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Assay Detail

CHEMBL975403

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Functional
Antagonist activity at human androgen receptor expressed in mouse NIH3T3 cells assessed as inhibition of DHT-induced transcriptional activation after 24 hrs by androgen response element-mediated luciferase reporter gene assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type NIH3T3
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of carborane-containing androgen receptor (AR) antagonist bearing a pyridine ring.
Ohta K, Goto T, Fijii S, Suzuki T, Ohta S, Endo Y.
Bioorg Med Chem (2008) 16 : 8022 -8028
PubMed 18707892 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.71 7.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL491 HYDROXYFLUTAMIDE 2.0 1 7.17
CHEMBL806 FLUTAMIDE 4.0 1 6.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL491 HYDROXYFLUTAMIDE IC50 = 67.0 nM 7.17
CHEMBL806 FLUTAMIDE IC50 = 580.0 nM 6.24