MK-0557 is a highly selective, orally administered neuropeptide NPY5R antagonist, could limit weight regain after very-low-calorie diet (VLCD)-induced weight loss.

MDK-5220(Orexin-2 receptor agonist) is the first selective nonpeptidic orexin 2 receptor (OX2R) agonist (OX2R EC50 = 0.023 μM, Emax = 98%; OX1R EC50 = 1.616 μM, Emax = 100%)

macitentan (Actelion-1, ACT-064992) is an orally active, non-peptide dual endothelin (ET)A/B receptor antagonist with IC50 of 0.5 nM/391 nM.

LY404039 is an inhibitor for mGluR1(Ki=149 nM) and mGluR2(Ki= 92 nM), which can also inhibit dopamine receptor.

LY310762 is a 5-HT1D receptor antagonist with Ki of 249 nM, having a weaker affinity for 5-HT1B receptor.

LY2119620 is a specific, and allosteric agonist of human M2 and M4 muscarinic acetylcholine receptors.

Losartan is an angiotensin II receptor antagonist, competes with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM.

Levobetaxolol hydrochloride is a beta-adrenergic receptor inhibitor (beta blocker), used to lower the pressure in the eye in treating conditions such as glaucoma.

Lasmiditan (COL-144; LY573144) is a high-affinity, highly selective 5-HT1F receptor agonist(Ki=2.1 nM), compared with Ki of 1043 nM and 1357 nM at the 5-HT(1B) and 5-HT(1D) receptors, respectively.

Ki16425 is a competitive, potent and reversible antagonist to LPA1, LPA2 and LPA3 with Ki of 0.34 μM, 6.5 μM and 0.93 μM, respectively, shows no activity at LPA4, LPA5, LPA6.

JNJ-63533054 is a potent and selective agonist of hGPR139 with an EC50 = 16 nM.

JNJ-10229570 (JNJ10229570) is a novel potent, selective melanocortin receptor MC1R and MC5R antagonist with binding IC50 of 270 nM and 200 nM, respectively.

JD5037 is an inverse agonist of peripheral cannabinoid 1 (CB1) receptors (Ki = 0.35 nM).

ISX-9 is a small molecule inducer of adult neural stem cell differentiation both in vitro and in vivo.

Istradefylline(KW6002) is a very potent, selective and orally active adenosine A2A receptor antagonist(Ki=2.2 nM) in experimental models of Parkinson's disease.

Inhibitor of protease-activated receptor 1 (PAR1)-mediated platelet activation (IC50 = 0.26 μM for the inhibition of platelet P-selectin expression on human platelets). Thought to act allosterically. