Page last updated: 2024-11-13

4-[(1-methyl-5-tetrazolyl)thio]-5-(4-phenylphenyl)thieno[2,3-d]pyrimidine

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID SourceID
PubMed CID44142140
CHEMBL ID1528672
CHEBI ID93542

Synonyms (9)

Synonym
NCGC00182378-01
smr001317760
MLS002264459
HMS2194M23
HMS3334N13
CHEMBL1528672
CHEBI:93542
Q27165236
4-[(1-methyl-5-tetrazolyl)thio]-5-(4-phenylphenyl)thieno[2,3-d]pyrimidine
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (2)

ClassDescription
biphenylsBenzenoid aromatic compounds containing two phenyl or substituted-phenyl groups which are joined together by a single bond.
thienopyrimidineA class of aromatic heterobicyclic compounds each of which contains a pyrimidine ring ortho fused to a 5-membered thiophene ring.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (18)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Nrf2Homo sapiens (human)Potency2.23870.09208.222223.1093AID624171
chaperonin-containing TCP-1 beta subunit homologHomo sapiens (human)Potency89.12513.981127.764939.8107AID504842
ATAD5 protein, partialHomo sapiens (human)Potency11.57740.004110.890331.5287AID504467
Smad3Homo sapiens (human)Potency19.95260.00527.809829.0929AID588855
chromobox protein homolog 1Homo sapiens (human)Potency100.00000.006026.168889.1251AID540317
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency35.48133.548119.542744.6684AID743266
huntingtin isoform 2Homo sapiens (human)Potency9.45630.000618.41981,122.0200AID2669; AID2673
importin subunit beta-1 isoform 1Homo sapiens (human)Potency141.25405.804836.130665.1308AID540263
snurportin-1Homo sapiens (human)Potency141.25405.804836.130665.1308AID540263
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency44.66840.425612.059128.1838AID504891
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency1.99530.15855.287912.5893AID540303
plasminogen precursorMus musculus (house mouse)Potency1.99530.15855.287912.5893AID540303
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency1.99530.15855.287912.5893AID540303
gemininHomo sapiens (human)Potency9.89080.004611.374133.4983AID624296; AID624297
DNA dC->dU-editing enzyme APOBEC-3G isoform 1Homo sapiens (human)Potency3.54810.058010.694926.6086AID602310
Rap guanine nucleotide exchange factor 3Homo sapiens (human)Potency112.20206.309660.2008112.2020AID720707
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Phosphatidylinositol 5-phosphate 4-kinase type-2 gammaHomo sapiens (human)Kd100.00000.00302.75228.8000AID1260401
[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)
HuntingtinHomo sapiens (human)AC5013.94753.16008.107810.0000AID1260397; AID1260398; AID1260399; AID1260400
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (43)

