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HIV-1 integrase inhibitor

An 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.

ChEBI ID: 67268

Members (12)

MemberDefinitionClass
australifunginA carbobicyclic compound that is 4a,5,6,7,8,8a-hexahydronaphthalen-1(4H)-one substituted by hydroxy groups at positions 2, 5 and 8, a (2Z)-3-hydroxyprop-2-enoyl group at position 4, methyl groups at positions 4 and 7 and a 2R-octan-2-yl group at position 3 (the 4S,4aR,5S,7R,8R,8aS stereoisomer). It is isolated from the fermentation extracts of Sporormiella australis and exhibits antifungal activity by interfering with the fungal lipid metabolism.australifungin
bictegravirA monocarboxylic acid amide obtained by formal condensation of the carboxy group of (2R,5S,13aR)-8-hydroxy-7,9-dioxo-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxylic acid with the amino group of 2,4,6-trifluorobenzylamine. It is a second-generation integrase strand transfer inhibitor (INSTI) and used (as its sodium salt) for the treatment of HIV-1.bictegravir
chicoric acidchicoric acid
complestatinA heterodetic cyclic peptide which is a atropisomer of complestatin. It is isolated from the culture broth of Streptomyces and has anti-HIV-1 activity.chloropeptin II; isocomplestatin
dolutegravirA 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.dolutegravir
equisetinA member of the class of tetramic acids that is trichosetin in which the hydrogen attached to the lactam nitrogen has been replaced by a methyl group. It is produced by the filamentous fungus Fusarium heterosporum.equisetin
gsk1265744A monocarboxylic acid amide obtained by formal condensation of the carboxy group of (3S,11aR)-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydro[1,3]oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxylic acid with the amino group of 2,4-difluorobenzylamine. Used (as its sodium salt) for treatment of HIV-1.cabotegravir
integric acidAn eremophilane sesquiterpenoid with anti-HIV-1 activity. It is isolated from Xylaria sp. MF6254.integric acid
jtk-303A quinolinemonocarboxylic acid that is 7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid substited at position 1 by a 1-hydroxy-3-methylbutan-2-yl group and at position 6 by a 3-chloro-2-fluorobenzyl group (the S-enantiomer). It is used in combination therapy for the treatment of HIV-1 infection.elvitegravir
laurolitsineAn aporphine alkaloid that is noraporphine substituted by hydroxy groups at positions 2 and 9 and methoxy groups at positions 1 and 10. Isolated from Litsea glutinosa and Lindera chunii, exhibits inhibitory activity against HIV-1 integrase.laurolistine
neuroprotectin aA heterodetic cyclic peptide that is chloropeptin II in which the indole moiety is oxidised to the corresponding 2-oxindole. It is a HIV-1 integrase inhibitor isolated from Streptomyces.complestatin A
raltegravirA pyrimidone that is pyrimidin-4(3H)-one in which the hydrogens at positions 2, 3, 5 and 6 are replaced by 2-[(5-methyl-1,3,4-oxadiazole-2-carbonyl)amino]propan-2-yl, methyl, hydroxy, and N-[(4-fluorophenyl)methyl]aminoacyl groups, respectively. It is an antiretroviral drug used for treatment of HIV infection.raltegravir

Research

Studies (1,992)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19904 (0.20)18.7374
1990's26 (1.31)18.2507
2000's127 (6.38)29.6817
2010's1,021 (51.26)24.3611
2020's814 (40.86)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials319 (14.21%)5.53%
Reviews239 (10.65%)6.00%
Case Studies133 (5.92%)4.05%
Observational83 (3.70%)0.25%
Other1,471 (65.52%)84.16%

