Assay Detail
Binding
CHEMBL4411916
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Antagonist activity at human androgen receptor expressed in HEK293 cells assessed as inhibition of R1881-induced receptor transactivation after 24 hrs by luciferase reporter gene assay
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
New Generation of Selective Androgen Receptor Degraders: Our Initial Design, Synthesis, and Biological Evaluation of New Compounds with Enzalutamide-Resistant Prostate Cancer Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 41 | 6.82 | 8.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1738889 | ENOBOSARM | 3.0 | 1 | 8.42 |
| CHEMBL3183409 | APALUTAMIDE | 4.0 | 1 | 7.80 |
| CHEMBL4521365 | — | — | 1 | 7.50 |
| CHEMBL4527176 | — | — | 1 | 7.43 |
| CHEMBL4436972 | — | — | 1 | 7.41 |
| CHEMBL4567476 | — | — | 1 | 7.35 |
| CHEMBL4584527 | — | — | 1 | 7.32 |
| CHEMBL4554646 | — | — | 1 | 7.24 |
| CHEMBL4438211 | — | — | 1 | 7.23 |
| CHEMBL4446471 | — | — | 1 | 7.19 |
| CHEMBL4444904 | — | — | 1 | 7.07 |
| CHEMBL4474096 | — | — | 1 | 7.07 |
| CHEMBL4586748 | — | — | 1 | 7.06 |
| CHEMBL4474118 | — | — | 1 | 7.03 |
| CHEMBL4590504 | — | — | 1 | 7.00 |
| CHEMBL4469605 | — | — | 1 | 7.00 |
| CHEMBL4527241 | — | — | 1 | 6.90 |
| CHEMBL4456765 | — | — | 1 | 6.90 |
| CHEMBL4542153 | — | — | 1 | 6.89 |
| CHEMBL4443566 | — | — | 1 | 6.85 |
| CHEMBL4483663 | — | — | 1 | 6.85 |
| CHEMBL4442857 | — | — | 1 | 6.80 |
| CHEMBL4447959 | — | — | 1 | 6.69 |
| CHEMBL1082407 | ENZALUTAMIDE | 4.0 | 1 | 6.67 |
| CHEMBL4460567 | — | — | 1 | 6.67 |
| CHEMBL4585987 | — | — | 1 | 6.63 |
| CHEMBL63560 | (R)-BICALUTAMIDE | — | 1 | 6.61 |
| CHEMBL4539953 | — | — | 1 | 6.61 |
| CHEMBL4571680 | — | — | 1 | 6.41 |
| CHEMBL4475765 | — | — | 1 | 6.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1738889 | ENOBOSARM | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL3183409 | APALUTAMIDE | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4521365 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4527176 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL4436972 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4567476 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4584527 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4554646 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL4438211 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL4446471 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL4474096 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL4444904 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL4586748 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL4474118 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL4469605 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL4590504 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL4527241 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL4456765 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL4542153 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4483663 | — | IC50 | = | 142.0 | nM | 6.85 |
| CHEMBL4443566 | — | IC50 | = | 142.0 | nM | 6.85 |
| CHEMBL4442857 | — | IC50 | = | 157.0 | nM | 6.80 |
| CHEMBL4447959 | — | IC50 | = | 203.0 | nM | 6.69 |
| CHEMBL1082407 | ENZALUTAMIDE | IC50 | = | 216.0 | nM | 6.67 |
| CHEMBL4460567 | — | IC50 | = | 215.0 | nM | 6.67 |
| CHEMBL4585987 | — | IC50 | = | 234.0 | nM | 6.63 |
| CHEMBL63560 | (R)-BICALUTAMIDE | IC50 | = | 248.0 | nM | 6.61 |
| CHEMBL4539953 | — | IC50 | = | 244.0 | nM | 6.61 |
| CHEMBL4571680 | — | IC50 | = | 392.0 | nM | 6.41 |
| CHEMBL4475765 | — | IC50 | = | 598.0 | nM | 6.22 |
| CHEMBL4583465 | — | IC50 | = | 686.0 | nM | 6.16 |
| CHEMBL4449952 | — | IC50 | = | 835.0 | nM | 6.08 |
| CHEMBL4475563 | — | IC50 | = | 898.0 | nM | 6.05 |
| CHEMBL4456781 | — | IC50 | = | 918.0 | nM | 6.04 |
| CHEMBL4542693 | — | IC50 | = | 985.0 | nM | 6.01 |
| CHEMBL4448937 | — | IC50 | = | 972.0 | nM | 6.01 |
| CHEMBL4520679 | — | IC50 | = | 1015.0 | nM | 5.99 |
| CHEMBL4451795 | — | IC50 | = | 1032.0 | nM | 5.99 |
| CHEMBL4588751 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4439702 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4439316 | — | IC50 | > | 10000.0 | nM | - |