gsk2656157 profile

ID Source	ID
PubMed CID	53469059
CHEMBL ID	2441340
CHEBI ID	139047
SCHEMBL ID	870782
MeSH ID	M000605050

Synonym
CHEBI:139047
gsk2656157 ,
5-{4-fluoro-1-[(6-methyl-2-pyridinyl)acetyl]-2,3-dihydro-1h-indol-5-yl}-7-methyl-7h-pyrrolo[2,3-d]pyrimidin-4-amine
5-{4-fluoro-1[(6-methyl-2-pyridinyl)acetyl]-2,3-dihydro-1h-indol-5-yl}-7-methyl-7h-pyrrolo[2,3-d]pyrimidin-4-amine
PRWSIEBRGXYXAJ-UHFFFAOYSA-N ,
S7033
SCHEMBL870782 ,
chembl2441340 ,
bdbm50442166
CS-3262
HY-13820
1-(5-(4-amino-7-methyl-7h-pyrrolo[2,3-d]pyrimidin-5-yl)-4-fluoroindolin-1-yl)-2-(6-methylpyridin-2-yl)ethan-1-one
1337532-29-2
gsk-2656157
agn-pc-09swn4
AC-32973
1-(5-(4-amino-7-methyl-7h-pyrrolo[2,3-d]pyrimidin-5-yl)-4-fluoroindolin-1-yl)-2-(6-methylpyridin-2-yl)ethanone
AKOS025404913
EX-A439
gtpl9544
compound 6 [pmid: 24900593]
1-[5-(4-amino-7-methylpyrrolo[2,3-d]pyrimidin-5-yl)-4-fluoro-2,3-dihydroindol-1-yl]-2-(6-methylpyridin-2-yl)ethanone
HMS3652P16
mfcd27997885
J-006434
NCGC00386314-03
SW222243-1
perk inhibitor gsk2656157
FT-0734440
AS-35165
BCP09007
gsk 2656157
SB19409
HMS3868L13
HMS3747M09
CCG-268839
NCGC00386314-01
1-[5-(4-amino-7-methyl-7h-pyrrolo[2,3-d]pyrimidin-5-yl)-4-fluoro-2,3-dihydro-1h-indol-1-yl]-2-(6-methyl-2-pyridinyl)ethanone
DTXSID101103941
1-[5-(4-amino-7-methyl-7h-pyrrolo[2,3-d]pyrimidin-5-yl)-4-fluoro-2,3-dihydro-1h-indol-1-yl]-2-(6-methyl-2-pyridinyl)-ethanone

Excerpt	Reference	Relevance
"GSK2656157 is an ATP-competitive inhibitor of PERK enzyme activity with an IC(50) of 0.9 nmol/L."	( Characterization of a novel PERK kinase inhibitor with antitumor and antiangiogenic activity. Alsaid, H; Atkins, C; Axten, JM; Choudhry, AE; Figueroa, DJ; Gaul, N; Goetz, A; Jucker, BM; Kumar, R; Liu, Q; Minthorn, E; Moss, K; Sanders, B; Stanley, TB; Zhang, SY, 2013)	1.11

Excerpt	Reference	Relevance
"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
" In this study, we report a series of 2-amino-3-amido-5-aryl-pyridines that we have identified as potent, selective, and orally bioavailable PERK inhibitors."	( Discovery of 2-amino-3-amido-5-aryl-pyridines as highly potent, orally bioavailable, and efficacious PERK kinase inhibitors. Adarasandi, R; Bandaru, M; Betzenhauser, M; Calvo, V; Chad, E; Du, H; Feldman, K; Gasparek, J; Guguloth, R; Jonnalagadda, SK; Koszelak-Rosenblum, M; Li, AH; Malibhatla, S; Mandati, C; Mulvihill, MJ; Nareddy, BR; Patil, BS; Rigby, AC; Sastry, V; Siddiqui, S; Singireddi, DRP; Surguladze, D; Surman, MD; Velmala, M; Velpuri, M; Wiens, B; Wolfley, J; Zhu, G, 2021)	0.62

Excerpt	Relevance	Reference
" Twice daily dosing of GSK2656157 results in dose-dependent inhibition of multiple human tumor xenografts growth in mice."	( Characterization of a novel PERK kinase inhibitor with antitumor and antiangiogenic activity. Alsaid, H; Atkins, C; Axten, JM; Choudhry, AE; Figueroa, DJ; Gaul, N; Goetz, A; Jucker, BM; Kumar, R; Liu, Q; Minthorn, E; Moss, K; Sanders, B; Stanley, TB; Zhang, SY, 2013)	0.7

Role	Description
EC 3.1.3.48 (protein-tyrosine-phosphatase) inhibitor	An EC 3.1.3.* (phosphoric monoester hydrolase) inhibitor which interferes with the activity of the enzyme protein tyrosine phosphatases (PTPs), EC 3.1.3.48, involved in the removal of phosphate groups from phosphorylated tyrosine residues on proteins.
PERK inhibitor	An EC 3.1.3.48 (protein-tyrosine-phosphatase) inhibitor that inhibits the expression of protein kinase RNA-like endoplasmic reticulum kinase.
antineoplastic agent	A substance that inhibits or prevents the proliferation of neoplasms.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Class	Description
pyrrolopyrimidine
biaryl	An organic aromatic compound whose structure contains two aromatic rings or ring systems, joined to each other by a single bond.
indoles	Any compound containing an indole skeleton.
methylpyridines	Any member of the class of pyridines that carries at least one methyl substituent.
organofluorine compound	An organofluorine compound is a compound containing at least one carbon-fluorine bond.
tertiary carboxamide	A carboxamide resulting from the formal condensation of a carboxylic acid with a secondary amine; formula RC(=O)NHR(1)R(2).
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (12)

