Page last updated: 2024-12-04

clemizole

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

Description

Clemizole is a histamine H1 receptor antagonist that was originally developed as an antihistamine. It has also been shown to have anticholinergic and antiemetic effects. Clemizole is synthesized via a multi-step process involving the reaction of 2-chloro-N-(2-dimethylaminoethyl)benzamide with 1-phenyl-1-propanol. The compound exhibits a high affinity for the H1 receptor, blocking the binding of histamine and thus preventing its effects. Research into Clemizole has focused on its potential therapeutic applications in conditions such as allergic rhinitis, urticaria, and motion sickness. However, it has not been widely used clinically due to its potential for side effects, including drowsiness, dry mouth, and blurred vision. Further research is needed to explore the therapeutic potential of Clemizole and to optimize its safety profile.'

clemizole: was heading 1966-94 (see under BENZIMIDAZOLES 1966-90); use BENZIMIDAZOLES to search CLEMIZOLE 1966-94; a histamine H1- blocker used to treat allergies [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

clemizole : A member of the class of benzimidazoles that is 1H-benzimidazole substituted by a pyrrolidin-1-ylmethyl and a 4-chlorobenzyl groups at positions 2 and 1 respectively. [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]

Cross-References

ID SourceID
PubMed CID2782
CHEMBL ID1407943
CHEBI ID52140
SCHEMBL ID29938
MeSH IDM0224666

Synonyms (88)

Synonym
BRD-K04704168-003-03-6
benzimidazole, 1-(p-chlorobenzyl)-2-(1-pyrrolidinylmethyl)-
histacur
nsc-46261
histakool
clemizol
442-52-4
clemizole
nsc46261
1h-benzimidazole, 1-[(4-chlorophenyl)methyl]-2-(1-pyrrolidinylmethyl)-
1-(p-chlorobenzyl)-2-pyrrolidylmethylenebenzimidazole
BPBIO1_000301
NCGC00015243-02
cas-1163-36-6
NCGC00015243-01
lopac-c-5040
BSPBIO_000273
PRESTWICK2_000227
PRESTWICK3_000227
OPREA1_226569
LOPAC0_000284
1-[(4-chlorophenyl)methyl]-2-(pyrrolidinylmethyl)-1h-benzimidazole
1-[(4-chlorophenyl)methyl]-2-(pyrrolidin-1-ylmethyl)benzimidazole
SPBIO_002194
PRESTWICK0_000227
PRESTWICK1_000227
NCGC00024376-03
NCGC00015243-03
lergopenin
depocural
clemizolum
CHEBI:52140 ,
1-(4-chlorobenzyl)-2-(pyrrolidin-1-ylmethyl)-1h-benzimidazole
NCGC00015243-07
L000853
AKOS001631429
nsc_2782
bdbm85747
cas_442-52-4
CCG-106577
NCGC00015243-05
NCGC00015243-06
NCGC00015243-04
einecs 207-133-5
clemizole [inn:ban]
1h-benzimidazole, 1-((4-chlorophenyl)methyl)-2-(1-pyrrolidinylmethyl)-
clemizolo [dcit]
clemizolo
clemizol [inn-spanish]
al 20 [as hydrochloride]
t97cb3796l ,
clemizolum [inn-latin]
nsc 46261
unii-t97cb3796l
1-p-chlorobenzyl-2-(1-pyrrolidinylmethyl)benzimidazole
clemizole [mi]
clemizole [who-dd]
clemizole [inn]
CHEMBL1407943
al-20 free base
S6410
HY-30234
CS-1481
1-(4-chlorobenzyl)-2-(pyrrolidin-1-ylmethyl)-1h-benzo[d]imidazole
SCHEMBL29938
DTXSID0046939
c19h20cln3
1-[(4-chlorophenyl)methyl]-2-(1-pyrrolidinylmethyl)-1h-benzimidazole
pyrrolidine, 1-[(1-p-chlorobenzyl-2-benzimidazolyl)methyl]-
1-(4-chlorobenzyl)-2-(1-pyrrolidinylmethyl)-1h-benzimidazole #
SR-01000000057-6
mfcd00051434
1-(4-chlorobenzyl)-2-pyrrolidinomethyl-benzimidazole
SR-01000000057-9
SBI-0050272.P002
NCGC00015243-11
clemizole (free base)
BCP07894
Q5131527
F0902-3266
BRD-K04704168-003-11-9
gtpl10285
SDCCGSBI-0050272.P003
NCGC00015243-20
NCGC00015243-21
(3-oxo-2-pentyl-cyclopentyl)-aceticacidmethylester
GX0 ,
AS-56130

