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Assay Detail

CHEMBL5658032

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

Binding
Inhibition of recombinant human C-terminal His-tagged HDAC3/NcoR2 using Boc-Lys-(Ac)-AMC as substrate measured after 60 mins by fluorescence assay
2
Total Activities
2
Compounds Tested
1
Activity Types
2
Assay Parameters

Assay Information

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

Publication

HDAC 3-selective inhibitor RGFP966 demonstrates anti-inflammatory properties in RAW 264.7 macrophages and mouse precision-cut lung slices by attenuating NF-κB p65 transcriptional activity.
Leus NG, van der Wouden PE, van den Bosch T, Hooghiemstra WTR, Ourailidou ME, Kistemaker LE, Bischoff R, Gosens R, Haisma HJ, Dekker FJ.
Biochem Pharmacol (2016) 108 : 58 -74
PubMed 26993378 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.00 7.31

Assay Parameters

Parameter Type Value Units Text
EFO_ID EFO_ID - EFO:0000341
EFO_TERM EFO_TERM - chronic obstructive pulmonary disease

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL98 VORINOSTAT 4.0 1 7.31
CHEMBL4078477 1 6.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL98 VORINOSTAT IC50 = 49.0 nM 7.31
CHEMBL4078477 IC50 = 210.0 nM 6.68