Processvia Protein(s)Taxonomy
angiogenesisRap guanine nucleotide exchange factor 3Homo sapiens (human)
adaptive immune responseRap guanine nucleotide exchange factor 3Homo sapiens (human)
signal transductionRap guanine nucleotide exchange factor 3Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayRap guanine nucleotide exchange factor 3Homo sapiens (human)
associative learningRap guanine nucleotide exchange factor 3Homo sapiens (human)
Rap protein signal transductionRap guanine nucleotide exchange factor 3Homo sapiens (human)
regulation of actin cytoskeleton organizationRap guanine nucleotide exchange factor 3Homo sapiens (human)
negative regulation of syncytium formation by plasma membrane fusionRap guanine nucleotide exchange factor 3Homo sapiens (human)
intracellular signal transductionRap guanine nucleotide exchange factor 3Homo sapiens (human)
positive regulation of GTPase activityRap guanine nucleotide exchange factor 3Homo sapiens (human)
regulation of angiogenesisRap guanine nucleotide exchange factor 3Homo sapiens (human)
positive regulation of angiogenesisRap guanine nucleotide exchange factor 3Homo sapiens (human)
positive regulation of protein export from nucleusRap guanine nucleotide exchange factor 3Homo sapiens (human)
positive regulation of stress fiber assemblyRap guanine nucleotide exchange factor 3Homo sapiens (human)
regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionRap guanine nucleotide exchange factor 3Homo sapiens (human)
positive regulation of syncytium formation by plasma membrane fusionRap guanine nucleotide exchange factor 3Homo sapiens (human)
establishment of endothelial barrierRap guanine nucleotide exchange factor 3Homo sapiens (human)
cellular response to cAMPRap guanine nucleotide exchange factor 3Homo sapiens (human)
Ras protein signal transductionRap guanine nucleotide exchange factor 3Homo sapiens (human)
regulation of insulin secretionRap guanine nucleotide exchange factor 3Homo sapiens (human)
regulation of phosphoprotein phosphatase activityHuntingtinHomo sapiens (human)
positive regulation of cilium assemblyHuntingtinHomo sapiens (human)
establishment of mitotic spindle orientationHuntingtinHomo sapiens (human)
retrograde vesicle-mediated transport, Golgi to endoplasmic reticulumHuntingtinHomo sapiens (human)
apoptotic processHuntingtinHomo sapiens (human)
Golgi organizationHuntingtinHomo sapiens (human)
positive regulation of inositol 1,4,5-trisphosphate-sensitive calcium-release channel activityHuntingtinHomo sapiens (human)
protein destabilizationHuntingtinHomo sapiens (human)
vocal learningHuntingtinHomo sapiens (human)
positive regulation of apoptotic processHuntingtinHomo sapiens (human)
vesicle transport along microtubuleHuntingtinHomo sapiens (human)
positive regulation of mitophagyHuntingtinHomo sapiens (human)
positive regulation of lipophagyHuntingtinHomo sapiens (human)
regulation of CAMKK-AMPK signaling cascadeHuntingtinHomo sapiens (human)
positive regulation of aggrephagyHuntingtinHomo sapiens (human)
regulation of cAMP-dependent protein kinase activityHuntingtinHomo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathwayHuntingtinHomo sapiens (human)
microtubule-based transportHuntingtinHomo sapiens (human)
regulation of autophagyPhosphatidylinositol 5-phosphate 4-kinase type-2 gammaHomo sapiens (human)
negative regulation of insulin receptor signaling pathwayPhosphatidylinositol 5-phosphate 4-kinase type-2 gammaHomo sapiens (human)
1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate biosynthetic processPhosphatidylinositol 5-phosphate 4-kinase type-2 gammaHomo sapiens (human)
positive regulation of autophagosome assemblyPhosphatidylinositol 5-phosphate 4-kinase type-2 gammaHomo sapiens (human)
phosphatidylinositol phosphate biosynthetic processPhosphatidylinositol 5-phosphate 4-kinase type-2 gammaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (16)

Processvia Protein(s)Taxonomy
guanyl-nucleotide exchange factor activityRap guanine nucleotide exchange factor 3Homo sapiens (human)
protein bindingRap guanine nucleotide exchange factor 3Homo sapiens (human)
protein domain specific bindingRap guanine nucleotide exchange factor 3Homo sapiens (human)
cAMP bindingRap guanine nucleotide exchange factor 3Homo sapiens (human)
p53 bindingHuntingtinHomo sapiens (human)
protein bindingHuntingtinHomo sapiens (human)
profilin bindingHuntingtinHomo sapiens (human)
kinase bindingHuntingtinHomo sapiens (human)
heat shock protein bindingHuntingtinHomo sapiens (human)
dynactin bindingHuntingtinHomo sapiens (human)
identical protein bindingHuntingtinHomo sapiens (human)
transmembrane transporter bindingHuntingtinHomo sapiens (human)
dynein intermediate chain bindingHuntingtinHomo sapiens (human)
beta-tubulin bindingHuntingtinHomo sapiens (human)
protein bindingPhosphatidylinositol 5-phosphate 4-kinase type-2 gammaHomo sapiens (human)
ATP bindingPhosphatidylinositol 5-phosphate 4-kinase type-2 gammaHomo sapiens (human)
1-phosphatidylinositol-4-phosphate 5-kinase activityPhosphatidylinositol 5-phosphate 4-kinase type-2 gammaHomo sapiens (human)
identical protein bindingPhosphatidylinositol 5-phosphate 4-kinase type-2 gammaHomo sapiens (human)
1-phosphatidylinositol-5-phosphate 4-kinase activityPhosphatidylinositol 5-phosphate 4-kinase type-2 gammaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (27)