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" It has many important toxic side effects; one of the most important of which is nephrotoxicity."( Clemizole hydrochloride, a potent TRPC5 calcium channel inhibitor, prevents cisplatin-induced nephrotoxicity in Spraque-Dawley rats.
Eşrefoğlu, M; Gepdiremen, A; Karataş, E; Kumaş-Kulualp, M, 2023
)
2.35

Compound-Compound Interactions

ExcerptReferenceRelevance
"Interspecies differences in drug metabolism have made it difficult to use preclinical animal testing data to predict the drug metabolites or potential drug-drug interactions (DDIs) that will occur in humans."( Using chimeric mice with humanized livers to predict human drug metabolism and a drug-drug interaction.
Angus, P; Chen, Y; Elazar, M; Fitch, WL; Glenn, J; Hu, Y; Idilman, R; Liu, M; Murphy, B; Nakamura, M; Nishimura, T; Nomura, T; Peltz, G; Pham, E; Stedman, C; Suemizu, H; Wu, M; Yurdaydin, C; Zheng, M, 2013
)
0.39

Bioavailability

ExcerptReferenceRelevance
"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
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
histamine antagonistHistamine antagonists are the drugs that bind to but do not activate histamine receptors, thereby blocking the actions of histamine or histamine agonists.
[role 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]

Drug Classes (3)

ClassDescription
pyrrolidinesAny of a class of heterocyclic amines having a saturated five-membered ring.
benzimidazolesAn organic heterocyclic compound containing a benzene ring fused to an imidazole ring.
monochlorobenzenesAny member of the class of chlorobenzenes containing a mono- or poly-substituted benzene ring in which only one substituent is chlorine.
[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 (46)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency22.38720.004023.8416100.0000AID485290
USP1 protein, partialHomo sapiens (human)Potency20.08270.031637.5844354.8130AID504865
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency11.89610.00137.762544.6684AID914; AID915
thyroid stimulating hormone receptorHomo sapiens (human)Potency12.58930.001318.074339.8107AID926; AID938
arylsulfatase AHomo sapiens (human)Potency0.00541.069113.955137.9330AID720538
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency1.02660.00207.533739.8107AID891
cytochrome P450 2C19 precursorHomo sapiens (human)Potency0.19950.00255.840031.6228AID899
cytochrome P450 2C9 precursorHomo sapiens (human)Potency25.11890.00636.904339.8107AID883
chromobox protein homolog 1Homo sapiens (human)Potency89.12510.006026.168889.1251AID488953
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency16.48160.00669.809418.4927AID1347050
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency12.58930.00798.23321,122.0200AID2546
gemininHomo sapiens (human)Potency9.03490.004611.374133.4983AID624297
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency13.78940.005612.367736.1254AID624032
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency6.30960.031610.279239.8107AID884; AID885
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency6.30960.00106.000935.4813AID943
lamin isoform A-delta10Homo sapiens (human)Potency0.15850.891312.067628.1838AID1487
pyruvate kinase PKM isoform bHomo sapiens (human)Potency0.00792.511912.262825.1189AID954; AID958
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency4.49650.316212.765731.6228AID881
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency13.33470.00638.235039.8107AID881; AID883
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
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 V member 1Rattus norvegicus (Norway rat)IC50 (µMol)20.00000.00040.21474.0000AID1578727
Short transient receptor potential channel 3Homo sapiens (human)IC50 (µMol)9.10000.47002.29299.1000AID1578724
Heat sensitive channel TRPV3Rattus norvegicus (Norway rat)IC50 (µMol)20.00000.75000.75000.7500AID1578729
Transient receptor potential cation channel subfamily V member 4 Mus musculus (house mouse)IC50 (µMol)20.00000.01702.95855.9000AID1578730
Short transient receptor potential channel 4 Mus musculus (house mouse)IC50 (µMol)6.40000.96003.41506.4000AID1578723
Short transient receptor potential channel 5Mus musculus (house mouse)IC50 (µMol)1.10001.10004.65008.2000AID1578722
Transient receptor potential cation channel subfamily V member 2Rattus norvegicus (Norway rat)IC50 (µMol)20.00000.03701.93458.6000AID1578728
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (35)

