Page last updated: 2024-12-10

ly 73497

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Description

LY 73497: HIV-1 reverse transcriptase inhibitor; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3001082
CHEMBL ID33981
SCHEMBL ID1520344
MeSH IDM0252202

Synonyms (20)

Synonym
1-(2-phenylethyl)-3-1,3-thiazol-2-ylthiourea
chembl33981 ,
bdbm1894
n-(2-phenethyl)-n -(2-thiazolyl)thiourea
MLS001243522
smr000841574
149485-30-3
thiourea, n-(2-phenylethyl)-n'-2-thiazolyl-
1-phenethyl-3-thiazol-2-yl-thiourea
ly73497
ly 73497
ly-73497
NCGC00247398-01
HMS2211G04
HMS3338J14
SCHEMBL1520344
DTXSID90164286
1-(2-phenylethyl)-3-(1,3-thiazol-2-yl)thiourea
1-phenethyl-3-(thiazol-2-yl)thiourea
STARBLD0049274
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (16)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency70.79460.631035.7641100.0000AID504339
LuciferasePhotinus pyralis (common eastern firefly)Potency13.45910.007215.758889.3584AID588342
thioredoxin reductaseRattus norvegicus (Norway rat)Potency19.95260.100020.879379.4328AID588453
BRCA1Homo sapiens (human)Potency8.91250.89137.722525.1189AID624202
TDP1 proteinHomo sapiens (human)Potency16.46870.000811.382244.6684AID686978; AID686979
thioredoxin glutathione reductaseSchistosoma mansoniPotency2.23870.100022.9075100.0000AID485364
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency1.58490.707912.194339.8107AID720542
67.9K proteinVaccinia virusPotency5.01190.00018.4406100.0000AID720579
P53Homo sapiens (human)Potency28.18380.07319.685831.6228AID504706
importin subunit beta-1 isoform 1Homo sapiens (human)Potency10.32255.804836.130665.1308AID540253
serine/threonine-protein kinase PLK1Homo sapiens (human)Potency29.93490.168316.404067.0158AID720504
snurportin-1Homo sapiens (human)Potency10.32255.804836.130665.1308AID540253
GTP-binding nuclear protein Ran isoform 1Homo sapiens (human)Potency10.32255.804816.996225.9290AID540253
Guanine nucleotide-binding protein GHomo sapiens (human)Potency11.22021.995325.532750.1187AID624287
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Gag-Pol polyproteinHIV-1 M:B_HXB2RIC50 (µMol)0.90000.00060.91418.3200AID1795346
Reverse transcriptase/RNaseH Human immunodeficiency virus 1IC50 (µMol)0.90000.00011.076810.0000AID1277311; AID197795; AID199241
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Reverse transcriptase/RNaseH Human immunodeficiency virus 1Activity1.30000.00091.30738.0000AID199980
Reverse transcriptase/RNaseH Human immunodeficiency virus 1ED501.30000.00020.99359.8000AID105522
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (7)

Processvia Protein(s)Taxonomy
viral life cycleGag-Pol polyproteinHIV-1 M:B_HXB2R
establishment of integrated proviral latencyGag-Pol polyproteinHIV-1 M:B_HXB2R
negative regulation of inflammatory response to antigenic stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
renal water homeostasisGuanine nucleotide-binding protein GHomo sapiens (human)
G protein-coupled receptor signaling pathwayGuanine nucleotide-binding protein GHomo sapiens (human)
regulation of insulin secretionGuanine nucleotide-binding protein GHomo sapiens (human)
cellular response to glucagon stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (4)

Processvia Protein(s)Taxonomy
peptidase activityGag-Pol polyproteinHIV-1 M:B_HXB2R
integrase activityGag-Pol polyproteinHIV-1 M:B_HXB2R
G protein activityGuanine nucleotide-binding protein GHomo sapiens (human)
adenylate cyclase activator activityGuanine nucleotide-binding protein GHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
plasma membraneGuanine nucleotide-binding protein GHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (23)

Assay IDTitleYearJournalArticle
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID248354Concentration required to inhibit 50% viral production of human immunodeficiency virus type 1 (HIV-1-IIIB)2005Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
Hierarchical database screenings for HIV-1 reverse transcriptase using a pharmacophore model, rigid docking, solvation docking, and MM-PB/SA.
AID1277311Inhibition of HIV-1 reverse transcriptase using and rCdC as template and tritium-labeled dGTP incubated for 30 mins by liquid scintillation counting method2016European journal of medicinal chemistry, Feb-15, Volume: 109Recent developments of 2-aminothiazoles in medicinal chemistry.
AID105577Compound was tested for its inhibitory effect on HIV-1 in MT-4 cells1998Bioorganic & medicinal chemistry letters, Jun-16, Volume: 8, Issue:12
Synthesis and anti-HIV activities of urea-PETT analogs belonging to a new class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID199241Antiviral activity was determined against HIV- 1 reverse transcriptase1998Bioorganic & medicinal chemistry letters, Jun-16, Volume: 8, Issue:12
Synthesis and anti-HIV activities of urea-PETT analogs belonging to a new class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID197795Inhibition of HIV-1 reverse transcriptase using rCdG as template and dGTP as substrate1995Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25
Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs.
AID105522Concentration which reduced the cytopathic effect of HIV-1 in MT-4 infected cells1995Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25
Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs.
AID104944Concentration which reduced the viability of the HIV-1 infected MT-4 cells to 50% compared to untreated control cells1995Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25
Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs.
AID310934Antiviral activity against HIV1 in MT4 cells assessed as reduction of virus-induced cytopathicity by XTT assay2007Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8
Predicting anti-HIV activity of PETT derivatives: CoMFA approach.
AID199980Inhibitory activity against human immunodeficiency virus type 1 reverse transcriptase (HIV-1 RT)2002Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
Prediction of activity for nonnucleoside inhibitors with HIV-1 reverse transcriptase based on Monte Carlo simulations.
AID1795346HIV-1 RT Assay from Article 10.1021/jm00025a010: \\Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs.\\1995Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25
Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (13)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's4 (30.77)18.2507
2000's4 (30.77)29.6817
2010's4 (30.77)24.3611
2020's1 (7.69)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.77

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

MetricThis Compound (vs All)
Research Demand Index11.77 (24.57)
Research Supply Index2.64 (2.92)
Research Growth Index4.41 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.77)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (7.69%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other12 (92.31%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]