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Assay Detail

CHEMBL4134685

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

Binding
Inhibition of C-terminal His-tagged full length human HDAC2 expressed in baculovirus expression system using Ac-peptide substrate incubated for 15 mins by fluorescence based assay
6
Total Activities
6
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 2 (CHEMBL1937)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of tranylcypromine derivatives as novel LSD1/HDACs dual inhibitors for cancer treatment.
Duan YC, Ma YC, Qin WP, Ding LN, Zheng YC, Zhu YL, Zhai XY, Yang J, Ma CY, Guan YY.
Eur J Med Chem (2017) 140 : 392 -402
PubMed 28987602 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.83 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4173338 1 7.64
CHEMBL4166084 1 7.60
CHEMBL98 VORINOSTAT 4.0 1 7.55
CHEMBL4162637 1 6.38
CHEMBL4176702 1 6.31
CHEMBL4169910 1 5.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4173338 IC50 = 23.0 nM 7.64
CHEMBL4166084 IC50 = 25.0 nM 7.60
CHEMBL98 VORINOSTAT IC50 = 28.0 nM 7.55
CHEMBL4162637 IC50 = 413.0 nM 6.38
CHEMBL4176702 IC50 = 491.0 nM 6.31
CHEMBL4169910 IC50 = 3103.0 nM 5.51