5-(1,1-dioxido-1,2-thiazinan-2-yl)-n-(4-fluorobenzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamide profile

5-(1,1-dioxido-1,2-thiazinan-2-yl)-N-(4-fluorobenzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamide: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	457930
CHEMBL ID	414850
SCHEMBL ID	1198641
MeSH ID	M0488132

Synonym
l-870810
5-(1,1-dioxothiazinan-2-yl)-n-[(4-fluorophenyl)methyl]-8-hydroxy-1,6-naphthyridine-7-carboxamide
410545-86-7
l-870,810
1,6-naphthyridine-7-carboxamide, n-[(4-fluorophenyl)methyl]-8-hydroxy-5-(tetrahydro-1,1-dioxido-2h-1,2-thiazin-2-yl)-
l-000870810
5-(1,1-dioxo-1$l^{6},2-thiazinan-2-yl)-n-[(4-fluorophenyl)methyl]-8-hydroxy-1,6-naphthyridine-7-carboxamide
bdbm23402
chembl414850 ,
zyp ,
5-(1,1-dioxido-1,2-thiazinan-2-yl)-n-(4-fluorobenzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamide
bdbm50021581
1,6-naphthyridine-7-carboxamide, n-((4-fluorophenyl)methyl)-8-hydroxy-5-(tetrahydro-1,1-dioxido-2h-1,2-thiazin-2-yl)-
l 870810
unii-6txl33zfop
410544-95-5
6txl33zfop ,
SCHEMBL1198641
DTXSID10194025
DIDKWCOCQJWMDJ-UHFFFAOYSA-N
5-(1,1 dioxido-1,2-thiazinan-2-yl)-n-(4-fluorobenzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamide
Q27265521
PD161862
AKOS040746039

Excerpt	Relevance	Reference
" The pharmacokinetic profile of GS-9160 in healthy human volunteers revealed that once-daily dosing was not likely to achieve antiviral efficacy; hence, the clinical development of this compound was discontinued."	( Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. Chen, J; Chen, X; Geleziunas, R; Hesselgesser, J; Jin, H; Jones, GS; Kim, CU; Tsiang, M; Wright, M; Yu, F; Zeynalzadegan, A, 2009)	0.35

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Gag-Pol polyprotein	HIV-1 M:B_HXB2R	IC50 (µMol)	0.0285	0.0006	0.9141	8.3200	AID1798319; AID1798876
Calcitonin gene-related peptide 1	Homo sapiens (human)	IC50 (µMol)	28.0000	0.0001	0.0012	0.0022	AID625502
Calcitonin gene-related peptide 1	Homo sapiens (human)	Ki	7.3000	0.0000	2.4336	7.3000	AID625500
Reverse transcriptase/RNaseH	Human immunodeficiency virus 1	IC50 (µMol)	0.0050	0.0001	1.0768	10.0000	AID1157011
Integrase	Human immunodeficiency virus 1	IC50 (µMol)	0.9932	0.0005	1.5443	10.0000	AID1157025; AID254835; AID254918; AID254935; AID254957; AID261280; AID268609; AID305890; AID327558; AID327560; AID327561; AID413246; AID413252; AID413253; AID414282; AID519018; AID519038; AID541108; AID573970; AID573971; AID710552; AID710553
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Integrase	Human immunodeficiency virus 1	Kd	0.0033	0.0033	1.0098	3.0000	AID519018
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
viral life cycle	Gag-Pol polyprotein	HIV-1 M:B_HXB2R
establishment of integrated proviral latency	Gag-Pol polyprotein	HIV-1 M:B_HXB2R
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
peptidase activity	Gag-Pol polyprotein	HIV-1 M:B_HXB2R
integrase activity	Gag-Pol polyprotein	HIV-1 M:B_HXB2R
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
extracellular region	Calcitonin gene-related peptide 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (183)

