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Assay Detail

CHEMBL4812286

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

Binding
Inhibition of human HDAC6 preincubated for 15 mins followed by substrate addition by fluorescence-based assay
24
Total Activities
24
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 brain penetrant benzazepine-based histone deacetylase 6 inhibitors for alleviating stroke-induced brain infarction.
Guo Z, Zhang Z, Zhang Y, Wang G, Huang Z, Zhang Q, Li J.
Eur J Med Chem (2021) 218 : 113383 -113383
PubMed 33799069 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 7.61 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4858994 1 8.74
CHEMBL4854123 1 8.25
CHEMBL4873296 1 8.21
CHEMBL4847454 1 8.19
CHEMBL4858810 1 8.19
CHEMBL2364628 RICOLINOSTAT 2.0 1 8.17
CHEMBL4875748 1 8.09
CHEMBL98 VORINOSTAT 4.0 1 7.92
CHEMBL4854768 1 7.92
CHEMBL4876815 1 7.89
CHEMBL4860396 1 7.85
CHEMBL4875969 1 7.85
CHEMBL4862139 1 7.72
CHEMBL4871812 1 7.66
CHEMBL4858918 1 7.54
CHEMBL4856735 1 7.43
CHEMBL4857891 1 7.37
CHEMBL4862419 1 7.35
CHEMBL4853358 1 7.00
CHEMBL4854716 1 6.96
CHEMBL4878252 1 6.89
CHEMBL4848981 1 6.59
CHEMBL4849884 1 6.50
CHEMBL4849225 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4858994 IC50 = 1.8 nM 8.74
CHEMBL4854123 IC50 = 5.6 nM 8.25
CHEMBL4873296 IC50 = 6.2 nM 8.21
CHEMBL4847454 IC50 = 6.4 nM 8.19
CHEMBL4858810 IC50 = 6.5 nM 8.19
CHEMBL2364628 RICOLINOSTAT IC50 = 6.8 nM 8.17
CHEMBL4875748 IC50 = 8.2 nM 8.09
CHEMBL98 VORINOSTAT IC50 = 12.0 nM 7.92
CHEMBL4854768 IC50 = 12.0 nM 7.92
CHEMBL4876815 IC50 = 13.0 nM 7.89
CHEMBL4860396 IC50 = 14.0 nM 7.85
CHEMBL4875969 IC50 = 14.0 nM 7.85
CHEMBL4862139 IC50 = 19.0 nM 7.72
CHEMBL4871812 IC50 = 22.0 nM 7.66
CHEMBL4858918 IC50 = 29.0 nM 7.54
CHEMBL4856735 IC50 = 37.0 nM 7.43
CHEMBL4857891 IC50 = 43.0 nM 7.37
CHEMBL4862419 IC50 = 45.0 nM 7.35
CHEMBL4853358 IC50 = 100.0 nM 7.00
CHEMBL4854716 IC50 = 111.0 nM 6.96
CHEMBL4878252 IC50 = 129.0 nM 6.89
CHEMBL4848981 IC50 = 255.0 nM 6.59
CHEMBL4849884 IC50 = 318.0 nM 6.50
CHEMBL4849225 IC50 = 497.0 nM 6.30