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Assay Detail

CHEMBL4184878

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Binding
Inhibition of full length recombinant C-terminal His8-tagged human NAMPT using 15N-CONH2Nicotinamide as substrate preincubated for 15 mins followed by substrate addition measured after 90 mins by mass spectrometric analysis
6
Total Activities
6
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 design of nicotinamide phosphoribosyltransferase (NAMPT) inhibitors from a phenotypic screen.
Palacios DS, Meredith E, Kawanami T, Adams C, Chen X, Darsigny V, Geno E, Palermo M, Baird D, Boynton G, Busby SA, George EL, Guy C, Hewett J, Tierney L, Thigale S, Weihofen W, Wang L, White N, Yin M, Argikar UA.
Bioorg Med Chem Lett (2018) 28 : 365 -370
PubMed 29275937 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 8.12 8.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4206641 1 8.51
CHEMBL4213004 1 8.37
CHEMBL4211993 1 8.00
CHEMBL4215088 1 7.60
CHEMBL4205098 1 -
CHEMBL4215893 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4206641 IC50 = 3.1 nM 8.51
CHEMBL4213004 IC50 = 4.3 nM 8.37
CHEMBL4211993 IC50 = 10.0 nM 8.00
CHEMBL4215088 IC50 = 25.0 nM 7.60
CHEMBL4205098 IC50 < 1.0 nM -
CHEMBL4215893 IC50 > 2500.0 nM -