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Assay Detail

CHEMBL3789206

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

Binding
Inhibition of recombinant human C-terminal FLAG-tagged KDM2B (1 to 650 residues) expressed in baculovirus infected sf9 cells using biotin-H3K36me2 as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by AlphaLisa assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Lysine-specific demethylase 2B (CHEMBL3779760)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Recent Progress in Histone Demethylase Inhibitors.
McAllister TE, England KS, Hopkinson RJ, Brennan PE, Kawamura A, Schofield CJ.
J Med Chem (2016) 59 : 1308 -1329
PubMed 26710088 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.00 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3787669 1 7.00
CHEMBL3787547 1 -
CHEMBL3786409 1 -
CHEMBL3787193 1 -
CHEMBL3785378 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3787669 IC50 = 100.0 nM 7.00
CHEMBL3787547 IC50 > 2500.0 nM -
CHEMBL3786409 IC50 > 2500.0 nM -
CHEMBL3787193 IC50 > 1000.0 nM -
CHEMBL3785378 IC50 < 250.0 nM -