Compounds > indoximod
Page last updated: 2024-11-08

indoximod

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID SourceID
PubMed CID405012
CHEMBL ID571209
SCHEMBL ID934800
MeSH IDM000606974

Synonyms (58)

Synonym
d-1mt
nlg-8189
nsc-721782
1-methyl-d-tryptophan
nsc721782
110117-83-4
SMP2_000028
1-methyl-d-tryptophan, 95%
(2r)-2-amino-3-(1-methylindol-3-yl)propanoic acid
d-1-methyltryptophan
indoximod
CHEMBL571209
1-methyltryptophan, d-
A802144
(2r)-2-azaniumyl-3-(1-methylindol-3-yl)propanoate
BRD-K93255255-001-01-3
d-(+)-1-methyltryptophan
tx5cyn1kmz ,
unii-tx5cyn1kmz
nlg 8189
indoximod [usan:inn]
nsc 721782
d-tryptophen, 1-methyl-
d-l-methyltryptophan
d-tryptophan, 1-methyl-
NCGC00346842-01
AKOS015850753
AKOS015898463
S7756
indoximod [inn]
indoximod [usan]
(2r)-2-amino-3-(1-methyl-1h-indol-3-yl)propanoic acid
indoximod [who-dd]
n-1-methyl-d-tryptophan
gtpl8226
CS-4941
ZADWXFSZEAPBJS-SNVBAGLBSA-N
SCHEMBL934800
D10640
indoximod (usan/inn)
(r)-2-amino-3-(1-methyl-1h-indol-3-yl)propanoic acid
indoximod (nlg-8189)
HY-16724
AC-32784
J-002381
1-methyl-d-tryptophan (h-d-trp(me)-oh)
indoximod (nlg-8189 pound(c)
bdbm50207089
DB12827
DTXSID40911500
d-trp(me)-oh
F20545
nlg-8189; d1mt; 1-methyl-d-tryptophan
Q27078057
AS-15999
AMY22762
A14397
CCG-266709

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
"A series of different prodrugs of indoximod, including estesrs and peptide amides were synthesized with the aim of improving its oral bioavailability in humans."( Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
Adams, J; Brincks, EL; Jaipuri, FA; Kumar, S; Link, C; Marcinowicz, A; Mautino, MR; Potturi, H; Vahanian, N; Van Allen, C; Waldo, JP; Zhuang, H, 2020)		1.21

Dosage Studied

ExcerptRelevanceReference
" The pharmacokinetics of prodrugs that were stable in buffers, plasma and simulated gastric and intestinal fluids was first assessed in rats after oral dosing in solution or in capsule formulation."( Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
Adams, J; Brincks, EL; Jaipuri, FA; Kumar, S; Link, C; Marcinowicz, A; Mautino, MR; Potturi, H; Vahanian, N; Van Allen, C; Waldo, JP; Zhuang, H, 2020)		0.93
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Indoleamine 2,3-dioxygenase 1Homo sapiens (human)IC50 (µMol)15,198.90000.05373.075710.0000AID1348816; AID1348817; AID1348820; AID1412580; AID1453694; AID1728747; AID1728748
Indoleamine 2,3-dioxygenase 1Homo sapiens (human)Ki30.50000.09402.37907.0000AID1855349; AID1882088; AID1916194; AID1916730
Indoleamine 2,3-dioxygenase 2Homo sapiens (human)IC50 (µMol)205.81251.80003.93675.0100AID1332706; AID1332708; AID1639963; AID1639966
[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)
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (20)

Processvia Protein(s)Taxonomy
regulation of activated T cell proliferationIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
positive regulation of T cell tolerance inductionIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
positive regulation of chronic inflammatory responseIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
positive regulation of type 2 immune responseIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
tryptophan catabolic processIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
inflammatory responseIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
female pregnancyIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
tryptophan catabolic process to kynurenineIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
response to lipopolysaccharideIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
negative regulation of interleukin-10 productionIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
positive regulation of interleukin-12 productionIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
multicellular organismal response to stressIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
kynurenic acid biosynthetic processIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
swimming behaviorIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
T cell proliferationIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
negative regulation of T cell proliferationIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
negative regulation of T cell apoptotic processIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
positive regulation of T cell apoptotic processIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
