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Assay Detail

CHEMBL5100171

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

Binding
Inhibition of recombinant human C-terminal FLAG-tagged HDAC2 (1 to 488 residues) expressed in Sf9 insect cells using Z-Lys(Ac)-AMC as fluorogenic substrate incubated for 90 mins by microplate reader analysis
3
Total Activities
2
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 2 (CHEMBL1937)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of Fluorinated Peptoid-Based Histone Deacetylase (HDAC) Inhibitors for Therapy-Resistant Acute Leukemia.
Reßing N, Schliehe-Diecks J, Watson PR, Sönnichsen M, Cragin AD, Schöler A, Yang J, Schäker-Hübner L, Borkhardt A, Christianson DW, Bhatia S, Hansen FK.
J Med Chem (2022) 65 : 15457 -15472
PubMed 36351184 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.60 7.85
IC5 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5187433 2 7.85
CHEMBL5170634 1 5.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5187433 IC50 = 14.0 nM 7.85
CHEMBL5170634 IC50 = 4480.0 nM 5.35
CHEMBL5187433 IC5 = 0.014 uM -