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Assay Detail

CHEMBL2427609

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

Binding
Inhibition of KDM4A (unknown origin) using H3K9me3 peptide and 2-oxoglutarate as substrate after 1 hr by FDH-coupled assay
12
Total Activities
12
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 4A (CHEMBL5896)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of the KDM2/7 histone lysine demethylase subfamily inhibitor and its antiproliferative activity.
Suzuki T, Ozasa H, Itoh Y, Zhan P, Sawada H, Mino K, Walport L, Ohkubo R, Kawamura A, Yonezawa M, Tsukada Y, Tumber A, Nakagawa H, Hasegawa M, Sasaki R, Mizukami T, Schofield CJ, Miyata N.
J Med Chem (2013) 56 : 7222 -7231
PubMed 23964788 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 4.62 6.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1229308 1 6.10
CHEMBL316034 1 5.38
CHEMBL2424816 1 4.19
CHEMBL2424809 1 4.04
CHEMBL2424815 1 4.00
CHEMBL2424811 1 4.00
CHEMBL2424814 1 -
CHEMBL2424813 1 -
CHEMBL2424812 1 -
CHEMBL2424810 1 -
CHEMBL2164243 1 -
CHEMBL90852 N-OXALYLGLYCINE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1229308 IC50 = 800.0 nM 6.10
CHEMBL316034 IC50 = 4200.0 nM 5.38
CHEMBL2424816 IC50 = 65000.0 nM 4.19
CHEMBL2424809 IC50 = 92000.0 nM 4.04
CHEMBL2424815 IC50 = 99000.0 nM 4.00
CHEMBL2424811 IC50 = 100000.0 nM 4.00
CHEMBL2424814 IC50 > 120000.0 nM -
CHEMBL2424813 IC50 > 120000.0 nM -
CHEMBL2424812 IC50 > 120000.0 nM -
CHEMBL2424810 IC50 > 120000.0 nM -
CHEMBL2164243 IC50 > 3300000.0 nM -
CHEMBL90852 N-OXALYLGLYCINE IC50 = 250000.0 nM -