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Assay Detail

CHEMBL5373345

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

Binding
Inhibition of HDAC6 in mouse LA-4 cells assessed as deacetylation of acetylated alpha-tubulin level incubated for 24 hrs by Western blot analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type LA-4
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histone deacetylase 6 (CHEMBL2878)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Selective and Bioavailable HDAC6 2-(Difluoromethyl)-1,3,4-oxadiazole Substrate Inhibitors and Modeling of Their Bioactivation Mechanism.
Ripa L, Sandmark J, Hughes G, Shamovsky I, Gunnarsson A, Johansson J, Llinas A, Collins M, Jung B, Novén A, Pemberton N, Mogemark M, Xiong Y, Li Q, Tångefjord S, Ek M, Åstrand A.
J Med Chem (2023) 66 : 14188 -14207
PubMed 37797307 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.20 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3935992 1 6.40
CHEMBL5429808 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3935992 IC50 = 398.11 nM 6.40
CHEMBL5429808 IC50 = 1000.0 nM 6.00