'de novo' NAD biosynthetic process from tryptophanIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
immune system processIndoleamine 2,3-dioxygenase 2Homo sapiens (human)
tryptophan catabolic process to kynurenineIndoleamine 2,3-dioxygenase 2Homo sapiens (human)
'de novo' NAD biosynthetic process from tryptophanIndoleamine 2,3-dioxygenase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (5)

Processvia Protein(s)Taxonomy
electron transfer activityIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
heme bindingIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
indoleamine 2,3-dioxygenase activityIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
metal ion bindingIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
tryptophan 2,3-dioxygenase activityIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
heme bindingIndoleamine 2,3-dioxygenase 2Homo sapiens (human)
indoleamine 2,3-dioxygenase activityIndoleamine 2,3-dioxygenase 2Homo sapiens (human)
metal ion bindingIndoleamine 2,3-dioxygenase 2Homo sapiens (human)
tryptophan 2,3-dioxygenase activityIndoleamine 2,3-dioxygenase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (4)

Processvia Protein(s)Taxonomy
cytosolIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
smooth muscle contractile fiberIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
stereocilium bundleIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
cytoplasmIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
cytoplasmIndoleamine 2,3-dioxygenase 2Homo sapiens (human)
cytosolIndoleamine 2,3-dioxygenase 2Homo sapiens (human)
cytoplasmIndoleamine 2,3-dioxygenase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (181)

Assay IDTitleYearJournalArticle
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
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.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
AID1347154Primary screen GU AMC 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.
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.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1777900Drug accumulation in monkey at 75 to 375 mg/kg, po BID2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777844Tmax in male cynomolgus monkey at 675 mg/kg, po measured on day 12020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777715Cmax in rat at 10 mg/kg, po measured upto 72 hrs by LC-MS/MS analysis2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777876Half life in female cynomolgus monkey at 375 mg/kg, po BID measured on day 82020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777829Cmax in male cynomolgus monkey at 225 mg/kg, po measured on day 12020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777853Clearance in female cynomolgus monkey at 75 mg/kg, po measured on day 12020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777945Change in Cmax in rat at 500 umol/kg, po measured upto 72 hrs by LC-MS/MS analysis2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777868Apparent oral clearance in male cynomolgus monkey at 150 mg/kg, po BID measured on day 82020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777941Change in normalised Cmax in rat at 10 mg/kg, po measured upto 72 hrs by LC-MS/MS analysis2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777946Change in AUC (infinity) in rat at 37 umol/kg, po measured upto 72 hrs by LC-MS/MS analysis2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777711Dose normalized AUC (0 to infinity) in rat at 50 mg/kg, po measured upto 72 hrs by LC-MS/MS analysis2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777936Stimulation of proliferation of CD8 positive T cells (unknown origin)2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777731AUC (0 to infinity) in cynomolgus monkey at 275 umol/kg, po measured after 0.083 to 48 hrs by LC-MS/MS analysis2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1453695Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells using L-tryptophan as substrate after 24 hrs2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Identification and preliminary structure-activity relationships of 1-Indanone derivatives as novel indoleamine-2,3-dioxygenase 1 (IDO1) inhibitors.
AID1348817Inhibition of IDO1 in human HeLa assessed as reduction in kynurenine production2018European journal of medicinal chemistry, Jan-01, Volume: 143Recent discovery of indoleamine-2,3-dioxygenase 1 inhibitors targeting cancer immunotherapy.