Assay ID	Title	Year	Journal	Article
AID1338583	Therapeutic Index, ratio of CC50 for human C8166 cells to EC50 for HIV1 3B infected in human C8166 cells	2017	European journal of medicinal chemistry, Jan-05, Volume: 125	Discovery of novel 3-hydroxypicolinamides as selective inhibitors of HIV-1 integrase-LEDGF/p75 interaction.
AID305897	Oral bioavailability in dog at 1 mg/kg	2007	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5	A potent and orally active HIV-1 integrase inhibitor.
AID1157025	Inhibition of HIV1 integrase bound with donor DNA-SPA beads using 3'-end fluorescein isothiocyanate labeled target DNA as substrate assessed as strand transfer activity incubated prior to substrate addition	2014	European journal of medicinal chemistry, Aug-18, Volume: 83	Pyridopyrimidinone inhibitors of HIV-1 RNase H.
AID305903	Clearance in dog at 1 mg/kg, iv	2007	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5	A potent and orally active HIV-1 integrase inhibitor.
AID541166	Selectivity ratio of EC50 for antiviral activity against HIV1 harboring G140S mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID413253	Inhibition of HIV1 integrase strand transfer activity	2008	Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24	Design, synthesis, and biological evaluation of a series of 2-hydroxyisoquinoline-1,3(2H,4H)-diones as dual inhibitors of human immunodeficiency virus type 1 integrase and the reverse transcriptase RNase H domain.
AID541126	Cytotoxicity against human SupT1 cells infected with HIV1 3B	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID541153	Selectivity ratio of EC50 for antiviral activity against EFV-resistant HIV1 selected after 7 passages to EC50 for antiviral activity against wild-type HIV1 3B	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID364243	Antiviral activity against HIV1 with integrase V151I mutation by single cycle infectivity assay in presence of 10%FBS	2008	Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18	Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection.
AID541165	Selectivity ratio of EC50 for antiviral activity against HIV1 harboring E138K mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID525105	Antiviral 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 compound	2008	Antimicrobial 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.
AID305911	Antiviral activity against HIV1 with integrase T66l/S153Y mutant	2007	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5	A potent and orally active HIV-1 integrase inhibitor.
AID305896	Oral bioavailability in rat at 10 mg/kg	2007	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5	A potent and orally active HIV-1 integrase inhibitor.
AID573995	Ratio 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 integrase	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID573974	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for Human immunodeficiency virus 1 3B	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID327557	Inhibition of HIV1 integrase using labelled oligonucleotide substrate in presence of bovine serum albumin by ELISA	2008	Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8	Reaction of rosmarinic acid with nitrite ions in acidic conditions: discovery of nitro- and dinitrorosmarinic acids as new anti-HIV-1 agents.
AID541112	Cytotoxicity against human MT2 cells infected with HIV1 3B by three fold dilution method in presence of 10% FBS	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID305908	Antiviral activity against HIV1 with integrase F121Y mutant	2007	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5	A potent and orally active HIV-1 integrase inhibitor.
AID541115	Cytotoxicity against human MT4 cells infected with HIV1 3B by three fold dilution method in presence of 10% FBS	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID573970	Inhibition of Human immunodeficiency virus 1 integrase	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID562351	Antiviral activity against HIV1 K-2 harboring integrase D10E, R20K, I113V, A124T, K188R, V201I, T206S, N232D, D278G mutant gene infected in human TZM-bl cells assessed as beta-galactosidase expression after 48 hrs by microplate luminometry relative to HIV	2009	Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10	Natural polymorphisms of human immunodeficiency virus type 1 integrase and inherent susceptibilities to a panel of integrase inhibitors.
AID305895	Solubility at pH 7.4 by equilibrium solubility assay	2007	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5	A potent and orally active HIV-1 integrase inhibitor.
AID541152	Selectivity ratio of EC50 for antiviral activity against EFV-resistant HIV1 selected after 3 passages to EC50 for antiviral activity against wild-type HIV1 3B	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID1338577	Inhibition of HIV1 recombinant GST/His-tagged integrase 3'-processing activity expressed in Escherichia coli BL21(DE3) assessed as reduction in 19-mer product using 5'-end 32P labeled linear 21-mer substrate preincubated for 30 mins followed by substrate	2017	European journal of medicinal chemistry, Jan-05, Volume: 125	Discovery of novel 3-hydroxypicolinamides as selective inhibitors of HIV-1 integrase-LEDGF/p75 interaction.
AID541108	Inhibition of HIV1 integrase strand transfer activity	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID305909	Antiviral activity against HIV1 with integrase T125K mutant	2007	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5	A potent and orally active HIV-1 integrase inhibitor.
AID327559	Inhibition of HIV1 integrase using labelled U5A/U5B double stranded DNA substrate	2008	Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8	Reaction of rosmarinic acid with nitrite ions in acidic conditions: discovery of nitro- and dinitrorosmarinic acids as new anti-HIV-1 agents.
AID562349	Antiviral activity against HIV1 G-8 harboring integrase D10E, L101I, S119T, A124T, M154L, V201I, N232D, S283G mutant gene infected in human TZM-bl cells assessed as beta-galactosidase expression after 48 hrs by microplate luminometry relative to HIV1 R7/3	2009	Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10	Natural polymorphisms of human immunodeficiency virus type 1 integrase and inherent susceptibilities to a panel of integrase inhibitors.
AID1338582	Cytotoxicity against human C8166 cells assessed as reduction in cell viability after 72 hrs by MTT assay	2017	European journal of medicinal chemistry, Jan-05, Volume: 125	Discovery of novel 3-hydroxypicolinamides as selective inhibitors of HIV-1 integrase-LEDGF/p75 interaction.
AID519041	Antiviral activity against vesicular stomatitis virus G-pseudotyped Human immunodeficiency virus infected in human MT-4 cells assessed as inhibition of viral replication	2008	Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3	The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
AID254835	Strand transfer inhibitory activity against HIV-1 integrase	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	Pharmacophore-based design of HIV-1 integrase strand-transfer inhibitors.
AID562348	Antiviral activity against HIV1 B-28 harboring integrase D10E, R20K, S39C, V72I, A124N, T125V, V201I, N232D mutant gene infected in human TZM-bl cells assessed as beta-galactosidase expression after 48 hrs by microplate luminometry relative to HIV1 R7/3 e	2009	Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10	Natural polymorphisms of human immunodeficiency virus type 1 integrase and inherent susceptibilities to a panel of integrase inhibitors.
AID710551	Antiviral activity against HIV1 3B infected in human C8166 cells assessed as reduction in virus-induced cytopathogenicity measured after 3 days by syncytium reduction assay	2012	Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22	Repositioning HIV-1 integrase inhibitors for cancer therapeutics: 1,6-naphthyridine-7-carboxamide as a promising scaffold with drug-like properties.
AID541129	Selectivity ratio of EC50 for antiviral activity against NRTI-resistant HIV1 harboring RTK65R mutant gene to EC50 for antiviral activity against wild-type HIV1 3B	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID305902	Clearance in rat at 2 mg/kg, iv	2007	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5	A potent and orally active HIV-1 integrase inhibitor.
AID305899	Half life in rat at 2 mg/kg, iv	2007	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5	A potent and orally active HIV-1 integrase inhibitor.
