Page last updated: 2024-11-12

gw 799388

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Description

4-(4-(3-(pyridin-2-yl)-1H-pyrazol-4-yl)pyridin-2-yl)-N-(tetrahydro-2H-pyran-4-yl)benzamide: a TGF type I receptor antagonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID10202642
CHEMBL ID202887
SCHEMBL ID373524
SCHEMBL ID17926774
MeSH IDM0497587

Synonyms (41)

Synonym
HY-10326
gw788388 ,
4-(4-(3-(pyridin-2-yl)-1h-pyrazol-4-yl)pyridin-2-yl)-n-(tetrahydro-2h-pyran-4-yl)benzamide
gw-788388
4-{4-[3-(pyridin-2-yl)-1h-pyrazol-4-yl]-pyridin-2-yl}-n-(tetrahydro-2h-pyran-4-yl)benzamide
bdbm50184872
CHEMBL202887 ,
gw 788388
AKOS016005022
BCP9000754
452342-67-5
n-(oxan-4-yl)-4-{4-[3-(pyridin-2-yl)-1h-pyrazol-4-yl]pyridin-2-yl}benzamide
BCP0726000062
NCGC00346679-01
CS-0254
S2750
n14114957j ,
4-(4-(3-(pyridin-2-yl)-1h-pyrazol-4-yl)pyridin-2-yl)-n-(tetrahydropyran-4-yl)benzamide
unii-n14114957j
benzamide, 4-(4-(3-(2-pyridinyl)-1h-pyrazol-4-yl)-2-pyridinyl)-n-(tetrahydro-2h-pyran-4-yl)-
SCHEMBL373524
4-[4-[3-(2-pyridinyl)-1h-pyrazol-4-yl]-2-pyridinyl]-n-(tetrahydro-2h-pyran-4-yl)-benzamide
4-[4-[3-(pyridin-2-yl)-1h-pyrazol-4-yl]pyridin-2-yl]-n-(tetrahydropyran-4-yl)benzamide
AC-31390
AKOS026750217
DTXSID70196444
EX-A122
SCHEMBL17926774
HMS3656N21
mfcd16038936
AS-74347
NCGC00346679-10
SW219194-1
BCP04559
FT-0700309
SB19488
CCG-268948
Q27284368
A872408
NCGC00346679-04
n-(oxan-4-yl)-4-[4-(5-pyridin-2-yl-1h-pyrazol-4-yl)pyridin-2-yl]benzamide

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

Dosage Studied

ExcerptRelevanceReference
" Sprague-Dawley rats underwent left anterior descending coronary artery ligation to induce experimental MI and then were randomized to receive GW788388 at a dosage of 50 mg."( Targeted inhibition of activin receptor-like kinase 5 signaling attenuates cardiac dysfunction following myocardial infarction.
Connelly, KA; Gilbert, RE; Kelly, DJ; Tan, SM; Zhang, Y, 2010
)
0.36
[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)Potency37.90830.01237.983543.2770AID1645841
EWS/FLI fusion proteinHomo sapiens (human)Potency19.38480.001310.157742.8575AID1259252; AID1259253; AID1259256
GVesicular stomatitis virusPotency21.31740.01238.964839.8107AID1645842
Interferon betaHomo sapiens (human)Potency21.31740.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency21.31740.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency21.31740.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency21.31740.01238.964839.8107AID1645842
[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)
Activin receptor type-1BHomo sapiens (human)IC50 (µMol)1.00000.01302.53009.6220AID618730
TGF-beta receptor type-1Homo sapiens (human)IC50 (µMol)0.16070.00100.643610.0000AID262766; AID447434; AID618729
Mitogen-activated protein kinase 14Homo sapiens (human)IC50 (µMol)7.28000.00010.72667.8000AID262781
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (186)