Potency Measurements

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4	Homo sapiens (human)	Potency	8.4866	0.0123	7.9835	43.2770	AID1645841
G	Vesicular stomatitis virus	Potency	10.6840	0.0123	8.9648	39.8107	AID1645842
Interferon beta	Homo sapiens (human)	Potency	10.6840	0.0033	9.1582	39.8107	AID1645842
HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)	Potency	10.6840	0.0123	8.9648	39.8107	AID1645842
Inositol hexakisphosphate kinase 1	Homo sapiens (human)	Potency	10.6840	0.0123	8.9648	39.8107	AID1645842
cytochrome P450 2C9, partial	Homo sapiens (human)	Potency	10.6840	0.0123	8.9648	39.8107	AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Cytochrome P450 3A4	Homo sapiens (human)	IC50 (µMol)	0.2450	0.0001	1.7536	10.0000	AID777347; AID777371
Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)	IC50 (µMol)	0.9050	0.1000	2.6782	8.0000	AID777369
Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)	IC50 (µMol)	0.0691	0.0120	0.5243	1.5000	AID1896658
Eukaryotic translation initiation factor 2-alpha kinase 1	Homo sapiens (human)	IC50 (µMol)	0.4600	0.4200	0.4400	0.4600	AID777371
Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)	IC50 (µMol)	0.0154	0.0004	0.0153	0.0300	AID777347; AID777348
eIF-2-alpha kinase GCN2	Homo sapiens (human)	IC50 (µMol)	3.3880	0.4500	1.9190	3.3880	AID777368
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (187)