AID625502	Inhibition of CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production after 1 hr	2011	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 21, Issue:22	Identification of a novel RAMP-independent CGRP receptor antagonist.
AID305892	Antiviral activity against HIV1 3B in MT4 cells assessed as decrease in HIV1 p24 core antigen in presence of normal human serum	2007	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5	A potent and orally active HIV-1 integrase inhibitor.
AID305907	Antiviral activity against HIV1 with integrase V151l mutant	2007	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5	A potent and orally active HIV-1 integrase inhibitor.
AID541173	Selectivity ratio of EC50 for antiviral activity against HIV1 harboring E138K and Q148K mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID519018	Displacement of 20 nM [3H]GSK304649 from Human immunodeficiency virus 1 integrase by scintillation proximity assay	2008	Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3	The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
AID541171	Selectivity ratio of EC50 for antiviral activity against HIV1 harboring L74M and E92V mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID541162	Selectivity ratio of EC50 for antiviral activity against HIV1 harboring L74M mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID327563	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction of virus-induced cytopathogenicity by MTT assay	2008	Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8	Reaction of rosmarinic acid with nitrite ions in acidic conditions: discovery of nitro- and dinitrorosmarinic acids as new anti-HIV-1 agents.
AID519022	Antiviral activity against Human immunodeficiency virus 1 NL432 infected in human MT-4 cells assessed as decrease in the integrated viral DNA	2008	Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3	The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
AID573999	Ratio of EC50 for Human immunodeficiency virus in presence of 10% FCS to EC50 for Human immunodeficiency virus in presence of 50% human serum	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID573973	Cytotoxicity against human MT4 cells by MTT assay	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID364242	Antiviral activity against HIV1 with integrase T66I mutation by single cycle infectivity assay in presence of 10%FBS	2008	Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18	Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection.
AID414283	Antiviral activity against HIV by pseudo-type HIV assay	2009	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6	The use of oxadiazole and triazole substituted naphthyridines as HIV-1 integrase inhibitors. Part 1: Establishing the pharmacophore.
AID305894	Partition coefficient, log P at pH 7.4	2007	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5	A potent and orally active HIV-1 integrase inhibitor.
AID541120	Selectivity index, ratio of CC50 for human T lymphocyte cells to EC50 for HIV1 BAL in presence of 10% FBS	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID541169	Selectivity ratio of EC50 for antiviral activity against HIV1 harboring N155H mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID305900	Half life in dog at 1 mg/kg, iv	2007	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5	A potent and orally active HIV-1 integrase inhibitor.
AID541168	Selectivity ratio of EC50 for antiviral activity against HIV1 harboring V151A mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID541172	Selectivity ratio of EC50 for antiviral activity against HIV1 harboring E92V and V151A mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID1295697	Inhibition of HIV Integrase assessed as suppression pre-Integrase complex catalyzed strand transfer to a labeled target piece of DNA	2016	Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7	Anti-HIV Drug Discovery and Development: Current Innovations and Future Trends.
AID573998	Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for CHI/1043-resistant Human immunodeficiency virus harboring T66I and Q146K mutations in integrase	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID541163	Selectivity ratio of EC50 for antiviral activity against HIV1 harboring E92Q mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID541130	Selectivity ratio of EC50 for antiviral activity against NRTI-resistant HIV1 harboring RTM184V mutant gene to EC50 for antiviral activity against wild-type HIV1 3B	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID525114	Antiviral 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 assay	2008	Antimicrobial 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.
AID710546	Cytotoxicity against p53 expressing human HCT116 cells incubated for 72 hrs by MTT assay	2012	Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22	Repositioning HIV-1 integrase inhibitors for cancer therapeutics: 1,6-naphthyridine-7-carboxamide as a promising scaffold with drug-like properties.
AID573972	Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as inhibition of viral replication	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID541161	Selectivity ratio of EC50 for antiviral activity against HIV1 harboring T66I mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID364245	Antiviral activity against HIV1 with integrase T125K mutation by single cycle infectivity assay in presence of 10%FBS	2008	Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18	Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection.
AID710544	Cytotoxicity against human MCF7 cells incubated for 72 hrs by MTT assay	2012	Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22	Repositioning HIV-1 integrase inhibitors for cancer therapeutics: 1,6-naphthyridine-7-carboxamide as a promising scaffold with drug-like properties.
AID541157	Selectivity ratio of EC50 for antiviral activity against GS-9160-resistant HIV1 selected after 6 low passages to EC50 for antiviral activity against wild-type HIV1 3B	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID268613	Antiviral activity against HIV1 3B assessed as protein binding effect in MT2 cells	2006	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15	Design, synthesis, and SAR studies of novel and highly active tri-cyclic HIV integrase inhibitors.
AID710548	Cytotoxicity against human MDA-MB-435 cells incubated for 72 hrs by MTT assay	2012	Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22	Repositioning HIV-1 integrase inhibitors for cancer therapeutics: 1,6-naphthyridine-7-carboxamide as a promising scaffold with drug-like properties.
AID562342	Antiviral activity against HIV1 F-15 harboring integrase D10E, K42T, A124N, T125A, V126L, M154L, V201I, T206S, N232D, V281S mutant gene infected in human TZM-bl cells assessed as beta-galactosidase expression after 48 hrs by microplate luminometry relativ	2009	Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10	Natural polymorphisms of human immunodeficiency virus type 1 integrase and inherent susceptibilities to a panel of integrase inhibitors.
AID1157011	Inhibition of HIV1 reverse transcriptase strand transfer activity	2014	European journal of medicinal chemistry, Aug-18, Volume: 83	Pyridopyrimidinone inhibitors of HIV-1 RNase H.
AID525109	Antiviral 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 compound	2008	Antimicrobial 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.
AID519038	Inhibition of Human immunodeficiency virus 1 integrase by strand transfer scintillation proximity assay	2008	Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3	The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
AID541175	Selectivity ratio of EC50 for antiviral activity against HIV1 harboring G140S and Q148H mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID710553	Inhibition of HIV1 integrase 3'-processing activity using [32P]-labeled linear oligonucleotide substrate	2012	Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22	Repositioning HIV-1 integrase inhibitors for cancer therapeutics: 1,6-naphthyridine-7-carboxamide as a promising scaffold with drug-like properties.
AID1295696	Antiviral activity against HIV infected in human MT4 cells assessed as suppression of viral replication	2016	Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7	Anti-HIV Drug Discovery and Development: Current Innovations and Future Trends.
AID541170	Selectivity ratio of EC50 for antiviral activity against HIV1 harboring N155S mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID525112	Antiviral 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 assay	2008	Antimicrobial 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.
