Assay Detail
Binding
CHEMBL5106948
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at androgen receptor (unknown origin) in human LNCap-ARR2PB-eGFP cells by measuring fluorescence intensity measured after 3 days by transcriptional assay
47
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | LNCaP |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of 2-(1-(3-Chloro-4-cyanophenyl)-1<i>H</i>-pyrazol-3-yl)acetamides as Potent, Selective, and Orally Available Antagonists Targeting the Androgen Receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 47 | 6.23 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1082407 | ENZALUTAMIDE | 4.0 | 1 | 7.60 |
| CHEMBL5206094 | — | — | 1 | 7.30 |
| CHEMBL5201101 | — | — | 1 | 7.16 |
| CHEMBL5175077 | — | — | 1 | 7.10 |
| CHEMBL5177079 | — | — | 1 | 6.92 |
| CHEMBL5203294 | — | — | 1 | 6.85 |
| CHEMBL5174154 | — | — | 1 | 6.77 |
| CHEMBL5188878 | — | — | 1 | 6.68 |
| CHEMBL5183890 | — | — | 1 | 6.66 |
| CHEMBL5200307 | — | — | 1 | 6.66 |
| CHEMBL5196306 | — | — | 1 | 6.52 |
| CHEMBL5185396 | — | — | 1 | 6.47 |
| CHEMBL5186580 | — | — | 1 | 6.47 |
| CHEMBL5185108 | — | — | 1 | 6.44 |
| CHEMBL5186217 | — | — | 1 | 6.35 |
| CHEMBL5182367 | — | — | 1 | 6.12 |
| CHEMBL5194539 | — | — | 1 | 6.11 |
| CHEMBL5194785 | — | — | 1 | 5.94 |
| CHEMBL5195872 | — | — | 1 | 5.73 |
| CHEMBL5208225 | — | — | 1 | 5.59 |
| CHEMBL5187028 | — | — | 1 | 5.34 |
| CHEMBL5201931 | — | — | 1 | 5.24 |
| CHEMBL5193409 | — | — | 1 | 5.20 |
| CHEMBL5197284 | — | — | 1 | 5.04 |
| CHEMBL5172818 | — | — | 1 | 4.83 |
| CHEMBL5194098 | — | — | 1 | 4.79 |
| CHEMBL5205113 | — | — | 1 | - |
| CHEMBL5191194 | — | — | 1 | - |
| CHEMBL5171887 | — | — | 1 | - |
| CHEMBL5176535 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1082407 | ENZALUTAMIDE | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5206094 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5201101 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL5175077 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL5177079 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5203294 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5174154 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL5188878 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL5183890 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL5200307 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL5196306 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL5185396 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL5186580 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL5185108 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL5186217 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL5182367 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL5194539 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL5194785 | — | IC50 | = | 1150.0 | nM | 5.94 |
| CHEMBL5195872 | — | IC50 | = | 1850.0 | nM | 5.73 |
| CHEMBL5208225 | — | IC50 | = | 2570.0 | nM | 5.59 |
| CHEMBL5187028 | — | IC50 | = | 4530.0 | nM | 5.34 |
| CHEMBL5201931 | — | IC50 | = | 5820.0 | nM | 5.24 |
| CHEMBL5193409 | — | IC50 | = | 6340.0 | nM | 5.20 |
| CHEMBL5197284 | — | IC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL5172818 | — | IC50 | = | 14900.0 | nM | 4.83 |
| CHEMBL5194098 | — | IC50 | = | 16240.0 | nM | 4.79 |
| CHEMBL5172944 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL5169354 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL5193077 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL5204961 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL5185081 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL5169913 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL5194465 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL5180473 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL5171911 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL5192790 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL5208207 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL5175229 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL5186400 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL5200523 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL5170285 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL5198604 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL5175232 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL5176535 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL5171887 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL5191194 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL5205113 | — | IC50 | > | 25000.0 | nM | - |