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Assay Detail

CHEMBL2167328

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

Binding
Competitive inhibition of human KDM2A expressed in Escherichia coli using 2-oxoglutarate by enzyme kinetic 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 2A (CHEMBL1938210)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Plant growth regulator daminozide is a selective inhibitor of human KDM2/7 histone demethylases.
Rose NR, Woon EC, Tumber A, Walport LJ, Chowdhury R, Li XS, King ON, Lejeune C, Ng SS, Krojer T, Chan MC, Rydzik AM, Hopkinson RJ, Che KH, Daniel M, Strain-Damerell C, Gileadi C, Kochan G, Leung IK, Dunford J, Yeoh KK, Ratcliffe PJ, Burgess-Brown N, von Delft F, Muller S, Marsden B, Brennan PE, McDonough MA, Oppermann U, Klose RJ, Schofield CJ, Kawamura A.
J Med Chem (2012) 55 : 6639 -6643
PubMed 22724510 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 5.71 5.71

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2164243 1 5.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2164243 Ki = 1970.0 nM 5.71