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Assay Detail

CHEMBL5585111

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

Binding
Inhibition of FTO (unknown origin) expressed in Escherichia coli BL21(DE3) using 5'-TAGACATTGCCATTCTCGATAGG(m6A)-TCCGGTCAAACCTAGACGAATTCCA-3' as substrate by FP assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Alpha-ketoglutarate-dependent dioxygenase FTO (CHEMBL2331065)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Small molecules that regulate the N<sup>6</sup>-methyladenosine RNA modification as potential anti-cancer agents.
Harrahill NJ, Hadden MK.
Eur J Med Chem (2024) 274 : 116526 -116526
PubMed 38805939 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.29 5.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL41286 DIACEREIN 3.0 1 5.82
CHEMBL5281651 1 5.82
CHEMBL426560 1 5.55
CHEMBL1230640 1 5.48
CHEMBL953 ENTACAPONE 4.0 1 5.46
CHEMBL3989553 NAFAMOSTAT MESYLATE 3.0 1 4.86
CHEMBL414883 RADICICOL 1 4.80
CHEMBL235934 CLAUSINE E 1 4.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL41286 DIACEREIN IC50 = 1500.0 nM 5.82
CHEMBL5281651 IC50 = 1500.0 nM 5.82
CHEMBL426560 IC50 = 2800.0 nM 5.55
CHEMBL1230640 IC50 = 3300.0 nM 5.48
CHEMBL953 ENTACAPONE IC50 = 3500.0 nM 5.46
CHEMBL3989553 NAFAMOSTAT MESYLATE IC50 = 13800.0 nM 4.86
CHEMBL414883 RADICICOL IC50 = 16000.0 nM 4.80
CHEMBL235934 CLAUSINE E IC50 = 28000.0 nM 4.55