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Assay Detail

CHEMBL4048832

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

ADMET
Inhibition of recombinant human C-terminal His-tagged HDAC5 (656 to 1122 residues) expressed in baculovirus-infected insect cells using Boc-Lys(TFA)-AMC as substrate after 60 mins by fluorimeter
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histone deacetylase 5 (CHEMBL2563)
Type SINGLE PROTEIN
Organism Homo sapiens

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 6.61 7.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3110004 1 7.06
CHEMBL4087616 1 6.15
CHEMBL99 TRICHOSTATIN 1.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3110004 Ki = 86.9 nM 7.06
CHEMBL4087616 Ki = 701.0 nM 6.15
CHEMBL99 TRICHOSTATIN Ki - -