Compounds > chi 1043
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chi 1043

Description

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

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Integrase Human immunodeficiency virus 1IC500.1155AID1129987; AID1174478; AID331697; AID331698; AID411788; AID411789; AID497131; AID497132; AID569000; AID573970; AID573971

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Integrase Human immunodeficiency virus 1C500.1400AID569001

Bioassays (73)

Assay IDTitleYearJournalArticle
AID331700Cytotoxicity against human MT4 cells2008Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
ISSN: 1464-3405		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
ISSN: 1098-6596		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
ISSN: 1098-6596		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
ISSN: 1098-6596		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
ISSN: 1098-6596		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
ISSN: 1098-6596		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
ISSN: 1098-6596		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
ISSN: 1098-6596		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: 125ISSN: 1768-3254Chemical 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
ISSN: 1520-4804		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
ISSN: 1098-6596		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: 89ISSN: 1768-3254A 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
ISSN: 1098-6596		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
ISSN: 1464-3391		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
ISSN: 1464-3405		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
ISSN: 1464-3405		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
ISSN: 1464-3391		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
ISSN: 1098-6596		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
ISSN: 1464-3391		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
ISSN: 1098-6596		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
ISSN: 1098-6596		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
ISSN: 1098-6596		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
ISSN: 1098-6596		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
ISSN: 1098-6596		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
ISSN: 1098-6596		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
ISSN: 1098-6596		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
ISSN: 1098-6596		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
ISSN: 1768-3254		HIV-1 integrase strand-transfer inhibitors: design, synthesis and molecular modeling investigation.
AID497131Inhibition of HIV1 integrase2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
ISSN: 1464-3391		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
ISSN: 1098-6596		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
ISSN: 1098-6596		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
ISSN: 1768-3254		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
ISSN: 1098-6596		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
ISSN: 1464-3391		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
ISSN: 1098-6596		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
ISSN: 1464-3391		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
ISSN: 1098-6596		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: 89ISSN: 1768-3254A 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
ISSN: 1464-3391		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
ISSN: 1098-6596		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
ISSN: 1098-6596		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
ISSN: 1098-6596		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
ISSN: 1520-4804		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
ISSN: 1098-6596		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
ISSN: 1464-3405		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
ISSN: 1520-4804		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
ISSN: 1098-6596		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
ISSN: 1098-6596		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
ISSN: 1098-6596		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
ISSN: 1768-3254		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
ISSN: 1464-3391		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
ISSN: 1098-6596		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
ISSN: 1098-6596		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
ISSN: 1098-6596		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
ISSN: 1520-4804		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
ISSN: 1098-6596		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
ISSN: 1520-4804		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
ISSN: 1098-6596		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
ISSN: 1098-6596		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
ISSN: 1768-3254		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
ISSN: 1098-6596		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
ISSN: 1768-3254		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
ISSN: 1098-6596		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
ISSN: 1098-6596		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
ISSN: 1464-3405		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
ISSN: 1098-6596		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
ISSN: 1098-6596		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
ISSN: 1464-3391		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
ISSN: 1098-6596		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
ISSN: 1098-6596		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
ISSN: 1098-6596		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
ISSN: 1098-6596		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
ISSN: 1464-3391		New chloro,fluorobenzylindole derivatives as integrase strand-transfer inhibitors (INSTIs) and their mode of action.

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

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%
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
kojic acid
1
4-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		201720177.0low000010
nevirapine
1
cyclopropanes;
dipyridodiazepine		antiviral drug;
HIV-1 reverse transcriptase inhibitor		2008200816.0low000100
zidovudine
2
azide;
pyrimidine 2',3'-dideoxyribonucleoside		antimetabolite;
antiviral drug;
HIV-1 reverse transcriptase inhibitor		2008200816.0low000200
atevirdine
1
201520159.0low000010
efavirenz
1
acetylenic compound;
benzoxazine;
cyclopropanes;
organochlorine compound;
organofluorine compound		antiviral drug;
HIV-1 reverse transcriptase inhibitor		2008200816.0low000100
nelfinavir
1
aryl sulfide;
benzamides;
organic heterobicyclic compound;
phenols;
secondary alcohol;
tertiary amino compound		antineoplastic agent;
HIV protease inhibitor		2008200816.0low000100
plerixafor
1
azacycloalkane;
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		2008200816.0low000100
ritonavir
2
1,3-thiazoles;
carbamate ester;
carboxamide;
L-valine derivative;
ureas		antiviral drug;
environmental contaminant;
HIV protease inhibitor;
xenobiotic		2008200816.0low000200
5-(1,1-dioxido-1,2-thiazinan-2-yl)-n-(4-fluorobenzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamide
2
2008200816.0medium000200
l 708906
1
2008200816.0medium000100
jtk-303
5
aromatic ether;
monochlorobenzenes;
organofluorine compound;
quinolinemonocarboxylic acid;
quinolone		HIV-1 integrase inhibitor2008201115.0high000410
raltegravir
5
1,2,4-oxadiazole;
dicarboxylic acid amide;
hydroxypyrimidine;
monofluorobenzenes;
pyrimidone;
secondary carboxamide		antiviral drug;
HIV-1 integrase inhibitor		2008201115.0high000410
trigonoliimine a
1
201520159.0medium000010
ConditionIndicatedStudiesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
HIV0
1
2008200816.0high000100
Malignant Melanoma0
1
201720177.0high000010
Melanoma0
1
201720177.0high000010

Bioavailability (1)

ArticleYear
Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
Antimicrobial agents and chemotherapy, , Volume: 52, Issue:8		2008