Page last updated: 2024-08-03 19:39:55

dolutegravir

Description

dolutegravir : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of (4R,12aS)-7-hydroxy-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazine-9-carboxylic acid with the amino group of 2,4-difluorobenzylamine. Used (as its sodium salt) for treatment of HIV-1. [CHeBI]

Cross-References

ID SourceID
PubMed CID54726191
CHEMBL ID1229211
SCHEMBL ID82071
CHEBI ID76010
MeSH IDM0562621

Synonyms (77)

Synonym
HY-13238
dolutegravir ,
chebi:76010 ,
s-349572
bdbm50062551
gsk1349572
gsk-1349572
s/gsk-1349572
1051375-16-6
dolutegravir (usan)
D10066
BCP9000620
S/GSK1349572 ,
dolutegravir [usan:inn]
s-gsk1349572
hsdb 8152
dko1w9h7m1 ,
2h-pyrido(1',2':4,5)pyrazino(2,1-b)(1,3)oxazine-9-carboxamide, n-((2,4-difluorophenyl)methyl)-3,4,6,8,12,12a-hexahydro-7-hydroxy-4-methyl-6,8-dioxo-, (4r,12as)-
gsk 1349572
unii-dko1w9h7m1
CHEMBL1229211
(4r,12as)-n-(2,4-difluorobenzyl)-7-hydroxy-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2h-pyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazine-9-carboxamide
(3s,7r)-n-[(2,4-difluorophenyl)methyl]-11-hydroxy-7-methyl-9,12-dioxo-4-oxa-1,8-diazatricyclo[8.4.0.0^{3,8}]tetradeca-10,13-diene-13-carboxamide
s/gsk1349572,gsk1349572
NCGC00346629-01
(4r,12as)-n-[(2,4-difluorophenyl)methyl]-7-hydroxy-4-methyl-6,8-dioxo-3,4,12,12a-tetrahydro-2h-pyrido[[?]:[?]]pyrazino[[?]][1,3]oxazine-9-carboxamide
CS-0454
dolutegravir [mi]
dolutegravir [inn]
dolutegravir [vandf]
(4r,12.alpha.s)-n-((2,4-difluorophenyl)methyl)-7-hydroxy-4-methyl-6,8-dioxo-3,4,6,8,12,12.alpha.-hexahydro-2h-pyrido(1',2':4,5)pyrazino(2,1-.beta.)(1,3)oxazine-9-carboxamide
dolutegravir [usan]
dolutegravir [who-dd]
S2667
(4r,12as)-n-[(2,4-difluorophenyl)methyl]-3,4,6,8,12,12a-hexahydro-7-hydroxy-4-methyl-6,8-dioxo-2h-pyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazine-9-carboxamide
(4r,12as)-n-[(2,4-difluorophenyl)methyl]-7-hydroxy-4-methyl-6,8-dioxo-3,4,12,12a-tetrahydro-2h-pyrido[5,6]pyrazino[2,6-b][1,3]oxazine-9-carboxamide
gtpl7365
DB08930
SCHEMBL82071
smr004702915
MLS006011137
3S3M
3S3N
3S3O
(4r,12as)-n-[(2,4-difluorophenyl)methyl]-3,4,6,8,12,12a-hexahydro-7-hydroxy-4-methyl-6,8-dioxo-2h-pyrido[1',2':4,5]pyrazino[2,1-b][1 ,3]oxazine-9-carboxamide
J-501471
dolutegravir (gsk1349572)
AC-28371
(4r,12as)-n-(2,4-difluorobenzyl)-7-hydroxy-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2h-[1,3]oxazino[3,2-a]pyrido[1,2-d]pyrazine-9-carboxamide
AKOS025396657
(3s,7r)-n-[(2,4-difluorophenyl)methyl]-11-hydroxy-7-methyl-9,12-dioxo-4-oxa-1,8-diazatricyclo[8.4.0.03,8]tetradeca-10,13-diene-13-carboxamide
mfcd20488027
RHWKPHLQXYSBKR-BMIGLBTASA-N
1051375-16-6 (free)
EX-A1695
(4r,12as)-n-(2,4-difluorobenzyl)-7-hydroxy-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2h-[1,3]oxazino[3,2-d]pyrido[1,2-a]pyrazine-9-carboxamide
soltegravir
(3s,7r)-n-[(2,4-difluorophenyl)methyl]-11-hydroxy-7-methyl-9,12-dioxo-4-oxa-1,8-diazatricyclo[8.4.0.0(3),?]tetradeca-10,13-diene-13-carboxamide
AS-75277
Q937224
CCG-268876
NCGC00346629-02
DTXSID90909356
A854801
dolutegravir dtg
(4r,12as)-n-((2,4-difluorophenyl)methyl)-3,4,6,8,12,12a-hexahydro-7-hydroxy-4-methyl-6,8-dioxo-2h-pyrido(1',2':4,5)pyrazino(2,1-b)(1,3)oxazine-9-carboxamide
dolutegravirum
(4r,12as)-n-
(4r,9as)-5-hydroxy-4-methyl-6,10-dioxo-3,4,6,9,9a,10-hexahydro-2h-1-oxa-4a,8a-diazaanthracene-7-carboxylic acid 2,4-difluorobenzylamide
(4r,9as)-5-hydroxy-4-methyl-6,10-dioxo-3,4,6,9,9a,10-hexahydro-2h-1-oxa-4a,8a-diaza-anthracene-7-carboxylic acid-2,4 difluorobenzylamide
(4r,12as)-n-(2,4-difluorobenzyl)-7-hydroxy-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2h-pyrido(1',2':4,5)pyrazino(2,1-b)(1,3)oxazine-9-carboxamide
j05ax12
(4r,12alphas)-n-((2,4-difluorophenyl)methyl)-7-hydroxy-4-methyl-6,8-dioxo-3,4,6,8,12,12alpha-hexahydro-2h-pyrido(1',2':4,5)pyrazino(2,1-beta)(1,3)oxazine-9-carboxamide
2h-pyrido(1',2':4,5)pyrazino(2,1-b)(1,3)oxazine-9-carboxamide, n-((2,4-difluorophenyl)methyl)-3,4,6,8,12,12a-hexahydro-7-hydroxy-4-methyl-6,8-dioxo-, (4r,12as)
Z2235801952
EN300-7409916
(3s,7r)-n-[(2,4-difluorophenyl)methyl]-11-hydroxy-7-methyl-9,12-dioxo-4-oxa-1,8-diazatricyclo[8.4.0.0,3,8]tetradeca-10,13-diene-13-carboxamide

Roles (1)

RoleDescription
HIV-1 integrase inhibitorAn inhibitor of HIV-1 integrase, an enzyme required for the integration of the genetic material of the retrovirus into the DNA of the infected cells.

Drug Classes (4)

ClassDescription
monocarboxylic acid amideA carboxamide derived from a monocarboxylic acid.
organic heterotricyclic compoundAn organic tricyclic compound in which at least one of the rings of the tricyclic skeleton contains one or more heteroatoms.
secondary carboxamideA carboxamide resulting from the formal condensation of a carboxylic acid with a primary amine; formula RC(=O)NHR(1).
difluorobenzeneAny member of the class of fluorobenzenes containing a mono- or poly-substituted benzene ring carrying two fluorine atoms.

Protein Targets (28)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Fumarate hydrataseHomo sapiens (human)Potency37.2212AID1347053
EWS/FLI fusion proteinHomo sapiens (human)Potency19.0694AID1259252; AID1259253; AID1259255; AID1259256
polyproteinZika virusPotency37.2212AID1347053
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency0.0096AID1479148

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Chain A, PFV integraseHuman spumaretrovirusIC500.0517AID977608
Chain A, PFV integraseHuman spumaretrovirusIC500.0517AID977608
Chain A, PFV integraseHuman spumaretrovirusIC500.0517AID977608
Solute carrier family 22 member 2Homo sapiens (human)IC501.9000AID1211974
Cytochrome P450 1A2Homo sapiens (human)IC5090.0000AID1212007
ATP-dependent translocase ABCB1Homo sapiens (human)IC5095.0000AID1211968; AID1212007
Cytochrome P450 3A4Homo sapiens (human)IC5067.0000AID1212009
Cytochrome P450 2C8Homo sapiens (human)IC5090.0000AID1212007
Cytochrome P450 2D6Homo sapiens (human)IC5090.0000AID1212007; AID1212008
Cytochrome P450 2A6Homo sapiens (human)IC50100.0000AID1211999
Cytochrome P450 2C9 Homo sapiens (human)IC5090.0000AID1212008
UDP-glucuronosyltransferase 1A1 Homo sapiens (human)IC50100.0000AID1211999
Cytochrome P450 2C19Homo sapiens (human)IC5067.0000AID1212009
Sigma intracellular receptor 2Homo sapiens (human)Ki0.0180AID1655661
Sigma intracellular receptor 2Rattus norvegicus (Norway rat)Ki0.0238AID1824523; AID1877931
Sigma non-opioid intracellular receptor 1Cavia porcellus (domestic guinea pig)Ki0.0975AID1191388; AID1877932
Vesicular acetylcholine transporterRattus norvegicus (Norway rat)Ki4.5230AID1506088
Reverse transcriptase/RNaseH Human immunodeficiency virus 1IC5010.0000AID1406290; AID1602241; AID1635810
Integrase Human immunodeficiency virus 1IC500.0414AID1406292; AID1588917; AID1602243; AID1635801; AID759973
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC5095.0000AID1211970; AID1212008
Solute carrier organic anion transporter family member 1B3Homo sapiens (human)IC50100.0000AID1211972
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)IC5048.5000AID1211969; AID1212009
Solute carrier organic anion transporter family member 1B1Homo sapiens (human)IC50100.0000AID1211971

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Integrase Human immunodeficiency virus 2EC500.0023AID1603996
Integrase Human immunodeficiency virus 1EC500.0034AID1604009; AID1604010; AID1604011; AID1604012

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
UDP-glucuronosyltransferase 1A1 Homo sapiens (human)Km21.0000AID1211925

Bioassays (235)

