Page last updated: 2024-11-13

gsk2256098

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

Description

GSK2256098: a focal adhesion kinase-1 antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID46214930
CHEMBL ID4742157
SCHEMBL ID691518
MeSH IDM000609321

Synonyms (39)

Synonym
S8523
gtpl7939
2-[(5-chloro-2-{[3-methyl-1-(propan-2-yl)-1h-pyrazol-5-yl]amino}pyridin-4-yl)amino]-n-methoxybenzamide
gsk2256098
gsk-2256098
SCHEMBL691518
BVAHPPKGOOJSPU-UHFFFAOYSA-N ,
2-[(5-chloro-2-{[3-methyl-1-(1-methylethyl)-1h-pyrazol-5-yl]amino}-4-pyridiny)amino]-n-(methyloxy)benzamide
2-[(5-chloro-2-{[3-methyl-1-(1-methylethyl)-1h-pyrazol-5-yl]amino}-4-pyridinyl)amino]-n-(methyloxy)benzamide
AC-29885
1224887-10-8
gsk 2256098
CS-6083
HY-100498
EX-A671
AS-74894
2-[[5-chloro-2-[[3-methyl-1-(1-methylethyl)-1h-pyrazol-5-yl]amino]-4-pyridinyl]amino]-n-methoxybenzamide
mfcd30502650
2-((5-chloro-2-((1-isopropyl-3-methyl-1h-pyrazol-5-yl)amino)pyridin-4-yl)amino)-n-methoxybenzamide
gsk2256098 [who-dd]
2-((5-chloro-2-((3-methyl-1-(1-methylethyl)-1h-pyrazol-5-yl)amino)-4-pyridinyl)amino)-n-methoxybenzamide
benzamide, 2-((5-chloro-2-((3-methyl-1-(1-methylethyl)-1h-pyrazol-5-yl)amino)-4-pyridinyl)amino)-n-methoxy-
R7O0O4110G ,
gtpl7939;2-[[5-chloro-2-[(5-methyl-2-propan-2-ylpyrazol-3-yl)amino]pyridin-4-yl]amino]-n-methoxybenzamide
unii-r7o0o4110g
A903443
AKOS030627136
BCP18311
Q27077884
AMY16729
2-[[5-chloro-2-[(5-methyl-2-propan-2-ylpyrazol-3-yl)amino]pyridin-4-yl]amino]-n-methoxybenzamide
benzamide, 2-[[5-chloro-2-[[3-methyl-1-(1-methylethyl)-1h-pyrazol-5-yl]amino]-4-pyridinyl]amino]-n-methoxy-
CCG-268826
B0084-470953
2-(5-chloro-2-(1-isopropyl-3-methyl-1h-pyrazol-5-ylamino)pyridin-4-ylamino)-n-methoxybenzamide
nsc-800999
nsc800999
CHEMBL4742157 ,
bdbm50568532

Research Excerpts

Overview

GSK2256098 is a novel oral focal adhesion kinase (FAK) inhibitor.

ExcerptReferenceRelevance
"GSK2256098 is a novel oral focal adhesion kinase (FAK) inhibitor. "( A study of the focal adhesion kinase inhibitor GSK2256098 in patients with recurrent glioblastoma with evaluation of tumor penetration of [11C]GSK2256098.
Arkenau, HT; Auger, KR; Blagden, S; Brown, NF; Cox, D; Fleming, RA; Lenox, L; Lewis, Y; Mulholland, P; Plisson, C; Saleem, A; Searle, G; Singh, R; Tolson, J; Williams, M; Yan, L; Zhang, J, 2018
)
2.18

Effects

ExcerptReferenceRelevance
"GSK2256098 has an acceptable safety profile, has evidence of target engagement at doses at or below the MTD, and has clinical activity in patients with mesothelioma, particularly those with merlin loss."( A phase I, pharmacokinetic and pharmacodynamic study of GSK2256098, a focal adhesion kinase inhibitor, in patients with advanced solid tumors.
Arkenau, HT; Auger, KR; Bahleda, R; Blagden, SP; Brown, J; Dean, E; Evans, TR; Fleming, RA; Gan, HK; Gibson, D; Hollebecque, A; Lemech, C; Mazumdar, J; Millward, M; Murray, S; Nebot, N; Peddareddigari, V; Plummer, R; Ranson, M; Singh, R; Soria, JC; Swartz, L; Zalcman, G, 2016
)
2.12

