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Assay Detail

CHEMBL4008463

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

Binding
Inhibition of NAMPT in human Jurkat T cells assessed as reduction in NAD levels
3
Total Activities
3
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

Nicotinamide phosphoribosyltransferase (CHEMBL1744525)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of Novel Triazole-Based Nicotinamide Phosphoribosyltransferase (NAMPT) Inhibitors Endowed with Antiproliferative and Antiinflammatory Activity.
Travelli C, Aprile S, Rahimian R, Grolla AA, Rogati F, Bertolotti M, Malagnino F, di Paola R, Impellizzeri D, Fusco R, Mercalli V, Massarotti A, Stortini G, Terrazzino S, Del Grosso E, Fakhfouri G, Troiani MP, Alisi MA, Grosa G, Sorba G, Canonico PL, Orsomando G, Cuzzocrea S, Genazzani AA, Galli U, Tron GC.
J Med Chem (2017) 60 : 1768 -1792
PubMed 28165742 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.20 8.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4061448 1 8.31
CHEMBL4074848 1 8.17
CHEMBL4066091 1 8.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4061448 IC50 = 4.9 nM 8.31
CHEMBL4074848 IC50 = 6.7 nM 8.17
CHEMBL4066091 IC50 = 7.8 nM 8.11