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Assay Detail

CHEMBL3867190

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

Binding
Inhibition of NAMPT in human A2780 cells assessed as decrease in cell viability after 72 hrs by SRB assay
63
Total Activities
63
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type A2780
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Nicotinamide phosphoribosyltransferase (CHEMBL1744525)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Minimizing CYP2C9 Inhibition of Exposed-Pyridine NAMPT (Nicotinamide Phosphoribosyltransferase) Inhibitors.
Zak M, Yuen PW, Liu X, Patel S, Sampath D, Oeh J, Liederer BM, Wang W, O'Brien T, Xiao Y, Skelton N, Hua R, Sodhi J, Wang Y, Zhang L, Zhao G, Zheng X, Ho YC, Bair KW, Dragovich PS.
J Med Chem (2016) 59 : 8345 -8368
PubMed 27541271 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 63 7.97 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3968268 1 9.40
CHEMBL3916438 1 9.22
CHEMBL3948584 1 9.00
CHEMBL17289 CHS-828 1.0 1 9.00
CHEMBL566757 DAPORINAD 2.0 1 9.00
CHEMBL3986197 1 9.00
CHEMBL3963163 1 8.80
CHEMBL3893879 1 8.80
CHEMBL3958233 1 8.80
CHEMBL3913883 1 8.80
CHEMBL2420629 1 8.70
CHEMBL3983716 1 8.66
CHEMBL3984355 1 8.46
CHEMBL3923552 1 8.42
CHEMBL3974268 1 8.40
CHEMBL3260358 1 8.40
CHEMBL3939767 1 8.37
CHEMBL3925878 1 8.36
CHEMBL3948512 1 8.32
CHEMBL2420620 1 8.30
CHEMBL3914526 1 8.28
CHEMBL3889487 1 8.24
CHEMBL3394734 1 8.22
CHEMBL3127521 1 8.22
CHEMBL3897803 1 8.22
CHEMBL3949594 1 8.21
CHEMBL3940454 1 8.19
CHEMBL3904503 1 8.16
CHEMBL3921809 1 8.12
CHEMBL2419504 1 8.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3968268 IC50 = 0.4 nM 9.40
CHEMBL3916438 IC50 = 0.6 nM 9.22
CHEMBL17289 CHS-828 IC50 = 1.0 nM 9.00
CHEMBL566757 DAPORINAD IC50 = 1.0 nM 9.00
CHEMBL3986197 IC50 = 1.0 nM 9.00
CHEMBL3948584 IC50 = 1.0 nM 9.00
CHEMBL3963163 IC50 = 1.6 nM 8.80
CHEMBL3893879 IC50 = 1.6 nM 8.80
CHEMBL3958233 IC50 = 1.6 nM 8.80
CHEMBL3913883 IC50 = 1.6 nM 8.80
CHEMBL2420629 IC50 = 2.0 nM 8.70
CHEMBL3983716 IC50 = 2.2 nM 8.66
CHEMBL3984355 IC50 = 3.5 nM 8.46
CHEMBL3923552 IC50 = 3.8 nM 8.42
CHEMBL3260358 IC50 = 4.0 nM 8.40
CHEMBL3974268 IC50 = 4.0 nM 8.40
CHEMBL3939767 IC50 = 4.3 nM 8.37
CHEMBL3925878 IC50 = 4.4 nM 8.36
CHEMBL3948512 IC50 = 4.8 nM 8.32
CHEMBL2420620 IC50 = 5.0 nM 8.30
CHEMBL3914526 IC50 = 5.3 nM 8.28
CHEMBL3889487 IC50 = 5.8 nM 8.24
CHEMBL3394734 IC50 = 6.0 nM 8.22
CHEMBL3127521 IC50 = 6.0 nM 8.22
CHEMBL3897803 IC50 = 6.0 nM 8.22
CHEMBL3949594 IC50 = 6.2 nM 8.21
CHEMBL3940454 IC50 = 6.5 nM 8.19
CHEMBL3904503 IC50 = 6.9 nM 8.16
CHEMBL3921809 IC50 = 7.5 nM 8.12
CHEMBL2419504 IC50 = 9.0 nM 8.05
CHEMBL3394738 IC50 = 11.0 nM 7.96
CHEMBL2419515 IC50 = 11.0 nM 7.96
CHEMBL3913503 IC50 = 11.2 nM 7.95
CHEMBL2417572 IC50 = 13.0 nM 7.89
CHEMBL3932498 IC50 = 13.3 nM 7.88
CHEMBL2419505 IC50 = 15.0 nM 7.82
CHEMBL3908644 IC50 = 16.0 nM 7.80
CHEMBL3930755 IC50 = 20.7 nM 7.68
CHEMBL3941475 IC50 = 24.8 nM 7.61
CHEMBL3907541 IC50 = 27.0 nM 7.57
CHEMBL3977721 IC50 = 29.4 nM 7.53
CHEMBL3895553 IC50 = 31.2 nM 7.51
CHEMBL2391568 IC50 = 32.0 nM 7.50
CHEMBL3920776 IC50 = 34.0 nM 7.47
CHEMBL3921880 IC50 = 36.0 nM 7.44
CHEMBL3986623 IC50 = 58.0 nM 7.24
CHEMBL3972073 IC50 = 70.0 nM 7.16
CHEMBL2393183 IC50 = 70.0 nM 7.16
CHEMBL2393163 IC50 = 76.0 nM 7.12
CHEMBL3981065 IC50 = 101.0 nM 7.00