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Assay Detail

CHEMBL4346147

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

Binding
Inhibition of recombinant human C-terminal GST/His-tagged HDAC3 (1 to 428 residues) co-expressed with human N-terminal GST-tagged NCOR2 (395 to 489 residues) in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as substrate preincubated for 60 mins followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 7 — Homologous single protein target
Curated By Autocuration

Publication

Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity.
Li X, Jiang Y, Peterson YK, Xu T, Himes RA, Luo X, Yin G, Inks ES, Dolloff N, Halene S, Chan SSL, Chou CJ.
J Med Chem (2020) 63 : 5501 -5525
PubMed 32321249 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 9.14 9.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4444219 1 9.59
CHEMBL483254 PANOBINOSTAT 4.0 1 8.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4444219 IC50 = 0.2553 nM 9.59
CHEMBL483254 PANOBINOSTAT IC50 = 2.059 nM 8.69