Page last updated: 2024-11-13

gsk2830371

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Description

GSK2830371: inhibits Wip1 phosphatase; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID70983932
CHEMBL ID3613749
SCHEMBL ID13739288
MeSH IDM0593217

Synonyms (28)

Synonym
bdbm50118478
chembl3613749 ,
S7573 ,
HY-15832
gsk 2830371
(s)-5-(((5-chloro-2-methylpyridin-3-yl)amino)methyl)-n-(3-cyclopentyl-1-(cyclopropylamino)-1-oxopropan-2-yl)thiophene-2-carboxamide
AKOS024458513
SCHEMBL13739288
1404456-53-6
gsk2830371
5-[[(5-chloro-2-methyl-3-pyridinyl)amino]methyl]-n-[(1s)-1-(cyclopentylmethyl)-2-(cycloprpylamino)-2-oxoethyl]-2-thiophenecarboxamide
gsk-2830371
compound 8 [pmid: 24390428]
gtpl11103
5-[[(5-chloro-2-methylpyridin-3-yl)amino]methyl]-n-[(2s)-3-cyclopentyl-1-(cyclopropylamino)-1-oxopropan-2-yl]thiophene-2-carboxamide
5-[[(5-chloro-2-methyl-3-pyridinyl)amino]methyl]-n-[(1s)-1-(cyclopentylmethyl)-2-(cyclopropylamino)-2-oxoethyl]-2-thiophenecarboxamide
EX-A2687
AS-16421
BCP27848
CCG-269347
2-thiophenecarboxamide, 5-[[(5-chloro-2-methyl-3-pyridinyl)amino]methyl]-n-[(1s)-1-(cyclopentylmethyl)-2-(cyclopropylamino)-2-oxoethyl]-
(s)-5-{[(5-chloro-2-methylpyridin-3-yl)amino]methyl}-n-[3-cyclopentyl-1-(cyclopropylamino)-1-oxopropan-2-yl]thiophene-2-carboxamide
A899200
NCGC00378628-07
(2s)-2-[(5-{[(5-chloro-2-methylpyridin-3-yl)amino]methyl}thiophen-2-yl)formamido]-3-cyclopentyl-n-cyclopropylpropanamide
EN300-179507
Z1791350440
AC-36606

Research Excerpts

Overview

GSK2830371 is a potent and selective allosteric inhibitor of PPM1D. Its mechanism of binding and inhibition of catalytic activity are unknown.

ExcerptReferenceRelevance
"GSK2830371 is a potent and selective allosteric inhibitor of PPM1D, but its mechanism of binding and inhibition of catalytic activity are unknown."( Allosteric inhibition of PPM1D serine/threonine phosphatase via an altered conformational state.
Bajrami, B; Brousseau, M; Caliman, A; Campbell, AJ; Ebert, BL; Fischer, ES; Garvie, CW; Giacomelli, AO; Gibson, CJ; Guo, Q; Iqbal, S; Jiang, W; Jin, C; Kahn, J; Lintner, R; Miller, PG; Moroco, JA; Piccioni, F; Qian, Y; Raffier, C; Ranaghan, M; Root, DE; Sathappa, M; Shaw, S; Sperling, AS; Vernier, C; Yang, X, 2022
)
1.44
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (8)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency2.39190.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency8.48660.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency15.09160.00108.379861.1304AID1645840
Interferon betaHomo sapiens (human)Potency8.48660.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency8.48660.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency8.48660.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency8.48660.01238.964839.8107AID1645842
[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)
Protein phosphatase 1DHomo sapiens (human)IC50 (µMol)0.03280.00600.03280.0863AID1245781; AID1625400; AID1674043
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (56)

Processvia Protein(s)Taxonomy
G2/M transition of mitotic cell cycleProtein phosphatase 1DHomo sapiens (human)
DNA methylation-dependent heterochromatin formationProtein phosphatase 1DHomo sapiens (human)
protein dephosphorylationProtein phosphatase 1DHomo sapiens (human)
negative regulation of cell population proliferationProtein phosphatase 1DHomo sapiens (human)
cellular response to starvationProtein phosphatase 1DHomo sapiens (human)
response to radiationProtein phosphatase 1DHomo sapiens (human)
response to bacteriumProtein phosphatase 1DHomo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorProtein phosphatase 1DHomo sapiens (human)
peptidyl-threonine dephosphorylationProtein phosphatase 1DHomo sapiens (human)
negative regulation of gene expression, epigeneticProtein phosphatase 1DHomo sapiens (human)
regulation of transcription initiation by RNA polymerase IIProtein phosphatase 1DHomo sapiens (human)
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)
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 (23)

Processvia Protein(s)Taxonomy
protein serine/threonine kinase activityProtein phosphatase 1DHomo sapiens (human)
protein serine/threonine phosphatase activityProtein phosphatase 1DHomo sapiens (human)
protein bindingProtein phosphatase 1DHomo sapiens (human)
myosin phosphatase activityProtein phosphatase 1DHomo sapiens (human)
metal ion bindingProtein phosphatase 1DHomo sapiens (human)
mitogen-activated protein kinase bindingProtein phosphatase 1DHomo sapiens (human)
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)
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 (23)

Processvia Protein(s)Taxonomy
nucleusProtein phosphatase 1DHomo sapiens (human)
nucleoplasmProtein phosphatase 1DHomo sapiens (human)
nucleolusProtein phosphatase 1DHomo sapiens (human)
cytosolProtein phosphatase 1DHomo sapiens (human)
cytosolProtein phosphatase 1DHomo sapiens (human)
nucleusProtein phosphatase 1DHomo sapiens (human)
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)
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 (6)

Assay IDTitleYearJournalArticle
AID1674043Allosteric inhibition of human Wip1 (2 to 420 residues) expressed in baculovirus infected sf9 cells using FDP as substrate by fluorescence method2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Recent Advances of SHP2 Inhibitors in Cancer Therapy: Current Development and Clinical Application.
AID1245781Inhibition of His-tagged PPM1D (1 to 420 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) pLysS cells using Ac-VEPPLS(P)QETFSDLW-NH2 substrate2015Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
Novel inhibitors targeting PPM1D phosphatase potently suppress cancer cell proliferation.
AID1245780Inhibition of cell proliferation of human MCF7 cells incubated for 24 hrs2015Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
Novel inhibitors targeting PPM1D phosphatase potently suppress cancer cell proliferation.
AID1245788Inhibition of cell proliferation of human H1299 cells at 5 to 20 incubated for 24 hrs2015Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
Novel inhibitors targeting PPM1D phosphatase potently suppress cancer cell proliferation.
AID1625400Inhibition of human Wip1 (2 to 420 residues) expressed in baculovirus-infected insect SF9 cells assessed as fluorescein diphosphate hydrolysis after 5 mins by fluorescence assay2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Chemical Space of DNA-Encoded Libraries.
AID1245787Inhibition of cell proliferation of human H1299 cells overexpressing HA-PPM1D at 5 to 20 incubated for 24 hrs2015Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
Novel inhibitors targeting PPM1D phosphatase potently suppress cancer cell proliferation.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (16)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's12 (75.00)24.3611
2020's4 (25.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 23.36

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 Index23.36 (24.57)
Research Supply Index2.83 (2.92)
Research Growth Index4.56 (4.65)
Search Engine Demand Index23.28 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (23.36)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (6.25%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other15 (93.75%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]