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Assay Detail

CHEMBL4257284

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

Binding
Inhibition of recombinant human N-terminal His-tagged JMJD2A (1 to 350 residues) expressed in Escherichia coli using H3K9me3-biotin peptide as substrate after 30 mins in presence of alpha-ketoglutaric acid by LANCE TR-FRET assay
ChEMBL ↗
49
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Lysine-specific demethylase 4A (CHEMBL5896) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Histone demethylase inhibitors
(2016)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 49 6.88 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4293159 — — 1 7.00
CHEMBL4295253 — — 1 7.00
CHEMBL4286665 — — 1 7.00
CHEMBL4285687 — — 1 7.00
CHEMBL4281219 — — 1 7.00
CHEMBL4281591 — — 1 7.00
CHEMBL4282667 — — 1 7.00
CHEMBL4278227 — — 1 7.00
CHEMBL4283431 — — 1 7.00
CHEMBL4280613 — — 1 7.00
CHEMBL4293359 — — 1 7.00
CHEMBL4290188 — — 1 7.00
CHEMBL4286102 — — 1 7.00
CHEMBL4286972 — — 1 7.00
CHEMBL4284008 — — 1 7.00
CHEMBL4291057 — — 1 6.00
CHEMBL4283417 — — 1 6.00
CHEMBL4279284 — — 1 -
CHEMBL4287989 — — 1 -
CHEMBL4294777 — — 1 -
CHEMBL4293019 — — 1 -
CHEMBL3787133 — — 1 -
CHEMBL4287682 — — 1 -
CHEMBL4291787 — — 1 -
CHEMBL4277136 — — 1 -
CHEMBL4285453 — — 1 -
CHEMBL4284366 — — 1 -
CHEMBL4282244 — — 1 -
CHEMBL4281193 — — 1 -
CHEMBL4288012 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4293159 — IC50 = 100.0 nM 7.00
CHEMBL4295253 — IC50 = 100.0 nM 7.00
CHEMBL4286665 — IC50 = 100.0 nM 7.00
CHEMBL4285687 — IC50 = 100.0 nM 7.00
CHEMBL4281219 — IC50 = 100.0 nM 7.00
CHEMBL4281591 — IC50 = 100.0 nM 7.00
CHEMBL4282667 — IC50 = 100.0 nM 7.00
CHEMBL4278227 — IC50 = 100.0 nM 7.00
CHEMBL4283431 — IC50 = 100.0 nM 7.00
CHEMBL4280613 — IC50 = 100.0 nM 7.00
CHEMBL4293359 — IC50 = 100.0 nM 7.00
CHEMBL4290188 — IC50 = 100.0 nM 7.00
CHEMBL4286102 — IC50 = 100.0 nM 7.00
CHEMBL4286972 — IC50 = 100.0 nM 7.00
CHEMBL4284008 — IC50 = 100.0 nM 7.00
CHEMBL4283417 — IC50 = 1000.0 nM 6.00
CHEMBL4291057 — IC50 = 1000.0 nM 6.00
CHEMBL4290755 — IC50 <= 100.0 nM -
CHEMBL4282856 — IC50 <= 100.0 nM -
CHEMBL4283918 — IC50 <= 100.0 nM -
CHEMBL4285323 — IC50 <= 100.0 nM -
CHEMBL4288025 — IC50 <= 100.0 nM -
CHEMBL4290173 — IC50 <= 100.0 nM -
CHEMBL4279259 — IC50 <= 100.0 nM -
CHEMBL4282361 — IC50 <= 100.0 nM -
CHEMBL3786225 — IC50 > 10000.0 nM -
CHEMBL4278375 — IC50 > 10000.0 nM -
CHEMBL4292346 — IC50 <= 100.0 nM -
CHEMBL4279762 — IC50 <= 100.0 nM -
CHEMBL4289159 — IC50 <= 100.0 nM -
CHEMBL4278732 — IC50 <= 100.0 nM -
CHEMBL4288875 — IC50 <= 100.0 nM -
CHEMBL4289917 — IC50 <= 100.0 nM -
CHEMBL4290010 — IC50 > 10000.0 nM -
CHEMBL4286301 — IC50 > 10000.0 nM -
CHEMBL4289071 — IC50 > 10000.0 nM -
CHEMBL4288012 — IC50 > 10000.0 nM -
CHEMBL4281193 — IC50 > 10000.0 nM -
CHEMBL4282244 — IC50 > 10000.0 nM -
CHEMBL4284366 — IC50 > 10000.0 nM -
CHEMBL4285453 — IC50 > 10000.0 nM -
CHEMBL4277136 — IC50 > 10000.0 nM -
CHEMBL4291787 — IC50 > 10000.0 nM -
CHEMBL4287682 — IC50 <= 100.0 nM -
CHEMBL3787133 — IC50 <= 100.0 nM -
CHEMBL4293019 — IC50 <= 100.0 nM -
CHEMBL4294777 — IC50 <= 100.0 nM -
CHEMBL4287989 — IC50 <= 100.0 nM -
CHEMBL4279284 — IC50 <= 100.0 nM -