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Assay Detail

CHEMBL5216110

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

Binding
Binding affinity to recombinant full length N-terminal hexahistidine-tagged human FTO expressed in Escherichia coli BL21 by competition-based NMR binding assay
4
Total Activities
4
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

Structure-Based Design of Selective Fat Mass and Obesity Associated Protein (FTO) Inhibitors.
Shishodia S, Demetriades M, Zhang D, Tam NY, Maheswaran P, Clunie-O'Connor C, Tumber A, Leung IKH, Ng YM, Leissing TM, El-Sagheer AH, Salah E, Brown T, Aik WS, McDonough MA, Schofield CJ.
J Med Chem (2021) 64 : 16609 -16625
PubMed 34762429 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 4 5.99 6.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5219846 1 6.47
CHEMBL5219336 1 6.17
CHEMBL5218636 1 5.92
CHEMBL5220246 1 5.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5219846 Kd = 340.0 nM 6.47
CHEMBL5219336 Kd = 670.0 nM 6.17
CHEMBL5218636 Kd = 1200.0 nM 5.92
CHEMBL5220246 Kd = 3900.0 nM 5.41