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Assay Detail

CHEMBL666399

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

Binding
Evaluated for its competitive inhibitory activity against Cytochrome P450 19A1 with the use of human placental microsomal preparation
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Placenta
Subcellular Microsomal
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Aromatase (CHEMBL1978)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and evaluation of 4-(substituted thio)-4-androstene-3,17-dione derivatives as potential aromatase inhibitors.
Abul-Hajj YJ.
J Med Chem (1986) 29 : 582 -584
PubMed 3959033 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 7.34 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL346234 1 7.75
CHEMBL336387 1 7.44
CHEMBL154104 1 7.39
CHEMBL132530 FORMESTANE 2.0 1 7.27
CHEMBL346952 1 7.23
CHEMBL154918 1 7.19
CHEMBL152237 1 7.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL346234 Ki = 18.0 nM 7.75
CHEMBL336387 Ki = 36.0 nM 7.44
CHEMBL154104 Ki = 41.0 nM 7.39
CHEMBL132530 FORMESTANE Ki = 54.0 nM 7.27
CHEMBL346952 Ki = 59.0 nM 7.23
CHEMBL154918 Ki = 65.0 nM 7.19
CHEMBL152237 Ki = 73.0 nM 7.14