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Assay Detail

CHEMBL2350561

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

Binding
Binding affinity to human NRAS G-quadruplex FAM-GGGAGGGGCGGGUCUGGG-TAMRA RNA assessed as quenching of fluorescence emission by FRET titration assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Guanidino anthrathiophenediones as G-quadruplex binders: uptake, intracellular localization, and anti-Harvey-Ras gene activity in bladder cancer cells.
Cogoi S, Shchekotikhin AE, Membrino A, Sinkevich YB, Xodo LE.
J Med Chem (2013) 56 : 2764 -2778
PubMed 23458775 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 5 6.91 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2349420 1 7.22
CHEMBL2349418 1 7.05
CHEMBL2349419 1 6.96
CHEMBL2349417 1 6.92
CHEMBL472033 1 6.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2349420 Kd = 60.0 nM 7.22
CHEMBL2349418 Kd = 90.0 nM 7.05
CHEMBL2349419 Kd = 110.0 nM 6.96
CHEMBL2349417 Kd = 120.0 nM 6.92
CHEMBL472033 Kd = 380.0 nM 6.42