Compounds > chi 1043
Page last updated: 2024-11-13

chi 1043

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 CID25066442
CHEMBL ID259011
MeSH IDM0569635

Synonyms (5)

Synonym
chi-1043 ,
(z)-4-[1-[(4-fluorophenyl)methyl]-4-methoxy-indol-3-yl]-2-hydroxy-4-oxo-but-2-enoic acid
CHEMBL259011 ,
bdbm50009453
(z)-4-[1-[(4-fluorophenyl)methyl]-4-methoxyindol-3-yl]-4-hydroxy-2-oxobut-3-enoic acid
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Integrase Human immunodeficiency virus 1IC50 (µMol)0.11550.00051.544310.0000AID1129987; AID1174478; AID331697; AID331698; AID411788; AID411789; AID497131; AID497132; AID569000; AID573970; AID573971
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Integrase Human immunodeficiency virus 1C500.14000.00700.05400.1400AID569001
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (73)

Assay IDTitleYearJournalArticle
AID331700Cytotoxicity against human MT4 cells2008Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
A refined pharmacophore model for HIV-1 integrase inhibitors: Optimization of potency in the 1H-benzylindole series.
AID525106Antiviral activity against HIV 1 3B harboring integrase E92Q, S230N and L34M triple mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 60 passages in presence of compound2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137.
AID525112Antiviral activity against HIV 1 NL4.3 harboring integrase L74M mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137.
AID573985Antiviral activity against Reverse transcriptase inhibitor-resistant Human immunodeficiency virus 1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID525114Antiviral activity against HIV 1 NL4.3 integrase S230N mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137.
AID573976Antiretroviral activity against Human immunodeficiency virus 1 NL4.3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID573993Antiviral activity against Human immunodeficiency virus 1 infected in 293T cells assessed as integrated proximal DNA by Q-PCR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID525107Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137.
AID1338605Inhibition of mushroom tyrosinase assessed as reduction in formation of dopachrome using L-DOPA as substrate2017European journal of medicinal chemistry, Jan-05, Volume: 125Chemical exploration of 4-(4-fluorobenzyl)piperidine fragment for the development of new tyrosinase inhibitors.
AID411789Inhibition of HIV1 integrase strand transfer activity by ELISA2009Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
Docking studies on a new human immunodeficiency virus integrase-Mg-DNA complex: phenyl ring exploration and synthesis of 1H-benzylindole derivatives through fluorine substitutions.
AID525105Antiviral activity against HIV 1 3B harboring integrase L34M mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 40 passages in presence of compound2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137.
AID1174479Inhibition of HIV-1 integrase LEDGF/p75 (unknown origin) interaction2015European journal of medicinal chemistry, Jan-07, Volume: 89A review on recent developments of indole-containing antiviral agents.
AID525108Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 20 passages selected in presence of compound2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137.
AID1129983Inhibition of His-6-tagged HIV-1 integrase-recombinant flag-tagged LEDGF/p75 (unknown origin) interaction after 1hr by AlphaScreen assay2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
A new potential approach to block HIV-1 replication via protein-protein interaction and strand-transfer inhibition.
AID331697Inhibition of HIV1 integrase2008Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
A refined pharmacophore model for HIV-1 integrase inhibitors: Optimization of potency in the 1H-benzylindole series.
AID331698Inhibition of HIV1 integrase strand transfer activity2008Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
A refined pharmacophore model for HIV-1 integrase inhibitors: Optimization of potency in the 1H-benzylindole series.
AID497135Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 cells2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
New chloro,fluorobenzylindole derivatives as integrase strand-transfer inhibitors (INSTIs) and their mode of action.
AID573999Ratio of EC50 for Human immunodeficiency virus in presence of 10% FCS to EC50 for Human immunodeficiency virus in presence of 50% human serum2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID497132Inhibition of HIV1 integrase strand transfer2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
New chloro,fluorobenzylindole derivatives as integrase strand-transfer inhibitors (INSTIs) and their mode of action.
AID573980Ratio of EC50 for Human immunodeficiency virus 1 3B after 70 passages to EC50 for wild-type Human immunodeficiency virus 1 3B2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID525113Antiviral activity against HIV 1 NL4.3 integrase E92Q mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137.
AID573990Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for non nucleoside Protease inhibitor-resistant Human immunodeficiency virus 12008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID573978Antiretroviral activity against Human immunodeficiency virus 2 EHO infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID573971Inhibition of Human immunodeficiency virus 1 integrase strand transfer activity2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID573991Antiviral activity against Human immunodeficiency virus 1 during lentiviral transduction process assessed as inhibition of early cDNA synthesis by Lentiviral vector transduction assay2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID573987Antiviral activity against Protease inhibitor-resistant Human immunodeficiency virus 1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID574002Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for wild-type Human immunodeficiency virus 2 ROD2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID569000Inhibition of HIV-1 integrase after 1 hr by ELISA2011European journal of medicinal chemistry, Feb, Volume: 46, Issue:2
HIV-1 integrase strand-transfer inhibitors: design, synthesis and molecular modeling investigation.
AID497131Inhibition of HIV1 integrase2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
New chloro,fluorobenzylindole derivatives as integrase strand-transfer inhibitors (INSTIs) and their mode of action.
AID573981Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for Human immunodeficiency virus 2 EHO2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID573972Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as inhibition of viral replication2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID569003Cytotoxicity against human MT4 cells by MTT assay2011European journal of medicinal chemistry, Feb, Volume: 46, Issue:2
HIV-1 integrase strand-transfer inhibitors: design, synthesis and molecular modeling investigation.
AID573983Antiviral activity against X4 tropic Human immunodeficiency virus 1 3B infected in PMBC2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID1129987Inhibition of HIV-1 integrase strand transfer activity using 3'-end biotin labelled oligonucleotide/5'-end digoxigenin labelled oligonucleotide as substrate after 1 hr by ELISA2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
A new potential approach to block HIV-1 replication via protein-protein interaction and strand-transfer inhibition.
AID573998Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for CHI/1043-resistant Human immunodeficiency virus harboring T66I and Q146K mutations in integrase2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID1129986Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 3B2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
