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Assay Detail

CHEMBL4737693

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

Binding
Inhibition of recombinant human HDAC8 using Ac-LGK(TFA)-AMC as substrate preincubated for 30 mins followed by substrate addition and measured after 90 mins by fluorescence based assay
6
Total Activities
6
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 8 (CHEMBL3192)
Type SINGLE PROTEIN
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 6 6.76 7.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4761013 1 7.15
CHEMBL4748500 1 7.14
CHEMBL4799406 1 7.06
CHEMBL191482 AR-42 2.0 1 6.77
CHEMBL4751615 1 5.68
CHEMBL356769 TUBACIN 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4761013 IC50 = 71.0 nM 7.15
CHEMBL4748500 IC50 = 72.0 nM 7.14
CHEMBL4799406 IC50 = 88.0 nM 7.06
CHEMBL191482 AR-42 IC50 = 170.0 nM 6.77
CHEMBL4751615 IC50 = 2100.0 nM 5.68
CHEMBL356769 TUBACIN IC50 - -