Process	via Protein(s)	Taxonomy
cell surface receptor signaling pathway via JAK-STAT	Interferon beta	Homo sapiens (human)
response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
B cell activation involved in immune response	Interferon beta	Homo sapiens (human)
cell surface receptor signaling pathway	Interferon beta	Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STAT	Interferon beta	Homo sapiens (human)
response to virus	Interferon beta	Homo sapiens (human)
positive regulation of autophagy	Interferon beta	Homo sapiens (human)
cytokine-mediated signaling pathway	Interferon beta	Homo sapiens (human)
natural killer cell activation	Interferon beta	Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT protein	Interferon beta	Homo sapiens (human)
cellular response to interferon-beta	Interferon beta	Homo sapiens (human)
B cell proliferation	Interferon beta	Homo sapiens (human)
negative regulation of viral genome replication	Interferon beta	Homo sapiens (human)
innate immune response	Interferon beta	Homo sapiens (human)
positive regulation of innate immune response	Interferon beta	Homo sapiens (human)
regulation of MHC class I biosynthetic process	Interferon beta	Homo sapiens (human)
negative regulation of T cell differentiation	Interferon beta	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Interferon beta	Homo sapiens (human)
defense response to virus	Interferon beta	Homo sapiens (human)
type I interferon-mediated signaling pathway	Interferon beta	Homo sapiens (human)
neuron cellular homeostasis	Interferon beta	Homo sapiens (human)
cellular response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
cellular response to virus	Interferon beta	Homo sapiens (human)
negative regulation of Lewy body formation	Interferon beta	Homo sapiens (human)
negative regulation of T-helper 2 cell cytokine production	Interferon beta	Homo sapiens (human)
positive regulation of apoptotic signaling pathway	Interferon beta	Homo sapiens (human)
response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
B cell differentiation	Interferon beta	Homo sapiens (human)
natural killer cell activation involved in immune response	Interferon beta	Homo sapiens (human)
adaptive immune response	Interferon beta	Homo sapiens (human)
T cell activation involved in immune response	Interferon beta	Homo sapiens (human)
humoral immune response	Interferon beta	Homo sapiens (human)
positive regulation of T cell mediated cytotoxicity	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
adaptive immune response	HLA 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-independent	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of T cell anergy	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
defense response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
detection of bacterium	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of interleukin-12 production	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of interleukin-6 production	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protection from natural killer cell mediated cytotoxicity	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
innate immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of dendritic cell differentiation	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class Ib	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
lipid hydroxylation	Cytochrome P450 3A4	Homo sapiens (human)
lipid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
steroid catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
androgen metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
alkaloid catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
calcitriol biosynthetic process from calciol	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
retinol metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
retinoic acid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 3A4	Homo sapiens (human)
aflatoxin metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 3A4	Homo sapiens (human)
positive regulation of cytokine production	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
translation	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
protein phosphorylation	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
negative regulation of cell population proliferation	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
response to virus	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
negative regulation of translation	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
endoplasmic reticulum unfolded protein response	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
positive regulation of chemokine production	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
positive regulation of stress-activated MAPK cascade	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
negative regulation of osteoblast proliferation	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
cellular response to amino acid starvation	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
response to interferon-alpha	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
negative regulation of apoptotic process	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
positive regulation of MAPK cascade	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
negative regulation of viral genome replication	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
protein autophosphorylation	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
positive regulation of NF-kappaB transcription factor activity	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
defense response to virus	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
antiviral innate immune response	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
regulation of NLRP3 inflammasome complex assembly	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
positive regulation of non-canonical NF-kappaB signal transduction	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
regulation of hematopoietic progenitor cell differentiation	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
regulation of hematopoietic stem cell proliferation	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
regulation of hematopoietic stem cell differentiation	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
eiF2alpha phosphorylation in response to endoplasmic reticulum stress	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
positive regulation of miRNA processing	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
MAPK cascade	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
positive regulation of protein phosphorylation	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
apoptotic process	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
inflammatory response	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
response to oxidative stress	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
positive regulation of gene expression	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
protein catabolic process	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
positive regulation of interleukin-8 production	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
positive regulation of tumor necrosis factor production	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
tumor necrosis factor-mediated signaling pathway	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
response to tumor necrosis factor	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
intracellular signal transduction	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
peptidyl-serine autophosphorylation	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
positive regulation of apoptotic process	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
negative regulation of apoptotic process	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
positive regulation of programmed cell death	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transduction	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
negative regulation of canonical NF-kappaB signal transduction	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
positive regulation of neuron apoptotic process	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
positive regulation of macrophage differentiation	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
positive regulation of JNK cascade	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
protein autophosphorylation	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
positive regulation of inflammatory response	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
positive regulation of NF-kappaB transcription factor activity	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
positive regulation of necroptotic process	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
negative regulation of necroptotic process	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
positive regulation of programmed necrotic cell death	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
positive regulation of interleukin-6-mediated signaling pathway	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
T cell apoptotic process	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
necroptotic process	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
cellular response to hydrogen peroxide	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
regulation of ATP:ADP antiporter activity	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
cellular response to tumor necrosis factor	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
cellular response to growth factor stimulus	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
extrinsic apoptotic signaling pathway	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
programmed necrotic cell death	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
ripoptosome assembly	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
necroptotic signaling pathway	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
positive regulation of execution phase of apoptosis	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
ripoptosome assembly involved in necroptotic process	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
positive regulation of non-canonical NF-kappaB signal transduction	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
positive regulation of tumor necrosis factor-mediated signaling pathway	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
amyloid fibril formation	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
positive regulation of reactive oxygen species metabolic process	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathway	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
positive regulation of extrinsic apoptotic signaling pathway	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathway in absence of ligand	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
inositol phosphate metabolic process	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic process	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
negative regulation of cold-induced thermogenesis	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol phosphate biosynthetic process	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
acute inflammatory response	Eukaryotic translation initiation factor 2-alpha kinase 1	Homo sapiens (human)
phagocytosis	Eukaryotic translation initiation factor 2-alpha kinase 1	Homo sapiens (human)
negative regulation of cell population proliferation	Eukaryotic translation initiation factor 2-alpha kinase 1	Homo sapiens (human)
regulation of eIF2 alpha phosphorylation by heme	Eukaryotic translation initiation factor 2-alpha kinase 1	Homo sapiens (human)
macrophage differentiation	Eukaryotic translation initiation factor 2-alpha kinase 1	Homo sapiens (human)
negative regulation of translational initiation by iron	Eukaryotic translation initiation factor 2-alpha kinase 1	Homo sapiens (human)
protoporphyrinogen IX metabolic process	Eukaryotic translation initiation factor 2-alpha kinase 1	Homo sapiens (human)
protein autophosphorylation	Eukaryotic translation initiation factor 2-alpha kinase 1	Homo sapiens (human)
negative regulation of hemoglobin biosynthetic process	Eukaryotic translation initiation factor 2-alpha kinase 1	Homo sapiens (human)
establishment of localization in cell	Eukaryotic translation initiation factor 2-alpha kinase 1	Homo sapiens (human)
multicellular organismal-level iron ion homeostasis	Eukaryotic translation initiation factor 2-alpha kinase 1	Homo sapiens (human)
integrated stress response signaling	Eukaryotic translation initiation factor 2-alpha kinase 1	Homo sapiens (human)
HRI-mediated signaling	Eukaryotic translation initiation factor 2-alpha kinase 1	Homo sapiens (human)
positive regulation of mitophagy	Eukaryotic translation initiation factor 2-alpha kinase 1	Homo sapiens (human)
response to iron ion starvation	Eukaryotic translation initiation factor 2-alpha kinase 1	Homo sapiens (human)
regulation of translational initiation by eIF2 alpha phosphorylation	Eukaryotic translation initiation factor 2-alpha kinase 1	Homo sapiens (human)
skeletal system development	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
ossification	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
angiogenesis	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
chondrocyte development	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
protein phosphorylation	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic process	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
ER overload response	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
endoplasmic reticulum organization	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
positive regulation of vascular endothelial growth factor production	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
positive regulation of gene expression	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
regulation of translational initiation by eIF2 alpha phosphorylation	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
negative regulation of translation	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
peptidyl-serine phosphorylation	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
calcium-mediated signaling	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
bone mineralization	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
endoplasmic reticulum unfolded protein response	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
endocrine pancreas development	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
negative regulation of myelination	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
negative regulation of translation in response to stress	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
negative regulation of translational initiation in response to stress	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
cellular response to amino acid starvation	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
response to endoplasmic reticulum stress	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
eiF2alpha phosphorylation in response to endoplasmic reticulum stress	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
PERK-mediated unfolded protein response	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
cellular response to glucose starvation	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
positive regulation of transcription by RNA polymerase I	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
negative regulation of translational initiation	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
protein autophosphorylation	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
insulin-like growth factor receptor signaling pathway	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
regulation of endoplasmic reticulum stress-induced eIF2 alpha phosphorylation	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
cellular response to cold	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
positive regulation of protein localization to nucleus	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
regulation of endoplasmic reticulum stress-induced intrinsic apoptotic signaling pathway	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
response to manganese-induced endoplasmic reticulum stress	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
DNA damage checkpoint signaling	eIF-2-alpha kinase GCN2	Homo sapiens (human)
positive regulation of defense response to virus by host	eIF-2-alpha kinase GCN2	Homo sapiens (human)
adaptive immune response	eIF-2-alpha kinase GCN2	Homo sapiens (human)
T cell activation involved in immune response	eIF-2-alpha kinase GCN2	Homo sapiens (human)
positive regulation of adaptive immune response	eIF-2-alpha kinase GCN2	Homo sapiens (human)
regulation of translational initiation	eIF-2-alpha kinase GCN2	Homo sapiens (human)
protein phosphorylation	eIF-2-alpha kinase GCN2	Homo sapiens (human)
learning	eIF-2-alpha kinase GCN2	Homo sapiens (human)
long-term memory	eIF-2-alpha kinase GCN2	Homo sapiens (human)
regulation of translational initiation by eIF2 alpha phosphorylation	eIF-2-alpha kinase GCN2	Homo sapiens (human)
viral translation	eIF-2-alpha kinase GCN2	Homo sapiens (human)
negative regulation of translational initiation in response to stress	eIF-2-alpha kinase GCN2	Homo sapiens (human)
negative regulation of CREB transcription factor activity	eIF-2-alpha kinase GCN2	Homo sapiens (human)
cellular response to amino acid starvation	eIF-2-alpha kinase GCN2	Homo sapiens (human)
cellular response to UV	eIF-2-alpha kinase GCN2	Homo sapiens (human)
eiF2alpha phosphorylation in response to endoplasmic reticulum stress	eIF-2-alpha kinase GCN2	Homo sapiens (human)
negative regulation by host of viral genome replication	eIF-2-alpha kinase GCN2	Homo sapiens (human)
negative regulation of neuron differentiation	eIF-2-alpha kinase GCN2	Homo sapiens (human)
negative regulation of translational initiation	eIF-2-alpha kinase GCN2	Homo sapiens (human)
protein autophosphorylation	eIF-2-alpha kinase GCN2	Homo sapiens (human)
defense response to virus	eIF-2-alpha kinase GCN2	Homo sapiens (human)
regulation of feeding behavior	eIF-2-alpha kinase GCN2	Homo sapiens (human)
cellular response to cold	eIF-2-alpha kinase GCN2	Homo sapiens (human)
positive regulation of translational initiation in response to starvation	eIF-2-alpha kinase GCN2	Homo sapiens (human)
GCN2-mediated signaling	eIF-2-alpha kinase GCN2	Homo sapiens (human)
positive regulation of long-term synaptic potentiation	eIF-2-alpha kinase GCN2	Homo sapiens (human)
neuron projection extension	eIF-2-alpha kinase GCN2	Homo sapiens (human)
negative regulation of cytoplasmic translational initiation in response to stress	eIF-2-alpha kinase GCN2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (60)

