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Assay Detail

CHEMBL4828677

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

Binding
Inhibition of recombinant human C-terminal His-tagged HDAC1 expressed in Sf9 insect cells using Fluor de Lys deacetylase or Fluor de Lys Green deacetylase as substrate by fluorescent microplate reader assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histone deacetylase 1 (CHEMBL325)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Role of Fluorination in the Histone Deacetylase 6 (HDAC6) Selectivity of Benzohydroxamate-Based Inhibitors.
Sandrone G, Cukier CD, Zrubek K, Marchini M, Vergani B, Caprini G, Fossati G, Steinkühler C, Stevenazzi A.
ACS Med Chem Lett (2021) 12 : 1810 -1817
PubMed 34795871 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 5.33 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1213492 GIVINOSTAT 4.0 1 7.16
CHEMBL4870227 1 6.14
CHEMBL4448410 1 6.03
CHEMBL4453121 1 6.03
CHEMBL4448978 1 5.72
CHEMBL4852256 1 5.51
CHEMBL4862508 1 5.49
CHEMBL4470373 1 5.40
CHEMBL154302 1 5.25
CHEMBL4873055 1 5.17
CHEMBL4862563 1 5.15
CHEMBL155579 1 5.15
CHEMBL4869421 1 5.13
CHEMBL4864065 1 5.01
CHEMBL4877419 1 4.94
CHEMBL4863455 1 4.86
CHEMBL4851389 1 4.80
CHEMBL16300 BENZOHYDROXAMATE 1 4.60
CHEMBL4850382 1 4.53
CHEMBL504369 NICOXAMAT 2.0 1 4.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1213492 GIVINOSTAT IC50 = 70.0 nM 7.16
CHEMBL4870227 IC50 = 718.0 nM 6.14
CHEMBL4448410 IC50 = 924.0 nM 6.03
CHEMBL4453121 IC50 = 930.0 nM 6.03
CHEMBL4448978 IC50 = 1914.0 nM 5.72
CHEMBL4852256 IC50 = 3064.0 nM 5.51
CHEMBL4862508 IC50 = 3211.0 nM 5.49
CHEMBL4470373 IC50 = 3960.0 nM 5.40
CHEMBL154302 IC50 = 5642.0 nM 5.25
CHEMBL4873055 IC50 = 6825.0 nM 5.17
CHEMBL4862563 IC50 = 7093.0 nM 5.15
CHEMBL155579 IC50 = 7138.0 nM 5.15
CHEMBL4869421 IC50 = 7394.0 nM 5.13
CHEMBL4864065 IC50 = 9710.0 nM 5.01
CHEMBL4877419 IC50 = 11378.0 nM 4.94
CHEMBL4863455 IC50 = 13812.0 nM 4.86
CHEMBL4851389 IC50 = 15797.0 nM 4.80
CHEMBL16300 BENZOHYDROXAMATE IC50 = 25380.0 nM 4.60
CHEMBL4850382 IC50 = 29367.0 nM 4.53
CHEMBL504369 NICOXAMAT IC50 = 34958.0 nM 4.46