Page last updated: 2024-11-13

gne-617

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Description

GNE-617: inhibits nicotinamide phosphoribosyltransferase; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID68277611
CHEMBL ID2420629
SCHEMBL ID12468183
MeSH IDM000597237

Synonyms (28)

Synonym
n-{4-[(3,5-difluorophenyl)sulfonyl]benzyl}imidazo[1,2-a]pyridine-6-carboxamide
S6629
SCHEMBL12468183
gne-617
bdbm50438936
chembl2420629 ,
CS-1695
HY-15766
1362154-70-8
4O28
AKOS030526453
n-{[4-(3,5-difluorobenzenesulfonyl)phenyl]methyl}imidazo[1,2-a]pyridine-6-carboxamide
NCGC00378624-01
BCP20092
gne617;gne 617
n-[[4-(3,5-difluorophenyl)sulfonylphenyl]methyl]imidazo[1,2-a]pyridine-6-carboxamide
EX-A2304
BS-15263
gne 617
n-(4-((3,5-difluorophenyl)sulfonyl)benzyl)imidazo[1,2-a]pyridine-6-carboxamide
gne617
Q27452357
C72455
n-[[4-[(3,5-difluorophenyl)sulfonyl]phenyl]methyl]imidazo[1,2-a]pyridine-6-carboxamide
A911828
nsc779407
nsc-779407
AC-35459

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (10)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency1.34500.01237.983543.2770AID1645841
cytochrome P450 2D6Homo sapiens (human)Potency26.83700.00108.379861.1304AID1645840
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cytochrome P450 1A2Homo sapiens (human)IC50 (µMol)0.00200.00011.774010.0000AID1327638
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)0.00200.00011.753610.0000AID1327638
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)0.00200.00002.800510.0000AID1327638
Cytochrome P450 2C19Homo sapiens (human)IC50 (µMol)0.00200.00002.398310.0000AID1327638
Nicotinamide phosphoribosyltransferaseHomo sapiens (human)IC50 (µMol)0.00440.00010.07102.1000AID1137960; AID1327637; AID1327638; AID1800299; AID765316
Nicotinamide phosphoribosyltransferase Rattus norvegicus (Norway rat)IC50 (µMol)0.02300.02300.02900.0350AID1137983
Nicotinamide phosphoribosyltransferaseMus musculus (house mouse)IC50 (µMol)0.02400.00270.02270.0590AID1137982
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Adenosine receptor A2aRattus norvegicus (Norway rat)EC50 (µMol)0.00120.00000.11560.7200AID1137987; AID1137989
Nicotinamide phosphoribosyltransferaseHomo sapiens (human)EC50 (µMol)0.00110.00110.00120.0012AID1137989
Nicotinamide phosphoribosyltransferaseMus musculus (house mouse)EC50 (µMol)0.00130.00130.03570.0700AID1137987
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (47)

