Assay Detail
Binding
CHEMBL1960482
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Displacement of [17-alpha-methyl-3H]mibolerone from androgen receptor expressed in HEK293 cells after 3 hrs
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis, and biological evaluation of 4-arylmethyl-1-phenylpyrazole and 4-aryloxy-1-phenylpyrazole derivatives as novel androgen receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 6.75 | 9.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1957612 | — | — | 1 | 9.33 |
| CHEMBL1957613 | — | — | 1 | 8.85 |
| CHEMBL1957621 | — | — | 1 | 7.80 |
| CHEMBL1957618 | — | — | 1 | 7.58 |
| CHEMBL1957622 | — | — | 1 | 7.57 |
| CHEMBL1957617 | — | — | 1 | 7.28 |
| CHEMBL409 | BICALUTAMIDE | 4.0 | 1 | 7.27 |
| CHEMBL1957611 | — | — | 1 | 7.04 |
| CHEMBL1957615 | — | — | 1 | 6.96 |
| CHEMBL1957607 | — | — | 1 | 6.96 |
| CHEMBL1957722 | — | — | 1 | 6.80 |
| CHEMBL1957616 | — | — | 1 | 6.75 |
| CHEMBL1957620 | — | — | 1 | 6.58 |
| CHEMBL1957608 | — | — | 1 | 6.47 |
| CHEMBL1957609 | — | — | 1 | 6.29 |
| CHEMBL1957721 | — | — | 1 | 6.04 |
| CHEMBL1957610 | — | — | 1 | 5.96 |
| CHEMBL1957726 | — | — | 1 | 5.92 |
| CHEMBL1957723 | — | — | 1 | 5.89 |
| CHEMBL1957614 | — | — | 1 | 5.82 |
| CHEMBL1957619 | — | — | 1 | 5.38 |
| CHEMBL1957725 | — | — | 1 | 5.37 |
| CHEMBL1957724 | — | — | 1 | 5.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1957612 | — | IC50 | = | 0.47 | nM | 9.33 |
| CHEMBL1957613 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL1957621 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1957618 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL1957622 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL1957617 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL409 | BICALUTAMIDE | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL1957611 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL1957615 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1957607 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1957722 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL1957616 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL1957620 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL1957608 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL1957609 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL1957721 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL1957610 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1957726 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL1957723 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL1957614 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL1957619 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL1957725 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL1957724 | — | IC50 | = | 5400.0 | nM | 5.27 |