Compounds > gsk364735
Page last updated: 2024-11-13

gsk364735

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Description

GSK364735: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID54718859
CHEMBL ID1256978
SCHEMBL ID5545304
MeSH IDM0585907

Synonyms (18)

Synonym
bdbm50045107
chembl1256978 ,
gsk364735
7-[(4-fluorophenyl)methyl]-4-hydroxy-n-(2-hydroxyethyl)-1-methyl-2-oxo-1,5-naphthyridine-3-carboxamide
s-364735
gsk-364735
QWLNINWUBHHOLU-UHFFFAOYSA-N
7-[(4-fluorophenyl)methyl]-4-hydroxy-n-(2-hydroxyethyl)-1-methyl-2-oxo-1,2-dihydro-1,5-naphthyridine-3-carboxamide
SCHEMBL5545304
7-((4-fluorophenyl)methyl)-4-hydroxy-n-(2-hydroxyethyl)-1-methyl-2-oxo-1,5-naphthyridine-3-carboxamide
1,5-naphthyridine-3-carboxamide, 7-((4-fluorophenyl)methyl)-1,2-dihydro-4-hydroxy-n-(2-hydroxyethyl)-1-methyl-2-oxo-
SXN0KXT60S ,
s/gsk 364735
s/gsk-364735
863434-13-3
unii-sxn0kxt60s
DB13119
Q27289447

Research Excerpts

Overview

GSK364735 is a human immunodeficiency virus (HIV) integrase strand transfer inhibitor with potent in vitro antiviral activity.

ExcerptReferenceRelevance
"GSK364735 is a human immunodeficiency virus (HIV) integrase strand transfer inhibitor with potent in vitro antiviral activity. "( Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
Borland, J; Lin, J; Min, SS; Palleja, S; Reddy, YS; Song, I; Symonds, WT, 2007)		2.07

Toxicity

ExcerptReferenceRelevance
" GSK364735 was safe and well tolerated after single- and repeated-dose administration."( Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
Borland, J; Lin, J; Min, SS; Palleja, S; Reddy, YS; Song, I; Symonds, WT, 2007)		1.54
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Integrase Human immunodeficiency virus 1IC50 (µMol)0.00760.00051.544310.0000AID1179454; AID1300822; AID519018; AID519038; AID722192
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Integrase Human immunodeficiency virus 1Kd0.02600.00331.00983.0000AID519015
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (171)

