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Assay Detail

CHEMBL4737696

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

Binding
Inhibition of Class 2a histone deacetylase in human THP-1 cells using Ac-LGK(TFA)-AMC as substrate incubated for 3 hrs followed by 50 uM SAHA addition and measured after 1 hr by fluorescence based assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type THP-1
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 4 6.27 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4748500 1 6.52
CHEMBL4799406 1 6.52
CHEMBL4761013 1 6.52
CHEMBL4751615 1 5.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4748500 IC50 = 300.0 nM 6.52
CHEMBL4799406 IC50 = 300.0 nM 6.52
CHEMBL4761013 IC50 = 300.0 nM 6.52
CHEMBL4751615 IC50 = 3000.0 nM 5.52