Page last updated: 2024-11-08

ag 3-5

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

Description

icilin: a cooling compound that activates TRPM8 [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID161930
CHEMBL ID258405
CHEBI ID92845
SCHEMBL ID663503
MeSH IDM0059785

Synonyms (90)

Synonym
2(1h)-pyrimidinone, 3,6-dihydro-1-(2-hydroxyphenyl)-4-(3-nitrophenyl)-
ag 3-5
brn 0700310
3,6-dihydro-1-(2-hydroxyphenyl)-4-(3-nitrophenyl)-2(1h)-pyrimidinone
1-(2-hydroxyphenyl)-4-(3-nitrophenyl)-1,2,3,6-tetrahydropyrimidine-2-one
MLS002153471
HMS3268C05
BRD-K48869804-001-04-7
1-(2-hydroxyphenyl)-4-(3-nitrophenyl)-3,6-dihydropyrimidin-2-one
gtpl2429
EU-0100426
icilin, >=97% (hplc), solid
icilin
3-(2-hydroxyphenyl)-6-(3-nitrophenyl)-3,4-dihydro-2(1h)-pyrimidinone
MLS000693445
smr000299977
LOPAC0_000426
tocris-1531
NCGC00025205-01
lopac-i-9532
NCGC00015571-01
SMP2_000128
NCGC00025205-02
NCGC00025205-03
1-(2-hydroxyphenyl)-4-(3-nitrophenyl)-1,2,3,6-tetrahydropyrimidin-2-one
STK134504
3-(2-hydroxyphenyl)-6-(3-nitrophenyl)-3,4-dihydropyrimidin-2(1h)-one
NCGC00015571-03
ag-3-5; 1-(2-hydroxyphenyl)-4-(3-nitrophenyl)-1,2,3,6-tetrahydropyrimidin-2-one
I 9532
bdbm50241426
NCGC00015571-05
CHEMBL258405 ,
icillin
AKOS000370368
3-(2-hydroxyphenyl)-6-(3-nitrophenyl)-1,4-dihydropyrimidin-2-one
HMS3261E14
C20171
CCG-204518
ag 3-5 cpd
unii-cs70pzq4qj
36945-98-9
5-24-03-00255 (beilstein handbook reference)
cs70pzq4qj ,
NCGC00015571-04
NCGC00015571-02
HMS2769B07
ag-3-5
LP00426
CCG-221730
HY-11062
CS-1922
mfcd01689072
SCHEMBL663503
1-(2'-hydroxyphenyl)-4-(3''-nitrophenyl)-1,2,3,6-tetrahydropyrimidine-2-one
icilin [mi]
tox21_500426
NCGC00261111-01
3,4-dihydro-3-(2-hydroxyphenyl)-6-(3-nitrophenyl)-(1h)-pyrimidin-2-one
AC-35209
RCEFMOGVOYEGJN-UHFFFAOYSA-N
HB1153
c16h13n3o4
HMS3648E15
DTXSID70190442
EX-A279
icilin(ag 3-5)
3-(2-hydroxyphenyl)-6-(3-nitrophenyl)-1,2,3,4-tetrahydropyrimidin-2-one
CHEBI:92845
SR-01000075377-1
SR-01000075377-2
sr-01000075377
SR-01000075377-4
NCGC00015571-07
'3-(2-hydroxyphenyl)-6-(3-nitrophenyl)-3,4-dihydropyrimidin-2(1h)-one'
Q5986473
FT-0700300
HMS3676H21
AS-35111
SR-01000075377-9
BCP27818
ag 3-5; ag3-5; ag-3-5
HMS3412H21
SDCCGSBI-0050411.P002
NCGC00015571-15
3-(2-hydroxyphenyl)-6-(3-nitrophenyl)-1,4-dihydropyrimidin-2-one.
I-145
A903163
BI164563
icilin- bio-x