Assay IDTitleYearJournalArticle
AID1211972Inhibition of human OATP1B3 expressed in BacMam baculovirus virus infected HEK MSR2 cells using [3H]estradiol 17beta-D-glucuronide as substrate by liquid scintillation counting analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1604000Inhibition of HIV-2 ROD9 integrase Y143C mutant2019European journal of medicinal chemistry, Nov-01, Volume: 181ISSN: 1768-3254Synthetic routes and structure-activity relationships (SAR) of anti-HIV agents: A key review.
AID1073335Antiviral activity against HIV-1 harboring integrase T97A mutant relative to wild type HIV12014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
ISSN: 1520-4804
Inhibiting the HIV integration process: past, present, and the future.
AID1073332Antiviral activity against HIV-1 harboring integrase G140S mutant relative to wild type HIV12014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
ISSN: 1520-4804
Inhibiting the HIV integration process: past, present, and the future.
AID1073324Antiviral activity against HIV-1 harboring integrase T66I/R263K double mutant relative to wild type HIV12014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
ISSN: 1520-4804
Inhibiting the HIV integration process: past, present, and the future.
AID1211953Activity at human BCRP expressed in MDCK2 cells assessed as apical efflux ratio by liquid scintillation counting analysis in presence of 3 uM P-gp and BCRP inhibitor GF1209182013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1604008Inhibition of HIV-2 ROD9 integrase T97A/N155H double mutant2019European journal of medicinal chemistry, Nov-01, Volume: 181ISSN: 1768-3254Synthetic routes and structure-activity relationships (SAR) of anti-HIV agents: A key review.
AID1300996Selectivity ratio of EC50 for raltegravir resistant HIV1 harboring integrase Q148H mutant infected in human MT4 cells to EC50 for wild type HIV1 3B infected in human MT4 cells2016European journal of medicinal chemistry, Jul-19, Volume: 117ISSN: 1768-32542-hydroxyisoquinoline-1,3(2H,4H)-diones (HIDs) as human immunodeficiency virus type 1 integrase inhibitors: Influence of the alkylcarboxamide substitution of position 4.
AID1635806Fold resistance, ratio of EC50 for raltegravir-resistant HIV1 1556-1 expressing integrase Y143C mutant to EC50 for HIV1 expressing wild-type integrase2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
ISSN: 1520-4804
3-Hydroxypyrimidine-2,4-dione-5-N-benzylcarboxamides Potently Inhibit HIV-1 Integrase and RNase H.
AID1211951Activity at human MDR1 expressed in MDCK2 cells assessed as apical efflux ratio at 3 uM by liquid scintillation counting analysis in presence of 3 uM P-gp and BCRP inhibitor GF1209182013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1212014Inhibition of CYP3A4 in human liver microsomes using atorvastatin as substrate preincubated for 20 mins with substrate prior to initiation of reaction with NADPH by HPLC analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211950Activity at human MDR1 expressed in MDCK2 cells assessed as apical efflux ratio at 3 uM by liquid scintillation counting analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1073318Antiviral activity against HIV-1 harboring integrase T97A/Y143C double mutant relative to wild type HIV12014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
ISSN: 1520-4804
Inhibiting the HIV integration process: past, present, and the future.
AID1191388Displacement of (+)-[3H]pentazocine from guinea pig brain cortex sigma1 receptor by scintillation analyzer2015European journal of medicinal chemistry, Jan-27, Volume: 90ISSN: 1768-3254Improving selectivity preserving affinity: new piperidine-4-carboxamide derivatives as effective sigma-1-ligands.
AID1073337Antiviral activity against HIV-1 harboring integrase T66R mutant relative to wild type HIV12014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
ISSN: 1520-4804
Inhibiting the HIV integration process: past, present, and the future.
AID1211964In vitro passive membrane permeability across dog MDCK2 cells at 3 uM using fasted state-simulated intestinal fluid buffer at pH 7.4 on donor side and 1% human serum albumin at pH 7.4 on receiver side by liquid scintillation counting analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1635807Fold resistance, ratio of EC50 for raltegravir-resistant HIV1 4736-2 expressing integrase N155H mutant to EC50 for HIV1 expressing wild-type integrase2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
ISSN: 1520-4804
3-Hydroxypyrimidine-2,4-dione-5-N-benzylcarboxamides Potently Inhibit HIV-1 Integrase and RNase H.
AID1211946Drug metabolism assessed as UDPGA-fortified human recombinant UGT1A4-mediated DTG glucuronide metabolite ((2S,3S,4S,5R,6S)-6-((4R,12aS)-9-(2,4-difluorobenzylcarbamoyl)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-[1,3]oxazino[3,2-d]pyrido[1,2-a]pyrazin-2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211936Drug metabolism in supersomes expressing human recombinant CYP2B6 assessed as NADPH-fortified enzyme-mediated metabolite formation at 5 uM after 120 mins by radio HPLC analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211981Ratio of peak plasma concentration in human at 50 mg administered as daily dose to IC50 for human OCT22013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1212006Drug excretion in human feces at 20 mg, po2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211949Drug metabolism assessed as UDPGA-fortified human recombinant UGT2B7-mediated DTG glucuronide metabolite ((2S,3S,4S,5R,6S)-6-((4R,12aS)-9-(2,4-difluorobenzylcarbamoyl)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-[1,3]oxazino[3,2-d]pyrido[1,2-a]pyrazin-2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1073334Antiviral activity against HIV-1 harboring integrase G118R mutant relative to wild type HIV12014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
ISSN: 1520-4804
Inhibiting the HIV integration process: past, present, and the future.
AID1211916Drug metabolism assessed as UDPGA-fortified human recombinant UGT2B15-mediated DTG glucuronide metabolite ((2S,3S,4S,5R,6S)-6-((4R,12aS)-9-(2,4-difluorobenzylcarbamoyl)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-[1,3]oxazino[3,2-d]pyrido[1,2-a]pyrazin2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211956Activity at human BCRP expressed in MDCK2 cells assessed as apical to basolateral mass balance at 3 uM by liquid scintillation counting analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211944Inhibition of CYP2C8 in human liver microsomes using rosiglitazone as substrate preincubated for 20 mins with substrate prior to initiation of reaction with NADPH by HPLC analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1212010Protein binding in plasma (unknown origin)2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1483418Cytotoxicity against human P4R5 cells by MTS assay2017Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
ISSN: 1520-4804
Double-Winged 3-Hydroxypyrimidine-2,4-diones: Potent and Selective Inhibition against HIV-1 RNase H with Significant Antiviral Activity.
AID1211983Ratio of drug level in human 250 ml gastrointestinal volume at 50 mg administered as daily dose to IC50 for human BCRP2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1073331Antiviral activity against HIV-1 harboring integrase Y143C mutant relative to wild type HIV12014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
ISSN: 1520-4804
Inhibiting the HIV integration process: past, present, and the future.
AID1406292Inhibition of HIV integrase strand transfer activity using 5'-biotin/3'-Cy5-labeled DNA substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by HTS assay2018European journal of medicinal chemistry, Aug-05, Volume: 156ISSN: 1768-32546-Arylthio-3-hydroxypyrimidine-2,4-diones potently inhibited HIV reverse transcriptase-associated RNase H with antiviral activity.
AID1212025Metabolism-dependent inhibition of CYP2C9 in human liver microsomes using diclofenac as substrate preincubated for 20 mins with NADPH prior to initiation of reaction with probe substrate by HPLC analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1073317Antiviral activity against HIV-1 harboring integrase T97A/Y143R double mutant relative to wild type HIV12014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
ISSN: 1520-4804
Inhibiting the HIV integration process: past, present, and the future.
AID1211978Ratio of peak plasma concentration in human at 50 mg administered as daily dose to IC50 for human OATP1B12013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1155173Antiviral activity against HIV-1 harboring wild type integrase infected in human HOS cells pretreated with compound for 3 hrs by single-round HIV-1 infectivity assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
ISSN: 1520-4804
4-amino-1-hydroxy-2-oxo-1,8-naphthyridine-containing compounds having high potency against raltegravir-resistant integrase mutants of HIV-1.
AID759973Inhibition of HIV-1 integrase strand transfer activity using [3H]-DNA as substrate preincubated for 60 mins prior to substrate addition measured after 25 to 45 mins2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
ISSN: 1520-4804
Carbamoyl pyridone HIV-1 integrase inhibitors 3. A diastereomeric approach to chiral nonracemic tricyclic ring systems and the discovery of dolutegravir (S/GSK1349572) and (S/GSK1265744).
AID1212021Metabolism-dependent inhibition of CYP1A2 in human liver microsomes using phenacetin as substrate preincubated for 20 mins with NADPH prior to initiation of reaction with probe substrate by HPLC analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211992Activity at human BCRP expressed in MDCK2 cells assessed as rate of passive membrane permeability from apical to basolateral side at 3 uM by liquid scintillation counting analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211922Drug metabolism in UDPGA-fortified human liver microsomes assessed as UGT1A1-mediated DTG glucuronide M2 ((2S,3S,4S,5R,6S)-6-((4R,12aS)-9-(2,4-difluorobenzylcarbamoyl)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-[1,3]oxazino[3,2-d]pyrido[1,2-a]pyrazin-2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1191391Displacement of [3H]MK801 from pig brain cortex NMDA receptor PCP binding site at 1 uM by scintillation analyzer2015European journal of medicinal chemistry, Jan-27, Volume: 90ISSN: 1768-3254Improving selectivity preserving affinity: new piperidine-4-carboxamide derivatives as effective sigma-1-ligands.
AID1212013Inhibition of CYP2D6 in human liver microsomes using bufuralol as substrate preincubated for 20 mins with substrate prior to initiation of reaction with NADPH by HPLC analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211995Activity at human MDR1 expressed in MDCK2 cells assessed as rate of passive membrane permeability from basolateral to apical side at 3 uM by liquid scintillation counting analysis in presence of 3 uM P-gp and BCRP inhibitor GF1209182013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1270893Inhibition of HIV integrase-mediated strand transfer activity using precleaved 19T duplex oligonucleotide after 2 hrs2015European journal of medicinal chemistry, Dec-01, Volume: 106ISSN: 1768-3254Anti-HIV-1 activity of a tripodal receptor that recognizes mannose oligomers.
AID1211966Inhibition of BCRP (unknown origin) expressed in MDCK2 cells assessed as basolateral to apical transport of [14C]cimetidine at 30 uM after 90 mins by liquid scintillation counting analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1212000Inhibition of human recombinant UGT2B7 expressed in supersomes assessed as 7-HFC glucuronidation up to 100 uM by fluoresence analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211937Drug metabolism in supersomes expressing human recombinant CYP2C8 assessed as NADPH-fortified enzyme-mediated metabolite formation at 5 uM after 120 mins by radio HPLC analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211938Drug metabolism in supersomes expressing human recombinant CYP2C9 assessed as NADPH-fortified enzyme-mediated metabolite formation at 5 uM after 120 mins by radio HPLC analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211968Inhibition of MDR1 (unknown origin) expressed in MDCK2 cells assessed as basolateral to apical transport of [3H]digoxin after 90 mins by liquid scintillation counting analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1603997Inhibition of HIV-2 ROD9 integrase E92Q mutant2019European journal of medicinal chemistry, Nov-01, Volume: 181ISSN: 1768-3254Synthetic routes and structure-activity relationships (SAR) of anti-HIV agents: A key review.
AID1211987Drug metabolism assessed as UDPGA-fortified human recombinant UGT1A3-mediated DTG glucuronide metabolite ((2S,3S,4S,5R,6S)-6-((4R,12aS)-9-(2,4-difluorobenzylcarbamoyl)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-[1,3]oxazino[3,2-d]pyrido[1,2-a]pyrazin-2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211930Drug metabolism in NADPH-fortified human liver microsomes assessed as metabolite M3 ((4R,12aS)-N-((3,5-difluorophenyl)(hydroxy)methyl)-7-hydroxy-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-[1,3]oxazino[3,2-d]pyrido[1,2-a]pyrazine-9-carboxamide) formati2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1603998Inhibition of HIV-2 ROD9 integrase T97A mutant2019European journal of medicinal chemistry, Nov-01, Volume: 181ISSN: 1768-3254Synthetic routes and structure-activity relationships (SAR) of anti-HIV agents: A key review.
AID759977Antiviral activity against Human immunodeficiency virus harboring integrase Q148K mutant infected in human HeLa cells expressing CD4 after 2 days by beta galactosidase assay relative to wild type HIV2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
ISSN: 1520-4804
Carbamoyl pyridone HIV-1 integrase inhibitors 3. A diastereomeric approach to chiral nonracemic tricyclic ring systems and the discovery of dolutegravir (S/GSK1349572) and (S/GSK1265744).
AID759971Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells after 4 to 5 days by bioluminescence assay2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
ISSN: 1520-4804
Carbamoyl pyridone HIV-1 integrase inhibitors 3. A diastereomeric approach to chiral nonracemic tricyclic ring systems and the discovery of dolutegravir (S/GSK1349572) and (S/GSK1265744).
AID1212027Metabolism-dependent inhibition of CYP2D6 in human liver microsomes using bufuralol as substrate preincubated for 20 mins with NADPH prior to initiation of reaction with probe substrate by HPLC analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1603996Inhibition of wild type HIV-2 ROD9 integrase2019European journal of medicinal chemistry, Nov-01, Volume: 181ISSN: 1768-3254Synthetic routes and structure-activity relationships (SAR) of anti-HIV agents: A key review.
AID1211982Ratio of drug level in human 250 ml gastrointestinal volume at 50 mg administered as daily dose to IC50 for human P-gp2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1073328Antiviral activity against HIV-1 harboring integrase Q148K mutant relative to wild type HIV12014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
ISSN: 1520-4804
Inhibiting the HIV integration process: past, present, and the future.
AID1406291Inhibition of HIV1 reverse transcriptase polymerase activity using 18 nucleotide DNA primer and 100 nucleotide DNA template after 30 mins2018European journal of medicinal chemistry, Aug-05, Volume: 156ISSN: 1768-32546-Arylthio-3-hydroxypyrimidine-2,4-diones potently inhibited HIV reverse transcriptase-associated RNase H with antiviral activity.
AID1212017Inhibition of CYP2C9 in human liver microsomes using diclofenac as substrate at 100 uM preincubated for 20 mins with substrate prior to initiation of reaction with NADPH by HPLC analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1212022Metabolism-dependent inhibition of CYP2A6 in human liver microsomes using coumarin as substrate preincubated for 20 mins with NADPH prior to initiation of reaction with probe substrate by HPLC analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1483415Inhibition of HIV integrase strand transfer activity expressed in Escherichia coli BL21 (DE3) using 5' biotin ATGTGGAAAATCTCTAGCA primer annealed with ACTGCTAGAGATTTTCCACAT 3' Cy5 template preincubated for 10 mins followed by primer/template addition meas2017Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
ISSN: 1520-4804
Double-Winged 3-Hydroxypyrimidine-2,4-diones: Potent and Selective Inhibition against HIV-1 RNase H with Significant Antiviral Activity.
AID1212019Inhibition of CYP2D6 in human liver microsomes using bufuralol as substrate at 100 uM preincubated for 20 mins with substrate prior to initiation of reaction with NADPH by HPLC analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211997Activity at human BCRP expressed in MDCK2 cells assessed as rate of passive membrane permeability from basolateral to apical side at 3 uM by liquid scintillation counting analysis in presence of 3 uM P-gp and BCRP inhibitor GF1209182013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID759972Antiviral activity against Human immunodeficiency virus 1 Ba-L infected human PBMC after 7 days by [methyl-3H]dTTP incorporation assay2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
ISSN: 1520-4804
Carbamoyl pyridone HIV-1 integrase inhibitors 3. A diastereomeric approach to chiral nonracemic tricyclic ring systems and the discovery of dolutegravir (S/GSK1349572) and (S/GSK1265744).
AID1211923Drug metabolism in UDPGA-fortified human liver microsomes assessed as UGT1A1-mediated DTG glucuronide M2 ((2S,3S,4S,5R,6S)-6-((4R,12aS)-9-(2,4-difluorobenzylcarbamoyl)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-[1,3]oxazino[3,2-d]pyrido[1,2-a]pyrazin-2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1655661Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor (unknown origin) incubated for 1 hr in presence of (+)SKF10047 by liquid scintillation counting method2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
ISSN: 1948-5875
AID1689343Antiviral activity against HIV1 3B2020European journal of medicinal chemistry, Mar-01, Volume: 189ISSN: 1768-3254Synthesis, biological evaluation and in silico modeling of novel integrase strand transfer inhibitors (INSTIs).
AID1602241Inhibition of HIV1 reverse transcriptase RNase H expressed in Escherichia coli JM109 using RNA/DNA duplex substrate HTS-12019European journal of medicinal chemistry, Mar-15, Volume: 166ISSN: 1768-3254Pharmacophore-based design of novel 3-hydroxypyrimidine-2,4-dione subtypes as inhibitors of HIV reverse transcriptase-associated RNase H: Tolerance of a nonflexible linker.
AID1602243Inhibition of HIV1 integrase strand transfer activity using 5'-biotinylated oligonucleotide as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins2019European journal of medicinal chemistry, Mar-15, Volume: 166ISSN: 1768-3254Pharmacophore-based design of novel 3-hydroxypyrimidine-2,4-dione subtypes as inhibitors of HIV reverse transcriptase-associated RNase H: Tolerance of a nonflexible linker.
AID1604004Inhibition of HIV-2 ROD9 integrase E92Q/Y143C double mutant2019European journal of medicinal chemistry, Nov-01, Volume: 181ISSN: 1768-3254Synthetic routes and structure-activity relationships (SAR) of anti-HIV agents: A key review.
AID1155176Antiviral activity against raltegravir-resistant HIV-1 harboring integrase G140S/Q148H double mutant infected in human HOS cells pretreated with compound for 3 hrs by single-round HIV-1 infectivity assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
ISSN: 1520-4804
4-amino-1-hydroxy-2-oxo-1,8-naphthyridine-containing compounds having high potency against raltegravir-resistant integrase mutants of HIV-1.
AID1604005Inhibition of HIV-2 ROD9 integrase T97A/Y143C double mutant2019European journal of medicinal chemistry, Nov-01, Volume: 181ISSN: 1768-3254Synthetic routes and structure-activity relationships (SAR) of anti-HIV agents: A key review.
AID1211925Drug metabolism assessed as human recombinant UGT1A1-mediated DTG glucuronide M2 ((2S,3S,4S,5R,6S)-6-((4R,12aS)-9-(2,4-difluorobenzylcarbamoyl)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-[1,3]oxazino[3,2-d]pyrido[1,2-a]pyrazin-7-yloxy)-3,4,5-trihydrox2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1073325Antiviral activity against HIV-1 harboring integrase R263K mutant relative to wild type HIV12014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
ISSN: 1520-4804
Inhibiting the HIV integration process: past, present, and the future.
AID1506086Displacement of (+)-[3H]pentazocine from sigma1 receptor in rat brain membranes after 60 mins by liquid scintillation counting method2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
ISSN: 1520-4804
Contilisant, a Tetratarget Small Molecule for Alzheimer's Disease Therapy Combining Cholinesterase, Monoamine Oxidase Inhibition, and H3R Antagonism with S1R Agonism Profile.
AID1073323Antiviral activity against HIV-1 harboring integrase E92Q/N155H double mutant relative to wild type HIV12014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
ISSN: 1520-4804
Inhibiting the HIV integration process: past, present, and the future.
AID1211991Activity at human MDR1 expressed in MDCK2 cells assessed as rate of passive membrane permeability from apical to basolateral side at 3 uM by liquid scintillation counting analysis in presence of 3 uM P-gp and BCRP inhibitor GF1209182013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211958Activity at human MDR1 expressed in MDCK2 cells assessed as basolateral to apical mass balance at 3 uM by liquid scintillation counting analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211961Activity at human BCRP expressed in MDCK2 cells assessed as basolateral to apical mass balance at 3 uM by liquid scintillation counting analysis in presence of 3 uM P-gp and BCRP inhibitor GF1209182013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211954Activity at human MDR1 expressed in MDCK2 cells assessed as apical to basolateral mass balance at 3 uM by liquid scintillation counting analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID759978Antiviral activity against pseudo Human immunodeficiency virus infected in HEK293T cells after 2 days in presence of human serum albumin2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
ISSN: 1520-4804
Carbamoyl pyridone HIV-1 integrase inhibitors 3. A diastereomeric approach to chiral nonracemic tricyclic ring systems and the discovery of dolutegravir (S/GSK1349572) and (S/GSK1265744).
AID1211943Inhibition of CYP2B6 in human liver microsomes using bupropion as substrate preincubated for 20 mins with substrate prior to initiation of reaction with NADPH by HPLC analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211998Inhibition of human recombinant UGT1A1 expressed in supersomes assessed as scopoletin glucuronidation at 100 uM by fluorescence analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211963In vitro passive membrane permeability across dog MDCK2 cells at 3 uM using fasted state-simulated intestinal fluid buffer at pH 5.5 on donor side and 1% human serum albumin at pH 7.4 on receiver side by liquid scintillation counting analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1212020Inhibition of CYP3A4 in human liver microsomes using nifedipine as substrate at 100 uM preincubated for 20 mins with substrate prior to initiation of reaction with NADPH by HPLC analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1212018Inhibition of CYP2C19 in human liver microsomes using S-mephenytoin as substrate at 100 uM preincubated for 20 mins with substrate prior to initiation of reaction with NADPH by HPLC analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1073336Antiviral activity against HIV-1 harboring integrase E92Q mutant relative to wild type HIV12014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
ISSN: 1520-4804
Inhibiting the HIV integration process: past, present, and the future.
AID1406290Inhibition of HIV1 reverse transcriptase RNaseH activity using 3'-fluorescein/5'-Dabcyl labeled HTS-1 substrate2018European journal of medicinal chemistry, Aug-05, Volume: 156ISSN: 1768-32546-Arylthio-3-hydroxypyrimidine-2,4-diones potently inhibited HIV reverse transcriptase-associated RNase H with antiviral activity.
AID1211984Ratio of drug level in human 250 ml gastrointestinal volume at 50 mg administered as daily dose to IC50 for human MRP22013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1073322Antiviral activity against HIV-1 harboring integrase E138K/Q148H double mutant relative to wild type HIV12014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
ISSN: 1520-4804
Inhibiting the HIV integration process: past, present, and the future.
AID1212008Inhibition of human MRP22013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1483417Antiviral activity against HIV1 infected in CD4/CXCR4/CCR5 expressing human P4R5 cells assessed as inhibition of viral replication preincubated with cells for 24 hrs followed by viral infection measured after 48 hrs by beta-galactosidase reporter gene ass2017Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
ISSN: 1520-4804
Double-Winged 3-Hydroxypyrimidine-2,4-diones: Potent and Selective Inhibition against HIV-1 RNase H with Significant Antiviral Activity.
AID1635805Antiviral activity against HIV1 infected in human P4R5 cells assessed as reduction of virus replication preincubated with cells for 24 hrs followed by viral infection for 48 hrs by 4-methylumbelliferylgalactoside-based MAGI assay2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
ISSN: 1520-4804
3-Hydroxypyrimidine-2,4-dione-5-N-benzylcarboxamides Potently Inhibit HIV-1 Integrase and RNase H.
AID1483413Inhibition of recombinant full length HIV1 reverse transcriptase RNase H domain using RNA/DNA duplex substrate HTS1 assessed as reduction in internal cleavage of RNA strand by fluoresence assay2017Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
ISSN: 1520-4804
Double-Winged 3-Hydroxypyrimidine-2,4-diones: Potent and Selective Inhibition against HIV-1 RNase H with Significant Antiviral Activity.
AID1824523Displacement of [3H]DTG from sigma 2 receptor in Wistar Han rat liver membranes measured after 120 mins by scintillation counting method2022European journal of medicinal chemistry, Jan-15, Volume: 228ISSN: 1768-3254Development of novel phenoxyalkylpiperidines as high-affinity Sigma-1 (σ
AID1602244Antiviral activity against HIV-1 infected in human P4R5 cells assessed as reduction in viral replication preincubated for 24 hrs followed by viral infection and measured after 48 hrs by MAGI assay2019European journal of medicinal chemistry, Mar-15, Volume: 166ISSN: 1768-3254Pharmacophore-based design of novel 3-hydroxypyrimidine-2,4-dione subtypes as inhibitors of HIV reverse transcriptase-associated RNase H: Tolerance of a nonflexible linker.
AID1603999Inhibition of HIV-2 ROD9 integrase G140S mutant2019European journal of medicinal chemistry, Nov-01, Volume: 181ISSN: 1768-3254Synthetic routes and structure-activity relationships (SAR) of anti-HIV agents: A key review.
AID1073321Antiviral activity against HIV-1 harboring integrase E138K/Q148K double mutant relative to wild type HIV12014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
ISSN: 1520-4804
Inhibiting the HIV integration process: past, present, and the future.
AID1212026Metabolism-dependent inhibition of CYP2C19 in human liver microsomes using S-mephenytoin as substrate preincubated for 20 mins with NADPH prior to initiation of reaction with probe substrate by HPLC analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1604010Inhibition of HIV-1 NL4-3 integrase T97A/Y143C double mutant2019European journal of medicinal chemistry, Nov-01, Volume: 181ISSN: 1768-3254Synthetic routes and structure-activity relationships (SAR) of anti-HIV agents: A key review.
AID1212009Inhibition of human BCRP2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211917Drug metabolism in human hepatocytes assessed as DTG glucuronide metabolite ((2S,3S,4S,5R,6S)-6-((4R,12aS)-9-(2,4-difluorobenzylcarbamoyl)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-[1,3]oxazino[3,2-d]pyrido[1,2-a]pyrazin-7-yloxy)-3,4,5-trihydroxytetr2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211980Ratio of peak plasma concentration in human at 50 mg administered as daily dose to IC50 for human MRP22013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1300997Selectivity ratio of EC50 for raltegravir resistant HIV1 harboring integrase N155H mutant infected in human MT4 cells to EC50 for wild type HIV1 3B infected in human MT4 cells2016European journal of medicinal chemistry, Jul-19, Volume: 117ISSN: 1768-32542-hydroxyisoquinoline-1,3(2H,4H)-diones (HIDs) as human immunodeficiency virus type 1 integrase inhibitors: Influence of the alkylcarboxamide substitution of position 4.
AID1155175Antiviral activity against raltegravir-resistant HIV-1 harboring integrase N155H mutant infected in human HOS cells pretreated with compound for 3 hrs by single-round HIV-1 infectivity assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
ISSN: 1520-4804
4-amino-1-hydroxy-2-oxo-1,8-naphthyridine-containing compounds having high potency against raltegravir-resistant integrase mutants of HIV-1.
AID1211999Inhibition of human recombinant UGT1A1 expressed in supersomes assessed as scopoletin glucuronidation by fluorescence analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211967Inhibition of BCRP (unknown origin) expressed in MDCK2 cells assessed as basolateral to apical transport of [14C]cimetidine at 100 uM after 90 mins by liquid scintillation counting analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1212024Metabolism-dependent inhibition of CYP2C8 in human liver microsomes using rosiglitazone as substrate preincubated for 20 mins with NADPH prior to initiation of reaction with probe substrate by HPLC analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211952Activity at human BCRP expressed in MDCK2 cells assessed as apical efflux ratio at 3 uM by liquid scintillation counting analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1380353Lipophilicity, log D of the compound at pH 7.4 by chromatographic method2018Journal of medicinal chemistry, 08-09, Volume: 61, Issue:15
ISSN: 1520-4804
Mapping the Efficiency and Physicochemical Trajectories of Successful Optimizations.
AID1211965Inhibition of MDR1 (unknown origin) expressed in MDCK2 cells assessed as basolateral to apical transport of [3H]digoxin at 100 uM after 90 mins by liquid scintillation counting analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1073333Antiviral activity against HIV-1 harboring integrase E138K mutant relative to wild type HIV12014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
ISSN: 1520-4804
Inhibiting the HIV integration process: past, present, and the future.
AID1604003Inhibition of HIV-2 ROD9 integrase N155H mutant2019European journal of medicinal chemistry, Nov-01, Volume: 181ISSN: 1768-3254Synthetic routes and structure-activity relationships (SAR) of anti-HIV agents: A key review.
AID1211969Inhibition of BCRP (unknown origin) expressed in MDCK2 cells assessed as basolateral to apical transport of [14C]cimetidine after 90 mins by liquid scintillation counting analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1212016Inhibition of CYP2B6 in human liver microsomes using bupropion as substrate at 100 uM preincubated for 20 mins with substrate prior to initiation of reaction with NADPH by HPLC analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1635808Fold resistance, ratio of EC50 for raltegravir-resistant HIV1 8070-1 expressing integrase G140S/Y143H/Q148H mutant to EC50 for HIV1 expressing wild-type integrase2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
ISSN: 1520-4804
3-Hydroxypyrimidine-2,4-dione-5-N-benzylcarboxamides Potently Inhibit HIV-1 Integrase and RNase H.
AID1212002Induction of CYP2B6 mRNA expression in human hepatocytes at 1 to 40 uM after 48 hrs by real time PCR analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1635810Inhibition of RNase H activity of full length HIV1 reverse transcriptase using RNA-DNA duplex HTS-1 substrate2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
ISSN: 1520-4804
3-Hydroxypyrimidine-2,4-dione-5-N-benzylcarboxamides Potently Inhibit HIV-1 Integrase and RNase H.
AID1191390Selectivity ratio of Ki for rat liver sigma2 receptor to Ki for guinea pig brain cortex sigma1 receptor2015European journal of medicinal chemistry, Jan-27, Volume: 90ISSN: 1768-3254Improving selectivity preserving affinity: new piperidine-4-carboxamide derivatives as effective sigma-1-ligands.
AID1211929Drug metabolism in supersomes expressing human recombinant CYP3A4 assessed as NADPH-fortified enzyme-mediated metabolite M3 ((4R,12aS)-N-((3,5-difluorophenyl)(hydroxy)methyl)-7-hydroxy-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-[1,3]oxazino[3,2-d]pyri2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1877931Displacement of [3H]-DTG from Sprague-Dawley rat liver Sigma 2 receptor incubated for 120 mins in presence of [3H]-(+)-pentazocine by liquid scintillation counting analysis2022European journal of medicinal chemistry, Feb-15, Volume: 230ISSN: 1768-3254Dual Sigma-1 receptor antagonists and hydrogen sulfide-releasing compounds for pain treatment: Design, synthesis, and pharmacological evaluation.
AID1211933Drug metabolism in supersomes expressing human recombinant CYP3A4 assessed as for NADPH-fortified enzyme-mediated metabolite M1 ((4R,12aS)-7-hydroxy-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-[1,3]oxazino[3,2-d]pyrido[1,2-a]pyrazine-9-carboxamide) for2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1155174Antiviral activity against raltegravir-resistant HIV-1 harboring integrase Y143R mutant infected in human HOS cells pretreated with compound for 3 hrs by single-round HIV-1 infectivity assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
ISSN: 1520-4804
4-amino-1-hydroxy-2-oxo-1,8-naphthyridine-containing compounds having high potency against raltegravir-resistant integrase mutants of HIV-1.
AID1212029Metabolism-dependent inhibition of CYP3A4 in human liver microsomes using nifedipine as substrate preincubated for 20 mins with NADPH prior to initiation of reaction with probe substrate by HPLC analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211927Drug metabolism assessed as intrinsic clearance for human recombinant UGT1A1-mediated DTG glucuronide M2 ((2S,3S,4S,5R,6S)-6-((4R,12aS)-9-(2,4-difluorobenzylcarbamoyl)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-[1,3]oxazino[3,2-d]pyrido[1,2-a]pyrazin-2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1604011Inhibition of HIV-1 NL4-3 integrase G140S/Q148R double mutant2019European journal of medicinal chemistry, Nov-01, Volume: 181ISSN: 1768-3254Synthetic routes and structure-activity relationships (SAR) of anti-HIV agents: A key review.
AID1211957Activity at human BCRP expressed in MDCK2 cells assessed as apical to basolateral mass balance at 3 uM by liquid scintillation counting analysis in presence of 3 uM P-gp and BCRP inhibitor GF1209182013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211962In vitro passive membrane permeability from basolateral to apical side of dog MDCK2 cells at 3 uM using Dulbecco's modified Eagle's medium as transport buffer at pH 7.4 on both donor and receiver side by liquid scintillation counting analysis in presence 2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1155179Ratio of EC50 for raltegravir-resistant HIV-1 harboring integrase G140S/Q148H double mutant infected in human HOS cells to EC50 for HIV-1 harboring integrase wild type integrase infected in human HOS cells2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
ISSN: 1520-4804
4-amino-1-hydroxy-2-oxo-1,8-naphthyridine-containing compounds having high potency against raltegravir-resistant integrase mutants of HIV-1.
AID1212004Drug excretion in human urine at 20 mg, po2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1635809Fold resistance, ratio of EC50 for raltegravir-resistant HIV1 8070-2 expressing integrase G140S/Q148H mutant to EC50 for HIV1 expressing wild-type integrase2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
ISSN: 1520-4804
3-Hydroxypyrimidine-2,4-dione-5-N-benzylcarboxamides Potently Inhibit HIV-1 Integrase and RNase H.
AID1211971Inhibition of human OATP1B1 expressed in CHO cells using [3H]estradiol 17beta-D-glucuronide as substrate by liquid scintillation counting analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID759979Antiviral activity against pseudo Human immunodeficiency virus infected in HEK293T cells after 2 days2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
ISSN: 1520-4804
Carbamoyl pyridone HIV-1 integrase inhibitors 3. A diastereomeric approach to chiral nonracemic tricyclic ring systems and the discovery of dolutegravir (S/GSK1349572) and (S/GSK1265744).
AID1211942Inhibition of CYP2A6 in human liver microsomes using coumarin as substrate preincubated for 20 mins with substrate prior to initiation of reaction with NADPH by HPLC analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211975Inhibition of human OCT2 expressed in MDCK2 cells using [14C]metformin as substrate at 25 uM by liquid scintillation counting analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211970Inhibition of human MRP2 expressed in baculovirus-infected Sf9 cell membrane vesicle using [3H]estradiol 17beta-D-glucuronide as substrate preincubated with vesicles for 5 mins prior to substrate addition by liquid scintillation counting analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211928Drug metabolism in supersomes expressing human recombinant CYP3A4 assessed as intrinsic clearance for NADPH-fortified enzyme-mediated metabolite M3 ((4R,12aS)-N-((3,5-difluorophenyl)(hydroxy)methyl)-7-hydroxy-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1483414Inhibition of recombinant full length HIV1 reverse transcriptase polymerase domain assessed as decrease in extension of 18 nucleotide DNA primer annealed to 100 nucleotide DNA template after 30 mins2017Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
ISSN: 1520-4804
Double-Winged 3-Hydroxypyrimidine-2,4-diones: Potent and Selective Inhibition against HIV-1 RNase H with Significant Antiviral Activity.
AID1211921Drug metabolism in UDPGA-fortified human liver microsomes assessed as DTG glucuronide metabolite ((2S,3S,4S,5R,6S)-6-((4R,12aS)-9-(2,4-difluorobenzylcarbamoyl)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-[1,3]oxazino[3,2-d]pyrido[1,2-a]pyrazin-7-yloxy)2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211974Inhibition of human OCT2 expressed in MDCK2 cells using [14C]metformin as substrate by liquid scintillation counting analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211994Activity at human MDR1 expressed in MDCK2 cells assessed as rate of passive membrane permeability from basolateral to apical side at 3 uM by liquid scintillation counting analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1073319Antiviral activity against HIV-1 harboring integrase G140S/Q148K double mutant relative to wild type HIV12014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
ISSN: 1520-4804
Inhibiting the HIV integration process: past, present, and the future.
AID1211948Drug metabolism assessed as UDPGA-fortified human recombinant UGT2B4-mediated DTG glucuronide metabolite ((2S,3S,4S,5R,6S)-6-((4R,12aS)-9-(2,4-difluorobenzylcarbamoyl)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-[1,3]oxazino[3,2-d]pyrido[1,2-a]pyrazin-2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211939Drug metabolism in supersomes expressing human recombinant CYP2C19 assessed as NADPH-fortified enzyme-mediated metabolite formation at 5 uM after 120 mins by radio HPLC analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211926Drug metabolism assessed as human recombinant UGT1A1-mediated DTG glucuronide M2 ((2S,3S,4S,5R,6S)-6-((4R,12aS)-9-(2,4-difluorobenzylcarbamoyl)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-[1,3]oxazino[3,2-d]pyrido[1,2-a]pyrazin-7-yloxy)-3,4,5-trihydrox2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211979Ratio of peak plasma concentration in human at 50 mg administered as daily dose to IC50 for human OTAP1B32013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211976Ratio of peak plasma concentration in human at 50 mg administered as daily dose to IC50 for human P-gp2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1604007Inhibition of HIV-2 ROD9 integrase E92Q/N155H double mutant2019European journal of medicinal chemistry, Nov-01, Volume: 181ISSN: 1768-3254Synthetic routes and structure-activity relationships (SAR) of anti-HIV agents: A key review.
AID1155180Antiviral activity against INSTI-resistant HIV-1 harboring integrase R263K mutant infected in human HOS cells pretreated with compound for 3 hrs by single-round HIV-1 infectivity assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
ISSN: 1520-4804
4-amino-1-hydroxy-2-oxo-1,8-naphthyridine-containing compounds having high potency against raltegravir-resistant integrase mutants of HIV-1.
AID1212023Metabolism-dependent inhibition of CYP2B6 in human liver microsomes using bupropion as substrate preincubated for 20 mins with NADPH prior to initiation of reaction with probe substrate by HPLC analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1212011Inhibition of CYP2C9 in human liver microsomes using diclofenac as substrate preincubated for 20 mins with substrate prior to initiation of reaction with NADPH by HPLC analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1270894Inhibition of HIV integrase-mediated strand transfer activity using 5'-[gamma-32P]-labeled full length 21T DNA at 50 nM after 2 hrs2015European journal of medicinal chemistry, Dec-01, Volume: 106ISSN: 1768-3254Anti-HIV-1 activity of a tripodal receptor that recognizes mannose oligomers.
AID1073327Antiviral activity against HIV-1 harboring integrase Q148R mutant relative to wild type HIV12014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
ISSN: 1520-4804
Inhibiting the HIV integration process: past, present, and the future.
AID1211941Inhibition of CYP1A2 in human liver microsomes using phenacetin as substrate preincubated for 20 mins with substrate prior to initiation of reaction with NADPH by HPLC analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1155183Ratio of EC50 for INSTI-resistant HIV-1 harboring integrase G118R mutant infected in human HOS cells to EC50 for HIV-1 harboring integrase wild type integrase infected in human HOS cells2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
ISSN: 1520-4804
4-amino-1-hydroxy-2-oxo-1,8-naphthyridine-containing compounds having high potency against raltegravir-resistant integrase mutants of HIV-1.
AID1211947Drug metabolism assessed as UDPGA-fortified human recombinant UGT1A6-mediated DTG glucuronide metabolite ((2S,3S,4S,5R,6S)-6-((4R,12aS)-9-(2,4-difluorobenzylcarbamoyl)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-[1,3]oxazino[3,2-d]pyrido[1,2-a]pyrazin-2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211955Activity at human MDR1 expressed in MDCK2 cells assessed as apical to basolateral mass balance at 3 uM by liquid scintillation counting analysis in presence of 3 uM P-gp and BCRP inhibitor GF1209182013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1155177Ratio of EC50 for raltegravir-resistant HIV-1 harboring integrase Y143R mutant infected in human HOS cells to EC50 for HIV-1 harboring integrase wild type integrase infected in human HOS cells2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
ISSN: 1520-4804
4-amino-1-hydroxy-2-oxo-1,8-naphthyridine-containing compounds having high potency against raltegravir-resistant integrase mutants of HIV-1.
AID1211919Drug metabolism in UDPGA-fortified human liver microsomes assessed as DTG glucuronide metabolite ((2S,3S,4S,5R,6S)-6-((4R,12aS)-9-(2,4-difluorobenzylcarbamoyl)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-[1,3]oxazino[3,2-d]pyrido[1,2-a]pyrazin-7-yloxy)2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211959Activity at human MDR1 expressed in MDCK2 cells assessed as basolateral to apical mass balance at 3 uM by liquid scintillation counting analysis in presence of 3 uM P-gp and BCRP inhibitor GF1209182013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211935Drug metabolism in supersomes expressing human recombinant CYP1A2 assessed as NADPH-fortified enzyme-mediated metabolite formation at 5 uM after 120 mins by radio HPLC analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1212015Inhibition of CYP3A4 in human liver microsomes using nifedipine as substrate preincubated for 20 mins with substrate prior to initiation of reaction with NADPH by HPLC analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1655660Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membranes incubated for 1 hr by liquid scintillation counting method2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
ISSN: 1948-5875
AID1211924Drug metabolism in UDPGA-fortified human liver microsomes assessed as intrinsic clearance for UGT1A1-mediated DTG glucuronide M2 ((2S,3S,4S,5R,6S)-6-((4R,12aS)-9-(2,4-difluorobenzylcarbamoyl)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-[1,3]oxazino[3,22013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1506087Displacement of [3H]DTG from sigma2 receptor in rat liver membranes after 60 mins by liquid scintillation counting method2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
ISSN: 1520-4804
Contilisant, a Tetratarget Small Molecule for Alzheimer's Disease Therapy Combining Cholinesterase, Monoamine Oxidase Inhibition, and H3R Antagonism with S1R Agonism Profile.
AID1604002Inhibition of HIV-2 ROD9 integrase Q148R mutant2019European journal of medicinal chemistry, Nov-01, Volume: 181ISSN: 1768-3254Synthetic routes and structure-activity relationships (SAR) of anti-HIV agents: A key review.
AID1212003Induction of CYP3A4 mRNA expression in human hepatocytes at 1 to 40 uM after 48 hrs by real time PCR analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1155181Antiviral activity against INSTI-resistant HIV-1 harboring integrase G118R mutant infected in human HOS cells pretreated with compound for 3 hrs by single-round HIV-1 infectivity assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
ISSN: 1520-4804
4-amino-1-hydroxy-2-oxo-1,8-naphthyridine-containing compounds having high potency against raltegravir-resistant integrase mutants of HIV-1.
AID1270892Inhibition of HIV integrase-mediated 3'-processing activity using 5'-[gamma-32P]-labeled full length 21T DNA after 2 hrs2015European journal of medicinal chemistry, Dec-01, Volume: 106ISSN: 1768-3254Anti-HIV-1 activity of a tripodal receptor that recognizes mannose oligomers.
AID1211940Drug metabolism in supersomes expressing human recombinant CYP2D6 assessed as NADPH-fortified enzyme-mediated metabolite formation at 5 uM after 120 mins by radio HPLC analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211932Drug metabolism in NADPH-fortified human liver microsomes assessed as metabolite M3 ((4R,12aS)-N-((3,5-difluorophenyl)(hydroxy)methyl)-7-hydroxy-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-[1,3]oxazino[3,2-d]pyrido[1,2-a]pyrazine-9-carboxamide) formati2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1073330Antiviral activity against HIV-1 harboring integrase Y143R mutant relative to wild type HIV12014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
ISSN: 1520-4804
Inhibiting the HIV integration process: past, present, and the future.
AID1212007Inhibition of human MDR12013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1406293Selectivity index, ratio of IC50 for HIV integrase strand transfer activity to IC50 for HIV1 reverse transcriptase RNaseH activity2018European journal of medicinal chemistry, Aug-05, Volume: 156ISSN: 1768-32546-Arylthio-3-hydroxypyrimidine-2,4-diones potently inhibited HIV reverse transcriptase-associated RNase H with antiviral activity.
AID1073329Antiviral activity against HIV-1 harboring integrase Q148H mutant relative to wild type HIV12014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
ISSN: 1520-4804
Inhibiting the HIV integration process: past, present, and the future.
AID1212028Metabolism-dependent inhibition of CYP3A4 in human liver microsomes using atorvastatin as substrate preincubated for 20 mins with NADPH prior to initiation of reaction with probe substrate by HPLC analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211989Drug metabolism assessed as UDPGA-fortified human recombinant UGT1A9-mediated DTG glucuronide metabolite ((2S,3S,4S,5R,6S)-6-((4R,12aS)-9-(2,4-difluorobenzylcarbamoyl)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-[1,3]oxazino[3,2-d]pyrido[1,2-a]pyrazin-2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1212012Inhibition of CYP2C19 in human liver microsomes using S-mephenytoin as substrate preincubated for 20 mins with substrate prior to initiation of reaction with NADPH by HPLC analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1073326Antiviral activity against HIV-1 harboring integrase N155H mutant relative to wild type HIV12014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
ISSN: 1520-4804
Inhibiting the HIV integration process: past, present, and the future.
AID1211977Ratio of peak plasma concentration in human at 50 mg administered as daily dose to IC50 for human BCRP2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211973Inhibition of human OCT1 expressed in HEK293 cells using [14C]metformin as substrate at 10 uM after 10 mins by liquid scintillation counting analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1604006Inhibition of HIV-2 ROD9 integrase G140S/Q148R double mutant2019European journal of medicinal chemistry, Nov-01, Volume: 181ISSN: 1768-3254Synthetic routes and structure-activity relationships (SAR) of anti-HIV agents: A key review.
AID1191389Displacement of [3H]DTG from rat liver sigma2 receptor by scintillation analyzer2015European journal of medicinal chemistry, Jan-27, Volume: 90ISSN: 1768-3254Improving selectivity preserving affinity: new piperidine-4-carboxamide derivatives as effective sigma-1-ligands.
AID1073320Antiviral activity against HIV-1 harboring integrase G140S/Q148H double mutant relative to wild type HIV12014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
ISSN: 1520-4804
Inhibiting the HIV integration process: past, present, and the future.
AID1211985Drug metabolism assessed as UDPGA-fortified human recombinant UGT1A1-mediated DTG glucuronide metabolite ((2S,3S,4S,5R,6S)-6-((4R,12aS)-9-(2,4-difluorobenzylcarbamoyl)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-[1,3]oxazino[3,2-d]pyrido[1,2-a]pyrazin-2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1155182Ratio of EC50 for INSTI-resistant HIV-1 harboring integrase R263K mutant infected in human HOS cells to EC50 for HIV-1 harboring integrase wild type integrase infected in human HOS cells2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
ISSN: 1520-4804
4-amino-1-hydroxy-2-oxo-1,8-naphthyridine-containing compounds having high potency against raltegravir-resistant integrase mutants of HIV-1.
AID1155178Ratio of EC50 for raltegravir-resistant HIV-1 harboring integrase N155H mutant infected in human HOS cells to EC50 for HIV-1 harboring integrase wild type integrase infected in human HOS cells2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
ISSN: 1520-4804
4-amino-1-hydroxy-2-oxo-1,8-naphthyridine-containing compounds having high potency against raltegravir-resistant integrase mutants of HIV-1.
AID1604009Inhibition of wild type HIV-1 NL4-3 integrase2019European journal of medicinal chemistry, Nov-01, Volume: 181ISSN: 1768-3254Synthetic routes and structure-activity relationships (SAR) of anti-HIV agents: A key review.
AID1588917Inhibition of HIV integrase strand transfer activity2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
ISSN: 1464-3391
Design, synthesis and biological evaluation of 3-hydroxyquinazoline-2,4(1H,3H)-diones as dual inhibitors of HIV-1 reverse transcriptase-associated RNase H and integrase.
AID1211990Activity at human MDR1 expressed in MDCK2 cells assessed as rate of passive membrane permeability from apical to basolateral side at 3 uM by liquid scintillation counting analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1604001Inhibition of HIV-2 ROD9 integrase Q148H mutant2019European journal of medicinal chemistry, Nov-01, Volume: 181ISSN: 1768-3254Synthetic routes and structure-activity relationships (SAR) of anti-HIV agents: A key review.
AID1877932Displacement of [3H]-(+)-pentazocine from Dunkin-Hartley guinea pig brain cortex Sigma 1 receptor incubated for 150 mins by liquid scintillation counting analysis2022European journal of medicinal chemistry, Feb-15, Volume: 230ISSN: 1768-3254Dual Sigma-1 receptor antagonists and hydrogen sulfide-releasing compounds for pain treatment: Design, synthesis, and pharmacological evaluation.
AID1604012Inhibition of HIV-1 NL4-3 integrase E92Q/N155H double mutant2019European journal of medicinal chemistry, Nov-01, Volume: 181ISSN: 1768-3254Synthetic routes and structure-activity relationships (SAR) of anti-HIV agents: A key review.
AID1212001Induction of CYP1A2 mRNA expression in human hepatocytes at 1 to 40 uM after 48 hrs by real time PCR analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1635801Inhibition of HIV1 recombinant integrase expressed in Escherichia coli using [32P]-labeled oligonucleotide as substrate after 60 mins by strand transfer activity assay2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
ISSN: 1520-4804
3-Hydroxypyrimidine-2,4-dione-5-N-benzylcarboxamides Potently Inhibit HIV-1 Integrase and RNase H.
AID1506088Displacement of (-)-[3H]vesamicol from rat VAChT expressed in rat PC12 cell membranes after 60 mins by liquid scintillation counting method2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
ISSN: 1520-4804
Contilisant, a Tetratarget Small Molecule for Alzheimer's Disease Therapy Combining Cholinesterase, Monoamine Oxidase Inhibition, and H3R Antagonism with S1R Agonism Profile.
AID1300998Selectivity ratio of EC50 for raltegravir resistant HIV1 harboring integrase G140S/Q148H double mutant infected in human MT4 cells to EC50 for wild type HIV1 3B infected in human MT4 cells2016European journal of medicinal chemistry, Jul-19, Volume: 117ISSN: 1768-32542-hydroxyisoquinoline-1,3(2H,4H)-diones (HIDs) as human immunodeficiency virus type 1 integrase inhibitors: Influence of the alkylcarboxamide substitution of position 4.
AID1211996Activity at human BCRP expressed in MDCK2 cells assessed as rate of passive membrane permeability from basolateral to apical side at 3 uM by liquid scintillation counting analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211960Activity at human BCRP expressed in MDCK2 cells assessed as basolateral to apical mass balance at 3 uM by liquid scintillation counting analysis2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1211993Activity at human BCRP expressed in MDCK2 cells assessed as rate of passive membrane permeability from apical to basolateral side at 3 uM by liquid scintillation counting analysis in presence of 3 uM P-gp and BCRP inhibitor GF1209182013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
ISSN: 1521-009X
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
AID1483416Selectivity index, ratio of IC50 for HIV integrase strand transfer activity to IC50 for recombinant full length HIV1 reverse transcriptase RNase H domain2017Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
ISSN: 1520-4804
Double-Winged 3-Hydroxypyrimidine-2,4-diones: Potent and Selective Inhibition against HIV-1 RNase H with Significant Antiviral Activity.
AID1602242Inhibition of HIV1 reverse transcriptase polymerase using deoxynucleotide triphosphates and 18 nucleotide DNA primer annealed to 100 nucleotide DNA template after 30 mins2019European journal of medicinal chemistry, Mar-15, Volume: 166ISSN: 1768-3254Pharmacophore-based design of novel 3-hydroxypyrimidine-2,4-dione subtypes as inhibitors of HIV reverse transcriptase-associated RNase H: Tolerance of a nonflexible linker.
AID759970Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells after 4 to 5 days by bioluminescence assay in presence of human serum relative to control2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
ISSN: 1520-4804
Carbamoyl pyridone HIV-1 integrase inhibitors 3. A diastereomeric approach to chiral nonracemic tricyclic ring systems and the discovery of dolutegravir (S/GSK1349572) and (S/GSK1265744).
AID1406294Antiviral activity against HIV1 infected in CD4/CXCR4/CCR5 expressing human P4R5 MAGI cells preincubated with cells for 24 hrs followed by viral infection measured after 48 hrs by beta-galactosidase reporter gene assay2018European journal of medicinal chemistry, Aug-05, Volume: 156ISSN: 1768-32546-Arylthio-3-hydroxypyrimidine-2,4-diones potently inhibited HIV reverse transcriptase-associated RNase H with antiviral activity.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
ISSN: 2472-5560
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
ISSN: 1091-6490
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
ISSN: 1521-0111
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173ISSN: 1872-9096A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173ISSN: 1872-9096A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
ISSN: 2211-1247
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression2022The Journal of biological chemistry, 08, Volume: 298, Issue:8
ISSN: 1083-351X
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173ISSN: 1872-9096A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
ISSN: 1521-0111
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB2011Molecular pharmacology, Oct, Volume: 80, Issue:4
ISSN: 1521-0111
Structural and functional analyses of the second-generation integrase strand transfer inhibitor dolutegravir (S/GSK1349572).

