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Assay Detail

CHEMBL3129508

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

Binding
Inhibition of mouse HDAC6 expressed in human 293T cells using Ac-KGLGK(Ac)-MCA as substrate after 30 mins by fluorescence assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type 293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
Fukui Y, Narita K, Dan S, Yamori T, Ito A, Yoshida M, Katoh T.
Eur J Med Chem (2014) 76 : 301 -313
PubMed 24589486 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.04 6.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL343448 ROMIDEPSIN 4.0 1 6.41
CHEMBL1836142 THAILANDEPSIN A 1 6.00
CHEMBL3126833 1 5.70
CHEMBL3126831 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL343448 ROMIDEPSIN IC50 = 390.0 nM 6.41
CHEMBL1836142 THAILANDEPSIN A IC50 = 992.0 nM 6.00
CHEMBL3126833 IC50 = 1975.0 nM 5.70
CHEMBL3126831 IC50 > 10000.0 nM -