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Assay Detail

CHEMBL883668

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

Binding
Inhibition constant against aromatase protein from human placental microsomes using [1-beta-3H]-androstenedione; Competitive inhibition
4
Total Activities
4
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

Structure-activity relationships of new A,D-ring modified steroids as aromatase inhibitors: design, synthesis, and biological activity evaluation.
Cepa MM, Tavares da Silva EJ, Correia-da-Silva G, Roleira FM, Teixeira NA.
J Med Chem (2005) 48 : 6379 -6385
PubMed 16190763 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 6.93 7.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1629802 1 7.42
CHEMBL194641 1 7.30
CHEMBL1630280 1 6.83
CHEMBL197451 1 6.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1629802 Ki = 38.0 nM 7.42
CHEMBL194641 Ki = 50.0 nM 7.30
CHEMBL1630280 Ki = 147.0 nM 6.83
CHEMBL197451 Ki = 660.0 nM 6.18