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)
G1/S transition of mitotic cell cycleActivin receptor type-1BHomo sapiens (human)
in utero embryonic developmentActivin receptor type-1BHomo sapiens (human)
hair follicle developmentActivin receptor type-1BHomo sapiens (human)
regulation of DNA-templated transcriptionActivin receptor type-1BHomo sapiens (human)
signal transductionActivin receptor type-1BHomo sapiens (human)
cell surface receptor protein serine/threonine kinase signaling pathwayActivin receptor type-1BHomo sapiens (human)
positive regulation of gene expressionActivin receptor type-1BHomo sapiens (human)
negative regulation of gene expressionActivin receptor type-1BHomo sapiens (human)
peptidyl-threonine phosphorylationActivin receptor type-1BHomo sapiens (human)
negative regulation of cell growthActivin receptor type-1BHomo sapiens (human)
activin receptor signaling pathwayActivin receptor type-1BHomo sapiens (human)
positive regulation of activin receptor signaling pathwayActivin receptor type-1BHomo sapiens (human)
nodal signaling pathwayActivin receptor type-1BHomo sapiens (human)
positive regulation of erythrocyte differentiationActivin receptor type-1BHomo sapiens (human)
protein autophosphorylationActivin receptor type-1BHomo sapiens (human)
extrinsic apoptotic signaling pathwayActivin receptor type-1BHomo sapiens (human)
positive regulation of trophoblast cell migrationActivin receptor type-1BHomo sapiens (human)
cellular response to growth factor stimulusActivin receptor type-1BHomo sapiens (human)
protein phosphorylationActivin receptor type-1BHomo sapiens (human)
nervous system developmentActivin receptor type-1BHomo sapiens (human)
proepicardium developmentTGF-beta receptor type-1Homo sapiens (human)
negative regulation of cell migrationTGF-beta receptor type-1Homo sapiens (human)
positive regulation of extracellular matrix assemblyTGF-beta receptor type-1Homo sapiens (human)
skeletal system developmentTGF-beta receptor type-1Homo sapiens (human)
in utero embryonic developmentTGF-beta receptor type-1Homo sapiens (human)
kidney developmentTGF-beta receptor type-1Homo sapiens (human)
blastocyst developmentTGF-beta receptor type-1Homo sapiens (human)
epithelial to mesenchymal transitionTGF-beta receptor type-1Homo sapiens (human)
endothelial cell proliferationTGF-beta receptor type-1Homo sapiens (human)
negative regulation of endothelial cell proliferationTGF-beta receptor type-1Homo sapiens (human)
positive regulation of endothelial cell proliferationTGF-beta receptor type-1Homo sapiens (human)
lens development in camera-type eyeTGF-beta receptor type-1Homo sapiens (human)
ventricular trabecula myocardium morphogenesisTGF-beta receptor type-1Homo sapiens (human)
ventricular compact myocardium morphogenesisTGF-beta receptor type-1Homo sapiens (human)
regulation of DNA-templated transcriptionTGF-beta receptor type-1Homo sapiens (human)
apoptotic processTGF-beta receptor type-1Homo sapiens (human)
signal transductionTGF-beta receptor type-1Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayTGF-beta receptor type-1Homo sapiens (human)
heart developmentTGF-beta receptor type-1Homo sapiens (human)
positive regulation of cell population proliferationTGF-beta receptor type-1Homo sapiens (human)
germ cell migrationTGF-beta receptor type-1Homo sapiens (human)
male gonad developmentTGF-beta receptor type-1Homo sapiens (human)
post-embryonic developmentTGF-beta receptor type-1Homo sapiens (human)
anterior/posterior pattern specificationTGF-beta receptor type-1Homo sapiens (human)
positive regulation of gene expressionTGF-beta receptor type-1Homo sapiens (human)
regulation of epithelial to mesenchymal transitionTGF-beta receptor type-1Homo sapiens (human)
positive regulation of epithelial to mesenchymal transitionTGF-beta receptor type-1Homo sapiens (human)
peptidyl-serine phosphorylationTGF-beta receptor type-1Homo sapiens (human)
collagen fibril organizationTGF-beta receptor type-1Homo sapiens (human)
positive regulation of cell growthTGF-beta receptor type-1Homo sapiens (human)
positive regulation of cell migrationTGF-beta receptor type-1Homo sapiens (human)
regulation of protein ubiquitinationTGF-beta receptor type-1Homo sapiens (human)
negative regulation of chondrocyte differentiationTGF-beta receptor type-1Homo sapiens (human)
activin receptor signaling pathwayTGF-beta receptor type-1Homo sapiens (human)
intracellular signal transductionTGF-beta receptor type-1Homo sapiens (human)
