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Assay Detail

CHEMBL4236293

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

Binding
Inhibition of human recombinant HDAC10 using fluorogenic HDAC substrate after 45 mins by fluorimetrc method
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Polyamine deacetylase HDAC10 (CHEMBL5103)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma.
Fournier JF, Bhurruth-Alcor Y, Musicki B, Aubert J, Aurelly M, Bouix-Peter C, Bouquet K, Chantalat L, Delorme M, Drean B, Duvert G, Fleury-Bregeot N, Gauthier B, Grisendi K, Harris CS, Hennequin LF, Isabet T, Joly F, Lafitte G, Millois C, Morgentin R, Pascau J, Piwnica D, Rival Y, Soulet C, Thoreau É, Tomas L.
Bioorg Med Chem Lett (2018) 28 : 2985 -2992
PubMed 30122227 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 8.28 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4237803 1 8.92
CHEMBL4241370 1 8.52
CHEMBL2105763 QUISINOSTAT 2.0 1 8.36
CHEMBL483254 PANOBINOSTAT 4.0 1 8.29
CHEMBL4244764 1 7.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4237803 Ki = 1.2 nM 8.92
CHEMBL4241370 Ki = 3.0 nM 8.52
CHEMBL2105763 QUISINOSTAT Ki = 4.4 nM 8.36
CHEMBL483254 PANOBINOSTAT Ki = 5.1 nM 8.29
CHEMBL4244764 Ki = 50.0 nM 7.30