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Assay Detail

CHEMBL4482120

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

Binding
Inhibition of HDAC1 (unknown origin) using Ac-Leu-GlyLys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence 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 1 (CHEMBL325)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis and activity evaluation of indole-based double - Branched HDAC1 inhibitors.
Zhang Q, Lv J, He F, Yu C, Qu Y, Zhang X, Xu A, Wu J.
Bioorg Med Chem (2019) 27 : 1595 -1604
PubMed 30879863 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 8.47 9.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4592929 1 9.04
CHEMBL408513 BELINOSTAT 4.0 1 8.86
CHEMBL4588104 1 8.66
CHEMBL4574697 1 8.23
CHEMBL4563800 1 8.06
CHEMBL4542734 1 7.99

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4592929 IC50 = 0.9177 nM 9.04
CHEMBL408513 BELINOSTAT IC50 = 1.376 nM 8.86
CHEMBL4588104 IC50 = 2.189 nM 8.66
CHEMBL4574697 IC50 = 5.929 nM 8.23
CHEMBL4563800 IC50 = 8.71 nM 8.06
CHEMBL4542734 IC50 = 10.31 nM 7.99