myofibroblast differentiationTGF-beta receptor type-1Homo sapiens (human)
wound healingTGF-beta receptor type-1Homo sapiens (human)
endothelial cell activationTGF-beta receptor type-1Homo sapiens (human)
extracellular structure organizationTGF-beta receptor type-1Homo sapiens (human)
endothelial cell migrationTGF-beta receptor type-1Homo sapiens (human)
positive regulation of DNA-templated transcriptionTGF-beta receptor type-1Homo sapiens (human)
filopodium assemblyTGF-beta receptor type-1Homo sapiens (human)
thymus developmentTGF-beta receptor type-1Homo sapiens (human)
neuron fate commitmentTGF-beta receptor type-1Homo sapiens (human)
embryonic cranial skeleton morphogenesisTGF-beta receptor type-1Homo sapiens (human)
skeletal system morphogenesisTGF-beta receptor type-1Homo sapiens (human)
mesenchymal cell differentiationTGF-beta receptor type-1Homo sapiens (human)
artery morphogenesisTGF-beta receptor type-1Homo sapiens (human)
cell motilityTGF-beta receptor type-1Homo sapiens (human)
positive regulation of filopodium assemblyTGF-beta receptor type-1Homo sapiens (human)
positive regulation of stress fiber assemblyTGF-beta receptor type-1Homo sapiens (human)
regulation of cell cycleTGF-beta receptor type-1Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionTGF-beta receptor type-1Homo sapiens (human)
parathyroid gland developmentTGF-beta receptor type-1Homo sapiens (human)
roof of mouth developmentTGF-beta receptor type-1Homo sapiens (human)
pharyngeal system developmentTGF-beta receptor type-1Homo sapiens (human)
regulation of cardiac muscle cell proliferationTGF-beta receptor type-1Homo sapiens (human)
cardiac epithelial to mesenchymal transitionTGF-beta receptor type-1Homo sapiens (human)
positive regulation of SMAD protein signal transductionTGF-beta receptor type-1Homo sapiens (human)
ventricular septum morphogenesisTGF-beta receptor type-1Homo sapiens (human)
angiogenesis involved in coronary vascular morphogenesisTGF-beta receptor type-1Homo sapiens (human)
coronary artery morphogenesisTGF-beta receptor type-1Homo sapiens (human)
response to cholesterolTGF-beta receptor type-1Homo sapiens (human)
cellular response to transforming growth factor beta stimulusTGF-beta receptor type-1Homo sapiens (human)
positive regulation of mesenchymal stem cell proliferationTGF-beta receptor type-1Homo sapiens (human)
positive regulation of vasculature developmentTGF-beta receptor type-1Homo sapiens (human)
positive regulation of epithelial to mesenchymal transition involved in endocardial cushion formationTGF-beta receptor type-1Homo sapiens (human)
positive regulation of tight junction disassemblyTGF-beta receptor type-1Homo sapiens (human)
epicardium morphogenesisTGF-beta receptor type-1Homo sapiens (human)
positive regulation of apoptotic signaling pathwayTGF-beta receptor type-1Homo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathwayTGF-beta receptor type-1Homo sapiens (human)
protein phosphorylationTGF-beta receptor type-1Homo sapiens (human)
cellular response to growth factor stimulusTGF-beta receptor type-1Homo sapiens (human)
nervous system developmentTGF-beta receptor type-1Homo sapiens (human)
positive regulation of blood vessel endothelial cell migrationMitogen-activated protein kinase 14Homo sapiens (human)
cellular response to lipopolysaccharideMitogen-activated protein kinase 14Homo sapiens (human)
DNA damage checkpoint signalingMitogen-activated protein kinase 14Homo sapiens (human)
cell morphogenesisMitogen-activated protein kinase 14Homo sapiens (human)
cartilage condensationMitogen-activated protein kinase 14Homo sapiens (human)
angiogenesisMitogen-activated protein kinase 14Homo sapiens (human)
osteoblast differentiationMitogen-activated protein kinase 14Homo sapiens (human)
placenta developmentMitogen-activated protein kinase 14Homo sapiens (human)
response to dietary excessMitogen-activated protein kinase 14Homo sapiens (human)
chondrocyte differentiationMitogen-activated protein kinase 14Homo sapiens (human)
negative regulation of inflammatory response to antigenic stimulusMitogen-activated protein kinase 14Homo sapiens (human)
glucose metabolic processMitogen-activated protein kinase 14Homo sapiens (human)
regulation of transcription by RNA polymerase IIMitogen-activated protein kinase 14Homo sapiens (human)
transcription by RNA polymerase IIMitogen-activated protein kinase 14Homo sapiens (human)
apoptotic processMitogen-activated protein kinase 14Homo sapiens (human)
