Assay Detail

CHEMBL3418492

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Binding

Displacement of [3H]R1881 from androgen receptor in human LNCAP cells

ChEMBL ↗

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Target

Androgen receptor (CHEMBL1871) ↗

Open DB target context

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Primary target Androgen receptor

CHEMBL1871

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	Homo sapiens
Cell Type	LNCaP
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Androgen receptor (CHEMBL1871) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery and development of Galeterone (TOK-001 or VN/124-1) for the treatment of all stages of prostate cancer.

Njar VC, Brodie AM.
J Med Chem (2015) 58 : 2077 -2087
PubMed 25591066 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
EC50	2	6.04	6.07

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL2105738	GALETERONE	3.0	1	6.07
CHEMBL409	BICALUTAMIDE	4.0	1	6.01

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL2105738	GALETERONE	EC50	=	845.0	nM	6.07
CHEMBL409	BICALUTAMIDE	EC50	=	971.0	nM	6.01