A new potential approach to block HIV-1 replication via protein-protein interaction and strand-transfer inhibition.
AID525102Antiviral activity against HIV 1 3B infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137.
AID1174478Inhibition of HIV-1 integrase strand transfer activity2015European journal of medicinal chemistry, Jan-07, Volume: 89A review on recent developments of indole-containing antiviral agents.
AID1129985Cytotoxicity against human MT4 cells assessed as cell viability by MTT assay2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
A new potential approach to block HIV-1 replication via protein-protein interaction and strand-transfer inhibition.
AID573996Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for L-870,810-resistant Human immunodeficiency virus harboring L74M, E92Q and S230N mutations in integrase2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID573994Antiviral activity against Human immunodeficiency virus 1 infected in 293T cells assessed as increase in amount of 2-LTR circles by Q-PCR in presence of 12.2 uM CHI/10432008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID573974Selectivity index, ratio of CC50 for human MT4 cells to EC50 for Human immunodeficiency virus 1 3B2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID411791Cytotoxicity against human MT4 cells by MTT assay2009Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
Docking studies on a new human immunodeficiency virus integrase-Mg-DNA complex: phenyl ring exploration and synthesis of 1H-benzylindole derivatives through fluorine substitutions.
AID573970Inhibition of Human immunodeficiency virus 1 integrase2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID331701Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B2008Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
A refined pharmacophore model for HIV-1 integrase inhibitors: Optimization of potency in the 1H-benzylindole series.
AID411792Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B2009Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
Docking studies on a new human immunodeficiency virus integrase-Mg-DNA complex: phenyl ring exploration and synthesis of 1H-benzylindole derivatives through fluorine substitutions.
AID573988Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for Reverse transcriptase inhibitor-resistant Human immunodeficiency virus 12008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID574000Intrinsic clearance in human liver microsome2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID573973Cytotoxicity against human MT4 cells by MTT assay2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID569001Inhibition of HIV-1 integrase strand transfer activity after 1 hr by ELISA2011European journal of medicinal chemistry, Feb, Volume: 46, Issue:2
HIV-1 integrase strand-transfer inhibitors: design, synthesis and molecular modeling investigation.
AID497133Antiviral activity against HIV1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
New chloro,fluorobenzylindole derivatives as integrase strand-transfer inhibitors (INSTIs) and their mode of action.
AID573997Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for MK-0518-resistant Human immunodeficiency virus harboring G140S and Q148H mutations in integrase2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID573975Antiretroviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID525104Antiviral activity against HIV 1 3B harboring integrase E92Q S230N double mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 20 passages in presence of compound2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137.
AID411790Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay2009Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
Docking studies on a new human immunodeficiency virus integrase-Mg-DNA complex: phenyl ring exploration and synthesis of 1H-benzylindole derivatives through fluorine substitutions.
AID573995Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for L-708,906-resistant Human immunodeficiency virus harboring T66I, L74M and S230R mutations in integrase2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID411788Inhibition of HIV1 integrase activity by ELISA2009Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
Docking studies on a new human immunodeficiency virus integrase-Mg-DNA complex: phenyl ring exploration and synthesis of 1H-benzylindole derivatives through fluorine substitutions.
AID525111Antiviral activity against HIV 1 NL4.3 assessed as inhibition of virus-induced cytopathic effect by MTT assay2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137.
AID574001Apparent permeability from apical to basolateral side of human Caco2 cells2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID569004Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV13B2011European journal of medicinal chemistry, Feb, Volume: 46, Issue:2
HIV-1 integrase strand-transfer inhibitors: design, synthesis and molecular modeling investigation.
AID525109Antiviral activity against HIV 1 RIN HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 40 passages selected in presence of compound2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137.
AID569002Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay2011European journal of medicinal chemistry, Feb, Volume: 46, Issue:2
HIV-1 integrase strand-transfer inhibitors: design, synthesis and molecular modeling investigation.
AID573977Antiretroviral activity against Human immunodeficiency virus 2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID525110Antiviral activity against HIV 1 RIN HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 60 passages selected in presence of compound2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137.
AID331699Antiviral activity against HIV1 3B assessed as inhibition of viral-induced cytopathic effect in human MT4 cells2008Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
A refined pharmacophore model for HIV-1 integrase inhibitors: Optimization of potency in the 1H-benzylindole series.
AID573979Antiretroviral activity against Simian immunodeficiency virus MAC 251 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID573992Antiviral activity against Human immunodeficiency virus 1 infected in 293T cells assessed as inhibition of early cDNA synthesis by Lentiviral vector transduction assay2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID1129984Antiviral activity against HIV-1 3B infected in MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
A new potential approach to block HIV-1 replication via protein-protein interaction and strand-transfer inhibition.
AID573982Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for Simian immunodeficiency virus MAC 2512008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID573986Antiviral activity against non nucleoside reverse transcriptase inhibitor-resistant Human immunodeficiency virus 1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID573984Antiviral activity against R5 tropic Human immunodeficiency virus 1 BAL infected in PMBC2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID573989Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for non nucleoside reverse transcriptase inhibitor-resistant Human immunodeficiency virus 12008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID497134Cytotoxicity against human MT4 cells by MTT assay2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
New chloro,fluorobenzylindole derivatives as integrase strand-transfer inhibitors (INSTIs) and their mode of action.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (9)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's4 (44.44)29.6817
2010's5 (55.56)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.15