Treatment

ExcerptReferenceRelevance
"Treatment with GSK2256098 resulted in greater inhibition of pFAK(Y397) in PTEN-mutated (Ishikawa) than in PTEN-wild-type (Hec1A) cells."( PTEN Expression as a Predictor of Response to Focal Adhesion Kinase Inhibition in Uterine Cancer.
Ali-Fehmi, R; Armaiz-Pena, GN; Coleman, RL; Dalton, HJ; Dorniak, PL; Hansen, JM; Hu, W; Huang, J; Ivan, C; Previs, RA; Rupaimoole, R; Sood, AK; Thanapprapasr, D, 2015
)
0.76

Dosage Studied

ExcerptRelevanceReference
"Thirteen patients were treated in 3 dose cohorts (1000 mg, 750 mg, 500 mg; all dosed twice daily)."( A study of the focal adhesion kinase inhibitor GSK2256098 in patients with recurrent glioblastoma with evaluation of tumor penetration of [11C]GSK2256098.
Arkenau, HT; Auger, KR; Blagden, S; Brown, NF; Cox, D; Fleming, RA; Lenox, L; Lewis, Y; Mulholland, P; Plisson, C; Saleem, A; Searle, G; Singh, R; Tolson, J; Williams, M; Yan, L; Zhang, J, 2018
)
0.74
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
PPM1D proteinHomo sapiens (human)Potency20.82120.00529.466132.9993AID1347411
Interferon betaHomo sapiens (human)Potency20.82120.00339.158239.8107AID1347411
[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)
Focal adhesion kinase 1Homo sapiens (human)IC50 (µMol)0.00900.00020.54168.3000AID1755623; AID1755624; AID1755625; AID1755626
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (77)

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 macrophage chemotaxisFocal adhesion kinase 1Homo sapiens (human)
positive regulation of macrophage proliferationFocal adhesion kinase 1Homo sapiens (human)
angiogenesisFocal adhesion kinase 1Homo sapiens (human)
placenta developmentFocal adhesion kinase 1Homo sapiens (human)
regulation of protein phosphorylationFocal adhesion kinase 1Homo sapiens (human)
positive regulation of protein phosphorylationFocal adhesion kinase 1Homo sapiens (human)
heart morphogenesisFocal adhesion kinase 1Homo sapiens (human)
signal complex assemblyFocal adhesion kinase 1Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayFocal adhesion kinase 1Homo sapiens (human)
integrin-mediated signaling pathwayFocal adhesion kinase 1Homo sapiens (human)
axon guidanceFocal adhesion kinase 1Homo sapiens (human)
positive regulation of cell population proliferationFocal adhesion kinase 1Homo sapiens (human)
regulation of cell shapeFocal adhesion kinase 1Homo sapiens (human)
regulation of endothelial cell migrationFocal adhesion kinase 1Homo sapiens (human)
regulation of epithelial cell migrationFocal adhesion kinase 1Homo sapiens (human)
positive regulation of epithelial cell migrationFocal adhesion kinase 1Homo sapiens (human)
positive regulation of epithelial to mesenchymal transitionFocal adhesion kinase 1Homo sapiens (human)
positive regulation of fibroblast migrationFocal adhesion kinase 1Homo sapiens (human)
cell migrationFocal adhesion kinase 1Homo sapiens (human)
peptidyl-tyrosine phosphorylationFocal adhesion kinase 1Homo sapiens (human)
negative regulation of cell-cell adhesionFocal adhesion kinase 1Homo sapiens (human)
establishment of cell polarityFocal adhesion kinase 1Homo sapiens (human)
positive regulation of cell migrationFocal adhesion kinase 1Homo sapiens (human)
regulation of cell adhesion mediated by integrinFocal adhesion kinase 1Homo sapiens (human)
detection of muscle stretchFocal adhesion kinase 1Homo sapiens (human)
netrin-activated signaling pathwayFocal adhesion kinase 1Homo sapiens (human)
Fc-gamma receptor signaling pathway involved in phagocytosisFocal adhesion kinase 1Homo sapiens (human)
regulation of cell population proliferationFocal adhesion kinase 1Homo sapiens (human)
negative regulation of apoptotic processFocal adhesion kinase 1Homo sapiens (human)
regulation of GTPase activityFocal adhesion kinase 1Homo sapiens (human)
regulation of osteoblast differentiationFocal adhesion kinase 1Homo sapiens (human)
positive regulation of protein kinase activityFocal adhesion kinase 1Homo sapiens (human)
protein autophosphorylationFocal adhesion kinase 1Homo sapiens (human)
vascular endothelial growth factor receptor signaling pathwayFocal adhesion kinase 1Homo sapiens (human)
ephrin receptor signaling pathwayFocal adhesion kinase 1Homo sapiens (human)
cell motilityFocal adhesion kinase 1Homo sapiens (human)
regulation of cytoskeleton organizationFocal adhesion kinase 1Homo sapiens (human)
regulation of focal adhesion assemblyFocal adhesion kinase 1Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionFocal adhesion kinase 1Homo sapiens (human)
growth hormone receptor signaling pathwayFocal adhesion kinase 1Homo sapiens (human)
positive regulation of wound healingFocal adhesion kinase 1Homo sapiens (human)
regulation of substrate adhesion-dependent cell spreadingFocal adhesion kinase 1Homo sapiens (human)
positive regulation of ubiquitin-dependent protein catabolic processFocal adhesion kinase 1Homo sapiens (human)
negative regulation of anoikisFocal adhesion kinase 1Homo sapiens (human)
protein phosphorylationFocal adhesion kinase 1Homo sapiens (human)
epidermal growth factor receptor signaling pathwayFocal adhesion kinase 1Homo sapiens (human)
regulation of cell adhesionFocal adhesion kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (16)

