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Assay Detail

CHEMBL1070280

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Binding
Inhibition of JMJD2E by FDH coupled assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Selective inhibitors of the JMJD2 histone demethylases: combined nondenaturing mass spectrometric screening and crystallographic approaches.
Rose NR, Woon EC, Kingham GL, King ON, Mecinović J, Clifton IJ, Ng SS, Talib-Hardy J, Oppermann U, McDonough MA, Schofield CJ.
J Med Chem (2010) 53 : 1810 -1818
PubMed 20088513 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 4.78 5.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL602503 1 5.27
CHEMBL600221 1 5.07
CHEMBL602502 1 4.93
CHEMBL602295 1 4.83
CHEMBL602673 1 4.83
CHEMBL599994 1 4.83
CHEMBL591925 1 4.78
CHEMBL600377 1 4.70
CHEMBL591689 1 4.43
CHEMBL600802 1 4.08
CHEMBL600803 1 -
CHEMBL600193 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL602503 IC50 = 5400.0 nM 5.27
CHEMBL600221 IC50 = 8600.0 nM 5.07
CHEMBL602502 IC50 = 11700.0 nM 4.93
CHEMBL602295 IC50 = 14700.0 nM 4.83
CHEMBL602673 IC50 = 14700.0 nM 4.83
CHEMBL599994 IC50 = 14800.0 nM 4.83
CHEMBL591925 IC50 = 16600.0 nM 4.78
CHEMBL600377 IC50 = 20100.0 nM 4.70
CHEMBL591689 IC50 = 37100.0 nM 4.43
CHEMBL600802 IC50 = 82900.0 nM 4.08
CHEMBL600803 IC50 = 185100.0 nM -
CHEMBL600193 IC50 = 326500.0 nM -