Assay Detail
Functional
CHEMBL1013144
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at wild type human recombinant androgen receptor assessed as inhibition of testosterone-induced growth of mouse androgen dependent SC3 cells by WST-1 method
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | SC-3 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
4-(Anilino)pyrrole-2-carboxamides: Novel non-steroidal/non-anilide type androgen antagonists effective upon human prostate tumor LNCaP cells with mutated nuclear androgen receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 5.51 | 6.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL63560 | (R)-BICALUTAMIDE | — | 1 | 6.57 |
| CHEMBL491 | HYDROXYFLUTAMIDE | 2.0 | 1 | 6.46 |
| CHEMBL480182 | — | — | 1 | 6.40 |
| CHEMBL518945 | — | — | 1 | 6.36 |
| CHEMBL480982 | — | — | 1 | 6.22 |
| CHEMBL480955 | — | — | 1 | 6.21 |
| CHEMBL519780 | — | — | 1 | 6.06 |
| CHEMBL521251 | — | — | 1 | 6.02 |
| CHEMBL503676 | — | — | 1 | 6.00 |
| CHEMBL481139 | — | — | 1 | 6.00 |
| CHEMBL520428 | — | — | 1 | 5.77 |
| CHEMBL521249 | — | — | 1 | 5.77 |
| CHEMBL480162 | — | — | 1 | 5.71 |
| CHEMBL479988 | — | — | 1 | 5.70 |
| CHEMBL480960 | — | — | 1 | 5.68 |
| CHEMBL481924 | — | — | 1 | 5.60 |
| CHEMBL482063 | — | — | 1 | 5.43 |
| CHEMBL481107 | — | — | 1 | 5.40 |
| CHEMBL806 | FLUTAMIDE | 4.0 | 1 | 5.38 |
| CHEMBL481939 | — | — | 1 | 5.33 |
| CHEMBL480934 | — | — | 1 | 5.32 |
| CHEMBL482064 | — | — | 1 | 5.31 |
| CHEMBL481746 | — | — | 1 | 5.26 |
| CHEMBL481686 | — | — | 1 | 5.24 |
| CHEMBL480959 | — | — | 1 | 5.21 |
| CHEMBL519112 | — | — | 1 | 5.21 |
| CHEMBL481302 | — | — | 1 | 5.21 |
| CHEMBL481515 | — | — | 1 | 5.18 |
| CHEMBL516752 | — | — | 1 | 5.00 |
| CHEMBL519292 | — | — | 1 | 4.86 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL63560 | (R)-BICALUTAMIDE | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL491 | HYDROXYFLUTAMIDE | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL480182 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL518945 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL480982 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL480955 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL519780 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL521251 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL503676 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL481139 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL520428 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL521249 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL480162 | — | IC50 | = | 1950.0 | nM | 5.71 |
| CHEMBL479988 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL480960 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL481924 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL482063 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL481107 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL806 | FLUTAMIDE | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL481939 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL480934 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL482064 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL481746 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL481686 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL480959 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL519112 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL481302 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL481515 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL516752 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL519292 | — | IC50 | = | 13700.0 | nM | 4.86 |
| CHEMBL481356 | — | IC50 | = | 14500.0 | nM | 4.84 |
| CHEMBL516610 | — | IC50 | = | 14700.0 | nM | 4.83 |
| CHEMBL444991 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL481355 | — | IC50 | = | 15500.0 | nM | 4.81 |
| CHEMBL481152 | — | IC50 | = | 22500.0 | nM | 4.65 |
| CHEMBL480183 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL481350 | — | IC50 | > | 30000.0 | nM | - |