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Assay Detail

CHEMBL3706299

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
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
(2015)

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