Processvia Protein(s)Taxonomy
lipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
phospholipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
apoptotic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell population proliferationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of macrophage derived foam cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell migrationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
prostate gland developmentPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
regulation of epithelial cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of chemokine productionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of peroxisome proliferator activated receptor signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of keratinocyte differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell cyclePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of growthPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
hepoxilin biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
endocannabinoid signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cannabinoid biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxin A4 biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid oxidationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxygenase pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
calcium ion transportShort transient receptor potential channel 3Homo sapiens (human)
phototransductionShort transient receptor potential channel 3Homo sapiens (human)
positive regulation of calcium ion transport into cytosolShort transient receptor potential channel 3Homo sapiens (human)
response to ATPShort transient receptor potential channel 3Homo sapiens (human)
response to calcium ionShort transient receptor potential channel 3Homo sapiens (human)
calcium ion transmembrane transportShort transient receptor potential channel 3Homo sapiens (human)
positive regulation of cardiac muscle hypertrophy in response to stressShort transient receptor potential channel 3Homo sapiens (human)
single fertilizationShort transient receptor potential channel 3Homo sapiens (human)
regulation of cytosolic calcium ion concentrationShort transient receptor potential channel 3Homo sapiens (human)
manganese ion transportShort transient receptor potential channel 7Mus musculus (house mouse)
calcium ion transportShort transient receptor potential channel 7Mus musculus (house mouse)
positive regulation of ion transmembrane transporter activityShort transient receptor potential channel 6Homo sapiens (human)
positive regulation of calcium ion transportShort transient receptor potential channel 6Homo sapiens (human)
monoatomic cation transportShort transient receptor potential channel 6Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationShort transient receptor potential channel 6Homo sapiens (human)
calcium ion transmembrane transportShort transient receptor potential channel 6Homo sapiens (human)
regulation of cytosolic calcium ion concentrationShort transient receptor potential channel 6Homo sapiens (human)
single fertilizationShort transient receptor potential channel 6Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (15)

Processvia Protein(s)Taxonomy
iron ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
calcium ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
protein bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 13S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 8(S)-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 15-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 9S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
calcium-activated cation channel activityShort transient receptor potential channel 3Homo sapiens (human)
calcium channel activityShort transient receptor potential channel 3Homo sapiens (human)
protein bindingShort transient receptor potential channel 3Homo sapiens (human)
metal ion bindingShort transient receptor potential channel 3Homo sapiens (human)
inositol 1,4,5 trisphosphate bindingShort transient receptor potential channel 3Homo sapiens (human)
store-operated calcium channel activityShort transient receptor potential channel 3Homo sapiens (human)
calcium channel activityShort transient receptor potential channel 7Mus musculus (house mouse)
monoatomic cation channel activityShort transient receptor potential channel 6Homo sapiens (human)
calcium channel activityShort transient receptor potential channel 6Homo sapiens (human)
protein bindingShort transient receptor potential channel 6Homo sapiens (human)
protein homodimerization activityShort transient receptor potential channel 6Homo sapiens (human)
inositol 1,4,5 trisphosphate bindingShort transient receptor potential channel 6Homo sapiens (human)
store-operated calcium channel activityShort transient receptor potential channel 6Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (11)

