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Assay Detail

CHEMBL5364259

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

Binding
Inhibition of human recombinant KDM4E using biotinylated-H3K9me3 peptide as substrate by SPE-MS analysis
5
Total Activities
5
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 4E (CHEMBL1293226)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

5-Substituted Pyridine-2,4-dicarboxylate Derivatives Have Potential for Selective Inhibition of Human Jumonji-C Domain-Containing Protein 5.
Brewitz L, Nakashima Y, Piasecka SK, Salah E, Fletcher SC, Tumber A, Corner TP, Kennedy TJ, Fiorini G, Thalhammer A, Christensen KE, Coleman ML, Schofield CJ.
J Med Chem (2023) 66 : 10849 -10865
PubMed 37527664 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.58 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5429223 1 6.00
CHEMBL5414235 1 5.63
CHEMBL5415306 1 5.61
CHEMBL5429166 1 5.43
CHEMBL5401915 1 5.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5429223 IC50 = 990.0 nM 6.00
CHEMBL5414235 IC50 = 2360.0 nM 5.63
CHEMBL5415306 IC50 = 2450.0 nM 5.61
CHEMBL5429166 IC50 = 3690.0 nM 5.43
CHEMBL5401915 IC50 = 5710.0 nM 5.24