Assay Detail
Binding
CHEMBL831137
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Inhibition of [3H]17-beta-estradiol binding to human estrogen receptor beta 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 | 8.04 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL363634 | — | — | 1 | 9.30 |
| CHEMBL192901 | — | — | 1 | 8.96 |
| CHEMBL193146 | — | — | 1 | 8.96 |
| CHEMBL191759 | — | — | 1 | 8.92 |
| CHEMBL447837 | — | — | 1 | 8.92 |
| CHEMBL195311 | — | — | 1 | 8.85 |
| CHEMBL363425 | — | — | 1 | 8.82 |
| CHEMBL192386 | — | — | 1 | 8.80 |
| CHEMBL195878 | — | — | 1 | 8.70 |
| CHEMBL194762 | — | — | 1 | 8.70 |
| CHEMBL192000 | — | — | 1 | 8.68 |
| CHEMBL426641 | — | — | 1 | 8.66 |
| CHEMBL192621 | — | — | 1 | 8.64 |
| CHEMBL371624 | — | — | 1 | 8.64 |
| CHEMBL363367 | — | — | 1 | 8.64 |
| CHEMBL193064 | — | — | 1 | 8.62 |
| CHEMBL364092 | — | — | 1 | 8.60 |
| CHEMBL191901 | — | — | 1 | 8.60 |
| CHEMBL195208 | — | — | 1 | 8.60 |
| CHEMBL192390 | — | — | 1 | 8.59 |
| CHEMBL192154 | — | — | 1 | 8.57 |
| CHEMBL195289 | — | — | 1 | 8.55 |
| CHEMBL192218 | — | — | 1 | 8.52 |
| CHEMBL191710 | — | — | 1 | 8.48 |
| CHEMBL365941 | — | — | 1 | 8.47 |
| CHEMBL192260 | — | — | 1 | 8.47 |
| CHEMBL135 | ESTRADIOL | 4.0 | 1 | 8.44 |
| CHEMBL191808 | — | — | 1 | 8.40 |
| CHEMBL195290 | — | — | 1 | 8.36 |
| CHEMBL195039 | — | — | 1 | 8.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL363634 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL192901 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL193146 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL191759 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL447837 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL195311 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL363425 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL192386 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL195878 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL194762 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL192000 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL426641 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL371624 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL363367 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL192621 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL193064 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL364092 | — | IC50 | = | 2.52 | nM | 8.60 |
| CHEMBL191901 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL195208 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL192390 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL192154 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL195289 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL192218 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL191710 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL192260 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL365941 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL135 | ESTRADIOL | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL191808 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL195290 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL195039 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL193727 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL192849 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL195280 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL193726 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL371126 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL195807 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL192016 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL194326 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL192782 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL191648 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL191716 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL363177 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL192876 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL44 | GENISTEIN | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL363633 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL195389 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL192068 | — | IC50 | = | 10.6 | nM | 7.97 |
| CHEMBL365999 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL191238 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL362966 | — | IC50 | = | 12.0 | nM | 7.92 |