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Assay Detail

CHEMBL4411615

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

Binding
Binding affinity to 5'-Biotinylated-AR1 G-quadruplex oligonucleotide (unknown origin) by SPR analysis
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Not specified
Confidence 3 — Cell-line / Tissue
Curated By Autocuration

Target

quadruplex DNA (CHEMBL3832742)
Type NUCLEIC-ACID
Organism Homo sapiens

Publication

Down-Regulation of the Androgen Receptor by G-Quadruplex Ligands Sensitizes Castration-Resistant Prostate Cancer Cells to Enzalutamide.
Tassinari M, Cimino-Reale G, Nadai M, Doria F, Butovskaya E, Recagni M, Freccero M, Zaffaroni N, Richter SN, Folini M.
J Med Chem (2018) 61 : 8625 -8638
PubMed 30188709 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 9 7.35 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4468209 1 7.75
CHEMBL4526946 1 7.67
CHEMBL4565909 1 7.47
CHEMBL4566017 1 7.42
CHEMBL4452581 1 7.38
CHEMBL4558509 1 7.36
CHEMBL4436828 1 7.03
CHEMBL4453055 1 6.74
CHEMBL4519317 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4468209 Kd = 17.9 nM 7.75
CHEMBL4526946 Kd = 21.4 nM 7.67
CHEMBL4565909 Kd = 34.2 nM 7.47
CHEMBL4566017 Kd = 38.3 nM 7.42
CHEMBL4452581 Kd = 41.2 nM 7.38
CHEMBL4558509 Kd = 43.9 nM 7.36
CHEMBL4436828 Kd = 92.5 nM 7.03
CHEMBL4453055 Kd = 181.6 nM 6.74
CHEMBL4519317 Kd - -