Assay Detail
Binding
CHEMBL4676574
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at recombinant human AR expressed in HEK293 cells assessed as inhibition of R1881-induced transcriptional activity measured after 24 hrs by dual luciferase reporter gene assay
50
Total Activities
50
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
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 |
|---|---|---|---|
| IC50 | 50 | 6.37 | 7.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4794467 | — | — | 1 | 7.46 |
| CHEMBL4753877 | — | — | 1 | 7.44 |
| CHEMBL4776248 | — | — | 1 | 7.35 |
| CHEMBL4778795 | — | — | 1 | 7.23 |
| CHEMBL4781335 | — | — | 1 | 7.21 |
| CHEMBL218490 | DORZOLAMIDE | 4.0 | 1 | 7.19 |
| CHEMBL4751646 | — | — | 1 | 7.15 |
| CHEMBL4746345 | — | — | 1 | 7.08 |
| CHEMBL4752991 | — | — | 1 | 6.87 |
| CHEMBL4757702 | — | — | 1 | 6.86 |
| CHEMBL3183409 | APALUTAMIDE | 4.0 | 1 | 6.80 |
| CHEMBL4739997 | — | — | 1 | 6.74 |
| CHEMBL4792938 | — | — | 1 | 6.72 |
| CHEMBL4783581 | — | — | 1 | 6.70 |
| CHEMBL4741569 | — | — | 1 | 6.69 |
| CHEMBL4790541 | — | — | 1 | 6.68 |
| CHEMBL1082407 | ENZALUTAMIDE | 4.0 | 1 | 6.67 |
| CHEMBL4740374 | — | — | 1 | 6.66 |
| CHEMBL4740742 | — | — | 1 | 6.61 |
| CHEMBL4794197 | — | — | 1 | 6.56 |
| CHEMBL4782992 | — | — | 1 | 6.54 |
| CHEMBL4752477 | — | — | 1 | 6.48 |
| CHEMBL4779527 | — | — | 1 | 6.37 |
| CHEMBL4797334 | — | — | 1 | 6.37 |
| CHEMBL4746960 | — | — | 1 | 6.33 |
| CHEMBL4758119 | — | — | 1 | 6.24 |
| CHEMBL4742694 | — | — | 1 | 6.12 |
| CHEMBL4741767 | — | — | 1 | 6.08 |
| CHEMBL4782924 | — | — | 1 | 6.04 |
| CHEMBL4746814 | — | — | 1 | 6.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4794467 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4753877 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4776248 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4778795 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL4781335 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL218490 | DORZOLAMIDE | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL4751646 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL4746345 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL4752991 | — | IC50 | = | 136.0 | nM | 6.87 |
| CHEMBL4757702 | — | IC50 | = | 138.0 | nM | 6.86 |
| CHEMBL3183409 | APALUTAMIDE | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4739997 | — | IC50 | = | 181.0 | nM | 6.74 |
| CHEMBL4792938 | — | IC50 | = | 192.0 | nM | 6.72 |
| CHEMBL4783581 | — | IC50 | = | 199.0 | nM | 6.70 |
| CHEMBL4741569 | — | IC50 | = | 205.0 | nM | 6.69 |
| CHEMBL4790541 | — | IC50 | = | 208.0 | nM | 6.68 |
| CHEMBL1082407 | ENZALUTAMIDE | IC50 | = | 216.0 | nM | 6.67 |
| CHEMBL4740374 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4740742 | — | IC50 | = | 248.0 | nM | 6.61 |
| CHEMBL4794197 | — | IC50 | = | 276.0 | nM | 6.56 |
| CHEMBL4782992 | — | IC50 | = | 285.0 | nM | 6.54 |
| CHEMBL4752477 | — | IC50 | = | 332.0 | nM | 6.48 |
| CHEMBL4779527 | — | IC50 | = | 427.0 | nM | 6.37 |
| CHEMBL4797334 | — | IC50 | = | 427.0 | nM | 6.37 |
| CHEMBL4746960 | — | IC50 | = | 462.0 | nM | 6.33 |
| CHEMBL4758119 | — | IC50 | = | 579.0 | nM | 6.24 |
| CHEMBL4742694 | — | IC50 | = | 758.0 | nM | 6.12 |
| CHEMBL4741767 | — | IC50 | = | 827.0 | nM | 6.08 |
| CHEMBL4782924 | — | IC50 | = | 901.0 | nM | 6.04 |
| CHEMBL4746814 | — | IC50 | = | 969.0 | nM | 6.01 |
| CHEMBL4793442 | — | IC50 | = | 1069.0 | nM | 5.97 |
| CHEMBL4800572 | — | IC50 | = | 1131.0 | nM | 5.95 |
| CHEMBL4752893 | — | IC50 | = | 1153.0 | nM | 5.94 |
| CHEMBL4758685 | — | IC50 | = | 1152.0 | nM | 5.94 |
| CHEMBL4779474 | — | IC50 | = | 1442.0 | nM | 5.84 |
| CHEMBL4798843 | — | IC50 | = | 2038.0 | nM | 5.69 |
| CHEMBL4747056 | — | IC50 | = | 2124.0 | nM | 5.67 |
| CHEMBL4741021 | — | IC50 | = | 2470.0 | nM | 5.61 |
| CHEMBL4778019 | — | IC50 | = | 4770.0 | nM | 5.32 |
| CHEMBL4784244 | — | IC50 | = | 5481.0 | nM | 5.26 |
| CHEMBL4800363 | — | IC50 | = | 5450.0 | nM | 5.26 |
| CHEMBL4776221 | — | IC50 | = | 6108.0 | nM | 5.21 |
| CHEMBL4747667 | — | IC50 | = | 8087.0 | nM | 5.09 |
| CHEMBL4787674 | — | IC50 | - | — | - | |
| CHEMBL4759376 | — | IC50 | - | — | - | |
| CHEMBL4750853 | — | IC50 | - | — | - | |
| CHEMBL4764521 | — | IC50 | - | — | - | |
| CHEMBL4775983 | — | IC50 | - | — | - | |
| CHEMBL4744252 | — | IC50 | - | — | - | |
| CHEMBL4777172 | — | IC50 | - | — | - |