Processvia Protein(s)Taxonomy
steroid catabolic processCytochrome P450 1A2Homo sapiens (human)
porphyrin-containing compound metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 1A2Homo sapiens (human)
cholesterol metabolic processCytochrome P450 1A2Homo sapiens (human)
estrogen metabolic processCytochrome P450 1A2Homo sapiens (human)
toxin biosynthetic processCytochrome P450 1A2Homo sapiens (human)
post-embryonic developmentCytochrome P450 1A2Homo sapiens (human)
alkaloid metabolic processCytochrome P450 1A2Homo sapiens (human)
regulation of gene expressionCytochrome P450 1A2Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 1A2Homo sapiens (human)
dibenzo-p-dioxin metabolic processCytochrome P450 1A2Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
lung developmentCytochrome P450 1A2Homo sapiens (human)
methylationCytochrome P450 1A2Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 1A2Homo sapiens (human)
retinol metabolic processCytochrome P450 1A2Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 1A2Homo sapiens (human)
cellular respirationCytochrome P450 1A2Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 1A2Homo sapiens (human)
hydrogen peroxide biosynthetic processCytochrome P450 1A2Homo sapiens (human)
oxidative demethylationCytochrome P450 1A2Homo sapiens (human)
cellular response to cadmium ionCytochrome P450 1A2Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C9 Homo sapiens (human)
steroid metabolic processCytochrome P450 2C9 Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2C9 Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C9 Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C9 Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
urea metabolic processCytochrome P450 2C9 Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 2C9 Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
amide metabolic processCytochrome P450 2C9 Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
oxidative demethylationCytochrome P450 2C9 Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid metabolic processCytochrome P450 2C19Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C19Homo sapiens (human)
steroid metabolic processCytochrome P450 2C19Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C19Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C19Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
insulin receptor signaling pathwayNicotinamide phosphoribosyltransferaseHomo sapiens (human)
adipose tissue developmentNicotinamide phosphoribosyltransferaseHomo sapiens (human)
signal transductionNicotinamide phosphoribosyltransferaseHomo sapiens (human)
cell-cell signalingNicotinamide phosphoribosyltransferaseHomo sapiens (human)
positive regulation of cell population proliferationNicotinamide phosphoribosyltransferaseHomo sapiens (human)
circadian regulation of gene expressionNicotinamide phosphoribosyltransferaseHomo sapiens (human)
NAD biosynthesis via nicotinamide riboside salvage pathwayNicotinamide phosphoribosyltransferaseHomo sapiens (human)
positive regulation of transcription by RNA polymerase IINicotinamide phosphoribosyltransferaseHomo sapiens (human)
positive regulation of nitric-oxide synthase biosynthetic processNicotinamide phosphoribosyltransferaseHomo sapiens (human)
NAD biosynthetic processNicotinamide phosphoribosyltransferaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (38)

Processvia Protein(s)Taxonomy
monooxygenase activityCytochrome P450 1A2Homo sapiens (human)
iron ion bindingCytochrome P450 1A2Homo sapiens (human)
protein bindingCytochrome P450 1A2Homo sapiens (human)
electron transfer activityCytochrome P450 1A2Homo sapiens (human)
oxidoreductase activityCytochrome P450 1A2Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 1A2Homo sapiens (human)
enzyme bindingCytochrome P450 1A2Homo sapiens (human)
heme bindingCytochrome P450 1A2Homo sapiens (human)
demethylase activityCytochrome P450 1A2Homo sapiens (human)
caffeine oxidase activityCytochrome P450 1A2Homo sapiens (human)
aromatase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
hydroperoxy icosatetraenoate dehydratase activityCytochrome P450 1A2Homo sapiens (human)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
iron ion bindingCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C9 Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
aromatase activityCytochrome P450 2C9 Homo sapiens (human)
heme bindingCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C9 Homo sapiens (human)
G protein-coupled adenosine receptor activityAdenosine receptor A2aRattus norvegicus (Norway rat)
monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
iron ion bindingCytochrome P450 2C19Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxygen bindingCytochrome P450 2C19Homo sapiens (human)
enzyme bindingCytochrome P450 2C19Homo sapiens (human)
heme bindingCytochrome P450 2C19Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
aromatase activityCytochrome P450 2C19Homo sapiens (human)
long-chain fatty acid omega-1 hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C19Homo sapiens (human)
cytokine activityNicotinamide phosphoribosyltransferaseHomo sapiens (human)
protein bindingNicotinamide phosphoribosyltransferaseHomo sapiens (human)
identical protein bindingNicotinamide phosphoribosyltransferaseHomo sapiens (human)
nicotinamide phosphoribosyltransferase activityNicotinamide phosphoribosyltransferaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (9)