Process	via Protein(s)	Taxonomy
cytokine activity	Interferon beta	Homo sapiens (human)
cytokine receptor binding	Interferon beta	Homo sapiens (human)
type I interferon receptor binding	Interferon beta	Homo sapiens (human)
protein binding	Interferon beta	Homo sapiens (human)
chloramphenicol O-acetyltransferase activity	Interferon beta	Homo sapiens (human)
TAP binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
signaling receptor binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protein binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
peptide antigen binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
TAP binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protein-folding chaperone binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
steroid binding	Cytochrome P450 3A4	Homo sapiens (human)
iron ion binding	Cytochrome P450 3A4	Homo sapiens (human)
protein binding	Cytochrome P450 3A4	Homo sapiens (human)
steroid hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
retinoic acid 4-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 3A4	Homo sapiens (human)
oxygen binding	Cytochrome P450 3A4	Homo sapiens (human)
enzyme binding	Cytochrome P450 3A4	Homo sapiens (human)
heme binding	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D3 25-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
caffeine oxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
quinine 3-monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
testosterone 6-beta-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 8,9 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 11,12 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 14,15 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
aromatase activity	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D 24-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
estrogen 16-alpha-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
estrogen 2-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
RNA binding	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
double-stranded RNA binding	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
protein kinase activity	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
protein serine/threonine kinase activity	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
eukaryotic translation initiation factor 2alpha kinase activity	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
non-membrane spanning protein tyrosine kinase activity	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
protein binding	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
ATP binding	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
kinase activity	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
protein phosphatase regulator activity	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
identical protein binding	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
protein serine kinase activity	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
protein kinase activity	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
protein serine/threonine kinase activity	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
death receptor binding	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
protein binding	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
ATP binding	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
ubiquitin protein ligase binding	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
signaling adaptor activity	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
identical protein binding	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
protein homodimerization activity	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
protein-containing complex binding	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
death domain binding	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
protein serine kinase activity	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
JUN kinase kinase kinase activity	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol heptakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 5-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
protein binding	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
ATP binding	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 1-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 3-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
eukaryotic translation initiation factor 2alpha kinase activity	Eukaryotic translation initiation factor 2-alpha kinase 1	Homo sapiens (human)
protein binding	Eukaryotic translation initiation factor 2-alpha kinase 1	Homo sapiens (human)
ATP binding	Eukaryotic translation initiation factor 2-alpha kinase 1	Homo sapiens (human)
heme binding	Eukaryotic translation initiation factor 2-alpha kinase 1	Homo sapiens (human)
protein homodimerization activity	Eukaryotic translation initiation factor 2-alpha kinase 1	Homo sapiens (human)
protein serine kinase activity	Eukaryotic translation initiation factor 2-alpha kinase 1	Homo sapiens (human)
protein kinase activity	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
protein serine/threonine kinase activity	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
eukaryotic translation initiation factor 2alpha kinase activity	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
protein binding	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
ATP binding	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
enzyme binding	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
protein phosphatase binding	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
identical protein binding	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
Hsp90 protein binding	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
protein serine kinase activity	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
tRNA binding	eIF-2-alpha kinase GCN2	Homo sapiens (human)
protein serine/threonine kinase activity	eIF-2-alpha kinase GCN2	Homo sapiens (human)
eukaryotic translation initiation factor 2alpha kinase activity	eIF-2-alpha kinase GCN2	Homo sapiens (human)
ATP binding	eIF-2-alpha kinase GCN2	Homo sapiens (human)
protein serine kinase activity	eIF-2-alpha kinase GCN2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (33)

Process	via Protein(s)	Taxonomy
extracellular space	Interferon beta	Homo sapiens (human)
extracellular region	Interferon beta	Homo sapiens (human)
Golgi membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
endoplasmic reticulum	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
Golgi apparatus	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
plasma membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
cell surface	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
ER to Golgi transport vesicle membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
secretory granule membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
phagocytic vesicle membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
early endosome membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
recycling endosome membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
extracellular exosome	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
lumenal side of endoplasmic reticulum membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
MHC class I protein complex	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
extracellular space	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
external side of plasma membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
cytoplasm	Cytochrome P450 3A4	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 3A4	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 3A4	Homo sapiens (human)
cytoplasm	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
nucleoplasm	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
cytoplasm	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
cytosol	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
ribosome	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
membrane	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
perinuclear region of cytoplasm	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
nucleus	Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)
mitochondrion	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
cytosol	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
plasma membrane	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
endosome membrane	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
death-inducing signaling complex	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
protein-containing complex	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
receptor complex	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
ripoptosome	Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)
fibrillar center	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
nucleoplasm	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
cytosol	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
nucleus	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
cytoplasm	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
cytosol	Eukaryotic translation initiation factor 2-alpha kinase 1	Homo sapiens (human)
cytosol	Eukaryotic translation initiation factor 2-alpha kinase 1	Homo sapiens (human)
nucleus	Eukaryotic translation initiation factor 2-alpha kinase 1	Homo sapiens (human)
cytoplasm	Eukaryotic translation initiation factor 2-alpha kinase 1	Homo sapiens (human)
cytoplasm	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
endoplasmic reticulum	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
endoplasmic reticulum membrane	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
cytosol	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
membrane	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
perinuclear region of cytoplasm	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
cytoplasm	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
nucleus	Eukaryotic translation initiation factor 2-alpha kinase 3	Homo sapiens (human)
cytoplasm	eIF-2-alpha kinase GCN2	Homo sapiens (human)
cytosolic ribosome	eIF-2-alpha kinase GCN2	Homo sapiens (human)
cytosol	eIF-2-alpha kinase GCN2	Homo sapiens (human)
cytoplasm	eIF-2-alpha kinase GCN2	Homo sapiens (human)
nucleus	eIF-2-alpha kinase GCN2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (55)

