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Assay Detail

CHEMBL5336081

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

Binding
Inhibition of full-length recombinant human NAMPT (2 to 491 residues) expressed in Escherichia coli using NAM as substrate preincubated for 5 mins followed by substrate addition measured after 15 mins by fluorescence based assay
5
Total Activities
5
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

Synthesis and structure-activity relationship of new nicotinamide phosphoribosyltransferase inhibitors with antitumor activity on solid and haematological cancer.
Fratta S, Biniecka P, Moreno-Vargas AJ, Carmona AT, Nahimana A, Duchosal MA, Piacente F, Bruzzone S, Caffa I, Nencioni A, Robina I.
Eur J Med Chem (2023) 250 : 115170 -115170
PubMed 36787658 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 8.06 8.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL566757 DAPORINAD 2.0 1 8.48
CHEMBL5428441 1 8.46
CHEMBL5416318 1 8.30
CHEMBL5421145 1 7.91
CHEMBL5396894 1 7.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL566757 DAPORINAD IC50 = 3.27 nM 8.48
CHEMBL5428441 IC50 = 3.5 nM 8.46
CHEMBL5416318 IC50 = 4.98 nM 8.30
CHEMBL5421145 IC50 = 12.45 nM 7.91
CHEMBL5396894 IC50 = 69.1 nM 7.16