Page last updated: 2024-08-05 15:50:23

PERK inhibitor

An EC 3.1.3.48 (protein-tyrosine-phosphatase) inhibitor that inhibits the expression of protein kinase RNA-like endoplasmic reticulum kinase.

ChEBI ID: 139055

Members (1)

MemberDefinitionClass
gsk2656157A pyrrolopyrimidine that is 7-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine which has been substituted at position 5 by a 4-fluoro-2,3-dihydro-1H-indol-5-yl group, the nitrogen of which has been acylated by a (6-methylpyridin-2-yl)acetyl group. An orally bioavailable PERK inhibitor.GSK2656157

Research

Studies (29)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's18 (62.07)24.3611
2020's11 (37.93)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (6.90%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other27 (93.10%)84.16%

Protein Targets (12)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
cytochrome P450 2C9, partialHomo sapiens (human)Potency10.684011
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency8.486611
GVesicular stomatitis virusPotency10.684011
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency10.684011
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency10.684012
Interferon betaHomo sapiens (human)Potency10.684011

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Cytochrome P450 3A4Homo sapiens (human)IC500.245022
eIF-2-alpha kinase GCN2Homo sapiens (human)IC503.388011
Eukaryotic translation initiation factor 2-alpha kinase 1Homo sapiens (human)IC500.460011
Eukaryotic translation initiation factor 2-alpha kinase 3Homo sapiens (human)IC500.015422
Interferon-induced, double-stranded RNA-activated protein kinaseHomo sapiens (human)IC500.905011
Receptor-interacting serine/threonine-protein kinase 1Homo sapiens (human)IC500.069111