Page last updated: 2024-11-13

gsk-7975a

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

Description

2,6-difluoro-N-(1-(4-hydroxy-2-(trifluoromethyl)benzyl)-1H-pyrazol-3-yl)benzamide: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID59547990
CHEMBL ID4570175
SCHEMBL ID705705
MeSH IDM0588099

Synonyms (18)

Synonym
SCHEMBL705705
2,6-difluoro-n-(1-{[4-hydroxy-2-(trifluoromethyl)phenyl]methyl}-1h-pyrazol-3-yl)benzamide
gsk-7975a
1253186-56-9
CS-8058
HY-12507
2,6-difluoro-n-(1-(4-hydroxy-2-(trifluoromethyl)benzyl)-1h-pyrazol-3-yl)benzamide
NCGC00402346-02
2,6-difluoro-n-[1-[[4-hydroxy-2-(trifluoromethyl)phenyl]methyl]pyrazol-3-yl]benzamide
E73436
gtpl10088
gsk7975a
example 36 [us20120053150a1]
SB19206
BS-44817
CHEMBL4570175 ,
bdbm50575335
AKOS040741814

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 (10)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency9.52210.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency6.00810.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency21.31740.00108.379861.1304AID1645840
Interferon betaHomo sapiens (human)Potency6.00810.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency6.00810.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency6.00810.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency6.00810.01238.964839.8107AID1645842
[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 1Homo sapiens (human)IC50 (µMol)4.00000.50002.78334.3000AID1774818; AID1774819
Calcium release-activated calcium channel protein 1Homo sapiens (human)IC50 (µMol)4.00000.50004.25009.8000AID1774818
Protein orai-3Homo sapiens (human)IC50 (µMol)4.00004.00007.50009.8000AID1774819
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (62)

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)
store-operated calcium entryStromal interaction molecule 1Homo sapiens (human)
detection of calcium ionStromal interaction molecule 1Homo sapiens (human)
activation of store-operated calcium channel activityStromal interaction molecule 1Homo sapiens (human)
positive regulation of adenylate cyclase activityStromal interaction molecule 1Homo sapiens (human)
positive regulation of angiogenesisStromal interaction molecule 1Homo sapiens (human)
regulation of calcium ion transportStromal interaction molecule 1Homo sapiens (human)
enamel mineralizationStromal interaction molecule 1Homo sapiens (human)
regulation of store-operated calcium entryStromal interaction molecule 1Homo sapiens (human)
intracellular calcium ion homeostasisStromal interaction molecule 1Homo 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)
store-operated calcium entryProtein orai-3Homo sapiens (human)
calcium ion transmembrane transportProtein orai-3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (26)

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)
protease bindingStromal interaction molecule 1Homo sapiens (human)
calcium channel regulator activityStromal interaction molecule 1Homo sapiens (human)
calcium ion bindingStromal interaction molecule 1Homo sapiens (human)
protein bindingStromal interaction molecule 1Homo sapiens (human)
identical protein bindingStromal interaction molecule 1Homo sapiens (human)
microtubule plus-end bindingStromal interaction molecule 1Homo 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)
protein bindingProtein orai-3Homo sapiens (human)
store-operated calcium channel activityProtein orai-3Homo 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)
endoplasmic reticulumStromal interaction molecule 1Homo sapiens (human)
endoplasmic reticulum membraneStromal interaction molecule 1Homo sapiens (human)
microtubuleStromal interaction molecule 1Homo sapiens (human)
plasma membraneStromal interaction molecule 1Homo sapiens (human)
cortical endoplasmic reticulumStromal interaction molecule 1Homo sapiens (human)
sarcoplasmic reticulum membraneStromal interaction molecule 1Homo sapiens (human)
plasma membrane raftStromal interaction molecule 1Homo sapiens (human)
endoplasmic reticulumStromal interaction molecule 1Homo sapiens (human)
plasma membraneStromal interaction molecule 1Homo 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 membraneProtein orai-3Homo sapiens (human)
membraneProtein orai-3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (7)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
AID1774818Inhibition of human STIM1/Orai1 expressed in HEK293 cells assessed as reduction in Orai1 current by electrophysiological method2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
Discovery of a Novel Potent and Selective Calcium Release-Activated Calcium Channel Inhibitor: 2,6-Difluoro-
AID1774819Inhibition of human STIM1/Orai3 expressed in HEK293 cells assessed as reduction in Orai3 current by electrophysiological method2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
Discovery of a Novel Potent and Selective Calcium Release-Activated Calcium Channel Inhibitor: 2,6-Difluoro-
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (12)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's7 (58.33)24.3611
2020's5 (41.67)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 21.35

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 Index21.35 (24.57)
Research Supply Index2.56 (2.92)
Research Growth Index4.62 (4.65)
Search Engine Demand Index18.60 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (21.35)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other12 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]