Assay IDTitleYearJournalArticle
AID424121Cmax in human at 200 mg administered with fat meal every 12 hrs for 8 days measured on day 12007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424279Plasma concentration in human at 100 mg administered with fat meal every 12 hrs for 8 days measured on day 1 after 12 hrs of first dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID519017Antiviral activity against Human immunodeficiency virus 1 Ba-L infected in human PBMCs assessed as inhibition of viral replication2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
AID424080Toxicity in human assessed as changes in hematology at 50 to 400 mg after sequential repeated administration for 8 days2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424295Cmax in human at 200 mg administered with fat meal every 12 hrs for 8 days measured on day 82007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424123Cmax in human at 200 mg administered with fat meal every 8 hrs for 8 days measured on day 12007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424124Tmax in human at 50 mg administered with fat meal every 12 hrs for 8 days measured on day 12007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID722189Therapeutic index, ratio of cytotoxicity against human MT4 cells to antiviral activity against HIV2013Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2
Naphthyridinone (NTD) integrase inhibitors: N1 protio and methyl combination substituent effects with C3 amide groups.
AID424314Apparent oral clearance in human at 100 mg administered with fat meal every 12 hrs for 8 days measured on day 82007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424118AUC (0 to infinity) in human at 200 mg administered with fat meal every 8 hrs for 8 days measured on day 12007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424283Apparent oral clearance in human at 50 mg administered with fat meal every 12 hrs for 8 days measured on day 12007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424061Toxicity in human assessed as changes in hematology at 50 to 200 mg administered as single dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424287Apparent oral clearance in human at 200 mg administered with fat meal every 8 hrs for 8 days measured on day 12007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424062Toxicity in human assessed as changes in vital signs at 50 to 200 mg administered as single dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424313Apparent oral clearance in human at 50 mg administered with fat meal every 12 hrs for 8 days measured on day 82007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424065Toxicity in human assessed as adverse effect at 50 mg administered every 12 hrs for 8 days2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424049Clearance in iv dosed monkey assessed as liver blood flow2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424101Tmax in fasted human at 400 mg administered with fat meal as single dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424076Toxicity in human assessed as dizziness at 400 mg daily for 8 days2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424086AUC (0 to infinity) in fasted human at 200 mg administered as single dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID1179454Inhibition of recombinant HIV-1 integrase by strand-transfer assay2014Bioorganic & medicinal chemistry letters, Jul-15, Volume: 24, Issue:14
Naphthyridinone (NTD) integrase inhibitors 4. Investigating N1 acetamide substituent effects with C3 amide groups.
AID519018Displacement of 20 nM [3H]GSK304649 from Human immunodeficiency virus 1 integrase by scintillation proximity assay2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
AID1300822Inhibition of pseudotype HIV1 integrase strand transfer activity assessed as reduction in viral replication in HIV1 infected human CIP4 cells after 2 days by luciferase reporter gene assay2016European journal of medicinal chemistry, Jul-19, Volume: 117The design of 8-hydroxyquinoline tetracyclic lactams as HIV-1 integrase strand transfer inhibitors.
AID424079Toxicity in human assessed as dizziness at 200 mg administered every 8 hrs for 8 days2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424092Cmax in fasted human at 200 mg administered as single dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424081Toxicity in human assessed as changes in vital sign at 50 to 400 mg after sequential repeated administration for 8 days2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424122Cmax in human at 400 mg administered with fat meal daily for 8 days measured on day 12007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424071Toxicity in human assessed as adverse effect at 200 mg administered every 12 hrs for 8 days2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424290AUC (0 to 12 hrs) in human at 200 mg administered with fat meal every 12 hrs for 8 days measured on day 82007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424277Terminal elimination half life in human at 200 mg administered with fat meal every 8 hrs for 8 days measured on day 12007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424117AUC (0 to infinity) in human at 400 mg administered with fat meal daily for 8 days measured on day 12007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID519023Antiviral activity against Human immunodeficiency virus 1 NL432 infected in human MT-4 cells assessed as increase in viral two-LTR circles2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
AID519028Antiviral activity against INI-resistant Human immunodeficiency virus 1 expressing integrase T124A mutant gene infected in human HeLa-CD4 cells after 3 days2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
AID424109Apparent oral clearance in fasted human at 100 mg administered as single dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424114AUC (0 to infinity) in human at 50 mg administered with fat meal every 12 hrs for 8 days measured on day 12007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424280Plasma concentration in human at 200 mg administered with fat meal every 12 hrs for 8 days measured on day 1 after 12 hrs of first dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424296Cmax in human at 400 mg administered with fat meal daily for 8 days measured on day 82007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424098Tmax in fasted human at 200 mg administered as single dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID519030Antiviral activity against INI-resistant Human immunodeficiency virus 1 expressing integrase Q146R mutant gene infected in human HeLa-CD4 cells after 3 days2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
