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Assay Detail

CHEMBL666799

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

Binding
Inhibitory activity against human placental cytochrome P450 19A1
20
Total Activities
20
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

Analogues of 3-ethyl-3-(4-pyridyl)piperidine-2,6-dione as selective inhibitors of aromatase: derivatives with variable 1-alkyl and 3-alkyl substituents.
Leung CS, Rowlands MG, Jarman M, Foster AB, Griggs LJ, Wilman DE.
J Med Chem (1987) 30 : 1550 -1554
PubMed 3625703 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 5.28 6.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38472 1 6.48
CHEMBL39661 1 6.10
CHEMBL38439 1 5.82
CHEMBL289766 1 5.62
CHEMBL288712 1 5.60
CHEMBL38550 1 5.52
CHEMBL41066 1 5.50
CHEMBL39152 1 5.44
CHEMBL40125 1 5.40
CHEMBL275594 1 5.22
CHEMBL37321 1 5.18
CHEMBL488 AMINOGLUTETHIMIDE 4.0 1 5.10
CHEMBL289116 ROGLETIMIDE 2.0 1 5.00
CHEMBL39840 1 5.00
CHEMBL39513 1 4.68
CHEMBL39782 1 4.52
CHEMBL38877 1 4.51
CHEMBL39275 1 4.40
CHEMBL38510 1 -
CHEMBL39781 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38472 IC50 = 330.0 nM 6.48
CHEMBL39661 IC50 = 800.0 nM 6.10
CHEMBL38439 IC50 = 1500.0 nM 5.82
CHEMBL289766 IC50 = 2400.0 nM 5.62
CHEMBL288712 IC50 = 2500.0 nM 5.60
CHEMBL38550 IC50 = 3000.0 nM 5.52
CHEMBL41066 IC50 = 3200.0 nM 5.50
CHEMBL39152 IC50 = 3600.0 nM 5.44
CHEMBL40125 IC50 = 4000.0 nM 5.40
CHEMBL275594 IC50 = 6000.0 nM 5.22
CHEMBL37321 IC50 = 6600.0 nM 5.18
CHEMBL488 AMINOGLUTETHIMIDE IC50 = 8000.0 nM 5.10
CHEMBL289116 ROGLETIMIDE IC50 = 10000.0 nM 5.00
CHEMBL39840 IC50 = 10000.0 nM 5.00
CHEMBL39513 IC50 = 21000.0 nM 4.68
CHEMBL39782 IC50 = 30000.0 nM 4.52
CHEMBL38877 IC50 = 31000.0 nM 4.51
CHEMBL39275 IC50 = 40000.0 nM 4.40
CHEMBL38510 IC50 = 245000.0 nM -
CHEMBL39781 IC50 = 385000.0 nM -