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Assay Detail

CHEMBL2423680

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Binding
Inhibition of C-terminal His-tagged NAMPT (unknown origin) expressed in Escherichia coli BL21 using nicotinamide as substrate preincubated for 15 mins before substrate addition measured after 30 mins by mass spectrometry-based assay
60
Total Activities
60
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 discovery of novel amide-containing 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, Gunzner-Toste J, Liederer BM, Ly J, O'Brien T, Oh A, Wang L, Wang W, Xiao Y, Zak M, Zhao G, Yuen PW, Bair KW.
J Med Chem (2013) 56 : 6413 -6433
PubMed 23859118 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 60 7.52 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2420634 1 9.00
CHEMBL2420633 1 9.00
CHEMBL17289 CHS-828 1.0 1 8.70
CHEMBL2420638 1 8.70
CHEMBL2420632 1 8.70
CHEMBL2420628 1 8.52
CHEMBL2420627 1 8.52
CHEMBL2420626 1 8.52
CHEMBL2420625 1 8.52
CHEMBL566757 DAPORINAD 2.0 1 8.52
CHEMBL2420637 1 8.52
CHEMBL2420629 1 8.30
CHEMBL2420651 1 8.30
CHEMBL2420624 1 8.30
CHEMBL2420631 1 8.22
CHEMBL2420659 1 8.15
CHEMBL2420622 1 8.15
CHEMBL2420620 1 8.10
CHEMBL2420630 1 8.10
CHEMBL2420661 1 8.10
CHEMBL2420647 1 8.10
CHEMBL2420649 1 8.10
CHEMBL2420670 1 8.05
CHEMBL2420619 1 8.00
CHEMBL2420658 1 7.96
CHEMBL2420646 1 7.92
CHEMBL2420623 1 7.85
CHEMBL2419504 1 7.82
CHEMBL2420650 1 7.80
CHEMBL2420618 1 7.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2420634 IC50 = 1.0 nM 9.00
CHEMBL2420633 IC50 = 1.0 nM 9.00
CHEMBL2420638 IC50 = 2.0 nM 8.70
CHEMBL2420632 IC50 = 2.0 nM 8.70
CHEMBL17289 CHS-828 IC50 = 2.0 nM 8.70
CHEMBL2420628 IC50 = 3.0 nM 8.52
CHEMBL2420627 IC50 = 3.0 nM 8.52
CHEMBL2420626 IC50 = 3.0 nM 8.52
CHEMBL2420625 IC50 = 3.0 nM 8.52
CHEMBL566757 DAPORINAD IC50 = 3.0 nM 8.52
CHEMBL2420637 IC50 = 3.0 nM 8.52
CHEMBL2420629 IC50 = 5.0 nM 8.30
CHEMBL2420651 IC50 = 5.0 nM 8.30
CHEMBL2420624 IC50 = 5.0 nM 8.30
CHEMBL2420631 IC50 = 6.0 nM 8.22
CHEMBL2420659 IC50 = 7.0 nM 8.15
CHEMBL2420622 IC50 = 7.0 nM 8.15
CHEMBL2420620 IC50 = 8.0 nM 8.10
CHEMBL2420630 IC50 = 8.0 nM 8.10
CHEMBL2420661 IC50 = 8.0 nM 8.10
CHEMBL2420647 IC50 = 8.0 nM 8.10
CHEMBL2420649 IC50 = 8.0 nM 8.10
CHEMBL2420670 IC50 = 9.0 nM 8.05
CHEMBL2420619 IC50 = 10.0 nM 8.00
CHEMBL2420658 IC50 = 11.0 nM 7.96
CHEMBL2420646 IC50 = 12.0 nM 7.92
CHEMBL2420623 IC50 = 14.0 nM 7.85
CHEMBL2419504 IC50 = 15.0 nM 7.82
CHEMBL2420650 IC50 = 16.0 nM 7.80
CHEMBL2420618 IC50 = 17.0 nM 7.77
CHEMBL2420667 IC50 = 18.0 nM 7.75
CHEMBL2420621 IC50 = 21.0 nM 7.68
CHEMBL2420648 IC50 = 24.0 nM 7.62
CHEMBL2420666 IC50 = 28.0 nM 7.55
CHEMBL2419503 IC50 = 29.0 nM 7.54
CHEMBL2420664 IC50 = 37.0 nM 7.43
CHEMBL2420657 IC50 = 40.0 nM 7.40
CHEMBL2420645 IC50 = 41.0 nM 7.39
CHEMBL2420644 IC50 = 43.0 nM 7.37
CHEMBL2420656 IC50 = 140.0 nM 6.85
CHEMBL2420639 IC50 = 150.0 nM 6.82
CHEMBL2420660 IC50 = 150.0 nM 6.82
CHEMBL2420663 IC50 = 210.0 nM 6.68
CHEMBL2420665 IC50 = 310.0 nM 6.51
CHEMBL2420640 IC50 = 370.0 nM 6.43
CHEMBL2420662 IC50 = 400.0 nM 6.40
CHEMBL2420654 IC50 = 410.0 nM 6.39
CHEMBL2420642 IC50 = 610.0 nM 6.21
CHEMBL2420672 IC50 = 970.0 nM 6.01
CHEMBL2420673 IC50 = 1000.0 nM 6.00