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Compound class: Synthetic organic
Comment: Compound 16 is a novel, potent and selective sphingosine-1-phosphate receptor 2 (S1P2 receptor) antagonist . The series of compounds including 16 is claimed in patent WO2013047701 .
Ligand Activity Visualisation Charts
These 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.✖
1. Kusumi K, Shinozaki K, Yamaura Y, Hashimoto A, Kurata H, Naganawa A, Otsuki K, Matsushita T, Sekiguchi T, Kakuuchi A et al.. (2016)
Discovery of novel S1P2 antagonists, part 3: Improving the oral bioavailability of a series of 1,3-bis(aryloxy)benzene derivatives.
Bioorg Med Chem Lett, 26 (4): 1209-13. [PMID:26794040]
2. Naganawa A, Kusumi K, Sekiguchi T, Kakuuchi A, Shinozaki K, Yamamoto H, Nonaka S. (2013)
Patent number: WO2013047701. Assignee: Ono Pharmaceutical Co., Ltd.. Priority date: 29/09/2011. Publication date: 04/04/2013.
3. Roviezzo F, Brancaleone V, De Gruttola L, Vellecco V, Bucci M, D'Agostino B, Cooper D, Sorrentino R, Perretti M, Cirino G. (2011)
Sphingosine-1-phosphate modulates vascular permeability and cell recruitment in acute inflammation in vivo.
J Pharmacol Exp Ther, 337 (3): 830-7. [PMID:21421740]