chemotaxisMitogen-activated protein kinase 14Homo sapiens (human)
signal transductionMitogen-activated protein kinase 14Homo sapiens (human)
cell surface receptor signaling pathwayMitogen-activated protein kinase 14Homo sapiens (human)
cell surface receptor protein serine/threonine kinase signaling pathwayMitogen-activated protein kinase 14Homo sapiens (human)
skeletal muscle tissue developmentMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of gene expressionMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of myotube differentiationMitogen-activated protein kinase 14Homo sapiens (human)
peptidyl-serine phosphorylationMitogen-activated protein kinase 14Homo sapiens (human)
fatty acid oxidationMitogen-activated protein kinase 14Homo sapiens (human)
platelet activationMitogen-activated protein kinase 14Homo sapiens (human)
regulation of ossificationMitogen-activated protein kinase 14Homo sapiens (human)
osteoclast differentiationMitogen-activated protein kinase 14Homo sapiens (human)
stress-activated protein kinase signaling cascadeMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of cyclase activityMitogen-activated protein kinase 14Homo sapiens (human)
lipopolysaccharide-mediated signaling pathwayMitogen-activated protein kinase 14Homo sapiens (human)
response to muramyl dipeptideMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of interleukin-12 productionMitogen-activated protein kinase 14Homo sapiens (human)
response to insulinMitogen-activated protein kinase 14Homo sapiens (human)
negative regulation of hippo signalingMitogen-activated protein kinase 14Homo sapiens (human)
intracellular signal transductionMitogen-activated protein kinase 14Homo sapiens (human)
cellular response to vascular endothelial growth factor stimulusMitogen-activated protein kinase 14Homo sapiens (human)
response to muscle stretchMitogen-activated protein kinase 14Homo sapiens (human)
p38MAPK cascadeMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of protein import into nucleusMitogen-activated protein kinase 14Homo sapiens (human)
signal transduction in response to DNA damageMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of erythrocyte differentiationMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of myoblast differentiationMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIMitogen-activated protein kinase 14Homo sapiens (human)
glucose importMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of glucose importMitogen-activated protein kinase 14Homo sapiens (human)
vascular endothelial growth factor receptor signaling pathwayMitogen-activated protein kinase 14Homo sapiens (human)
stem cell differentiationMitogen-activated protein kinase 14Homo sapiens (human)
striated muscle cell differentiationMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of muscle cell differentiationMitogen-activated protein kinase 14Homo sapiens (human)
stress-activated MAPK cascadeMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of cardiac muscle cell proliferationMitogen-activated protein kinase 14Homo sapiens (human)
bone developmentMitogen-activated protein kinase 14Homo sapiens (human)
3'-UTR-mediated mRNA stabilizationMitogen-activated protein kinase 14Homo sapiens (human)
cellular response to lipoteichoic acidMitogen-activated protein kinase 14Homo sapiens (human)
cellular response to tumor necrosis factorMitogen-activated protein kinase 14Homo sapiens (human)
cellular response to ionizing radiationMitogen-activated protein kinase 14Homo sapiens (human)
cellular response to UV-BMitogen-activated protein kinase 14Homo sapiens (human)
negative regulation of canonical Wnt signaling pathwayMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of brown fat cell differentiationMitogen-activated protein kinase 14Homo sapiens (human)
cellular senescenceMitogen-activated protein kinase 14Homo sapiens (human)
stress-induced premature senescenceMitogen-activated protein kinase 14Homo sapiens (human)
cellular response to virusMitogen-activated protein kinase 14Homo sapiens (human)
regulation of synaptic membrane adhesionMitogen-activated protein kinase 14Homo sapiens (human)
regulation of cytokine production involved in inflammatory responseMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of myoblast fusionMitogen-activated protein kinase 14Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processMitogen-activated protein kinase 14Homo 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (41)

