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Assay Detail

CHEMBL4008461

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

Binding
Inhibition of recombinant mouse NAMPT expressed in bacterial expression system using nicotinamide as substrate after 1 hr by fluorescence based NMNAT-3 enzyme coupled assay
39
Total Activities
39
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 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 39 7.72 8.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4061448 1 8.51
CHEMBL4074848 1 8.42
CHEMBL566757 DAPORINAD 2.0 1 8.31
CHEMBL4066091 1 8.09
CHEMBL4078882 1 7.81
CHEMBL4083606 1 7.59
CHEMBL4101611 1 7.50
CHEMBL4088492 1 7.49
CHEMBL4064240 1 7.33
CHEMBL4094769 1 7.30
CHEMBL4087071 1 6.57
CHEMBL4070645 1 -
CHEMBL4078160 1 -
CHEMBL4096215 1 -
CHEMBL4086051 1 -
CHEMBL4103975 1 -
CHEMBL4093808 1 -
CHEMBL4095411 1 -
CHEMBL4101530 1 -
CHEMBL4103162 1 -
CHEMBL4097857 1 -
CHEMBL4079833 1 -
CHEMBL4089512 1 -
CHEMBL4068350 1 -
CHEMBL4097217 1 -
CHEMBL4079201 1 -
CHEMBL4104924 1 -
CHEMBL4067311 1 -
CHEMBL4091979 1 -
CHEMBL4099274 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4061448 IC50 = 3.1 nM 8.51
CHEMBL4074848 IC50 = 3.8 nM 8.42
CHEMBL566757 DAPORINAD IC50 = 4.9 nM 8.31
CHEMBL4066091 IC50 = 8.1 nM 8.09
CHEMBL4078882 IC50 = 15.6 nM 7.81
CHEMBL4083606 IC50 = 25.4 nM 7.59
CHEMBL4101611 IC50 = 31.3 nM 7.50
CHEMBL4088492 IC50 = 32.4 nM 7.49
CHEMBL4064240 IC50 = 47.0 nM 7.33
CHEMBL4094769 IC50 = 49.9 nM 7.30
CHEMBL4087071 IC50 = 269.0 nM 6.57
CHEMBL4103975 IC50 - -
CHEMBL4091075 IC50 - -
CHEMBL4086051 IC50 - -
CHEMBL4096215 IC50 - -
CHEMBL4078160 IC50 - -
CHEMBL4070645 IC50 - -
CHEMBL4067233 IC50 - -
CHEMBL4070595 IC50 - -
CHEMBL4098820 IC50 - -
CHEMBL4088652 IC50 - -
CHEMBL4060420 IC50 - -
CHEMBL4068019 IC50 - -
CHEMBL4083283 IC50 - -
CHEMBL4070110 IC50 - -
CHEMBL4093808 IC50 - -
CHEMBL4095411 IC50 - -
CHEMBL4101530 IC50 - -
CHEMBL4103162 IC50 - -
CHEMBL4097857 IC50 - -
CHEMBL4079833 IC50 - -
CHEMBL4089512 IC50 - -
CHEMBL4068350 IC50 - -
CHEMBL4097217 IC50 - -
CHEMBL4079201 IC50 - -
CHEMBL4104924 IC50 - -
CHEMBL4067311 IC50 - -
CHEMBL4091979 IC50 - -
CHEMBL4099274 IC50 - -