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Assay Detail

CHEMBL3607998

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

Binding
Inhibition of androgen receptor in human LNCAP cells assessed as inhibition of DHT-induced SPDEF gene expression by Array Plate assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
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 of Potent 17β-Hydroxywithanolides for Castration-Resistant Prostate Cancer by High-Throughput Screening of a Natural Products Library for Androgen-Induced Gene Expression Inhibitors.
Xu YM, Liu MX, Grunow N, Wijeratne EM, Paine-Murrieta G, Felder S, Kris RM, Gunatilaka AA.
J Med Chem (2015) 58 : 6984 -6993
PubMed 26305181 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.77 6.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3605564 1 6.11
CHEMBL3605563 1 5.92
CHEMBL3605562 1 5.57
CHEMBL3605560 1 5.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3605564 IC50 = 770.0 nM 6.11
CHEMBL3605563 IC50 = 1200.0 nM 5.92
CHEMBL3605562 IC50 = 2720.0 nM 5.57
CHEMBL3605560 IC50 = 3280.0 nM 5.48