AID305890	Inhibition of HIV1 recombinant integrase catalyzed strand transfer activity	2007	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5	A potent and orally active HIV-1 integrase inhibitor.
AID364248	Antiviral activity against HIV1 with integrase N155S mutation by single cycle infectivity assay in presence of 10%FBS	2008	Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18	Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection.
AID525107	Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay	2008	Antimicrobial 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.
AID541160	Selectivity ratio of EC50 for antiviral activity against GS-9160-resistant HIV1 selected after 9 passages to EC50 for antiviral activity against wild-type HIV1 3B	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID525106	Antiviral 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 compound	2008	Antimicrobial 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.
AID525103	Antiviral activity against HIV 1 3B infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 50 passages in presence of compound	2008	Antimicrobial 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.
AID541128	Antiviral activity against HIV1 infected in SupT1 cells assessed as accumulation of integrated junction products after 48 hrs by Alu-PCR assay	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID541123	Antiviral activity against HIV1 3B infected in SupT1 cells assessed as fold increase in viral 2-LTR circles accumulation after 3 hrs postinfection by TaqMan real-time PCR	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID625500	Displacement of [125I]adrenomedullin form CGRP receptor in human SK-N-MC cell membrane by competitive binding assay	2011	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 21, Issue:22	Identification of a novel RAMP-independent CGRP receptor antagonist.
AID256472	Selectivity index was measured by the ratio of CC50/EC50	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	Pharmacophore-based design of HIV-1 integrase strand-transfer inhibitors.
AID541155	Selectivity ratio of EC50 for antiviral activity against APV-resistant HIV1 selected after 4 passages to EC50 for antiviral activity against wild-type HIV1 3B	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID573997	Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for MK-0518-resistant Human immunodeficiency virus harboring G140S and Q148H mutations in integrase	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID268614	Solubility at pH 7.3	2006	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15	Design, synthesis, and SAR studies of novel and highly active tri-cyclic HIV integrase inhibitors.
AID541134	Selectivity ratio of EC50 for antiviral activity against PI-resistant HIV1 harboring RTI84V, L90M mutant gene to EC50 for antiviral activity against wild-type HIV1 3B	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID305904	Clearance in rhesus monkey at 1 mg/kg, iv	2007	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5	A potent and orally active HIV-1 integrase inhibitor.
AID541135	Selectivity ratio of EC50 for antiviral activity against PI-resistant HIV1 harboring RTG48V, V82A and L90M mutant gene to EC50 for antiviral activity against wild-type HIV1 3B	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID305893	Protein binding in human plasma by ultrafiltration method	2007	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5	A potent and orally active HIV-1 integrase inhibitor.
AID562343	Antiviral activity against HIV1 A-6 harboring integrase D10E, V72I, A124T, M154I, R199K, V201I, N232D mutant gene infected in human TZM-bl cells assessed as beta-galactosidase expression after 48 hrs by microplate luminometry relative to HIV1 R7/3 express	2009	Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10	Natural polymorphisms of human immunodeficiency virus type 1 integrase and inherent susceptibilities to a panel of integrase inhibitors.
AID255621	Cytotoxic concentration required to reduce MT-4 cell viability	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	Pharmacophore-based design of HIV-1 integrase strand-transfer inhibitors.
AID710534	Inhibition of ErbB2 at 10 uM incubated for 60 mins using poly(Glu,Tyr)4:1 substrate and 10 uM ATP by ELISA	2012	Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22	Repositioning HIV-1 integrase inhibitors for cancer therapeutics: 1,6-naphthyridine-7-carboxamide as a promising scaffold with drug-like properties.
AID710549	Therapeutic index, ratio of CC50 for human C8166 cells to EC50 for HIV1 3B	2012	Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22	Repositioning HIV-1 integrase inhibitors for cancer therapeutics: 1,6-naphthyridine-7-carboxamide as a promising scaffold with drug-like properties.
AID305906	Antiviral activity against HIV1 with integrase T661 mutant	2007	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5	A potent and orally active HIV-1 integrase inhibitor.
AID541117	Antiviral activity against 0.001 MOI HIV1 BAL infected in human T lymphocyte cells by p24 antigen ELISA in presence of 10% FBS	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID413252	Inhibition of HIV1 integrase 3'-end processing activity	2008	Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24	Design, synthesis, and biological evaluation of a series of 2-hydroxyisoquinoline-1,3(2H,4H)-diones as dual inhibitors of human immunodeficiency virus type 1 integrase and the reverse transcriptase RNase H domain.
AID1338578	Inhibition of HIV1 recombinant GST/His-tagged integrase strand transfer activity expressed in Escherichia coli BL21(DE3) using 5'-end 32P labeled linear 21-mer substrate preincubated for 30 mins followed by substrate addition measured after 1 hr by PAGE a	2017	European journal of medicinal chemistry, Jan-05, Volume: 125	Discovery of novel 3-hydroxypicolinamides as selective inhibitors of HIV-1 integrase-LEDGF/p75 interaction.
AID562350	Antiviral activity against HIV1 G-4 harboring integrase K7R, D10E, S39C, L74I, K156R, K215N, T218I, N232D, L234I mutant gene infected in human TZM-bl cells assessed as beta-galactosidase expression after 48 hrs by microplate luminometry relative to HIV1 R	2009	Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10	Natural polymorphisms of human immunodeficiency virus type 1 integrase and inherent susceptibilities to a panel of integrase inhibitors.
AID541109	Antiviral activity against HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 10% FBS	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID519017	Antiviral activity against Human immunodeficiency virus 1 Ba-L infected in human PBMCs assessed as inhibition of viral replication	2008	Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3	The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
AID255649	Effective concentration required to reduce HIV-1-induced cytopathic effect in MT-4 cells	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	Pharmacophore-based design of HIV-1 integrase strand-transfer inhibitors.
AID305910	Antiviral activity against HIV1 with integrase T66l/M154l mutant	2007	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5	A potent and orally active HIV-1 integrase inhibitor.
AID541131	Selectivity ratio of EC50 for antiviral activity against NRTI-resistant HIV1 harboring RT-6TAMs mutant gene to EC50 for antiviral activity against wild-type HIV1 3B	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID327560	Inhibition of HIV1 integrase 3'-processing activity using labelled oligonucleotide substrate by ELISA	2008	Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8	Reaction of rosmarinic acid with nitrite ions in acidic conditions: discovery of nitro- and dinitrorosmarinic acids as new anti-HIV-1 agents.
AID541150	Selectivity ratio of EC50 for antiviral activity against 3TC-resistant HIV1 selected after 4 passages to EC50 for antiviral activity against wild-type HIV1 3B	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID562345	Antiviral activity against HIV1 R-31 harboring integrase D10E, E11D, V32I, V37I, V72I, L101I, T112I, A124N, T125A, K173R, A205S, Q216H, N222K, S230N, N232D mutant gene infected in human TZM-bl cells assessed as beta-galactosidase expression after 48 hrs b	2009	Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10	Natural polymorphisms of human immunodeficiency virus type 1 integrase and inherent susceptibilities to a panel of integrase inhibitors.
