Assay Detail

CHEMBL3864026

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Binding

Displacement of fluormone-DHT green from His/GST-tagged rat AR ligand binding domain after 4 to 8 hrs by fluorescence polarization assay

ChEMBL ↗

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Target

Androgen receptor (CHEMBL3072) ↗

Open DB target context

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Androgen receptor (CHEMBL3072) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Androgen receptor

CHEMBL3072

Anchored from Assay target.

Protein identity Androgen receptor

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Rattus norvegicus
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Androgen receptor (CHEMBL3072) ↗

Type	SINGLE PROTEIN
Organism	Rattus norvegicus

Publication

Identification of Triptophenolide from Tripterygium wilfordii as a Pan-antagonist of Androgen Receptor.

He Y, Wu M, Liu Y, Li Q, Li X, Hu L, Cen S, Zhou J.
ACS Med Chem Lett (2016) 7 : 1024 -1027
PubMed 27994731 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	2	6.43	6.53
Inhibition	1	-	-

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1082407	ENZALUTAMIDE	4.0	1	6.53
CHEMBL3039217	TRIPTOPHENOLIDE	—	2	6.33

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1082407	ENZALUTAMIDE	IC50	=	294.0	nM	6.53
CHEMBL3039217	TRIPTOPHENOLIDE	IC50	=	467.0	nM	6.33
CHEMBL3039217	TRIPTOPHENOLIDE	Inhibition		-	%	-