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Assay Detail

CHEMBL873205

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

Binding
Inhibition of recombinant human 5-alpha reductase-2 at a concentration of 5 microL after pre-incubation for 10 minutes
23
Total Activities
23
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 2 (CHEMBL1856)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

6-Azasteroids: potent dual inhibitors of human type 1 and 2 steroid 5 alpha-reductase.
Frye SV, Haffner CD, Maloney PR, Mook RA, Dorsey GF, Hiner RN, Batchelor KW, Bramson HN, Stuart JD, Schweiker SL.
J Med Chem (1993) 36 : 4313 -4315
PubMed 8277514 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 9.20 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL138173 1 10.40
CHEMBL137733 1 10.15
CHEMBL420020 1 10.10
CHEMBL24088 1 10.05
CHEMBL308258 1 10.05
CHEMBL412425 1 9.92
CHEMBL436215 1 9.89
CHEMBL306722 1 9.80
CHEMBL710 FINASTERIDE 4.0 1 9.74
CHEMBL312531 1 9.64
CHEMBL137691 1 9.44
CHEMBL77328 1 9.40
CHEMBL135780 1 9.24
CHEMBL76192 1 9.06
CHEMBL73816 1 8.89
CHEMBL76648 1 8.82
CHEMBL307626 1 8.62
CHEMBL136863 1 8.55
CHEMBL297524 1 8.49
CHEMBL135313 1 8.17
CHEMBL24291 1 8.15
CHEMBL138225 EPRISTERIDE 2.0 1 7.52
CHEMBL310710 1 7.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL138173 IC50 = 0.04 nM 10.40
CHEMBL137733 IC50 = 0.07 nM 10.15
CHEMBL420020 IC50 = 0.08 nM 10.10
CHEMBL24088 IC50 = 0.09 nM 10.05
CHEMBL308258 IC50 = 0.09 nM 10.05
CHEMBL412425 IC50 = 0.12 nM 9.92
CHEMBL436215 IC50 = 0.13 nM 9.89
CHEMBL306722 IC50 = 0.16 nM 9.80
CHEMBL710 FINASTERIDE IC50 = 0.18 nM 9.74
CHEMBL312531 IC50 = 0.23 nM 9.64
CHEMBL137691 IC50 = 0.36 nM 9.44
CHEMBL77328 IC50 = 0.4 nM 9.40
CHEMBL135780 IC50 = 0.58 nM 9.24
CHEMBL76192 IC50 = 0.88 nM 9.06
CHEMBL73816 IC50 = 1.3 nM 8.89
CHEMBL76648 IC50 = 1.5 nM 8.82
CHEMBL307626 IC50 = 2.4 nM 8.62
CHEMBL136863 IC50 = 2.8 nM 8.55
CHEMBL297524 IC50 = 3.2 nM 8.49
CHEMBL135313 IC50 = 6.7 nM 8.17
CHEMBL24291 IC50 = 7.1 nM 8.15
CHEMBL138225 EPRISTERIDE IC50 = 30.0 nM 7.52
CHEMBL310710 IC50 = 33.0 nM 7.48