Synonyms: AR-11324 | AR11324 | ester 60 [PMID: 27072905] | Rhokiinsa® | Rhopressa®
netarsudil is an approved drug (FDA (2017), EMA (2019))
Compound class:
Synthetic organic
Comment: Netarsudil (AR-11324) is a combination Rho-associated protein kinase (Rho or ROCK) and norepinephrine transporter (NET) inhibitor [2,5]. Netarsudil is the S-enantiomeric, 2,4-dimethyl benzoate ester of compound 29 (Ki 0.2nM) described in [5]. Esterification improves bioavailability and corneal penetrating ability of the compound. It is an ocular hypotensive medication.
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 |
At 10 μM, AR-13324 inhibits NET by 96% and SERT by 94% [5]. In a kinase screening panel 0.5 μM AR-13324 inhibited 11 kinases by >90%. Of these 11, ROCK1, ROCK2, PKCδ and PKCη are the only four identified as potential targets for lowering intra-ocular pressure. The S-enantiomer is the more active isomer, with the R-enantiomer having a lower Ki of 106nM and the racemate having a Ki of 4.2nM vs. ROCK2 [5]. Preclinical evaluation is reported in [2]. |
Selectivity at enzymes | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
|