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Assay Detail

CHEMBL4327281

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

Binding
Inhibition of recombinant human HDAC4 using Boc-Lys(trifluoroacetyl)-AMC as substrate by homogeneous fluorescence release assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Histone deacetylase 4 (CHEMBL3524)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of novel quinazoline derivatives as potent antiplasmodial agents.
Bouchut A, Rotili D, Pierrot C, Valente S, Lafitte S, Schultz J, Hoglund U, Mazzone R, Lucidi A, Fabrizi G, Pechalrieu D, Arimondo PB, Skinner-Adams TS, Chua MJ, Andrews KT, Mai A, Khalife J.
Eur J Med Chem (2019) 161 : 277 -291
PubMed 30366254 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.62 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3110004 1 6.52
CHEMBL4550522 1 5.57
CHEMBL99 TRICHOSTATIN 1.0 1 5.42
CHEMBL4435005 1 4.96
CHEMBL4593437 1 -
CHEMBL4476057 1 -
CHEMBL4469596 1 -
CHEMBL4521590 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3110004 IC50 = 300.0 nM 6.52
CHEMBL4550522 IC50 = 2700.0 nM 5.57
CHEMBL99 TRICHOSTATIN IC50 = 3800.0 nM 5.42
CHEMBL4435005 IC50 = 11000.0 nM 4.96
CHEMBL4593437 IC50 > 50000.0 nM -
CHEMBL4476057 IC50 > 50000.0 nM -
CHEMBL4469596 IC50 > 50000.0 nM -
CHEMBL4521590 IC50 > 50000.0 nM -