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Assay Detail

CHEMBL3830868

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Binding
Inhibition of C-terminal His-tagged and C-terminal FLAG-tagged full length human recombinant HDAC1 expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate after 60 mins by fluorescence assay
14
Total Activities
12
Compounds Tested
2
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

Kinetic and structural insights into the binding of histone deacetylase 1 and 2 (HDAC1, 2) inhibitors.
Wagner FF, Weïwer M, Steinbacher S, Schomburg A, Reinemer P, Gale JP, Campbell AJ, Fisher SL, Zhao WN, Reis SA, Hennig KM, Thomas M, Müller P, Jefson MR, Fass DM, Haggarty SJ, Zhang YL, Holson EB.
Bioorg Med Chem (2016) 24 : 4008 -4015
PubMed 27377864 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.71 9.00
Ki 3 6.92 7.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL483254 PANOBINOSTAT 4.0 1 9.00
CHEMBL3828396 2 7.54
CHEMBL3827993 1 7.35
CHEMBL3827363 1 7.14
CHEMBL3827262 1 6.91
CHEMBL3827611 2 6.75
CHEMBL3827766 1 6.33
CHEMBL3827412 1 5.91
CHEMBL3828496 1 5.84
CHEMBL3827055 1 5.84
CHEMBL3828015 1 5.25
CHEMBL235842 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL483254 PANOBINOSTAT IC50 = 1.0 nM 9.00
CHEMBL3828396 IC50 = 29.0 nM 7.54
CHEMBL3827993 IC50 = 45.0 nM 7.35
CHEMBL3827363 IC50 = 72.0 nM 7.14
CHEMBL3828396 Ki = 84.0 nM 7.08
CHEMBL3827262 IC50 = 123.0 nM 6.91
CHEMBL3827611 Ki = 176.0 nM 6.75
CHEMBL3827611 IC50 = 192.0 nM 6.72
CHEMBL3827766 IC50 = 467.0 nM 6.33
CHEMBL3827412 IC50 = 1220.0 nM 5.91
CHEMBL3828496 IC50 = 1430.0 nM 5.84
CHEMBL3827055 IC50 = 1450.0 nM 5.84
CHEMBL3828015 IC50 = 5590.0 nM 5.25
CHEMBL235842 Ki < 0.2 nM -