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Assay Detail

CHEMBL701910

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

Binding
Inhibition of recombinant human 5-alpha reductase-1 at a concentration of 5 microL after pre-incubation for 10 minutes
22
Total Activities
22
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

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
Ki 22 6.86 8.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL138173 1 8.16
CHEMBL308258 1 8.09
CHEMBL420020 1 8.05
CHEMBL137733 1 7.96
CHEMBL312531 1 7.85
CHEMBL412425 1 7.70
CHEMBL77328 1 7.70
CHEMBL306722 1 7.70
CHEMBL24088 1 7.52
CHEMBL436215 1 7.12
CHEMBL297524 1 6.82
CHEMBL137691 1 6.72
CHEMBL135780 1 6.44
CHEMBL73816 1 6.24
CHEMBL136863 1 6.14
CHEMBL76648 1 6.12
CHEMBL76192 1 6.09
CHEMBL24291 1 5.66
CHEMBL307626 1 5.64
CHEMBL135313 1 5.22
CHEMBL310710 1 5.07
CHEMBL138225 EPRISTERIDE 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL138173 Ki = 6.9 nM 8.16
CHEMBL308258 Ki = 8.2 nM 8.09
CHEMBL420020 Ki = 9.0 nM 8.05
CHEMBL137733 Ki = 11.0 nM 7.96
CHEMBL312531 Ki = 14.0 nM 7.85
CHEMBL412425 Ki = 20.0 nM 7.70
CHEMBL77328 Ki = 20.0 nM 7.70
CHEMBL306722 Ki = 20.0 nM 7.70
CHEMBL24088 Ki = 30.0 nM 7.52
CHEMBL436215 Ki = 75.0 nM 7.12
CHEMBL297524 Ki = 150.0 nM 6.82
CHEMBL137691 Ki = 190.0 nM 6.72
CHEMBL135780 Ki = 360.0 nM 6.44
CHEMBL73816 Ki = 570.0 nM 6.24
CHEMBL136863 Ki = 720.0 nM 6.14
CHEMBL76648 Ki = 750.0 nM 6.12
CHEMBL76192 Ki = 820.0 nM 6.09
CHEMBL24291 Ki = 2200.0 nM 5.66
CHEMBL307626 Ki = 2300.0 nM 5.64
CHEMBL135313 Ki = 6000.0 nM 5.22
CHEMBL310710 Ki = 8600.0 nM 5.07
CHEMBL138225 EPRISTERIDE Ki > 5000.0 nM -