Research

Studies (1,108)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's614 (55.42)24.3611
2020's494 (44.58)2.80

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials179 (15.87%)5.53%
Reviews119 (10.55%)6.00%
Case Studies95 (8.42%)4.05%
Observational58 (5.14%)0.25%
Other677 (60.02%)84.16%
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
acetamideacetamides;
carboximidic acid;
monocarboxylic acid amide;
N-acylammonia
00low000000
indoleacetamideindoles;
monocarboxylic acid amide;
N-acylammonia
bacterial metabolite;
fungal metabolite;
plant metabolite
00low000000
dihydrolipoamidedithiol;
monocarboxylic acid amide
cofactor;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
00low000000
formamidecarboximidic acid;
formamides;
monocarboxylic acid amide;
one-carbon compound
solvent00low000000
lipoamidedithiolanes;
monocarboxylic acid amide
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
00low000000
pyrazinamidemonocarboxylic acid amide;
N-acylammonia;
pyrazines
antitubercular agent;
prodrug
00low000000
ureaisourea;
monocarboxylic acid amide;
one-carbon compound
Daphnia magna metabolite;
Escherichia coli metabolite;
fertilizer;
flour treatment agent;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
00low000000
pk 11195aromatic amide;
isoquinolines;
monocarboxylic acid amide;
monochlorobenzenes
antineoplastic agent00low000000
5-(n,n-hexamethylene)amiloridearomatic amine;
azepanes;
guanidines;
monocarboxylic acid amide;
organochlorine compound;
pyrazines
antineoplastic agent;
apoptosis inducer;
odorant receptor antagonist;
sodium channel blocker
00low000000
ethylisopropylamiloridearomatic amine;
guanidines;
monocarboxylic acid amide;
organochlorine compound;
pyrazines;
tertiary amino compound
anti-arrhythmia drug;
neuroprotective agent;
sodium channel blocker
00low000000
acebutololaromatic amide;
ethanolamines;
ether;
monocarboxylic acid amide;
propanolamine;
secondary amino compound
anti-arrhythmia drug;
antihypertensive agent;
beta-adrenergic antagonist;
sympathomimetic agent
00low000000
acetazolamidemonocarboxylic acid amide;
sulfonamide;
thiadiazoles
anticonvulsant;
diuretic;
EC 4.2.1.1 (carbonic anhydrase) inhibitor
00low000000
acetochloraromatic amide;
monocarboxylic acid amide;
organochlorine compound
environmental contaminant;
herbicide;
xenobiotic
00low000000
alachloraromatic amide;
monocarboxylic acid amide;
organochlorine compound
environmental contaminant;
herbicide;
xenobiotic
00low000000
alfuzosinmonocarboxylic acid amide;
quinazolines;
tetrahydrofuranol
alpha-adrenergic antagonist;
antihypertensive agent;
antineoplastic agent
00low000000
ampiroxicamacetal;
aminopyridine;
benzothiazine;
etabonate ester;
monocarboxylic acid amide;
sulfonamide
analgesic;
antirheumatic drug;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-steroidal anti-inflammatory drug;
prodrug
00low000000
atenololethanolamines;
monocarboxylic acid amide;
propanolamine
anti-arrhythmia drug;
antihypertensive agent;
beta-adrenergic antagonist;
environmental contaminant;
sympatholytic agent;
xenobiotic
00low000000
benzquinamidemonocarboxylic acid amideantiemetic;
antipsychotic agent;
H1-receptor antagonist;
muscarinic antagonist;
sedative
00low000000
bicalutamide(trifluoromethyl)benzenes;
monocarboxylic acid amide;
monofluorobenzenes;
nitrile;
sulfone;
tertiary alcohol
00low000000
carcininebeta-alanine derivative;
imidazoles;
monocarboxylic acid amide;
organonitrogen compound;
organooxygen compound
antioxidant;
crustacean metabolite
00low000000
dacarbazineimidazoles;
monocarboxylic acid amide;
triazene derivative
alkylating agent;
antineoplastic agent;
carcinogenic agent;
prodrug
00low000000
dibucainearomatic ether;
monocarboxylic acid amide;
tertiary amino compound
topical anaesthetic00low000000
dimethoatemonocarboxylic acid amide;
organic thiophosphate
acaricide;
agrochemical;
EC 3.1.1.7 (acetylcholinesterase) inhibitor;
EC 3.1.1.8 (cholinesterase) inhibitor;
environmental contaminant;
insecticide;
xenobiotic
00low000000
disopyramidemonocarboxylic acid amide;
pyridines;
tertiary amino compound
anti-arrhythmia drug00low000000
doxazosinaromatic amine;
benzodioxine;
monocarboxylic acid amide;
N-acylpiperazine;
N-arylpiperazine;
quinazolines
alpha-adrenergic antagonist;
antihyperplasia drug;
antihypertensive agent;
antineoplastic agent;
vasodilator agent
00low000000
etanidazoleC-nitro compound;
imidazoles;
monocarboxylic acid amide
alkylating agent;
antineoplastic agent;
prodrug;
radiosensitizing agent
00low000000
fentanylanilide;
monocarboxylic acid amide;
piperidines
adjuvant;
anaesthesia adjuvant;
anaesthetic;
intravenous anaesthetic;
mu-opioid receptor agonist;
opioid analgesic
00low000000
flecainidearomatic ether;
monocarboxylic acid amide;
organofluorine compound;
piperidines
anti-arrhythmia drug00low000000
flutamide(trifluoromethyl)benzenes;
monocarboxylic acid amide
androgen antagonist;
antineoplastic agent
00low000000
glipizidearomatic amide;
monocarboxylic acid amide;
N-sulfonylurea;
pyrazines
EC 2.7.1.33 (pantothenate kinase) inhibitor;
hypoglycemic agent;
insulin secretagogue
00low000000
lidocainebenzenes;
monocarboxylic acid amide;
tertiary amino compound
anti-arrhythmia drug;
drug allergen;
environmental contaminant;
local anaesthetic;
xenobiotic
00low000000
leflunomide(trifluoromethyl)benzenes;
isoxazoles;
monocarboxylic acid amide
antineoplastic agent;
antiparasitic agent;
EC 1.3.98.1 [dihydroorotate oxidase (fumarate)] inhibitor;
EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor;
hepatotoxic agent;
immunosuppressive agent;
non-steroidal anti-inflammatory drug;
prodrug;
pyrimidine synthesis inhibitor;
tyrosine kinase inhibitor
00low000000
qx-314monocarboxylic acid amidelocal anaesthetic00low000000
loperamidemonocarboxylic acid amide;
monochlorobenzenes;
piperidines;
tertiary alcohol
anticoronaviral agent;
antidiarrhoeal drug;
mu-opioid receptor agonist
00low000000
modafinilmonocarboxylic acid amide;
sulfoxide
00low000000
deetbenzamides;
monocarboxylic acid amide
environmental contaminant;
insect repellent;
xenobiotic
00low000000
pipamperonearomatic ketone;
bipiperidines;
monocarboxylic acid amide;
organofluorine compound;
tertiary amino compound
dopaminergic antagonist;
first generation antipsychotic;
serotonergic antagonist
00low000000
prazosinaromatic ether;
furans;
monocarboxylic acid amide;
piperazines;
quinazolines
alpha-adrenergic antagonist;
antihypertensive agent;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor
00low000000
prilocaineamino acid amide;
monocarboxylic acid amide
anticonvulsant;
local anaesthetic
00low000000
propachloranilide;
monocarboxylic acid amide;
organochlorine compound
environmental contaminant;
herbicide;
xenobiotic
00low000000
carbamylhydrazinecarbohydrazide;
monocarboxylic acid amide;
one-carbon compound;
ureas
00low000000
temozolomideimidazotetrazine;
monocarboxylic acid amide;
triazene derivative
alkylating agent;
antineoplastic agent;
prodrug
00low000000
lysergic acid diethylamideergoline alkaloid;
monocarboxylic acid amide;
organic heterotetracyclic compound
dopamine agonist;
hallucinogen;
serotonergic agonist
00low000000
propionamidemonocarboxylic acid amide;
primary fatty amide
00low000000
n-methylacetamideacetamides;
monocarboxylic acid amide
metabolite00low000000
2-phenylacetamidemonocarboxylic acid amidemouse metabolite00low000000
6-aminonicotinamideaminopyridine;
monocarboxylic acid amide;
primary amino compound
antimetabolite;
EC 1.1.1.44 (NADP(+)-dependent decarboxylating phosphogluconate dehydrogenase) inhibitor;
teratogenic agent
00low000000
aminoimidazole carboxamideaminoimidazole;
monocarboxylic acid amide
mouse metabolite00low000000
valeramidemonocarboxylic acid amide00low000000
devrinolaromatic ether;
monocarboxylic acid amide;
naphthalenes
00low000000
thiamphenicolmonocarboxylic acid amide;
sulfone
antimicrobial agent;
immunosuppressive agent
00low000000
lisuridemonocarboxylic acid amideantidyskinesia agent;
antiparkinson drug;
dopamine agonist;
serotonergic agonist
00low000000
dimethylacetamideacetamides;
monocarboxylic acid amide
human metabolite00low000000
benzonidazoleC-nitro compound;
imidazoles;
monocarboxylic acid amide
antiprotozoal drug00low000000
n-methyl-n-(trimethylsilyl)trifluoroacetamidemonocarboxylic acid amide;
N-silyl compound;
trifluoroacetamide
chromatographic reagent00low000000
ribavirin1-ribosyltriazole;
aromatic amide;
monocarboxylic acid amide;
primary carboxamide
anticoronaviral agent;
antiinfective agent;
antimetabolite;
antiviral agent;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor
00low000000
tocainidemonocarboxylic acid amideanti-arrhythmia drug;
local anaesthetic;
sodium channel blocker
00low000000
bezafibratearomatic ether;
monocarboxylic acid amide;
monocarboxylic acid;
monochlorobenzenes
antilipemic drug;
environmental contaminant;
geroprotector;
xenobiotic
00low000000
closantelaromatic amide;
monocarboxylic acid amide;
monochlorobenzenes;
nitrile;
organoiodine compound;
phenols
00low000000
alfentanilmonocarboxylic acid amide;
piperidines
central nervous system depressant;
intravenous anaesthetic;
mu-opioid receptor agonist;
opioid analgesic;
peripheral nervous system drug
00low000000
ranolazinearomatic amide;
monocarboxylic acid amide;
monomethoxybenzene;
N-alkylpiperazine;
secondary alcohol
00low000000
remifentanilalpha-amino acid ester;
anilide;
monocarboxylic acid amide;
piperidinecarboxylate ester
intravenous anaesthetic;
mu-opioid receptor agonist;
opioid analgesic;
sedative
00low000000
valsartanbiphenylyltetrazole;
monocarboxylic acid amide;
monocarboxylic acid
angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
00low000000
3-methylfentanylmonocarboxylic acid amide;
piperidines
mu-opioid receptor agonist;
opioid analgesic;
sedative
00low000000
4-fluorofentanylmonocarboxylic acid amide;
organofluorine compound;
piperidines
00low000000
1,2,4-triazole-3-carboxamidearomatic amide;
monocarboxylic acid amide;
primary carboxamide;
triazoles
drug metabolite;
human urinary metabolite
00low000000
aloxistatinepoxide;
ethyl ester;
L-leucine derivative;
monocarboxylic acid amide
anticoronaviral agent;
cathepsin B inhibitor
00low000000
phenylacetylglycinemonocarboxylic acid amide;
monocarboxylic acid;
N-acylglycine
human metabolite;
mouse metabolite
00low000000
mandelamidebenzyl alcohols;
monocarboxylic acid amide;
secondary alcohol
00low000000
5-(3-methyl-1-triazeno)imidazole-4-carboxamideimidazoles;
monocarboxylic acid amide;
triazene derivative
alkylating agent;
antineoplastic agent
00low000000
biocytinazabicycloalkane;
L-alpha-amino acid zwitterion;
L-lysine derivative;
monocarboxylic acid amide;
non-proteinogenic L-alpha-amino acid;
thiabicycloalkane;
ureas
mouse metabolite00low000000
biotinamidebiotins;
monocarboxylic acid amide
human metabolite00low000000
lactamidemonocarboxylic acid amide;
secondary alcohol
00low000000
ribavirin 5'-diphosphate1-ribosyltriazole;
aromatic amide;
monocarboxylic acid amide;
primary carboxamide;
ribose monophosphate
antiviral agent;
drug metabolite;
EC 1.1.1.205 (IMP dehydrogenase) inhibitor;
human blood serum metabolite
00low000000
difenpiramidebiphenyls;
monocarboxylic acid amide;
pyridines
antipyretic;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
00low000000
u 69593monocarboxylic acid amide;
N-alkylpyrrolidine;
organic heterobicyclic compound;
oxaspiro compound
anti-inflammatory agent;
diuretic;
kappa-opioid receptor agonist
00low000000
phenazine-1-carboxamidearomatic amide;
monocarboxylic acid amide;
phenazines
00low000000
ribavirin 5'-triphosphate1-ribosyltriazole;
aromatic amide;
monocarboxylic acid amide;
primary carboxamide;
ribose triphosphate
antiviral agent;
drug metabolite;
EC 2.7.7.48 (RNA-directed RNA polymerase) inhibitor;
eukaryotic initiation factor 4F inhibitor;
human blood serum metabolite
00low000000
n(6)-(3-iodobenzyl)-5'-n-methylcarboxamidoadenosineadenosines;
monocarboxylic acid amide;
organoiodine compound
adenosine A3 receptor agonist00low000000
4-carbamoylimidazolium 5-olatehydroxyimidazole;
monocarboxylic acid amide
antineoplastic agent00low000000
ribavirin 5'-diphosphate1-ribosyltriazole;
aromatic amide;
monocarboxylic acid amide;
primary carboxamide;
ribose diphosphate
antiviral agent;
drug metabolite
00low000000
methotrexatedicarboxylic acid;
monocarboxylic acid amide;
pteridines
abortifacient;
antimetabolite;
antineoplastic agent;
antirheumatic drug;
dermatologic drug;
DNA synthesis inhibitor;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
immunosuppressive agent
00low000000
dexpanthenolamino alcohol;
monocarboxylic acid amide
cholinergic drug;
provitamin
00low000000
cercosporamidedibenzofurans;
methyl ketone;
monocarboxylic acid amide;
polyphenol
antifungal agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
fungal metabolite;
phytotoxin
00low000000
cyclazosinaromatic amide;
aromatic ether;
furans;
monocarboxylic acid amide;
quinazolines;
quinoxaline derivative
adenosine A2A receptor antagonist00low000000
nepafenacmonocarboxylic acid amidecyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
prodrug
00low000000
rp 73401aromatic ether;
benzamides;
chloropyridine;
monocarboxylic acid amide
anti-asthmatic drug;
anti-inflammatory agent;
bronchodilator agent;
phosphodiesterase IV inhibitor
00low000000
n-(2,3-dichloro-4-hydroxyphenyl)-1-methylcyclohexanecarboxamideanilide fungicide;
aromatic amide;
dichlorobenzene;
monocarboxylic acid amide;
phenols
antifungal agrochemical;
EC 1.14.13.72 (methylsterol monooxygenase) inhibitor;
sterol biosynthesis inhibitor
00low000000
norfentanylanilide;
monocarboxylic acid amide;
piperidines
drug metabolite;
opioid analgesic
00low000000
rocaglamidemonocarboxylic acid amide;
monomethoxybenzene;
organic heterotricyclic compound
antileishmanial agent;
antineoplastic agent;
metabolite
00low000000
taurolithocholic acidbile acid taurine conjugate;
monocarboxylic acid amide
human metabolite00low000000
ochratoxin aisochromanes;
monocarboxylic acid amide;
N-acyl-L-phenylalanine;
organochlorine compound;
phenylalanine derivative
Aspergillus metabolite;
calcium channel blocker;
carcinogenic agent;
mycotoxin;
nephrotoxin;
Penicillium metabolite;
teratogenic agent
00low000000
ergonovineergot alkaloid;
monocarboxylic acid amide;
organic heterotetracyclic compound;
primary alcohol;
secondary amino compound;
tertiary amino compound
diagnostic agent;
fungal metabolite;
oxytocic;
toxin
00low000000
darifenacin1-benzofurans;
monocarboxylic acid amide;
pyrrolidines
antispasmodic drug;
muscarinic antagonist
00low000000
adenosine-5'-(n-ethylcarboxamide)adenosines;
monocarboxylic acid amide
adenosine A1 receptor agonist;
adenosine A2A receptor agonist;
antineoplastic agent;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
vasodilator agent
00low000000
tiazofurin1,3-thiazoles;
C-glycosyl compound;
monocarboxylic acid amide
antineoplastic agent;
EC 1.1.1.205 (IMP dehydrogenase) inhibitor;
prodrug
00low000000
glucuronamidemonocarboxylic acid amide;
monosaccharide derivative
00low000000
n-methyl-n-(tert-butyldimethylsilyl)trifluoroacetamidemonocarboxylic acid amide;
N-silyl compound;
trifluoroacetamide
chromatographic reagent00low000000
n-(3-chloro-4-methylphenyl)-4-methyl-1,2,3-thiadiazole-5-carboxamideanilide fungicide;
monocarboxylic acid amide;
monochlorobenzenes;
organosulfur compound;
thiadiazoles
antifungal agrochemical00low000000
lincomycincarbohydrate-containing antibiotic;
L-proline derivative;
monocarboxylic acid amide;
pyrrolidinecarboxamide;
S-glycosyl compound
antimicrobial agent;
bacterial metabolite
00low000000
u-50488dichlorobenzene;
monocarboxylic acid amide;
N-alkylpyrrolidine
analgesic;
antitussive;
calcium channel blocker;
diuretic;
kappa-opioid receptor agonist
00low000000
N-octylhomovanillamideguaiacols;
monocarboxylic acid amide
protective agent00low000000
adenosine-5'-(N-propyl)carboxamideadenosines;
monocarboxylic acid amide
00low000000
dasatinib1,3-thiazoles;
aminopyrimidine;
monocarboxylic acid amide;
N-(2-hydroxyethyl)piperazine;
N-arylpiperazine;
organochlorine compound;
secondary amino compound;
tertiary amino compound
anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor
00low000000
ex 527carbazoles;
monocarboxylic acid amide;
organochlorine compound
00low000000
entacapone2-nitrophenols;
catechols;
monocarboxylic acid amide;
nitrile
antidyskinesia agent;
antiparkinson drug;
central nervous system drug;
EC 2.1.1.6 (catechol O-methyltransferase) inhibitor
00low000000
ceruleninepoxide;
monocarboxylic acid amide
antifungal agent;
antiinfective agent;
antilipemic drug;
antimetabolite;
antimicrobial agent;
fatty acid synthesis inhibitor
00low000000
fortimicin aamino cyclitol glycoside;
aminoglycoside antibiotic;
diol;
monocarboxylic acid amide;
primary amino compound
antibacterial agent;
metabolite
00low000000
fenretinidemonocarboxylic acid amide;
retinoid
antineoplastic agent;
antioxidant
00low000000
bimatoprostmonocarboxylic acid amideantiglaucoma drug;
antihypertensive agent
00low000000
ag-490catechols;
enamide;
monocarboxylic acid amide;
nitrile;
secondary carboxamide
anti-inflammatory agent;
antioxidant;
apoptosis inducer;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
geroprotector;
STAT3 inhibitor
00low000000
su 11248monocarboxylic 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
00low000000
monocrotophosalkenyl phosphate;
dialkyl phosphate;
monocarboxylic acid amide;
organophosphate insecticide
acaricide;
agrochemical;
avicide;
EC 1.4.3.4 (monoamine oxidase) inhibitor;
EC 3.1.1.7 (acetylcholinesterase) inhibitor;
EC 3.1.1.8 (cholinesterase) inhibitor
00low000000
l 685458carbamate ester;
monocarboxylic acid amide;
peptide;
secondary alcohol
EC 3.4.23.46 (memapsin 2) inhibitor;
peptidomimetic
00low000000
aliskirenmonocarboxylic acid amide;
monomethoxybenzene
antihypertensive agent00low000000
su 1498enamide;
monocarboxylic acid amide;
nitrile;
phenols;
secondary carboxamide
vascular endothelial growth factor receptor antagonist00low000000
n(3)-(4-methoxyfumaroyl)-2,3-diaminopropionic acidenoate ester;
methyl ester;
monocarboxylic acid amide
metabolite00low000000
ekb 569aminoquinoline;
monocarboxylic acid amide;
monochlorobenzenes;
nitrile
protein kinase inhibitor00low000000
netupitantaminopyridine;
monocarboxylic acid amide;
N-alkylpiperazine;
N-arylpiperazine;
organofluorine compound;
toluenes
antiemetic;
neurokinin-1 receptor antagonist
00low000000
2-(4-fluoro-3-(trifluoromethyl)phenoxy)-n-(phenylmethyl)butanamide(trifluoromethyl)benzenes;
aromatic ether;
monocarboxylic acid amide;
monofluorobenzenes
00low000000
1-methyl-d-lysergic acid butanolamideergot alkaloid;
monocarboxylic acid amide
serotonergic antagonist;
sympatholytic agent;
vasoconstrictor agent
00low000000
platensimycinaromatic amide;
cyclic ether;
cyclic ketone;
dihydroxybenzoic acid;
monocarboxylic acid amide;
polycyclic cage
antibacterial agent;
antimicrobial agent;
bacterial metabolite;
EC 2.3.1.85 (fatty acid synthase) inhibitor
00low000000
vilazodone1-benzofurans;
indoles;
monocarboxylic acid amide;
N-alkylpiperazine;
N-arylpiperazine;
nitrile
antidepressant;
serotonergic agonist;
serotonin uptake inhibitor
00low000000
n-demethylloperamidemonocarboxylic acid amide;
monochlorobenzenes;
piperidines;
tertiary alcohol
drug metabolite00low000000
lenvatinibaromatic amide;
aromatic ether;
cyclopropanes;
monocarboxylic acid amide;
monochlorobenzenes;
phenylureas;
quinolines
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
fibroblast growth factor receptor antagonist;
orphan drug;
vascular endothelial growth factor receptor antagonist
00low000000
avibactamazabicycloalkane;
hydroxylamine O-sulfonic acid;
monocarboxylic acid amide;
ureas
antibacterial drug;
antimicrobial agent;
EC 3.5.2.6 (beta-lactamase) inhibitor
00low000000
mirabegron1,3-thiazoles;
aromatic amide;
ethanolamines;
monocarboxylic acid amide
beta-adrenergic agonist00low000000
avanafilaromatic amide;
monocarboxylic acid amide;
organochlorine compound;
prolinols;
pyrimidines
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
vasodilator agent
00low000000
rivaroxabanaromatic amide;
lactam;
monocarboxylic acid amide;
morpholines;
organochlorine compound;
oxazolidinone;
thiophenes
anticoagulant;
EC 3.4.21.6 (coagulation factor Xa) inhibitor
00low000000
selexipagaromatic amine;
ether;
monocarboxylic acid amide;
N-sulfonylcarboxamide;
pyrazines;
tertiary amino compound
orphan drug;
platelet aggregation inhibitor;
prodrug;
prostacyclin receptor agonist;
vasodilator agent
00low000000
3-iodo-4-aminobenzyl-5'-N-methylcarboxamidoadenosineadenosines;
monocarboxylic acid amide;
organoiodine compound
00low000000
ly-2157299aromatic amide;
methylpyridines;
monocarboxylic acid amide;
pyrrolopyrazole;
quinolines
antineoplastic agent;
TGFbeta receptor antagonist
00low000000
SIS3 free basearomatic ether;
enamide;
isoquinolines;
monocarboxylic acid amide;
pyrrolopyridine;
tertiary carboxamide
Smad3 inhibitor00low000000
bl1521enamide;
hydroxamic acid;
monocarboxylic acid amide
antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor
00low000000
tasimelteon1-benzofurans;
cyclopropanes;
monocarboxylic acid amide
melatonin receptor agonist00low000000
edoxabanchloropyridine;
monocarboxylic acid amide;
tertiary amino compound;
thiazolopyridine
anticoagulant;
EC 3.4.21.6 (coagulation factor Xa) inhibitor;
platelet aggregation inhibitor
00low000000
fr 901464acetate ester;
cyclic hemiketal;
monocarboxylic acid amide;
pyrans;
spiro-epoxide
antimicrobial agent;
antineoplastic agent;
bacterial metabolite
00low000000
bms 477118adamantanes;
azabicycloalkane;
monocarboxylic acid amide;
nitrile;
tertiary alcohol
EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor;
hypoglycemic agent
00low000000
mandipropamidaromatic ether;
monocarboxylic acid amide;
monochlorobenzenes;
terminal acetylenic compound
00low000000
bay 60-6583aminopyridine;
aromatic ether;
aryl sulfide;
cyanopyridine;
cyclopropanes;
monocarboxylic acid amide
adenosine A2B receptor agonist;
anti-inflammatory agent;
cardioprotective agent
00low000000
vx-770aromatic amide;
monocarboxylic acid amide;
phenols;
quinolone
CFTR potentiator;
orphan drug
00low000000
platencinaromatic amide;
cyclic ketone;
dihydroxybenzoic acid;
monocarboxylic acid amide;
polycyclic cage
antibacterial agent;
antimicrobial agent;
bacterial metabolite;
EC 2.3.1.85 (fatty acid synthase) inhibitor
00low000000
tenovin-6monocarboxylic acid amide;
tertiary amino compound;
thioureas
antineoplastic agent;
p53 activator;
Sir2 inhibitor
00low000000
bacillaeneenamine;
monocarboxylic acid amide;
polyene antibiotic;
polyketide;
secondary alcohol
antibacterial agent;
antimicrobial agent;
bacterial metabolite
00low000000
cobicistat1,3-thiazoles;
carbamate ester;
monocarboxylic acid amide;
morpholines;
ureas
P450 inhibitor00low000000
fluazaindolizinearomatic amide;
imidazopyridine;
monocarboxylic acid amide;
monochlorobenzenes;
monomethoxybenzene;
N-sulfonylcarboxamide;
organofluorine pesticide
agrochemical;
nematicide
00low000000
crambescidin 800alkaloid;
carboxylic ester;
guanidines;
monocarboxylic acid amide;
organic heteropentacyclic compound;
primary amino compound;
secondary alcohol;
spiro compound
anti-HIV-1 agent;
anti-HSV-1 agent;
antimalarial;
marine metabolite
00low000000
novobiocincarbamate ester;
ether;
hexoside;
hydroxycoumarin;
monocarboxylic acid amide;
monosaccharide derivative;
phenols
antibacterial agent;
antimicrobial agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
Escherichia coli metabolite;
hepatoprotective agent
00low000000
piroxicambenzothiazine;
monocarboxylic acid amide;
pyridines
analgesic;
antirheumatic drug;
cyclooxygenase 1 inhibitor;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-steroidal anti-inflammatory drug
00low000000
mobic1,3-thiazoles;
benzothiazine;
monocarboxylic acid amide
analgesic;
antirheumatic drug;
cyclooxygenase 2 inhibitor;
non-steroidal anti-inflammatory drug
00low000000
mobiflexheteroaryl hydroxy compound;
monocarboxylic acid amide;
pyridines;
thienothiazine
antipyretic;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
00low000000
isoxicambenzothiazine;
isoxazoles;
monocarboxylic acid amide
antirheumatic drug;
non-steroidal anti-inflammatory drug
00low000000
lornoxicamheteroaryl hydroxy compound;
monocarboxylic acid amide;
organochlorine compound;
pyridines;
thienothiazine
antipyretic;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
00low000000
streptolydiginbridged compound;
cyclic ketal;
enol;
monocarboxylic acid amide;
N-glycosyl compound;
organic heterobicyclic compound;
pyrrolidinone;
spiro-epoxide
antimicrobial agent;
bacterial metabolite;
EC 2.7.7.6 (RNA polymerase) inhibitor
00low000000
gsk1265744difluorobenzene;
monocarboxylic acid amide;
organic heterotricyclic compound;
secondary carboxamide
HIV-1 integrase inhibitor00low000000
3-(difluoromethyl)-N-methoxy-1-methyl-N-[1-(2,4,6-trichlorophenyl)propan-2-yl]pyrazole-4-carboxamidearomatic amide;
monocarboxylic acid amide;
organofluorine compound;
pyrazoles;
trichlorobenzene
00low000000
HG-10-102-01aminopyrimidine;
aromatic ether;
monocarboxylic acid amide;
morpholines;
organochlorine compound;
secondary amino compound
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor00low000000
bictegravirmonocarboxylic acid amide;
organic heterotetracyclic compound;
secondary carboxamide;
trifluorobenzene
HIV-1 integrase inhibitor00low000000
ver 52296aromatic amide;
isoxazoles;
monocarboxylic acid amide;
morpholines;
resorcinols
angiogenesis inhibitor;
antineoplastic agent;
Hsp90 inhibitor
00low000000
5-methoxypsoralen5-methoxyfurocoumarin;
organic heterotricyclic compound;
psoralens
hepatoprotective agent;
plant metabolite
00low000000
beta-naphthoflavoneextended flavonoid;
naphtho-gamma-pyrone;
organic heterotricyclic compound
aryl hydrocarbon receptor agonist00low000000
etodolacmonocarboxylic acid;
organic heterotricyclic compound
antipyretic;
cyclooxygenase 2 inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
00low000000
fluorescitebenzoic acids;
cyclic ketone;
hydroxy monocarboxylic acid;
organic heterotricyclic compound;
phenols;
xanthene dye
fluorescent dye;
radioopaque medium
00low000000
ketotifencyclic ketone;
olefinic compound;
organic heterotricyclic compound;
organosulfur heterocyclic compound;
piperidines;
tertiary amino compound
anti-asthmatic drug;
H1-receptor antagonist
00low000000
khellinfuranochromone;
organic heterotricyclic compound;
oxacycle
anti-asthmatic agent;
bronchodilator agent;
cardiovascular drug;
vasodilator agent
00low000000
oxolinic acidaromatic carboxylic acid;
organic heterotricyclic compound;
oxacycle;
quinolinemonocarboxylic acid;
quinolone antibiotic
antibacterial drug;
antifungal agent;
antiinfective agent;
antimicrobial agent;
enzyme inhibitor
00low000000
ro 15-4513organic heterotricyclic compound;
organonitrogen heterocyclic compound
00low000000
skimmianinealkaloid antibiotic;
organic heterotricyclic compound;
organonitrogen heterocyclic compound;
oxacycle
00low000000
benzo(b)naphtho(2,1-d)thiopheneorganic heterotricyclic compound;
organosulfur heterocyclic compound
00low000000
kokusaginineorganic heterotricyclic compound;
organonitrogen heterocyclic compound;
oxacycle
00low000000
cytisinealkaloid;
bridged compound;
lactam;
organic heterotricyclic compound;
secondary amino compound
nicotinic acetylcholine receptor agonist;
phytotoxin;
plant metabolite
00low000000
alpha-naphthoflavoneextended flavonoid;
naphtho-gamma-pyrone;
organic heterotricyclic compound
aryl hydrocarbon receptor agonist;
aryl hydrocarbon receptor antagonist;
EC 1.14.14.14 (aromatase) inhibitor
00low000000
naftalofosorganic heterotricyclic compoundanthelminthic drug00low000000
helenalincyclic ketone;
gamma-lactone;
organic heterotricyclic compound;
secondary alcohol;
sesquiterpene lactone
anti-inflammatory agent;
antineoplastic agent;
metabolite;
plant metabolite
00low000000
ancitabinediol;
organic heterotricyclic compound
antimetabolite;
antineoplastic agent;
prodrug
00low000000
1-(3-chloro-5-benzo[b][1]benzoxepinyl)-4-methylpiperazineN-alkylpiperazine;
organic heterotricyclic compound
00low000000
colforsinacetate ester;
cyclic ketone;
labdane diterpenoid;
organic heterotricyclic compound;
tertiary alpha-hydroxy ketone;
triol
adenylate cyclase agonist;
anti-HIV agent;
antihypertensive agent;
plant metabolite;
platelet aggregation inhibitor;
protein kinase A agonist
00low000000
nedocromildicarboxylic acid;
organic heterotricyclic compound
anti-allergic agent;
anti-asthmatic drug;
non-steroidal anti-inflammatory drug
00low000000
naxagolideorganic heterotricyclic compound;
phenols;
tertiary amino compound
anticonvulsant;
antiparkinson drug;
dopamine agonist
00low000000
depsidonedepsidones;
organic heterotricyclic compound
00low000000
droxicamorganic heterotricyclic compound;
pyridines
cyclooxygenase 1 inhibitor;
hepatotoxic agent;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
platelet aggregation inhibitor;
prodrug
00low000000
dictamninealkaloid antibiotic;
organic heterotricyclic compound;
organonitrogen heterocyclic compound;
oxacycle
00low000000
flindersiamineorganic heterotricyclic compound;
organonitrogen heterocyclic compound;
oxacycle
00low000000
flindersineorganic heterotricyclic compound;
organonitrogen heterocyclic compound;
oxacycle
00low000000
maculineorganic heterotricyclic compound;
organonitrogen heterocyclic compound;
oxacycle
00low000000
zaluzanin Cgamma-lactone;
guaiane sesquiterpenoid;
organic heterotricyclic compound;
secondary alcohol;
sesquiterpene lactone
EC 1.14.13.39 (nitric oxide synthase) inhibitor;
metabolite
00low000000
alpha-lapachoneorganic heterotricyclic compound;
organooxygen compound
00low000000
dehydrocostus lactonegamma-lactone;
guaiane sesquiterpenoid;
organic heterotricyclic compound;
sesquiterpene lactone
antimycobacterial drug;
antineoplastic agent;
apoptosis inducer;
cyclooxygenase 2 inhibitor;
metabolite;
trypanocidal drug
00low000000
Evoxineorganic heterotricyclic compound;
organonitrogen heterocyclic compound;
oxacycle
00low000000
galaxolideisochromenes;
organic heterotricyclic compound
fragrance00low000000
aurofusarinorganic heterotricyclic compound;
organooxygen compound
00low000000
geographutoxin iorganic heterotricyclic compoundmarine metabolite00low000000
gamma-fagarineorganic heterotricyclic compound;
organonitrogen heterocyclic compound;
oxacycle
00low000000
1,9-dideoxyforskolinacetate ester;
labdane diterpenoid;
organic heterotricyclic compound
plant metabolite00low000000
paspalineorganic heterotricyclic compound;
organooxygen compound
00low000000
salvinorin aorganic heterotricyclic compound;
organooxygen compound
metabolite;
oneirogen
00low000000
sch 45752organic heterotricyclic compound;
organooxygen compound
00low000000
pannarinaldehyde;
aromatic ether;
depsidones;
organic heterotricyclic compound;
organochlorine compound;
phenols
antimicrobial agent;
antineoplastic agent;
apoptosis inducer;
lichen metabolite
00low000000
mirestrolorganic heterotricyclic compound;
organooxygen compound
00low000000
confertincyclic ketone;
gamma-lactone;
organic heterotricyclic compound;
pseudoguaianolide
anti-inflammatory agent;
metabolite;
plant metabolite
00low000000
inuviscolidegamma-lactone;
organic heterotricyclic compound;
sesquiterpene lactone;
tertiary alcohol
anti-inflammatory agent;
plant metabolite
00low000000
ergolideacetate ester;
cyclic ketone;
gamma-lactone;
organic heterotricyclic compound;
sesquiterpene lactone
anti-inflammatory agent;
antineoplastic agent;
metabolite;
NF-kappaB inhibitor;
plant metabolite
00low000000
fk 1052imidazoles;
organic heterotricyclic compound
antiemetic;
serotonergic antagonist
00low000000
noscapinearomatic ether;
benzylisoquinoline alkaloid;
cyclic acetal;
isobenzofuranone;
organic heterobicyclic compound;
organic heterotricyclic compound;
tertiary amino compound
antineoplastic agent;
antitussive;
apoptosis inducer;
plant metabolite
00low000000
aromaticincyclic ketone;
gamma-lactone;
organic heterotricyclic compound;
sesquiterpene lactone
anti-inflammatory agent;
metabolite;
plant metabolite
00low000000
aglafolinemethyl ester;
organic heterotricyclic compound
metabolite;
platelet aggregation inhibitor
00low000000
cimifuginorganic heterotricyclic compound;
oxacycle
00low000000
khellosideorganic heterotricyclic compound;
oxacycle
00low000000
columbinorganic heterotricyclic compound;
organooxygen compound
00low000000
decursinolcyclic ether;
delta-lactone;
organic heterotricyclic compound;
secondary alcohol
analgesic;
antineoplastic agent;
EC 3.1.1.7 (acetylcholinesterase) inhibitor;
metabolite
00low000000
cleomiscosin aaromatic ether;
delta-lactone;
organic heterotricyclic compound;
phenols;
primary alcohol
anti-inflammatory agent;
metabolite
00low000000
Dubinidineorganic heterotricyclic compound;
organonitrogen heterocyclic compound;
oxacycle
00low000000
colforsin daropateacetate ester;
carboxylic ester;
cyclic ketone;
diol;
organic heterotricyclic compound;
tertiary amino compound
adenylate cyclase agonist;
antihypertensive agent;
cardiotonic drug;
vasodilator agent
00low000000
thapsigarginbutyrate ester;
organic heterotricyclic compound;
sesquiterpene lactone
calcium channel blocker;
EC 3.6.3.8 (Ca(2+)-transporting ATPase) inhibitor
00low000000
reynosinorganic heterotricyclic compound;
sesquiterpene lactone
metabolite00low000000
5',7'-dimethylspiro[cyclohexane-1,3'-pyrimido[5,4-c][1,2,5]oxadiazine]-6',8'-dioneorganic heterotricyclic compound;
spiro compound
00low000000
vedelianincyclic ether;
organic heterotricyclic compound;
resorcinols;
stilbenoid
antineoplastic agent;
plant metabolite
00low000000
haplamineorganic heterotricyclic compound;
organonitrogen heterocyclic compound;
oxacycle
00low000000
(2R)-1-[(4,8-dimethoxy-7-furo[2,3-b]quinolinyl)oxy]-3-methylbutane-2,3-diolorganic heterotricyclic compound;
organonitrogen heterocyclic compound;
oxacycle
00low000000
acetic acid (11-oxo-6H-benzo[c][1]benzoxepin-2-yl) esterorganic heterotricyclic compound00low000000
2-oxo-3-benzo[h][1]benzopyrancarboxylic acid ethyl esterorganic heterotricyclic compound;
organooxygen compound
00low000000
huperzine aorganic heterotricyclic compound;
primary amino compound;
pyridone;
sesquiterpene alkaloid
EC 3.1.1.7 (acetylcholinesterase) inhibitor;
neuroprotective agent;
nootropic agent;
plant metabolite
00low000000
CHIC-35aromatic compound;
organic heterotricyclic compound;
organochlorine compound;
primary carboxamide
EC 3.5.1.98 (histone deacetylase) inhibitor00low000000
3-imino-2-benzo[f][1]benzopyrancarbothioamideorganic heterotricyclic compound;
organooxygen compound
00low000000
2-benzamido-4,5-dihydrobenzo[g][1]benzothiole-3-carboxamideorganic heterotricyclic compound;
organosulfur heterocyclic compound
00low000000
3-(3-oxo-2-benzo[f][1]benzopyranyl)-1-phenyl-4-pyrazolecarboxaldehydeorganic heterotricyclic compound;
organooxygen compound
00low000000
2-benzo[b][1]benzoxepinamineorganic heterotricyclic compound00low000000
LSM-33589organic heterotricyclic compound;
organosulfur heterocyclic compound
00low000000
2-(difluoromethyl)-4-benzo[h][1]benzopyranoneorganic heterotricyclic compound;
organooxygen compound
00low000000
bigelovinacetate ester;
cyclic ketone;
gamma-lactone;
organic heterotricyclic compound;
sesquiterpene lactone
antineoplastic agent;
apoptosis inducer;
immunomodulator;
plant metabolite
00low000000
momilactone borganic heterotricyclic compound;
organooxygen compound
00low000000
quinagolideorganic heterotricyclic compound;
organonitrogen heterocyclic compound
00low000000
6,8-difluoro-4-(pyridin-3-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolineorganic heterotricyclic compound;
organofluorine compound;
pyridines;
secondary amino compound
00low000000
uccf-029organic heterotricyclic compound;
organooxygen compound
00low000000
4-[oxo-(4-oxo-5H-thieno[3,2-c]quinolin-2-yl)methyl]-1-piperazinecarboxylic acid ethyl esterorganic heterotricyclic compound;
organonitrogen heterocyclic compound;
organosulfur heterocyclic compound
00low000000
[4-(1,3-benzodioxol-5-ylmethyl)-1-piperazinyl]-(7-methoxy-2-furo[2,3-b]quinolinyl)methanoneorganic heterotricyclic compound;
organonitrogen heterocyclic compound;
oxacycle
00low000000
1-[(6-methoxy-2-furo[2,3-b]quinolinyl)-oxomethyl]-4-piperidinecarboxylic acid ethyl esterorganic heterotricyclic compound;
organonitrogen heterocyclic compound;
oxacycle
00low000000
N-[2-(dipropylamino)ethyl]-4-methyl-2-furo[3,2-c]quinolinecarboxamideorganic heterotricyclic compound;
organonitrogen heterocyclic compound;
oxacycle
00low000000
6-methoxy-N-(thiophen-2-ylmethyl)-2-furo[2,3-b]quinolinecarboxamideorganic heterotricyclic compound;
organonitrogen heterocyclic compound;
oxacycle
00low000000
LSM-1924organic heterotricyclic compound;
organooxygen compound
00low000000
LSM-22738organic heterotricyclic compound;
organooxygen compound
00low000000
7-methoxy-N-(3-pyridinylmethyl)-2-furo[2,3-b]quinolinecarboxamideorganic heterotricyclic compound;
organonitrogen heterocyclic compound;
oxacycle
00low000000
LSM-26445organic heterotricyclic compound;
organooxygen compound
00low000000
LSM-1925organic heterotricyclic compound;
organooxygen compound
00low000000
acetic acid [1-[(4,8-dimethoxy-7-furo[2,3-b]quinolinyl)oxy]-3-hydroxy-3-methylbutan-2-yl] esterorganic heterotricyclic compound;
organonitrogen heterocyclic compound;
oxacycle
00low000000
LSM-25964organic heterotricyclic compound;
organooxygen compound
00low000000
N-(3-oxo-2-benzo[f][1]benzopyranyl)acetamideorganic heterotricyclic compound;
organooxygen compound
00low000000
chanoclavinebenzoindole;
ergot alkaloid;
organic heterotricyclic compound;
primary alcohol;
secondary amino compound
00low000000
riddelliinemacrodiolide;
olefinic compound;
organic heterotricyclic compound;
pyrrolizine alkaloid
carcinogenic agent;
genotoxin;
mutagen
00low000000
irilonehydroxyisoflavone;
organic heterotricyclic compound;
oxacycle
antineoplastic agent;
immunomodulator;
metabolite
00low000000
heliparvifolineorganic heterotricyclic compound;
organonitrogen heterocyclic compound;
oxacycle
00low000000
sirolimusantibiotic antifungal drug;
cyclic acetal;
cyclic ketone;
ether;
macrolide lactam;
organic heterotricyclic compound;
secondary alcohol
antibacterial drug;
anticoronaviral agent;
antineoplastic agent;
bacterial metabolite;
geroprotector;
immunosuppressive agent;
mTOR inhibitor
00low000000
5-ethyl-4-oxo-N-(thiophen-2-ylmethyl)-2-thieno[3,2-c]quinolinecarboxamideorganic heterotricyclic compound;
organonitrogen heterocyclic compound;
organosulfur heterocyclic compound
00low000000
8-methyl-1-[2-(2-methyl-1-piperidinyl)-2-oxoethyl]-4-[1]benzopyrano[4,3-c]pyrazoloneorganic heterotricyclic compound00low000000
cytochalasin bcytochalasin;
lactam;
lactone;
organic heterotricyclic compound
actin polymerisation inhibitor;
metabolite;
mycotoxin;
platelet aggregation inhibitor
00low000000
(3r)-((2,3-dihydro-5-methyl-3-((4-morpholinyl)methyl)pyrrolo-(1,2,3-de)-1,4-benzoxazin-6-yl)(1-naphthalenyl))methanonemorpholines;
