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Assay Detail

CHEMBL4425876

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

Binding
Inhibition of recombinant NAMPT (unknown origin) using nicotinamide as substrate measured every 5 mins for 30 mins in presence of recombinant NMNAT1
22
Total Activities
22
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 Potent Nicotinamide Phosphoribosyltransferase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.
Bai J, Liao C, Liu Y, Qin X, Chen J, Qiu Y, Qin D, Li Z, Tu ZC, Jiang S.
J Med Chem (2016) 59 : 5766 -5779
PubMed 27224875 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.67 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4544378 1 7.60
CHEMBL566757 DAPORINAD 2.0 1 7.50
CHEMBL4437678 1 7.28
CHEMBL4467850 1 7.26
CHEMBL4445749 1 7.17
CHEMBL4436777 1 7.08
CHEMBL4443275 1 7.00
CHEMBL4573977 1 6.92
CHEMBL4516235 1 6.83
CHEMBL4552050 1 6.74
CHEMBL4544855 1 6.71
CHEMBL4585844 1 6.67
CHEMBL4458686 1 6.54
CHEMBL4439790 1 6.44
CHEMBL4466939 1 6.42
CHEMBL4519620 1 6.26
CHEMBL4518730 1 6.15
CHEMBL4456190 1 6.15
CHEMBL4457097 1 6.11
CHEMBL4436253 1 6.06
CHEMBL4455440 1 6.00
CHEMBL4589960 1 5.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4544378 IC50 = 25.3 nM 7.60
CHEMBL566757 DAPORINAD IC50 = 32.0 nM 7.50
CHEMBL4437678 IC50 = 52.7 nM 7.28
CHEMBL4467850 IC50 = 54.8 nM 7.26
CHEMBL4445749 IC50 = 66.9 nM 7.17
CHEMBL4436777 IC50 = 82.5 nM 7.08
CHEMBL4443275 IC50 = 99.6 nM 7.00
CHEMBL4573977 IC50 = 120.0 nM 6.92
CHEMBL4516235 IC50 = 149.0 nM 6.83
CHEMBL4552050 IC50 = 181.0 nM 6.74
CHEMBL4544855 IC50 = 195.0 nM 6.71
CHEMBL4585844 IC50 = 213.0 nM 6.67
CHEMBL4458686 IC50 = 285.0 nM 6.54
CHEMBL4439790 IC50 = 362.0 nM 6.44
CHEMBL4466939 IC50 = 381.0 nM 6.42
CHEMBL4519620 IC50 = 544.0 nM 6.26
CHEMBL4518730 IC50 = 715.0 nM 6.15
CHEMBL4456190 IC50 = 702.0 nM 6.15
CHEMBL4457097 IC50 = 780.0 nM 6.11
CHEMBL4436253 IC50 = 873.0 nM 6.06
CHEMBL4455440 IC50 = 1000.0 nM 6.00
CHEMBL4589960 IC50 = 1410.0 nM 5.85