Receptor Ligand Structure (or Sequence) Mode of action Highest status References
ADGRG2 Tethered peptide agonist TSFGILLDLSRTSLP Agonist Demberg et al., 2015
AGTR2
Angiotensin II (ANG II)
Asp1-Arg2-Val3-Tyr4-Ile5-His6-Pro7-Phe8
Agonist
Clinic
Guimond et al., 2014; Hallberg et al., 2018
Saralasin [Sar1,Val5,Ala8]Ang II Agonist Clinic Guimond et al., 2014; Hallberg et al., 2018
Sarile [Sar1,Ile8]Ang II Agonist Clinic Guimond et al., 2014; Hallberg et al., 2018
MP-157 No structural formula is disclosed Agonist Phase I Hallberg et al., 2018
C21/M24 Agonist Phase II Hallberg et al., 2018
C38/M132 Antagonist Hallberg et al., 2018
LGR4 R-spondins R-spondin1-4(RSPO1-4) Agonist Carmon et al., 2011; de Lau et al., 2011; Glinka et al., 2011
Norrin MRKHVLAASFSMLSLLVIMGDTDSKTDSSFIMDSDPRRCMRHHYVDSISHPLYKCSSKMVLLARCEGHCSQASRSEPLVSFSTVLKQPFRSSCHCCRPQTSKLKALRLRCSGGMRLTATYRYILSCHCEECNS Agonist Deng et al., 2013
TNFSF11(RANKL) Tumor necrosis factor (TNF) superfamily member 11 Agonist Luo et al., 2016
GPER G-1 Agonist Bologa et al., 2006
G15 Antagonist Dennis et al., 2009; Dennis et al., 2011
G36 Antagonist Dennis et al., 2011
A1AR
Trabodenoson (INO-8875)
partial agonist
Phase III
Jacobson et al., 2019
A2AAR Regadenoson agonist Jacobson et al., 2019
A3AR IB-MECA agonist Phase III Jacobson et al., 2019