naphthyl ketone;
organic heterotricyclic compound;
synthetic cannabinoid
analgesic;
apoptosis inhibitor;
neuroprotective agent
00low000000
methyl brevifolincarboxylatecyclic ketone;
delta-lactone;
organic heterotricyclic compound;
phenols
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
metabolite;
platelet aggregation inhibitor;
radical scavenger;
vasodilator agent
00low000000
palonosetronazabicycloalkane;
delta-lactam;
organic heterotricyclic compound
antiemetic;
serotonergic antagonist
00low000000
himbacinegamma-lactone;
organic heterotricyclic compound;
piperidine alkaloid
muscarinic antagonist00low000000
riddelliine n-oxidediol;
macrocyclic lactone;
olefinic compound;
organic heterotricyclic compound;
primary alcohol;
pyrrolizine alkaloid;
tertiary alcohol;
tertiary amine oxide
carcinogenic agent;
genotoxin;
human xenobiotic metabolite;
Jacobaea metabolite;
mutagen;
rat metabolite
00low000000
chaetoviridin aazaphilone;
beta-hydroxy ketone;
enone;
gamma-lactone;
organic heterotricyclic compound;
organochlorine compound;
secondary alcohol
antifungal agent;
Chaetomium metabolite
00low000000
tremortin aorganic heterotricyclic compound;
organooxygen compound
00low000000
4-methyl-N-[(4-methylphenyl)methyl]-2-furo[3,2-c]quinolinecarboxamideorganic heterotricyclic compound;
organonitrogen heterocyclic compound;
oxacycle
00low000000
beraprostenyne;
monocarboxylic acid;
organic heterotricyclic compound;
secondary alcohol;
secondary allylic alcohol
anti-inflammatory agent;
antihypertensive agent;
platelet aggregation inhibitor;
prostaglandin receptor agonist;
vasodilator agent
00low000000
jwh-133benzochromene;
dibenzopyran;
organic heterotricyclic compound
analgesic;
anti-inflammatory agent;
antineoplastic agent;
apoptosis inhibitor;
CB2 receptor agonist;
opioid analgesic;
vasodilator agent
00low000000
nu 7026organic heterotricyclic compound;
organooxygen compound
00low000000
pi103aromatic amine;
morpholines;
organic heterotricyclic compound;
phenols;
tertiary amino compound
antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
mTOR inhibitor
00low000000
terpendole eorganic heterotricyclic compound;
organooxygen compound
00low000000
epicoccononeorganic heterotricyclic compoundfluorochrome00low000000
pentalenolactone falpha,beta-unsaturated monocarboxylic acid;
organic heterotricyclic compound;
sesquiterpene lactone;
spiro-epoxide
bacterial metabolite00low000000
jnj16259685organic heterotricyclic compound;
organonitrogen heterocyclic compound;
oxacycle
00low000000
episilvestroldioxanes;
ether;
methyl ester;
organic heterotricyclic compound
antineoplastic agent;
metabolite
00low000000
silvestroldioxanes;
ether;
methyl ester;
organic heterotricyclic compound
antineoplastic agent;
metabolite
00low000000
4-chloro-N-(3,4-dimethoxyphenyl)-2-thieno[3,2-c]quinolinecarboxamideorganic heterotricyclic compound;
organonitrogen heterocyclic compound;
organosulfur heterocyclic compound
00low000000
monascinalpha,beta-unsaturated ketone;
gamma-lactone;
organic heterotricyclic compound;
polyketide
antilipemic drug;
antineoplastic agent;
fungal metabolite;
PPARgamma agonist
00low000000
batzelladine aalkaloid;
carboxylic ester;
guanidines;
organic heterotricyclic compound;
pyrrolopyrimidine;
triazaacenaphthylene
anti-HIV-1 agent;
metabolite
00low000000
prim-o-glucosylcimifuginorganic heterotricyclic compound;
oxacycle
00low000000
4-chloro-N-[3-(3-methyl-1-piperidinyl)propyl]-2-thieno[3,2-c]quinolinecarboxamideorganic heterotricyclic compound;
organonitrogen heterocyclic compound;
organosulfur heterocyclic compound
00low000000
schweinfurthin gcyclic ether;
organic heterotricyclic compound;
resorcinols;
stilbenoid
antineoplastic agent;
metabolite
00low000000
8-methyl-4-oxo-N-[3-(4-propyl-1-piperazinyl)propyl]-5H-thieno[3,2-c]quinoline-2-carboxamideorganic heterotricyclic compound;
organonitrogen heterocyclic compound;
organosulfur heterocyclic compound
00low000000
N,8-dimethyl-N-(3-methylphenyl)-4-oxo-5H-thieno[3,2-c]quinoline-2-carboxamideorganic heterotricyclic compound;
organonitrogen heterocyclic compound;
organosulfur heterocyclic compound
00low000000
N-[2-(dipropylamino)ethyl]-5-ethyl-4-oxo-2-thieno[3,2-c]quinolinecarboxamideorganic heterotricyclic compound;
organonitrogen heterocyclic compound;
organosulfur heterocyclic compound
00low000000
schweinfurthin fcyclic ether;
organic heterotricyclic compound;
resorcinols;
stilbenoid
metabolite00low000000
thallusinorganic heterotricyclic compound;
organooxygen compound
00low000000
aflatremorganic heterotricyclic compound;
organooxygen compound
00low000000
dihydroagarofuranbridged compound;
cyclic ether;
eudesmane sesquiterpenoid;
organic heterotricyclic compound
metabolite00low000000
4'-epichaetoviridin Aazaphilone;
beta-hydroxy ketone;
enone;
gamma-lactone;
organic heterotricyclic compound;
organochlorine compound;
secondary alcohol
Chaetomium metabolite00low000000
arenaemycin ealpha,beta-unsaturated monocarboxylic acid;
organic heterotricyclic compound;
sesquiterpene lactone;
spiro-epoxide
antimicrobial agent;
bacterial metabolite;
EC 1.2.1.12 [glyceraldehyde-3-phosphate dehydrogenase (phosphorylating)] inhibitor
00low000000
mk 2206organic heterotricyclic compoundEC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor00low000000
chaetoviridin Eazaphilone;
enone;
gamma-lactone;
organic heterotricyclic compound;
organochlorine compound
Chaetomium metabolite00low000000
LSM-1873organic heterotricyclic compound;
organooxygen compound
00low000000
LSM-1834organic heterotricyclic compound;
organooxygen compound
00low000000
LSM-1287organic heterotricyclic compound;
organooxygen compound
00low000000
LSM-1675organic heterotricyclic compound;
organooxygen compound
00low000000
LSM-1312organic heterotricyclic compound;
organooxygen compound
00low000000
LSM-1315organic heterotricyclic compound;
organooxygen compound
00low000000
debromoaplysiatoxinaplysiatoxins;
cyclic hemiketal;
ether;
organic heterotricyclic compound;
phenols;
secondary alcohol;
spiroketal
algal metabolite;
carcinogenic agent;
cyanotoxin;
marine metabolite;
protein kinase C agonist
00low000000
aplysiatoxinaplysiatoxins;
bromophenol;
cyclic hemiketal;
ether;
organic heterotricyclic compound;
secondary alcohol;
spiroketal
algal metabolite;
carcinogenic agent;
cyanotoxin;
marine metabolite;
protein kinase C agonist
00low000000
gonyautoxin vorganic heterotricyclic compound;
paralytic shellfish toxin
marine metabolite00low000000
4-hydroxy-6-propan-2-ylpyrano[3,2-c]quinoline-2,5-dioneorganic heterotricyclic compound;
organonitrogen heterocyclic compound;
oxacycle
00low000000
pelabresibmonochlorobenzenes;
organic heterotricyclic compound;
primary carboxamide
antineoplastic agent;
bromodomain-containing protein 4 inhibitor
00low000000
gonyautoxin iiorganic heterotricyclic compound;
paralytic shellfish toxin
marine metabolite00low000000
8-epidiosbulbin e acetateorganic heterotricyclic compound;
organooxygen compound
00low000000
conocurvoneorganic heterotricyclic compound;
organooxygen compound
00low000000
scytoneminenone;
organic heterotricyclic compound;
organonitrogen heterocyclic compound;
polyphenol;
ring assembly
bacterial metabolite;
biological pigment;
ultraviolet filter
00low000000
liproxstatin-1azaspiro compound;
monochlorobenzenes;
organic heterotricyclic compound;
secondary amino compound
antioxidant;
cardioprotective agent;
ferroptosis inhibitor;
radical scavenger
00low000000
butoctamide succinatedicarboxylic acid monoester;
hemisuccinate;
secondary carboxamide
00low000000
cl 387785bromobenzenes;
quinazolines;
secondary carboxamide;
ynamide
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
epidermal growth factor receptor antagonist
00low000000
iodipamidebenzoic acids;
organoiodine compound;
secondary carboxamide
radioopaque medium00low000000
4-(dimethylamino)-n-(7-(hydroxyamino)-7-oxoheptyl)benzamidebenzamides;
hydroxamic acid;
secondary carboxamide;
tertiary amino compound
antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor
00low000000
nemonapridebenzamides;
monochlorobenzenes;
monomethoxybenzene;
N-alkylpyrrolidine;
secondary amino compound;
secondary carboxamide;
substituted aniline
00low000000
niclosamidebenzamides;
C-nitro compound;
monochlorobenzenes;
salicylanilides;
secondary carboxamide
anthelminthic drug;
anticoronaviral agent;
antiparasitic agent;
apoptosis inducer;
molluscicide;
piscicide;
STAT3 inhibitor
00low000000
pd168393acrylamides;
bromobenzenes;
quinazolines;
secondary carboxamide;
substituted aniline
epidermal growth factor receptor antagonist00low000000
pilsicainideorganic heterobicyclic compound;
secondary carboxamide
anti-arrhythmia drug;
sodium channel blocker
00low000000
pj-34phenanthridines;
secondary carboxamide;
tertiary amino compound
angiogenesis inhibitor;
anti-inflammatory agent;
antiatherosclerotic agent;
antineoplastic agent;
apoptosis inducer;
cardioprotective agent;
EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor;
neuroprotective agent
00low000000
opc 12759secondary carboxamide00low000000
suraminnaphthalenesulfonic acid;
phenylureas;
secondary carboxamide
angiogenesis inhibitor;
antinematodal drug;
antineoplastic agent;
apoptosis inhibitor;
EC 2.7.11.13 (protein kinase C) inhibitor;
GABA antagonist;
GABA-gated chloride channel antagonist;
purinergic receptor P2 antagonist;
ryanodine receptor agonist;
trypanocidal drug
00low000000
2-[[3-(3,4-dimethoxyphenyl)-1-oxoprop-2-enyl]amino]benzoic acidamidobenzoic acid;
cinnamamides;
secondary carboxamide
00low000000
acedapsoneacetamides;
anilide;
secondary carboxamide;
sulfone
antimalarial;
antimicrobial drug
00low000000
salicylurateN-acylglycine;
secondary carboxamide
human xenobiotic metabolite;
uremic toxin
00low000000
monoacetyldapsoneacetamides;
anilide;
secondary carboxamide;
sulfone
00low000000
n-methylolacrylamidesecondary carboxamide00low000000
win 18446organochlorine compound;
secondary carboxamide
EC 1.2.1.3 [aldehyde dehydrogenase (NAD(+))] inhibitor00low000000
carboxinanilide fungicide;
anilide;
enamide;
organosulfur heterocyclic compound;
oxacycle;
secondary carboxamide
antifungal agrochemical;
EC 1.3.5.1 [succinate dehydrogenase (quinone)] inhibitor
00low000000
tromantadinesecondary carboxamide00low000000
aureothricindithiolopyrrolone antibiotic;
secondary carboxamide
angiogenesis inhibitor;
antibacterial agent;
bacterial metabolite;
EC 2.7.7.6 (RNA polymerase) inhibitor
00low000000
morphazinamidemorpholines;
pyrazines;
secondary carboxamide
00low000000
amperozidediarylmethane;
monofluorobenzenes;
N-alkylpiperazine;
secondary carboxamide;
ureas
anxiolytic drug;
dopamine uptake inhibitor;
geroprotector;
second generation antipsychotic;
serotonergic antagonist
00low000000
n-acetyltryptophanamideacetamides;
L-tryptophan derivative;
primary carboxamide;
secondary carboxamide
00low000000
gamma-glutamyltyrosinedicarboxylic acid;
dipeptide;
phenols;
primary amino compound;
secondary carboxamide
human metabolite00low000000
n-acetyldopamineacetamides;
catechols;
N-(fatty acyl)-dopamine;
secondary carboxamide
human urinary metabolite;
marine metabolite
00low000000
n-acetylcytidineacetamides;
cytidines;
secondary carboxamide
metabolite00low000000
florfenicolorganochlorine compound;
organofluorine compound;
secondary alcohol;
secondary carboxamide;
sulfone
antimicrobial agent00low000000
marimastathydroxamic acid;
secondary carboxamide
antineoplastic agent;
matrix metalloproteinase inhibitor
00low000000
n-(3-oxohexanoyl)-3-aminodihydro-2(3h)-furanoneN-acyl homoserine lactone;
secondary carboxamide
00low000000
mosapridearomatic ether;
benzamides;
monochlorobenzenes;
monofluorobenzenes;
morpholines;
secondary carboxamide;
substituted aniline;
tertiary amino compound
00low000000
benzyloxycarbonylphenylalanylphenylalanine diazomethyl ketonecarboxylic ester;
diazo compound;
L-phenylalanine derivative;
secondary carboxamide
cathepsin L (EC 3.4.22.15) inhibitor00low000000
yh 439aromatic amide;
isopropyl ester;
secondary carboxamide
00low000000
cyc 682nitrile;
nucleoside analogue;
secondary carboxamide
antimetabolite;
antineoplastic agent;
DNA synthesis inhibitor;
prodrug
00low000000
sceptrinpyrroles;
secondary carboxamide
00low000000
n(beta)-alanyldopaminecatechols;
primary amino compound;
secondary carboxamide
00low000000
monoacetylcadaverineacetamides;
N-substituted cadaverine;
primary amino compound;
secondary carboxamide
human metabolite00low000000
N-(1-phenylethyl)acetamideacetamides;
secondary carboxamide
00low000000
2,2,2-trifluoro-N-[2-(1H-indol-3-yl)ethyl]acetamideindoles;
secondary carboxamide;
trifluoroacetamide
00low000000
xv 6381,3-thiazoles;
benzamides;
diazepanone;
diol;
secondary alcohol;
secondary carboxamide;
ureas
HIV protease inhibitor00low000000
vibriobactin1,3-oxazoles;
secondary carboxamide
siderophore00low000000
bms 195614benzoic acids;
quinolines;
secondary carboxamide
retinoic acid receptor alpha antagonist00low000000
tempaceaminoxyls;
piperidinecarboxamide;
secondary carboxamide
radiation protective agent;
radical scavenger
00low000000
dimethyloxalylglycineglycine derivative;
methyl ester;
secondary carboxamide
EC 1.14.11.29 (hypoxia-inducible factor-proline dioxygenase) inhibitor;
neuroprotective agent
00low000000
s 1033(trifluoromethyl)benzenes;
imidazoles;
pyridines;
pyrimidines;
secondary amino compound;
secondary carboxamide
anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor
00low000000
3-methyl-2-[[oxo-(4-pentoxyphenyl)methyl]amino]butanoic acidsecondary carboxamide00low000000
cinromidecinnamamides;
secondary carboxamide
00low000000
4-[[2-furanyl(oxo)methyl]amino]benzoic acid propan-2-yl esteraromatic amide;
furans;
isopropyl ester;
secondary carboxamide
00low000000
2,2,2-trifluoro-N-(2-methyl-8-quinolinyl)acetamidequinolines;
secondary carboxamide;
trifluoroacetamide
00low000000
N-(3-carbamoyl-4,5,6,7-tetrahydro-1-benzothiophen-2-yl)-2-pyrazinecarboxamideprimary carboxamide;
pyrazines;
secondary carboxamide
00low000000
2-[[oxo(thiophen-2-yl)methyl]amino]-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxylic acid propan-2-yl esteraromatic amide;
isopropyl ester;
secondary carboxamide;
thiophenes
00low000000
N-[1-[(4-chlorophenyl)methyl]-4-pyrazolyl]-2-pyrazinecarboxamidepyrazines;
secondary carboxamide
00low000000
4-[[(4-bromo-2-ethyl-3-pyrazolyl)-oxomethyl]amino]benzoic acid propan-2-yl esteraromatic amide;
isopropyl ester;
secondary carboxamide
00low000000
(2S)-2-[[(2-chlorophenyl)-oxomethyl]amino]-3-methylbutanoic acid (6-nitro-4H-1,3-benzodioxin-8-yl)methyl estersecondary carboxamide00low000000
N-[(2S)-1-(1H-benzimidazol-2-ylamino)-3-methyl-1-oxobutan-2-yl]-3,5-dimethoxybenzamidesecondary carboxamide00low000000
2-(2,4-dioxo-1H-pyrimidin-6-yl)-N-[2-(4-morpholinyl)ethyl]acetamidemorpholines;
pyrimidone;
secondary carboxamide;
tertiary amino compound
00low000000
N-[(4-chlorophenyl)methyl]-2-(2,4-dioxo-1H-pyrimidin-6-yl)acetamidemonochlorobenzenes;
pyrimidone;
secondary carboxamide
00low000000
N-[(2S)-1-(1H-benzimidazol-2-ylamino)-3-methyl-1-oxobutan-2-yl]-3-methylbenzamidesecondary carboxamide00low000000
2,2,2-trifluoro-N-(5-oxo-1-phenyl-4H-pyrazol-3-yl)acetamidepyrazoles;
secondary carboxamide;
trifluoroacetamide
00low000000
N-(2-anilino-2-oxoethyl)-2-methoxybenzamidesecondary carboxamide00low000000
N-[5-[(2,6-dichlorophenyl)methylthio]-1,3,4-thiadiazol-2-yl]-5-methyl-2-pyrazinecarboxamidepyrazines;
secondary carboxamide
00low000000
(2S)-3-methyl-2-[[(3-methylphenyl)-oxomethyl]amino]butanoic acid (4-oxo-2-pyrimido[2,1-b][1,3]benzothiazolyl)methyl estersecondary carboxamide00low000000
n-(1-oxyl-2,2,6,6-tetramethyl-4-piperidinyl)iodoacetamideaminoxyls;
organoiodine compound;
piperidinecarboxamide;
secondary carboxamide
radical scavenger;
spin label
00low000000
ANA-121-benzothiophenes;
caprolactams;
secondary carboxamide
antidepressant;
anxiolytic drug;
tropomyosin-related kinase B receptor antagonist
00low000000
N-([biphenyl]-2-yl)-3-cyclopentylpropanamidebiphenyls;
cyclopentanes;
secondary carboxamide
00low000000
bms 3870321,3-oxazoles;
1,3-thiazoles;
organic sulfide;
piperidinecarboxamide;
secondary carboxamide
angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor
00low000000
sr 144528bridged compound;
monochlorobenzenes;
pyrazoles;
secondary carboxamide
CB2 receptor antagonist;
EC 2.3.1.26 (sterol O-acyltransferase) inhibitor
00low000000
N-(1,3-benzodioxol-5-ylmethyl)-N-[2-(cyclohexylamino)-2-oxo-1-pyridin-4-ylethyl]-2,2,2-trifluoroacetamidebenzodioxoles;
pyridines;
secondary carboxamide;
tertiary carboxamide;
trifluoroacetamide
00low000000
N-[2-(cyclohexylamino)-2-oxo-1-thiophen-2-ylethyl]-2,2,2-trifluoro-N-(4-methylphenyl)acetamidesecondary carboxamide;
tertiary carboxamide;
thiophenes;
trifluoroacetamide
00low000000
ML162monochlorobenzenes;
monomethoxybenzene;
organochlorine compound;
secondary carboxamide;
tertiary carboxamide;
thiophenes
EC 1.11.1.9 (glutathione peroxidase) inhibitor;
ferroptosis inducer
00low000000
N-[3-(N-(2-chloro-1-oxoethyl)-4-nitroanilino)propyl]-2,2,2-trifluoroacetamideC-nitro compound;
secondary carboxamide;
tertiary carboxamide;
trifluoroacetamide
00low000000
2-[[2-(3,4-dimethoxyanilino)-2-oxoethyl]thio]-3-pyridinecarboxylic acid propan-2-yl esterdimethoxybenzene;
isopropyl ester;
secondary carboxamide
00low000000
fagaramidecinnamamides;
secondary carboxamide
00low000000
arachidonyl dopaminecatechols;
fatty amide;
N-(fatty acyl)-dopamine;
secondary carboxamide
00low000000
n-oleoyldopaminecatechols;
fatty amide;
N-(fatty acyl)-dopamine;
secondary carboxamide
TRPV1 agonist00low000000
tranilastamidobenzoic acid;
cinnamamides;
dimethoxybenzene;
secondary carboxamide
anti-allergic agent;
anti-asthmatic drug;
antineoplastic agent;
aryl hydrocarbon receptor agonist;
calcium channel blocker;
hepatoprotective agent;
nephroprotective agent
00low000000
arachidonyl-2-chloroethylamidefatty amide;
organochlorine compound;
secondary carboxamide;
synthetic cannabinoid
CB1 receptor agonist;
CB2 receptor agonist;
neuroprotective agent
00low000000
l796778benzenes;
C-nitro compound;
L-lysine derivative;
L-phenylalanine derivative;
methyl ester;
oligopeptide;
secondary carboxamide;
ureas
somatostatin receptor agonist00low000000
l803087benzenes;
fluoroindole;
guanidines;
L-arginine derivative;
methyl ester;
phenylindole;
secondary carboxamide
somatostatin receptor agonist00low000000
n-cinnamoyltyraminecinnamamides;
phenols;
secondary carboxamide
allelochemical;
antimicrobial agent;
phytoalexin;
platelet aggregation inhibitor
00low000000
4-amylcinnamoylanthranilic acidamidobenzoic acid;
cinnamamides;
secondary carboxamide
EC 3.1.1.4 (phospholipase A2) inhibitor;
TRP channel blocker
00low000000
batimastathydroxamic acid;
L-phenylalanine derivative;
organic sulfide;
secondary carboxamide;
thiophenes;
triamide
angiogenesis inhibitor;
antineoplastic agent;
matrix metalloproteinase inhibitor
00low000000
pipercallosidinealkaloid;
benzodioxoles;
enamide;
secondary carboxamide
apoptosis inducer;
metabolite;
plant metabolite
00low000000
pederincyclic ketal;
diol;
oxanes;
polyketide;
secondary alcohol;
secondary carboxamide
antimitotic;
antineoplastic agent;
bacterial metabolite;
vesicant
00low000000
streptogramin a1,3-oxazoles;
cyclic ketone;
enamide;
lactam;
macrolide antibiotic;
macrolide;
pyrroline;
secondary alcohol;
secondary carboxamide;
tertiary carboxamide
antibacterial drug;
Mycoplasma genitalium metabolite
00low000000
cinanserinaryl sulfide;
cinnamamides;
secondary carboxamide;
tertiary amino compound
anticoronaviral agent;
antiviral agent;
EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor
00low000000
pepstatinpentapeptide;
secondary carboxamide
bacterial metabolite;
EC 3.4.23.* (aspartic endopeptidase) inhibitor
00low000000
ximelagatranamidoxime;
azetidines;
carboxamide;
ethyl ester;
hydroxylamines;
secondary amino compound;
secondary carboxamide;
tertiary carboxamide
anticoagulant;
EC 3.4.21.5 (thrombin) inhibitor;
prodrug;
serine protease inhibitor
00low000000
(6R,7R)-7-[[(2R)-2-carboxy-2-(4-hydroxyphenyl)-1-oxoethyl]amino]-7-methoxy-3-[[(1-methyl-5-tetrazolyl)thio]methyl]-8-oxo-5-oxa-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic aciddicarboxylic acid;
secondary carboxamide
00low000000
salubrinalaminal;
organochlorine compound;
quinolines;
secondary carboxamide;
thioureas
00low000000
DPI2benzenes;
morpholines;
secondary carboxamide;
tertiary amino compound;
thiazolidinone
ferroptosis inducer00low000000
n-feruloylserotoninaromatic ether;
cinnamamides;
hydroxyindoles;
phenols;
secondary carboxamide
plant metabolite00low000000
oroidinpyrroles;
secondary carboxamide
metabolite00low000000
ro 42-5892cyclopropanes;
diol;
L-histidine derivative;
secondary carboxamide;
sulfone
antihypertensive agent;
EC 3.4.23.15 (renin) inhibitor;
peptidomimetic;
vasodilator agent
00low000000
s 10061,3-thiazoles;
carbamate ester;
carboxylic acid;
cephalosporin;
enamide;
secondary carboxamide
antibacterial drug00low000000
manumycinenamide;
epoxide;
organic heterobicyclic compound;
polyketide;
secondary carboxamide;
tertiary alcohol
antiatherosclerotic agent;
antimicrobial agent;
antineoplastic agent;
apoptosis inducer;
bacterial metabolite;
EC 1.8.1.9 (thioredoxin reductase) inhibitor;
EC 2.5.1.58 (protein farnesyltransferase) inhibitor;
marine metabolite
00low000000
asukamycinenamide;
epoxide;
organic heterobicyclic compound;
polyketide;
secondary carboxamide;
tertiary alcohol
antibacterial agent;
antifungal agent;
antimicrobial agent;
antineoplastic agent;
bacterial metabolite
00low000000
kalimantacin aalpha,beta-unsaturated monocarboxylic acid;
carbamate ester;
fatty acid derivative;
secondary carboxamide
antibacterial agent;
antimicrobial agent;
bacterial metabolite
00low000000
l 744832benzenes;
ether;
isopropyl ester;
secondary carboxamide;
sulfone;
thiol
antineoplastic agent;
EC 2.5.1.58 (protein farnesyltransferase) inhibitor;
geroprotector
00low000000
mocetinostataminopyrimidine;
benzamides;
pyridines;
secondary amino compound;
secondary carboxamide;
substituted aniline
antineoplastic agent;
apoptosis inducer;
autophagy inducer;
cardioprotective agent;
EC 3.5.1.98 (histone deacetylase) inhibitor;
hepatotoxic agent
00low000000
l 779976benzimidazoles;
indoles;
piperidinecarboxamide;
primary amino compound;
secondary carboxamide
neuroprotective agent;
somatostatin receptor agonist
00low000000
ustiloxin baromatic ether;
heterodetic cyclic peptide;
macrocycle;
phenols;
secondary alcohol;
secondary carboxamide;
sulfoxide
Aspergillus metabolite;
microtubule-destabilising agent;
mycotoxin
00low000000
dysidenin1,3-thiazoles;
organochlorine compound;
secondary carboxamide;
tertiary carboxamide
animal metabolite;
marine metabolite;
toxin
00low000000
avenanthramide bamidobenzoic acid;
cinnamamides;
monohydroxybenzoic acid;
monomethoxybenzene;
phenols;
secondary carboxamide
antineoplastic agent;
apoptosis inducer;
phytoalexin
00low000000
azd2858aromatic amine;
N-methylpiperazine;
pyrazines;
pyridines;
secondary carboxamide;
sulfonamide
antineoplastic agent;
bone density conservation agent;
EC 2.7.11.26 (tau-protein kinase) inhibitor;
Wnt signalling activator
00low000000
bibw 2992aromatic ether;
enamide;
furans;
monochlorobenzenes;
organofluorine compound;
quinazolines;
secondary carboxamide;
tertiary amino compound
antineoplastic agent;
tyrosine kinase inhibitor
00low000000
betrixabanbenzamides;
guanidines;
monochloropyridine;
monomethoxybenzene;
secondary carboxamide
anticoagulant;
EC 3.4.21.6 (coagulation factor Xa) inhibitor
00low000000
fr 900848cyclopropanes;
nucleoside analogue;
olefinic compound;
polyketide;
secondary carboxamide
antifungal agent;
bacterial metabolite
00low000000
pha 665752dichlorobenzene;
enamide;
indolones;
N-acylpyrrolidine;
pyrrolecarboxamide;
secondary carboxamide;
sulfone;
tertiary carboxamide
antineoplastic agent;
c-Met tyrosine kinase inhibitor
00low000000
n-benzylhexadecanamidemacamide;
secondary carboxamide
EC 3.5.1.99 (fatty acid amide hydrolase) inhibitor;
neuroprotective agent;
plant metabolite
00low000000
chlorantranilipolemonochlorobenzenes;
organobromine compound;
pyrazole insecticide;
pyrazoles;
pyridines;
secondary carboxamide
ryanodine receptor agonist00low000000
cenicrivirocaromatic ether;
benzazocine;
diether;
imidazoles;
secondary carboxamide;
sulfoxide
anti-HIV agent;
anti-inflammatory agent;
antirheumatic drug;
chemokine receptor 2 antagonist;
chemokine receptor 5 antagonist
00low000000
at 7519dichlorobenzene;
piperidines;
pyrazoles;
secondary carboxamide
antineoplastic agent;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor
00low000000
azd 1152anilide;
monoalkyl phosphate;
monofluorobenzenes;
pyrazoles;
quinazolines;
secondary amino compound;
secondary carboxamide;
tertiary amino compound
antineoplastic agent;
Aurora kinase inhibitor;
prodrug
00low000000
pf 00299804enamide;
monochlorobenzenes;
monofluorobenzenes;
piperidines;
quinazolines;
secondary amino compound;
secondary carboxamide;
tertiary amino compound
antineoplastic agent;
epidermal growth factor receptor antagonist
00low000000
MI-63azaspiro compound;
monochlorobenzenes;
monofluorobenzenes;
morpholines;
oxindoles;
pyrrolidines;
secondary carboxamide
apoptosis inducer00low000000
PF-00835231aromatic ether;
indolecarboxamide;
L-leucine derivative;
primary alcohol;
pyrrolidin-2-ones;
secondary carboxamide
anticoronaviral agent;
drug metabolite;
EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor
00low000000
cyantraniliprolenitrile;
organobromine compound;
organochlorine compound;
pyrazole insecticide;
pyridines;
secondary carboxamide
ryanodine receptor agonist00low000000
VPC 23019aromatic amide;
D-serine derivative;
organic phosphate;
phosphoric ester;
secondary carboxamide
sphingosine-1-phosphate receptor 1 antagonist;
sphingosine-1-phosphate receptor 3 antagonist
00low000000
pd 0348292monochlorobenzenes;
monofluorobenzenes;
pyridone;
pyrrolidines;
secondary carboxamide;
ureas
anticoagulant;
EC 3.4.21.6 (coagulation factor Xa) inhibitor;
serine protease inhibitor
00low000000
narlaprevirazabicyclohexane;
cyclopropanes;
pyrrolidinecarboxamide;
secondary carboxamide;
sulfone;
tertiary carboxamide;
ureas
anticoronaviral agent;
antiviral drug;
EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor;
hepatitis C protease inhibitor
00low000000
tosedostatcarboxylic ester;
hydroxamic acid;
secondary carboxamide
00low000000
4-chloro-N-[1-[[5-(ethylthio)-1,3,4-thiadiazol-2-yl]amino]-3-methyl-1-oxobutan-2-yl]benzamidesecondary carboxamide00low000000
azd 1152-hqpaanilide;
monofluorobenzenes;
primary alcohol;
pyrazoles;
quinazolines;
secondary amino compound;
secondary carboxamide;
tertiary amino compound
antineoplastic agent;
Aurora kinase inhibitor
00low000000
CDN1163aromatic ether;
quinolines;
secondary carboxamide
SERCA activator00low000000
(2S)-2-[[[5-[[5-[[(2-methylpropan-2-yl)oxy-oxomethyl]amino]pentylamino]-oxomethyl]-1H-imidazol-4-yl]-oxomethyl]amino]propanoic acid tert-butyl estersecondary carboxamide;
tert-butyl ester
00low000000
(2S)-2-[[[5-[[methyl-(phenylmethyl)amino]-oxomethyl]-1H-imidazol-4-yl]-oxomethyl]amino]-6-[[(2-methylpropan-2-yl)oxy-oxomethyl]amino]hexanoic acid tert-butyl estersecondary carboxamide;
tert-butyl ester;
tertiary carboxamide
00low000000
(2S,3S,4R)-4-cyclopropyl-2-ethoxy-3-(3-hydroxypropyl)-N-prop-2-ynyl-3,4-dihydro-2H-pyran-6-carboxamidesecondary carboxamide00low000000
sid 26681509carbohydrazide;
L-tryptophan derivative;
secondary carboxamide;
tert-butyl ester;
thioester
antiplasmodial drug;
cathepsin L (EC 3.4.22.15) inhibitor
00low000000
azd 7545benzamides;
monochlorobenzenes;
organofluorine compound;
secondary carboxamide;
sulfone;
tertiary alcohol;
tertiary carboxamide
EC 2.7.11.2 - [pyruvate dehydrogenase (acetyl-transferring)] kinase inhibitor;
hypoglycemic agent
00low000000
sm 164benzenes;
organic heterobicyclic compound;
secondary carboxamide;
triazoles
antineoplastic agent;
apoptosis inducer;
radiosensitizing agent
00low000000
sch772984biaryl;
indazoles;
N-acylpiperazine;
N-alkylpyrrolidine;
N-arylpiperazine;
pyridines;
pyrimidines;
pyrrolidinecarboxamide;
secondary carboxamide;
tertiary amino compound;
tertiary carboxamide
analgesic;
antineoplastic agent;
apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor
00low000000
GRL-0617benzamides;
naphthalenes;
secondary carboxamide;
substituted aniline
anticoronaviral agent;
protease inhibitor
00low000000
entrectinibbenzamides;
difluorobenzene;
indazoles;
N-methylpiperazine;
oxanes;
secondary amino compound;
secondary carboxamide
antibacterial agent;
antineoplastic agent;
apoptosis inducer;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor
00low000000
TAK-5801,3-thiazolecarboxamide;
aminopyrimidine;
chloropyridine;
organofluorine compound;
pyrimidinecarboxamide;
secondary carboxamide
antineoplastic agent;
apoptosis inducer;
B-Raf inhibitor
00low000000
cx 5461diazepine;
naphthyridine derivative;
organic heterotetracyclic compound;
pyrazines;
secondary carboxamide
antineoplastic agent;
apoptosis inducer;
EC 2.7.7.6 (RNA polymerase) inhibitor
00low000000
KOM70144acetamides;
benzamides;
naphthalenes;
secondary carboxamide
anticoronaviral agent;
protease inhibitor
00low000000
monepantel(trifluoromethyl)benzenes;
aromatic ether;
aryl sulfide;
nitrile;
secondary carboxamide
anthelminthic drug;
nematicide
00low000000
ulixacaltamidebenzamides;
monochlorobenzenes;
monofluorobenzenes;
piperidines;
secondary carboxamide
non-narcotic analgesic;
T-type calcium channel blocker
00low000000
EG00229benzothiadiazole;
dicarboxylic acid monoamide;
L-arginine derivative;
secondary carboxamide;
sulfonamide;
thiophenes
angiogenesis inhibitor;
antineoplastic agent;
neuropilin receptor antagonist
00low000000
tak-632(trifluoromethyl)benzenes;
aromatic ether;
benzothiazoles;
cyclopropylcarboxamide;
monofluorobenzenes;
nitrile;
secondary carboxamide
antineoplastic agent;
apoptosis inducer;
B-Raf inhibitor;
EC 2.7.11.26 (tau-protein kinase) inhibitor;
necroptosis inhibitor
00low000000
lgk974bipyridines;
pyrazines;
pyridines;
secondary carboxamide
Wnt signalling inhibitor00low000000
gsk-5498a(trifluoromethyl)benzenes;
difluorobenzene;
pyrazoles;
secondary carboxamide
calcium channel blocker00low000000
2-methoxy-N-[3-[4-[3-methyl-4-[(6-methyl-3-pyridinyl)oxy]anilino]-6-quinazolinyl]prop-2-enyl]acetamidearomatic ether;
methylpyridines;
olefinic compound;
quinazolines;
secondary amino compound;
secondary carboxamide;
toluenes
00low000000
raltegravir1,2,4-oxadiazole;
dicarboxylic acid amide;
hydroxypyrimidine;
monofluorobenzenes;
pyrimidone;
secondary carboxamide
antiviral drug;
HIV-1 integrase inhibitor
00low000000
lfm a13aromatic amide;
dibromobenzene;
enamide;
enol;
nitrile;
secondary carboxamide
antineoplastic agent;
apoptosis inducer;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
EC 2.7.11.21 (polo kinase) inhibitor;
geroprotector;
platelet aggregation inhibitor
00low000000
teriflunomide(trifluoromethyl)benzenes;
aromatic amide;
enamide;
enol;
nitrile;
secondary carboxamide
drug metabolite;
EC 1.3.98.1 [dihydroorotate oxidase (fumarate)] inhibitor;
hepatotoxic agent;
non-steroidal anti-inflammatory drug;
tyrosine kinase inhibitor
00low000000
LimKi 31,3-thiazoles;
dichlorobenzene;
organofluorine compound;
pyrazoles;
secondary carboxamide
LIM kinase inhibitor00low000000
MK-8353aromatic ether;
dihydropyridine;
indazoles;
methyl sulfide;
N-alkylpyrrolidine;
pyridines;
pyrrolidinecarboxamide;
secondary carboxamide;
tertiary carboxamide;
triazoles
antineoplastic agent;
apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor
00low000000
acp-196aromatic amine;
benzamides;
imidazopyrazine;
pyridines;
pyrrolidinecarboxamide;
secondary carboxamide;
tertiary carboxamide;
ynone
antineoplastic agent;
apoptosis inducer;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
00low000000
gsk343aminopyridine;
indazoles;
N-alkylpiperazine;
N-arylpiperazine;
pyridone;
secondary carboxamide
antineoplastic agent;
apoptosis inducer;
EC 2.1.1.43 (enhancer of zeste homolog 2) inhibitor
00low000000
osimertinibacrylamides;
aminopyrimidine;
biaryl;
indoles;
monomethoxybenzene;
secondary amino compound;
secondary carboxamide;
substituted aniline;
tertiary amino compound
antineoplastic agent;
epidermal growth factor receptor antagonist
00low000000
ivosidenibcyanopyridine;
monochlorobenzenes;
organofluorine compound;
pyrrolidin-2-ones;
secondary carboxamide;
tertiary carboxamide
antineoplastic agent;
EC 1.1.1.42 (isocitrate dehydrogenase) inhibitor
00low000000
atogepantazaspiro compound;
organic heterotetracyclic compound;
piperidones;
secondary carboxamide;
trifluorobenzene
calcitonin gene-related peptide receptor antagonist00low000000
DDR1-IN-1(trifluoromethyl)benzenes;
aromatic ether;
benzamides;
N-alkylpiperazine;
oxindoles;
secondary carboxamide
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor00low000000
THZ531aminopyrimidine;
enamide;
indoles;
N-acylpiperidine;
organochlorine compound;
secondary amino compound;
secondary carboxamide
antineoplastic agent;
apoptosis inducer;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor
00low000000
AZ3451benzimidazoles;
benzodioxoles;
nitrile;
organobromine compound;
secondary carboxamide
anti-inflammatory agent;
autophagy inducer;
PAR2 negative allosteric modulator
00low000000
MMP-9-IN-1aromatic compound;
organic sulfide;
organofluorine compound;
pyrimidone;
secondary carboxamide
antineoplastic agent;
EC 3.4.24.35 (gelatinase B) inhibitor
00low000000
althiomycin1,3-thiazoles;
aldoxime;
ether;
gamma-lactam;
pentapeptide;
peptide antibiotic;
primary alcohol;
pyrroline;
secondary carboxamide;
tertiary carboxamide
antibacterial agent;
bacterial metabolite;
protein synthesis inhibitor
00low000000
colibactin1,3-thiazoles;
azaspiro compound;
polyketide;
pyrroline;
secondary carboxamide
alkylating agent;
carcinogenic agent;
Escherichia coli metabolite;
genotoxin
00low000000
N-[(2S)-3-cyclohexyl-1-oxo-1-({(2S)-1-oxo-3-[(3S)-2-oxopyrrolidin-3-yl]propan-2-yl}amino)propan-2-yl]-1H-indole-2-carboxamidealdehyde;
indolecarboxamide;
oligopeptide;
pyrrolidin-2-ones;
secondary carboxamide
anticoronaviral agent;
EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor
00low000000
3-fluoro-Nalpha-(1H-indol-2-ylcarbonyl)-N-{(2S)-1-oxo-3-[(3S)-2-oxopyrrolidin-3-yl]propan-2-yl}-L-phenylalaninamidealdehyde;
indolecarboxamide;
monofluorobenzenes;
oligopeptide;
pyrrolidin-2-ones;
secondary carboxamide
anticoronaviral agent;
EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor
00low000000
PF-07304814aromatic ether;
indolecarboxamide;
L-leucine derivative;
phosphate monoester;
pyrrolidin-2-ones;
secondary carboxamide
anticoronaviral agent;
EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor;
prodrug
00low000000
nirmatrelvirazabicyclohexane;
nitrile;
organofluorine compound;
pyrrolidin-2-ones;
pyrrolidinecarboxamide;
secondary carboxamide;
tertiary carboxamide
anticoronaviral agent;
EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor
00low000000
fleroxacindifluorobenzene;
fluoroquinolone antibiotic;
monocarboxylic acid;
N-alkylpiperazine;
quinolines
antibacterial drug;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
topoisomerase IV inhibitor
00low000000
fluconazoleconazole antifungal drug;
difluorobenzene;
tertiary alcohol;
triazole antifungal drug
environmental contaminant;
P450 inhibitor;
xenobiotic
00low000000
1,2-difluorobenzenedifluorobenzeneanaesthetic00low000000
voriconazoleconazole antifungal drug;
difluorobenzene;
pyrimidines;
tertiary alcohol;
triazole antifungal drug
P450 inhibitor00low000000
teflubenzurondichlorobenzene;
difluorobenzene;
N-acylurea
environmental contaminant;
insecticide;
xenobiotic
00low000000
flufenoxuron(trifluoromethyl)benzenes;
benzoylurea insecticide;
difluorobenzene;
monochlorobenzenes;
monofluorobenzenes
mite growth regulator00low000000
vx-745aryl sulfide;
dichlorobenzene;
difluorobenzene;
pyrimidopyridazine
anti-inflammatory drug;
apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor
00low000000
n-(n-(3,5-difluorophenacetyl)alanyl)phenylglycine tert-butyl estercarboxylic ester;
difluorobenzene;
dipeptide;
tert-butyl ester
EC 3.4.23.46 (memapsin 2) inhibitor00low000000
isavuconazole1,3-thiazoles;
conazole antifungal drug;
difluorobenzene;
nitrile;
tertiary alcohol;
triazole antifungal drug
EC 1.14.13.70 (sterol 14alpha-demethylase) inhibitor;
ergosterol biosynthesis inhibitor;
orphan drug
00low000000
pd 0325901difluorobenzene;
hydroxamic acid ester;
monofluorobenzenes;
organoiodine compound;
propane-1,2-diols;
secondary amino compound
antineoplastic agent;
EC 2.7.12.2 (mitogen-activated protein kinase kinase) inhibitor
00low000000
ly 411575dibenzoazepine;
difluorobenzene;
lactam;
secondary alcohol
EC 3.4.23.46 (memapsin 2) inhibitor00low000000
dafadine Caromatic amide;
aromatic ether;
difluorobenzene;
isoxazoles;
N-acylpiperidine;
pyridines
P450 inhibitor00low000000
pamapimodaromatic amine;
aromatic ether;
difluorobenzene;
diol;
primary alcohol;
pyridopyrimidine;
secondary amino compound
antirheumatic drug;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor
00low000000
gdc-0973aromatic amine;
difluorobenzene;
N-acylazetidine;
organoiodine compound;
piperidines;
secondary amino compound;
tertiary alcohol
antineoplastic agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor
00low000000
plx 4720aromatic ketone;
difluorobenzene;
organochlorine compound;
pyrrolopyridine;
sulfonamide
antineoplastic agent;
B-Raf inhibitor
00low000000
gsk 2126458aromatic ether;
difluorobenzene;
pyridazines;
pyridines;
quinolines;
sulfonamide
anticoronaviral agent;
antineoplastic agent;
autophagy inducer;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
mTOR inhibitor;
radiosensitizing agent
00low000000
plx4032aromatic ketone;
difluorobenzene;
monochlorobenzenes;
pyrrolopyridine;
sulfonamide
antineoplastic agent;
B-Raf inhibitor
00low000000
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
laurolitsineaporphine alkaloid;
aromatic ether;
phenols
HIV-1 integrase inhibitor;
metabolite
00low000000
australifungincarbobicyclic compound;
enol;
enone;
secondary alcohol
antifungal agent;
EC 2.3.1.24 (sphingosine N-acyltransferase) inhibitor;
HIV-1 integrase inhibitor;
metabolite
00low000000
jtk-303aromatic ether;
monochlorobenzenes;
organofluorine compound;
quinolinemonocarboxylic acid;
quinolone
HIV-1 integrase inhibitor00low000000
chicoric acidorganooxygen compoundgeroprotector;
HIV-1 integrase inhibitor
00low000000
complestatincyclic ether;
heterodetic cyclic peptide;
indoles;
organic heterobicyclic compound;
organochlorine compound;
peptide antibiotic;
polyphenol
anti-HIV-1 agent;
antimicrobial agent;
HIV-1 integrase inhibitor;
metabolite
00low000000
neuroprotectin acyclic ether;
heterodetic cyclic peptide;
indoles;
organochlorine compound;
polyphenol
HIV-1 integrase inhibitor;
metabolite
00low000000
integric acidcarboxylic ester;
cyclic ketone;
dioxo monocarboxylic acid;
enal;
enone;
eremophilane sesquiterpenoid
HIV-1 integrase inhibitor;
metabolite
00low000000