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)
activin receptor activityActivin receptor type-1BHomo sapiens (human)
growth factor bindingActivin receptor type-1BHomo sapiens (human)
activin bindingActivin receptor type-1BHomo sapiens (human)
protein serine/threonine kinase activityActivin receptor type-1BHomo sapiens (human)
transmembrane receptor protein serine/threonine kinase activityActivin receptor type-1BHomo sapiens (human)
protein bindingActivin receptor type-1BHomo sapiens (human)
ATP bindingActivin receptor type-1BHomo sapiens (human)
activin receptor activity, type IActivin receptor type-1BHomo sapiens (human)
activin receptor activityActivin receptor type-1BHomo sapiens (human)
ubiquitin protein ligase bindingActivin receptor type-1BHomo sapiens (human)
inhibin bindingActivin receptor type-1BHomo sapiens (human)
SMAD bindingActivin receptor type-1BHomo sapiens (human)
metal ion bindingActivin receptor type-1BHomo sapiens (human)
I-SMAD bindingActivin receptor type-1BHomo sapiens (human)
transforming growth factor beta receptor activityTGF-beta receptor type-1Homo sapiens (human)
growth factor bindingTGF-beta receptor type-1Homo sapiens (human)
transforming growth factor beta bindingTGF-beta receptor type-1Homo sapiens (human)
protein kinase activityTGF-beta receptor type-1Homo sapiens (human)
protein serine/threonine kinase activityTGF-beta receptor type-1Homo sapiens (human)
transmembrane receptor protein serine/threonine kinase activityTGF-beta receptor type-1Homo sapiens (human)
transforming growth factor beta receptor activityTGF-beta receptor type-1Homo sapiens (human)
transforming growth factor beta receptor activity, type ITGF-beta receptor type-1Homo sapiens (human)
type II transforming growth factor beta receptor bindingTGF-beta receptor type-1Homo sapiens (human)
protein bindingTGF-beta receptor type-1Homo sapiens (human)
ATP bindingTGF-beta receptor type-1Homo sapiens (human)
ubiquitin protein ligase bindingTGF-beta receptor type-1Homo sapiens (human)
SMAD bindingTGF-beta receptor type-1Homo sapiens (human)
metal ion bindingTGF-beta receptor type-1Homo sapiens (human)
transforming growth factor beta bindingTGF-beta receptor type-1Homo sapiens (human)
I-SMAD bindingTGF-beta receptor type-1Homo sapiens (human)
activin receptor activity, type ITGF-beta receptor type-1Homo sapiens (human)
activin bindingTGF-beta receptor type-1Homo sapiens (human)
protein serine/threonine kinase activityMitogen-activated protein kinase 14Homo sapiens (human)
MAP kinase activityMitogen-activated protein kinase 14Homo sapiens (human)
MAP kinase kinase activityMitogen-activated protein kinase 14Homo sapiens (human)
protein bindingMitogen-activated protein kinase 14Homo sapiens (human)
ATP bindingMitogen-activated protein kinase 14Homo sapiens (human)
enzyme bindingMitogen-activated protein kinase 14Homo sapiens (human)
protein phosphatase bindingMitogen-activated protein kinase 14Homo sapiens (human)
mitogen-activated protein kinase p38 bindingMitogen-activated protein kinase 14Homo sapiens (human)
NFAT protein bindingMitogen-activated protein kinase 14Homo sapiens (human)
protein serine kinase activityMitogen-activated protein kinase 14Homo 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (34)

