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Assay Detail

CHEMBL5044663

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

Binding
Inhibition of recombinant human N-terminal GST tagged HDAC6 expressed in baculovirus infected Sf9 insect cells 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
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histone deacetylase 6 (CHEMBL1865)
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 26 6.23 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL511749 1 7.75
CHEMBL5093832 1 7.51
CHEMBL5092352 1 7.32
CHEMBL5093602 1 7.17
CHEMBL5085871 1 7.12
CHEMBL5080669 1 6.23
CHEMBL5094432 1 6.21
CHEMBL5083767 1 6.21
CHEMBL5082644 1 6.19
CHEMBL5086629 1 6.15
CHEMBL5085919 1 6.12
CHEMBL5085234 1 6.11
CHEMBL5075320 1 6.10
CHEMBL98 VORINOSTAT 4.0 1 6.07
CHEMBL5076163 1 6.04
CHEMBL5093312 1 6.03
CHEMBL5077333 1 6.01
CHEMBL5069541 1 5.96
CHEMBL5079482 1 5.68
CHEMBL5077674 1 5.05
CHEMBL5070026 1 5.03
CHEMBL5079646 1 5.02
CHEMBL5081121 1 -
CHEMBL5072579 1 -
CHEMBL5078614 1 -
CHEMBL5078008 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL511749 IC50 = 18.0 nM 7.75
CHEMBL5093832 IC50 = 31.0 nM 7.51
CHEMBL5092352 IC50 = 48.0 nM 7.32
CHEMBL5093602 IC50 = 67.0 nM 7.17
CHEMBL5085871 IC50 = 76.0 nM 7.12
CHEMBL5080669 IC50 = 590.0 nM 6.23
CHEMBL5094432 IC50 = 610.0 nM 6.21
CHEMBL5083767 IC50 = 620.0 nM 6.21
CHEMBL5082644 IC50 = 650.0 nM 6.19
CHEMBL5086629 IC50 = 710.0 nM 6.15
CHEMBL5085919 IC50 = 760.0 nM 6.12
CHEMBL5085234 IC50 = 770.0 nM 6.11
CHEMBL5075320 IC50 = 800.0 nM 6.10
CHEMBL98 VORINOSTAT IC50 = 860.0 nM 6.07
CHEMBL5076163 IC50 = 910.0 nM 6.04
CHEMBL5093312 IC50 = 940.0 nM 6.03
CHEMBL5077333 IC50 = 970.0 nM 6.01
CHEMBL5069541 IC50 = 1090.0 nM 5.96
CHEMBL5079482 IC50 = 2100.0 nM 5.68
CHEMBL5077674 IC50 = 8810.0 nM 5.05
CHEMBL5070026 IC50 = 9330.0 nM 5.03
CHEMBL5079646 IC50 = 9530.0 nM 5.02
CHEMBL5081121 IC50 > 10000.0 nM -
CHEMBL5072579 IC50 > 10000.0 nM -
CHEMBL5078614 IC50 > 10000.0 nM -
CHEMBL5078008 IC50 > 10000.0 nM -