raltegravir1,2,4-oxadiazole;
dicarboxylic acid amide;
hydroxypyrimidine;
monofluorobenzenes;
pyrimidone;
secondary carboxamide
antiviral drug;
HIV-1 integrase inhibitor
00low000000
equisetinenol;
octahydronaphthalenes;
primary alcohol;
tetramic acids
antibacterial agent;
fungal metabolite;
HIV-1 integrase inhibitor;
quorum sensing inhibitor
00low000000
gsk1265744difluorobenzene;
monocarboxylic acid amide;
organic heterotricyclic compound;
secondary carboxamide
HIV-1 integrase inhibitor00low000000
bictegravirmonocarboxylic acid amide;
organic heterotetracyclic compound;
secondary carboxamide;
trifluorobenzene
HIV-1 integrase inhibitor00low000000
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
raltegravir1,2,4-oxadiazole;
dicarboxylic acid amide;
hydroxypyrimidine;
monofluorobenzenes;
pyrimidone;
secondary carboxamide
antiviral drug;
HIV-1 integrase inhibitor
00low000000
gsk1265744difluorobenzene;
monocarboxylic acid amide;
organic heterotricyclic compound;
secondary carboxamide
HIV-1 integrase inhibitor00low000000
bictegravirmonocarboxylic acid amide;
organic heterotetracyclic compound;
secondary carboxamide;
trifluorobenzene
HIV-1 integrase inhibitor00low000000
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
verapamilaromatic ether;
nitrile;
polyether;
tertiary amino compound
201620168.0low000010
donepezilaromatic ether;
indanones;
piperidines;
racemate
EC 3.1.1.7 (acetylcholinesterase) inhibitor;
EC 3.1.1.8 (cholinesterase) inhibitor;
nootropic agent
201820186.0low000010
e 4031sulfonamide201620168.0low000010
furafyllineoxopurine201620168.0low000010
haloperidolaromatic ketone;
hydroxypiperidine;
monochlorobenzenes;
organofluorine compound;
tertiary alcohol
antidyskinesia agent;
antiemetic;
dopaminergic antagonist;
first generation antipsychotic;
serotonergic antagonist
201520225.7low000021
ketoconazoledichlorobenzene;
dioxolane;
ether;
imidazoles;
N-acylpiperazine;
N-arylpiperazine
201620168.0low000010
metoprololaromatic ether;
propanolamine;
secondary alcohol;
secondary amino compound
antihypertensive agent;
beta-adrenergic antagonist;
environmental contaminant;
geroprotector;
xenobiotic
201920195.0low000010
nadololtetralins201920195.0low000010
sulfaphenazoleprimary amino compound;
pyrazoles;
substituted aniline;
sulfonamide antibiotic;
sulfonamide
antibacterial drug;
EC 1.14.13.181 (13-deoxydaunorubicin hydroxylase) inhibitor;
EC 1.14.13.67 (quinine 3-monooxygenase) inhibitor;
P450 inhibitor
201620168.0low000010
vesamicolpiperidines201820186.0low000010
zidovudineazide;
pyrimidine 2',3'-dideoxyribonucleoside
antimetabolite;
antiviral drug;
HIV-1 reverse transcriptase inhibitor
201620197.0low000030
carbidopacatechols;
hydrate;
hydrazines;
monocarboxylic acid
antidyskinesia agent;
antiparkinson drug;
dopaminergic agent;
EC 4.1.1.28 (aromatic-L-amino-acid decarboxylase) inhibitor
2014201410.0low000010
atorvastatinaromatic amide;
dihydroxy monocarboxylic acid;
monofluorobenzenes;
pyrroles;
statin (synthetic)
environmental contaminant;
xenobiotic
2014201410.0low000010
beta-thujaplicinol201920195.0low000010
beta-carboline-3-carboxylic acid ethyl esterbeta-carbolines201820186.0low000010
tadalafilbenzodioxoles;
pyrazinopyridoindole
EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor;
vasodilator agent
201820186.0low000010
4-(4-(4-chlorophenyl)-4-hydroxy-1-piperidinyl)-1-(4-fluorophenyl)-1-butanolpiperidines202220222.0low000001
birb 796aromatic ether;
morpholines;
naphthalenes;
pyrazoles;
ureas
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
immunomodulator
201820186.0low000010
dizocilpinesecondary amino compound;
tetracyclic antidepressant
anaesthetic;
anticonvulsant;
neuroprotective agent;
nicotinic antagonist;
NMDA receptor antagonist
201520159.0low000010
ritonavir1,3-thiazoles;
carbamate ester;
carboxamide;
L-valine derivative;
ureas
antiviral drug;
environmental contaminant;
HIV protease inhibitor;
xenobiotic
201620168.0low000010
quinidinecinchona alkaloidalpha-adrenergic antagonist;
anti-arrhythmia drug;
antimalarial;
drug allergen;
EC 1.14.13.181 (13-deoxydaunorubicin hydroxylase) inhibitor;
EC 3.6.3.44 (xenobiotic-transporting ATPase) inhibitor;
muscarinic antagonist;
P450 inhibitor;
potassium channel blocker;
sodium channel blocker
201620168.0low000010
pentazocinebenzazocine202220222.0low000002
cerivastatindihydroxy monocarboxylic acid;
pyridines;
statin (synthetic)
201620168.0low000010
1-(3-tert-butyl-1-methylpyrazol-5-yl)-3-(4-chlorophenyl)ureamonochlorobenzenes;
phenylureas;
pyrazoles
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor201820186.0low000010
bd 1063primary amine202220222.0medium000001
telaprevircyclopentapyrrole;
cyclopropanes;
oligopeptide;
pyrazines
antiviral drug;
hepatitis C protease inhibitor;
peptidomimetic
201820186.0low000010
u-50488dichlorobenzene;
monocarboxylic acid amide;
N-alkylpyrrolidine
analgesic;
antitussive;
calcium channel blocker;
diuretic;
kappa-opioid receptor agonist
202220222.0low000001
jtk-303aromatic ether;
monochlorobenzenes;
organofluorine compound;
quinolinemonocarboxylic acid;
quinolone
HIV-1 integrase inhibitor201420197.0low000030
eprosartandicarboxylic acid;
imidazoles;
thiophenes
angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
2014201410.0low000010
enkephalin, ala(2)-mephe(4)-gly(5)-peptide202220222.0low000001
pradimicin aaromatic ether;
carboxylic acid;
disaccharide derivative;
L-alanine derivative;
p-quinones;
polyphenol;
pradimicin;
secondary alcohol
201520159.0low000010
naltrindoleisoquinolines202220222.0low000001
scio-469aromatic amide;
aromatic ketone;
chloroindole;
dicarboxylic acid diamide;
indolecarboxamide;
monofluorobenzenes;
N-acylpiperazine;
N-alkylpiperazine
antineoplastic agent;
apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor
201820186.0low000010
sa 4503201820186.0low000010
raltegravir potassium2013201311.0low000010
bms-790052biphenyls;
carbamate ester;
carboxamide;
imidazoles;
valine derivative
antiviral drug;
nonstructural protein 5A inhibitor
201820186.0low000010
azd3839201820186.0medium000010
abt-199aromatic ether;
C-nitro compound;
monochlorobenzenes;
N-alkylpiperazine;
N-arylpiperazine;
N-sulfonylcarboxamide;
oxanes;
pyrrolopyridine
antineoplastic agent;
apoptosis inducer;
B-cell lymphoma 2 inhibitor
201820186.0low000010
ass234201820186.0medium000010
raltegravir1,2,4-oxadiazole;
dicarboxylic acid amide;
hydroxypyrimidine;
monofluorobenzenes;
pyrimidone;
secondary carboxamide
antiviral drug;
HIV-1 integrase inhibitor
201420196.9low000080
a 769662biphenyls201820186.0low000010
gsk1265744difluorobenzene;
monocarboxylic acid amide;
organic heterotricyclic compound;
secondary carboxamide
HIV-1 integrase inhibitor201320207.5low000020
bictegravirmonocarboxylic acid amide;
organic heterotetracyclic compound;
secondary carboxamide;
trifluorobenzene
HIV-1 integrase inhibitor201920204.5low000020
sildenafilpiperazines;
pyrazolopyrimidine;
sulfonamide
EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor;
vasodilator agent
201820186.0low000010
zaprinasttriazolopyrimidines201820186.0low000010
vardenafilimidazotriazine;
N-alkylpiperazine;
N-sulfonylpiperazine
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
vasodilator agent
201820186.0low000010
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
adenine6-aminopurines;
purine nucleobase
Daphnia magna metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
201220234.8low160002511
bromidehalide anion;
monoatomic bromine
202120213.0low000001
carbamatesamino-acid anion201420197.2low400050
cytosineaminopyrimidine;
pyrimidine nucleobase;
pyrimidone
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
201920195.0low100010
glycinealpha-amino acid;
amino acid zwitterion;
proteinogenic amino acid;
serine family amino acid
EC 2.1.2.1 (glycine hydroxymethyltransferase) inhibitor;
fundamental metabolite;
hepatoprotective agent;
micronutrient;
neurotransmitter;
NMDA receptor agonist;
nutraceutical
202020204.0low000010
kynureninearomatic ketone;
non-proteinogenic alpha-amino acid;
substituted aniline
human metabolite201920195.0low000010
uracilpyrimidine nucleobase;
pyrimidone
allergen;
Daphnia magna metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
prodrug;
Saccharomyces cerevisiae metabolite
201620196.5low200020
p-aminohippuric acidN-acylglycineDaphnia magna metabolite2013201311.0low100010
amlodipinedihydropyridine;
ethyl ester;
methyl ester;
monochlorobenzenes;
primary amino compound
antihypertensive agent;
calcium channel blocker;
vasodilator agent
202020204.0low000010
amodiaquineaminoquinoline;
organochlorine compound;
phenols;
secondary amino compound;
tertiary amino compound
anticoronaviral agent;
antimalarial;
drug allergen;
EC 2.1.1.8 (histamine N-methyltransferase) inhibitor;
non-steroidal anti-inflammatory drug;
prodrug
201920214.5low000031
antipyrinepyrazoloneantipyretic;
cyclooxygenase 3 inhibitor;
environmental contaminant;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic
201920195.0low000010
aztreonam201620168.0low000010
carbamazepinedibenzoazepine;
ureas
analgesic;
anticonvulsant;
antimanic drug;
drug allergen;
EC 3.5.1.98 (histone deacetylase) inhibitor;
environmental contaminant;
glutamate transporter activator;
mitogen;
non-narcotic analgesic;
sodium channel blocker;
xenobiotic
201620206.0low100020
dichlorodiphenyl dichloroethylenechlorophenylethylene;
monochlorobenzenes
human xenobiotic metabolite;
persistent organic pollutant
201920195.0low000010
valproic acidbranched-chain fatty acid;
branched-chain saturated fatty acid
anticonvulsant;
antimanic drug;
EC 3.5.1.98 (histone deacetylase) inhibitor;
GABA agent;
neuroprotective agent;
psychotropic drug;
teratogenic agent
201820214.7low100021
foscarnetcarboxylic acid;
one-carbon compound;
phosphonic acids
antiviral drug;
geroprotector;
HIV-1 reverse transcriptase inhibitor;
sodium-dependent Pi-transporter inhibitor
201420169.0low000020
hydroxychloroquineaminoquinoline;
organochlorine compound;
primary alcohol;
secondary amino compound;
tertiary amino compound
anticoronaviral agent;
antimalarial;
antirheumatic drug;
dermatologic drug
202120213.0low100001
iohexolbenzenedicarboxamide;
organoiodine compound
environmental contaminant;
radioopaque medium;
xenobiotic
2013201311.0low100010
isoniazidcarbohydrazideantitubercular agent;
drug allergen
201820232.8low300033
metforminguanidinesenvironmental contaminant;
geroprotector;
hypoglycemic agent;
xenobiotic
201620187.0low100050
methadonebenzenes;
diarylmethane;
ketone;
tertiary amino compound
2013201311.0low100010
nevirapinecyclopropanes;
dipyridodiazepine
antiviral drug;
HIV-1 reverse transcriptase inhibitor
201520235.0low100021
oxolinic acidaromatic carboxylic acid;
organic heterotricyclic compound;
oxacycle;
quinolinemonocarboxylic acid;
quinolone antibiotic
antibacterial drug;
antifungal agent;
antiinfective agent;
antimicrobial agent;
enzyme inhibitor
201620168.0low000010
phenobarbitalbarbituratesanticonvulsant;
drug allergen;
excitatory amino acid antagonist;
sedative
201820186.0low000010
sulfisoxazoleisoxazoles;
sulfonamide antibiotic;
sulfonamide
antibacterial drug;
drug allergen
201820186.0low000010
tazaroteneacetylenic compound;
ethyl ester;
pyridines;
retinoid;
thiochromane
keratolytic drug;
prodrug;
teratogenic agent
201920195.0low000010
thyroxine2-halophenol;
iodophenol;
L-phenylalanine derivative;
non-proteinogenic L-alpha-amino acid;
thyroxine zwitterion;
thyroxine
antithyroid drug;
human metabolite;
mouse metabolite;
thyroid hormone
201720177.0low000010
prednisone11-oxo steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
C21-steroid;
glucocorticoid;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone
adrenergic agent;
anti-inflammatory drug;
antineoplastic agent;
immunosuppressive agent;
prodrug
2013201311.0low100010
penicillin gpenicillin allergen;
penicillin
antibacterial drug;
drug allergen;
epitope
202020204.0low000010
alaninealanine zwitterion;
alanine;
L-alpha-amino acid;
proteinogenic amino acid;
pyruvate family amino acid
EC 4.3.1.15 (diaminopropionate ammonia-lyase) inhibitor;
fundamental metabolite
201720234.2low110001711
serineL-alpha-amino acid;
proteinogenic amino acid;
serine family amino acid;
serine zwitterion;
serine
algal metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
202020204.0low000010
glutamineamino acid zwitterion;
glutamine family amino acid;
glutamine;
L-alpha-amino acid;
polar amino acid zwitterion;
proteinogenic amino acid
EC 1.14.13.39 (nitric oxide synthase) inhibitor;
Escherichia coli metabolite;
human metabolite;
metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
Saccharomyces cerevisiae metabolite
202020204.0low000010
ethinyl estradiol17-hydroxy steroid;
3-hydroxy steroid;
terminal acetylenic compound
xenoestrogen201520159.0low100010
uridine monophosphatepyrimidine ribonucleoside 5'-monophosphate;
uridine 5'-phosphate
Escherichia coli metabolite;
human metabolite;
mouse metabolite
2014201410.0low000010
carbostyrilmonohydroxyquinoline;
quinolone
bacterial xenobiotic metabolite201120227.4low3000856
phenylalanineamino acid zwitterion;
erythrose 4-phosphate/phosphoenolpyruvate family amino acid;
L-alpha-amino acid;
phenylalanine;
proteinogenic amino acid
algal metabolite;
EC 3.1.3.1 (alkaline phosphatase) inhibitor;
Escherichia coli metabolite;
human xenobiotic metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
plant metabolite;
Saccharomyces cerevisiae metabolite
201920195.0low000010
histidineamino acid zwitterion;
histidine;
L-alpha-amino acid;
polar amino acid zwitterion;
proteinogenic amino acid
algal metabolite;
Escherichia coli metabolite;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
Saccharomyces cerevisiae metabolite
202020204.0low000010
valineL-alpha-amino acid zwitterion;
L-alpha-amino acid;
proteinogenic amino acid;
pyruvate family amino acid;
valine
algal metabolite;
Escherichia coli metabolite;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
Saccharomyces cerevisiae metabolite
201620168.0low200020
tryptophanerythrose 4-phosphate/phosphoenolpyruvate family amino acid;
L-alpha-amino acid zwitterion;
L-alpha-amino acid;
proteinogenic amino acid;
tryptophan zwitterion;
tryptophan
antidepressant;
Escherichia coli metabolite;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
plant metabolite;
Saccharomyces cerevisiae metabolite
201920195.0low000010
quinoxalinesmancude organic heterobicyclic parent;
naphthyridine;
ortho-fused heteroarene
201920195.0low100010
2-naphthylaminenaphthylaminecarcinogenic agent201620168.0low100010
xanthenesxanthene202120213.0low000001
pyrrolespyrrole;
secondary amine
201720177.0low000010
limestonecalcium salt;
carbonate salt;
inorganic calcium salt;
one-carbon compound
antacid;
fertilizer;
food colouring;
food firming agent
201520159.0low100010
myristic acidlong-chain fatty acid;
straight-chain saturated fatty acid
algal metabolite;
Daphnia magna metabolite;
EC 3.1.1.1 (carboxylesterase) inhibitor;
human metabolite
202220222.0low000001
resazurinphenoxazine202120213.0low000001
2,6-dichloro-4-nitrophenol202320231.0low000001
deoxycytidinepyrimidine 2'-deoxyribonucleosideEscherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
201420178.5low000040
ethambutolethanolamines;
ethylenediamine derivative
antitubercular agent;
environmental contaminant;
xenobiotic
201920195.0low000010
fluorescein-5-isothiocyanatefluorescein isothiocyanate201920195.0low000010
dithiothreitol1,4-dimercaptobutane-2,3-diol;
butanediols;
dithiol;
glycol;
thiol
chelator;
human metabolite;
reducing agent
2014201410.0low000010
silvercopper group element atom;
elemental silver
Escherichia coli metabolite202320231.0low000001
europiumf-block element atom;
lanthanoid atom
201820186.0low000010
pregnanolone3-hydroxy-5beta-pregnan-20-one;
3alpha-hydroxy steroid
human metabolite;
intravenous anaesthetic;
sedative
201920195.0low000010
oxcarbazepinecyclic ketone;
dibenzoazepine
anticonvulsant;
drug allergen
201820205.0low000020
zidovudineazide;
pyrimidine 2',3'-dideoxyribonucleoside
antimetabolite;
antiviral drug;
HIV-1 reverse transcriptase inhibitor
201620224.8low200033
miloxacinquinolines201620168.0low000010
desogestrel17beta-hydroxy steroid;
terminal acetylenic compound
contraceptive drug;
progestin;
synthetic oral contraceptive
202020204.0low000010
pefloxacinfluoroquinolone antibiotic;
monocarboxylic acid;
N-alkylpiperazine;
N-arylpiperazine;
quinolone antibiotic;
quinolone
antibacterial drug;
antiinfective agent;
DNA synthesis inhibitor
201620168.0low000010
gemcitabineorganofluorine compound;
pyrimidine 2'-deoxyribonucleoside
antimetabolite;
antineoplastic agent;
antiviral drug;
DNA synthesis inhibitor;
EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor;
environmental contaminant;
immunosuppressive agent;
photosensitizing agent;
prodrug;
radiosensitizing agent;
xenobiotic
201720177.0low000010
atorvastatinaromatic amide;
dihydroxy monocarboxylic acid;
monofluorobenzenes;
pyrroles;
statin (synthetic)
environmental contaminant;
xenobiotic
202020204.0low000010
lamivudinemonothioacetal;
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
201320234.1medium5500012999
irinotecancarbamate ester;
delta-lactone;
N-acylpiperidine;
pyranoindolizinoquinoline;
ring assembly;
tertiary alcohol;
tertiary amino compound
antineoplastic agent;
apoptosis inducer;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
prodrug
202120213.0low000001
emtricitabinemonothioacetal;
nucleoside analogue;
organofluorine compound;
pyrimidone
antiviral drug;
HIV-1 reverse transcriptase inhibitor
201420233.8low290004137
trovafloxacin201620168.0low000010
efavirenzacetylenic compound;
benzoxazine;
cyclopropanes;
organochlorine compound;
organofluorine compound
antiviral drug;
HIV-1 reverse transcriptase inhibitor
201220234.0low180004037
nelfinaviraryl sulfide;
benzamides;
organic heterobicyclic compound;
phenols;
secondary alcohol;
tertiary amino compound
antineoplastic agent;
HIV protease inhibitor
201720177.0low000010
emivirinepyrimidoneantiviral drug;
HIV-1 reverse transcriptase inhibitor
201920195.0low100010
amprenavircarbamate ester;
sulfonamide;
tetrahydrofuryl ester
antiviral drug;
HIV protease inhibitor
2014201410.0low100010
cephalosporin ccephalosporinfungal metabolite201620168.0low000010
triazoles1,2,3-triazole201220217.8low300071
sertralinedichlorobenzene;
secondary amino compound;
tetralins
antidepressant;
serotonin uptake inhibitor
202020204.0low000010
artemetherartemisinin derivative;
cyclic acetal;
organic peroxide;
semisynthetic derivative;
sesquiterpenoid
antimalarial201920214.5low000031
uk 68798aromatic ether;
sulfonamide;
tertiary amino compound
anti-arrhythmia drug;
potassium channel blocker
2014201410.0low000020
alafosfalin202020204.0low000010
doripenemcarbapenems201620168.0low000010
lopinaviramphetamines;
dicarboxylic acid diamide
anticoronaviral agent;
antiviral drug;
HIV protease inhibitor
201420235.2low200063
brexanolone3-hydroxy-5alpha-pregnan-20-oneantidepressant;
GABA modulator;
human metabolite;
intravenous anaesthetic;
sedative
201920195.0low000010
imipenem, anhydrousbeta-lactam antibiotic allergen;
carbapenems;
zwitterion
antibacterial drug201620168.0low000010
artesunic acid201920214.5low000031
piperaquineaminoquinoline;
N-arylpiperazine;
organochlorine compound
antimalarial202220222.0low200002
fosamprenavirsulfonamideprodrug2014201410.0low100010
carbapenems201620168.0low000010
prolineamino acid zwitterion;
glutamine family amino acid;
L-alpha-amino acid;
proline;
proteinogenic amino acid
algal metabolite;
compatible osmolytes;
Escherichia coli metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
Saccharomyces cerevisiae metabolite
201420169.0low200020
docetaxel anhydroussecondary alpha-hydroxy ketone;
tetracyclic diterpenoid
antimalarial;
antineoplastic agent;
photosensitizing agent
201720177.0low000010
moxifloxacinaromatic ether;
cyclopropanes;
fluoroquinolone antibiotic;
pyrrolidinopiperidine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone
antibacterial drug2012201212.0low100010
atazanavir sulfateorganic sulfate salt201120235.4low3000154
organophosphonatesdivalent inorganic anion;
phosphite ion
2012201510.5low200040
etravirineaminopyrimidine;
aromatic ether;
dinitrile;
organobromine compound
antiviral agent;
HIV-1 reverse transcriptase inhibitor
201220216.7low100051
darunavircarbamate ester;
furofuran;
sulfonamide
antiviral drug;
HIV protease inhibitor
201320234.8low120003316
benzofurans201920195.0low100010
trimethoprim, sulfamethoxazole drug combination201620168.0low000010
ritonavir1,3-thiazoles;
carbamate ester;
carboxamide;
L-valine derivative;
ureas
antiviral drug;
environmental contaminant;
HIV protease inhibitor;
xenobiotic
201120236.2low17000379
abacavir2,6-diaminopurinesantiviral drug;
drug allergen;
HIV-1 reverse transcriptase inhibitor
201320235.5low140004310
linezolidacetamides;
morpholines;
organofluorine compound;
oxazolidinone
antibacterial drug;
protein synthesis inhibitor
201620168.0low000010
betadexcyclodextrin201920195.0low000010
zithromaxmacrolide antibioticantibacterial drug;
environmental contaminant;
xenobiotic
201920195.0low000010
tenofovirnucleoside analogue;
phosphonic acids
antiviral drug;
drug metabolite;
HIV-1 reverse transcriptase inhibitor
201220234.0medium380006358
maraviroctropane alkaloid201220208.1low300070
telaprevircyclopentapyrrole;
cyclopropanes;
oligopeptide;
pyrazines
antiviral drug;
hepatitis C protease inhibitor;
peptidomimetic
2014201410.0low100010
abacavir, lamivudine drug combination201320226.7high8000303
jtk-303aromatic ether;
monochlorobenzenes;
organofluorine compound;
quinolinemonocarboxylic acid;
quinolone
HIV-1 integrase inhibitor201120237.4high3000856
bilirubinbiladienes;
dicarboxylic acid
antioxidant;
human metabolite;
mouse metabolite
201820224.0low000011
amphotericin bantibiotic antifungal drug;
macrolide antibiotic;
polyene antibiotic
antiamoebic agent;
antiprotozoal drug;
bacterial metabolite
201920195.0low000010
morphinemorphinane alkaloid;
organic heteropentacyclic compound;
tertiary amino compound
anaesthetic;
drug allergen;
environmental contaminant;
geroprotector;
mu-opioid receptor agonist;
opioid analgesic;
plant metabolite;
vasodilator agent;
xenobiotic
201920195.0low000020
clobetasol11beta-hydroxy steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
3-oxo-Delta(1),Delta(4)-steroid;
chlorinated steroid;
fluorinated steroid;
glucocorticoid;
tertiary alpha-hydroxy ketone
anti-inflammatory drug;
SMO receptor agonist
201920195.0low000010
halobetasolcorticosteroid hormone201920195.0low000010
indinavir sulfatedicarboxylic acid diamide;
N-(2-hydroxyethyl)piperazine;
piperazinecarboxamide
HIV protease inhibitor202020204.0low000010
fumaratesbutenedioate;
C4-dicarboxylate
human metabolite;
metabolite;
Saccharomyces cerevisiae metabolite
202320231.0low100003
cefepimecephalosporin;
oxime O-ether
antibacterial drug202020204.0low000010
ferrous fumaratedicarboxylic acid201520159.0low100010
lumefantrinefluorenes;
monochlorobenzenes;
secondary alcohol;
tertiary amine
antimalarial201920195.0low000010
cgp-56697201920214.3low000021
rilpivirineaminopyrimidine;
nitrile
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor;
HIV-1 reverse transcriptase inhibitor
201320235.2medium70004516
epoxyfarnesyl diazoacetate201920214.0low100011
carumonammonobactamantibacterial drug201620168.0low000010
etonogestrel17beta-hydroxy steroid;
3-oxo-Delta(4) steroid;
terminal acetylenic compound
contraceptive drug;
female contraceptive drug;
progestin
202020204.0low000010
tri-cyclen201520159.0low100010
gs-73406-aminopurines;
ether;
isopropyl ester;
L-alanine derivative;
phosphoramidate ester
antiviral drug;
HIV-1 reverse transcriptase inhibitor;
prodrug
201720233.9low110001413
efavirenz, emtricitabine, tenofovir disoproxil fumarate drug combination201620168.0low000010
pasireotidehomodetic cyclic peptide;
peptide hormone
antineoplastic agent2014201410.0low000010
artenimol202220222.0low200002
aclidinium bromideorganic bromide salt;
quaternary ammonium salt
bronchodilator agent;
muscarinic antagonist
201920195.0low000010
emtricitabine, tenofovir disoproxil fumarate drug combination201720177.0low000010
norelgestromin201520159.0low100010
mdv 3100(trifluoromethyl)benzenes;
benzamides;
imidazolidinone;
monofluorobenzenes;
nitrile;
thiocarbonyl compound
androgen antagonist;
antineoplastic agent
202220222.0low000001
alx-0600polypeptideantioxidant;
glucagon-like peptide-2 receptor agonist;
metabolite;
protective agent
2014201410.0low000010
chitosan202120222.5low000002
raltegravir potassium201120227.4high900012614
cardiovascular agents202020204.0low000010
cobicistat1,3-thiazoles;
carbamate ester;
monocarboxylic acid amide;
morpholines;
ureas
P450 inhibitor201620235.2low3000155
bms-790052biphenyls;
carbamate ester;
carboxamide;
imidazoles;
valine derivative
antiviral drug;
nonstructural protein 5A inhibitor
201620168.0low100010
quad pill201620216.0low000021
siponimod201920195.0low000010
grazopreviraromatic ether;
azamacrocycle;
carbamate ester;
cyclopropanes;
lactam;
N-sulfonylcarboxamide;
quinoxaline derivative
antiviral drug;
hepatitis C protease inhibitor;
hepatoprotective agent
201920195.0low100010
abt-450201620168.0low100010
sofosbuvirisopropyl ester;
L-alanyl ester;
nucleotide conjugate;
organofluorine compound;
phosphoramidate ester
antiviral drug;
hepatitis C protease inhibitor;
prodrug
201420236.5low100031
warfarinbenzenes;
hydroxycoumarin;
methyl ketone
201720177.0low000010
tipranavirsulfonamideantiviral drug;
HIV protease inhibitor
201420207.0low100020
gsk1265744difluorobenzene;
monocarboxylic acid amide;
organic heterotricyclic compound;
secondary carboxamide
HIV-1 integrase inhibitor201320235.7low1000103
urmc-099201720177.0low000010
abt-267aromatic amide;
carbamate ester;
dipeptide;
pyrrolidines
antiviral drug;
hepatitis C virus nonstructural protein 5A inhibitor
201620168.0low100010
abt-333aromatic ether;
naphthalenes;
pyrimidone;
sulfonamide
antiviral drug;
nonnucleoside hepatitis C virus polymerase inhibitor
201620168.0low100010
doravirine201720233.4low100034
gs-5816carbamate ester;
ether;
imidazoles;
L-valine derivative;
N-acylpyrrolidine;
organic heteropentacyclic compound;
ring assembly
antiviral drug;
hepatitis C virus nonstructural protein 5A inhibitor
202320231.0low000001
mk-8742carbamate ester;
imidazoles;
L-valine derivative;
N-acylpyrrolidine;
organic heterotetracyclic compound;
ring assembly
antiviral drug;
hepatitis C virus nonstructural protein 5A inhibitor;
hepatoprotective agent
201920195.0low100010
bictegravirmonocarboxylic acid amide;
organic heterotetracyclic compound;
secondary carboxamide;
trifluorobenzene
HIV-1 integrase inhibitor201620234.0high80002314
vitamin b 12202320231.0low100001
norgestrel201520159.0low100010
albuvirtide202320231.0medium000001
levoleucovorin5-formyltetrahydrofolic acidantineoplastic agent;
metabolite
201720177.0low000010
folic acidfolic acids;
N-acyl-amino acid
human metabolite;
mouse metabolite;
nutrient
201820233.9low200063
rifampincyclic ketal;
hydrazone;
N-iminopiperazine;
N-methylpiperazine;
rifamycins;
semisynthetic derivative;
zwitterion
angiogenesis inhibitor;
antiamoebic agent;
antineoplastic agent;
antitubercular agent;
DNA synthesis inhibitor;
EC 2.7.7.6 (RNA polymerase) inhibitor;
Escherichia coli metabolite;
geroprotector;
leprostatic drug;
neuroprotective agent;
pregnane X receptor agonist;
protein synthesis inhibitor
201320234.1low6000106
rifapentineN-alkylpiperazine;
N-iminopiperazine;
rifamycins
antitubercular agent;
leprostatic drug
201620234.0low200042
pemetrexedN-acyl-L-glutamic acid;
pyrrolopyrimidine
antimetabolite;
antineoplastic agent;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
EC 2.1.1.45 (thymidylate synthase) inhibitor;
EC 2.1.2.2 (phosphoribosylglycinamide formyltransferase) inhibitor
201620168.0low000010
leptin201920223.5low000011
pyrimidinones201620168.0low000010
ConditionIndicatedStudiesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
2019 Novel Coronavirus Disease0202020232.6low200027
Abnormalities, Congenital0201820214.8low000041
Abnormalities, Drug-Induced0201820205.0low000030
Abortion, Spontaneous0201920214.0low000011
Abortion, Tubal0201920214.0low000011
Absence Seizure0201920204.5low000020
Ache0202220222.0low000001
Acquired Immune Deficiency Syndrome0201720233.2low100066
Acquired Immunodeficiency Syndrome1201720233.2low100066
Acquired-Immune Deficiency Syndrome Dementia Complex0201720205.5low000020
Acrania0201820234.5low0000176
Acute Confusional Senile Dementia0201820186.0low000010
Acute Disease0201920195.0low100010
Acute Hepatic Failure0201820186.0low000010
Acute Ischemic Stroke0202020204.0low000010
Acute Liver Injury, Drug-Induced0201320197.3low000030
Acute Necrotizing Pancreatitis0201520159.0low000010
Addiction, Opioid02013201311.0low100010
Adenocarcinoma0201920195.0low000010
Adenocarcinoma, Basal Cell0201920195.0low000010
Adverse Drug Event0201220234.9low5000198
Affective Disorders0201520206.5low000020
African Sleeping Sickness0201720177.0low000010
Age-Related Osteoporosis0201820186.0low100010
Aging0202020213.8low000031
AIDS Dementia Complex0201720205.5low000020
AIDS Seroconversion0201620233.5low60001317
AIDS-Related Opportunistic Infections0201420205.8low000060
AIDS, Simian0201620168.0low000010
Allergic Cutaneous Angiitis0201920195.0low000010
Allergy, Drug0201520178.0low000030
ALS - Amyotrophic Lateral Sclerosis0201920195.0low000010
Alzheimer Disease0201820186.0low000010
Amnesia0202220222.0low000001
Amnesia-Memory Loss0202220222.0low000001
Amyotrophic Lateral Sclerosis1201920195.0low000010
Anoxemia0202220222.0low000001
Anxiety0201720196.3low000030
Aortic Stenosis0201720177.0low000010
Aortic Valve Stenosis0201720177.0low000010
Apoplexy0201720177.0low000010
Arthralgia0202020204.0low000010
Asymptomatic Conditions0202020204.0low000010
Atherogenesis0202220231.7low200003
Atherosclerosis0202220231.7low200003
Atypical Mycobacterial Infection, Disseminated0201920195.0low000010
B Virus Infection0201920195.0low000010
Bacteremia0201920204.5low000020
Bacterial Eye Infections0202020204.0low000010
Basal Ganglia Diseases0201920195.0low000010
Behavior Disorders0201520206.1low000080
Benign Neoplasms0201720177.0low000010
Bilateral Headache02010201610.3low100120
Bile Duct Obstruction0201820186.0low000010
Body Weight0202020232.5low300015
Bone Diseases, Metabolic0202120213.0low000001
Cancer of Lung0201620177.5low000020
Cancer of Prostate0202220231.5low000002
Cancer of Skin0202020204.0low000020
Cancer of Stomach0201920195.0low000010
Carcinoma, Non-Small Cell Lung0201620177.5low000020
Carcinoma, Non-Small-Cell Lung0201620177.5low000020
Cardiometabolic Syndrome0202120213.0low100001
Cardiovascular Diseases0201720233.7low600054
Cardiovascular Stroke0202020204.0low000010
Carditis0201620196.5low000020
Central Nervous System Disease0201920195.0low000010
Central Nervous System Diseases0201920195.0low000010
Central Nervous System Infection0201920195.0low000010
Central Nervous System Syphilis0202020204.0low000010
Central Nervous System Toxoplasmosis0201720177.0low000010
Cerebellar Diseases0201620168.0low000010
Chemical and Drug Induced Liver Injury0201320197.3low000030
Chemical Dependence0202120213.0low000001
Child Development Deviations0201920195.0low000010
Child Mental Disorders0202120213.0low000001
Cholera Infantum0201520159.0low000010
Cholestasis0201820186.0low000010
Chronic Esophagitis, Eosinophilic0202020204.0low000010
Chronic Hepatitis C0201620235.5low100031
Chronic Insomnia0201520187.2low000060
Chronic Kidney Diseases0201620225.7low000021
Chronic Kidney Failure0201620196.2low100050
Cirrhosis0202220222.0low000001
Cirrhosis, Liver0201720177.0low000010
Clerambault Syndrome0201620196.5low000020
Co-infection0201220234.9low5000166
Cognition Disorders0201920195.0low000010
Cognitive Decline0202020204.0low000030
Cognitive Dysfunction0202020204.0low000030
Colitis0201620206.0low000020
Colitis, Lymphocytic0201920195.0low000010
Colorectal Cancer0202120213.0low000001
Colorectal Neoplasms0202120213.0low000001
Complication, Postoperative0202020204.0low000010
Complications, Infectious Pregnancy0201520235.2low3000244
Complications, Parasitic Pregnancy0202220222.0low100001
Complications, Pregnancy0201920204.3low000030
Congenital Familial Lymphedema0202020204.0low000010
Congenital Zika Syndrome0202020204.0low000010
Coronavirus Infections0202020204.0low000020
Critical Illness0202220222.0low000001
Cytomegaloviral Retinitis0202020204.0low000010
Cytomegalovirus Retinitis0202020204.0low000010
Deficiency, Folic Acid0201920233.0low000011
Deglutition Disorders0202020204.0low000010
Delayed Effects, Prenatal Exposure0201620195.6low000050
Depression0201720215.0low000041
Dermatitis, Contact, Photoallergic0201820186.0low000010
Developmental Disabilities0201920195.0low000010
Diabetes Mellitus0202220222.0low000001
Diabetes Mellitus, Adult-Onset0201720234.0low000022
Diabetes Mellitus, Gestational0202120213.0low000001
Diabetes Mellitus, Type 20201720234.0low000022
Diabetes, Gestational0202120213.0low000001
Diathesis0202120213.0low000001
Disease Exacerbation0201720196.0low000020
Disease Models, Animal0201720234.2low000042
Dizziness0201720177.0low000010
Dizzyness0201720177.0low000010
DRESS Syndrome0201820186.0low000010
Drug Abuse, Intravenous02013201311.0low100010
Drug Hypersensitivity0201520178.0low000030
Drug Withdrawal Symptoms02013201311.0low100010
Drug-Related Side Effects and Adverse Reactions0201220234.9low5000198
Dysesthesia0201720177.0low000010
Dysphagia0202020204.0low000010
Electrocardiogram QT Prolonged02012201212.0low100010
Encephalopathy, Toxic0202120213.0low000001
Eosinophilia0201820186.0low000010
Eosinophilia, Tropical0201820186.0low000010
Eosinophilic Esophagitis0202020204.0low000010
Erectile Dysfunction0202020204.0low000010
Exanthem0201820186.0low000010
Exanthema0201820186.0low000010
Experimental Lung Inflammation0201920195.0low000010
Extravascular Hemolysis0201620168.0low000010
Fatty Liver0202320231.0low000001
Fibrosis0202220222.0low000001
Folic Acid Deficiency0201920233.0low000011
Fungemia0201920195.0low000010
Gastric Outlet Obstruction0201920195.0low000010
Genetic Predisposition0201720177.0low000010
Great Pox0202020204.0low000020
Headache02010201610.3low100120
Hemolysis0201620168.0low000010
Hepatic Failure0201720177.0low000010
Hepatitis B0202020204.0low000010
Hepatitis B Virus Infection0202020204.0low000010
Hepatitis C0201220236.2low200051
Hepatitis C, Chronic0201620235.5low100031
Hepatitis, Viral, Human0201520159.0low000010
Hepatitis, Viral, Non-A, Non-B, Parenterally-Transmitted0201220236.2low200051
Histoplasma capsulatum Infection0201920195.0low000010
Histoplasmosis0201920195.0low000010
HIV0201320235.0low70002813
HIV Coinfection0201120234.8high148000589321
HIV Infections1201120234.8high148000589321
HIV Lipodystrophy Syndrome0201820186.0low000010
HIV-Associated Lipodystrophy Syndrome0201820186.0low000010
Hyperglycemia0201820232.8low000024
Hyperglycemia, Postprandial0201820232.8low000024
Hyperlactatemia0201720186.5low000020
Hyperthyroid0201720177.0low000010
Hyperthyroidism0201720177.0low000010
Hypertrophy0202220222.0low000001
Hypocalcemia0201920195.0low000010
Hypoxia0202220222.0low000001
Immune Reconstitution Disease0201520215.8low000031
Impotence0202020204.0low000010
Infection, Mycobacterium avium-intracellulare0202020223.0low000011
Infections, Coronavirus0202020204.0low000020
Infections, Plasmodium0202220222.0low200002
Inflammation0201820232.8low100035
Innate Inflammatory Response0201820232.8low100035
Insulin Resistance0201920232.7low200036
Insulin Sensitivity0201920232.7low200036
Ischemic Stroke0202020204.0low000010
Joint Pain0202020204.0low000010
Kaposi Sarcoma0202020204.0low000030
Kidney Diseases0201720177.0low000010
Kidney Failure0201420178.5low100020
Kidney Failure, Chronic0201620196.2low100050
Koch's Disease0201820233.3low5000119
Latent Tuberculosis0201820232.7low100012
Leanness0202220231.5low100002
Liver Cirrhosis0201720177.0low000010
Liver Failure0201720177.0low000010
Liver Failure, Acute0201820186.0low000010
Liver Steatosis0202320231.0low000001
Long QT Syndrome02012201212.0low100010
Long Sleeper Syndrome0201820195.5low000020
Low Bone Density0202120213.0low000001
Lung Neoplasms0201620177.5low000020
Lymphedema0202020204.0low000010
Lymphocytic Colitis0201920195.0low000010
Lymphoma, Primary Effusion0201920195.0low000010
Malaria1202220222.0low200002
Malaria, Falciparum0202120213.0low000001
Menopause0202120213.0low000001
Mental Disorders0201520206.1low000080
Metabolic Syndrome0202120213.0low100001
Mitral Incompetence0201720177.0low000010
Mitral Valve Insufficiency0201720177.0low000010
Mood Disorders0201520206.5low000020
Morbid Obesity0202020204.0low000010
Mycobacterium avium-intracellulare Infection0202020223.0low000011
Myelopathy0202020204.0low000010
Myocardial Infarction0202020204.0low000010
Myocarditis0201620196.5low000020
Nausea0202020204.0low000010
Neoplasms0201720177.0low000010
Nervous System Diseases0201820195.5low000020
Nervous System Disorders0201820195.5low000020
Neural Tube Defects0201820234.5low0000176
Neurodevelopmental Disorders0202120213.0low000001
Obesity0201920214.0low100011
Obesity, Morbid0202020204.0low000010
Opioid-Related Disorders02013201311.0low100010
Osteoporosis0201820186.0low100010
P carinii Pneumonia0201620168.0low000010
Pain0202220222.0low000001
Plasmodium falciparum Malaria0202120213.0low000001
Pneumonia0201920195.0low000010
Pneumonia, Pneumocystis0201620168.0low000010
Pneumonia, Viral0202020204.0low000020
Postoperative Complications0202020204.0low000010
Pregnancy0201520234.3low120005731
Premature Birth0201920223.5low000011
Preterm Birth0201920223.5low000011
Prostatic Neoplasms0202220231.5low000002
Proteinuria0201720177.0low000010
Psychoses, Drug0201720186.5low000020
Recrudescence0201620168.0low000010
Renal Insufficiency0201420178.5low100020
Renal Insufficiency, Chronic0201620225.7low000021
Respiration Disorders0201520159.0low000010
Sarcoma, Kaposi0202020204.0low000030
Seizures0201920204.5low000020
Sensitivity and Specificity0201420188.0low000020
Skin Neoplasms0202020204.0low000020
Sleep Initiation and Maintenance Disorders0201520187.2low000060
Sleep Wake Disorders0201820195.5low000020
Spinal Cord Diseases0202020204.0low000010
Stillbirth0201920214.0low000011
Stomach Neoplasms0201920195.0low000010
Stroke0201720177.0low000010
Substance Withdrawal Syndrome02013201311.0low100010
Substance-Related Disorders0202120213.0low000001
Suicidal Ideation0201720205.5low000020
Syphilis0202020204.0low000020
Teratogenesis0201820186.0low000010
Thrombocytopenia0201720177.0low000010
Thrombopenia0201720177.0low000010
Toxoplasmosis, Cerebral0201720177.0low000010
Trypanosomiasis, African0201720177.0low000010
Tuberculosis0201820233.3low5000119
Tuberculosis, Drug-Resistant0202120213.0low000001
Tuberculosis, Multidrug-Resistant0202120213.0low000001
Uveitis0202020204.0low000010
Vaccine Preventable Diseases0201920195.0low000020
Viral Hepatitis, Human0201520159.0low000010
Viremia0201520233.5low300058
Weight Gain0201220233.3low40001521
Zika Virus Infection0202020204.0low000010

