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Assay Detail

CHEMBL4729414

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

Binding
Inhibition of human recombinant HDAC6 using ZMAL (Z-Lys(Ac)-AMC) fluorogenic substrate incubated for 90 mins by fluorescence based assay
17
Total Activities
17
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

Multicomponent Synthesis, Binding Mode, and Structure-Activity Relationship of Selective Histone Deacetylase 6 (HDAC6) Inhibitors with Bifurcated Capping Groups.
Reßing N,Sönnichsen M,Osko JD,Schöler A,Schliehe-Diecks J,Skerhut A,Borkhardt A,Hauer J,Kassack MU,Christianson DW,Bhatia S,Hansen FK
J Med Chem (2020) 63 : 10339 -10351
PubMed 32803970 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.18 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2018302 TUBASTATIN A 1 7.85
CHEMBL2364628 RICOLINOSTAT 2.0 1 7.70
CHEMBL2179618 NEXTURASTAT A 1 7.70
CHEMBL4800426 1 7.52
CHEMBL4786332 1 7.52
CHEMBL98 VORINOSTAT 4.0 1 7.40
CHEMBL4781216 1 7.22
CHEMBL4748093 1 7.16
CHEMBL4740787 1 7.10
CHEMBL4066043 1 7.07
CHEMBL4752076 1 7.00
CHEMBL4780849 1 7.00
CHEMBL4754868 1 6.92
CHEMBL4760090 1 6.92
CHEMBL4756672 1 6.92
CHEMBL4761974 1 6.50
CHEMBL4754795 1 6.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2018302 TUBASTATIN A IC50 = 14.0 nM 7.85
CHEMBL2364628 RICOLINOSTAT IC50 = 20.0 nM 7.70
CHEMBL2179618 NEXTURASTAT A IC50 = 20.0 nM 7.70
CHEMBL4800426 IC50 = 30.0 nM 7.52
CHEMBL4786332 IC50 = 30.0 nM 7.52
CHEMBL98 VORINOSTAT IC50 = 40.0 nM 7.40
CHEMBL4781216 IC50 = 60.0 nM 7.22
CHEMBL4748093 IC50 = 70.0 nM 7.16
CHEMBL4740787 IC50 = 80.0 nM 7.10
CHEMBL4066043 IC50 = 85.0 nM 7.07
CHEMBL4752076 IC50 = 100.0 nM 7.00
CHEMBL4780849 IC50 = 100.0 nM 7.00
CHEMBL4754868 IC50 = 120.0 nM 6.92
CHEMBL4760090 IC50 = 120.0 nM 6.92
CHEMBL4756672 IC50 = 120.0 nM 6.92
CHEMBL4761974 IC50 = 320.0 nM 6.50
CHEMBL4754795 IC50 = 330.0 nM 6.48