AID1777878AUC (0 to 24 hrs) in female cynomolgus monkey at 675 mg/kg, po measured on day 12020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777710AUC (0 to infinity) in rat at 50 mg/kg, po measured upto 72 hrs by LC-MS/MS analysis2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777883Apparent oral clearance in male cynomolgus monkey at 675 mg/kg, po measured on day 12020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1882088Binding affinity to IDO1 (unknown origin)2022European journal of medicinal chemistry, Jan-05, Volume: 227Indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors and PROTAC-based degraders for cancer therapy.
AID1777902Half life in rat at 20 to 900 mg/kg, po2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777717AUC (0 to infinity) in rat at 10 mg/kg, po measured upto 72 hrs by LC-MS/MS analysis2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777955Clearance in female cynomolgus monkey at 15 mg/kg, iv measured on day 12020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777842Tmax in female cynomolgus monkey at 375 mg/kg, po BID measured on day 82020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777939Change in normalised Cmax in rat at 50 mg/kg, po measured upto 72 hrs by LC-MS/MS analysis2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777690AUC (0 to 12 hrs) in human up to 1200 mg administered bid2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777812AUC (0 to 24 hrs) in mouse at 287 micromol/kg administered as single dose2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777840Tmax in male cynomolgus monkey at 225 mg/kg, po measured on day 12020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777866AUC (0 to 24 hrs) in male cynomolgus monkey at 150 mg/kg, po BID measured on day 82020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777818Half life in mouse at 287 micromol/kg administered as single dose2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777861Half life in male cynomolgus monkey at 75 mg/kg, po measured on day 12020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777880Apparent oral clearance in female cynomolgus monkey at 675 mg/kg, po measured on day 12020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777852AUC (0 to 24 hrs) in female cynomolgus monkey at 75 mg/kg, po measured on day 12020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777713AUC (0 to 24 hrs) at steady state in mouse at 1200 mg, BID2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1855349Inhibition of human IDO12022European journal of medicinal chemistry, Nov-05, Volume: 2414,6-Disubstituted-1H-Indazole-4-Amine derivatives with immune-chemotherapy effect and in vivo antitumor activity.
AID1777874Apparent oral clearance in female cynomolgus monkey at 225 mg/kg, po measured on day 12020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777826Cmax in male cynomolgus monkey at 75 mg/kg, po measured on day 12020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777869AUC (0 to 24 hrs) in male cynomolgus monkey at 225 mg/kg, po measured on day 12020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777689AUC (0 to infinity) in human up to 1200 mg administered bid2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777808Cmax in mouse at 1147 micromol/kg administered as single dose2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1728747Inhibition of human IDO12020Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
Development of Indoleamine 2,3-Dioxygenase 1 Inhibitors for Cancer Therapy and Beyond: A Recent Perspective.
AID1777862Apparent oral clearance in male cynomolgus monkey at 75 mg/kg, po measured on day 12020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777823Cmax in female cynomolgus monkey at 75 mg/kg, po measured on day 12020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777872AUC (0 to 24 hrs) in female cynomolgus monkey at 225 mg/kg, po measured on day 12020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777725AUC (0 to infinity) in rat at 185 umol/kg, po measured upto 72 hrs by LC-MS/MS analysis2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777846Half life in male cynomolgus monkey at 15 mg/kg, iv measured on day 12020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777947Change in AUC(infinity) in rat at 185 umol/kg, po measured upto 72 hrs by LC-MS/MS analysis2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777721Cmax in rat at 500 umol/kg, po measured upto 72 hrs by LC-MS/MS analysis2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777943Change in Cmax in rat at 37 umol/kg, po measured upto 72 hrs by LC-MS/MS analysis2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1689084Inhibition of IDO1 expression in hIFNgamma-stimulated human HeLa cells assessed as decrease in kynurenine production at 0.1 uM measured after 48 hrs by reverse-phase HPLC analysis2020European journal of medicinal chemistry, Mar-01, Volume: 189Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase.
