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Assay Detail

CHEMBL5099291

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

Binding
Inhibition of HDAC6 (unknown origin)
27
Total Activities
27
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 6 (CHEMBL1865)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis and biological evaluation of novel pyrazinone derivatives as PI3K/HDAC dual inhibitors.
Wang ZX, Wang S, Qiao XP, Li WB, Shi JT, Wang YR, Chen SW.
Bioorg Med Chem (2022) 74 : 117067 -117067
PubMed 36272186 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 7.70 8.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5192159 1 8.38
CHEMBL5201448 1 8.38
CHEMBL5180796 1 8.35
CHEMBL5184950 1 8.16
CHEMBL5190763 1 8.13
CHEMBL5180870 1 8.10
CHEMBL5202725 1 8.04
CHEMBL5191006 1 7.92
CHEMBL5192044 1 7.89
CHEMBL5174437 1 7.89
CHEMBL5206969 1 7.85
CHEMBL5175778 1 7.85
CHEMBL5194733 1 7.82
CHEMBL5204426 1 7.82
CHEMBL5179687 1 7.82
CHEMBL5172884 1 7.70
CHEMBL5182660 1 7.68
CHEMBL5170590 1 7.64
CHEMBL5186022 1 7.52
CHEMBL5171575 1 7.50
CHEMBL5202781 1 7.46
CHEMBL5187051 1 7.27
CHEMBL98 VORINOSTAT 4.0 1 7.15
CHEMBL5183646 1 6.96
CHEMBL5185319 1 6.71
CHEMBL5172866 1 6.19
CHEMBL2017974 BUPARLISIB 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5192159 IC50 = 4.2 nM 8.38
CHEMBL5201448 IC50 = 4.2 nM 8.38
CHEMBL5180796 IC50 = 4.5 nM 8.35
CHEMBL5184950 IC50 = 6.9 nM 8.16
CHEMBL5190763 IC50 = 7.4 nM 8.13
CHEMBL5180870 IC50 = 7.9 nM 8.10
CHEMBL5202725 IC50 = 9.1 nM 8.04
CHEMBL5191006 IC50 = 12.0 nM 7.92
CHEMBL5192044 IC50 = 13.0 nM 7.89
CHEMBL5174437 IC50 = 13.0 nM 7.89
CHEMBL5206969 IC50 = 14.0 nM 7.85
CHEMBL5175778 IC50 = 14.0 nM 7.85
CHEMBL5194733 IC50 = 15.0 nM 7.82
CHEMBL5204426 IC50 = 15.0 nM 7.82
CHEMBL5179687 IC50 = 15.0 nM 7.82
CHEMBL5172884 IC50 = 20.0 nM 7.70
CHEMBL5182660 IC50 = 21.0 nM 7.68
CHEMBL5170590 IC50 = 23.0 nM 7.64
CHEMBL5186022 IC50 = 30.0 nM 7.52
CHEMBL5171575 IC50 = 32.0 nM 7.50
CHEMBL5202781 IC50 = 35.0 nM 7.46
CHEMBL5187051 IC50 = 54.0 nM 7.27
CHEMBL98 VORINOSTAT IC50 = 71.0 nM 7.15
CHEMBL5183646 IC50 = 109.0 nM 6.96
CHEMBL5185319 IC50 = 194.0 nM 6.71
CHEMBL5172866 IC50 = 650.0 nM 6.19
CHEMBL2017974 BUPARLISIB IC50 - -