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Assay Detail

CHEMBL2394700

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

Binding
Competitive inhibition of Nampt (unknown origin) after 15 mins in presence of 25 uM NAM
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

Structure-based identification of ureas as novel nicotinamide phosphoribosyltransferase (Nampt) inhibitors.
Zheng X, Bauer P, 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, Gunzner-Toste J, Zhao G, Yuen PW, Bair KW.
J Med Chem (2013) 56 : 4921 -4937
PubMed 23617784 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.15 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2391568 1 7.72
CHEMBL2391590 1 7.29
CHEMBL2391591 1 7.09
CHEMBL2391582 1 6.92
CHEMBL2391550 1 6.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2391568 IC50 = 19.0 nM 7.72
CHEMBL2391590 IC50 = 51.0 nM 7.29
CHEMBL2391591 IC50 = 82.0 nM 7.09
CHEMBL2391582 IC50 = 121.0 nM 6.92
CHEMBL2391550 IC50 = 195.0 nM 6.71