AID1777819Half life in mouse at 573 micromol/kg administered as single dose2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777693Solubility of compound at pH 12020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777684AUC (0 to 24 hrs) at steady state in mouse at 62 mg/kg administered bid2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1689083Inhibition of IDO1 expression in hIFNgamma-stimulated human HeLa cells at 0.5 uM measured after 24 hrs by western blot assay2020European journal of medicinal chemistry, Mar-01, Volume: 189Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase.
AID1689067Anticancer activity against human HeLa cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay2020European journal of medicinal chemistry, Mar-01, Volume: 189Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase.
AID1332708Inhibition of recombinant human IDO2 expressed in human U87MG cells assessed as reduction in kynurenine formation using L-tryptophan as substrate after 6 hrs by spectrophotometry2016European journal of medicinal chemistry, Nov-10, Volume: 123Establishment of a human indoleamine 2, 3-dioxygenase 2 (hIDO2) bioassay system and discovery of tryptanthrin derivatives as potent hIDO2 inhibitors.
AID1689068Anticancer activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay2020European journal of medicinal chemistry, Mar-01, Volume: 189Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase.
AID1777825Cmax in male cynomolgus monkey at 75 mg/kg, po BID measured on day 82020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777841Tmax in female cynomolgus monkey at 225 mg/kg, po measured on day 12020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777805Cmax in mouse at 143 micromol/kg administered as single dose2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777950Change in Cmax in cynomolgus monkey at 275 umol/kg, po measured after 0.083 to 48 hrs by LC-MS/MS analysis2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777859Half life in female cynomolgus monkey at 75 mg/kg, po measured on day 12020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777949Change in Cmax in cynomolgus monkey at 92 umol/kg, po measured after 0.083 to 48 hrs by LC-MS/MS analysis2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777948Change in AUC(infinity) in rat at 500 umol/kg, po measured upto 72 hrs by LC-MS/MS analysis2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777833Cmax in male cynomolgus monkey at 675 mg/kg, po measured on day 12020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777694Solubility of compound at pH 7.42020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1916194Binding affinity to human IDO1 assessed as inhibition constant2021Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12
X-ray Structure-Guided Discovery of a Potent, Orally Bioavailable, Dual Human Indoleamine/Tryptophan 2,3-Dioxygenase (hIDO/hTDO) Inhibitor That Shows Activity in a Mouse Model of Parkinson's Disease.
AID1777882Half life in male cynomolgus monkey at 675 mg/kg, po measured on day 12020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777732AUC (0 to infinity) in cynomolgus monkey at 825 umol/kg, po measured after 0.083 to 48 hrs by LC-MS/MS analysis2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777951Change in Cmax in cynomolgus monkey at 825 umol/kg, po measured after 0.083 to 48 hrs by LC-MS/MS analysis2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1412580Inhibition of human HuH7 cell derived IDO1 expressed in Escherichia coli BL21 codon plus using L-tryptophan as substrate measured after 1 hr by fluorescence assay2018MedChemComm, Jun-01, Volume: 9, Issue:6
Discovery of indoleamine 2,3-dioxygenase inhibitors using machine learning based virtual screening.
AID1777901Half life in mouse at 20 to 900 mg/kg, po2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777688Cmax in human up to 1200 mg administered bid2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777843Tmax in female cynomolgus monkey at 675 mg/kg, po measured on day 12020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777709Dose normalized Cmax in rat at 50 mg/kg, po measured upto 72 hrs by LC-MS/MS analysis2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777867Half life in male cynomolgus monkey at 150 mg/kg, po BID measured on day 82020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777899Drug accumulation in rat at 100 to 900 mg/kg, po BID2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777828Cmax in male cynomolgus monkey at 150 mg/kg, po BID measured on day 82020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1453694Inhibition of recombinant human His-tagged IDO1 expressed in Escherichia coli BL21(DE3) cells assessed as inhibition of kynurenine production using L-tryptophan as substrate after 1 hr by fluorescence assay relative to control2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Identification and preliminary structure-activity relationships of 1-Indanone derivatives as novel indoleamine-2,3-dioxygenase 1 (IDO1) inhibitors.