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)
actin bindingFocal adhesion kinase 1Homo sapiens (human)
protein tyrosine kinase activityFocal adhesion kinase 1Homo sapiens (human)
non-membrane spanning protein tyrosine kinase activityFocal adhesion kinase 1Homo sapiens (human)
protein tyrosine phosphatase activityFocal adhesion kinase 1Homo sapiens (human)
integrin bindingFocal adhesion kinase 1Homo sapiens (human)
protein bindingFocal adhesion kinase 1Homo sapiens (human)
ATP bindingFocal adhesion kinase 1Homo sapiens (human)
JUN kinase bindingFocal adhesion kinase 1Homo sapiens (human)
protein kinase bindingFocal adhesion kinase 1Homo sapiens (human)
protein phosphatase bindingFocal adhesion kinase 1Homo sapiens (human)
SH2 domain bindingFocal adhesion kinase 1Homo sapiens (human)
molecular function activator activityFocal adhesion kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (15)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
stress fiberFocal adhesion kinase 1Homo sapiens (human)
nucleusFocal adhesion kinase 1Homo sapiens (human)
cytoplasmFocal adhesion kinase 1Homo sapiens (human)
centrosomeFocal adhesion kinase 1Homo sapiens (human)
cytosolFocal adhesion kinase 1Homo sapiens (human)
cytoskeletonFocal adhesion kinase 1Homo sapiens (human)
plasma membraneFocal adhesion kinase 1Homo sapiens (human)
focal adhesionFocal adhesion kinase 1Homo sapiens (human)
cell cortexFocal adhesion kinase 1Homo sapiens (human)
ciliary basal bodyFocal adhesion kinase 1Homo sapiens (human)
intracellular membrane-bounded organelleFocal adhesion kinase 1Homo sapiens (human)
perinuclear region of cytoplasmFocal adhesion kinase 1Homo sapiens (human)
plasma membraneFocal adhesion kinase 1Homo sapiens (human)
focal adhesionFocal adhesion kinase 1Homo sapiens (human)
dendritic spineFocal adhesion kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (14)

