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Assay Detail

CHEMBL3776328

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

Binding
Competitive inhibition of N-terminal His6-tagged KDM4C (1 to 352 residues) (unknown origin) expressed in Escherichia coli Rosetta 2(DE3)pLysS using 250 uM ARK(Me3)STGGK peptide/50 uM alpha-ketoglutarate as substrate/cofactor by FDH coupling-based Lineweaver-Burk plot analysis
3
Total Activities
3
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 4C (CHEMBL6175)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Docking and Linking of Fragments To Discover Jumonji Histone Demethylase Inhibitors.
Korczynska M, Le DD, Younger N, Gregori-Puigjané E, Tumber A, Krojer T, Velupillai S, Gileadi C, Nowak RP, Iwasa E, Pollock SB, Ortiz Torres I, Oppermann U, Shoichet BK, Fujimori DG.
J Med Chem (2016) 59 : 1580 -1598
PubMed 26699912 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.27 5.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL316034 1 5.72
CHEMBL3775262 1 5.26
CHEMBL3775380 1 4.83

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL316034 IC50 = 1900.0 nM 5.72
CHEMBL3775262 IC50 = 5500.0 nM 5.26
CHEMBL3775380 IC50 = 14900.0 nM 4.83