Assay Detail
Binding
CHEMBL3706299
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In Vitro Inhibition Assay: This work was performed at the MDS Pharma Services, Pharmacology Laboratories, Taiwan. The assay was an in vitro evaluation of the ability of an extract or a pure compound to inhibit the steroid 5alpha -reductase enzyme from metabolizing testosterone into dihydrotestosterone. This is an enzyme-immunoassay (EIA) for quantitative determination of testosterone in human serum or plasma. The significance of this type of inhibition is that it can lead to eradication of benign prostatic hyperplasia (BPH). Two distinct isozymes are found in mice, rats, monkeys and humans: type 1 and II. Each of these isozymes is differentially expressed in tissues and developmental stages. In human, type 1 steroid 5alpha -reductase is predominant in the sebaceous glands of most regions of skin, including scalp and liver and is responsible for approximately one third of circulating DHT. Inhibitors of steroid 5alpha -reductase may be of benefit in the treatment of androgenetic alopecia.
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Sebaceous gland |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
3-oxo-5-alpha-steroid 4-dehydrogenase 2 (CHEMBL1856) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Management and treatment of benign prostatic hyperplasia
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 6.23 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL710 | FINASTERIDE | 4.0 | 1 | 7.60 |
| CHEMBL464982 | GAMOLENIC ACID | 3.0 | 1 | 4.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL710 | FINASTERIDE | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL464982 | GAMOLENIC ACID | IC50 | = | 14000.0 | nM | 4.85 |