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Assay Detail

CHEMBL3755458

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

Binding
Inhibition of recombinant mouse NAMPT expressed in bacteria assessed as reduction in NADH formation using [14C]NAM as substrate measured for 1 hr by coupled enzymatic assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Nicotinamide phosphoribosyltransferase (CHEMBL3259474)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Identification of a novel NAMPT inhibitor by combinatorial click chemistry and chemical refinement
Theeramunkong S, Galli U, Grolla AA, Caldarelli A, Travelli C, Massarotti A, Troiani MP, Alisi MA, Orsomando G, Genazzani AA, Tron GC
Medchemcomm (2015) 6 : 1891 -1897
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.87 7.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL566757 DAPORINAD 2.0 1 7.21
CHEMBL3753643 1 6.94
CHEMBL3752157 1 6.77
CHEMBL3753517 1 6.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL566757 DAPORINAD IC50 = 61.0 nM 7.21
CHEMBL3753643 IC50 = 114.0 nM 6.94
CHEMBL3752157 IC50 = 170.0 nM 6.77
CHEMBL3753517 IC50 = 267.0 nM 6.57