Processvia Protein(s)Taxonomy
endoplasmic reticulum membraneCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C9 Homo sapiens (human)
plasma membraneCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
cytoplasmCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
Golgi membraneAdenosine receptor A2aRattus norvegicus (Norway rat)
endoplasmic reticulum membraneCytochrome P450 2C19Homo sapiens (human)
plasma membraneCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
cytoplasmCytochrome P450 2C19Homo sapiens (human)
cytosolNicotinamide phosphoribosyltransferaseHomo sapiens (human)
nuclear speckNicotinamide phosphoribosyltransferaseHomo sapiens (human)
cell junctionNicotinamide phosphoribosyltransferaseHomo sapiens (human)
extracellular exosomeNicotinamide phosphoribosyltransferaseHomo sapiens (human)
cytosolNicotinamide phosphoribosyltransferaseMus musculus (house mouse)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (74)

Assay IDTitleYearJournalArticle
AID1137982Inhibition of mouse NAMPT after 30 mins by mass spectrometry-based analysis2013Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
AID765301Tmax in NCR nude mouse at 10 mg/kg, po2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Structure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (nampt) inhibitors.
AID1137999Antiproliferative activity against mouse KPR cells assessed as cell viability after 96 hrs by CyQuant staining-based assay2013Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
AID1190263Time-dependent inhibition of CYP3A4 (unknown origin) using midazolam as substrate assessed as AUC shift2015Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
Identification of nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with no evidence of CYP3A4 time-dependent inhibition and improved aqueous solubility.
AID1137984Cellular uptake in mouse KPP cells at 1000 nM2013Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
AID1327684Reversible inhibition of CYP2C9 in human liver microsomes using diclofenac as substrate in presence of NADPH by LC-MS/MS analysis2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Minimizing CYP2C9 Inhibition of Exposed-Pyridine NAMPT (Nicotinamide Phosphoribosyltransferase) Inhibitors.
AID765295Antitumor activity against human U251 cells xenografted in athymic nu/nu mouse assessed as reduction in tumor size at 25 mg/kg, po QD for 7 days measured on day 132013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Structure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (nampt) inhibitors.
AID1137974Drug uptake in Sprague-Dawley rat retina at 30 mg/kg, po qd for 2 days measured 1 hr after last dose in presence of nicotinic acid2013Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
AID765313Metabolic stability in human liver microsomes assessed as compound remaining at 1 uM after 30 mins LC-MS analysis2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Structure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (nampt) inhibitors.
AID1137995Antiproliferative activity against human MIAPaCa2 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay2013Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
AID1190265Kinetic solubility of the compound in aqueous buffer at pH 7.4 after 24 hrs2015Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
Identification of nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with no evidence of CYP3A4 time-dependent inhibition and improved aqueous solubility.
AID1137994Antiproliferative activity against human PC3 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay2013Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
AID1327639Reversible inhibition of CYP2C9 in human liver microsomes using (S)-warfarin as substrate in presence of NADPH by LC-MS/MS analysis2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Minimizing CYP2C9 Inhibition of Exposed-Pyridine NAMPT (Nicotinamide Phosphoribosyltransferase) Inhibitors.
AID1190266Thermodynamic solubility of the compound in aqueous buffer at pH 7.4 after 24 hrs2015Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
Identification of nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with no evidence of CYP3A4 time-dependent inhibition and improved aqueous solubility.
AID1137997Antiproliferative activity against human Calu6 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay2013Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
AID765312Intrinsic clearance in CD-1 mouse hepatocytes at 1 uM after 10 mins by LC-MS/MS analysis2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Structure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (nampt) inhibitors.
AID765300Clearance in NCR nude mouse plasma at 5 mg/kg, iv2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Structure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (nampt) inhibitors.
AID1137960Inhibition of C-terminal His-6-tagged full length human NAMPT expressed in Escherichia coli (DE3) cells after 30 mins by mass spectrometry-based analysis2013Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
AID765303Antiproliferative activity against human HCT116 cells assessed as cell viability after 72 hrs2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Structure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (nampt) inhibitors.
AID1327640Inhibition of CYP3A4 in human liver microsomes using testosterone as substrate in presence of NADPH by LC-MS/MS analysis2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Minimizing CYP2C9 Inhibition of Exposed-Pyridine NAMPT (Nicotinamide Phosphoribosyltransferase) Inhibitors.
