Assay Detail
Functional
CHEMBL1960485
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at androgen receptor T877A mutant expressed in Cos7 cells assessed as inhibition of dihydrotestosterone-induced luciferase activity after 24 hrs by reporter gene assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | COS-7 |
| 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 | 6.35 | 6.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1957622 | — | — | 1 | 6.96 |
| CHEMBL1957615 | — | — | 1 | 6.96 |
| CHEMBL1957617 | — | — | 1 | 6.85 |
| CHEMBL1957621 | — | — | 1 | 6.85 |
| CHEMBL1957611 | — | — | 1 | 6.77 |
| CHEMBL1957610 | — | — | 1 | 6.75 |
| CHEMBL1957618 | — | — | 1 | 6.75 |
| CHEMBL1957725 | — | — | 1 | 6.72 |
| CHEMBL1957616 | — | — | 1 | 6.57 |
| CHEMBL1957726 | — | — | 1 | 6.46 |
| CHEMBL409 | BICALUTAMIDE | 4.0 | 1 | 6.33 |
| CHEMBL1957723 | — | — | 1 | 6.14 |
| CHEMBL1957607 | — | — | 1 | 6.11 |
| CHEMBL1957614 | — | — | 1 | 6.09 |
| CHEMBL1957608 | — | — | 1 | 5.96 |
| CHEMBL1957724 | — | — | 1 | 5.80 |
| CHEMBL1957620 | — | — | 1 | 5.72 |
| CHEMBL1957722 | — | — | 1 | 5.68 |
| CHEMBL1957721 | — | — | 1 | 5.20 |
| CHEMBL1957619 | — | — | 1 | - |
| CHEMBL1957609 | — | — | 1 | - |
| CHEMBL1957613 | — | — | 1 | - |
| CHEMBL1957612 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1957622 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1957615 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1957617 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL1957621 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL1957611 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL1957610 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL1957618 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL1957725 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL1957616 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL1957726 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL409 | BICALUTAMIDE | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL1957723 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL1957607 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL1957614 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL1957608 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1957724 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL1957620 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL1957722 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL1957721 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL1957619 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1957609 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1957613 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1957612 | — | IC50 | > | 10000.0 | nM | - |