Processvia Protein(s)Taxonomy
nucleusPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytosolPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytoskeletonPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
plasma membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
adherens junctionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
focal adhesionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
extracellular exosomePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
plasma membraneShort transient receptor potential channel 3Homo sapiens (human)
cation channel complexShort transient receptor potential channel 3Homo sapiens (human)
plasma membraneShort transient receptor potential channel 3Homo sapiens (human)
cytoplasmShort transient receptor potential channel 6Homo sapiens (human)
plasma membraneShort transient receptor potential channel 6Homo sapiens (human)
membraneShort transient receptor potential channel 6Homo sapiens (human)
slit diaphragmShort transient receptor potential channel 6Homo sapiens (human)
plasma membraneShort transient receptor potential channel 6Homo sapiens (human)
cation channel complexShort transient receptor potential channel 6Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (48)

Assay IDTitleYearJournalArticle
AID1578731Selectivity ratio of IC50 for YFP-tagged human TRPC6 expressed in thapsigargin treated HEK293 cells to IC50 for mouse TRPC5 expressed in thapsigargin treated HEK293/TREx cells2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Review of Transient Receptor Potential Canonical (TRPC5) Channel Modulators and Diseases.
AID1072668Cytotoxicity against human Huh7.5 cells assessed as cell viability at 10 uM after 72 hrs by MTT assay relative to control2014European journal of medicinal chemistry, Mar-21, Volume: 75Chemical genetics-based discovery of indole derivatives as HCV NS5B polymerase inhibitors.
AID1578729Inhibition of YFP-tagged rat TRPV3 expressed in HEK293 cells assessed as reduction in calcium level by fluo-4 dye based fluorescence assay2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Review of Transient Receptor Potential Canonical (TRPC5) Channel Modulators and Diseases.
AID1578728Inhibition of YFP-tagged rat TRPV2 expressed in HEK293 cells assessed as reduction in calcium level by fluo-4 dye based fluorescence assay2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Review of Transient Receptor Potential Canonical (TRPC5) Channel Modulators and Diseases.
AID1578727Inhibition of CFP-tagged rat TRPV1 expressed in HEK293 cells assessed as reduction in calcium level by fluo-4 dye based fluorescence assay2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Review of Transient Receptor Potential Canonical (TRPC5) Channel Modulators and Diseases.
AID1578733Selectivity ratio of IC50 for YFP-tagged mouse TRPC7 expressed in thapsigargin treated HEK293 cells to IC50 for mouse TRPC5 expressed in thapsigargin treated HEK293/TREx cells2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Review of Transient Receptor Potential Canonical (TRPC5) Channel Modulators and Diseases.
AID1578732Selectivity ratio of IC50 for YFP-tagged human TRPC3 expressed in thapsigargin treated HEK293 cells to IC50 for mouse TRPC5 expressed in thapsigargin treated HEK293/TREx cells2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Review of Transient Receptor Potential Canonical (TRPC5) Channel Modulators and Diseases.
AID1578724Inhibition of YFP-tagged human TRPC3 expressed in thapsigargin treated HEK293 cells assessed as reduction in amix-induced calcium level by fluo-4 dye based fluorescence assay2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Review of Transient Receptor Potential Canonical (TRPC5) Channel Modulators and Diseases.
AID1578730Inhibition of YFP-tagged mouse TRPV4 expressed in HEK293 cells assessed as reduction in calcium level by fluo-4 dye based fluorescence assay2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Review of Transient Receptor Potential Canonical (TRPC5) Channel Modulators and Diseases.
AID1578734Selectivity ratio of IC50 for YFP-tagged mouse TRPC4 beta expressed in thapsigargin treated HEK293 cells co-expressing M3 receptor to IC50 for mouse TRPC5 expressed in thapsigargin treated HEK293/TREx cells2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Review of Transient Receptor Potential Canonical (TRPC5) Channel Modulators and Diseases.
AID1072666Antiviral activity against Hepatitis C virus JFH-1 J6 genotype 2a infected in human Huh7.5 cells assessed as inhibition of viral RNA replication after 72 hrs by luciferase reporter gene assay2014European journal of medicinal chemistry, Mar-21, Volume: 75Chemical genetics-based discovery of indole derivatives as HCV NS5B polymerase inhibitors.