Processvia Protein(s)Taxonomy
plasma membraneRap guanine nucleotide exchange factor 3Homo sapiens (human)
cortical actin cytoskeletonRap guanine nucleotide exchange factor 3Homo sapiens (human)
plasma membraneRap guanine nucleotide exchange factor 3Homo sapiens (human)
microvillusRap guanine nucleotide exchange factor 3Homo sapiens (human)
endomembrane systemRap guanine nucleotide exchange factor 3Homo sapiens (human)
membraneRap guanine nucleotide exchange factor 3Homo sapiens (human)
lamellipodiumRap guanine nucleotide exchange factor 3Homo sapiens (human)
filopodiumRap guanine nucleotide exchange factor 3Homo sapiens (human)
extracellular exosomeRap guanine nucleotide exchange factor 3Homo sapiens (human)
presynaptic cytosolHuntingtinHomo sapiens (human)
postsynaptic cytosolHuntingtinHomo sapiens (human)
nucleusHuntingtinHomo sapiens (human)
nucleoplasmHuntingtinHomo sapiens (human)
cytoplasmHuntingtinHomo sapiens (human)
early endosomeHuntingtinHomo sapiens (human)
late endosomeHuntingtinHomo sapiens (human)
autophagosomeHuntingtinHomo sapiens (human)
endoplasmic reticulumHuntingtinHomo sapiens (human)
Golgi apparatusHuntingtinHomo sapiens (human)
centrioleHuntingtinHomo sapiens (human)
cytosolHuntingtinHomo sapiens (human)
inclusion bodyHuntingtinHomo sapiens (human)
axonHuntingtinHomo sapiens (human)
dendriteHuntingtinHomo sapiens (human)
cytoplasmic vesicle membraneHuntingtinHomo sapiens (human)
perinuclear region of cytoplasmHuntingtinHomo sapiens (human)
protein-containing complexHuntingtinHomo sapiens (human)
cytoplasmHuntingtinHomo sapiens (human)
nucleoplasmPhosphatidylinositol 5-phosphate 4-kinase type-2 gammaHomo sapiens (human)
autophagosomePhosphatidylinositol 5-phosphate 4-kinase type-2 gammaHomo sapiens (human)
endoplasmic reticulumPhosphatidylinositol 5-phosphate 4-kinase type-2 gammaHomo sapiens (human)
cytosolPhosphatidylinositol 5-phosphate 4-kinase type-2 gammaHomo sapiens (human)
plasma membranePhosphatidylinositol 5-phosphate 4-kinase type-2 gammaHomo sapiens (human)
intracellular organellePhosphatidylinositol 5-phosphate 4-kinase type-2 gammaHomo sapiens (human)
extracellular exosomePhosphatidylinositol 5-phosphate 4-kinase type-2 gammaHomo sapiens (human)
plasma membranePhosphatidylinositol 5-phosphate 4-kinase type-2 gammaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (13)

Assay IDTitleYearJournalArticle
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (20.00)29.6817
2010's3 (60.00)24.3611
2020's1 (20.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.56

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

MetricThis Compound (vs All)
Research Demand Index12.56 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.36 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.56)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other5 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]