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Assay Detail

CHEMBL3788932

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

Binding
Inhibition of recombinant human C-terminal FLAG-tagged KDM5A (1 to 1090 residues) expressed in baculovirus infected sf9 cells using biotin-H3K4me3 substrate incubated for 30 mins by TR-FRET assay
14
Total Activities
14
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 5A (CHEMBL2424504)
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 14 6.83 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3786803 1 7.00
CHEMBL3786225 1 7.00
CHEMBL3786596 1 7.00
CHEMBL3787548 1 7.00
CHEMBL3785421 1 7.00
CHEMBL3786108 1 6.00
CHEMBL3787133 1 -
CHEMBL3787664 1 -
CHEMBL3785832 1 -
CHEMBL3786952 1 -
CHEMBL3786579 1 -
CHEMBL3785470 1 -
CHEMBL3786617 1 -
CHEMBL3787438 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3786803 IC50 = 100.0 nM 7.00
CHEMBL3786225 IC50 = 100.0 nM 7.00
CHEMBL3786596 IC50 = 100.0 nM 7.00
CHEMBL3787548 IC50 = 100.0 nM 7.00
CHEMBL3785421 IC50 = 100.0 nM 7.00
CHEMBL3786108 IC50 = 1000.0 nM 6.00
CHEMBL3787133 IC50 < 100.0 nM -
CHEMBL3787664 IC50 < 100.0 nM -
CHEMBL3785832 IC50 < 100.0 nM -
CHEMBL3786952 IC50 < 100.0 nM -
CHEMBL3786579 IC50 < 100.0 nM -
CHEMBL3785470 IC50 < 100.0 nM -
CHEMBL3786617 IC50 < 100.0 nM -
CHEMBL3787438 IC50 < 100.0 nM -