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Assay Detail

CHEMBL2427136

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

Binding
Inhibition of human recombinant HDAC6 expressed in baculovirus/sf9 cells using RHKKAc as substrate
22
Total Activities
22
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

Quinazolin-4-one derivatives as selective histone deacetylase-6 inhibitors for the treatment of Alzheimer's disease.
Yu CW, Chang PT, Hsin LW, Chern JW.
J Med Chem (2013) 56 : 6775 -6791
PubMed 23905680 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 7.47 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL99 TRICHOSTATIN 1.0 1 9.05
CHEMBL2425968 1 8.10
CHEMBL2425971 1 8.05
CHEMBL2425961 1 7.96
CHEMBL2425970 1 7.96
CHEMBL2425964 1 7.89
CHEMBL2425967 1 7.85
CHEMBL2425959 1 7.82
CHEMBL2018302 TUBASTATIN A 1 7.82
CHEMBL2425957 1 7.62
CHEMBL2425958 1 7.54
CHEMBL2425954 1 7.50
CHEMBL2425962 1 7.48
CHEMBL2425960 1 7.46
CHEMBL2425963 1 7.39
CHEMBL2425965 1 7.39
CHEMBL2425966 1 7.37
CHEMBL2425952 1 7.10
CHEMBL2425955 1 7.06
CHEMBL2425956 1 6.16
CHEMBL2425969 1 6.13
CHEMBL2425953 1 5.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL99 TRICHOSTATIN IC50 = 0.9 nM 9.05
CHEMBL2425968 IC50 = 8.0 nM 8.10
CHEMBL2425971 IC50 = 9.0 nM 8.05
CHEMBL2425961 IC50 = 11.0 nM 7.96
CHEMBL2425970 IC50 = 11.0 nM 7.96
CHEMBL2425964 IC50 = 13.0 nM 7.89
CHEMBL2425967 IC50 = 14.0 nM 7.85
CHEMBL2425959 IC50 = 15.0 nM 7.82
CHEMBL2018302 TUBASTATIN A IC50 = 15.0 nM 7.82
CHEMBL2425957 IC50 = 24.0 nM 7.62
CHEMBL2425958 IC50 = 29.0 nM 7.54
CHEMBL2425954 IC50 = 32.0 nM 7.50
CHEMBL2425962 IC50 = 33.0 nM 7.48
CHEMBL2425960 IC50 = 35.0 nM 7.46
CHEMBL2425963 IC50 = 41.0 nM 7.39
CHEMBL2425965 IC50 = 41.0 nM 7.39
CHEMBL2425966 IC50 = 43.0 nM 7.37
CHEMBL2425952 IC50 = 79.0 nM 7.10
CHEMBL2425955 IC50 = 88.0 nM 7.06
CHEMBL2425956 IC50 = 690.0 nM 6.16
CHEMBL2425969 IC50 = 747.0 nM 6.13
CHEMBL2425953 IC50 = 1920.0 nM 5.72