AID254957	In vitro concentration required to inhibit the overall HIV-1 integrase strand transfer	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	Pharmacophore-based design of HIV-1 integrase strand-transfer inhibitors.
AID562353	Antiviral activity against HIV1 harboring integrase N155H mutant infected in human TZM-bl cells assessed as beta-galactosidase expression after 48 hrs by microplate luminometry relative to HIV1 R7/3 expressing wild type integrase enzyme relative to HIV1 R	2009	Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10	Natural polymorphisms of human immunodeficiency virus type 1 integrase and inherent susceptibilities to a panel of integrase inhibitors.
AID562344	Antiviral activity against HIV1 R-6 harboring integrase D10E, E11D, S17N, A23V, L28I, P30A, V72I, L101I, S119T, T122I, A124T, V201I, N222D, N232D, S230G, D253E, N254G mutant gene infected in human TZM-bl cells assessed as beta-galactosidase expression aft	2009	Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10	Natural polymorphisms of human immunodeficiency virus type 1 integrase and inherent susceptibilities to a panel of integrase inhibitors.
AID364247	Antiviral activity against HIV1 with integrase T66I/S153Y mutation by single cycle infectivity assay in presence of 10%FBS	2008	Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18	Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection.
AID525108	Antiviral 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 compound	2008	Antimicrobial 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.
AID562352	Antiviral activity against HIV1 harboring integrase T97A mutant infected in human TZM-bl cells assessed as beta-galactosidase expression after 48 hrs by microplate luminometry relative to HIV1 R7/3 expressing wild type integrase enzyme relative to HIV1 R7	2009	Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10	Natural polymorphisms of human immunodeficiency virus type 1 integrase and inherent susceptibilities to a panel of integrase inhibitors.
AID541158	Selectivity ratio of EC50 for antiviral activity against GS-9160-resistant HIV1 selected after 6 passages to EC50 for antiviral activity against wild-type HIV1 3B	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID413246	Inhibition of HIV1 integrase	2008	Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24	Design, synthesis, and biological evaluation of a series of 2-hydroxyisoquinoline-1,3(2H,4H)-diones as dual inhibitors of human immunodeficiency virus type 1 integrase and the reverse transcriptase RNase H domain.
AID541116	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B in presence of 10% FBS	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID268612	Cytotoxicity against MT4 cells	2006	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15	Design, synthesis, and SAR studies of novel and highly active tri-cyclic HIV integrase inhibitors.
AID541122	Antiviral activity against 0.04 MOI HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 100% human serum	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID541154	Selectivity ratio of EC50 for antiviral activity against APV-resistant HIV1 selected after 2 passages to EC50 for antiviral activity against wild-type HIV1 3B	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID261281	Antiviral activity against HIV1 3b in human MT4 cells	2006	Journal of medicinal chemistry, Mar-09, Volume: 49, Issue:5	Novel HIV-1 integrase inhibitors derived from quinolone antibiotics.
AID710547	Cytotoxicity against p53 deficient human HCT116 cells incubated for 72 hrs by MTT assay	2012	Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22	Repositioning HIV-1 integrase inhibitors for cancer therapeutics: 1,6-naphthyridine-7-carboxamide as a promising scaffold with drug-like properties.
AID710532	Inhibition of KDR at 10 uM incubated for 60 mins using poly(Glu,Tyr)4:1 substrate and 10 uM ATP by ELISA	2012	Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22	Repositioning HIV-1 integrase inhibitors for cancer therapeutics: 1,6-naphthyridine-7-carboxamide as a promising scaffold with drug-like properties.
AID541167	Selectivity ratio of EC50 for antiviral activity against HIV1 harboring Q148K mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID562347	Antiviral activity against HIV1 B-27 harboring integrase D10E, R20K, S39C, V72I, A124N, T125M, V201I, N232D mutant gene infected in human TZM-bl cells assessed as beta-galactosidase expression after 48 hrs by microplate luminometry relative to HIV1 R7/3 e	2009	Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10	Natural polymorphisms of human immunodeficiency virus type 1 integrase and inherent susceptibilities to a panel of integrase inhibitors.
AID519021	Antiviral activity against Human immunodeficiency virus 1 NL432 infected in human MT-4 cells assessed as effect on total viral DNA	2008	Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3	The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
AID364250	Antiviral activity against HIV1 with integrase T66I/L74M/V151I mutation by single cycle infectivity assay in presence of 10%FBS	2008	Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18	Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection.
AID305901	Half life in rhesus monkey at 1 mg/kg, iv	2007	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5	A potent and orally active HIV-1 integrase inhibitor.
AID305898	Oral bioavailability in rhesus monkey at 1 mg/kg	2007	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5	A potent and orally active HIV-1 integrase inhibitor.
AID541110	Antiviral activity against HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 10% FBS, HSA and alpha1-AGP	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID541156	Selectivity ratio of EC50 for antiviral activity against GS-9160-resistant HIV1 selected after 5 passages to EC50 for antiviral activity against wild-type HIV1 3B	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID268609	Inhibition of strand transfer activity of HIV integrase	2006	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15	Design, synthesis, and SAR studies of novel and highly active tri-cyclic HIV integrase inhibitors.
AID710535	Inhibition of EGFR at 10 uM incubated for 60 mins using poly(Glu,Tyr)4:1 substrate and 10 uM ATP by ELISA	2012	Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22	Repositioning HIV-1 integrase inhibitors for cancer therapeutics: 1,6-naphthyridine-7-carboxamide as a promising scaffold with drug-like properties.
AID541164	Selectivity ratio of EC50 for antiviral activity against HIV1 harboring E92V mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID414282	Inhibition of HIV1 recombinant integrase strand transfer activity	2009	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6	The use of oxadiazole and triazole substituted naphthyridines as HIV-1 integrase inhibitors. Part 1: Establishing the pharmacophore.
AID541127	Antiviral activity against HIV1 infected in SupT1 cells assessed as accumulation of late RT products after 12 hrs	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID573971	Inhibition of Human immunodeficiency virus 1 integrase strand transfer activity	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID541132	Selectivity ratio of EC50 for antiviral activity against NNRTI-resistant HIV1 harboring RTK103N mutant gene to EC50 for antiviral activity against wild-type HIV1 3B	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID261280	Inhibition of recombinant HIV1 integrase strand transfer activity	2006	Journal of medicinal chemistry, Mar-09, Volume: 49, Issue:5	Novel HIV-1 integrase inhibitors derived from quinolone antibiotics.
AID327561	Inhibition of HIV1 integrase strand transfer activity using labelled oligonucleotide substrate by ELISA	2008	Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8	Reaction of rosmarinic acid with nitrite ions in acidic conditions: discovery of nitro- and dinitrorosmarinic acids as new anti-HIV-1 agents.
AID710550	Toxicity against human C8166 cells incubated for 72 hrs by MTT assay	2012	Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22	Repositioning HIV-1 integrase inhibitors for cancer therapeutics: 1,6-naphthyridine-7-carboxamide as a promising scaffold with drug-like properties.