Assay IDTitleYearJournalArticle
AID1755625Inhibition of FAK in human OVCAR8 cells assessed as reduction in phosphorylation at Y397 residue incubated for 30 mins by Western blot analysis2020Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
Progress in the Development of Small Molecular Inhibitors of Focal Adhesion Kinase (FAK).
AID1755623Inhibition of FAK in human U87MG cells assessed as reduction in phosphorylation at Y397 residue incubated for 30 mins by Western blot analysis2020Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
Progress in the Development of Small Molecular Inhibitors of Focal Adhesion Kinase (FAK).
AID1755626Inhibition of FAK (unknown origin)2020Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
Progress in the Development of Small Molecular Inhibitors of Focal Adhesion Kinase (FAK).
AID1675117Selectivity ratio of inhibition of Pyk2 (unknown origin) to inhibition of tracer 236 binding to recombinant human GST-tagged full length FAK expressed in baculovirus expression system incubated for 1 hr by Lanthascreen TR-FRET assay2020Bioorganic & medicinal chemistry letters, 11-01, Volume: 30, Issue:21
Design, synthesis and biological evaluation of ring-fused pyrazoloamino pyridine/pyrimidine derivatives as potential FAK inhibitors.
AID1675123Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability2020Bioorganic & medicinal chemistry letters, 11-01, Volume: 30, Issue:21
Design, synthesis and biological evaluation of ring-fused pyrazoloamino pyridine/pyrimidine derivatives as potential FAK inhibitors.
AID1755624Inhibition of FAK in human A549 cells assessed as reduction in phosphorylation at Y397 residue incubated for 30 mins by Western blot analysis2020Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
Progress in the Development of Small Molecular Inhibitors of Focal Adhesion Kinase (FAK).
AID1675126Inhibition of FAK (unknown origin)2020Bioorganic & medicinal chemistry letters, 11-01, Volume: 30, Issue:21
Design, synthesis and biological evaluation of ring-fused pyrazoloamino pyridine/pyrimidine derivatives as potential FAK inhibitors.
AID1675121Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability2020Bioorganic & medicinal chemistry letters, 11-01, Volume: 30, Issue:21
Design, synthesis and biological evaluation of ring-fused pyrazoloamino pyridine/pyrimidine derivatives as potential FAK inhibitors.
AID1675124Inhibition of tracer 236 binding to recombinant human GST-tagged full length FAK expressed in baculovirus expression system incubated for 1 hr by Lanthascreen TR-FRET assay2020Bioorganic & medicinal chemistry letters, 11-01, Volume: 30, Issue:21
Design, synthesis and biological evaluation of ring-fused pyrazoloamino pyridine/pyrimidine derivatives as potential FAK inhibitors.
AID1675119Antiproliferative activity against human 786-O cells assessed as reduction in cell viability2020Bioorganic & medicinal chemistry letters, 11-01, Volume: 30, Issue:21
Design, synthesis and biological evaluation of ring-fused pyrazoloamino pyridine/pyrimidine derivatives as potential FAK inhibitors.
AID1675118Inhibition of FAK autophosphorylation assessed as decrease in ratio of Phospho-Tyr397-FAK to total FAK in human MDA-MB-231 cells ast 0.1 uM incubated for 1 hr by ELISA2020Bioorganic & medicinal chemistry letters, 11-01, Volume: 30, Issue:21
Design, synthesis and biological evaluation of ring-fused pyrazoloamino pyridine/pyrimidine derivatives as potential FAK inhibitors.
AID1675120Antiproliferative activity against human DU-145 cells assessed as reduction in cell viability2020Bioorganic & medicinal chemistry letters, 11-01, Volume: 30, Issue:21
Design, synthesis and biological evaluation of ring-fused pyrazoloamino pyridine/pyrimidine derivatives as potential FAK inhibitors.
AID1675122Antiproliferative activity against human BXPC-3 cells assessed as reduction in cell viability2020Bioorganic & medicinal chemistry letters, 11-01, Volume: 30, Issue:21
Design, synthesis and biological evaluation of ring-fused pyrazoloamino pyridine/pyrimidine derivatives as potential FAK inhibitors.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (11)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's6 (54.55)24.3611
2020's5 (45.45)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 29.43

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 Index29.43 (24.57)
Research Supply Index2.77 (2.92)
Research Growth Index4.58 (4.65)
Search Engine Demand Index31.18 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (29.43)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials4 (36.36%)5.53%
Reviews2 (18.18%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other5 (45.45%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]