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Assay Detail

CHEMBL3100993

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

Binding
Inhibition of Nampt (unknown origin) using nicotinamide as substrate preincubated for 15 mins measured after 30 mins by mass spectrometry analysis
14
Total Activities
14
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

Discovery of potent and efficacious cyanoguanidine-containing nicotinamide phosphoribosyltransferase (Nampt) inhibitors.
Zheng X, Baumeister T, Buckmelter AJ, Caligiuri M, Clodfelter KH, Han B, Ho YC, Kley N, Lin J, Reynolds DJ, Sharma G, Smith CC, Wang Z, Dragovich PS, Oh A, Wang W, Zak M, Wang Y, Yuen PW, Bair KW.
Bioorg Med Chem Lett (2014) 24 : 337 -343
PubMed 24279990 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 8.50 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3098518 1 9.22
CHEMBL3098517 1 8.77
CHEMBL3098610 1 8.72
CHEMBL3098516 1 8.70
CHEMBL3098512 1 8.66
CHEMBL3098608 1 8.62
CHEMBL3098511 1 8.62
CHEMBL3098510 1 8.60
CHEMBL3098611 1 8.44
CHEMBL3098609 1 8.36
CHEMBL3098513 1 8.36
CHEMBL3098515 1 8.27
CHEMBL3098514 1 8.12
CHEMBL2419503 1 7.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3098518 IC50 = 0.6 nM 9.22
CHEMBL3098517 IC50 = 1.7 nM 8.77
CHEMBL3098610 IC50 = 1.9 nM 8.72
CHEMBL3098516 IC50 = 2.0 nM 8.70
CHEMBL3098512 IC50 = 2.2 nM 8.66
CHEMBL3098608 IC50 = 2.4 nM 8.62
CHEMBL3098511 IC50 = 2.4 nM 8.62
CHEMBL3098510 IC50 = 2.5 nM 8.60
CHEMBL3098611 IC50 = 3.6 nM 8.44
CHEMBL3098609 IC50 = 4.4 nM 8.36
CHEMBL3098513 IC50 = 4.4 nM 8.36
CHEMBL3098515 IC50 = 5.4 nM 8.27
CHEMBL3098514 IC50 = 7.5 nM 8.12
CHEMBL2419503 IC50 = 29.0 nM 7.54