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Assay Detail

CHEMBL1015470

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

Binding
Inhibition of HDAC1/2 from human HeLa cells nuclear extract by cell free fluorimetric assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Histone deacetylase (HDAC1 and HDAC2) (CHEMBL2111429)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Non-peptide macrocyclic histone deacetylase inhibitors.
Oyelere AK, Chen PC, Guerrant W, Mwakwari SC, Hood R, Zhang Y, Fan Y.
J Med Chem (2009) 52 : 456 -468
PubMed 19093884 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 7.28 8.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL472250 1 8.72
CHEMBL455735 1 8.39
CHEMBL504040 1 7.97
CHEMBL506834 1 7.86
CHEMBL498908 1 7.43
CHEMBL501640 1 7.35
CHEMBL502430 1 7.25
CHEMBL455342 1 7.23
CHEMBL98 VORINOSTAT 4.0 1 7.19
CHEMBL507617 1 7.14
CHEMBL490446 1 7.05
CHEMBL446811 1 7.04
CHEMBL510806 AZITHROMYCINARYLALKYLHYDROXAMIC ACID 1 6.97
CHEMBL454025 DESCLASINOSE AZITHROMYCINARYLALKYL HYDROXAMATE 1 6.96
CHEMBL503113 1 6.91
CHEMBL509089 1 6.84
CHEMBL499994 1 6.77
CHEMBL452168 1 6.65
CHEMBL496761 1 6.64
CHEMBL505410 AZITHROMYCINARYLALKYL METHYL ESTER 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL472250 IC50 = 1.9 nM 8.72
CHEMBL455735 IC50 = 4.1 nM 8.39
CHEMBL504040 IC50 = 10.6 nM 7.97
CHEMBL506834 IC50 = 13.9 nM 7.86
CHEMBL498908 IC50 = 37.0 nM 7.43
CHEMBL501640 IC50 = 44.3 nM 7.35
CHEMBL502430 IC50 = 55.6 nM 7.25
CHEMBL455342 IC50 = 58.9 nM 7.23
CHEMBL98 VORINOSTAT IC50 = 65.0 nM 7.19
CHEMBL507617 IC50 = 72.4 nM 7.14
CHEMBL490446 IC50 = 88.8 nM 7.05
CHEMBL446811 IC50 = 91.6 nM 7.04
CHEMBL510806 AZITHROMYCINARYLALKYLHYDROXAMIC ACID IC50 = 107.1 nM 6.97
CHEMBL454025 DESCLASINOSE AZITHROMYCINARYLALKYL HYDROXAMATE IC50 = 109.8 nM 6.96
CHEMBL503113 IC50 = 123.0 nM 6.91
CHEMBL509089 IC50 = 145.5 nM 6.84
CHEMBL499994 IC50 = 169.8 nM 6.77
CHEMBL452168 IC50 = 223.4 nM 6.65
CHEMBL496761 IC50 = 226.7 nM 6.64
CHEMBL505410 AZITHROMYCINARYLALKYL METHYL ESTER IC50 - -