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Assay Detail

CHEMBL3778170

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

Binding
Inhibition of KDM4E (unknown origin) using H3K9Me3 peptide as substrate assessed as demethylation of substrate by Rapidfire mass spectrometric 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

Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 1. 3-Amino-4-pyridine Carboxylate Derivatives.
Westaway SM, Preston AG, Barker MD, Brown F, Brown JA, Campbell M, Chung CW, Diallo H, Douault C, Drewes G, Eagle R, Gordon L, Haslam C, Hayhow TG, Humphreys PG, Joberty G, Katso R, Kruidenier L, Leveridge M, Liddle J, Mosley J, Muelbaier M, Randle R, Rioja I, Rueger A, Seal GA, Sheppard RJ, Singh O, Taylor J, Thomas P, Thomson D, Wilson DM, Lee K, Prinjha RK.
J Med Chem (2016) 59 : 1357 -1369
PubMed 26771107 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.37 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3775237 1 7.40
CHEMBL3775612 1 7.40
CHEMBL3775889 1 7.30
CHEMBL3774615 1 -
CHEMBL3774435 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3775237 IC50 = 39.81 nM 7.40
CHEMBL3775612 IC50 = 39.81 nM 7.40
CHEMBL3775889 IC50 = 50.12 nM 7.30
CHEMBL3774615 IC50 > 100000.0 nM -
CHEMBL3774435 IC50 > 100000.0 nM -