Compound class:
Synthetic organic
Comment: NF-56-EJ40 is a potent succinate receptor antagonist [2].
![]() 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. ✖ |
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References |
1. Cho EH. (2018)
Succinate as a Regulator of Hepatic Stellate Cells in Liver Fibrosis. Front Endocrinol (Lausanne), 9: 455. [PMID:30186230] |
2. Haffke M, Fehlmann D, Rummel G, Boivineau J, Duckely M, Gommermann N, Cotesta S, Sirockin F, Freuler F, Littlewood-Evans A et al.. (2019)
Structural basis of species-selective antagonist binding to the succinate receptor. Nature, 574 (7779): 581-585. DOI: 10.1038/s41586-019-1663-8 [PMID:31645725] |
3. Littlewood-Evans A, Sarret S, Apfel V, Loesle P, Dawson J, Zhang J, Muller A, Tigani B, Kneuer R, Patel S et al.. (2016)
GPR91 senses extracellular succinate released from inflammatory macrophages and exacerbates rheumatoid arthritis. J Exp Med, 213 (9): 1655-62. [PMID:27481132] |
4. Rubic T, Lametschwandtner G, Jost S, Hinteregger S, Kund J, Carballido-Perrig N, Schwärzler C, Junt T, Voshol H, Meingassner JG et al.. (2008)
Triggering the succinate receptor GPR91 on dendritic cells enhances immunity. Nat Immunol, 9 (11): 1261-9. [PMID:18820681] |