AID541119	Cytotoxicity against human T lymphocyte cells infected with HIV1 BAL by XTT method in presence of 10% FBS	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID541159	Selectivity ratio of EC50 for antiviral activity against GS-9160-resistant HIV1 selected after 8 passages to EC50 for antiviral activity against wild-type HIV1 3B	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID541151	Selectivity ratio of EC50 for antiviral activity against 3TC-resistant HIV1 selected after 8 passages to EC50 for antiviral activity against wild-type HIV1 3B	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID305912	Antiviral activity against HIV1 with integrase N155S mutant	2007	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5	A potent and orally active HIV-1 integrase inhibitor.
AID541113	Selectivity index, ratio of CC50 for human MT2 cells to EC50 for HIV1 3B in presence of 10% FBS	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID541121	Antiviral activity against 0.02 MOI HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 100% human serum	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID327565	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B	2008	Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8	Reaction of rosmarinic acid with nitrite ions in acidic conditions: discovery of nitro- and dinitrorosmarinic acids as new anti-HIV-1 agents.
AID562346	Antiviral activity against HIV1 N-19 harboring integrase D10E, E11D, D25E, V31I, I113V, S119G, A124N, V151I, V201I, N232D mutant gene infected in human TZM-bl cells assessed as beta-galactosidase expression after 48 hrs by microplate luminometry relative	2009	Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10	Natural polymorphisms of human immunodeficiency virus type 1 integrase and inherent susceptibilities to a panel of integrase inhibitors.
AID310942	Antiviral activity against human immunodeficiency virus 1 in cell culture	2007	European journal of medicinal chemistry, Sep, Volume: 42, Issue:9	Development of integrase inhibitors for treatment of AIDS: an overview.
AID541174	Selectivity ratio of EC50 for antiviral activity against HIV1 harboring E92V, G140S and V151A mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID254918	In vitro concentration required to inhibit the HIV-1 integrase strand transfer	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	Pharmacophore-based design of HIV-1 integrase strand-transfer inhibitors.
AID261282	Cytotoxic activity against human MT4 cells infected with HIV1 by MTT assay	2006	Journal of medicinal chemistry, Mar-09, Volume: 49, Issue:5	Novel HIV-1 integrase inhibitors derived from quinolone antibiotics.
AID541114	Antiviral activity against HIV1 3B infected in human MT-4 cells by two fold dilution method in presence of 10% FBS	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID525111	Antiviral activity against HIV 1 NL4.3 assessed as inhibition of virus-induced cytopathic effect by MTT assay	2008	Antimicrobial 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.
AID413254	Ratio of IC50 for HIV1 integrase 3'-end processing activity to IC50 for HIV1 integrase strand transfer activity	2008	Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24	Design, synthesis, and biological evaluation of a series of 2-hydroxyisoquinoline-1,3(2H,4H)-diones as dual inhibitors of human immunodeficiency virus type 1 integrase and the reverse transcriptase RNase H domain.
AID268611	Antiviral activity against HIV1 3B in MT2 cells	2006	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15	Design, synthesis, and SAR studies of novel and highly active tri-cyclic HIV integrase inhibitors.
AID573996	Ratio 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 integrase	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors.
AID327562	Ratio of IC50 for HIV1 integrase 3'-processing activity to IC50 for HIV1 integrase strand transfer activity	2008	Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8	Reaction of rosmarinic acid with nitrite ions in acidic conditions: discovery of nitro- and dinitrorosmarinic acids as new anti-HIV-1 agents.
AID1338581	Antiviral activity against HIV1 3B infected in human C8166 cells assessed as reduction in virus-induced cytopathic effect by MTT assay	2017	European journal of medicinal chemistry, Jan-05, Volume: 125	Discovery of novel 3-hydroxypicolinamides as selective inhibitors of HIV-1 integrase-LEDGF/p75 interaction.
AID327564	Cytotoxicity against human MT4 cells by MTT method	2008	Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8	Reaction of rosmarinic acid with nitrite ions in acidic conditions: discovery of nitro- and dinitrorosmarinic acids as new anti-HIV-1 agents.
AID364244	Antiviral activity against HIV1 with integrase F121Y mutation by single cycle infectivity assay in presence of 10%FBS	2008	Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18	Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection.
AID710533	Inhibition of SRC at 10 uM incubated for 60 mins using poly(Glu,Tyr)4:1 substrate and 10 uM ATP by ELISA	2012	Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22	Repositioning HIV-1 integrase inhibitors for cancer therapeutics: 1,6-naphthyridine-7-carboxamide as a promising scaffold with drug-like properties.
AID541118	Antiviral activity against 0.001 MOI HIV1 BAL infected in human T lymphocyte cells by p24 antigen ELISA in presence of 10% FBS, HSA and alpha1-AGP	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID519023	Antiviral activity against Human immunodeficiency virus 1 NL432 infected in human MT-4 cells assessed as increase in viral two-LTR circles	2008	Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3	The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
AID364246	Antiviral activity against HIV1 with integrase T66I/M154 mutation by single cycle infectivity assay in presence of 10%FBS	2008	Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18	Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection.
AID525110	Antiviral 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 compound	2008	Antimicrobial 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.
AID525104	Antiviral 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 compound	2008	Antimicrobial 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.
AID541133	Selectivity ratio of EC50 for antiviral activity against NNRTI-resistant HIV1 harboring RTY181C mutant gene to EC50 for antiviral activity against wild-type HIV1 3B	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID541111	Antiviral activity against 0.01 MOI HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 100% human serum	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
AID364249	Antiviral activity against HIV1 with integrase T125K/F121Y mutation by single cycle infectivity assay in presence of 10%FBS	2008	Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18	Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection.
AID710552	Inhibition of HIV1 integrase strand transfer activity using [32P]-labeled linear oligonucleotide substrate	2012	Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22	Repositioning HIV-1 integrase inhibitors for cancer therapeutics: 1,6-naphthyridine-7-carboxamide as a promising scaffold with drug-like properties.
AID519016	Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT-4 cells assessed as inhibition of viral replication	2008	Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3	The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
AID305891	Antiviral activity against HIV1 3B in MT4 cells assessed as decrease in HIV1 p24 core antigen in presence of FBS	2007	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5	A potent and orally active HIV-1 integrase inhibitor.
AID525102	Antiviral activity against HIV 1 3B infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay	2008	Antimicrobial 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.
AID327558	Inhibition of HIV1 integrase using labelled oligonucleotide substrate by ELISA	2008	Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8	Reaction of rosmarinic acid with nitrite ions in acidic conditions: discovery of nitro- and dinitrorosmarinic acids as new anti-HIV-1 agents.
AID525113	Antiviral 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 assay	2008	Antimicrobial 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.
AID254935	In vitro concentration required to inhibit the HIV-1 integrase 3' strand transfer	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	Pharmacophore-based design of HIV-1 integrase strand-transfer inhibitors.
