Assay Detail
Binding
CHEMBL649835
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Binding Affinity towards Rat Androgen Receptor was determined using [3H]- mibolerone as radioligand.
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Chiral nonsteroidal affinity ligands for the androgen receptor. 1. Bicalutamide analogues bearing electrophilic groups in the B aromatic ring.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 7.17 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1744065 | — | — | 1 | 9.22 |
| CHEMBL333745 | — | — | 1 | 8.78 |
| CHEMBL125425 | — | — | 1 | 7.97 |
| CHEMBL63560 | (R)-BICALUTAMIDE | — | 1 | 7.96 |
| CHEMBL178599 | — | — | 1 | 7.39 |
| CHEMBL424787 | — | — | 1 | 7.19 |
| CHEMBL340668 | — | — | 1 | 7.05 |
| CHEMBL125649 | — | — | 1 | 7.00 |
| CHEMBL442019 | — | — | 1 | 6.89 |
| CHEMBL121992 | — | — | 1 | 6.89 |
| CHEMBL433754 | — | — | 1 | 6.85 |
| CHEMBL123673 | — | — | 1 | 6.70 |
| CHEMBL121783 | — | — | 1 | 6.64 |
| CHEMBL124881 | (S)-BICALUTAMIDE | — | 1 | 6.44 |
| CHEMBL360058 | — | — | 1 | 6.44 |
| CHEMBL178788 | — | — | 1 | 6.37 |
| CHEMBL341272 | — | — | 1 | 6.10 |
| CHEMBL1744064 | — | — | 1 | - |
| CHEMBL125562 | — | — | 1 | - |
| CHEMBL1744063 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1744065 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL333745 | — | Ki | = | 1.65 | nM | 8.78 |
| CHEMBL125425 | — | Ki | = | 10.7 | nM | 7.97 |
| CHEMBL63560 | (R)-BICALUTAMIDE | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL178599 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL424787 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL340668 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL125649 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL442019 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL121992 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL433754 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL123673 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL121783 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL124881 | (S)-BICALUTAMIDE | Ki | = | 365.0 | nM | 6.44 |
| CHEMBL360058 | — | Ki | = | 360.0 | nM | 6.44 |
| CHEMBL178788 | — | Ki | = | 430.0 | nM | 6.37 |
| CHEMBL341272 | — | Ki | = | 800.0 | nM | 6.10 |
| CHEMBL1744064 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL125562 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1744063 | — | Ki | > | 1000.0 | nM | - |