Assay Detail
Binding
CHEMBL5729815
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding Assay: The competition assay was performed in a 96-well plate (polystyrene*) which binds <2.0% of the total input [3H]-17beta-estradiol and each data point was gathered in triplicate. 100 uG/100 uL of the receptor preparation was aliquoted per well. A saturating dose of 2.5 nM [3H]17beta-estradiol+competitor (or buffer) in a 50 uL volume was added in the preliminary competition when 100x and 500x competitor were evaluated, only 0.8 nM [3H]17beta-estradiol was used. The plate was incubated at room temperature for 2.5 h. At the end of this incubation period 150 uL of ice-cold dextran coated charcoal (5% activated charcoal coated with 0.05% 69K dextran) was added to each well and the plate was immediately centrifuged at 99 g for 5 minutes at 4 C. 200 uL of the supernatant solution was then removed for scintillation counting. Samples were counted to 2% or 10 minutes, whichever occurs first.
162
Total Activities
53
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole and estrogen formulations
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 54 | 7.23 | 9.00 |
| kon | 54 | - | - |
| k_off | 54 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3657181 | — | — | 3 | 9.00 |
| CHEMBL3657166 | — | — | 3 | 8.40 |
| CHEMBL3657162 | — | — | 3 | 8.26 |
| CHEMBL3657161 | — | — | 3 | 8.05 |
| CHEMBL3657171 | — | — | 3 | 7.96 |
| CHEMBL3657163 | — | — | 3 | 7.89 |
| CHEMBL3657169 | — | — | 3 | 7.89 |
| CHEMBL3657160 | — | — | 3 | 7.72 |
| CHEMBL3657149 | — | — | 3 | 7.70 |
| CHEMBL3657172 | — | — | 3 | 7.64 |
| CHEMBL3657167 | — | — | 3 | 7.62 |
| CHEMBL3657148 | — | — | 3 | 7.55 |
| CHEMBL3657168 | — | — | 3 | 7.54 |
| CHEMBL3657136 | — | — | 3 | 7.52 |
| CHEMBL3657144 | — | — | 3 | 7.52 |
| CHEMBL3657151 | — | — | 3 | 7.43 |
| CHEMBL3657155 | — | — | 3 | 7.40 |
| CHEMBL3657178 | — | — | 3 | 7.40 |
| CHEMBL3657153 | — | — | 3 | 7.33 |
| CHEMBL46740 | BAZEDOXIFENE | 4.0 | 3 | 7.30 |
| CHEMBL3657165 | — | — | 3 | 7.30 |
| CHEMBL3657175 | — | — | 3 | 7.24 |
| CHEMBL3657177 | — | — | 3 | 7.22 |
| CHEMBL44426 | PIPENDOXIFENE | 2.0 | 6 | 7.22 |
| CHEMBL3657141 | — | — | 3 | 7.21 |
| CHEMBL3657180 | — | — | 3 | 7.16 |
| CHEMBL3657184 | — | — | 3 | 7.16 |
| CHEMBL3657145 | — | — | 3 | 7.10 |
| CHEMBL3657185 | — | — | 3 | 7.10 |
| CHEMBL3657174 | — | — | 3 | 7.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3657181 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3657166 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3657162 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL3657161 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3657171 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3657163 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3657169 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3657160 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3657149 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3657172 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3657167 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3657148 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3657168 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3657144 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3657136 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3657151 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3657155 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3657178 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3657153 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL3657165 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL46740 | BAZEDOXIFENE | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3657175 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL44426 | PIPENDOXIFENE | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3657177 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL44426 | PIPENDOXIFENE | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3657141 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL3657180 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3657184 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3657174 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3657145 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3657185 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3657156 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3657142 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL3657154 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3705039 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3657173 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL3657147 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3657183 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3657158 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3657159 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3657164 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3657135 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3657182 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3657152 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3657170 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3657157 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3657150 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3657143 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3657146 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3657138 | — | IC50 | = | 300.0 | nM | 6.52 |