AID424302Tmax in human at 200 mg administered with fat meal every 8 hrs for 8 days measured on day 82007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424318Toxicity in human assessed as increase in LDL cholesterol level at 50 to 400 mg after sequential repeated dose administration for 8 days relative to basal level2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424085AUC (0 to infinity) in fasted human at 100 mg administered as single dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424289AUC (0 to 12 hrs) in human at 100 mg administered with fat meal every 12 hrs for 8 days measured on day 82007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424078Toxicity in human assessed as headache at 200 mg administered every 8 hrs for 8 days2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424305Terminal elimination half life in human at 200 mg administered with fat meal every 12 hrs for 8 days measured on day 82007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424304Terminal elimination half life in human at 100 mg administered with fat meal every 12 hrs for 8 days measured on day 82007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424291AUC (0 to 24 hrs) in human at 400 mg administered with fat meal daily for 8 days measured on day 82007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424126Tmax in human at 200 mg administered with fat meal every 12 hrs for 8 days measured on day 12007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID722185Ratio of plasma concentration in CD rat at 1 mg/kg, iv and 5 mg/kg, po after 24 hrs to IC50 for HIV in presence of 40 mg/mL of purified human serum albumin2013Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2
Naphthyridinone (NTD) integrase inhibitors: N1 protio and methyl combination substituent effects with C3 amide groups.
AID424077Toxicity in human assessed as adverse effect at 200 mg administered every 8 hrs for 8 days2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424104Terminal elimination half life in fasted human at 200 mg administered as single dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID519039Antiviral activity against vesicular stomatitis virus G-pseudotyped Human immunodeficiency virus infected in human MT-4 cells assessed as inhibition of viral replication in presence of 40 mg/ml HSA2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
AID424301Tmax in human at 400 mg administered with fat meal daily for 8 days measured on day 82007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424057Toxicity in human assessed as adverse effect at 50 to 200 mg administered as single dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424293Cmax in human at 50 mg administered with fat meal every 12 hrs for 8 days measured on day 82007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID1179455Antiviral activity against pseudotyped HIV by luciferase reporter gene assay2014Bioorganic & medicinal chemistry letters, Jul-15, Volume: 24, Issue:14
Naphthyridinone (NTD) integrase inhibitors 4. Investigating N1 acetamide substituent effects with C3 amide groups.
AID519041Antiviral activity against vesicular stomatitis virus G-pseudotyped Human immunodeficiency virus infected in human MT-4 cells assessed as inhibition of viral replication2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
AID424113Apparent oral clearance in human at 400 mg administered with fat meal as single dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424294Cmax in human at 100 mg administered with fat meal every 12 hrs for 8 days measured on day 82007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID519027Antiviral activity against INI-resistant Human immunodeficiency virus 1 expressing integrase E92Q mutant gene infected in human HeLa-CD4 cells after 3 days2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
AID424292AUC (0 to 8 hrs) in human at 200 mg administered with fat meal every 8 hrs for 8 days measured on day 82007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID722186Half life in CD rat at 1 mg/kg, iv and 5 mg/kg, po2013Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2
Naphthyridinone (NTD) integrase inhibitors: N1 protio and methyl combination substituent effects with C3 amide groups.
AID424127Tmax in human at 400 mg administered with fat meal daily for 8 days measured on day 12007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424069Toxicity in human assessed as headache at 100 mg administered every 12 hrs for 8 days2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424088AUC (0 to infinity) in human at 200 mg administered with fat meal as single dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424120Cmax in human at 100 mg administered with fat meal every 12 hrs for 8 days measured on day 12007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424315Apparent oral clearance in human at 200 mg administered with fat meal every 12 hrs for 8 days measured on day 82007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID519025Antiviral activity against PI-resistant Human immunodeficiency virus 12008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
AID424046Antiviral activity against HIV1 BaL in peripheral blood lymphocytes in presence of 100% human serum2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID519037Antiviral activity against INI-resistant Human immunodeficiency virus 1 expressing integrase N155S mutant gene infected in human HeLa-CD4 cells after 3 days2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
AID424119Cmax in human at 50 mg administered with fat meal every 12 hrs for 8 days measured on day 12007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424129Terminal elimination half life in human at 50 mg administered with fat meal every 12 hrs for 8 days measured on day 12007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424055Oral bioavailability in monkey2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424075Toxicity in human assessed as headache at 400 mg daily for 8 days2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424059Toxicity in human assessed as diarrhea at 50 to 200 mg administered as single dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424093Cmax in fasted human at 400 mg administered as single dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424052Terminal elimination half life in iv dosed monkey2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424300Tmax in human at 200 mg administered with fat meal every 12 hrs for 8 days measured on day 82007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424056Protein binding in human plasma by equilibrium dialysis assay2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID519020Antiviral activity against Human immunodeficiency virus 1 Ba-L infected in human PBMCs assessed as inhibition of viral replication in presence of human serum2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