AID1270709Antiviral activity against HCV genotype 1b infected in Huh7.5 cells assessed as inhibition of viral replication at 72 hrs by luciferase reporter-based viral replicon assay2016Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
A Journey around the Medicinal Chemistry of Hepatitis C Virus Inhibitors Targeting NS4B: From Target to Preclinical Drug Candidates.
AID1072669Antiviral activity against Hepatitis C virus JFH-1 J6 genotype 2a infected in human Huh7.5 cells assessed as inhibition of viral RNA replication at 10 uM after 72 hrs by luciferase reporter gene assay relative to control2014European journal of medicinal chemistry, Mar-21, Volume: 75Chemical genetics-based discovery of indole derivatives as HCV NS5B polymerase inhibitors.
AID1072667Ratio of cytotoxicity against human Huh7.5 cells assessed as cell viability to antiviral activity against Hepatitis C virus JFH-1 J6 genotype 2a infected in human Huh7.5 cells assessed as inhibition of viral RNA replication2014European journal of medicinal chemistry, Mar-21, Volume: 75Chemical genetics-based discovery of indole derivatives as HCV NS5B polymerase inhibitors.
AID1270708Antiviral activity against HCV genotype 2a infected in Huh7.5 cells assessed as inhibition of viral replication at 72 hrs by luciferase reporter-based viral replicon assay2016Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
A Journey around the Medicinal Chemistry of Hepatitis C Virus Inhibitors Targeting NS4B: From Target to Preclinical Drug Candidates.
AID1578722Inhibition of mouse TRPC5 expressed in thapsigargin treated HEK293/TREx cells assessed as reduction in intracellular calcium level in presence of GPCR agonist by fluorescence method2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Review of Transient Receptor Potential Canonical (TRPC5) Channel Modulators and Diseases.
AID1072665Cytotoxicity against human Huh7.5 cells assessed as cell viability after 72 hrs by MTT assay2014European journal of medicinal chemistry, Mar-21, Volume: 75Chemical genetics-based discovery of indole derivatives as HCV NS5B polymerase inhibitors.
AID1578725Inhibition of YFP-tagged human TRPC6 expressed in thapsigargin treated HEK293 cells assessed as reduction in amix-induced calcium level by fluo-4 dye based fluorescence assay2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Review of Transient Receptor Potential Canonical (TRPC5) Channel Modulators and Diseases.
AID1270707Inhibition of HCV GST-tagged recombinant NS3/4A protease expressed in Escherichia coli by microfluidic affinity assay2016Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
A Journey around the Medicinal Chemistry of Hepatitis C Virus Inhibitors Targeting NS4B: From Target to Preclinical Drug Candidates.
AID1578723Inhibition of YFP-tagged mouse TRPC4 beta expressed in thapsigargin treated HEK293 cells co-expressing M3 receptor assessed as reduction in carbachol-induced calcium level by fluo-4 dye based fluorescence assay2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Review of Transient Receptor Potential Canonical (TRPC5) Channel Modulators and Diseases.
AID1072664Selectivity index, ratio of CC50 for human Huh7.5 cells to EC50 for Hepatitis C virus JFH-1 J6 genotype 2a infected in human Huh7.5 cells2014European journal of medicinal chemistry, Mar-21, Volume: 75Chemical genetics-based discovery of indole derivatives as HCV NS5B polymerase inhibitors.
AID1578726Inhibition of YFP-tagged mouse TRPC7 expressed in thapsigargin treated HEK293 cells assessed as reduction in amix-induced calcium level by fluo-4 dye based fluorescence assay2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Review of Transient Receptor Potential Canonical (TRPC5) Channel Modulators and Diseases.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
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.
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS 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.
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.
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.
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.
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.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (43)

TimeframeStudies, This Drug (%)All Drugs %
pre-19905 (11.63)18.7374
1990's1 (2.33)18.2507
2000's3 (6.98)29.6817
2010's21 (48.84)24.3611
2020's13 (30.23)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 38.34

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 strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index38.34 (24.57)
Research Supply Index3.78 (2.92)
Research Growth Index5.40 (4.65)
Search Engine Demand Index50.91 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (38.34)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews3 (6.98%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other40 (93.02%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]