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Assay Detail

CHEMBL2167520

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

Binding
Inhibition of human KDM3A catalytic domain expressed in Sf9 cells methyl lysine peptide substrate by AlphaScreen assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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
IC50 10 5.21 5.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL51979 1 5.52
CHEMBL222824 SUCCINYLACETONE 1 4.90
CHEMBL2164250 1 -
CHEMBL2164249 1 -
CHEMBL2164248 1 -
CHEMBL2164247 1 -
CHEMBL2164246 1 -
CHEMBL2164245 1 -
CHEMBL2164244 1 -
CHEMBL2164243 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL51979 IC50 = 3000.0 nM 5.52
CHEMBL222824 SUCCINYLACETONE IC50 = 12700.0 nM 4.90
CHEMBL2164250 IC50 > 100000.0 nM -
CHEMBL2164249 IC50 > 100000.0 nM -
CHEMBL2164248 IC50 > 100000.0 nM -
CHEMBL2164247 IC50 > 100000.0 nM -
CHEMBL2164246 IC50 > 100000.0 nM -
CHEMBL2164245 IC50 > 100000.0 nM -
CHEMBL2164244 IC50 > 100000.0 nM -
CHEMBL2164243 IC50 = 127000.0 nM -