Assay ID	Title	Year	Journal	Article
AID777360	Volume of distribution at steady state in CD1 mouse at 2 mg/kg, iv by LC-MS/MS analysis	2013	ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10	Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
AID777346	Blood clearance in Sprague-Dawley rat at 2.2 mg/kg, iv by LC-MS/MS analysis	2013	ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10	Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
AID777367	Selectivity ratio of IC50 for PKR (unknown origin) to IC50 for GST-tagged PERK cytoplasmic domain (536 to 1116)	2013	ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10	Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
AID1763245	Inhibition of wild-type human partial length KIT (I571 to D952 residues) expressed in bacterial expression system assessed as residual activity at 10 uM by Kinomescan method relative to control	2021	Bioorganic & medicinal chemistry letters, 07-01, Volume: 43	Discovery of 2-amino-3-amido-5-aryl-pyridines as highly potent, orally bioavailable, and efficacious PERK kinase inhibitors.
AID777365	AUC (0 to infinity) in CD1 mouse at 2 mg/kg, iv by LC-MS/MS analysis	2013	ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10	Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
AID777372	Inhibition of CYP3A4 in human liver microsomes using nifedipine as substrate after 5 to 60 mins by LC-MS/MS analysis	2013	ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10	Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
AID777347	Inhibition of thapsigargin-induced autophosphorylation of PERK in human A549 cells preincubated for 1 hr followed by thapsigargin-induction measured after 1 hr by Western blotting analysis	2013	ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10	Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
AID777363	AUC (0 to infinity) in beagle dog at 2.9 mg/kg, iv by LC-MS/MS analysis	2013	ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10	Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
AID1896659	Anti-necroptic activity in TNF mediated cell death in human MEF cells preincubated for 30 mins in presence of TAK1 inhibitor/ZVAD-fmk and measured after 24 hrs by Sytox-green reagent based analysis	2022	Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22	Small-Molecule Receptor-Interacting Protein 1 (RIP1) Inhibitors as Therapeutic Agents for Multifaceted Diseases: Current Medicinal Chemistry Insights and Emerging Opportunities.
AID1896660	Anti-necroptic activity in TNF mediated cell death in mouse L929sAhFas cells preincubated for 30 mins in presence of TAK1 inhibitor/ZVAD-fmk and measured after 24 hrs by Sytox-green reagent based analysis	2022	Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22	Small-Molecule Receptor-Interacting Protein 1 (RIP1) Inhibitors as Therapeutic Agents for Multifaceted Diseases: Current Medicinal Chemistry Insights and Emerging Opportunities.
AID777364	AUC (0 to infinity) in Sprague-Dawley rat at 2.2 mg/kg, iv by LC-MS/MS analysis	2013	ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10	Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
AID777362	Blood clearance in CD1 mouse at 2 mg/kg, iv by LC-MS/MS analysis	2013	ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10	Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
AID777359	Volume of distribution at steady state in Sprague-Dawley rat at 2.2 mg/kg, iv by LC-MS/MS analysis	2013	ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10	Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
AID1763250	Inhibition of wild-type human partial length TIE2 (N804 to T1112 residues) expressed in bacterial expression system assessed as residual activity at 10 uM by Kinomescan method relative to control	2021	Bioorganic & medicinal chemistry letters, 07-01, Volume: 43	Discovery of 2-amino-3-amido-5-aryl-pyridines as highly potent, orally bioavailable, and efficacious PERK kinase inhibitors.
AID1763251	Inhibition of wild-type human partial length TRKB (Q547 to G838 residues) expressed in mammalian expression system assessed as residual activity at 10 uM by Kinomescan method relative to control	2021	Bioorganic & medicinal chemistry letters, 07-01, Volume: 43	Discovery of 2-amino-3-amido-5-aryl-pyridines as highly potent, orally bioavailable, and efficacious PERK kinase inhibitors.
AID777342	Inhibition of CYP2D6 in human liver microsomes using bufuralol as substrate after 5 to 60 mins by LC-MS/MS analysis	2013	ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10	Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
AID777373	Inhibition of CYP2C8 in human liver microsomes using paclitaxel as substrate after 5 to 60 mins by LC-MS/MS analysis	2013	ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10	Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
AID777369	Inhibition of PKR (unknown origin) assessed as EIF2AK2 phosphorylation	2013	ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10	Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
AID1763240	Inhibition of human non-phosphorylated ABL1 F317L mutant (S229 to K512 residues) expressed in mammalian expression system assessed as residual activity at 10 uM by Kinomescan method relative to control	2021	Bioorganic & medicinal chemistry letters, 07-01, Volume: 43	Discovery of 2-amino-3-amido-5-aryl-pyridines as highly potent, orally bioavailable, and efficacious PERK kinase inhibitors.
AID777353	AUC (0 to infinity) in Sprague-Dawley rat at 4.3 mg/kg, po by LC-MS/MS analysis	2013	ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10	Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
AID777345	Inhibition of CYP1A2 in human liver microsomes using phenacetin as substrate after 5 to 60 mins by LC-MS/MS analysis	2013	ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10	Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
AID777361	Blood clearance in beagle dog at 2.9 mg/kg, iv by LC-MS/MS analysis	2013	ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10	Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
AID1896658	Inhibition of GST tagged human recombinant RIPK1 incubated for 4 hrs by ADP-Glo luminescence assay	2022	Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22	Small-Molecule Receptor-Interacting Protein 1 (RIP1) Inhibitors as Therapeutic Agents for Multifaceted Diseases: Current Medicinal Chemistry Insights and Emerging Opportunities.
AID777357	Half life in CD1 mouse at 2 mg/kg, iv by LC-MS/MS analysis	2013	ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10	Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
AID1763246	Inhibition of wild-type human full length p38-gamma (M1 to L367 residues) expressed in mammalian expression system assessed as residual activity at 10 uM by Kinomescan method relative to control	2021	Bioorganic & medicinal chemistry letters, 07-01, Volume: 43	Discovery of 2-amino-3-amido-5-aryl-pyridines as highly potent, orally bioavailable, and efficacious PERK kinase inhibitors.
