Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL816487

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

Binding
Inhibition of type 1 steroid-5-alpha-reductase
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

4,7 beta-Dimethyl-4-azacholestan-3-one (MK-386) and related 4-azasteroids as selective inhibitors of human type 1 5 alpha-reductase.
Bakshi RK, Patel GF, Rasmusson GH, Baginsky WF, Cimis G, Ellsworth K, Chang B, Bull H, Tolman RL, Harris GS.
J Med Chem (1994) 37 : 3871 -3874
PubMed 7966146 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 8.14 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL421627 1 9.22
CHEMBL25448 1 9.05
CHEMBL126686 1 8.80
CHEMBL340027 1 8.77
CHEMBL128023 1 8.70
CHEMBL338376 1 8.60
CHEMBL340715 1 8.59
CHEMBL340181 1 8.59
CHEMBL340684 1 8.57
CHEMBL340305 1 8.48
CHEMBL125855 1 8.37
CHEMBL338207 1 8.30
CHEMBL127702 1 8.24
CHEMBL125209 1 8.08
CHEMBL332781 1 8.07
CHEMBL24955 BEXLOSTERIDE 2.0 1 8.07
CHEMBL414427 1 8.02
CHEMBL125260 1 8.02
CHEMBL338707 1 7.72
CHEMBL126968 1 7.70
CHEMBL127760 1 7.38
CHEMBL710 FINASTERIDE 4.0 1 7.28
CHEMBL124750 1 7.24
CHEMBL339912 1 6.87
CHEMBL323996 1 6.73
CHEMBL124803 1 -
CHEMBL414428 1 -
CHEMBL125579 1 -
CHEMBL138225 EPRISTERIDE 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL421627 IC50 = 0.6 nM 9.22
CHEMBL25448 IC50 = 0.9 nM 9.05
CHEMBL126686 IC50 = 1.6 nM 8.80
CHEMBL340027 IC50 = 1.7 nM 8.77
CHEMBL128023 IC50 = 2.0 nM 8.70
CHEMBL338376 IC50 = 2.5 nM 8.60
CHEMBL340715 IC50 = 2.6 nM 8.59
CHEMBL340181 IC50 = 2.6 nM 8.59
CHEMBL340684 IC50 = 2.7 nM 8.57
CHEMBL340305 IC50 = 3.3 nM 8.48
CHEMBL125855 IC50 = 4.3 nM 8.37
CHEMBL338207 IC50 = 5.0 nM 8.30
CHEMBL127702 IC50 = 5.7 nM 8.24
CHEMBL125209 IC50 = 8.4 nM 8.08
CHEMBL332781 IC50 = 8.6 nM 8.07
CHEMBL24955 BEXLOSTERIDE IC50 = 8.6 nM 8.07
CHEMBL414427 IC50 = 9.5 nM 8.02
CHEMBL125260 IC50 = 9.5 nM 8.02
CHEMBL338707 IC50 = 19.1 nM 7.72
CHEMBL126968 IC50 = 20.0 nM 7.70
CHEMBL127760 IC50 = 42.0 nM 7.38
CHEMBL710 FINASTERIDE IC50 = 52.0 nM 7.28
CHEMBL124750 IC50 = 58.0 nM 7.24
CHEMBL339912 IC50 = 134.0 nM 6.87
CHEMBL323996 IC50 = 186.0 nM 6.73
CHEMBL124803 IC50 > 1000.0 nM -
CHEMBL414428 IC50 > 1000.0 nM -
CHEMBL125579 IC50 > 1000.0 nM -
CHEMBL138225 EPRISTERIDE IC50 > 1000.0 nM -