Synonyms: compound 6 [PMID: 24900593] | GSK-2656157
Compound class:
Synthetic organic
Comment: GSK2656157 is an optimised, ATP-competitive inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK), designed using the structural scaffold of GSK2606414 [2]. Preclinical evaluation is reported in [1].
![]() Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
|
Bioactivity Comments |
In a screening panel of >300 kinases 10μM GSK2656157 inhibited only 17 kinases >80% [2]. GSK2656157 has an improved pharmacokinetic profile compared to GSK2606414 and exhibits antitumor and antiangiogenic activity in preclinical testing [1] |
Selectivity at enzymes | ||||||||||||||||||||||||||||||||||
Key to terms and symbols | Click column headers to sort | |||||||||||||||||||||||||||||||||
|