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Assay Detail

CHEMBL3761048

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

Binding
Inhibition of HDAC in human HeLa cell nuclear extract using BML-KI104 Fluor de Lys as substrate by fluorescence-based assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HeLa
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Histone deacetylase (CHEMBL2093865)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Can Small Chemical Modifications of Natural Pan-inhibitors Modulate the Biological Selectivity? The Case of Curcumin Prenylated Derivatives Acting as HDAC or mPGES-1 Inhibitors.
Iranshahi M, Chini MG, Masullo M, Sahebkar A, Javidnia A, Chitsazian Yazdi M, Pergola C, Koeberle A, Werz O, Pizza C, Terracciano S, Piacente S, Bifulco G.
J Nat Prod (2015) 78 : 2867 -2879
PubMed 26588603 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.47 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL99 TRICHOSTATIN 1.0 1 8.85
CHEMBL3759529 1 4.08
CHEMBL3759749 1 -
CHEMBL3759699 1 -
CHEMBL3758656 1 -
CHEMBL3758253 1 -
CHEMBL3758791 1 -
CHEMBL3758432 1 -
CHEMBL3758528 1 -
CHEMBL1087807 1 -
CHEMBL1087690 1 -
CHEMBL140 CURCUMIN 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL99 TRICHOSTATIN IC50 = 1.42 nM 8.85
CHEMBL3759529 IC50 = 84200.0 nM 4.08
CHEMBL3759749 IC50 = 122000.0 nM -
CHEMBL3759699 IC50 = 786000.0 nM -
CHEMBL3758656 IC50 = 217000.0 nM -
CHEMBL3758253 IC50 = 188000.0 nM -
CHEMBL3758791 IC50 = 495000.0 nM -
CHEMBL3758432 IC50 - -
CHEMBL3758528 IC50 - -
CHEMBL1087807 IC50 = 347000.0 nM -
CHEMBL1087690 IC50 = 5620000.0 nM -
CHEMBL140 CURCUMIN IC50 = 187000.0 nM -