AID1777863AUC (0 to 24 hrs) in female cynomolgus monkey at 150 mg/kg, po BID measured on day 82020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777851Volume of distribution in female cynomolgus monkey at 15 mg/kg, iv measured on day 12020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777718Dose normalized AUC (0 to infinity) in rat at 10 mg/kg, po measured upto 72 hrs by LC-MS/MS analysis2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777835Tmax in female cynomolgus monkey at 75 mg/kg, po measured on day 82020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1689066Antitumor immunity against IFN-gamma stimulated human HeLa cells co-cultured with PHA-M-stimulated human PBMC cells assessed as induction of CD3+ T cell proliferation at 0.1 uM preincubated for 2 days measured after co-culturing with PBMC for 6 days by fl2020European journal of medicinal chemistry, Mar-01, Volume: 189Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase.
AID1777940Change in normalised AUC (infinity) in rat at 50 mg/kg, po measured upto 72 hrs by LC-MS/MS analysis2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777716Dose normalized Cmax in rat at 10 mg/kg, po measured upto 72 hrs by LC-MS/MS analysis2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777692AUC (0 to infinity) in human at 2400 mg administered bid2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777816Tmax in mouse at 287 micromol/kg administered as single dose2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777873Half life in female cynomolgus monkey at 225 mg/kg, po measured on day 12020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1348816Inhibition of human IDO1 assessed as reduction in kynurenine production2018European journal of medicinal chemistry, Jan-01, Volume: 143Recent discovery of indoleamine-2,3-dioxygenase 1 inhibitors targeting cancer immunotherapy.
AID1777831Cmax in female cynomolgus monkey at 375 mg/kg, po BID measured on day 82020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777938Half life in rat2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777942Change in normalised AUCinfinity in rat at 10 mg/kg, po measured upto 72 hrs by LC-MS/MS analysis2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1689065Cytotoxicity against HUVEC cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay2020European journal of medicinal chemistry, Mar-01, Volume: 189Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase.
AID1777954Change in AUC(infinity) in cynomolgus monkey at 825 umol/kg, po measured after 0.083 to 48 hrs by LC-MS/MS analysis2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777719Cmax in rat at 37 umol/kg, po measured upto 72 hrs by LC-MS/MS analysis2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777927Cmax in po BID dosed cynomolgus monkey administered for 28 days2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777712Cmax in mouse at 62 mg/kg administered bid2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777708Cmax in rat at 50 mg/kg, po measured upto 72 hrs by LC-MS/MS analysis2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777879Half life in female cynomolgus monkey at 675 mg/kg, po measured on day 12020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777850Half life in female cynomolgus monkey at 15 mg/kg, iv measured on day 12020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777881AUC (0 to 24 hrs) in male cynomolgus monkey at 675 mg/kg, po measured on day 12020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777724AUC (0 to infinity) in rat at 37 umol/kg, po measured upto 72 hrs by LC-MS/MS analysis2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777728Cmax in cynomolgus monkey at 275 umol/kg, po measured after 0.083 to 48 hrs by LC-MS/MS analysis2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777811AUC (0 to 24 hrs) in mouse at 143 micromol/kg administered as single dose2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777937Oral bioavailability in rat2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777849AUC (0 to 24 hrs) in female cynomolgus monkey at 15 mg/kg, iv measured on day 12020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777727Cmax in cynomolgus monkey at 92 umol/kg, po measured after 0.083 to 48 hrs by LC-MS/MS analysis2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777837Tmax in male cynomolgus monkey at 75 mg/kg, po measured on day 12020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777839Tmax in male cynomolgus monkey at 150 mg/kg, po BID measured on day 82020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777813AUC (0 to 24 hrs) in mouse at 573 micromol/kg administered as single dose2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777944Change in Cmax in rat at 185 umol/kg, po measured upto 72 hrs by LC-MS/MS analysis2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1453693Inhibition of recombinant human His-tagged IDO1 expressed in Escherichia coli BL21(DE3) cells assessed as inhibition of kynurenine production at 10 uM using L-tryptophan as substrate after 1 hr by fluorescence assay relative to control2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Identification and preliminary structure-activity relationships of 1-Indanone derivatives as novel indoleamine-2,3-dioxygenase 1 (IDO1) inhibitors.
