Assay Detail
Binding
CHEMBL805444
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibition of human steroid 5-alpha-reductase type I in Du-145 cells
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | DU-145 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
3-oxo-5-alpha-steroid 4-dehydrogenase 1 (CHEMBL1787) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and in vitro activity of 17 beta-(N-alkyl/arylformamido)- and 17 beta-[(N-alkyl/aryl)alkyl/arylamido]-4-methyl-4-aza-3-oxo-5 alpha-androstan-3-ones as inhibitors of human 5 alpha-reductases and antagonists of the androgen receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 8.02 | 9.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL275153 | — | — | 1 | 9.04 |
| CHEMBL280015 | — | — | 1 | 8.75 |
| CHEMBL17245 | — | — | 1 | 8.68 |
| CHEMBL17222 | — | — | 1 | 8.66 |
| CHEMBL16863 | — | — | 1 | 8.63 |
| CHEMBL274269 | — | — | 1 | 8.62 |
| CHEMBL276320 | — | — | 1 | 8.53 |
| CHEMBL277053 | — | — | 1 | 8.52 |
| CHEMBL16784 | — | — | 1 | 8.49 |
| CHEMBL278490 | — | — | 1 | 8.48 |
| CHEMBL2298601 | — | — | 1 | 8.38 |
| CHEMBL17194 | — | — | 1 | 8.34 |
| CHEMBL274276 | — | — | 1 | 8.29 |
| CHEMBL16700 | — | — | 1 | 8.26 |
| CHEMBL276527 | — | — | 1 | 8.25 |
| CHEMBL17506 | — | — | 1 | 8.14 |
| CHEMBL16690 | — | — | 1 | 8.14 |
| CHEMBL17206 | — | — | 1 | 8.02 |
| CHEMBL17268 | — | — | 1 | 8.02 |
| CHEMBL266519 | — | — | 1 | 7.98 |
| CHEMBL16533 | — | — | 1 | 7.97 |
| CHEMBL276355 | — | — | 1 | 7.95 |
| CHEMBL17514 | — | — | 1 | 7.93 |
| CHEMBL16927 | — | — | 1 | 7.92 |
| CHEMBL417627 | — | — | 1 | 7.77 |
| CHEMBL710 | FINASTERIDE | 4.0 | 1 | 7.58 |
| CHEMBL17193 | — | — | 1 | 7.54 |
| CHEMBL17473 | — | — | 1 | 7.48 |
| CHEMBL17422 | — | — | 1 | 7.22 |
| CHEMBL443995 | — | — | 1 | 5.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL275153 | — | IC50 | = | 0.91 | nM | 9.04 |
| CHEMBL280015 | — | IC50 | = | 1.77 | nM | 8.75 |
| CHEMBL17245 | — | IC50 | = | 2.11 | nM | 8.68 |
| CHEMBL17222 | — | IC50 | = | 2.19 | nM | 8.66 |
| CHEMBL16863 | — | IC50 | = | 2.35 | nM | 8.63 |
| CHEMBL274269 | — | IC50 | = | 2.42 | nM | 8.62 |
| CHEMBL276320 | — | IC50 | = | 2.93 | nM | 8.53 |
| CHEMBL277053 | — | IC50 | = | 3.05 | nM | 8.52 |
| CHEMBL16784 | — | IC50 | = | 3.22 | nM | 8.49 |
| CHEMBL278490 | — | IC50 | = | 3.31 | nM | 8.48 |
| CHEMBL2298601 | — | IC50 | = | 4.14 | nM | 8.38 |
| CHEMBL17194 | — | IC50 | = | 4.56 | nM | 8.34 |
| CHEMBL274276 | — | IC50 | = | 5.08 | nM | 8.29 |
| CHEMBL16700 | — | IC50 | = | 5.44 | nM | 8.26 |
| CHEMBL276527 | — | IC50 | = | 5.63 | nM | 8.25 |
| CHEMBL16690 | — | IC50 | = | 7.31 | nM | 8.14 |
| CHEMBL17506 | — | IC50 | = | 7.25 | nM | 8.14 |
| CHEMBL17206 | — | IC50 | = | 9.57 | nM | 8.02 |
| CHEMBL17268 | — | IC50 | = | 9.53 | nM | 8.02 |
| CHEMBL266519 | — | IC50 | = | 10.5 | nM | 7.98 |
| CHEMBL16533 | — | IC50 | = | 10.6 | nM | 7.97 |
| CHEMBL276355 | — | IC50 | = | 11.2 | nM | 7.95 |
| CHEMBL17514 | — | IC50 | = | 11.8 | nM | 7.93 |
| CHEMBL16927 | — | IC50 | = | 11.9 | nM | 7.92 |
| CHEMBL417627 | — | IC50 | = | 16.9 | nM | 7.77 |
| CHEMBL710 | FINASTERIDE | IC50 | = | 26.3 | nM | 7.58 |
| CHEMBL17193 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL17473 | — | IC50 | = | 32.8 | nM | 7.48 |
| CHEMBL17422 | — | IC50 | = | 59.8 | nM | 7.22 |
| CHEMBL443995 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL16743 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL17025 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL277563 | — | IC50 | > | 100.0 | nM | - |