Safety/Toxicity (90)

ArticleYear
Efficacy and safety profiles of dolutegravir plus lamivudine vs . bictegravir/emtricitabine/tenofovir alafenamide in therapy-naïve adults with HIV-1.
Chinese medical journal, , Nov-20, Volume: 136, Issue:22
2023
Effectiveness, durability and safety of dolutegravir and lamivudine versus bictegravir, emtricitabine and tenofovir alafenamide in a real-world cohort of HIV-infected adults.
PloS one, , Volume: 18, Issue:9
2023
Metabolic implications and safety of dolutegravir use in pregnancy.
The lancet. HIV, , Volume: 10, Issue:9
2023
Safety and Efficacy of Triple Therapy With Dolutegravir Plus 2 Nucleoside Reverse Transcriptase Inhibitors in Treatment-Naive Human Immunodeficiency Virus Type 2 Patients: Results From a 48-Week Phase 2 Study.
Clinical infectious diseases : an official publication of the Infectious Diseases Society of America, , 09-11, Volume: 77, Issue:5
2023
Efficacy and safety of pan-genotypic sofosbuvir and velpatasvir in patients with hepatitis C and HIV coinfection on dolutegravir-based antiretroviral therapy.
Journal of viral hepatitis, , Volume: 30, Issue:9
2023
Efficacy and Safety of Two-Drug Regimens with Dolutegravir plus Rilpivirine or Lamivudine in HIV-1 Virologically Suppressed People Living with HIV.
Viruses, , 04-10, Volume: 15, Issue:4
2023
Efficacy and safety of dolutegravir/rilpivirine in real-world clinical practice. GeSIDA study 1119.
HIV medicine, , Volume: 24, Issue:8
2023
An indirect comparison of 144-week efficacy, safety, and tolerability of dolutegravir plus lamivudine and second-generation integrase inhibitor-based, 3-drug, single-tablet regimens in therapy-naive people with HIV-1.
AIDS research and therapy, , 03-22, Volume: 20, Issue:1
2023
Safety and Effectiveness Analyses of Dolutegravir/Lamivudine in Patients with HIV: 2-Year Report of Post-Marketing Surveillance in Japan.
Advances in therapy, , Volume: 40, Issue:4
2023
Real-World Effectiveness, Tolerability, and Safety of Dolutegravir/Lamivudine in Korea.
Viruses, , 11-18, Volume: 14, Issue:11
2022
Effectiveness and safety of dolutegravir and raltegravir for treating children and adolescents living with HIV: a systematic review.
Journal of the International AIDS Society, , Volume: 25, Issue:11
2022
Prevalence of neuropsychiatric adverse events and associated factors among adult patients on dolutegravir attending Mulago ISS clinic.
HIV medicine, , Volume: 24, Issue:4
2023
Real-world efficacy and safety of dolutegravir plus lamivudine versus tenofovir plus lamivudine and efavirenz in ART-naïve HIV-1-infected adults.
Medicine, , Oct-21, Volume: 101, Issue:42
2022
Efficacy and Safety of a Simplified Lamivudine Plus Dolutegravir Dual Therapy in HIV-1-Infected Patients: A Multicenter Cohort Study in China.
Journal of acquired immune deficiency syndromes (1999), , 10-01, Volume: 91, Issue:S1
2022
Effectiveness and Safety of Dolutegravir Versus Efavirenz-Based Antiviral Regimen in People Living With HIV-1 in Sichuan Province of China: A Real-World Study.
Journal of acquired immune deficiency syndromes (1999), , 10-01, Volume: 91, Issue:S1
2022
Pharmacokinetic and pharmacogenetic associations with dolutegravir neuropsychiatric adverse events in an African population.
The Journal of antimicrobial chemotherapy, , 10-28, Volume: 77, Issue:11
2022
Brief Report: Efficacy and Safety of Efavirenz, Raltegravir, and Dolutegravir in HIV-1/TB Coinfection. A Multicenter Retrospective Cohort Study in France.
Journal of acquired immune deficiency syndromes (1999), , 09-01, Volume: 91, Issue:1
2022
Active Pharmacovigilance Project on the safety profile of Dolutegravir in Brazil.
AIDS care, , Volume: 35, Issue:5
2023
Pharmacokinetics, safety, tolerability, and antiviral activity of dolutegravir dispersible tablets in infants and children with HIV-1 (IMPAACT P1093): results of an open-label, phase 1-2 trial.
The lancet. HIV, , Volume: 9, Issue:5
2022
Efficacy and safety of dolutegravir or darunavir in combination with lamivudine plus either zidovudine or tenofovir for second-line treatment of HIV infection (NADIA): week 96 results from a prospective, multicentre, open-label, factorial, randomised, non
The lancet. HIV, , Volume: 9, Issue:6
2022
Efficacy and Safety of Switching to the 2-Drug Regimen Dolutegravir/Lamivudine Versus Continuing a 3- or 4-Drug Regimen for Maintaining Virologic Suppression in Adults Living With Human Immunodeficiency Virus 1 (HIV-1): Week 48 Results From the Phase 3, N
Clinical infectious diseases : an official publication of the Infectious Diseases Society of America, , 02-18, Volume: 76, Issue:4
2023
Efficacy and Safety of Switching to Dolutegravir/Lamivudine Versus Continuing a Tenofovir Alafenamide-Based 3- or 4-Drug Regimen for Maintenance of Virologic Suppression in Adults Living With Human Immunodeficiency Virus Type 1: Results Through Week 144 F
Clinical infectious diseases : an official publication of the Infectious Diseases Society of America, , 09-29, Volume: 75, Issue:6
2022
Dolutegravir Impairs Stem Cell-Based 3D Morphogenesis Models in a Manner Dependent on Dose and Timing of Exposure: An Implication for Its Developmental Toxicity.
Toxicological sciences : an official journal of the Society of Toxicology, , 11-24, Volume: 184, Issue:2
2021
Protocol for active safety monitoring of a cohort of patients using a dolutegravir-based antiretroviral regimen in Mozambique.
BMJ open, , 09-07, Volume: 11, Issue:9
2021
Efficacy and safety of switching to dolutegravir plus lamivudine versus continuing triple antiretroviral therapy in virologically suppressed adults with HIV at 48 weeks (DOLAM): a randomised non-inferiority trial.
The lancet. HIV, , Volume: 8, Issue:8
2021
Effectiveness, Durability, and Safety of Dolutegravir and Lamivudine Versus Dolutegravir, Lamivudine, and Abacavir in a Real-Life Cohort of HIV-Infected Adults.
The Annals of pharmacotherapy, , Volume: 56, Issue:4
2022
Safety and Effectiveness Analysis of Dolutegravir in Patients with HIV-1: Interim Report of Post-Marketing Surveillance in Japan.
Advances in therapy, , Volume: 38, Issue:8
2021
Efficacy and Safety of Triple versus Dolutegravir-based Dual Therapy in Patients with HIV-1 Infection: A Meta-analysis of Randomized Controlled Trials.
AIDS reviews, , 06-03, Volume: 23, Issue:3
2021
Efficacy and safety of dolutegravir with emtricitabine and tenofovir alafenamide fumarate or tenofovir disoproxil fumarate, and efavirenz, emtricitabine, and tenofovir disoproxil fumarate HIV antiretroviral therapy regimens started in pregnancy (IMPAACT 2
Lancet (London, England), , 04-03, Volume: 397, Issue:10281
2021
ODYSSEY clinical trial design: a randomised global study to evaluate the efficacy and safety of dolutegravir-based antiretroviral therapy in HIV-positive children, with nested pharmacokinetic sub-studies to evaluate pragmatic WHO-weight-band based doluteg
BMC infectious diseases, , Jan-04, Volume: 21, Issue:1
2021
Longitudinal trends and determinants of patient-reported side effects on ART-a Swedish national registry study.
PloS one, , Volume: 15, Issue:12
2020
Efficacy and safety of dolutegravir plus emtricitabine versus standard ART for the maintenance of HIV-1 suppression: 48-week results of the factorial, randomized, non-inferiority SIMPL'HIV trial.
PLoS medicine, , Volume: 17, Issue:11
2020
Discontinuation due to neuropsychiatric adverse events with efavirenz- and dolutegravir-based antiretroviral therapy: a comparative real-life study.
European journal of hospital pharmacy : science and practice, , Volume: 29, Issue:4
2022
Nothing is perfect: the safety issues of integrase inhibitor regimens.
Expert opinion on drug safety, , Volume: 19, Issue:6
2020
Neuropsychiatric adverse effects of dolutegravir in real-life clinical practice.
Enfermedades infecciosas y microbiologia clinica (English ed.), , Volume: 39, Issue:2
2021
Pharmacokinetics, SAfety/tolerability, and EFficacy of high-dose RIFampicin in tuberculosis-HIV co-infected patients on efavirenz- or dolutegravir-based antiretroviral therapy: study protocol for an open-label, phase II clinical trial (SAEFRIF).
Trials, , Feb-13, Volume: 21, Issue:1
2020
Efficacy and Safety of Switching to Dolutegravir/Lamivudine Fixed-Dose 2-Drug Regimen vs Continuing a Tenofovir Alafenamide-Based 3- or 4-Drug Regimen for Maintenance of Virologic Suppression in Adults Living With Human Immunodeficiency Virus Type 1: Phas
Clinical infectious diseases : an official publication of the Infectious Diseases Society of America, , 11-05, Volume: 71, Issue:8
2020
Absence of developmental and reproductive toxicity in animals exposed to dolutegravir.
Birth defects research, , 02-01, Volume: 112, Issue:3
2020
Analysis of Pharmacovigilance Databases for Dolutegravir Safety in Pregnancy.
Clinical infectious diseases : an official publication of the Infectious Diseases Society of America, , 06-10, Volume: 70, Issue:12
2020
Safety and pharmacokinetics of dolutegravir in pregnant mothers with HIV infection and their neonates: A randomised trial (DolPHIN-1 study).
PLoS medicine, , Volume: 16, Issue:9
2019
Two-drug regimens with dolutegravir plus rilpivirine or lamivudine in HIV-1 treatment-naïve, virologically-suppressed patients: Latest evidence from the literature on their efficacy and safety.
Journal of global antimicrobial resistance, , Volume: 20
2020
DOLAMA study: Effectiveness, safety and pharmacoeconomic analysis of dual therapy with dolutegravir and lamivudine in virologically suppressed HIV-1 patients.
Medicine, , Volume: 98, Issue:32
2019
Safety and efficacy of elvitegravir, dolutegravir, and raltegravir in a real-world cohort of treatment-naïve and -experienced patients.
Medicine, , Volume: 98, Issue:32
2019
Dual therapy with renally adjusted lamivudine and dolutegravir: a switch strategy to manage comorbidity and toxicity in older, suppressed patients?
HIV medicine, , Volume: 20, Issue:9
2019
Efficacy and safety of dolutegravir-rilpivirine for maintenance of virological suppression in adults with HIV-1: 100-week data from the randomised, open-label, phase 3 SWORD-1 and SWORD-2 studies.
The lancet. HIV, , Volume: 6, Issue:9
2019
Optimizing responses to drug safety signals in pregnancy: the example of dolutegravir and neural tube defects.
Journal of the International AIDS Society, , Volume: 22, Issue:7
2019
Efficacy and safety of dolutegravir-based regimens in advanced HIV-infected naïve patients: results from a multicenter cohort study.
Antiviral research, , Volume: 169
2019
The antagonism of folate receptor by dolutegravir: developmental toxicity reduction by supplemental folic acid.
AIDS (London, England), , 11-01, Volume: 33, Issue:13
2019
Comparative efficacy and safety and dolutegravir and lamivudine in treatment naive HIV patients.
AIDS (London, England), , 09-01, Volume: 33, Issue:11
2019
Efficacy and safety of dolutegravir plus boosted-darunavir dual therapy among highly treatment-experienced patients.
Antiviral therapy, , Volume: 24, Issue:6
2019
Increasing levels of pretreatment HIV drug resistance and safety concerns for dolutegravir use in women of reproductive age.
AIDS (London, England), , 09-01, Volume: 33, Issue:11
2019
Similar efficacy and safety of dolutegravir between age groups of HIV-1-infected paediatric and young adult patients aged 5 years and older.
HIV medicine, , Volume: 20, Issue:8
2019
Safety and efficacy of dolutegravir in hemodialysis.
International journal of STD & AIDS, , Volume: 30, Issue:6
2019
Is There a Safety Signal for Dolutegravir and Integrase Inhibitors During Pregnancy?
Journal of acquired immune deficiency syndromes (1999), , 08-01, Volume: 81, Issue:4
2019
Long-Term Safety and Efficacy of Dolutegravir in Treatment-Experienced Adolescents With Human Immunodeficiency Virus Infection: Results of the IMPAACT P1093 Study.
Journal of the Pediatric Infectious Diseases Society, , Apr-30, Volume: 9, Issue:2
2020
Neuropsychiatric Adverse Events with Dolutegravir and Other Integrase Strand Transfer Inhibitors
AIDS reviews, , Volume: 21, Issue:1
2019
Discontinuation of dolutegravir, elvitegravir/cobicistat and raltegravir because of toxicity in a prospective cohort.
HIV medicine, , Volume: 20, Issue:3
2019
Integrase strand transfer inhibitors and neuropsychiatric adverse events in a large prospective cohort.
The Journal of antimicrobial chemotherapy, , 03-01, Volume: 74, Issue:3
2019
Tryptophan metabolism and its relationship with central nervous system toxicity in people living with HIV switching from efavirenz to dolutegravir.
Journal of neurovirology, , Volume: 25, Issue:1
2019
Efficacy and safety of switching to dolutegravir plus emtricitabine/tenofovir disoproxil fumarate (TDF) or elvitegravir/cobicistat/emtricitabine/TDF in virologically suppressed HIV-infected patients in clinical practice: results from a multicentre, observ
HIV medicine, , Volume: 20, Issue:2
2019
Efficacy and safety of the switch of Triumeq® to generic (abacavir + lamivudine) + Tivicay®: data at 24 weeks.
BMC pharmacology & toxicology, , Oct-10, Volume: 19, Issue:1
2018
Safety, Tolerability, and Efficacy of Generic Dolutegravir-containing Antiretroviral Therapy Regimens Among South Indian Human Immunodeficiency Virus-infected Patients.
Clinical infectious diseases : an official publication of the Infectious Diseases Society of America, , 03-05, Volume: 68, Issue:6
2019
Comparative safety of dolutegravir-based or efavirenz-based antiretroviral treatment started during pregnancy in Botswana: an observational study.
The Lancet. Global health, , Volume: 6, Issue:7
2018
Dolutegravir Neuropsychiatric Adverse Events: Specific Drug Effect or Class Effect.
AIDS reviews, , Volume: 20, Issue:1
Dolutegravir-based anti-retroviral therapy is effective and safe in HIV-infected paediatric patients.
Italian journal of pediatrics, , Mar-20, Volume: 44, Issue:1
2018
Safety and Efficacy of Dolutegravir Plus Rilpivirine in Treatment-Experienced HIV-Infected Patients: The DORIVIR Study.
Journal of the International Association of Providers of AIDS Care, , Volume: 17
Dolutegravir-Related Neurological Adverse Events: A Case Report of Successful Management with Therapeutic Drug Monitoring.
Current drug safety, , Volume: 13, Issue:1
2018
Efficacy, safety, and tolerability of dolutegravir-rilpivirine for the maintenance of virological suppression in adults with HIV-1: phase 3, randomised, non-inferiority SWORD-1 and SWORD-2 studies.
Lancet (London, England), , 03-03, Volume: 391, Issue:10123
2018
Risks of cardiovascular or central nervous system adverse events and immune reconstitution inflammatory syndrome, for dolutegravir versus other antiretrovirals: meta-analysis of randomized trials.
Current opinion in HIV and AIDS, , Volume: 13, Issue:2
2018
Impact of UGT1A1 gene polymorphisms on plasma dolutegravir trough concentrations and neuropsychiatric adverse events in Japanese individuals infected with HIV-1.
BMC infectious diseases, , 09-16, Volume: 17, Issue:1
2017
Effectiveness, Safety, and Costs of a Treatment Switch to Dolutegravir Plus Rilpivirine Dual Therapy in Treatment-Experienced HIV Patients.
The Annals of pharmacotherapy, , Volume: 52, Issue:1
2018
Adverse events of raltegravir and dolutegravir.
AIDS (London, England), , 08-24, Volume: 31, Issue:13
2017
Clinical Experience with the Integrase Inhibitors Dolutegravir and Elvitegravir in HIV-infected Patients: Efficacy, Safety and Tolerance.
Basic & clinical pharmacology & toxicology, , Volume: 121, Issue:5
2017
Higher rates of neuropsychiatric adverse events leading to dolutegravir discontinuation in women and older patients.
HIV medicine, , Volume: 18, Issue:1
2017
Clinical experience with dolutegravir/abacavir/lamivudine in HIV-HCV co-infected patients treated with a sofosbuvir-based regimen-safety and efficacy.
HIV clinical trials, , Volume: 17, Issue:6
2016
Comparative efficacy and safety of first-line antiretroviral therapy for the treatment of HIV infection: a systematic review and network meta-analysis.
The lancet. HIV, , Volume: 3, Issue:11
2016
An Indirect Comparison of Efficacy and Safety of Elvitegravir/Cobicistat/Emtricitabine/Tenofovir Disoproxil Fumarate and Abacavir/Lamivudine + Dolutegravir in Initial Therapy.
PloS one, , Volume: 11, Issue:5
2016
Safety, Pharmacokinetics and Efficacy of Dolutegravir in Treatment-experienced HIV-1 Infected Adolescents: Forty-eight-week Results from IMPAACT P1093.
The Pediatric infectious disease journal, , Volume: 34, Issue:11
2015
A two-week regimen of high-dose integrase inhibitors does not cause nephrotoxicity in mice.
Antiviral chemistry & chemotherapy, , Volume: 24, Issue:2
2015
Dolutegravir - a review of the pharmacology, efficacy, and safety in the treatment of HIV.
Drug design, development and therapy, , Volume: 9
2015
[Safety profile of dolutegravir].
Enfermedades infecciosas y microbiologia clinica, , Volume: 33 Suppl 1
2015
Dolutegravir: clinical and laboratory safety in integrase inhibitor-naive patients.
HIV clinical trials, , Volume: 15, Issue:5
Evaluation of dolutegravir safety for the treatment of HIV-1.
Expert opinion on drug safety, , Volume: 14, Issue:1
2015
48-week efficacy and safety of dolutegravir relative to commonly used third agents in treatment-naive HIV-1-infected patients: a systematic review and network meta-analysis.
PloS one, , Volume: 9, Issue:9
2014
[Pharmacokinetics and safety of dolutegravir in healthy Japanese subjects].
The Japanese journal of antibiotics, , Volume: 66, Issue:1
2013
Hepatoxicity of new antiretrovirals: a systematic review.
Clinics and research in hepatology and gastroenterology, , Volume: 37, Issue:2
2013
Safety and efficacy of dolutegravir in treatment-experienced subjects with raltegravir-resistant HIV type 1 infection: 24-week results of the VIKING Study.
The Journal of infectious diseases, , Mar-01, Volume: 207, Issue:5
2013
Assessing a theoretical risk of dolutegravir-induced developmental immunotoxicity in juvenile rats.
Toxicological sciences : an official journal of the Society of Toxicology, , Volume: 130, Issue:1
2012
Antiviral activity, safety, and pharmacokinetics/pharmacodynamics of dolutegravir as 10-day monotherapy in HIV-1-infected adults.
AIDS (London, England), , Sep-10, Volume: 25, Issue:14
2011
Pharmacokinetics and safety of S/GSK1349572, a next-generation HIV integrase inhibitor, in healthy volunteers.
Antimicrobial agents and chemotherapy, , Volume: 54, Issue:1
2010

