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Assay Detail

CHEMBL663241

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

Binding
In vitro competitive inhibitory activity was measured on Cytochrome P450 19A1 of human placental microsomes
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Aromatase (CHEMBL1978)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis of androst-5-en-7-ones and androsta-3,5-dien-7-ones and their related 7-deoxy analogs as conformational and catalytic probes for the active site of aromatase.
Numazawa M, Mutsumi A, Tachibana M, Hoshi K.
J Med Chem (1994) 37 : 2198 -2205
PubMed 8035427 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 4.89 6.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL71152 1 6.47
CHEMBL2311169 1 6.18
CHEMBL70367 1 5.75
CHEMBL262723 1 5.75
CHEMBL1630911 1 5.16
CHEMBL302305 1 4.96
CHEMBL71117 1 4.75
CHEMBL71082 1 4.55
CHEMBL68674 1 4.52
CHEMBL71612 1 4.48
CHEMBL311400 1 4.38
CHEMBL302249 1 4.38
CHEMBL71363 1 4.26
CHEMBL302741 1 4.25
CHEMBL302530 1 4.22
CHEMBL71169 1 4.22
CHEMBL421491 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL71152 IC50 = 340.0 nM 6.47
CHEMBL2311169 IC50 = 660.0 nM 6.18
CHEMBL70367 IC50 = 1800.0 nM 5.75
CHEMBL262723 IC50 = 1800.0 nM 5.75
CHEMBL1630911 IC50 = 6900.0 nM 5.16
CHEMBL302305 IC50 = 11000.0 nM 4.96
CHEMBL71117 IC50 = 18000.0 nM 4.75
CHEMBL71082 IC50 = 28000.0 nM 4.55
CHEMBL68674 IC50 = 30000.0 nM 4.52
CHEMBL71612 IC50 = 33000.0 nM 4.48
CHEMBL311400 IC50 = 42000.0 nM 4.38
CHEMBL302249 IC50 = 42000.0 nM 4.38
CHEMBL71363 IC50 = 55000.0 nM 4.26
CHEMBL302741 IC50 = 56000.0 nM 4.25
CHEMBL302530 IC50 = 60000.0 nM 4.22
CHEMBL71169 IC50 = 60000.0 nM 4.22
CHEMBL421491 IC50 = 140000.0 nM -