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Assay Detail

CHEMBL4823888

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

Binding
Inhibition of recombinant human HDAC6 using Ac-GAK(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition and measured after 30 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

Tetrahydroquinoline-Capped Histone Deacetylase 6 Inhibitor SW-101 Ameliorates Pathological Phenotypes in a Charcot-Marie-Tooth Type 2A Mouse Model.
Shen S, Picci C, Ustinova K, Benoy V, Kutil Z, Zhang G, Tavares MT, Pavlíček J, Zimprich CA, Robers MB, Van Den Bosch L, Bařinka C, Langley B, Kozikowski AP.
J Med Chem (2021) 64 : 4810 -4840
PubMed 33830764 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 8.65 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4863515 1 9.52
CHEMBL4536605 1 9.30
CHEMBL4846435 1 9.15
CHEMBL4846714 1 9.10
CHEMBL4857825 1 9.05
CHEMBL4856735 1 9.00
CHEMBL4874875 1 8.89
CHEMBL2179618 NEXTURASTAT A 1 8.80
CHEMBL4847663 1 8.62
CHEMBL4847122 1 8.57
CHEMBL4859648 1 8.54
CHEMBL4856920 1 8.34
CHEMBL4847454 1 8.30
CHEMBL98 VORINOSTAT 4.0 1 8.17
CHEMBL4856207 1 8.05
CHEMBL4873778 1 7.92
CHEMBL4866436 1 7.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4863515 IC50 = 0.3 nM 9.52
CHEMBL4536605 IC50 = 0.5 nM 9.30
CHEMBL4846435 IC50 = 0.7 nM 9.15
CHEMBL4846714 IC50 = 0.8 nM 9.10
CHEMBL4857825 IC50 = 0.9 nM 9.05
CHEMBL4856735 IC50 = 1.0 nM 9.00
CHEMBL4874875 IC50 = 1.3 nM 8.89
CHEMBL2179618 NEXTURASTAT A IC50 = 1.6 nM 8.80
CHEMBL4847663 IC50 = 2.4 nM 8.62
CHEMBL4847122 IC50 = 2.7 nM 8.57
CHEMBL4859648 IC50 = 2.9 nM 8.54
CHEMBL4856920 IC50 = 4.6 nM 8.34
CHEMBL4847454 IC50 = 5.0 nM 8.30
CHEMBL98 VORINOSTAT IC50 = 6.7 nM 8.17
CHEMBL4856207 IC50 = 9.0 nM 8.05
CHEMBL4873778 IC50 = 12.0 nM 7.92
CHEMBL4866436 IC50 = 17.0 nM 7.77