Long-term Use (3)

ArticleYear
Dolutegravir 50 mg thrice weekly plus atazanavir 400 mg daily in a long-term virologically suppressed HIV-infected patient.
International journal of STD & AIDS, , Volume: 28, Issue:7
2017
Comparative changes of lipid levels in treatment-naive, HIV-1-infected adults treated with dolutegravir vs. efavirenz, raltegravir, and ritonavir-boosted darunavir-based regimens over 48 weeks.
Clinical drug investigation, , Volume: 35, Issue:3
2015
Addition of E138K to R263K in HIV integrase increases resistance to dolutegravir, but fails to restore activity of the HIV integrase enzyme and viral replication capacity.
The Journal of antimicrobial chemotherapy, , Volume: 69, Issue:10
2014

Pharmacokinetics (69)

ArticleYear
Effect of dolutegravir on folate, vitamin B12 and mean corpuscular volume levels among children and adolescents with HIV: a sub-study of the ODYSSEY randomized controlled trial.
Journal of the International AIDS Society, , Volume: 26, Issue:9
2023
Population Pharmacokinetic Modeling of Dolutegravir to Optimize Pediatric Dosing in HIV-1-Infected Infants, Children, and Adolescents.
Clinical pharmacokinetics, , Volume: 62, Issue:10
2023
First Pharmacokinetic Data of Tenofovir Alafenamide Fumarate and Tenofovir With Dolutegravir or Boosted Protease Inhibitors in African Children: A Substudy of the CHAPAS-4 Trial.
Clinical infectious diseases : an official publication of the Infectious Diseases Society of America, , 09-18, Volume: 77, Issue:6
2023
Pharmacokinetic Data of Dolutegravir in Second-line Treatment of Children With Human Immunodeficiency Virus: Results From the CHAPAS4 Trial.
Clinical infectious diseases : an official publication of the Infectious Diseases Society of America, , 11-11, Volume: 77, Issue:9
2023
Pharmacokinetics and pharmacodynamics of adult dolutegravir tablets in treatment-experienced children with HIV weighing at least 20 kg.
AIDS (London, England), , 07-15, Volume: 37, Issue:9
2023
Population pharmacokinetics of unbound and total dolutegravir concentrations in children aged 12 years and older: a PK substudy of the SMILE trial.
The Journal of antimicrobial chemotherapy, , 04-03, Volume: 78, Issue:4
2023
Pharmacokinetic and pharmacogenetic associations with dolutegravir neuropsychiatric adverse events in an African population.
The Journal of antimicrobial chemotherapy, , 10-28, Volume: 77, Issue:11
2022
Pharmacokinetics, safety, tolerability, and antiviral activity of dolutegravir dispersible tablets in infants and children with HIV-1 (IMPAACT P1093): results of an open-label, phase 1-2 trial.
The lancet. HIV, , Volume: 9, Issue:5
2022
Pharmacokinetics and tissue distribution of tenofovir, emtricitabine and dolutegravir in mice.
The Journal of antimicrobial chemotherapy, , 03-31, Volume: 77, Issue:4
2022
Pharmacokinetic features of dolutegravir with rifampicin and rifabutin among patients coinfected with human immunodeficiency virus and tuberculosis/mycobacterium avium complex.
International journal of infectious diseases : IJID : official publication of the International Society for Infectious Diseases, , Volume: 116
2022
Optimizing Dolutegravir Initiation in Neonates Using Population Pharmacokinetic Modeling and Simulation.
Journal of acquired immune deficiency syndromes (1999), , 01-01, Volume: 89, Issue:1
2022
Pharmacokinetics and placental transfer of dolutegravir in pregnancy.
The Journal of antimicrobial chemotherapy, , 02-02, Volume: 77, Issue:2
2022
Ultra-long acting prodrug of dolutegravir and delivery system - Physicochemical, pharmacokinetic and formulation characterizations.
International journal of pharmaceutics, , Sep-25, Volume: 607
2021
Point-of-Care Detection of Nonadherence to Antiretroviral Treatment for HIV-1 in Resource-Limited Settings Using Drug Level Testing for Efavirenz, Lopinavir, and Dolutegravir: A Validation and Pharmacokinetic Simulation Study.
Journal of acquired immune deficiency syndromes (1999), , 08-01, Volume: 87, Issue:4
2021
Pharmacokinetic parameters and weight change in HIV patients newly switched to dolutegravir-based regimens in SIMPL'HIV clinical trial.
British journal of clinical pharmacology, , Volume: 87, Issue:11
2021
Dolutegravir pharmacokinetics during co-administration with either artemether/lumefantrine or artesunate/amodiaquine.
The Journal of antimicrobial chemotherapy, , 04-13, Volume: 76, Issue:5
2021
Phase I evaluation of pharmacokinetics and tolerability of the HIV-1 maturation inhibitor GSK3640254 and dolutegravir in healthy adults.
British journal of clinical pharmacology, , Volume: 87, Issue:9
2021
Physiologically Based Pharmacokinetic Modeling Framework to Predict Neonatal Pharmacokinetics of Transplacentally Acquired Emtricitabine, Dolutegravir, and Raltegravir.
Clinical pharmacokinetics, , Volume: 60, Issue:6
2021
ODYSSEY clinical trial design: a randomised global study to evaluate the efficacy and safety of dolutegravir-based antiretroviral therapy in HIV-positive children, with nested pharmacokinetic sub-studies to evaluate pragmatic WHO-weight-band based doluteg
BMC infectious diseases, , Jan-04, Volume: 21, Issue:1
2021
Infant Exposure to Dolutegravir Through Placental and Breast Milk Transfer: A Population Pharmacokinetic Analysis of DolPHIN-1.
Clinical infectious diseases : an official publication of the Infectious Diseases Society of America, , 09-07, Volume: 73, Issue:5
2021
Prediction of Maternal and Fetal Pharmacokinetics of Dolutegravir and Raltegravir Using Physiologically Based Pharmacokinetic Modeling.
Clinical pharmacokinetics, , Volume: 59, Issue:11
2020
The effect of veno-arterial extracorporeal oxygenation and nasogastric tube administration on the pharmacokinetic profile of abacavir, lamivudine and dolutegravir: a case report.
Antiviral therapy, , Volume: 25, Issue:2
2020
ABCG2 Deficiency Does Not Alter Dolutegravir Metabolism and Pharmacokinetics.
The Journal of pharmacology and experimental therapeutics, , Volume: 374, Issue:1
2020
The Effect of Pregnancy on the Pharmacokinetics of Total and Unbound Dolutegravir and Its Main Metabolite in Women Living With Human Immunodeficiency Virus.
Clinical infectious diseases : an official publication of the Infectious Diseases Society of America, , 01-23, Volume: 72, Issue:1
2021
Pharmacokinetics, SAfety/tolerability, and EFficacy of high-dose RIFampicin in tuberculosis-HIV co-infected patients on efavirenz- or dolutegravir-based antiretroviral therapy: study protocol for an open-label, phase II clinical trial (SAEFRIF).
Trials, , Feb-13, Volume: 21, Issue:1
2020
Genetic influence of ABCG2, UGT1A1 and NR1I2 on dolutegravir plasma pharmacokinetics.
The Journal of antimicrobial chemotherapy, , 05-01, Volume: 75, Issue:5
2020
Assessment of Maternal and Fetal Dolutegravir Exposure by Integrating Ex Vivo Placental Perfusion Data and Physiologically-Based Pharmacokinetic Modeling.
Clinical pharmacology and therapeutics, , Volume: 107, Issue:6
2020
Prediction of dolutegravir pharmacokinetics and dose optimization in neonates via physiologically based pharmacokinetic (PBPK) modelling.
The Journal of antimicrobial chemotherapy, , 03-01, Volume: 75, Issue:3
2020
Safety and pharmacokinetics of dolutegravir in pregnant mothers with HIV infection and their neonates: A randomised trial (DolPHIN-1 study).
PLoS medicine, , Volume: 16, Issue:9
2019
Pharmacokinetic profiles of boosted darunavir, dolutegravir and lamivudine in aging people living with HIV.
AIDS (London, England), , 01-01, Volume: 34, Issue:1
2020
Population pharmacokinetics of dolutegravir: influence of drug-drug interactions in a real-life setting.
The Journal of antimicrobial chemotherapy, , 09-01, Volume: 74, Issue:9
2019
Dolutegravir Population Pharmacokinetics in a Real-Life Cohort of People Living With HIV Infection: A Covariate Analysis.
Therapeutic drug monitoring, , Volume: 41, Issue:4
2019
Pharmacokinetics of dolutegravir with and without darunavir/cobicistat in healthy volunteers.
The Journal of antimicrobial chemotherapy, , 01-01, Volume: 74, Issue:1
2019
Pharmacokinetics of HIV-Integrase Inhibitors During Pregnancy: Mechanisms, Clinical Implications and Knowledge Gaps.
Clinical pharmacokinetics, , Volume: 58, Issue:3
2019
Increased Dolutegravir Peak Concentrations in People Living With Human Immunodeficiency Virus Aged 60 and Over, and Analysis of Sleep Quality and Cognition.
Clinical infectious diseases : an official publication of the Infectious Diseases Society of America, , 01-01, Volume: 68, Issue:1
2019
Dolutegravir pharmacokinetics in pregnant and postpartum women living with HIV.
AIDS (London, England), , 03-27, Volume: 32, Issue:6
2018
Clinical benefits of using inulin clearance and cystatin C for determining glomerular filtration rate in HIV-1-infected individuals treated with dolutegravir.
Journal of infection and chemotherapy : official journal of the Japan Society of Chemotherapy, , Volume: 24, Issue:3
2018
Pregnancy-related changes of antiretroviral pharmacokinetics: an argument for therapeutic drug monitoring.
Antiviral therapy, , Volume: 22, Issue:4
2017
How recent findings on the pharmacokinetics and pharmacodynamics of integrase inhibitors can inform clinical use.
Current opinion in infectious diseases, , Volume: 30, Issue:1
2017
A Two-Way Steady-State Pharmacokinetic Interaction Study of Doravirine (MK-1439) and Dolutegravir.
Clinical pharmacokinetics, , Volume: 56, Issue:6
2017
Simultaneous quantification of tenofovir, emtricitabine, rilpivirine, elvitegravir and dolutegravir in mouse biological matrices by LC-MS/MS and its application to a pharmacokinetic study.
Journal of pharmaceutical and biomedical analysis, , Sep-10, Volume: 129
2016
No clinically significant pharmacokinetic interactions between dolutegravir and daclatasvir in healthy adult subjects.
BMC infectious diseases, , 07-22, Volume: 16
2016
The Effect of Dolutegravir on the Pharmacokinetics of Metformin in Healthy Subjects.
Journal of acquired immune deficiency syndromes (1999), , 08-01, Volume: 72, Issue:4
2016
Effect of carbamazepine on dolutegravir pharmacokinetics and dosing recommendation.
European journal of clinical pharmacology, , Volume: 72, Issue:6
2016
Influence of nevirapine administration on the pharmacokinetics of dolutegravir in patients infected with HIV-1.
The Journal of antimicrobial chemotherapy, , Volume: 70, Issue:12
2015
Safety, Pharmacokinetics and Efficacy of Dolutegravir in Treatment-experienced HIV-1 Infected Adolescents: Forty-eight-week Results from IMPAACT P1093.
The Pediatric infectious disease journal, , Volume: 34, Issue:11
2015
[The in vitro HAART pharmacodynamics study with dolutegravir as the "anchor"].
Yao xue xue bao = Acta pharmaceutica Sinica, , Volume: 50, Issue:1
2015
Dolutegravir Has No Effect on the Pharmacokinetics of Oral Contraceptives With Norgestimate and Ethinyl Estradiol.
The Annals of pharmacotherapy, , Volume: 49, Issue:7
2015
Pharmacokinetics of dolutegravir in a premature neonate after HIV treatment intensification during pregnancy.
Antimicrobial agents and chemotherapy, , Volume: 59, Issue:6
2015
Population pharmacokinetics of dolutegravir in HIV-infected treatment-naive patients.
British journal of clinical pharmacology, , Volume: 80, Issue:3
2015
Pharmacokinetic profile of raltegravir, elvitegravir and dolutegravir in plasma and mucosal secretions in rhesus macaques.
The Journal of antimicrobial chemotherapy, , Volume: 70, Issue:5
2015
Pharmacokinetics of dolutegravir when administered with mineral supplements in healthy adult subjects.
Journal of clinical pharmacology, , Volume: 55, Issue:5
2015
Effect of fosamprenavir-ritonavir on the pharmacokinetics of dolutegravir in healthy subjects.
Antimicrobial agents and chemotherapy, , Volume: 58, Issue:11
2014
Effects of enzyme inducers efavirenz and tipranavir/ritonavir on the pharmacokinetics of the HIV integrase inhibitor dolutegravir.
European journal of clinical pharmacology, , Volume: 70, Issue:10
2014
Effects of boceprevir and telaprevir on the pharmacokinetics of dolutegravir.
British journal of clinical pharmacology, , Volume: 78, Issue:5
2014
Evaluation of the effect of UGT1A1 polymorphisms on dolutegravir pharmacokinetics.
Pharmacogenomics, , Volume: 15, Issue:1
2014
Pharmacokinetics of dolutegravir in HIV-seronegative subjects with severe renal impairment.
European journal of clinical pharmacology, , Volume: 70, Issue:1
2014
Dolutegravir does not affect methadone pharmacokinetics in opioid-dependent, HIV-seronegative subjects.
Drug and alcohol dependence, , Dec-01, Volume: 133, Issue:2
2013
Lack of pharmacokinetic interaction between rilpivirine and integrase inhibitors dolutegravir and GSK1265744.
Antimicrobial agents and chemotherapy, , Volume: 57, Issue:11
2013
Dolutegravir pharmacokinetics in the genital tract and colorectum of HIV-negative men after single and multiple dosing.
Journal of acquired immune deficiency syndromes (1999), , Sep-01, Volume: 64, Issue:1
2013
Single and multiple dose pharmacokinetics of dolutegravir in the genital tract of HIV-negative women.
Antiviral therapy, , Volume: 18, Issue:8
2013
Clinical pharmacokinetic, pharmacodynamic and drug-interaction profile of the integrase inhibitor dolutegravir.
Clinical pharmacokinetics, , Volume: 52, Issue:11
2013
Effect of prednisone on the pharmacokinetics of the integrase inhibitor dolutegravir.
Antimicrobial agents and chemotherapy, , Volume: 57, Issue:9
2013
[Pharmacokinetics and safety of dolutegravir in healthy Japanese subjects].
The Japanese journal of antibiotics, , Volume: 66, Issue:1
2013
Safety, tolerability, and pharmacokinetics of the HIV integrase inhibitor dolutegravir given twice daily with rifampin or once daily with rifabutin: results of a phase 1 study among healthy subjects.
Journal of acquired immune deficiency syndromes (1999), , Jan-01, Volume: 62, Issue:1
2013
A phase 1 study to evaluate the effect of dolutegravir on renal function via measurement of iohexol and para-aminohippurate clearance in healthy subjects.
British journal of clinical pharmacology, , Volume: 75, Issue:4
2013
Antiviral activity, safety, and pharmacokinetics/pharmacodynamics of dolutegravir as 10-day monotherapy in HIV-1-infected adults.
AIDS (London, England), , Sep-10, Volume: 25, Issue:14
2011
Effect of atazanavir and atazanavir/ritonavir on the pharmacokinetics of the next-generation HIV integrase inhibitor, S/GSK1349572.
British journal of clinical pharmacology, , Volume: 72, Issue:1
2011
Pharmacokinetics and safety of S/GSK1349572, a next-generation HIV integrase inhibitor, in healthy volunteers.
Antimicrobial agents and chemotherapy, , Volume: 54, Issue:1
2010

