2CTAP is a small molecule inverse agonist of FFA2 receptor signalling, inhibits constitutive Ca2+ levels, antagonised acetate-induced pERK1/2 and prevents damage following IRI, has no effect on cAMP.

AZ13595491 (AZ491) is a potent, selective G-protein-coupled receptor GPR120 (FFAR4) agonist with IC50 of 0.74/1.0 uM for huamn/mouse GPR120, respectively.

AZ423 (AZ13595423, AZ-423) is a potent, selective G-protein-coupled receptor GPR120 (FFAR4) agonist with IC50 of 0.36/0.51 uM for huamn/mouse GPR120, respectively.

CPL207280 (CPL 207280) is a novel potent, selective GPR40/FFA1 agonist with EC50 of 80 nM in a Ca2+ influx assay, shows greater potency than fasiglifam (EC50=270 nM).

MK-2305 (MK2305) is a potent and selective partial GPR40 (FFAR1) agonist with EC50 of 6 nM (rat GPR40), stimulates glucose stimulated insulin secretion (GSIS).

Phenylacetamide 2 (FFA2 allosteric agonist 2) is a potent, specific and allosteric agonist of FFA2 (GPR43) with cAMP IC50 of 0.48 and 0.66 uM for hFFA2 and mFFA2, respectively.

TUG-2304 (TUG2304) is a highly potent FFA2 (GPR43) antagonist with IC50 of 3-4 nM in both cAMP and GTPγS assays.

Merigolix is a potent, selective gonadotrophin releasing hormone (GnRH) antagonist.

SCH900271 is a potent nicotinic acid receptor GPR109A agonist with EC50 of 2 nM in hu-GPR109a assays.

AS1535907 is a potent GPR119 agonist with EC50 of 4.8 uM in HEK293 cells stably expressing human GPR119.

AS1907417 is a potent, selective GPR119 agonist with cAMP EC50 of 1.1 uM (human GPR119).

HBK001 (HBK-001) is a dual-target DPP4 inhibitor and GPR119 agonist with IC50 of 66 nM for DPP4 and EC50 of 30 nM for GPR119 transactivation activity.

JTP-109192 (JTP109192) is a potent GPR119 agonist with EC50 of 3.6. 4.5 and 5.2 nM for human, rat and mouse GPR119 respectively (increased intracellular cAMP levels).

ZB-16 (ZB40-0016) is a potent, selective GPR119 agonist, increase intracellular cAMP with EC50 of 7.25 nM, stimulates incretin secretion.

CID1792197 is a potent, selective GPR55 agonist with EC50 of 110 nM in the β-arrestin trafficking assay,100-fold selectivity for GPR55 over GPR35, CB1 and CB2.

OX04528 is a highly potent, selective, G-protein pathway biased and orally bioavailable GPR84 agonist with EC50 of 5.98 pM for inhibition of FSK (25 uM)-induced cAMP production in CHO-hGPR84 cells.

OX04529 is a highly potent, selective, G-protein pathway biased and orally bioavailable GPR84 agonist with EC50 of 18.5 pM for inhibition of FSK (25 uM)-induced cAMP production in CHO-hGPR84 cells.

RTI-122 (RTI 122) is a highly potent, selective and brain permeable GPR88 agonist with cAMP EC50 of 11 nM (hGPR88 CHO).

RGH-235 is a potent, selective, and orally active H3 receptor antagonist/inverse agonist with high affinity (Ki=3.0-9.2 nM, depending on species), without affinity to H1, H2 or H4 receptors.

UR-MB-69 is a potent agonist of histamine H2 receptor (H2R) dopamine receptor D3R with pKi of 8.69 and 8.06, respectively.

LY290154 is a leukotriene LTD4/E4 antagonist.

ACT-1016-0707 is a potent, selective, and orally active lysophosphatidic acid receptor subtype 1 receptor (LPA1 receptor, LPAR1) antagonist with IC50 of 3.1 nM, highly selective over LPAR2 or LPAR3.