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Assay Detail

CHEMBL3271333

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

Binding
Inhibition of C-terminal His-6-tagged full length human NAMPT expressed in Escherichia coli (DE3) cells after 30 mins by mass spectrometry-based analysis
29
Total Activities
29
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

Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
Zheng X, Bair KW, Bauer P, Baumeister T, Bowman KK, Buckmelter AJ, Caligiuri M, Clodfelter KH, Feng Y, Han B, Ho YC, Kley N, Li H, Liang X, Liederer BM, Lin J, Ly J, O'Brien T, Oeh J, Oh A, Reynolds DJ, Sampath D, Sharma G, Skelton N, Smith CC, Tremayne J, Wang L, Wang W, Wang Z, Wu H, Wu J, Xiao Y, Yang G, Yuen PW, Zak M, Dragovich PS.
Bioorg Med Chem Lett (2013) 23 : 5488 -5497
PubMed 24021463 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 7.17 8.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3260362 1 8.35
CHEMBL2420629 1 8.30
CHEMBL3260358 1 8.21
CHEMBL3260359 1 8.11
CHEMBL3260357 1 8.10
CHEMBL3260364 1 8.09
CHEMBL3260360 1 8.00
CHEMBL3260366 1 8.00
CHEMBL3260361 1 7.96
CHEMBL3260363 1 7.92
CHEMBL2420667 1 7.75
CHEMBL2420666 1 7.55
CHEMBL3260347 1 7.27
CHEMBL3260367 1 7.00
CHEMBL3260346 1 7.00
CHEMBL3260356 1 6.96
CHEMBL3260365 1 6.72
CHEMBL3260353 1 6.52
CHEMBL3260355 1 6.43
CHEMBL3259825 1 6.41
CHEMBL3260351 1 6.40
CHEMBL3260350 1 6.39
CHEMBL3260352 1 6.39
CHEMBL3260354 1 6.36
CHEMBL3260344 1 5.89
CHEMBL3260348 1 5.77
CHEMBL3260349 1 5.72
CHEMBL3260343 1 -
CHEMBL3260345 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3260362 IC50 = 4.5 nM 8.35
CHEMBL2420629 IC50 = 5.0 nM 8.30
CHEMBL3260358 IC50 = 6.1 nM 8.21
CHEMBL3260359 IC50 = 7.7 nM 8.11
CHEMBL3260357 IC50 = 7.9 nM 8.10
CHEMBL3260364 IC50 = 8.2 nM 8.09
CHEMBL3260360 IC50 = 10.0 nM 8.00
CHEMBL3260366 IC50 = 10.0 nM 8.00
CHEMBL3260361 IC50 = 11.0 nM 7.96
CHEMBL3260363 IC50 = 12.0 nM 7.92
CHEMBL2420667 IC50 = 18.0 nM 7.75
CHEMBL2420666 IC50 = 28.0 nM 7.55
CHEMBL3260347 IC50 = 54.0 nM 7.27
CHEMBL3260367 IC50 = 99.0 nM 7.00
CHEMBL3260346 IC50 = 100.0 nM 7.00
CHEMBL3260356 IC50 = 110.0 nM 6.96
CHEMBL3260365 IC50 = 190.0 nM 6.72
CHEMBL3260353 IC50 = 300.0 nM 6.52
CHEMBL3260355 IC50 = 370.0 nM 6.43
CHEMBL3259825 IC50 = 390.0 nM 6.41
CHEMBL3260351 IC50 = 400.0 nM 6.40
CHEMBL3260350 IC50 = 410.0 nM 6.39
CHEMBL3260352 IC50 = 410.0 nM 6.39
CHEMBL3260354 IC50 = 440.0 nM 6.36
CHEMBL3260344 IC50 = 1300.0 nM 5.89
CHEMBL3260348 IC50 = 1700.0 nM 5.77
CHEMBL3260349 IC50 = 1900.0 nM 5.72
CHEMBL3260343 IC50 > 2000.0 nM -
CHEMBL3260345 IC50 > 2000.0 nM -