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Assay Detail

CHEMBL663078

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

Binding
Inhibition of Cytochrome P450 19A1 against testosterone at 1.5 uM (Km=0.13 uM)
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Aromatase (CHEMBL1978)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biochemical evaluation of analogues of aminoglutethimide based on phenylpyrrolidine-2,5-dione.
Daly MJ, Jones GW, Nicholls PJ, Smith HJ, Rowlands MG, Bunnett MA.
J Med Chem (1986) 29 : 520 -523
PubMed 3754286 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 4.88 5.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL488 AMINOGLUTETHIMIDE 4.0 1 5.21
CHEMBL149238 1 4.90
CHEMBL151212 1 4.87
CHEMBL151691 1 4.80
CHEMBL357775 1 4.78
CHEMBL148903 1 4.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL488 AMINOGLUTETHIMIDE IC50 = 6130.0 nM 5.21
CHEMBL149238 IC50 = 12500.0 nM 4.90
CHEMBL151212 IC50 = 13500.0 nM 4.87
CHEMBL151691 IC50 = 15660.0 nM 4.80
CHEMBL357775 IC50 = 16600.0 nM 4.78
CHEMBL148903 IC50 = 20000.0 nM 4.70