Page last updated: 2024-11-04

ym 58483

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 CID2455
CHEMBL ID262766
SCHEMBL ID676045
MeSH IDM0472656

Synonyms (44)

Synonym
gtpl2438
ym-58483
btp2
IDI1_018066
crac channel inhibitor, btp2
MAYBRIDGE3_006679
SR-01000644222-1
HMS1449P13
CHEMBL262766 ,
n-[4-[3,5-bis(trifluoromethyl)pyrazol-1-yl]phenyl]-4-methylthiadiazole-5-carboxamide
CCG-55182
223499-30-7
S8380
btp-2
SCHEMBL676045
ym 58483
n-[4-[3,5-bis(trifluoromethyl)-1h-pyrazol-1-yl]phenyl]-4-methyl-1,2,3-thiadiazole-5-carboxamide
AKOS024457886
HMS3648I22
ym-58483 (btp2)
DTXSID50274370
ym-58483, >=98% (hplc)
HY-100831
CS-6047
J-014660
NCGC00344111-03
bdbm50204544
1,2,3-thiadiazole-5-carboxamide,n-[4-[3,5-bis(trifluoromethyl)-1h-pyrazol-1-yl]phenyl]-4-methyl-
n-(4-(3,5-bis(trifluoromethyl)-1h-pyrazol-1-yl)phenyl)-4-methyl-1,2,3-thiadiazole-5-carboxamide
BCP19298
EX-A2467
Q27075544
AS-16763
SR-01000644222-3
sr-01000644222
ym58483
A16346
HMS3886H10
C74150
A910597
crac channel inhibitor, btp2 - cas 223499-30-7
4-methyl-[1,2,3]thiadiazole-5-carboxylic acid [4-(3,5-bis-trifluoromethyl-pyrazol-1-yl)-phenyl]-amide
xprziordevhurq-uhfffaoysa-n
AC-35791

Research Excerpts

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]

