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Assay Detail

CHEMBL2319003

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

Binding
Inhibition of HDAC in cisplatin resistant human MDA-MB-231 cells after 18 hrs by fluorescence assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MDA-MB-231
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Histone deacetylase (CHEMBL2093865)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
Marek L, Hamacher A, Hansen FK, Kuna K, Gohlke H, Kassack MU, Kurz T.
J Med Chem (2013) 56 : 427 -436
PubMed 23252603 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.07 6.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2312168 1 6.39
CHEMBL98 VORINOSTAT 4.0 1 6.21
CHEMBL2312164 1 5.89
CHEMBL2312167 1 5.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2312168 IC50 = 410.0 nM 6.39
CHEMBL98 VORINOSTAT IC50 = 610.0 nM 6.21
CHEMBL2312164 IC50 = 1280.0 nM 5.89
CHEMBL2312167 IC50 = 1660.0 nM 5.78