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Assay Detail

CHEMBL4770959

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

Binding
Inhibition of recombinant human HDAC6 using Z-(Ac)Lys-AMC as substrate after 90 mins by fluorescence based micro plate assay
6
Total Activities
6
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 dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1.
Ghazy E,Zeyen P,Herp D,Hügle M,Schmidtkunz K,Erdmann F,Robaa D,Schmidt M,Morales ER,Romier C,Günther S,Jung M,Sippl W
Eur J Med Chem (2020) 200 : 112338 -112338
PubMed 32497960 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.98 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4077645 1 8.22
CHEMBL4649617 1 7.85
CHEMBL4788940 1 6.82
CHEMBL4789481 1 6.46
CHEMBL3220922 1 6.38
CHEMBL4789607 1 6.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4077645 IC50 = 6.0 nM 8.22
CHEMBL4649617 IC50 = 14.0 nM 7.85
CHEMBL4788940 IC50 = 152.0 nM 6.82
CHEMBL4789481 IC50 = 344.0 nM 6.46
CHEMBL3220922 IC50 = 420.0 nM 6.38
CHEMBL4789607 IC50 = 709.0 nM 6.15