AID1763249	Inhibition of wild-type human partial length SRC (L240 to L536 residues) expressed in bacterial expression system assessed as residual activity at 10 uM by Kinomescan method relative to control	2021	Bioorganic & medicinal chemistry letters, 07-01, Volume: 43	Discovery of 2-amino-3-amido-5-aryl-pyridines as highly potent, orally bioavailable, and efficacious PERK kinase inhibitors.
AID777370	Selectivity ratio of IC50 for HRI (unknown origin) to IC50 for GST-tagged PERK cytoplasmic domain (536 to 1116)	2013	ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10	Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
AID777355	Half life in beagle dog at 2.9 mg/kg, iv by LC-MS/MS analysis	2013	ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10	Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
AID777374	Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate after 5 to 60 mins by LC-MS/MS analysis	2013	ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10	Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
AID1763242	Inhibition of wild-type human partial length AXL (R497 to Y821 residues) expressed in bacterial expression system assessed as residual activity at 10 uM by Kinomescan method relative to control	2021	Bioorganic & medicinal chemistry letters, 07-01, Volume: 43	Discovery of 2-amino-3-amido-5-aryl-pyridines as highly potent, orally bioavailable, and efficacious PERK kinase inhibitors.
AID1763247	Inhibition of wild-type human partial length PDGFRbeta (V582 to Y1009 residues) expressed in bacterial expression system assessed as residual activity at 10 uM by Kinomescan method relative to control	2021	Bioorganic & medicinal chemistry letters, 07-01, Volume: 43	Discovery of 2-amino-3-amido-5-aryl-pyridines as highly potent, orally bioavailable, and efficacious PERK kinase inhibitors.
AID777356	Half life in Sprague-Dawley rat at 2.2 mg/kg, iv by LC-MS/MS analysis	2013	ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10	Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
AID777371	Inhibition of HRI (unknown origin) assessed as EIF2AK1 phosphorylation	2013	ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10	Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
AID777352	AUC (0 to infinity) in beagle dog at 5.2 mg/kg, po by LC-MS/MS analysis	2013	ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10	Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
AID1763244	Inhibition of wild-type human partial length DDR1 (R565 to V876 residues) expressed in bacterial expression system assessed as residual activity at 10 uM by Kinomescan method relative to control	2021	Bioorganic & medicinal chemistry letters, 07-01, Volume: 43	Discovery of 2-amino-3-amido-5-aryl-pyridines as highly potent, orally bioavailable, and efficacious PERK kinase inhibitors.
AID777368	Inhibition of GCN2 (unknown origin) assessed as EIF2AK4 phosphorylation	2013	ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10	Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
AID777366	Selectivity ratio of IC50 for GCN2 (unknown origin) to IC50 for GST-tagged PERK cytoplasmic domain (536 to 1116)	2013	ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10	Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
AID777358	Volume of distribution at steady state in beagle dog at 2.9 mg/kg, iv by LC-MS/MS analysis	2013	ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10	Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
AID777349	Oral bioavailability in beagle dog at 5.2 mg/kg by LC-MS/MS analysis	2013	ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10	Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
AID777343	Inhibition of CYP2C19 in human liver microsomes using mephenytoin as substrate after 5 to 60 mins by LC-MS/MS analysis	2013	ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10	Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
AID1763241	Inhibition of wild-type human partial length AURKB (D25 to A303 residues) expressed in mammalian expression system assessed as residual activity at 10 uM by Kinomescan method relative to control	2021	Bioorganic & medicinal chemistry letters, 07-01, Volume: 43	Discovery of 2-amino-3-amido-5-aryl-pyridines as highly potent, orally bioavailable, and efficacious PERK kinase inhibitors.
AID777351	Oral bioavailability in CD1 mouse at 13.4 mg/kg by LC-MS/MS analysis	2013	ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10	Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
AID777354	AUC (0 to infinity) in CD1 mouse at 13.4 mg/kg, po by LC-MS/MS analysis	2013	ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10	Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
AID1763243	Inhibition of wild-type human partial length CSF1R (I564 to S939 residues) expressed in bacterial expression system assessed as residual activity at 10 uM by Kinomescan method relative to control	2021	Bioorganic & medicinal chemistry letters, 07-01, Volume: 43	Discovery of 2-amino-3-amido-5-aryl-pyridines as highly potent, orally bioavailable, and efficacious PERK kinase inhibitors.
AID777348	Inhibition of GST-tagged PERK cytoplasmic domain (536 to 1116) (unknown origin) assessed as biotinylated His6-tagged EIF2alpha phosphorylation preincubated for 30 mins followed by ATP and eIF2alpha addition measured after 1 hr by HTRF assay	2013	ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10	Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
AID777344	Inhibition of CYP2C9 in human liver microsomes using diclofenac as substrate after 5 to 60 mins by LC-MS/MS analysis	2013	ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10	Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
AID777350	Oral bioavailability in Sprague-Dawley rat at 4.3 mg/kg by LC-MS/MS analysis	2013	ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10	Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
AID1763248	Inhibition of wild-type human partial length RIPK1 (M1 to K305 residues) expressed in bacterial expression system assessed as residual activity at 10 uM by Kinomescan method relative to control	2021	Bioorganic & medicinal chemistry letters, 07-01, Volume: 43	Discovery of 2-amino-3-amido-5-aryl-pyridines as highly potent, orally bioavailable, and efficacious PERK kinase inhibitors.
AID1296008	Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening	2020	SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347160	Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors	2020	Proceedings 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.
AID1347159	Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay	2020	Proceedings 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.
AID1347411	qHTS 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) Libary	2020	ACS 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.
AID1345631	Human eukaryotic translation initiation factor 2 alpha kinase 3 (PEK subfamily)	2013	ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10	Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	0 (0.00)	29.6817
2010's	18 (62.07)	24.3611
