | — | — | 1 | 7.01 |
| CHEMBL371624 | — | — | 1 | 6.98 |
| CHEMBL365999 | — | — | 1 | 6.97 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL195311 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL192621 | — | IC50 | = | 10.3 | nM | 7.99 |
| CHEMBL363425 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL193726 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL192386 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL195878 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL363634 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL195289 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL363367 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL192260 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL191710 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL195389 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL193146 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL191300 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL192876 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL426641 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL192390 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL447837 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL192901 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL191759 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL192782 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL194762 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL191716 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL193727 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL364092 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL192000 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL192218 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL371624 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL365999 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL195807 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL195208 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL195039 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL363177 | — | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL191901 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL362966 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL191808 | — | IC50 | = | 143.0 | nM | 6.84 |
| CHEMBL427180 | — | IC50 | = | 174.0 | nM | 6.76 |
| CHEMBL192849 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL194326 | — | IC50 | = | 186.0 | nM | 6.73 |
| CHEMBL192154 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL191974 | — | IC50 | = | 211.0 | nM | 6.68 |
| CHEMBL195217 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL365941 | — | IC50 | = | 231.0 | nM | 6.64 |
| CHEMBL193064 | — | IC50 | = | 235.0 | nM | 6.63 |
| CHEMBL192016 | — | IC50 | = | 247.0 | nM | 6.61 |
| CHEMBL195290 | — | IC50 | = | 254.0 | nM | 6.59 |
| CHEMBL194936 | — | IC50 | = | 266.0 | nM | 6.58 |
| CHEMBL372030 | — | IC50 | = | 282.0 | nM | 6.55 |
| CHEMBL191238 | — | IC50 | = | 299.0 | nM | 6.52 |