Orphan

Besides the increasing number of categorized GPCRs with assigned endogenous ligands and (partially) elucidated signaling pathways, a large number of GPCRs remain whose endogenous ligands are unknown, and are classified as orphan GPCRs. Traditionally this class of GPCRs has been difficult to study and although molecular biological and bioinformatics techniques made the identification of orphan GPCRs amenable, the development of therapeutic compounds targeting these receptors has been extremely slow. Nevertheless, these GPCRs are considered important targets based on their distribution and behavioral phenotype as revealed by animals lacking the receptor[1] and [2]


[1] S Chung et al. Orphan GPCR research. Br J Pharmacol. 2008 Mar;153 Suppl 1:S339-46.
[2] JA Stockert et al. Advancements in therapeutically targeting orphan GPCRs. Front Pharmacol. 2015 May 8;6:100.

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Axon ID Name Description From price
2569 JNJ 63533054 Potent, brain-penetrant, selective agonist of GPR139 €90.00
2609 NCRW0005-F05 GPR139 antagonist; useful tool to study GPR139 pharmacology €125.00

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