2020's	11 (37.93)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	2 (6.90%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	27 (93.10%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
adenine [no description available]	7.41	22	6-aminopurines; purine nucleobase	Daphnia magna metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite
phenytoin [no description available]	3.51	1	imidazolidine-2,4-dione	anticonvulsant; drug allergen; sodium channel blocker; teratogenic agent
glimepiride glimepiride: structure given in first source	2.21	1	sulfonamide
sevoflurane Sevoflurane: A non-explosive inhalation anesthetic used in the induction and maintenance of general anesthesia. It does not cause respiratory irritation and may also prevent PLATELET AGGREGATION.. sevoflurane : An ether compound having fluoromethyl and 1,1,1,3,3,3-hexafluoroisopropyl as the two alkyl groups.	2.15	1	ether; organofluorine compound	central nervous system depressant; inhalation anaesthetic; platelet aggregation inhibitor
thiophenes Thiophenes: A monocyclic heteroarene furan in which the oxygen atom is replaced by a sulfur.. thiophenes : Compounds containing at least one thiophene ring.	2.15	1	mancude organic heteromonocyclic parent; monocyclic heteroarene; thiophenes; volatile organic compound	non-polar solvent
deoxyglucose Deoxyglucose: 2-Deoxy-D-arabino-hexose. An antimetabolite of glucose with antiviral activity.. deoxyglucose : A deoxyhexose comprising glucose having at least one hydroxy group replaced by hydrogen.	2.25	1
sorafenib [no description available]	3.51	1	(trifluoromethyl)benzenes; aromatic ether; monochlorobenzenes; phenylureas; pyridinecarboxamide	angiogenesis inhibitor; anticoronaviral agent; antineoplastic agent; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; ferroptosis inducer; tyrosine kinase inhibitor
resveratrol trans-resveratrol : A resveratrol in which the double bond has E configuration.	2.15	1	resveratrol	antioxidant; phytoalexin; plant metabolite; quorum sensing inhibitor; radical scavenger
stilbenes Stilbenes: Organic compounds that contain 1,2-diphenylethylene as a functional group.. trans-stilbene : The trans-isomer of stilbene.	2.15	1	stilbene
thiourea Thiourea: A photographic fixative used also in the manufacture of resins. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), this substance may reasonably be anticipated to be a carcinogen (Merck Index, 9th ed). Many of its derivatives are ANTITHYROID AGENTS and/or FREE RADICAL SCAVENGERS.. thiourea : The simplest member of the thiourea class, consisting of urea with the oxygen atom substituted by sulfur.	2.61	2	one-carbon compound; thioureas; ureas	antioxidant; chromophore
ginsenosides ginsenoside : Triterpenoid saponins with a dammarane-like skeleton originally isolated from ginseng (Panax) species. Use of the term has been extended to include semi-synthetic derivatives.	2.21	1
hymecromone Hymecromone: A coumarin derivative possessing properties as a spasmolytic, choleretic and light-protective agent. It is also used in ANALYTICAL CHEMISTRY TECHNIQUES for the determination of NITRIC ACID.	2.31	1	hydroxycoumarin	antineoplastic agent; hyaluronic acid synthesis inhibitor
su 11248 [no description available]	3.51	1	monocarboxylic acid amide; pyrroles	angiogenesis inhibitor; antineoplastic agent; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor; immunomodulator; neuroprotective agent; vascular endothelial growth factor receptor antagonist
guanabenz Guanabenz: An alpha-2 selective adrenergic agonist used as an antihypertensive agent.	3.25	1	dichlorobenzene
salubrinal salubrinal: prevents dephosphorylation of eIF2alpha; structure in first source. salubrinal : A member of the class of quinolines that is a mixed aminal resulting from the formal condensation oftrichloroacetaldehyde with the amide nitrogen of trans-cinnamamide and the primary amino group of 1-quinolin-8-ylthiourea. It is a selective inhibitor of cellular complexes that dephosphorylate eukaryotic translation initiation factor 2 subunit alpha (eIF2alpha).	2.61	2	aminal; organochlorine compound; quinolines; secondary carboxamide; thioureas
pi103 PI103: pyridofuropyrimidine antineoplastic; a potent inhibitor of class I phosphatidylinositide 3-kinases (PI3K); structure in first soruce	2.31	1	aromatic amine; morpholines; organic heterotricyclic compound; phenols; tertiary amino compound	antineoplastic agent; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor; mTOR inhibitor
pazopanib pazopanib: a protein kinase inhibitor. pazopanib : A pyrimidine that is 5-(pyrimidin-2-yl}amino-2-methylbenzenesulfonamide substituted at position 4 by a (2,3-dimethylindazol-6-yl)(methyl)amino group. Used as its hydrochloride salt for treatment of kidney cancer.	3.51	1	aminopyrimidine; indazoles; sulfonamide	angiogenesis modulating agent; antineoplastic agent; tyrosine kinase inhibitor; vascular endothelial growth factor receptor antagonist
nvp-ast487 NVP-AST487: antineoplastic; a RET kinase inhibitor that blocks growth and calcitonin gene expression through distinct mechanisms in medullary thyroid cancer cells	3.51	1
kw 2449 KW 2449: has both multikinase inhibitory activity and antineoplastic activity; structure in first source	3.51	1
jnj 28312141 [no description available]	3.51	1
ginsenoside rb3 [no description available]	2.21	1	12beta-hydroxy steroid; beta-D-glucoside; disaccharide derivative; ginsenoside; tetracyclic triterpenoid	antidepressant; antioxidant; cardioprotective agent; neuroprotective agent; NMDA receptor antagonist; plant metabolite
ponatinib [no description available]	3.51	1	(trifluoromethyl)benzenes; acetylenic compound; benzamides; imidazopyridazine; N-methylpiperazine	antineoplastic agent; tyrosine kinase inhibitor
quizartinib [no description available]	3.51	1	benzoimidazothiazole; isoxazoles; morpholines; phenylureas	antineoplastic agent; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor; necroptosis inhibitor
gsk 1363089 GSK 1363089: a multikinase inhibitor that acts on Met, RON, Axl, and VEGFR; structure in first source	3.51	1	aromatic ether
tak-632 TAK-632 : A member of the class of benzothiazoles that is 1,3-benzothiazole substituted by (cyclopropanecarbonyl)amino, 4-fluoro-3-{2-[3-(trifluoromethyl)phenyl]acetamido}phenoxy, and cyano groups at positions 2, 6 and 7, respectively. It is a potent pan-RAF inhibitor with IC50 of 1.4, 2.4 and 8.3 nM for CRAF, BRAF(V600E), BRAF(WT), respectively.	3.51	1	(trifluoromethyl)benzenes; aromatic ether; benzothiazoles; cyclopropylcarboxamide; monofluorobenzenes; nitrile; secondary carboxamide	antineoplastic agent; apoptosis inducer; B-Raf inhibitor; EC 2.7.11.26 (tau-protein kinase) inhibitor; necroptosis inhibitor
7-methyl-5-(1-((3-(trifluoromethyl)phenyl)acetyl)-2,3-dihydro-1h-indol-5-yl)-7h-pyrrolo(2,3-d)pyrimidin-4-amine 7-methyl-5-(1-((3-(trifluoromethyl)phenyl)acetyl)-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo(2,3-d)pyrimidin-4-amine: inhibits protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK); structure in first source	5.17	7
chir 258 [no description available]	3.51	1
stf 083010 STF 083010: inhibits Ire1 endonuclease; structure in first source	2.15	1

