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Assay Detail

CHEMBL1113403

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

Functional
Antagonist activity at AR in human MDA-kb2 cells co-transfected with MMTV-luc assessed as decrease in DHT-induced luciferase activity by reporter gene assay
13
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MDA-kb2
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Effect of essential oils, such as raspberry ketone and its derivatives, on antiandrogenic activity based on in vitro reporter gene assay.
Ogawa Y, Akamatsu M, Hotta Y, Hosoda A, Tamura H.
Bioorg Med Chem Lett (2010) 20 : 2111 -2114
PubMed 20226658 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.15 6.00
Activity 4 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL806 FLUTAMIDE 4.0 1 6.00
CHEMBL42710 EUGENOL 0.5 3 4.72
CHEMBL105912 RASPBERRYKETONE 3 -
CHEMBL25894 ZINGERONE 3 -
CHEMBL1090553 3 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL806 FLUTAMIDE IC50 = 1000.0 nM 6.00
CHEMBL42710 EUGENOL IC50 = 19000.0 nM 4.72
CHEMBL42710 EUGENOL IC50 = 19054.61 nM 4.72
CHEMBL105912 RASPBERRYKETONE IC50 = 252000.0 nM -
CHEMBL25894 ZINGERONE IC50 = 153000.0 nM -
CHEMBL1090553 IC50 = 420000.0 nM -
CHEMBL105912 RASPBERRYKETONE IC50 = 251188.64 nM -
CHEMBL25894 ZINGERONE IC50 = 151356.12 nM -
CHEMBL1090553 IC50 = 416869.38 nM -
CHEMBL105912 RASPBERRYKETONE Activity - -
CHEMBL42710 EUGENOL Activity - -
CHEMBL25894 ZINGERONE Activity - -
CHEMBL1090553 Activity - -