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" However, additional studies have revealed potential adverse effects with KPR-2579, such as the formation of a reactive metabolite, CYP3A4 induction, and convulsions."( Identification of N-acyl-N-indanyl-α-phenylglycinamides as selective TRPM8 antagonists designed to mitigate the risk of adverse effects.
Fujimori, Y; Hirasawa, H; Ikeda, T; Kamada, N; Kanbe, H; Kobayashi, JI; Nakanishi, O; Yamamoto, A, 2021
)
0.62

Pharmacokinetics

ExcerptReferenceRelevance
" This manuscript outlines new developments in the SAR of a lead series of 1,2,3,4-tetrahydroisoquinoline derivatives with emphasis on strategies to improve pharmacokinetic properties and potency."( Optimization of potency and pharmacokinetic properties of tetrahydroisoquinoline transient receptor potential melastatin 8 (TRPM8) antagonists.
Bartberger, MD; Bo, Y; Clarine, J; Davis, CD; Gavva, NR; Gore, VK; Horne, DB; Kaller, MR; Lehto, SG; Ma, VV; Monenschein, H; Nguyen, TT; Nishimura, N; Norman, MH; Tamayo, NA; Tang, P; Wang, W; Youngblood, BD; Zhang, M, 2014
)
0.4

Bioavailability

ExcerptReferenceRelevance
" Exploration of the structure-activity relationships of 4 led to the identification of a potent and orally bioavailable TRPM8 antagonist, tetrahydroisoquinoline 87."( Fused piperidines as a novel class of potent and orally available transient receptor potential melastatin type 8 (TRPM8) antagonists.
Bartberger, MD; Bo, Y; Chen, J; Correll, TL; Deng, H; Gavva, NR; Gore, V; Klionsky, L; Lehto, SG; Ma, V; Nishimura, N; Norman, MH; Tamayo, NA; Tang, P; Wang, W; Youngblood, B, 2012
)
0.38
" AMG2850 is potent in vitro at rat TRPM8 (IC90 against icilin activation of 204 ± 28 nM), highly selective (>100-fold IC90 over TRPV1 and TRPA1 channels), and orally bioavailable (F po > 40 %)."( AMG2850, a potent and selective TRPM8 antagonist, is not effective in rat models of inflammatory mechanical hypersensitivity and neuropathic tactile allodynia.
Davis, C; Gavva, NR; Kerstein, PC; Lehto, SG; Stucky, CL; Wang, J; Wang, W; Weyer, AD; Wild, KD; Youngblood, BD; Zhang, M, 2015
)
0.42
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" Both 8-Br-cAMP (100 microM) and forskolin (10 microM) right-shifted the dose-response curves for the TRPM8-mediated effect of icilin and menthol on intracellular Ca(2+)."( Regulation of transient receptor potential channels of melastatin type 8 (TRPM8): effect of cAMP, cannabinoid CB(1) receptors and endovanilloids.
De Petrocellis, L; Di Marzo, V; Moriello, AS; Orlando, P; Starowicz, K; Vivese, M, 2007
)
0.34
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
C-nitro compoundA nitro compound having the nitro group (-NO2) attached to a carbon atom.
[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 (29)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency0.05010.004023.8416100.0000AID485290
Chain A, Ferritin light chainEquus caballus (horse)Potency35.48135.623417.292931.6228AID2323
Nrf2Homo sapiens (human)Potency25.11890.09208.222223.1093AID624171
thioredoxin reductaseRattus norvegicus (Norway rat)Potency16.83360.100020.879379.4328AID588453
NFKB1 protein, partialHomo sapiens (human)Potency28.18380.02827.055915.8489AID895; AID928
GLS proteinHomo sapiens (human)Potency10.00000.35487.935539.8107AID624146
TDP1 proteinHomo sapiens (human)Potency15.30430.000811.382244.6684AID686978; AID686979
Microtubule-associated protein tauHomo sapiens (human)Potency15.84890.180013.557439.8107AID1460
thioredoxin glutathione reductaseSchistosoma mansoniPotency44.66840.100022.9075100.0000AID485364
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency25.11890.011212.4002100.0000AID1030
thyroid stimulating hormone receptorHomo sapiens (human)Potency3.98110.001318.074339.8107AID926
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency14.14670.001530.607315,848.9004AID1224819; AID1224820
arylsulfatase AHomo sapiens (human)Potency3.79331.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency37.89160.035520.977089.1251AID504332
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency19.95260.00207.533739.8107AID891
cytochrome P450 2C19 precursorHomo sapiens (human)Potency6.30960.00255.840031.6228AID899
cytochrome P450 2C9 precursorHomo sapiens (human)Potency1.00000.00636.904339.8107AID883
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency30.30010.001815.663839.8107AID894
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency1.00000.15855.287912.5893AID540303
plasminogen precursorMus musculus (house mouse)Potency1.00000.15855.287912.5893AID540303
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency1.00000.15855.287912.5893AID540303
gemininHomo sapiens (human)Potency0.00460.004611.374133.4983AID624297
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency11.29470.00419.962528.1838AID2675
lamin isoform A-delta10Homo sapiens (human)Potency6.30960.891312.067628.1838AID1487
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency1.00000.00638.235039.8107AID883
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency8.49210.060110.745337.9330AID485368
[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)
Transient receptor potential cation channel subfamily M member 8Rattus norvegicus (Norway rat)IC50 (µMol)0.05800.05802.65048.3000AID1204201
[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)
Transient receptor potential cation channel subfamily A member 1Homo sapiens (human)EC50 (µMol)100.00000.00033.166210.0000AID482143
Transient receptor potential cation channel subfamily M member 8Homo sapiens (human)EC50 (µMol)0.18000.06001.12003.0000AID482150; AID780253
Transient receptor potential cation channel subfamily M member 8Rattus norvegicus (Norway rat)EC50 (µMol)0.15000.11000.46671.1000AID1204200; AID392794
[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)
Transient receptor potential cation channel subfamily A member 1Homo sapiens (human)Activity0.09900.09908.019810.0000AID500219
Transient receptor potential cation channel subfamily M member 8Homo sapiens (human)Activity0.09900.09905.049510.0000AID500218
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (18)