AID1798319	Integrase 3-End Joining Assay from Article 10.1016/j.jmb.2008.04.054: \\Modeling, analysis, and validation of a novel HIV integrase structure provide insights into the binding modes of potent integrase inhibitors.\\	2008	Journal of molecular biology, Jul-11, Volume: 380, Issue:3	Modeling, analysis, and validation of a novel HIV integrase structure provide insights into the binding modes of potent integrase inhibitors.
AID1798876	HIV Integrase Strand Transfer Scintillation Proximity Assay (SPA) from Article 10.1016/j.bmcl.2009.01.090: \\The use of oxadiazole and triazole substituted naphthyridines as HIV-1 integrase inhibitors. Part 1: Establishing the pharmacophore.\\	2009	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6	The use of oxadiazole and triazole substituted naphthyridines as HIV-1 integrase inhibitors. Part 1: Establishing the pharmacophore.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	16 (76.19)	29.6817
2010's	5 (23.81)	24.3611
2020's	0 (0.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	2 (9.52%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	19 (90.48%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
ag-1549 capravirine: a non-nucleoside reverse transcriptase inhibitor	2.05	1
ciprofloxacin Ciprofloxacin: A broad-spectrum antimicrobial carboxyfluoroquinoline.. ciprofloxacin : A quinolone that is quinolin-4(1H)-one bearing cyclopropyl, carboxylic acid, fluoro and piperazin-1-yl substituents at positions 1, 3, 6 and 7, respectively.	2.03	1	aminoquinoline; cyclopropanes; fluoroquinolone antibiotic; N-arylpiperazine; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone; zwitterion	antibacterial drug; antiinfective agent; antimicrobial agent; DNA synthesis inhibitor; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; environmental contaminant; topoisomerase IV inhibitor; xenobiotic
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.	2.04	1	cyclopropanes; dipyridodiazepine	antiviral drug; HIV-1 reverse transcriptase inhibitor
ag 1879 3-(4-chlorophenyl)-1-(1,1-dimethylethyl)-1H-pyrazolo(3,4-d)pyrimidin-4-amine: Fyn kinase inhibitor	2.07	1	aromatic amine; monochlorobenzenes; pyrazolopyrimidine	beta-adrenergic antagonist; EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor; geroprotector
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.	2.44	2	azide; pyrimidine 2',3'-dideoxyribonucleoside	antimetabolite; antiviral drug; HIV-1 reverse transcriptase inhibitor
lamivudine [no description available]	2.05	1	monothioacetal; nucleoside analogue; oxacycle; primary alcohol	allergen; anti-HBV agent; antiviral drug; EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor; HIV-1 reverse transcriptase inhibitor; prodrug
emtricitabine Emtricitabine: A deoxycytidine analog and REVERSE TRANSCRIPTASE INHIBITOR with antiviral activity against HIV-1 and HEPATITIS B viruses. It is used to treat HIV INFECTIONS.. emtricitabine : An organofluorine compound that is 5-fluorocytosine substituted at the 1 position by a 2-(hydroxymethyl)-1,3-oxathiolan-5-yl group (2R,5S configuration). It is used in combination therapy for the treatment of HIV-1 infection.	2.05	1	monothioacetal; nucleoside analogue; organofluorine compound; pyrimidone	antiviral drug; HIV-1 reverse transcriptase inhibitor
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.	2.73	3	acetylenic 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.	2.04	1	aryl 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.	2.04	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
amprenavir [no description available]	2.05	1	carbamate ester; sulfonamide; tetrahydrofuryl ester	antiviral drug; HIV protease inhibitor
sesamol sesamol: constituent of sesame oil; RN given refers to parent cpd; structure in first source	3.23	1	benzodioxoles
lopinavir [no description available]	3.58	2	amphetamines; dicarboxylic acid diamide	anticoronaviral agent; antiviral drug; HIV protease inhibitor
5,6-dihydroxy-2-indolylcarboxylic acid 5,6-dihydroxyindole-2-carboxylic acid : A dihydroxyindole that is indole-2-carboxylic acid substituted by hydroxy groups at positions 5 and 6.	3.13	1	dihydroxyindole	mouse metabolite
1-(2',6'-difluorophenyl)-1h,3h-thiazolo(3,4-a)benzimidazole 1-(2',6'-difluorophenyl)-1H,3H-thiazolo(3,4-a)benzimidazole: anti-HIV agent; a non-nucleoside reverse transcriptase inhibitor; structure given in first source	3.23	1
lapatinib [no description available]	2.07	1	furans; organochlorine compound; organofluorine compound; quinazolines	antineoplastic agent; tyrosine kinase inhibitor
darunavir Darunavir: An HIV PROTEASE INHIBITOR that is used in the treatment of AIDS and HIV INFECTIONS. Due to the emergence of ANTIVIRAL DRUG RESISTANCE when used alone, it is administered in combination with other ANTI-HIV AGENTS.. darunavir : An N,N-disubstituted benzenesulfonamide bearing an unsubstituted amino group at the 4-position, used for the treatment of HIV infection. A second-generation HIV protease inhibitor, darunavir was designed to form robust interactions with the protease enzyme from many strains of HIV, including those from treatment-experienced patients with multiple resistance mutations to other protease inhibitors.	3.23	1	carbamate ester; furofuran; sulfonamide	antiviral drug; HIV protease inhibitor
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.	3.85	3	1,3-thiazoles; carbamate ester; carboxamide; L-valine derivative; ureas	antiviral drug; environmental contaminant; HIV protease inhibitor; xenobiotic
l 731988 L 731988: structure in first source	3.54	2
l 708906 [no description available]	3.54	2
bms-488043 BMS-488043: anti-HIV agent	3.23	1
2-hydroxy-4h-isoquinoline-1,3-dione 2-hydroxy-4H-isoquinoline-1,3-dione: structure in first source	2.47	2
jtk-303 [no description available]	4.52	7	aromatic ether; monochlorobenzenes; organofluorine compound; quinolinemonocarboxylic acid; quinolone	HIV-1 integrase inhibitor
rosmarinic acid rosmarinic acid: RN given refers to parent cpd; promote OT project. (R)-rosmarinic acid : A stereoisomer of rosmarinic acid having (R)-configuration.. rosmarinic acid : The 1-carboxy-2-(2,4-dihydroxyphenyl)ethyl ester of trans-caffeic acid.	2.04	1	rosmarinic acid	geroprotector; plant metabolite
ellagic acid [no description available]	3.13	1	catechols; cyclic ketone; lactone; organic heterotetracyclic compound; polyphenol	antioxidant; EC 1.14.18.1 (tyrosinase) inhibitor; EC 2.3.1.5 (arylamine N-acetyltransferase) inhibitor; EC 2.4.1.1 (glycogen phosphorylase) inhibitor; EC 2.5.1.18 (glutathione transferase) inhibitor; EC 2.7.1.127 (inositol-trisphosphate 3-kinase) inhibitor; EC 2.7.1.151 (inositol-polyphosphate multikinase) inhibitor; EC 2.7.4.6 (nucleoside-diphosphate kinase) inhibitor; EC 2.7.7.7 (DNA-directed DNA polymerase) inhibitor; EC 5.99.1.2 (DNA topoisomerase) inhibitor; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; food additive; fungal metabolite; geroprotector; plant metabolite; skin lightening agent
su 11248 [no description available]	2.07	1	monocarboxylic acid amide; pyrroles	angiogenesis inhibitor; antineoplastic agent; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor; immunomodulator; neuroprotective agent; vascular endothelial growth factor receptor antagonist
bms 806 BMS 806: prevents entry of HIV into cells by binding HIV envelope protein gp120; no further info available 4/2002	3.23	1
tenofovir disoproxil fumarate tenofovir disoproxil fumarate : A fumarate salt prepared from equimolar amounts of tenofovir disoproxil and fumaric acid. It is used in combination therapy for the treatment of HIV infection.	2.05	1	fumarate salt	antiviral drug; HIV-1 reverse transcriptase inhibitor; prodrug
s 1360 [no description available]	2.44	2
n-(4-fluorobenzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamide N-(4-fluorobenzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamide: HIV-1 integrase inhibitor; structure in first source	2.44	2
bms-626529 [no description available]	3.23	1
telcagepant telcagepant: structure in first source	2.06	1
raltegravir potassium Raltegravir Potassium: A pyrrolidinone derivative and HIV INTEGRASE INHIBITOR that is used in combination with other ANTI-HIV AGENTS for the treatment of HIV INFECTION.	2.04	1
mk 3207 [no description available]	2.06	1
chi 1043 [no description available]	2.44	2
raltegravir [no description available]	3.43	7	1,2,4-oxadiazole; dicarboxylic acid amide; hydroxypyrimidine; monofluorobenzenes; pyrimidone; secondary carboxamide	antiviral drug; HIV-1 integrase inhibitor
gsk364735 GSK364735: structure in first source	2.04	1