AID1138000Antiproliferative activity against mouse B16F10 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay2013Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
AID1327643Inhibition of CYP1A2 in human liver microsomes using tacrine as substrate in presence of NADPH by LC-MS/MS analysis2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Minimizing CYP2C9 Inhibition of Exposed-Pyridine NAMPT (Nicotinamide Phosphoribosyltransferase) Inhibitors.
AID1137996Antiproliferative activity against human HCT116 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay2013Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
AID1137979Ratio of drug level in retina to plasma of Sprague-Dawley rat at 30 mg/kg, po qd for 2 days measured 6.5 hrs after last dose in presence of nicotinic acid2013Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
AID765296Toxicity in human U251 cells xenografted in athymic nu/nu mouse assessed as change in body weight at 25 mg/kg, po QD for 7 days2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Structure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (nampt) inhibitors.
AID765305Antiproliferative activity against human MIAPaCa2 cells assessed as cell viability after 72 hrs2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Structure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (nampt) inhibitors.
AID1327644Inhibition of CYP2C19 in human liver microsomes using mephenytoin as substrate in presence of NADPH by LC-MS/MS analysis2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Minimizing CYP2C9 Inhibition of Exposed-Pyridine NAMPT (Nicotinamide Phosphoribosyltransferase) Inhibitors.
AID1137975Drug uptake in Sprague-Dawley rat retina at 30 mg/kg, po qd for 2 days measured 6.5 hrs after last dose in presence of nicotinic acid2013Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
AID1137983Inhibition of rat NAMPT after 30 mins by mass spectrometry-based analysis2013Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
AID1137990Cytotoxicity against rhesus monkey RF/6A cells assessed as cell viability after 96 hrs by CyQuant staining-based assay2013Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
AID1137992Inhibition of C-terminal His-6-tagged cynomolgus monkey NAMPT expressed in Escherichia coli (DE3)-RIL cells after 30 mins by mass spectrometry-based analysis2013Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
AID1138007Dissociation constant, pKa of the compound2013Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
AID1327642Inhibition of CYP2D6 in human liver microsomes using dextromethorphan as substrate in presence of NADPH by LC-MS/MS analysis2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Minimizing CYP2C9 Inhibition of Exposed-Pyridine NAMPT (Nicotinamide Phosphoribosyltransferase) Inhibitors.
AID1137963Fraction unbound in mouse plasma at 5 uM by LC-MS/MS analysis2013Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
AID1138008Octanol-PBS buffer distribution coefficient, log D of the compound at pH 7.4 by shake flask method2013Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
AID1137991Inhibition of C-terminal His-6-tagged dog NAMPT expressed in Escherichia coli (DE3)-RIL cells after 30 mins by mass spectrometry-based analysis2013Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
AID765299Volume of distribution at steady state in NCR nude mouse at 5 mg/kg, iv2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Structure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (nampt) inhibitors.
AID1327638Inhibition of NAMPT in human A2780 cells assessed as decrease in cell viability after 72 hrs by SRB assay2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Minimizing CYP2C9 Inhibition of Exposed-Pyridine NAMPT (Nicotinamide Phosphoribosyltransferase) Inhibitors.
AID765315Antiproliferative activity against human A2780 cells assessed as growth inhibition after 72 hrs by SRB-based microplate reader analysis2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Structure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (nampt) inhibitors.
AID1327641Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate in presence of NADPH by LC-MS/MS analysis2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Minimizing CYP2C9 Inhibition of Exposed-Pyridine NAMPT (Nicotinamide Phosphoribosyltransferase) Inhibitors.
AID1138001Antiproliferative activity against dog A72 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay2013Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
AID765307Antiproliferative activity against human U251 cells assessed as cell viability after 72 hrs by SRB assay2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Structure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (nampt) inhibitors.
AID1138004Cytotoxicity against African green monkey COS1 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay2013Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
AID1137998Antiproliferative activity against mouse KPP cells assessed as cell viability after 96 hrs by CyQuant staining-based assay2013Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
AID1138003Antiproliferative activity against dog DH82 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay2013Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
AID765302Cmax in NCR nude mouse at 10 mg/kg, po2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Structure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (nampt) inhibitors.
