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Assay Detail

CHEMBL4737695

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

Binding
Inhibition of Class 1 histone deacetylase in human THP-1 cells using Ac-LGK(Ac)-AMC as substrate incubated for 3 hrs followed by 50 uM SAHA addition and measured after 1 hr by fluorescence based assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type THP-1
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Class 1 histone deacetylase (CHEMBL4523988)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

HDAC7 Inhibition by Phenacetyl and Phenylbenzoyl Hydroxamates.
Mak JYW,Wu KC,Gupta PK,Barbero S,McLaughlin MG,Lucke AJ,Tng J,Lim J,Loh Z,Sweet MJ,Reid RC,Liu L,Fairlie DP
J Med Chem (2021) 64 : 2186 -2204
PubMed 33570940 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.52 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL191482 AR-42 2.0 1 6.52
CHEMBL4748500 1 -
CHEMBL4799406 1 -
CHEMBL4761013 1 -
CHEMBL4751615 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL191482 AR-42 IC50 = 300.0 nM 6.52
CHEMBL4748500 IC50 > 30000.0 nM -
CHEMBL4799406 IC50 > 30000.0 nM -
CHEMBL4761013 IC50 > 30000.0 nM -
CHEMBL4751615 IC50 > 30000.0 nM -