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Assay Detail

CHEMBL4312389

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

Binding
Inhibition of human N-terminal tagged human HDAC6 expressed in HEK293T/17 using Ac-Gly-Ala-[Ac-Lys]-AMC as substrate preincubated for 10 mins followed by substrate addition and measured after 15 mins by fluorescence assay
2
Total Activities
2
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

Development of Multifunctional Histone Deacetylase 6 Degraders with Potent Antimyeloma Activity.
Wu H, Yang K, Zhang Z, Leisten ED, Li Z, Xie H, Liu J, Smith KA, Novakova Z, Barinka C, Tang W.
J Med Chem (2019) 62 : 7042 -7057
PubMed 31271281 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.24 8.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2179618 NEXTURASTAT A 1 8.42
CHEMBL4465902 1 8.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2179618 NEXTURASTAT A IC50 = 3.8 nM 8.42
CHEMBL4465902 IC50 = 8.7 nM 8.06