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

MetricThis Compound (vs All)
Research Demand Index12.15 (24.57)
Research Supply Index2.30 (2.92)
Research Growth Index4.46 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.15)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (11.11%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other8 (88.89%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
kojic acid
[no description available]		2.15104-pyranones;
enol;
primary alcohol		Aspergillus metabolite;
EC 1.10.3.1 (catechol oxidase) inhibitor;
EC 1.10.3.2 (laccase) inhibitor;
EC 1.13.11.24 (quercetin 2,3-dioxygenase) inhibitor;
EC 1.14.18.1 (tyrosinase) inhibitor;
EC 1.4.3.3 (D-amino-acid oxidase) inhibitor;
NF-kappaB inhibitor;
skin lightening agent
nevirapine
Nevirapine: A potent, non-nucleoside reverse transcriptase inhibitor used in combination with nucleoside analogues for treatment of HIV INFECTIONS and AIDS.. nevirapine : A dipyridodiazepine that is 5,11-dihydro-6H-dipyrido[3,2-b:2',3'-e][1,4]diazepine which is substituted by methyl, oxo, and cyclopropyl groups at positions 4, 6, and 11, respectively. A non-nucleoside reverse transcriptase inhibitor with activity against HIV-1, it is used in combination with other antiretrovirals for the treatment of HIV infection.		2.0410cyclopropanes;
dipyridodiazepine		antiviral drug;
HIV-1 reverse transcriptase inhibitor
zidovudine
Zidovudine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by an azido group. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA during reverse transcription. It improves immunologic function, partially reverses the HIV-induced neurological dysfunction, and improves certain other clinical abnormalities associated with AIDS. Its principal toxic effect is dose-dependent suppression of bone marrow, resulting in anemia and leukopenia.. zidovudine : A pyrimidine 2',3'-dideoxyribonucleoside compound having a 3'-azido substituent and thymine as the nucleobase.		2.4420azide;
pyrimidine 2',3'-dideoxyribonucleoside		antimetabolite;
antiviral drug;
HIV-1 reverse transcriptase inhibitor
atevirdine
atevirdine: inhibits replication of HIV-1; U 87201E is the methanesulfonate salt		3.2110
efavirenz
efavirenz: HIV-1 reverse transcriptase inhibitor. efavirenz : 1,4-Dihydro-2H-3,1-benzoxazin-2-one substituted at the 4 position by cyclopropylethynyl and trifluoromethyl groups (S configuration) and at the 6 position by chlorine. A non-nucleoside reverse transcriptase inhibitor with activity against HIV, it is used with other antiretrovirals for combination therapy of HIV infection.		2.0410acetylenic compound;
benzoxazine;
cyclopropanes;
organochlorine compound;
organofluorine compound		antiviral drug;
HIV-1 reverse transcriptase inhibitor
nelfinavir
Nelfinavir: A potent HIV protease inhibitor. It is used in combination with other antiviral drugs in the treatment of HIV in both adults and children.. nelfinavir : An aryl sulfide that is used (as its mesylate salt) for treatment of HIV and also exhibits some anticancer properties.		2.0410aryl sulfide;
benzamides;
organic heterobicyclic compound;
phenols;
secondary alcohol;
tertiary amino compound		antineoplastic agent;
HIV protease inhibitor
plerixafor