AID765298Oral bioavailability in NCR nude mouse at 10 mg/kg2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Structure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (nampt) inhibitors.
AID1137987Inhibition of NAMPT in mouse cells assessed as reduction in NAD level after 48 hrs by mass spectrometry2013Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
AID1137988Cellular uptake in human PC3 cells at 200 nM2013Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
AID765308Fraction unbound in mouse plasma at 5 uM after 4 hrs by LC-MS/MS analysis2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Structure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (nampt) inhibitors.
AID765316Inhibition 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 assay2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Structure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (nampt) inhibitors.
AID765304Antiproliferative activity against human PC3 cells assessed as cell viability after 72 hrs2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Structure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (nampt) inhibitors.
AID765297AUC (infinity) in NCR nude mouse at 10 mg/kg, po2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Structure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (nampt) inhibitors.
AID765310Apparent permeability across apical to basolateral side in dog MDCK cells at 10 uM by LC-MS/MS analysis2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Structure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (nampt) inhibitors.
AID1137978Ratio of drug level in retina to plasma of Sprague-Dawley rat at 30 mg/kg, po qd for 2 days measured 1 hr after last dose in presence of nicotinic acid2013Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
AID1190264Time-dependent inhibition of CYP3A4 (unknown origin) using testosterone as substrate assessed as AUC shift2015Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
Identification of nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with no evidence of CYP3A4 time-dependent inhibition and improved aqueous solubility.
AID765311Intrinsic clearance in human hepatocytes at 1 uM after 10 mins by LC-MS/MS analysis2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Structure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (nampt) inhibitors.
AID1137993Antiproliferative activity against human HT1080 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay2013Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
AID1138002Antiproliferative activity against dog D17 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay2013Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
AID1137989Inhibition of NAMPT in human PC3 cells assessed as reduction in NAD level after 48 hrs by mass spectrometry2013Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
AID1327637Inhibition of human full length C-terminal His6-tagged NAMPT expressed in Escherichia coli Rosetta (DE3) cells using nicotinamide as substrate incubated for 15 mins prior to substrate addition measured after 30 mins in presence of PRPP2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Minimizing CYP2C9 Inhibition of Exposed-Pyridine NAMPT (Nicotinamide Phosphoribosyltransferase) Inhibitors.
AID1137986Cellular uptake in human PC3 cells at 1000 nM2013Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
AID765309Fraction unbound in human plasma at 5 uM after 4 hrs by LC-MS/MS analysis2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Structure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (nampt) inhibitors.
AID1138005Cytotoxicity against African green monkey COS7 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay2013Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
AID1137985Cellular uptake in mouse KPP cells at 200 nM2013Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
AID765314Metabolic stability in mouse liver microsomes assessed as compound remaining at 1 uM after 30 mins LC-MS analysis2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Structure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (nampt) inhibitors.
AID765306Antiproliferative activity against human HT1080 cells assessed as cell viability after 72 hrs2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Structure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (nampt) inhibitors.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB2014PloS one, , Volume: 9, Issue:10
Structural basis for resistance to diverse classes of NAMPT inhibitors.
AID1800299NAMPT enzyme assay from Article 10.1002/cbic.201402023: \\Structural and biochemical analyses of the catalysis and potency impact of inhibitor phosphoribosylation by human nicotinamide phosphoribosyltransferase.\\2014Chembiochem : a European journal of chemical biology, May-26, Volume: 15, Issue:8
Structural and biochemical analyses of the catalysis and potency impact of inhibitor phosphoribosylation by human nicotinamide phosphoribosyltransferase.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (14)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's12 (85.71)24.3611
2020's2 (14.29)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 16.98

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index16.98 (24.57)
Research Supply Index2.71 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (16.98)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other14 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]