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Assay Detail

CHEMBL5216099

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

Binding
Inhibition of KDM6A (unknown origin) expressed in Escherichia coli using Biotin-H3(14-34)K27me3 peptide and measured after 1 hrs by alpha screen assay
1
Total Activities
1
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

Lysine-specific demethylase 6A (CHEMBL2069164)
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
IC50 1 6.70 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1230640 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1230640 IC50 = 200.0 nM 6.70