Protein Targets (12)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency2.68370.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency15.09160.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency10.68400.00108.379861.1304AID1645840
Interferon betaHomo sapiens (human)Potency15.09160.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency15.09160.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency15.09160.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency15.09160.01238.964839.8107AID1645842
[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)
Stromal interaction molecule 1Rattus norvegicus (Norway rat)IC50 (µMol)0.59000.54000.56500.5900AID1578744
Short transient receptor potential channel 3Homo sapiens (human)IC50 (µMol)4.21000.47002.29299.1000AID1578743
Calcium release-activated calcium channel protein 1Rattus norvegicus (Norway rat)IC50 (µMol)0.59000.54000.56500.5900AID1578744
Calcium release-activated calcium channel protein 1Homo sapiens (human)IC50 (µMol)2.80000.50004.25009.8000AID1330311
Short transient receptor potential channel 5Homo sapiens (human)IC50 (µMol)0.30000.30002.78756.5000AID1578740
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (75)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo 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)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
store-operated calcium entryCalcium release-activated calcium channel protein 1Homo sapiens (human)
adaptive immune responseCalcium release-activated calcium channel protein 1Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayCalcium release-activated calcium channel protein 1Homo sapiens (human)
positive regulation of insulin secretionCalcium release-activated calcium channel protein 1Homo sapiens (human)
positive regulation of adenylate cyclase activityCalcium release-activated calcium channel protein 1Homo sapiens (human)
regulation of calcium ion transportCalcium release-activated calcium channel protein 1Homo sapiens (human)
positive regulation of calcium ion transportCalcium release-activated calcium channel protein 1Homo sapiens (human)
mammary gland epithelium developmentCalcium release-activated calcium channel protein 1Homo sapiens (human)
calcium ion importCalcium release-activated calcium channel protein 1Homo sapiens (human)
calcium ion transmembrane transportCalcium release-activated calcium channel protein 1Homo sapiens (human)
ion channel modulating, G protein-coupled receptor signaling pathwayCalcium release-activated calcium channel protein 1Homo sapiens (human)
ligand-gated ion channel signaling pathwayCalcium release-activated calcium channel protein 1Homo sapiens (human)
calcium ion transportShort transient receptor potential channel 5Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationShort transient receptor potential channel 5Homo sapiens (human)
nervous system developmentShort transient receptor potential channel 5Homo sapiens (human)
positive regulation of cell population proliferationShort transient receptor potential channel 5Homo sapiens (human)
positive regulation of peptidyl-threonine phosphorylationShort transient receptor potential channel 5Homo sapiens (human)
neuron differentiationShort transient receptor potential channel 5Homo sapiens (human)
positive regulation of neuron differentiationShort transient receptor potential channel 5Homo sapiens (human)
positive regulation of axon extensionShort transient receptor potential channel 5Homo sapiens (human)
negative regulation of dendrite morphogenesisShort transient receptor potential channel 5Homo sapiens (human)
neuron apoptotic processShort transient receptor potential channel 5Homo sapiens (human)
calcium ion transmembrane transportShort transient receptor potential channel 5Homo sapiens (human)
phosphatidylserine exposure on apoptotic cell surfaceShort transient receptor potential channel 5Homo sapiens (human)
regulation of membrane hyperpolarizationShort transient receptor potential channel 5Homo sapiens (human)
regulation of cytosolic calcium ion concentrationShort transient receptor potential channel 5Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (29)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo 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)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
calcium channel activityCalcium release-activated calcium channel protein 1Homo sapiens (human)
protein bindingCalcium release-activated calcium channel protein 1Homo sapiens (human)
calmodulin bindingCalcium release-activated calcium channel protein 1Homo sapiens (human)
store-operated calcium channel activityCalcium release-activated calcium channel protein 1Homo sapiens (human)
identical protein bindingCalcium release-activated calcium channel protein 1Homo sapiens (human)
actin bindingShort transient receptor potential channel 5Homo sapiens (human)
calcium channel activityShort transient receptor potential channel 5Homo sapiens (human)
protein bindingShort transient receptor potential channel 5Homo sapiens (human)
clathrin bindingShort transient receptor potential channel 5Homo sapiens (human)
actinin bindingShort transient receptor potential channel 5Homo sapiens (human)
ATPase bindingShort transient receptor potential channel 5Homo sapiens (human)
store-operated calcium channel activityShort transient receptor potential channel 5Homo sapiens (human)
inositol 1,4,5 trisphosphate bindingShort transient receptor potential channel 5Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (30)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
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)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
plasma membraneCalcium release-activated calcium channel protein 1Homo sapiens (human)
membraneCalcium release-activated calcium channel protein 1Homo sapiens (human)
basolateral plasma membraneCalcium release-activated calcium channel protein 1Homo sapiens (human)
plasma membrane raftCalcium release-activated calcium channel protein 1Homo sapiens (human)
membrane raftCalcium release-activated calcium channel protein 1Homo sapiens (human)
calcium channel complexCalcium release-activated calcium channel protein 1Homo sapiens (human)
membraneCalcium release-activated calcium channel protein 1Homo sapiens (human)
plasma membraneShort transient receptor potential channel 5Homo sapiens (human)
dendriteShort transient receptor potential channel 5Homo sapiens (human)
growth coneShort transient receptor potential channel 5Homo sapiens (human)
neuronal cell bodyShort transient receptor potential channel 5Homo sapiens (human)
calcium channel complexShort transient receptor potential channel 5Homo sapiens (human)
cation channel complexShort transient receptor potential channel 5Homo sapiens (human)
plasma membraneShort transient receptor potential channel 5Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (34)