AID424286Apparent oral clearance in human at 400 mg administered with fat meal daily for 8 days measured on day 12007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424115AUC (0 to infinity) in human at 100 mg administered with fat meal every 12 hrs for 8 days measured on day 12007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424130Terminal elimination half life in human at 100 mg administered with fat meal every 12 hrs for 8 days measured on day 12007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424066Toxicity in human assessed as headache at 50 mg administered every 12 hrs for 8 days2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424045Antiviral activity against HIV1 BaL in peripheral blood lymphocytes2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424310Cmin in human at 200 mg administered with fat meal every 12 hrs for 8 days measured on day 82007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424090Cmax in fasted human at 50 mg administered as single dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424316Apparent oral clearance in human at 400 mg administered with fat meal daily for 8 days measured on day 82007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424102Terminal elimination half life in fasted human at 50 mg administered as single dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424111Apparent oral clearance in fasted human at 400 mg administered as single dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424070Toxicity in human assessed as dizziness at 100 mg administered every 12 hrs for 8 days2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424068Toxicity in human assessed as adverse effect at 100 mg administered every 12 hrs for 8 days2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424063Toxicity in human assessed as changes in 12-lead ECG at 50 to 200 mg administered as single dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424050Terminal elimination half life in iv dosed rat2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424108Apparent oral clearance in fasted human at 50 mg administered as single dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID519035Antiviral activity against INI-resistant Human immunodeficiency virus 1 expressing integrase Q148K mutant gene infected in human HeLa-CD4 cells after 3 days2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
AID424082Toxicity in human assessed as changes in 12-lead ECG at 50 to 400 mg after sequential repeated administration for 8 days2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID519034Antiviral activity against INI-resistant Human immunodeficiency virus 1 expressing integrase F121Y mutant gene infected in human HeLa-CD4 cells after 3 days2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
AID424060Toxicity in human assessed as flatulence at 50 to 200 mg administered as single dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID519015Displacement of [3H]GSK304649 from Human immunodeficiency virus 1 integrase by scintillation proximity assay2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
AID424087AUC (0 to infinity) in fasted human at 400 mg administered as single dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID519024Antiviral activity against RTI-resistant Human immunodeficiency virus 12008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
AID424285Apparent oral clearance in human at 200 mg administered with fat meal every 12 hrs for 8 days measured on day 12007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID519021Antiviral activity against Human immunodeficiency virus 1 NL432 infected in human MT-4 cells assessed as effect on total viral DNA2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
AID424311Cmin in human at 400 mg administered with fat meal daily for 8 days measured on day 82007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424306Terminal elimination half life in human at 400 mg administered with fat meal daily for 8 days measured on day 82007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID519022Antiviral activity against Human immunodeficiency virus 1 NL432 infected in human MT-4 cells assessed as decrease in the integrated viral DNA2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
AID424128Tmax in human at 200 mg administered with fat meal every 8 hrs for 8 days measured on day 12007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424312Cmin in human at 200 mg administered with fat meal every 8 hrs for 8 days measured on day 82007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424058Toxicity in human assessed as headache at 50 to 200 mg administered as single dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424112Apparent oral clearance in human at 200 mg administered with fat meal as single dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424089AUC (0 to infinity) in human at 400 mg administered with fat meal as single dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424284Apparent oral clearance in human at 100 mg administered with fat meal every 12 hrs for 8 days measured on day 12007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424298Tmax in human at 50 mg administered with fat meal every 12 hrs for 8 days measured on day 82007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424131Terminal elimination half life in human at 200 mg administered with fat meal every 12 hrs for 8 days measured on day 12007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424100Tmax in fasted human at 200 mg administered with fat meal as single dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424106Terminal elimination half life in human at 200 mg administered with fat meal as single dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID722187AUC in CD rat at 5 mg/kg, po2013Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2
Naphthyridinone (NTD) integrase inhibitors: N1 protio and methyl combination substituent effects with C3 amide groups.
AID424105Terminal elimination half life in fasted human at 400 mg administered as single dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID722190Antiviral activity against HIV infected in human MT4 cells2013Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2
Naphthyridinone (NTD) integrase inhibitors: N1 protio and methyl combination substituent effects with C3 amide groups.
AID424099Tmax in fasted human at 400 mg administered as single dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424048Clearance in iv dosed dog assessed as liver blood flow2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424317Apparent oral clearance in human at 200 mg administered with fat meal every 8 hrs for 8 days measured on day 82007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424097Tmax in fasted human at 100 mg administered as single dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424067Toxicity in human assessed as dizziness at 50 mg administered every 12 hrs for 8 days2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424047Clearance in iv dosed rat assessed as liver blood flow2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424308Cmin in human at 50 mg administered with fat meal every 12 hrs for 8 days measured on day 82007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID1179456Antiviral activity against pseudotyped HIV by luciferase reporter gene assay in presence of human serum albumin2014Bioorganic & medicinal chemistry letters, Jul-15, Volume: 24, Issue:14
Naphthyridinone (NTD) integrase inhibitors 4. Investigating N1 acetamide substituent effects with C3 amide groups.
AID424095Cmax in human at 400 mg administered with fat meal as single dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424116AUC (0 to infinity) in human at 200 mg administered with fat meal every 12 hrs for 8 days measured on day 12007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID519026Antiviral activity against INI-resistant Human immunodeficiency virus 1 expressing integrase T66I mutant gene infected in human HeLa-CD4 cells after 3 days2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