plerixafor: a bicyclam derivate, highly potent & selective inhibitor of HIV-1 & HIV-2. plerixafor : An azamacrocycle consisting of two cyclam rings connected by a 1,4-phenylenebis(methylene) linker. It is a CXCR4 chemokine receptor antagonist and a hematopoietic stem cell mobilizer. It is used in combination with grulocyte-colony stimulating factor (G-CSF) to mobilize hematopoietic stem cells to the perpheral blood for collection and subsequent autologous transplantation in patients with non-Hodgkin's lymphoma and multiple myeloma.		2.0410azacycloalkane;
azamacrocycle;
benzenes;
crown amine;
secondary amino compound;
tertiary amino compound		anti-HIV agent;
antineoplastic agent;
C-X-C chemokine receptor type 4 antagonist;
immunological adjuvant
ritonavir
Ritonavir: An HIV protease inhibitor that works by interfering with the reproductive cycle of HIV. It also inhibits CYTOCHROME P-450 CYP3A.. ritonavir : An L-valine derivative that is L-valinamide in which alpha-amino group has been acylated by a [(2-isopropyl-1,3-thiazol-4-yl)methyl]methylcarbamoyl group and in which a hydrogen of the carboxamide amino group has been replaced by a (2R,4S,5S)-4-hydroxy-1,6-diphenyl-5-{[(1,3-thiazol-5-ylmethoxy)carbonyl]amino}hexan-2-yl group. A CYP3A inhibitor and antiretroviral drug from the protease inhibitor class used to treat HIV infection and AIDS, it is often used as a fixed-dose combination with another protease inhibitor, lopinavir. Also used in combination with dasabuvir sodium hydrate, ombitasvir and paritaprevir (under the trade name Viekira Pak) for treatment of chronic hepatitis C virus genotype 1 infection as well as cirrhosis of the liver.		2.44201,3-thiazoles;
carbamate ester;
carboxamide;
L-valine derivative;
ureas		antiviral drug;
environmental contaminant;
HIV protease inhibitor;
xenobiotic
5-(1,1-dioxido-1,2-thiazinan-2-yl)-n-(4-fluorobenzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamide
5-(1,1-dioxido-1,2-thiazinan-2-yl)-N-(4-fluorobenzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamide: structure in first source		2.4420
l 708906
[no description available]		2.0410
jtk-303
[no description available]		3.1450aromatic ether;
monochlorobenzenes;
organofluorine compound;
quinolinemonocarboxylic acid;
quinolone		HIV-1 integrase inhibitor
raltegravir
[no description available]		3.14501,2,4-oxadiazole;
dicarboxylic acid amide;
hydroxypyrimidine;
monofluorobenzenes;
pyrimidone;
secondary carboxamide		antiviral drug;
HIV-1 integrase inhibitor
trigonoliimine a
trigonoliimine A: from the leaves of Trigonostemon lii; structure in first source		3.2110
ConditionIndicatedRelationship StrengthStudiesTrials
HIV
Human immunodeficiency virus. A non-taxonomic and historical term referring to any of two species, specifically HIV-1 and/or HIV-2. Prior to 1986, this was called human T-lymphotropic virus type III/lymphadenopathy-associated virus (HTLV-III/LAV). From 1986-1990, it was an official species called HIV. Since 1991, HIV was no longer considered an official species name; the two species were designated HIV-1 and HIV-2.		02.0410
Malignant Melanoma
[description not available]		02.1510
Melanoma
A malignant neoplasm derived from cells that are capable of forming melanin, which may occur in the skin of any part of the body, in the eye, or, rarely, in the mucous membranes of the genitalia, anus, oral cavity, or other sites. It occurs mostly in adults and may originate de novo or from a pigmented nevus or malignant lentigo. Melanomas frequently metastasize widely, and the regional lymph nodes, liver, lungs, and brain are likely to be involved. The incidence of malignant skin melanomas is rising rapidly in all parts of the world. (Stedman, 25th ed; from Rook et al., Textbook of Dermatology, 4th ed, p2445)		02.1510