AID1332713Inhibition of recombinant human IDO2 (14-420 residues) expressed in Escherichia coli BL21(DE3) assessed as reduction in L-kynurenine formation using L-tryptophan as substrate after 30 mins in presence of catalase2016European journal of medicinal chemistry, Nov-10, Volume: 123Establishment of a human indoleamine 2, 3-dioxygenase 2 (hIDO2) bioassay system and discovery of tryptanthrin derivatives as potent hIDO2 inhibitors.
AID1777729Cmax in cynomolgus monkey at 825 umol/kg, po measured after 0.083 to 48 hrs by LC-MS/MS analysis2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777865Apparent oral clearance in female cynomolgus monkey at 150 mg/kg, po BID measured on day 82020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777806Cmax in mouse at 287 micromol/kg administered as single dose2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777810Tmax in mouse at 573 micromol/kg administered as single dose2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777686Average plasma concentration at steady state in mouse at 250 mg/kg administered bid2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1332706Inhibition of recombinant human C-terminal His6-tagged IDO2 (14-420 residues) expressed in Escherichia coli BL21(DE3) assessed as reduction in L-kynurenine formation using L-tryptophan as substrate after 30 mins in presence of catalase by methylene blue d2016European journal of medicinal chemistry, Nov-10, Volume: 123Establishment of a human indoleamine 2, 3-dioxygenase 2 (hIDO2) bioassay system and discovery of tryptanthrin derivatives as potent hIDO2 inhibitors.
AID1777817Half life in mouse at 143 micromol/kg administered as single dose2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777952Change in AUC(infinity) in cynomolgus monkey at 92 umol/kg, po measured after 0.083 to 48 hrs by LC-MS/MS analysis2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777720Cmax in rat at 185 umol/kg, po measured upto 72 hrs by LC-MS/MS analysis2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID443994Inhibition of IDO by cell-free assay2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Rational design of indoleamine 2,3-dioxygenase inhibitors.
AID1777830Cmax in female cynomolgus monkey at 225 mg/kg, po measured on day 12020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1332702Competitive inhibition of recombinant human C-terminal His6-tagged IDO2 (14-420 residues) expressed in Escherichia coli BL21(DE3) in presence of varying concentration of L-tryptophan substrate after 30 mins2016European journal of medicinal chemistry, Nov-10, Volume: 123Establishment of a human indoleamine 2, 3-dioxygenase 2 (hIDO2) bioassay system and discovery of tryptanthrin derivatives as potent hIDO2 inhibitors.
AID1777827Cmax in female cynomolgus monkey at 150 mg/kg, po measured on day 82020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777730AUC (0 to infinity) in cynomolgus monkey at 92 umol/kg, po measured after 0.083 to 48 hrs by LC-MS/MS analysis2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777815Tmax in mouse at 143 micromol/kg administered as single dose2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777807Cmax in mouse at 573 micromol/kg administered as single dose2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777832Cmax in female cynomolgus monkey at 675 mg/kg, po measured on day 12020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777860AUC (0 to 24 hrs) in male cynomolgus monkey at 75 mg/kg, po measured on day 12020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777871Half life in male cynomolgus monkey at 225 mg/kg, po measured on day 12020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777821Cmax in male cynomolgus monkey at 15 mg/kg, iv measured on day 12020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777820Half life in mouse at 1147 micromol/kg administered as single dose2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777928AUC (0 to 12 hrs) in po BID dosed cynomolgus monkey administered for 28 days2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1916730Binding affinity to IDO1 (unknown origin) assessed as inhibition constant2022European journal of medicinal chemistry, Aug-05, Volume: 238Dual-target inhibitors of indoleamine 2, 3 dioxygenase 1 (Ido1): A promising direction in cancer immunotherapy.
