Assay Detail
Binding
CHEMBL4820469
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at VP16-AR F877L mutant (unknown origin) transfected in human HepG2 cells cotransfected with ARE-LUC incubated for 48 hrs by steady-glo luciferase reporter gene assay
10
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HepG2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of JNJ-63576253: A Clinical Stage Androgen Receptor Antagonist for F877L Mutant and Wild-Type Castration-Resistant Prostate Cancer (mCRPC).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 9 | 6.71 | 7.35 |
| Activity | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4862827 | — | — | 1 | 7.35 |
| CHEMBL1082407 | ENZALUTAMIDE | 4.0 | 2 | 7.21 |
| CHEMBL4869652 | — | — | 1 | 6.19 |
| CHEMBL4860547 | — | — | 1 | 6.08 |
| CHEMBL4865865 | — | — | 1 | - |
| CHEMBL4858811 | TRC-253 | 1.0 | 1 | - |
| CHEMBL4876579 | — | — | 1 | - |
| CHEMBL4879319 | — | — | 1 | - |
| CHEMBL4849570 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4862827 | — | EC50 | = | 45.0 | nM | 7.35 |
| CHEMBL1082407 | ENZALUTAMIDE | EC50 | = | 61.8 | nM | 7.21 |
| CHEMBL4869652 | — | EC50 | = | 649.0 | nM | 6.19 |
| CHEMBL4860547 | — | EC50 | = | 838.0 | nM | 6.08 |
| CHEMBL4865865 | — | EC50 | - | — | - | |
| CHEMBL1082407 | ENZALUTAMIDE | Activity | - | — | - | |
| CHEMBL4858811 | TRC-253 | EC50 | - | — | - | |
| CHEMBL4876579 | — | EC50 | - | — | - | |
| CHEMBL4879319 | — | EC50 | - | — | - | |
| CHEMBL4849570 | — | EC50 | - | — | - |