Condition	Relationship Strength	Studies
Acquired Immune Deficiency Syndrome [description not available]	2.95	1
Acquired Immunodeficiency Syndrome An acquired defect of cellular immunity associated with infection by the human immunodeficiency virus (HIV), a CD4-positive T-lymphocyte count under 200 cells/microliter or less than 14% of total lymphocytes, and increased susceptibility to opportunistic infections and malignant neoplasms. Clinical manifestations also include emaciation (wasting) and dementia. These elements reflect criteria for AIDS as defined by the CDC in 1993.	2.95	1
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.	2.46	2
HIV Coinfection [description not available]	3.16	5
HIV Infections Includes the spectrum of human immunodeficiency virus infections that range from asymptomatic seropositivity, thru AIDS-related complex (ARC), to acquired immunodeficiency syndrome (AIDS).	3.16	5
Sensitivity and Specificity Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)	2.44	2
Benign Neoplasms [description not available]	2.07	1
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.	2.07	1

5-(1,1-dioxido-1,2-thiazinan-2-yl)-n-(4-fluorobenzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamide

Description

Cross-References

Synonyms (24)

Research Excerpts

Dosage Studied

Protein Targets (4)

Inhibition Measurements

Activation Measurements

Other Measurements

Biological Processes (2)

Molecular Functions (2)

Ceullar Components (1)

Bioassays (183)

Research

Studies (21)

Market Indicators

Research Demand Index: 11.22

Study Types

5-(1,1-dioxido-1,2-thiazinan-2-yl)-n-(4-fluorobenzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamide

Description

Cross-References

Synonyms (24)

Research Excerpts

Dosage Studied

Protein Targets (4)

Inhibition Measurements

Activation Measurements

Other Measurements

Biological Processes (2)

Molecular Functions (2)

Ceullar Components (1)

Bioassays (183)

Research

Studies (21)

Market Indicators

Research Demand Index: 11.22

Study Types

Related Drugs (37)

Related Conditions (8)