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Assay Detail

CHEMBL5142379

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

Binding
Inhibition of recombinant FTO (unknown origin) using m6A Broccoli as substrate incubated for 2 hrs
30
Total Activities
30
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

Rational Design and Optimization of m<sup>6</sup>A-RNA Demethylase FTO Inhibitors as Anticancer Agents.
Huff S, Kummetha IR, Zhang L, Wang L, Bray W, Yin J, Kelley V, Wang Y, Rana TM.
J Med Chem (2022) 65 : 10920 -10937
PubMed 35939803 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 6.02 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5195767 1 7.16
CHEMBL5200892 1 6.96
CHEMBL5207866 1 6.80
CHEMBL5194680 1 6.57
CHEMBL5204291 1 6.46
CHEMBL5207797 1 6.46
CHEMBL5203668 1 6.36
CHEMBL5186890 1 6.17
CHEMBL5181285 1 6.09
CHEMBL5199622 1 6.08
CHEMBL5177222 1 6.06
CHEMBL5182180 1 6.05
CHEMBL5191997 1 6.02
CHEMBL5208073 1 6.00
CHEMBL5174078 1 6.00
CHEMBL5174480 1 5.96
CHEMBL5184614 1 5.89
CHEMBL5195274 1 5.89
CHEMBL5205687 1 5.89
CHEMBL5205984 1 5.82
CHEMBL5188113 1 5.77
CHEMBL5208226 1 5.70
CHEMBL5208008 1 5.70
CHEMBL5195210 1 5.68
CHEMBL5198269 1 5.66
CHEMBL5182267 1 5.60
CHEMBL5169524 1 5.52
CHEMBL5176984 1 5.47
CHEMBL5197784 1 5.40
CHEMBL5196700 1 5.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5195767 IC50 = 70.0 nM 7.16
CHEMBL5200892 IC50 = 110.0 nM 6.96
CHEMBL5207866 IC50 = 160.0 nM 6.80
CHEMBL5194680 IC50 = 270.0 nM 6.57
CHEMBL5204291 IC50 = 350.0 nM 6.46
CHEMBL5207797 IC50 = 350.0 nM 6.46
CHEMBL5203668 IC50 = 440.0 nM 6.36
CHEMBL5186890 IC50 = 670.0 nM 6.17
CHEMBL5181285 IC50 = 810.0 nM 6.09
CHEMBL5199622 IC50 = 830.0 nM 6.08
CHEMBL5177222 IC50 = 870.0 nM 6.06
CHEMBL5182180 IC50 = 900.0 nM 6.05
CHEMBL5191997 IC50 = 950.0 nM 6.02
CHEMBL5208073 IC50 = 1000.0 nM 6.00
CHEMBL5174078 IC50 = 1000.0 nM 6.00
CHEMBL5174480 IC50 = 1100.0 nM 5.96
CHEMBL5184614 IC50 = 1300.0 nM 5.89
CHEMBL5195274 IC50 = 1300.0 nM 5.89
CHEMBL5205687 IC50 = 1300.0 nM 5.89
CHEMBL5205984 IC50 = 1500.0 nM 5.82
CHEMBL5188113 IC50 = 1700.0 nM 5.77
CHEMBL5208226 IC50 = 2000.0 nM 5.70
CHEMBL5208008 IC50 = 2000.0 nM 5.70
CHEMBL5195210 IC50 = 2100.0 nM 5.68
CHEMBL5198269 IC50 = 2200.0 nM 5.66
CHEMBL5182267 IC50 = 2500.0 nM 5.60
CHEMBL5169524 IC50 = 3000.0 nM 5.52
CHEMBL5176984 IC50 = 3400.0 nM 5.47
CHEMBL5197784 IC50 = 4000.0 nM 5.40
CHEMBL5196700 IC50 = 4300.0 nM 5.37