Bioavailability (14)

ArticleYear
Development of Dolutegravir Single-entity and Fixed-dose Combination Formulations for Children.
The Pediatric infectious disease journal, , 03-01, Volume: 41, Issue:3
2022
Dolutegravir pharmacokinetics during co-administration with either artemether/lumefantrine or artesunate/amodiaquine.
The Journal of antimicrobial chemotherapy, , 04-13, Volume: 76, Issue:5
2021
Raltegravir, Indinavir, Tipranavir, Dolutegravir, and Etravirine against main protease and RNA-dependent RNA polymerase of SARS-CoV-2: A molecular docking and drug repurposing approach.
Journal of infection and public health, , Volume: 13, Issue:12
2020
Investigation of drug-polymer miscibility, biorelevant dissolution, and bioavailability improvement of Dolutegravir-polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer solid dispersions.
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, , Jan-15, Volume: 142
2020
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Molecular pharmacology, , Volume: 96, Issue:5
2019
Low plasmatic concentration of intensified antiretroviral therapy in a pregnant woman: a case report.
Journal of medical case reports, , Jul-23, Volume: 13, Issue:1
2019
Population pharmacokinetics of dolutegravir: influence of drug-drug interactions in a real-life setting.
The Journal of antimicrobial chemotherapy, , 09-01, Volume: 74, Issue:9
2019
Effects of Low- and High-Mineral Content Water on the Relative Bioavailability of a Coformulated Abacavir/Dolutegravir/Lamivudine Dispersible Tablet in Healthy Adults.
Journal of acquired immune deficiency syndromes (1999), , 12-15, Volume: 79, Issue:5
2018
Relative Bioavailability of a Dolutegravir Dispersible Tablet and the Effects of Low- and High-Mineral-Content Water on the Tablet in Healthy Adults.
Clinical pharmacology in drug development, , Volume: 6, Issue:6
2017
Population pharmacokinetics of dolutegravir in HIV-infected treatment-naive patients.
British journal of clinical pharmacology, , Volume: 80, Issue:3
2015
The comparative disposition and metabolism of dolutegravir, a potent HIV-1 integrase inhibitor, in mice, rats, and monkeys.
Xenobiotica; the fate of foreign compounds in biological systems, , Volume: 45, Issue:1
2015
Relative bioavailability of a paediatric granule formulation of the HIV integrase inhibitor dolutegravir in healthy adult subjects.
Antiviral therapy, , Volume: 19, Issue:3
2014
Pharmacology of HIV integrase inhibitors.
Current opinion in HIV and AIDS, , Volume: 7, Issue:5
2012
Effect of food on the pharmacokinetics of the integrase inhibitor dolutegravir.
Antimicrobial agents and chemotherapy, , Volume: 56, Issue:3
2012

Dosage (98)

ArticleYear
Alternative dolutegravir dosing strategies with concurrent rifapentine utilized for latent tuberculosis treatment.
International journal of STD & AIDS, , Volume: 34, Issue:14
2023
A novel formulation enabled transformation of 3-HIV drugs tenofovir-lamivudine-dolutegravir from short-acting to long-acting all-in-one injectable.
AIDS (London, England), , 11-15, Volume: 37, Issue:14
2023
Population Pharmacokinetic Modeling of Dolutegravir to Optimize Pediatric Dosing in HIV-1-Infected Infants, Children, and Adolescents.
Clinical pharmacokinetics, , Volume: 62, Issue:10
2023
First Pharmacokinetic Data of Tenofovir Alafenamide Fumarate and Tenofovir With Dolutegravir or Boosted Protease Inhibitors in African Children: A Substudy of the CHAPAS-4 Trial.
Clinical infectious diseases : an official publication of the Infectious Diseases Society of America, , 09-18, Volume: 77, Issue:6
2023
Pharmacokinetic Data of Dolutegravir in Second-line Treatment of Children With Human Immunodeficiency Virus: Results From the CHAPAS4 Trial.
Clinical infectious diseases : an official publication of the Infectious Diseases Society of America, , 11-11, Volume: 77, Issue:9
2023
Standard-dose versus double-dose dolutegravir in HIV-associated tuberculosis in South Africa (RADIANT-TB): a phase 2, non-comparative, randomised controlled trial.
The lancet. HIV, , Volume: 10, Issue:7
2023
Initial Supplementary Dose of Dolutegravir in Second-Line Antiretroviral Therapy: A Noncomparative, Double-Blind, Randomized Placebo-Controlled Trial.
Clinical infectious diseases : an official publication of the Infectious Diseases Society of America, , 05-24, Volume: 76, Issue:10
2023
Inflammation and intracellular exposure of dolutegravir, darunavir, tenofovir and emtricitabine in people living with HIV.
British journal of clinical pharmacology, , Volume: 89, Issue:3
2023
Once-daily dolutegravir-based antiretroviral therapy in infants and children living with HIV from age 4 weeks: results from the below 14 kg cohort in the randomised ODYSSEY trial.
The lancet. HIV, , Volume: 9, Issue:9
2022
Effect of Rifabutin in Dolutegravir Dosing: A Case Series.
Journal of the International Association of Providers of AIDS Care, , Volume: 21
Real-world use and outcomes of dolutegravir-containing antiretroviral therapy in HIV and tuberculosis co-infection: a site survey and cohort study in sub-Saharan Africa.
Journal of the International AIDS Society, , Volume: 25, Issue:7
2022
Transformation of dolutegravir into an ultra-long-acting parenteral prodrug formulation.
Nature communications, , 06-09, Volume: 13, Issue:1
2022
Pharmacokinetics, safety, tolerability, and antiviral activity of dolutegravir dispersible tablets in infants and children with HIV-1 (IMPAACT P1093): results of an open-label, phase 1-2 trial.
The lancet. HIV, , Volume: 9, Issue:5
2022
South African healthcare workers' knowledge of dolutegravir's drug-drug interactions in the first year of its rollout: a cross-sectional online survey.
Journal of the International AIDS Society, , Volume: 25, Issue:3
2022
An eco- friendly, selective, and sensitive spectrofluorimetric method for the quantification of Dolutegravir in its bulk and tablet dosage form.
Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy, , May-15, Volume: 273
2022
Concentration-response relationships of dolutegravir and efavirenz with weight change after starting antiretroviral therapy.
British journal of clinical pharmacology, , Volume: 88, Issue:3
2022
Development and validation of ultra performance liquid chromatography-tandem mass spectrometry method for the simultaneous estimation of dolutegravir, lamivudine and tenofovir in bulk and tablet dosage form.
European journal of mass spectrometry (Chichester, England), , Volume: 27, Issue:6
2021
Development of Dolutegravir Single-entity and Fixed-dose Combination Formulations for Children.
The Pediatric infectious disease journal, , 03-01, Volume: 41, Issue:3
2022
Patient experiences of switching from Efavirenz- to Dolutegravir-based antiretroviral therapy: a qualitative study in Uganda.
BMC infectious diseases, , Nov-13, Volume: 21, Issue:1
2021
Validation and Clinical Application of a Liquid Chromatography-Ultraviolet Detection Method to Quantify Dolutegravir in Dried Blood Spots.
Therapeutic drug monitoring, , 06-01, Volume: 44, Issue:3
2022
Optimizing Dolutegravir Initiation in Neonates Using Population Pharmacokinetic Modeling and Simulation.
Journal of acquired immune deficiency syndromes (1999), , 01-01, Volume: 89, Issue:1
2022
Analysis of the ternary antiretroviral therapy dolutegravir, lamivudine and abacavir using UV spectrophotometry and chemometric tools.
Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy, , Jan-05, Volume: 264
2022
Dolutegravir in Mexico for special populations: A cost analysis perspective.
AIDS reviews, , 07-01, Volume: 23, Issue:3
2021
Phase I evaluation of pharmacokinetics and tolerability of the HIV-1 maturation inhibitor GSK3640254 and dolutegravir in healthy adults.
British journal of clinical pharmacology, , Volume: 87, Issue:9
2021
ODYSSEY clinical trial design: a randomised global study to evaluate the efficacy and safety of dolutegravir-based antiretroviral therapy in HIV-positive children, with nested pharmacokinetic sub-studies to evaluate pragmatic WHO-weight-band based doluteg
BMC infectious diseases, , Jan-04, Volume: 21, Issue:1
2021
Dolutegravir in pregnant mice is associated with increased rates of fetal defects at therapeutic but not at supratherapeutic levels.
EBioMedicine, , Volume: 63
2021
2019 update of the European AIDS Clinical Society Guidelines for treatment of people living with HIV version 10.0.
HIV medicine, , Volume: 21, Issue:10
2020
Pharmacokinetics, SAfety/tolerability, and EFficacy of high-dose RIFampicin in tuberculosis-HIV co-infected patients on efavirenz- or dolutegravir-based antiretroviral therapy: study protocol for an open-label, phase II clinical trial (SAEFRIF).
Trials, , Feb-13, Volume: 21, Issue:1
2020
Assessment of Maternal and Fetal Dolutegravir Exposure by Integrating Ex Vivo Placental Perfusion Data and Physiologically-Based Pharmacokinetic Modeling.
Clinical pharmacology and therapeutics, , Volume: 107, Issue:6
2020
Prediction of dolutegravir pharmacokinetics and dose optimization in neonates via physiologically based pharmacokinetic (PBPK) modelling.
The Journal of antimicrobial chemotherapy, , 03-01, Volume: 75, Issue:3
2020
Successful use of once-daily high-dose darunavir and dolutegravir in multidrug-resistant HIV.
Journal of clinical pharmacy and therapeutics, , Volume: 45, Issue:2
2020
Cell-type specific differences in antiretroviral penetration and the effects of HIV-1 Tat and morphine among primary human brain endothelial cells, astrocytes, pericytes, and microglia.
Neuroscience letters, , 11-01, Volume: 712
2019
Clinical and Virological Outcomes of TB/HIV Coinfected Patients Treated With Dolutegravir-Based HIV Antiretroviral Regimens: Programmatic Experience From Botswana.
Journal of acquired immune deficiency syndromes (1999), , 10-01, Volume: 82, Issue:2
2019
Population pharmacokinetics of dolutegravir: influence of drug-drug interactions in a real-life setting.
The Journal of antimicrobial chemotherapy, , 09-01, Volume: 74, Issue:9
2019
Safety and efficacy of dolutegravir in hemodialysis.
International journal of STD & AIDS, , Volume: 30, Issue:6
2019
A model-based comparative meta-analysis of the efficacy of dolutegravir-based and efavirenz-based regimens in HIV-infected patients.
Journal of infection and chemotherapy : official journal of the Japan Society of Chemotherapy, , Volume: 25, Issue:9
2019
Dolutegravir Population Pharmacokinetics in a Real-Life Cohort of People Living With HIV Infection: A Covariate Analysis.
Therapeutic drug monitoring, , Volume: 41, Issue:4
2019
Increased dose of dolutegravir as a potential rescue therapy in multi-experienced patients.
Antiviral therapy, , Volume: 24, Issue:1
2019
Pharmacokinetics of dolutegravir with and without darunavir/cobicistat in healthy volunteers.
The Journal of antimicrobial chemotherapy, , 01-01, Volume: 74, Issue:1
2019
Effects of Low- and High-Mineral Content Water on the Relative Bioavailability of a Coformulated Abacavir/Dolutegravir/Lamivudine Dispersible Tablet in Healthy Adults.
Journal of acquired immune deficiency syndromes (1999), , 12-15, Volume: 79, Issue:5
2018
Nanoformulated Antiretroviral Therapy Attenuates Brain Metabolic Oxidative Stress.
Molecular neurobiology, , Volume: 56, Issue:4
2019
Bioequivalence of a Fixed-Dose Combination Tablet of the Complete Two-Drug Regimen of Dolutegravir and Rilpivirine for Treatment of HIV-1 Infection.
Antimicrobial agents and chemotherapy, , Volume: 62, Issue:9
2018
Hybrid stochastic framework predicts efficacy of prophylaxis against HIV: An example with different dolutegravir prophylaxis schemes.
PLoS computational biology, , Volume: 14, Issue:6
2018
Dolutegravir Dual Therapy as Maintenance Treatment in HIV-Infected Patients: A Review.
The Annals of pharmacotherapy, , Volume: 52, Issue:7
2018
A potential drug interaction between phenobarbital and dolutegravir: A case report.
Journal of infection and chemotherapy : official journal of the Japan Society of Chemotherapy, , Volume: 24, Issue:6
2018
Dolutegravir pharmacokinetics in pregnant and postpartum women living with HIV.
AIDS (London, England), , 03-27, Volume: 32, Issue:6
2018
Sustained viral suppression with co-administration of oxcarbazepine and dolutegravir.
International journal of STD & AIDS, , Volume: 29, Issue:8
2018
Dolutegravir-Related Neurological Adverse Events: A Case Report of Successful Management with Therapeutic Drug Monitoring.
Current drug safety, , Volume: 13, Issue:1
2018
Development of an oral once-weekly drug delivery system for HIV antiretroviral therapy.
Nature communications, , 01-09, Volume: 9, Issue:1
2018
Small increase in dolutegravir trough, but equivalent total dolutegravir exposure with simeprevir in HIV/HCV seronegative volunteers.
The Journal of antimicrobial chemotherapy, , Jan-01, Volume: 73, Issue:1
2018
High plasma concentrations of dolutegravir in patients with ABCG2 genetic variants.
Pharmacogenetics and genomics, , Volume: 27, Issue:11
2017
Decreased Absorption of Dolutegravir and Tenofovir Disoproxil Fumarate, But Not Emtricitabine, in an HIV-Infected Patient Following Oral and Jejunostomy-Tube Administration.
Pharmacotherapy, , Volume: 37, Issue:8
2017
Dolutegravir/abacavir/lamivudine versus current ART in virally suppressed patients (STRIIVING): a 48-week, randomized, non-inferiority, open-label, Phase IIIb study.
Antiviral therapy, , Volume: 22, Issue:4
2017
Dolutegravir plasma concentrations according to companion antiretroviral drug: unwanted drug interaction or desirable boosting effect?
Antiviral therapy, , Volume: 22, Issue:4
2017
Quantitative evaluation of the antiretroviral efficacy of dolutegravir.
JCI insight, , 11-17, Volume: 1, Issue:19
2016
How recent findings on the pharmacokinetics and pharmacodynamics of integrase inhibitors can inform clinical use.
Current opinion in infectious diseases, , Volume: 30, Issue:1
2017
A Two-Way Steady-State Pharmacokinetic Interaction Study of Doravirine (MK-1439) and Dolutegravir.
Clinical pharmacokinetics, , Volume: 56, Issue:6
2017
Dolutegravir(DTG, S/GSK1349572) combined with other ARTs is superior to RAL- or EFV-based regimens for treatment of HIV-1 infection: a meta-analysis of randomized controlled trials.
AIDS research and therapy, , Volume: 13, Issue:1
2016
No clinically significant pharmacokinetic interactions between dolutegravir and daclatasvir in healthy adult subjects.
BMC infectious diseases, , 07-22, Volume: 16
2016
Usefulness of Integrase resistance testing in proviral HIV-1 DNA in patients with Raltegravir prior failure.
BMC infectious diseases, , May-13, Volume: 16
2016
The Promise of Dolutegravir: A Novel Second Generation Integrase Strand Transfer Inhibitor.
Current clinical pharmacology, , Volume: 11, Issue:2
2016
Effect of carbamazepine on dolutegravir pharmacokinetics and dosing recommendation.
European journal of clinical pharmacology, , Volume: 72, Issue:6
2016
Removal of Dolutegravir by Hemodialysis in HIV-Infected Patients with End-Stage Renal Disease.
Antimicrobial agents and chemotherapy, , Volume: 60, Issue:4
2016
Dolutegravir and elvitegravir plasma concentrations following cessation of drug intake.
The Journal of antimicrobial chemotherapy, , Volume: 71, Issue:4
2016
The preclinical discovery and development of dolutegravir for the treatment of HIV.
Expert opinion on drug discovery, , Volume: 10, Issue:11
2015
Efficacy and Tolerability of Integrase Inhibitors in Antiretroviral-Naive Patients.
AIDS reviews, , Volume: 17, Issue:3
Influence of nevirapine administration on the pharmacokinetics of dolutegravir in patients infected with HIV-1.
The Journal of antimicrobial chemotherapy, , Volume: 70, Issue:12
2015
Safety, Pharmacokinetics and Efficacy of Dolutegravir in Treatment-experienced HIV-1 Infected Adolescents: Forty-eight-week Results from IMPAACT P1093.
The Pediatric infectious disease journal, , Volume: 34, Issue:11
2015
HIV integrase inhibitors: a new era in the treatment of HIV.
Expert opinion on pharmacotherapy, , Volume: 16, Issue:9
2015
Dolutegravir Has No Effect on the Pharmacokinetics of Oral Contraceptives With Norgestimate and Ethinyl Estradiol.
The Annals of pharmacotherapy, , Volume: 49, Issue:7
2015
[Mechanisms of action, pharmacology and interactions of dolutegravir].
Enfermedades infecciosas y microbiologia clinica, , Volume: 33 Suppl 1
2015
Antiviral characteristics of GSK1265744, an HIV integrase inhibitor dosed orally or by long-acting injection.
Antimicrobial agents and chemotherapy, , Volume: 59, Issue:1
2015
HIV: new drugs, new guidelines.
Current opinion in infectious diseases, , Volume: 27, Issue:6
2014
Effect of fosamprenavir-ritonavir on the pharmacokinetics of dolutegravir in healthy subjects.
Antimicrobial agents and chemotherapy, , Volume: 58, Issue:11
2014
Effects of boceprevir and telaprevir on the pharmacokinetics of dolutegravir.
British journal of clinical pharmacology, , Volume: 78, Issue:5
2014
Dolutegravir, abacavir and lamivudine as HIV therapy.
Expert opinion on pharmacotherapy, , Volume: 15, Issue:7
2014
Dolutegravir: a next-generation integrase inhibitor for treatment of HIV infection.
Clinical infectious diseases : an official publication of the Infectious Diseases Society of America, , Jul-15, Volume: 59, Issue:2
2014
Dolutegravir for the treatment of adult patients with HIV-1 infection.
Expert review of anti-infective therapy, , Volume: 12, Issue:5
2014
Dolutegravir: a new integrase strand transfer inhibitor for the treatment of HIV.
Pharmacotherapy, , Volume: 34, Issue:5
2014
Once-daily dolutegravir versus twice-daily raltegravir in antiretroviral-naive adults with HIV-1 infection (SPRING-2 study): 96 week results from a randomised, double-blind, non-inferiority trial.
The Lancet. Infectious diseases, , Volume: 13, Issue:11
2013
Lack of pharmacokinetic interaction between rilpivirine and integrase inhibitors dolutegravir and GSK1265744.
Antimicrobial agents and chemotherapy, , Volume: 57, Issue:11
2013
Dolutegravir pharmacokinetics in the genital tract and colorectum of HIV-negative men after single and multiple dosing.
Journal of acquired immune deficiency syndromes (1999), , Sep-01, Volume: 64, Issue:1
2013
Single and multiple dose pharmacokinetics of dolutegravir in the genital tract of HIV-negative women.
Antiviral therapy, , Volume: 18, Issue:8
2013
Carbamoyl pyridone HIV-1 integrase inhibitors 3. A diastereomeric approach to chiral nonracemic tricyclic ring systems and the discovery of dolutegravir (S/GSK1349572) and (S/GSK1265744).
Journal of medicinal chemistry, , Jul-25, Volume: 56, Issue:14
2013
Effect of prednisone on the pharmacokinetics of the integrase inhibitor dolutegravir.
Antimicrobial agents and chemotherapy, , Volume: 57, Issue:9
2013
[Pharmacokinetics and safety of dolutegravir in healthy Japanese subjects].
The Japanese journal of antibiotics, , Volume: 66, Issue:1
2013
Next-generation integrase inhibitors : where to after raltegravir?
Drugs, , Volume: 73, Issue:3
2013
Safety and efficacy of dolutegravir in treatment-experienced subjects with raltegravir-resistant HIV type 1 infection: 24-week results of the VIKING Study.
The Journal of infectious diseases, , Mar-01, Volume: 207, Issue:5
2013
Pharmacology of HIV integrase inhibitors.
Current opinion in HIV and AIDS, , Volume: 7, Issue:5
2012
The use of HIV-1 integrase inhibitors in antiretroviral naive patients.
Current opinion in HIV and AIDS, , Volume: 7, Issue:5
2012
Update on raltegravir and the development of new integrase strand transfer inhibitors.
Southern medical journal, , Volume: 105, Issue:7
2012
From in vitro EC₅₀ to in vivo dose-response for antiretrovirals using an HIV disease model. Part I: a framework.
Journal of pharmacokinetics and pharmacodynamics, , Volume: 39, Issue:4
2012
Effect of a single supratherapeutic dose of dolutegravir on cardiac repolarization.
Pharmacotherapy, , Volume: 32, Issue:4
2012
Once daily dolutegravir (S/GSK1349572) in combination therapy in antiretroviral-naive adults with HIV: planned interim 48 week results from SPRING-1, a dose-ranging, randomised, phase 2b trial.
The Lancet. Infectious diseases, , Volume: 12, Issue:2
2012
Antiviral activity, safety, and pharmacokinetics/pharmacodynamics of dolutegravir as 10-day monotherapy in HIV-1-infected adults.
AIDS (London, England), , Sep-10, Volume: 25, Issue:14
2011
Pharmacokinetics of the HIV integrase inhibitor S/GSK1349572 co-administered with acid-reducing agents and multivitamins in healthy volunteers.
The Journal of antimicrobial chemotherapy, , Volume: 66, Issue:7
2011
Effect of atazanavir and atazanavir/ritonavir on the pharmacokinetics of the next-generation HIV integrase inhibitor, S/GSK1349572.
British journal of clinical pharmacology, , Volume: 72, Issue:1
2011
Pharmacokinetics and safety of S/GSK1349572, a next-generation HIV integrase inhibitor, in healthy volunteers.
Antimicrobial agents and chemotherapy, , Volume: 54, Issue:1
2010

Interactions (26)

ArticleYear
Tolerability and effectiveness of albuvirtide combined with dolutegravir for hospitalized people living with HIV/AIDS.
Medicine, , Nov-10, Volume: 102, Issue:45
2023
Mechanistic Modeling of the Drug-Drug Interaction Between Efavirenz and Dolutegravir: Is This Interaction Clinically Relevant When Switching From Efavirenz to Dolutegravir During Pregnancy?
Journal of clinical pharmacology, , Volume: 63 Suppl 1
2023
Efficacy and safety of dolutegravir or darunavir in combination with lamivudine plus either zidovudine or tenofovir for second-line treatment of HIV infection (NADIA): week 96 results from a prospective, multicentre, open-label, factorial, randomised, non
The lancet. HIV, , Volume: 9, Issue:6
2022
South African healthcare workers' knowledge of dolutegravir's drug-drug interactions in the first year of its rollout: a cross-sectional online survey.
Journal of the International AIDS Society, , Volume: 25, Issue:3
2022
Lack of a Clinically Meaningful Drug Interaction Between the HIV-1 Antiretroviral Agents Islatravir, Dolutegravir, and Tenofovir Disoproxil Fumarate.
Clinical pharmacology in drug development, , Volume: 10, Issue:12
2021
Dolutegravir-based dual maintenance regimens combined with lamivudine/emtricitabine or rilpivirine: risk of virological failure in a real-life setting.
The Journal of antimicrobial chemotherapy, , 12-24, Volume: 77, Issue:1
2021
Dolutegravir or Darunavir in Combination with Zidovudine or Tenofovir to Treat HIV.
The New England journal of medicine, , 07-22, Volume: 385, Issue:4
2021
The dolutegravir/valproic acid drug-drug interaction is primarily based on protein displacement.
The Journal of antimicrobial chemotherapy, , 04-13, Volume: 76, Issue:5
2021
Aging does not impact drug--drug interaction magnitudes with antiretrovirals.
AIDS (London, England), , 05-01, Volume: 34, Issue:6
2020
Drug-Drug Interactions Between Antiretrovirals and Carbamazepine/Oxcarbazepine: A Real-Life Investigation.
Therapeutic drug monitoring, , Volume: 42, Issue:2
2020
Population pharmacokinetics of dolutegravir: influence of drug-drug interactions in a real-life setting.
The Journal of antimicrobial chemotherapy, , 09-01, Volume: 74, Issue:9
2019
Drug-drug interactions of a two-drug regimen of dolutegravir and lamivudine for HIV treatment.
Expert opinion on drug metabolism & toxicology, , Volume: 15, Issue:3
2019
Barrier to Resistance of Dolutegravir in Two-Drug Combinations.
Antimicrobial agents and chemotherapy, , Volume: 63, Issue:3
2019
Assessment of drug interaction potential between the HCV direct-acting antiviral agents elbasvir/grazoprevir and the HIV integrase inhibitors raltegravir and dolutegravir.
The Journal of antimicrobial chemotherapy, , 03-01, Volume: 74, Issue:3
2019
Drug Interactions between Dolutegravir and Artemether-Lumefantrine or Artesunate-Amodiaquine.
Antimicrobial agents and chemotherapy, , Volume: 63, Issue:2
2019
Optimizing concentrations of concomitant antiretrovirals by reducing etravirine doses: two case reports of complex drug-drug interactions.
Antiviral therapy, , Volume: 24, Issue:1
2019
Cytokine-Mediated Systemic Adverse Drug Reactions in a Drug-Drug Interaction Study of Dolutegravir With Once-Weekly Isoniazid and Rifapentine.
Clinical infectious diseases : an official publication of the Infectious Diseases Society of America, , 07-02, Volume: 67, Issue:2
2018
Effect of dolutegravir in combination with Nucleoside Reverse Transcriptase Inhibitors (NRTIs) on people living with HIV who have pre-existing NRTI mutations.
International journal of antimicrobial agents, , Volume: 51, Issue:5
2018
Prevalence of drug-drug interactions in the era of HIV integrase inhibitors: a retrospective clinical study.
The Netherlands journal of medicine, , Volume: 75, Issue:6
2017
Dolutegravir plasma concentrations according to companion antiretroviral drug: unwanted drug interaction or desirable boosting effect?
Antiviral therapy, , Volume: 22, Issue:4
2017
Pharmacokinetics of dolutegravir and rilpivirine in combination with simeprevir and sofosbuvir in HIV/hepatitis C virus-coinfected patients with liver cirrhosis.
The Journal of antimicrobial chemotherapy, , 03-01, Volume: 72, Issue:3
2017
Dolutegravir(DTG, S/GSK1349572) combined with other ARTs is superior to RAL- or EFV-based regimens for treatment of HIV-1 infection: a meta-analysis of randomized controlled trials.
AIDS research and therapy, , Volume: 13, Issue:1
2016
Drug-Drug Interaction between the Direct-Acting Antiviral Regimen of Ombitasvir-Paritaprevir-Ritonavir plus Dasabuvir and the HIV Antiretroviral Agent Dolutegravir or Abacavir plus Lamivudine.
Antimicrobial agents and chemotherapy, , Volume: 60, Issue:10
2016
Pharmacokinetics of dolutegravir when administered with mineral supplements in healthy adult subjects.
Journal of clinical pharmacology, , Volume: 55, Issue:5
2015
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
Drug metabolism and disposition: the biological fate of chemicals, , Volume: 41, Issue:2
2013
Pharmacokinetics of the HIV integrase inhibitor S/GSK1349572 co-administered with acid-reducing agents and multivitamins in healthy volunteers.
The Journal of antimicrobial chemotherapy, , Volume: 66, Issue:7
2011