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Assay Detail

CHEMBL2396471

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

Binding
Inhibition of NAMPT in human A2780 cells assessed as reduction in NAD level after 48 hrs by mass spectrophotometric analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type A2780
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Nicotinamide phosphoribosyltransferase (CHEMBL1744525)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of potent and efficacious urea-containing nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with reduced CYP2C9 inhibition properties.
Gunzner-Toste J, Zhao G, Bauer P, Baumeister T, Buckmelter AJ, Caligiuri M, Clodfelter KH, Fu B, Han B, Ho YC, Kley N, Liang X, Liederer BM, Lin J, Mukadam S, O'Brien T, Oh A, Reynolds DJ, Sharma G, Skelton N, Smith CC, Sodhi J, Wang W, Wang Z, Xiao Y, Yuen PW, Zak M, Zhang L, Zheng X, Bair KW, Dragovich PS.
Bioorg Med Chem Lett (2013) 23 : 3531 -3538
PubMed 23668988 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.52 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2393183 1 7.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2393183 IC50 = 30.0 nM 7.52