AID1777814AUC (0 to 24 hrs) in mouse at 1147 micromol/kg administered as single dose2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777685Average plasma concentration at steady state in mouse at 62 mg/kg administered bid2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1689069Anticancer activity against human PC3 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay2020European journal of medicinal chemistry, Mar-01, Volume: 189Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase.
AID1348820Inhibition of IDO1 in human HT-29 assessed as reduction in kynurenine production2018European journal of medicinal chemistry, Jan-01, Volume: 143Recent discovery of indoleamine-2,3-dioxygenase 1 inhibitors targeting cancer immunotherapy.
AID1777824Cmax in female cynomolgus monkey at 75 mg/kg, po BID measured on day 82020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777953Change in AUC(infinity) in cynomolgus monkey at 275 umol/kg, po measured after 0.083 to 48 hrs by LC-MS/MS analysis2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777836Tmax in male cynomolgus monkey at 75 mg/kg, po BID measured on day 82020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777687Cmax in mouse at 250 mg/kg administered bid2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777864Half life in female cynomolgus monkey at 150 mg/kg, po measured on day 82020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777822Cmax in female cynomolgus monkey at 15 mg/kg, iv measured on day 12020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777809Tmax in mouse at 1147 micromol/kg administered as single dose2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777691Cmax in human at 2400 mg administered bid2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1728748Inhibition of IDO1 in human HeLa cells2020Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
Development of Indoleamine 2,3-Dioxygenase 1 Inhibitors for Cancer Therapy and Beyond: A Recent Perspective.
AID1777870Apparent oral clearance in male cynomolgus monkey at 225 mg/kg, po measured on day 12020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1777726AUC (0 to infinity) in rat at 500 umol/kg, po measured upto 72 hrs by LC-MS/MS analysis2020European journal of medicinal chemistry, Jul-15, Volume: 198Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (20)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's7 (35.00)24.3611
2020's13 (65.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 36.55

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 strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index36.55 (24.57)
Research Supply Index3.04 (2.92)
Research Growth Index5.94 (4.65)
Search Engine Demand Index45.89 (26.88)
Search Engine Supply Index2.09 (0.95)

This Compound (36.55)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews4 (20.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other16 (80.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
oxyquinoline
Oxyquinoline: An antiseptic with mild fungistatic, bacteriostatic, anthelmintic, and amebicidal action. It is also used as a reagent and metal chelator, as a carrier for radio-indium for diagnostic purposes, and its halogenated derivatives are used in addition as topical anti-infective agents and oral antiamebics.. quinolin-8-ol : A monohydroxyquinoline that is quinoline substituted by a hydroxy group at position 8. Its fungicidal properties are used for the control of grey mould on vines and tomatoes.		2.0510monohydroxyquinolineantibacterial agent;
antifungal agrochemical;
antiseptic drug;
iron chelator
dichlorophen
Dichlorophen: Nontoxic laxative vermicide effective for taenia infestation. It tends to produce colic and nausea. It is also used as a veterinary fungicide, anthelmintic, and antiprotozoan. (From Merck, 11th ed.)		2.0510bridged diphenyl fungicide;
diarylmethane
benzophenone
benzophenone : The simplest member of the class of benzophenones, being formaldehyde in which both hydrogens are replaced by phenyl groups.		2.0510benzophenonesphotosensitizing agent;
plant metabolite
