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Assay Detail

CHEMBL5044661

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

Binding
Inhibition of recombinant human HDAC1 expressed in baculovirus expression system using Ac-Leu-Gly-Lys (Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence microtiter plate reader assay
14
Total Activities
14
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 1 (CHEMBL325)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Novel Histone Deacetylase 6 (HDAC6) Inhibitors with Enhanced Antitumor Immunity of Anti-PD-L1 Immunotherapy in Melanoma.
Peng X, Li L, Chen J, Ren Y, Liu J, Yu Z, Cao H, Chen J.
J Med Chem (2022) 65 : 2434 -2457
PubMed 35043615 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.47 7.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL98 VORINOSTAT 4.0 1 7.54
CHEMBL511749 1 6.58
CHEMBL5093832 1 5.50
CHEMBL5079482 1 5.49
CHEMBL5080669 1 5.41
CHEMBL5076163 1 5.36
CHEMBL5092352 1 5.33
CHEMBL5069541 1 5.30
CHEMBL5082644 1 5.29
CHEMBL5093602 1 5.03
CHEMBL5070026 1 5.01
CHEMBL5077674 1 4.98
CHEMBL5085871 1 4.95
CHEMBL5079646 1 4.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL98 VORINOSTAT IC50 = 29.0 nM 7.54
CHEMBL511749 IC50 = 260.0 nM 6.58
CHEMBL5093832 IC50 = 3190.0 nM 5.50
CHEMBL5079482 IC50 = 3210.0 nM 5.49
CHEMBL5080669 IC50 = 3930.0 nM 5.41
CHEMBL5076163 IC50 = 4340.0 nM 5.36
CHEMBL5092352 IC50 = 4660.0 nM 5.33
CHEMBL5069541 IC50 = 5030.0 nM 5.30
CHEMBL5082644 IC50 = 5130.0 nM 5.29
CHEMBL5093602 IC50 = 9320.0 nM 5.03
CHEMBL5070026 IC50 = 9790.0 nM 5.01
CHEMBL5077674 IC50 = 10430.0 nM 4.98
CHEMBL5085871 IC50 = 11210.0 nM 4.95
CHEMBL5079646 IC50 = 13520.0 nM 4.87