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)
cytosolActivin receptor type-1BHomo sapiens (human)
plasma membraneActivin receptor type-1BHomo sapiens (human)
cell surfaceActivin receptor type-1BHomo sapiens (human)
receptor complexActivin receptor type-1BHomo sapiens (human)
activin receptor complexActivin receptor type-1BHomo sapiens (human)
plasma membraneActivin receptor type-1BHomo sapiens (human)
nucleusTGF-beta receptor type-1Homo sapiens (human)
endosomeTGF-beta receptor type-1Homo sapiens (human)
plasma membraneTGF-beta receptor type-1Homo sapiens (human)
bicellular tight junctionTGF-beta receptor type-1Homo sapiens (human)
cell surfaceTGF-beta receptor type-1Homo sapiens (human)
membrane raftTGF-beta receptor type-1Homo sapiens (human)
transforming growth factor beta ligand-receptor complexTGF-beta receptor type-1Homo sapiens (human)
receptor complexTGF-beta receptor type-1Homo sapiens (human)
plasma membraneTGF-beta receptor type-1Homo sapiens (human)
activin receptor complexTGF-beta receptor type-1Homo sapiens (human)
cytosolMitogen-activated protein kinase 14Homo sapiens (human)
spindle poleMitogen-activated protein kinase 14Homo sapiens (human)
extracellular regionMitogen-activated protein kinase 14Homo sapiens (human)
nucleusMitogen-activated protein kinase 14Homo sapiens (human)
nucleoplasmMitogen-activated protein kinase 14Homo sapiens (human)
cytoplasmMitogen-activated protein kinase 14Homo sapiens (human)
mitochondrionMitogen-activated protein kinase 14Homo sapiens (human)
cytosolMitogen-activated protein kinase 14Homo sapiens (human)
nuclear speckMitogen-activated protein kinase 14Homo sapiens (human)
secretory granule lumenMitogen-activated protein kinase 14Homo sapiens (human)
glutamatergic synapseMitogen-activated protein kinase 14Homo sapiens (human)
ficolin-1-rich granule lumenMitogen-activated protein kinase 14Homo sapiens (human)
nucleusMitogen-activated protein kinase 14Homo sapiens (human)
cytoplasmMitogen-activated protein kinase 14Homo 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (66)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID262783Inhibition of Chk1 at 10 uM in presence of 100 uM ATP2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.
AID262780Inhibition of PAN-induced renal collagen IA1 expression by TGF beta in Sprague-Dawley rat at 10 mg/kg, po2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.
AID262770Plasma clearance in Sprague-Dawley rat at 2 mg/kg, iv or 4 mg/kg, po2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.
AID262792Inhibition of PhosK at 10 uM in presence of 100 uM ATP2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.
AID262768Intrinsic clearance in Sprague-Dawley rat liver microsome2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.
AID262794Inhibition of PKC A at 10 uM in presence of 100 uM ATP2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.
AID262769Oral bioavailability in Sprague-Dawley rat at 2 mg/kg, iv and 4 mg/kg, po2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.
AID262797Inhibition of P38-beta at 10 uM in presence of 100 uM ATP2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.
AID262789Inhibition of MAPK2 at 10 uM in presence of 100 uM ATP2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.
AID262786Inhibition of LCK at 10 uM in presence of 100 uM ATP2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.
AID262771Volume of distribution in Sprague-Dawley rat at 2 mg/kg, iv or 4 mg/kg, po2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.
AID262785Inhibition of JNK1 at 10 uM in presence of 100 uM ATP2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.
AID262790Inhibition of P70S6K at 10 uM in presence of 100 uM ATP2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.
AID262779Inhibition of PAN-induced renal collagen IA1 expression by TGF beta in Sprague-Dawley rat at 3 mg/kg, po2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.
AID262791Inhibition of PDK1 at 10 uM in presence of 100 uM ATP2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.