Processvia Protein(s)Taxonomy
monoatomic ion transportTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
intracellular calcium ion homeostasisTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
cell surface receptor signaling pathwayTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
response to coldTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
response to xenobiotic stimulusTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
response to organic substanceTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
response to organic cyclic compoundTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
sensory perception of painTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
calcium-mediated signalingTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
response to painTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
thermoceptionTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
detection of mechanical stimulus involved in sensory perception of painTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
detection of chemical stimulus involved in sensory perception of painTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
protein homotetramerizationTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
cellular response to hydrogen peroxideTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
calcium ion transmembrane transportTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
cellular response to organic substanceTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
intracellular calcium ion homeostasisTransient receptor potential cation channel subfamily M member 8Homo sapiens (human)
response to coldTransient receptor potential cation channel subfamily M member 8Homo sapiens (human)
calcium-mediated signalingTransient receptor potential cation channel subfamily M member 8Homo sapiens (human)
thermoceptionTransient receptor potential cation channel subfamily M member 8Homo sapiens (human)
calcium ion transmembrane transportTransient receptor potential cation channel subfamily M member 8Homo sapiens (human)
positive regulation of cold-induced thermogenesisTransient receptor potential cation channel subfamily M member 8Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (7)

Processvia Protein(s)Taxonomy
calcium channel activityTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
channel activityTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
intracellularly gated calcium channel activityTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
identical protein bindingTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
temperature-gated cation channel activityTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
calcium channel activityTransient receptor potential cation channel subfamily M member 8Homo sapiens (human)
protein bindingTransient receptor potential cation channel subfamily M member 8Homo sapiens (human)
identical protein bindingTransient receptor potential cation channel subfamily M member 8Homo sapiens (human)
ligand-gated calcium channel activityTransient receptor potential cation channel subfamily M member 8Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (5)