beta-lapachone
beta-lapachone: antineoplastic inhibitor of reverse transcriptase, DNA topoisomerase, and DNA polymerase. beta-lapachone : A benzochromenone that is 3,4-dihydro-2H-benzo[h]chromene-5,6-dione substituted by geminal methyl groups at position 2. Isolated from Tabebuia avellanedae, it exhibits antineoplastic and anti-inflammatory activities.		3.3510benzochromenone;
orthoquinones		anti-inflammatory agent;
antineoplastic agent;
plant metabolite
4-aminodiphenylamine
4-aminodiphenylamine: RN given refers to parent cpd. p-aminodiphenylamine : An aromatic amine that is the 4-amino derivative of diphenylamine.		2.0510aromatic amine;
secondary amino compound		allergen
9-fluorenone
fluoren-9-one : The simplest member of the class fluoren-9-ones that is 9H-fluorene bearing an oxo substituent at position 9.		2.0510fluoren-9-onesfungal xenobiotic metabolite
1,4-naphthohydroquinone
naphthohydroquinone : A hydroxynaphthalene that is naphthalene-1,4-diol and its C-substituted derivatives.		2.0510naphthalenediol;
naphthohydroquinone
phenthiazamine
phenthiazamine: RN given refers to parent cpd		2.0510
norharman
norharman: RN given refers to parent cpd. beta-carboline : The parent compound of the beta-carbolines, a tricyclic structure comprising an indole ring system ortho- fused to C-3 and C-4 of a pyridine ring.		3.3510beta-carbolines;
mancude organic heterotricyclic parent		fungal metabolite;
marine metabolite
4(5)-phenylimidazole
4(5)-phenylimidazole: tautomeric cpd; cytochrome P450 14alpha-sterol demethylase, CYP51 antagonist		3.7320
tryptanthrine
tryptanthrine: minor constituent of traditional Chinese medicine qing dai		2.1310alkaloid antibiotic;
organic heterotetracyclic compound;
organonitrogen heterocyclic compound
fluoren-9-ol
fluoren-9-ol : A member of the class of hydroxyfluorenes that is 9H-fluorene substituted by a hydroxy group at position 9 (the non-aromatic carbon).		2.0510hydroxyfluorenes;
secondary alcohol		animal metabolite
1-methyltryptophan
[no description available]		3.2710non-proteinogenic alpha-amino acid;
tryptophan derivative		antineoplastic agent;
EC 1.13.11.52 (indoleamine 2,3-dioxygenase) inhibitor
4-hydroxycarbazole
4-hydroxycarbazole: structure in first source		2.0510
5-amino-8-hydroxyquinoline
5-amino-8-hydroxyquinoline: structure in first source		2.0510
piplartine
piplartine: Antineoplastic Agent, Phytogenic; alkaloid from Piper; structure in first source		3.5110cinnamamides;
dicarboximide
1-methyltryptophan
1-methyltryptophan: an immunomodulator. 1-methyltryptophan : A tryptophan derivative that is tryptophan carrying a single methyl substituent at position 1 on the indole.		3.9130indolyl carboxylic acid
methyl-thiohydantoin-tryptophan
methyl-thiohydantoin-tryptophan: structure in first source		3.5110organonitrogen compound;
organooxygen compound
4-phenyl-3H-thiazole-2-thione
[no description available]		2.0510benzenes
fosbretabulin
[no description available]		2.2510stilbenoid
3-hydroxy-4,3',4',5'-tetramethoxychalcone
3-hydroxy-4,3',4',5'-tetramethoxychalcone: structure in first source		2.2510
ConditionIndicatedRelationship StrengthStudiesTrials
Benign Neoplasms
[description not available]		05.4760
Neoplasms
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.		17.4760
Congenital Zika Syndrome
[description not available]		02.2510
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.2510
Zika Virus Infection
A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.		02.2510
Atherosclerotic Parkinsonism
[description not available]		02.3110
Parkinson Disease, Secondary
Conditions which feature clinical manifestations resembling primary Parkinson disease that are caused by a known or suspected condition. Examples include parkinsonism caused by vascular injury, drugs, trauma, toxin exposure, neoplasms, infections and degenerative or hereditary conditions. Clinical features may include bradykinesia, rigidity, parkinsonian gait, and masked facies. In general, tremor is less prominent in secondary parkinsonism than in the primary form. (From Joynt, Clinical Neurology, 1998, Ch38, pp39-42)		02.3110