AID618729Inhibition of TGF-beta1 signaling in human HEK293 cells transfected with luciferase and FAST-2 gene expression vector A3-LUX after 16 hrs by luciferase reporter gene assay2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
2-Phenyl and 2-heterocyclic-4-(3-(pyridin-2-yl)-1H-pyrazol-4-yl)pyridines as inhibitors of TGF-β1 and activin A signalling.
AID262772Half life in Sprague-Dawley rat plasma2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.
AID618726Inhibition of TGF-beta1 signaling in human HEK293 cells transfected with luciferase and FAST-2 gene expression vector A3-LUX at 100 nM after 16 hrs by luciferase reporter gene assay relative to control2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
2-Phenyl and 2-heterocyclic-4-(3-(pyridin-2-yl)-1H-pyrazol-4-yl)pyridines as inhibitors of TGF-β1 and activin A signalling.
AID262767Inhibition of TGF beta-induced transcription of firefly luciferase reporter gene in HepG2 cells2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.
AID262777Inhibition of DMN-induced collagen IA1 expression by TGF beta in Sprague-Dawley rat liver at 5 mg/kg, po2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.
AID447434Inhibition of TGFR12009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Pharmacophore modeling and virtual screening for the discovery of new transforming growth factor-beta type I receptor (ALK5) inhibitors.
AID262795Inhibition of SGK at 10 uM in presence of 100 uM ATP2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.
AID262784Inhibition of CSK at 10 uM in presence of 100 uM ATP2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.
AID262787Inhibition of MKK1 at 10 uM in presence of 100 uM ATP2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.
AID262778Inhibition of DMN-induced collagen IA1 expression by TGF beta in Sprague-Dawley rat liver at 10 mg/kg, po2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.
AID262782Inhibition of AMPK at 10 uM in presence of 100 uM ATP2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.
AID262781Displacement of rhodamine green fluorescently labeled ATP from recombinant GST-p38alpha2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.
AID262776Inhibition of DMN-induced collagen IA1 expression by TGF beta in Sprague-Dawley rat liver at 1 mg/kg, po2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.
AID262796Inhibition of P38-alpha at 10 uM in presence of 100 uM ATP2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.
AID262788Inhibition of MSK1 at 10 uM in presence of 100 uM ATP2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.
AID262793Inhibition of PKA at 10 uM in presence of 100 uM ATP2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.
AID262766Displacement of rhodamine green fluorescently labeled ATP from recombinant GST-ALK5 by FP assay2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.
AID618730Inhibition of Activin A in human HEK293 cells transfected with luciferase and FAST-2 gene expression vector A3-LUX after 16 hrs by luciferase reporter gene assay2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
2-Phenyl and 2-heterocyclic-4-(3-(pyridin-2-yl)-1H-pyrazol-4-yl)pyridines as inhibitors of TGF-β1 and activin A signalling.
AID618727Inhibition of Activin A in human HEK293 cells transfected with luciferase and FAST-2 gene expression vector A3-LUX at 1 uM after 16 hrs by luciferase reporter gene assay relative to control2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
2-Phenyl and 2-heterocyclic-4-(3-(pyridin-2-yl)-1H-pyrazol-4-yl)pyridines as inhibitors of TGF-β1 and activin A signalling.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (34)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's5 (14.71)29.6817
2010's18 (52.94)24.3611
2020's11 (32.35)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.43

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

MetricThis Compound (vs All)
Research Demand Index11.43 (24.57)
Research Supply Index3.56 (2.92)
Research Growth Index4.98 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.43)

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%
Other34 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]