Assay IDTitleYearJournalArticle
AID1640018Luciferase/luciferin-expressing antifolate-resistant parasites were used to infect a culture of HepG2 cells that were pre-incubated with compounds. Infected hepatocytes emit light due to the luciferase reaction. Assay results are presented as the percent 2018Science (New York, N.Y.), 12-07, Volume: 362, Issue:6419
Open-source discovery of chemical leads for next-generation chemoprotective antimalarials.
AID388936Inhibition of CRAC channel-mediated calcium influx in human Jurkat cells2008Bioorganic & medicinal chemistry, Nov-01, Volume: 16, Issue:21
Novel potent and selective Ca2+ release-activated Ca2+ (CRAC) channel inhibitors. Part 3: synthesis and CRAC channel inhibitory activity of 4'-[(trifluoromethyl)pyrazol-1-yl]carboxanilides.
AID1330315Antagonist activity at rat TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin-stimulated Ca2+ flux up to 100 uM after 30 mins by calcium-4 dye based FLIPR assay2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Evaluation of known and novel inhibitors of Orai1-mediated store operated Ca
AID1578744Inhibition of ORAI/STIM1 in thapsigargin treated rat RBL2H3 cells assessed as reduction in store-operated calcium entry after 5 mins by fura-2-AM dye based assay2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Review of Transient Receptor Potential Canonical (TRPC5) Channel Modulators and Diseases.
AID1330310Inhibition of Orai1-mediated store operated Ca2+ entry in human MDA-MB-231 cells assessed as reduction of SERCA inhibition-induced ER release at 100 uM preincubated for 15 mins followed by CPA addition by PBX-based FLIPR assay2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Evaluation of known and novel inhibitors of Orai1-mediated store operated Ca
AID16042In vitro protein binding in human serum at 5 ug/ml2000Journal of medicinal chemistry, Aug-10, Volume: 43, Issue:16
3,5-Bis(trifluoromethyl)pyrazoles: a novel class of NFAT transcription factor regulator.
AID388938Inhibition of VOC channel-mediated calcium influx in mouse PC12-h5 cells2008Bioorganic & medicinal chemistry, Nov-01, Volume: 16, Issue:21
Novel potent and selective Ca2+ release-activated Ca2+ (CRAC) channel inhibitors. Part 3: synthesis and CRAC channel inhibitory activity of 4'-[(trifluoromethyl)pyrazol-1-yl]carboxanilides.
AID388942Inhibition of trinitrochlorobenzene-induced contact hypersensitivity in 1 hr before pretreated CD1 mouse assessed as ear swelling at 30 mg/kg, po2008Bioorganic & medicinal chemistry, Nov-01, Volume: 16, Issue:21
Novel potent and selective Ca2+ release-activated Ca2+ (CRAC) channel inhibitors. Part 3: synthesis and CRAC channel inhibitory activity of 4'-[(trifluoromethyl)pyrazol-1-yl]carboxanilides.
AID1578743Inhibition of YFP-tagged TRPC3 (unknown origin) expressed in HEK293 cells assessed as reduction carbhocol-induced receptor operated Calcium influx after 5 mins by fura-2-AM dye based assay2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Review of Transient Receptor Potential Canonical (TRPC5) Channel Modulators and Diseases.
AID152934Inhibition of concanavalin A (con A)-induced proliferation of human peripheral blood mononuclear cells.2000Journal of medicinal chemistry, Aug-10, Volume: 43, Issue:16
3,5-Bis(trifluoromethyl)pyrazoles: a novel class of NFAT transcription factor regulator.
AID1330311Inhibition of Orai1-mediated store operated Ca2+ entry in human MDA-MB-231 cells assessed as reduction in BAPTA-induced Ca2+ depletion-stimulated SOCE activity preincubated for 15 mins followed by BAPTA addition in presence of extracellular Ca2+ by PBX-ba2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Evaluation of known and novel inhibitors of Orai1-mediated store operated Ca
AID1192970Lipophilicity, log D of the compound at pH 7.42015Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
Discovery of 7-azaindole derivatives as potent Orai inhibitors showing efficacy in a preclinical model of asthma.
AID1578740Inhibition of TRPC5 (unknown origin)2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Review of Transient Receptor Potential Canonical (TRPC5) Channel Modulators and Diseases.
AID1330319Ratio of IC50 for Kcl-induced voltage-gated calcium channel in rat PC12-h cells to IC50 for thapsigargin-induced SOC in human Jurkat cells2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Evaluation of known and novel inhibitors of Orai1-mediated store operated Ca
AID1640019Luciferase/luciferin-expressing antifolate-resistant parasites were used to infect a culture of HepG2 cells that were pre-incubated with compounds. Infected hepatocytes emit light due to the luciferase reaction. Assay results are presented as the percent 2018Science (New York, N.Y.), 12-07, Volume: 362, Issue:6419
Open-source discovery of chemical leads for next-generation chemoprotective antimalarials.
AID388944Inhibition of ovalbumin-induced airway eosinophilia in BN rat po dosed 1 hr before antigen challenge assessed as number of eosinophils in bronchoalveolar levage fluid after 24 hrs2008Bioorganic & medicinal chemistry, Nov-01, Volume: 16, Issue:21