AID424094Cmax in human at 200 mg administered with fat meal as single dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID722193Antiviral activity against HIV2013Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2
Naphthyridinone (NTD) integrase inhibitors: N1 protio and methyl combination substituent effects with C3 amide groups.
AID519019Selectivity index, ratio of EC50 for Human immunodeficiency virus 1 3B infected in human MT-4 cells assessed as inhibition of viral replication to IC50 for human MT-4 cells2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
AID519033Antiviral activity against INI-resistant Human immunodeficiency virus 1 expressing integrase T66K mutant gene infected in human HeLa-CD4 cells after 3 days2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
AID424073Toxicity in human assessed as dizziness at 200 mg administered every 12 hrs for 8 days2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424072Toxicity in human assessed as headache at 200 mg administered every 12 hrs for 8 days2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424083Toxicity in human assessed as changes in continuous telemetry monitoring at 50 to 400 mg after sequential repeated administration for 8 days2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424053Oral bioavailability rat2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID519038Inhibition of Human immunodeficiency virus 1 integrase by strand transfer scintillation proximity assay2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
AID424299Tmax in human at 100 mg administered with fat meal every 12 hrs for 8 days measured on day 82007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424297Cmax in human at 200 mg administered with fat meal every 8 hrs for 8 days measured on day 82007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424303Terminal elimination half life in human at 50 mg administered with fat meal every 12 hrs for 8 days measured on day 82007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424288AUC (0 to 12 hrs) in human at 50 mg administered with fat meal every 12 hrs for 8 days measured on day 82007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424091Cmax in fasted human at 100 mg administered as single dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424084AUC (0 to infinity) in fasted human at 50 mg administered as single dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID722192Inhibition of HIV1 integrase strand transfer activity2013Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2
Naphthyridinone (NTD) integrase inhibitors: N1 protio and methyl combination substituent effects with C3 amide groups.
AID722188Plasma clearance in CD rat at 1 mg/kg, iv and 5 mg/kg, po2013Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2
Naphthyridinone (NTD) integrase inhibitors: N1 protio and methyl combination substituent effects with C3 amide groups.
AID424307Terminal elimination half life in human at 200 mg administered with fat meal every 8 hrs for 8 days measured on day 82007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424276Terminal elimination half life in human at 400 mg administered with fat meal daily for 8 days measured on day 12007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID519040Antiviral activity against vesicular stomatitis virus G-pseudotyped Human immunodeficiency virus infected in human MT-4 cells assessed as inhibition of viral replication in presence of 2 mg/ml AAG2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
AID424064Toxicity in human assessed as changes in continuous telemetry monitoring at 50 to 200 mg administered as single dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID519029Antiviral activity against INI-resistant Human immunodeficiency virus 1 expressing integrase P145S mutant gene infected in human HeLa-CD4 cells after 3 days2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
AID424125Tmax in human at 100 mg administered with fat meal every 12 hrs for 8 days measured on day 12007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID519032Antiviral activity against INI-resistant Human immunodeficiency virus 1 expressing integrase M154I mutant gene infected in human HeLa-CD4 cells after 3 days2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
AID519036Antiviral activity against INI-resistant Human immunodeficiency virus 1 expressing integrase Q148R mutant gene infected in human HeLa-CD4 cells after 3 days2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
AID424051Terminal elimination half life in iv dosed dog2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID519016Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT-4 cells assessed as inhibition of viral replication2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
AID424278Plasma concentration in human at 50 mg administered with fat meal every 12 hrs for 8 days measured on day 1 after 12 hrs of first dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID722191Antiviral activity against HIV in presence of 40 mg/mL of purified human serum albumin2013Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2
Naphthyridinone (NTD) integrase inhibitors: N1 protio and methyl combination substituent effects with C3 amide groups.
AID424309Cmin in human at 100 mg administered with fat meal every 12 hrs for 8 days measured on day 82007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424096Tmax in fasted human at 50 mg administered as single dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424107Terminal elimination half life in human at 400 mg administered with fat meal as single dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID1300825Inhibition of pseudotype HIV1 integrase Q148K mutant strand transfer activity in HIV1 infected human CIP4 cells assessed as ratio of IC50 for pseudotype HIV1 integrase Q148K mutant strand transfer activity to IC50 for pseudotype HIV1 integrase strand tran2016European journal of medicinal chemistry, Jul-19, Volume: 117The design of 8-hydroxyquinoline tetracyclic lactams as HIV-1 integrase strand transfer inhibitors.
AID424054Oral bioavailability in dog2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424103Terminal elimination half life in fasted human at 100 mg administered as single dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424110Apparent oral clearance in fasted human at 200 mg administered as single dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424281Plasma concentration in human at 400 mg administered with fat meal every 12 hrs for 8 days measured on day 1 after 12 hrs of first dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID519031Antiviral activity against INI-resistant Human immunodeficiency virus 1 expressing integrase S153Y mutant gene infected in human HeLa-CD4 cells after 3 days2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
AID424074Toxicity in human assessed as adverse effect at 400 mg daily for 8 days2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
AID424282Plasma concentration in human at 200 mg administered with fat meal every 8 hrs for 8 days measured on day 1 after 12 hrs of first dose2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's2 (40.00)29.6817
2010's3 (60.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.68

