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Assay Detail

CHEMBL4048830

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

Binding
Inhibition of full length recombinant human C-terminal His-tagged HDAC3/N-terminal GST-tagged recombinant human NCOR2 (395 to 489 residues) expressed in baculovirus-infected insect cells using RHKK(Ac)AMC as substrate after 60 mins by fluorimeter
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Publication

Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors.
Sellmer A, Stangl H, Beyer M, Grünstein E, Leonhardt M, Pongratz H, Eichhorn E, Elz S, Striegl B, Jenei-Lanzl Z, Dove S, Straub RH, Krämer OH, Mahboobi S.
J Med Chem (2018) 61 : 3454 -3477
PubMed 29589441 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 7.80 9.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL99 TRICHOSTATIN 1.0 1 9.08
CHEMBL4087616 1 6.51
CHEMBL3110004 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL99 TRICHOSTATIN Ki = 0.84 nM 9.08
CHEMBL4087616 Ki = 306.0 nM 6.51
CHEMBL3110004 Ki - -