Condition	Relationship Strength	Studies
Congenital Zika Syndrome [description not available]	2.25	1
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	5.51	7
Zika Virus Infection A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.	2.25	1
Cancer of Pancreas [description not available]	2.21	1
Pancreatic Neoplasms Tumors or cancer of the PANCREAS. Depending on the types of ISLET CELLS present in the tumors, various hormones can be secreted: GLUCAGON from PANCREATIC ALPHA CELLS; INSULIN from PANCREATIC BETA CELLS; and SOMATOSTATIN from the SOMATOSTATIN-SECRETING CELLS. Most are malignant except the insulin-producing tumors (INSULINOMA).	2.21	1
Neuroendocrine Tumors Tumors whose cells possess secretory granules and originate from the neuroectoderm, i.e., the cells of the ectoblast or epiblast that program the neuroendocrine system. Common properties across most neuroendocrine tumors include ectopic hormone production (often via APUD CELLS), the presence of tumor-associated antigens, and isozyme composition.	2.21	1
Aseptic Necrosis of Femur Head [description not available]	2.25	1
Brain Hemorrhage, Cerebral [description not available]	2.31	1
Cerebral Hemorrhage Bleeding into one or both CEREBRAL HEMISPHERES including the BASAL GANGLIA and the CEREBRAL CORTEX. It is often associated with HYPERTENSION and CRANIOCEREBRAL TRAUMA.	2.31	1
Infections, Coronavirus [description not available]	2.31	1
2019 Novel Coronavirus Disease [description not available]	2.31	1
Coronavirus Infections Virus diseases caused by the CORONAVIRUS genus. Some specifics include transmissible enteritis of turkeys (ENTERITIS, TRANSMISSIBLE, OF TURKEYS); FELINE INFECTIOUS PERITONITIS; and transmissible gastroenteritis of swine (GASTROENTERITIS, TRANSMISSIBLE, OF SWINE).	2.31	1
Degenerative Diseases, Central Nervous System [description not available]	3.06	1
Protein Folding Diseases [description not available]	3.06	1
Aging The gradual irreversible changes in structure and function of an organism that occur as a result of the passage of time.	3.06	1
Neurodegenerative Diseases Hereditary and sporadic conditions which are characterized by progressive nervous system dysfunction. These disorders are often associated with atrophy of the affected central or peripheral nervous system structures.	3.06	1
Brain Swelling [description not available]	2.15	1
Brain Inflammation [description not available]	2.15	1
Hemorrhage, Subarachnoid [description not available]	2.15	1
Brain Edema Increased intracellular or extracellular fluid in brain tissue. Cytotoxic brain edema (swelling due to increased intracellular fluid) is indicative of a disturbance in cell metabolism, and is commonly associated with hypoxic or ischemic injuries (see HYPOXIA, BRAIN). An increase in extracellular fluid may be caused by increased brain capillary permeability (vasogenic edema), an osmotic gradient, local blockages in interstitial fluid pathways, or by obstruction of CSF flow (e.g., obstructive HYDROCEPHALUS). (From Childs Nerv Syst 1992 Sep; 8(6):301-6)	2.15	1
Encephalitis Inflammation of the BRAIN due to infection, autoimmune processes, toxins, and other conditions. Viral infections (see ENCEPHALITIS, VIRAL) are a relatively frequent cause of this condition.	2.15	1
Subarachnoid Hemorrhage Bleeding into the intracranial or spinal SUBARACHNOID SPACE, most resulting from INTRACRANIAL ANEURYSM rupture. It can occur after traumatic injuries (SUBARACHNOID HEMORRHAGE, TRAUMATIC). Clinical features include HEADACHE; NAUSEA; VOMITING, nuchal rigidity, variable neurological deficits and reduced mental status.	2.15	1
Esophageal Squamous Cell Carcinoma A carcinoma that originates usually from cells on the surface of the middle and lower third of the ESOPHAGUS. Tumor cells exhibit typical squamous morphology and form large polypoid lesions. Mutations in RNF6, LZTS1, TGFBR2, DEC1, and WWOX1 genes are associated with this cancer.	2.15	1
Carcinoma, Epidermoid [description not available]	2.15	1
Cancer of Esophagus [description not available]	2.15	1
Carcinoma, Squamous Cell A carcinoma derived from stratified SQUAMOUS EPITHELIAL CELLS. It may also occur in sites where glandular or columnar epithelium is normally present. (From Stedman, 25th ed)	2.15	1
Esophageal Neoplasms Tumors or cancer of the ESOPHAGUS.	2.15	1
Diabetes Mellitus, Adult-Onset [description not available]	2.21	1
Hyperglycemia, Postprandial Abnormally high BLOOD GLUCOSE level after a meal.	2.21	1
Diabetes Mellitus, Type 2 A subclass of DIABETES MELLITUS that is not INSULIN-responsive or dependent (NIDDM). It is characterized initially by INSULIN RESISTANCE and HYPERINSULINEMIA; and eventually by GLUCOSE INTOLERANCE; HYPERGLYCEMIA; and overt diabetes. Type II diabetes mellitus is no longer considered a disease exclusively found in adults. Patients seldom develop KETOSIS but often exhibit OBESITY.	2.21	1
Hyperglycemia Abnormally high BLOOD GLUCOSE level.	2.21	1
Peripheral Nerve Injury [description not available]	5.01	4
Peripheral Nerve Injuries Injuries to the PERIPHERAL NERVES.	5.01	4

gsk2656157

Cross-References

Synonyms (40)

Research Excerpts

Overview

Bioavailability

Dosage Studied

Roles (3)

Drug Classes (6)

Protein Targets (12)

Potency Measurements

Inhibition Measurements

Biological Processes (187)

Molecular Functions (60)

Ceullar Components (33)

Bioassays (55)

Research

Studies (29)

Market Indicators

Research Demand Index: 25.87

Study Types

gsk2656157

Cross-References

Synonyms (40)

Research Excerpts

Overview

Bioavailability

Dosage Studied

Roles (3)

Drug Classes (6)

Protein Targets (12)

Potency Measurements

Inhibition Measurements

Biological Processes (187)

Molecular Functions (60)

Ceullar Components (33)

Bioassays (55)

Research

Studies (29)

Market Indicators

Research Demand Index: 25.87

Study Types

Related Drugs (28)

Related Conditions (33)