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

MetricThis Compound (vs All)
Research Demand Index12.68 (24.57)
Research Supply Index1.95 (2.92)
Research Growth Index4.63 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.68)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (20.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other4 (80.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
efavirenz
efavirenz: HIV-1 reverse transcriptase inhibitor. efavirenz : 1,4-Dihydro-2H-3,1-benzoxazin-2-one substituted at the 4 position by cyclopropylethynyl and trifluoromethyl groups (S configuration) and at the 6 position by chlorine. A non-nucleoside reverse transcriptase inhibitor with activity against HIV, it is used with other antiretrovirals for combination therapy of HIV infection.		2.0410acetylenic compound;
benzoxazine;
cyclopropanes;
organochlorine compound;
organofluorine compound		antiviral drug;
HIV-1 reverse transcriptase inhibitor
5-(1,1-dioxido-1,2-thiazinan-2-yl)-n-(4-fluorobenzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamide
5-(1,1-dioxido-1,2-thiazinan-2-yl)-N-(4-fluorobenzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamide: structure in first source		2.0410
jtk-303
[no description available]		2.0410aromatic ether;
monochlorobenzenes;
organofluorine compound;
quinolinemonocarboxylic acid;
quinolone		HIV-1 integrase inhibitor
raltegravir
[no description available]		2.04101,2,4-oxadiazole;
dicarboxylic acid amide;
hydroxypyrimidine;
monofluorobenzenes;
pyrimidone;
secondary carboxamide		antiviral drug;
HIV-1 integrase inhibitor
ConditionIndicatedRelationship StrengthStudiesTrials
Dizzyness
[description not available]		03.4211
Bilateral Headache
[description not available]		03.4211
Dizziness
An imprecise term which may refer to a sense of spatial disorientation, motion of the environment, or lightheadedness.		03.4211
Headache
The symptom of PAIN in the cranial region. It may be an isolated benign occurrence or manifestation of a wide variety of HEADACHE DISORDERS.		03.4211