Novel potent and selective Ca2+ release-activated Ca2+ (CRAC) channel inhibitors. Part 3: synthesis and CRAC channel inhibitory activity of 4'-[(trifluoromethyl)pyrazol-1-yl]carboxanilides.
AID152960Inhibition of concanavalin A (con A)-induced proliferation of rat peripheral blood mononuclear cells.2000Journal of medicinal chemistry, Aug-10, Volume: 43, Issue:16
3,5-Bis(trifluoromethyl)pyrazoles: a novel class of NFAT transcription factor regulator.
AID1330316Antagonist activity at rat TRPM8 expressed in HEK293 cells assessed as inhibition of menthol-stimulated Ca2+ flux up to 100 uM after 30 mins by calcium-4 dye based FLIPR assay2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Evaluation of known and novel inhibitors of Orai1-mediated store operated Ca
AID1634820Cytotoxicity in mouse B16F10 cells at <3 ug/ml measured after 48 hrs by MTT assay2016Journal of natural products, Apr-22, Volume: 79, Issue:4
Valencene from the Rhizomes of Cyperus rotundus Inhibits Skin Photoaging-Related Ion Channels and UV-Induced Melanogenesis in B16F10 Melanoma Cells.
AID1192972Inhibition of Orai channel in phytohemagglutinin-stimulated human Jurkat E6-1 cells assessed as NFAT-induced transcription measured as IL-2 level after 20 hrs by ELISA2015Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
Discovery of 7-azaindole derivatives as potent Orai inhibitors showing efficacy in a preclinical model of asthma.
AID388940Selectivity ratio of IC50 for CRAC channel in human Jurkat cells over IC50 for VOC channel in mouse PC12-h5 cells2008Bioorganic & medicinal chemistry, Nov-01, Volume: 16, Issue:21
Novel potent and selective Ca2+ release-activated Ca2+ (CRAC) channel inhibitors. Part 3: synthesis and CRAC channel inhibitory activity of 4'-[(trifluoromethyl)pyrazol-1-yl]carboxanilides.
AID388941Inhibition of PHA-induced IL2 production in human Jurkat T lymphocytes2008Bioorganic & medicinal chemistry, Nov-01, Volume: 16, Issue:21
Novel potent and selective Ca2+ release-activated Ca2+ (CRAC) channel inhibitors. Part 3: synthesis and CRAC channel inhibitory activity of 4'-[(trifluoromethyl)pyrazol-1-yl]carboxanilides.
AID1330317Antagonist activity at Cav2.2 in human SH-SY5Y cells assessed as inhibition of KCl/CaCl2-stimulated Ca2+ flux up to 100 uM after 30 mins in presence of nifedipine by Fuo-4 dye based FLIPR assay2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Evaluation of known and novel inhibitors of Orai1-mediated store operated Ca
AID92874Inhibition of interleukin-2 (IL-2) synthesis in human whole blood stimulated by PMA/ionomycin.2000Journal of medicinal chemistry, Aug-10, Volume: 43, Issue:16
3,5-Bis(trifluoromethyl)pyrazoles: a novel class of NFAT transcription factor regulator.
AID1192971Inhibition of Orai-mediated calcium entry in human Jurkat E6-1 cells after 1 hr by FLIPR assay2015Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
Discovery of 7-azaindole derivatives as potent Orai inhibitors showing efficacy in a preclinical model of asthma.
AID388943Inhibition of trinitrochlorobenzene-induced contact hypersensitivity in 1 hr before orally pretreated CD1 mouse assessed as ear swelling2008Bioorganic & medicinal chemistry, Nov-01, Volume: 16, Issue:21
Novel potent and selective Ca2+ release-activated Ca2+ (CRAC) channel inhibitors. Part 3: synthesis and CRAC channel inhibitory activity of 4'-[(trifluoromethyl)pyrazol-1-yl]carboxanilides.
AID1496393Inhibition of CRAC in human Jurkat T cells assessed as increase in TG-stimulated intracellular calcium depletion measured every 8 secs by Ca2+ dye based fluorescence assay2018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
An SAR study of hydroxy-trifluoromethylpyrazolines as inhibitors of Orai1-mediated store operated Ca
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.
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.
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.
AID1346599Human TRPM4 (Transient Receptor Potential channels)2006Molecular pharmacology, Apr, Volume: 69, Issue:4
A pyrazole derivative potently inhibits lymphocyte Ca2+ influx and cytokine production by facilitating transient receptor potential melastatin 4 channel activity.
AID1346581Human TRPC3 (Transient Receptor Potential channels)2005The Journal of biological chemistry, Mar-25, Volume: 280, Issue:12
A functional link between store-operated and TRPC channels revealed by the 3,5-bis(trifluoromethyl)pyrazole derivative, BTP2.
[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's0 (0.00)18.2507
2000's4 (30.77)29.6817
2010's7 (53.85)24.3611
2020's2 (15.38)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 27.04

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

MetricThis Compound (vs All)
Research Demand Index27.04 (24.57)
Research Supply Index2.64 (2.92)
Research Growth Index5.12 (4.65)
Search Engine Demand Index29.12 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (27.04)

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]