Assay Detail
Binding
CHEMBL2329799
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at androgen receptor (unknown origin) expressed in HeLa cells co-expressing PSA-(ARE)4-Luc13 assessed as induction of DHT-induced luciferase activity after 20 mins by luciferase reporter gene assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Development of potent and selective indomethacin analogues for the inhibition of AKR1C3 (Type 5 17β-hydroxysteroid dehydrogenase/prostaglandin F synthase) in castrate-resistant prostate cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 4 | 9.88 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2323490 | — | — | 1 | 10.00 |
| CHEMBL6 | INDOMETHACIN | 4.0 | 1 | 9.85 |
| CHEMBL2323511 | — | — | 1 | 9.85 |
| CHEMBL2323507 | — | — | 1 | 9.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2323490 | — | EC50 | = | 0.1 | nM | 10.00 |
| CHEMBL6 | INDOMETHACIN | EC50 | = | 0.14 | nM | 9.85 |
| CHEMBL2323511 | — | EC50 | = | 0.14 | nM | 9.85 |
| CHEMBL2323507 | — | EC50 | = | 0.15 | nM | 9.82 |