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Assay Detail

CHEMBL5132491

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

Binding
Inhibition of FTO (unknown origin) demethylation activity by HPLC assay
3
Total Activities
3
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

Identification of Potent and Selective Inhibitors of Fat Mass Obesity-Associated Protein Using a Fragment-Merging Approach.
Prakash M, Itoh Y, Fujiwara Y, Takahashi Y, Takada Y, Mellini P, Elboray EE, Terao M, Yamashita Y, Yamamoto C, Yamaguchi T, Kotoku M, Kitao Y, Singh R, Roy R, Obika S, Oba M, Wang DO, Suzuki T.
J Med Chem (2021) 64 : 15810 -15824
PubMed 34727689 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.44 7.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5196484 1 7.06
CHEMBL5183243 1 6.24
CHEMBL5173876 1 6.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5196484 IC50 = 87.0 nM 7.06
CHEMBL5183243 IC50 = 570.0 nM 6.24
CHEMBL5173876 IC50 = 930.0 nM 6.03