Protein Targets (71)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-lipoxygenase, partialHomo sapiens (human)Potency39.810711
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency0.006311
Chain A, HADH2 proteinHomo sapiens (human)Potency16.062022
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency3.981111
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency0.794311
Chain B, HADH2 proteinHomo sapiens (human)Potency16.062022
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency0.061711
estrogen nuclear receptor alphaHomo sapiens (human)Potency61.584511
EWS/FLI fusion proteinHomo sapiens (human)Potency22.527248
Fumarate hydrataseHomo sapiens (human)Potency37.221212
GLI family zinc finger 3Homo sapiens (human)Potency22.966422
Histone H2A.xCricetulus griseus (Chinese hamster)Potency40.046611
Integrin alpha-IIbHomo sapiens (human)Potency0.006311
Integrin beta-3Homo sapiens (human)Potency0.006311
interleukin 8Homo sapiens (human)Potency74.978011
lethal factor (plasmid)Bacillus anthracis str. A2012Potency15.848911
LuciferasePhotinus pyralis (common eastern firefly)Potency70.922011
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency0.027311
Nuclear receptor ROR-gammaHomo sapiens (human)Potency3.349112
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency29.847011
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency23.708311
polyproteinZika virusPotency37.221212
RAR-related orphan receptor gammaMus musculus (house mouse)Potency19.982622
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency32.277433
SMAD family member 2Homo sapiens (human)Potency10.682211
SMAD family member 3Homo sapiens (human)Potency10.682211
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency0.035212

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
ATP-dependent translocase ABCB1Homo sapiens (human)IC5095.000022
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)IC5048.500022
C-C chemokine receptor type 1Homo sapiens (human)Ki0.005011
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC5095.000022
Chain A, PFV integraseHuman spumaretrovirusIC500.051719
Cytochrome P450 1A2Homo sapiens (human)IC5070.000022
Cytochrome P450 2A6Homo sapiens (human)IC50100.000011
Cytochrome P450 2C19Homo sapiens (human)IC5067.000012
Cytochrome P450 2C8Homo sapiens (human)IC5090.000011
Cytochrome P450 2C9 Homo sapiens (human)IC5070.000022
Cytochrome P450 2D6Homo sapiens (human)IC5080.000034
Cytochrome P450 3A4Homo sapiens (human)IC5058.500022
DRattus norvegicus (Norway rat)IC502.500011
D(2) dopamine receptorRattus norvegicus (Norway rat)IC506.800011
DNA polymerase betaHomo sapiens (human)IC5050.000011
Gag-Pol polyproteinHIV-1 M:B_HXB2RIC500.015011
Integrase Human immunodeficiency virus 1IC502.432278103
Potassium voltage-gated channel subfamily D member 3Homo sapiens (human)IC505,011.870011
Potassium voltage-gated channel subfamily E member 1Homo sapiens (human)IC5025.118911
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC501,278.349544
Potassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)IC5025.118911
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2Ki302.000011
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusKi302.000011
Reverse transcriptase/RNaseH Human immunodeficiency virus 1IC5041.0909611
Sigma intracellular receptor 2Homo sapiens (human)Ki0.018011
Sigma intracellular receptor 2Rattus norvegicus (Norway rat)Ki0.023822
Sigma non-opioid intracellular receptor 1Cavia porcellus (domestic guinea pig)Ki0.097522
Sodium channel protein type 5 subunit alphaHomo sapiens (human)IC50950.559022
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)IC5016.500011
Solute carrier family 22 member 2Homo sapiens (human)IC501.900011
Solute carrier organic anion transporter family member 1B1Homo sapiens (human)IC50100.000011
Solute carrier organic anion transporter family member 1B3Homo sapiens (human)IC50100.000011
T-cell surface glycoprotein CD4Homo sapiens (human)IC500.130011
Tyrosine-protein phosphatase non-receptor type 1Homo sapiens (human)Ki1,400.000011
Tyrosine-protein phosphatase YopHYersinia enterocoliticaIC50379.000011
Tyrosine-protein phosphatase YopHYersinia enterocoliticaKi40.400022
UDP-glucuronosyltransferase 1A1 Homo sapiens (human)IC50153.333333
Vesicular acetylcholine transporterRattus norvegicus (Norway rat)Ki4.523011
Voltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)IC50246.700011
Voltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)IC50246.700011
Voltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)IC50246.700011
Voltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)IC50246.700011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Integrase Human immunodeficiency virus 1EC500.002466
Integrase Human immunodeficiency virus 2EC500.002311
Integrase Human immunodeficiency virus 1Kd3.000011
Tyrosine-protein phosphatase non-receptor type 1Homo sapiens (human)Kd1,600.000011

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Integrase Human immunodeficiency virus 1C500.011012
Integrase Human immunodeficiency virus 1MI50100.000011
UDP-glucuronosyltransferase 1A1 Homo sapiens (human)Km21.000011