Assay Detail
Binding
CHEMBL4676575
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-MIB from wild-type rat AR LBD measured after 16 hrs by scintillation counting method
43
Total Activities
43
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Pyrazol-1-yl-propanamides as SARD and Pan-Antagonists for the Treatment of Enzalutamide-Resistant Prostate Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 42 | 6.07 | 7.96 |
| IC50 | 1 | 9.00 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL27769 | STANOLONE | 2.0 | 1 | 9.00 |
| CHEMBL218490 | DORZOLAMIDE | 4.0 | 1 | 7.96 |
| CHEMBL4778795 | — | — | 1 | 7.05 |
| CHEMBL4739997 | — | — | 1 | 6.70 |
| CHEMBL4777131 | — | — | 1 | 6.65 |
| CHEMBL4740742 | — | — | 1 | 6.29 |
| CHEMBL4741569 | — | — | 1 | 6.29 |
| CHEMBL4794467 | — | — | 1 | 6.25 |
| CHEMBL4782992 | — | — | 1 | 6.22 |
| CHEMBL4746345 | — | — | 1 | 6.22 |
| CHEMBL4746814 | — | — | 1 | 6.21 |
| CHEMBL4740374 | — | — | 1 | 6.09 |
| CHEMBL4751646 | — | — | 1 | 6.05 |
| CHEMBL4742694 | — | — | 1 | 5.98 |
| CHEMBL4752477 | — | — | 1 | 5.87 |
| CHEMBL4752893 | — | — | 1 | 5.86 |
| CHEMBL3183409 | APALUTAMIDE | 4.0 | 1 | 5.84 |
| CHEMBL4776248 | — | — | 1 | 5.82 |
| CHEMBL4747667 | — | — | 1 | 5.81 |
| CHEMBL4753877 | — | — | 1 | 5.65 |
| CHEMBL4790541 | — | — | 1 | 5.64 |
| CHEMBL1082407 | ENZALUTAMIDE | 4.0 | 1 | 5.44 |
| CHEMBL4778019 | — | — | 1 | 5.44 |
| CHEMBL4757702 | — | — | 1 | 5.31 |
| CHEMBL4779474 | — | — | 1 | 5.13 |
| CHEMBL4741767 | — | — | 1 | - |
| CHEMBL4797334 | — | — | 1 | - |
| CHEMBL4752991 | — | — | 1 | - |
| CHEMBL4783581 | — | — | 1 | - |
| CHEMBL4758685 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL27769 | STANOLONE | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL218490 | DORZOLAMIDE | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL4778795 | — | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL4739997 | — | Ki | = | 202.0 | nM | 6.70 |
| CHEMBL4777131 | — | Ki | = | 223.0 | nM | 6.65 |
| CHEMBL4740742 | — | Ki | = | 509.0 | nM | 6.29 |
| CHEMBL4741569 | — | Ki | = | 512.0 | nM | 6.29 |
| CHEMBL4794467 | — | Ki | = | 567.0 | nM | 6.25 |
| CHEMBL4782992 | — | Ki | = | 601.0 | nM | 6.22 |
| CHEMBL4746345 | — | Ki | = | 607.0 | nM | 6.22 |
| CHEMBL4746814 | — | Ki | = | 612.0 | nM | 6.21 |
| CHEMBL4740374 | — | Ki | = | 821.0 | nM | 6.09 |
| CHEMBL4751646 | — | Ki | = | 898.0 | nM | 6.05 |
| CHEMBL4742694 | — | Ki | = | 1056.0 | nM | 5.98 |
| CHEMBL4752477 | — | Ki | = | 1345.0 | nM | 5.87 |
| CHEMBL4752893 | — | Ki | = | 1382.0 | nM | 5.86 |
| CHEMBL3183409 | APALUTAMIDE | Ki | = | 1452.0 | nM | 5.84 |
| CHEMBL4776248 | — | Ki | = | 1499.0 | nM | 5.82 |
| CHEMBL4747667 | — | Ki | = | 1552.0 | nM | 5.81 |
| CHEMBL4753877 | — | Ki | = | 2225.0 | nM | 5.65 |
| CHEMBL4790541 | — | Ki | = | 2286.0 | nM | 5.64 |
| CHEMBL1082407 | ENZALUTAMIDE | Ki | = | 3641.0 | nM | 5.44 |
| CHEMBL4778019 | — | Ki | = | 3660.0 | nM | 5.44 |
| CHEMBL4757702 | — | Ki | = | 4935.0 | nM | 5.31 |
| CHEMBL4779474 | — | Ki | = | 7398.0 | nM | 5.13 |
| CHEMBL4747056 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4746960 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4792938 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4759376 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4787674 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4779527 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4776221 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4781335 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4782924 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4764521 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4775983 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4750853 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4793442 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4758685 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4783581 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4752991 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4797334 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4741767 | — | Ki | > | 10000.0 | nM | - |