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Assay Detail

CHEMBL4019753

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

Binding
Inhibition of human recombinant HDAC3/GST tagged NCOR1 (397 to 503 residues) expressed in insect cells using Ac-Leu-Gly-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay
2
Total Activities
2
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

Target

Histone deacetylase 3/NCoR1 (CHEMBL3038484)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Small Molecule Inhibitors Simultaneously Targeting Cancer Metabolism and Epigenetics: Discovery of Novel Nicotinamide Phosphoribosyltransferase (NAMPT) and Histone Deacetylase (HDAC) Dual Inhibitors.
Dong G, Chen W, Wang X, Yang X, Xu T, Wang P, Zhang W, Rao Y, Miao C, Sheng C.
J Med Chem (2017) 60 : 7965 -7983
PubMed 28885834 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.51 7.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL98 VORINOSTAT 4.0 1 7.29
CHEMBL4065412 1 5.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL98 VORINOSTAT IC50 = 51.0 nM 7.29
CHEMBL4065412 IC50 = 1867.0 nM 5.73