Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4768535

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

Binding
Inhibition of recombinant human full length C-terminal His-tagged HDAC8 expressed in sf9 insect cells using Boc-Lys(TFA)-AM as substrate incubated for 60 mins by fluorescence assay
23
Total Activities
23
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 8 (CHEMBL3192)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening.
Liu J,Zhou J,He F,Gao L,Wen Y,Gao L,Wang P,Kang D,Hu L
Eur J Med Chem (2020) 192 : 112189 -112189
PubMed 32151834 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 8.05 8.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4786031 1 8.62
CHEMBL4790137 1 8.52
CHEMBL4793650 1 8.49
CHEMBL4777182 1 8.48
CHEMBL4786350 1 8.48
CHEMBL4776328 1 8.47
CHEMBL4788954 1 8.44
CHEMBL4792980 1 8.42
CHEMBL4792567 1 8.40
CHEMBL4782066 1 8.39
CHEMBL4786063 1 8.38
CHEMBL4776974 1 8.36
CHEMBL4788942 1 8.36
CHEMBL4782988 1 8.35
CHEMBL4799886 1 8.31
CHEMBL4776599 1 8.14
CHEMBL4782327 1 7.90
CHEMBL4792025 1 7.61
CHEMBL4792705 1 7.49
CHEMBL4797623 1 7.39
CHEMBL98 VORINOSTAT 4.0 1 7.36
CHEMBL4779831 1 7.27
CHEMBL4784481 1 5.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4786031 IC50 = 2.4 nM 8.62
CHEMBL4790137 IC50 = 3.0 nM 8.52
CHEMBL4793650 IC50 = 3.2 nM 8.49
CHEMBL4777182 IC50 = 3.3 nM 8.48
CHEMBL4786350 IC50 = 3.3 nM 8.48
CHEMBL4776328 IC50 = 3.4 nM 8.47
CHEMBL4788954 IC50 = 3.6 nM 8.44
CHEMBL4792980 IC50 = 3.8 nM 8.42
CHEMBL4792567 IC50 = 4.0 nM 8.40
CHEMBL4782066 IC50 = 4.1 nM 8.39
CHEMBL4786063 IC50 = 4.2 nM 8.38
CHEMBL4776974 IC50 = 4.4 nM 8.36
CHEMBL4788942 IC50 = 4.4 nM 8.36
CHEMBL4782988 IC50 = 4.5 nM 8.35
CHEMBL4799886 IC50 = 4.9 nM 8.31
CHEMBL4776599 IC50 = 7.2 nM 8.14
CHEMBL4782327 IC50 = 12.6 nM 7.90
CHEMBL4792025 IC50 = 24.5 nM 7.61
CHEMBL4792705 IC50 = 32.5 nM 7.49
CHEMBL4797623 IC50 = 41.0 nM 7.39
CHEMBL98 VORINOSTAT IC50 = 44.0 nM 7.36
CHEMBL4779831 IC50 = 54.0 nM 7.27
CHEMBL4784481 IC50 = 3340.0 nM 5.48