Processvia Protein(s)Taxonomy
plasma membraneTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
stereocilium bundleTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
endoplasmic reticulum membraneTransient receptor potential cation channel subfamily M member 8Homo sapiens (human)
plasma membraneTransient receptor potential cation channel subfamily M member 8Homo sapiens (human)
external side of plasma membraneTransient receptor potential cation channel subfamily M member 8Homo sapiens (human)
membrane raftTransient receptor potential cation channel subfamily M member 8Homo sapiens (human)
plasma membraneTransient receptor potential cation channel subfamily M member 8Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (52)

Assay IDTitleYearJournalArticle
AID1346567Mouse TRPA1 (Transient Receptor Potential channels)2003Cell, Mar-21, Volume: 112, Issue:6
ANKTM1, a TRP-like channel expressed in nociceptive neurons, is activated by cold temperatures.
AID1508628Confirmatory 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
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
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
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1508629Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1508627Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
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
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika 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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
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: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID482143Agonist activity at human TRPA1 channel expressed in HEK293 cells assessed as increase in intracellular calcium influx2010Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14
Transient receptor potential ankyrin 1 (TRPA1) channel as emerging target for novel analgesics and anti-inflammatory agents.
AID1204199Agonist activity at rat TRPM8 expressed in HEK293 cells assessed as induction of intracellular Ca2+ level by Fluo-4-AM dye based spectrofluorimetry relative to 4 uM ionomycin2015Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11
Structure-activity relationships of the prototypical TRPM8 agonist icilin.
AID1204201Antagonist activity against rat TRPM8 expressed in HEK293 cells assessed as inhibition of icilin-induced intracellular Ca2+ level pre-treated 5 mins before icilin stimulation by Fluo-4-AM dye based spectrofluorimetry2015Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11
Structure-activity relationships of the prototypical TRPM8 agonist icilin.
AID780253Inhibition of human TRPM8 (unknown origin) expressed in HEK293 cells assessed as inhibition of WS12-induced Ca2+ elevation by FLIPR assay2013Bioorganic & medicinal chemistry letters, Nov-15, Volume: 23, Issue:22
Serendipity in drug-discovery: a new series of 2-(benzyloxy)benzamides as TRPM8 antagonists.
AID329108Activation of mouse TRPA1 expressed in HEK293T cells at 100 uM assessed as activation of cation conductance by electrophysiology2007Nature, Feb-01, Volume: 445, Issue:7127
Noxious compounds activate TRPA1 ion channels through covalent modification of cysteines.
AID500219Agonist activity at TRPA12005Nature chemical biology, Jul, Volume: 1, Issue:2
Sensing with TRP channels.
AID500218Agonist activity at TRPM82005Nature chemical biology, Jul, Volume: 1, Issue:2
Sensing with TRP channels.
AID482150Activation of TRPM8 channel2010Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14
Transient receptor potential ankyrin 1 (TRPA1) channel as emerging target for novel analgesics and anti-inflammatory agents.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID392794Agonist activity at rat recombinant TRPM8 receptor expressed in HEK293 cells assessed as increase in intracellular calcium concentration by fluorimetric test2009Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4
Taste-guided identification of high potency TRPA1 agonists from Perilla frutescens.
AID1204200Agonist activity at rat TRPM8 expressed in HEK293 cells assessed as induction of intracellular Ca2+ level by Fluo-4-AM dye based spectrofluorimetry2015Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11
Structure-activity relationships of the prototypical TRPM8 agonist icilin.
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.
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.
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.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (125)

TimeframeStudies, This Drug (%)All Drugs %
pre-19903 (2.40)18.7374
1990's0 (0.00)18.2507
2000's42 (33.60)29.6817
2010's67 (53.60)24.3611
2020's13 (10.40)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 14.73

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 Index14.73 (24.57)
Research Supply Index4.84 (2.92)
Research Growth Index4.39 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (14.73)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews3 (2.38%)6.00%
Case Studies1 (0.79%)4.05%
Observational0 (0.00%)0.25%
Other122 (96.83%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]