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Assay Detail

CHEMBL857529

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

Binding
Inhibition of type-1 human steroid 5-alpha-reductase
17
Total Activities
16
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

A comparison of steroidal and non-steroidal inhibitors of human steroid 5-reductase: New tricyclic aryl acid inhibitors of the type-1 isozyme
Abell AD, Brandt M, Levy MA, Holt DA
Bioorg Med Chem Lett (1996) 6 : 481 -484
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 6.67 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2298601 1 8.52
CHEMBL29166 2 8.05
CHEMBL420020 1 8.05
CHEMBL25578 1 7.58
CHEMBL341625 1 6.50
CHEMBL356780 1 6.50
CHEMBL138225 EPRISTERIDE 2.0 1 6.39
CHEMBL76192 1 6.09
CHEMBL97266 1 6.04
CHEMBL25081 1 5.92
CHEMBL1627951 1 5.80
CHEMBL439804 1 5.72
CHEMBL143220 1 5.50
CHEMBL110001 1 5.38
CHEMBL144346 1 -
CHEMBL341666 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2298601 Ki = 3.0 nM 8.52
CHEMBL420020 Ki = 9.0 nM 8.05
CHEMBL29166 Ki = 9.0 nM 8.05
CHEMBL29166 Ki = 10.0 nM 8.00
CHEMBL25578 Ki = 26.0 nM 7.58
CHEMBL356780 Ki = 320.0 nM 6.50
CHEMBL341625 Ki = 315.0 nM 6.50
CHEMBL138225 EPRISTERIDE Ki = 410.0 nM 6.39
CHEMBL76192 Ki = 820.0 nM 6.09
CHEMBL97266 Ki = 920.0 nM 6.04
CHEMBL25081 Ki = 1200.0 nM 5.92
CHEMBL1627951 Ki = 1600.0 nM 5.80
CHEMBL439804 Ki = 1900.0 nM 5.72
CHEMBL143220 Ki = 3200.0 nM 5.50
CHEMBL110001 Ki = 4200.0 nM 5.38
CHEMBL144346 Ki > 2500.0 nM -
CHEMBL341666 Ki > 2500.0 nM -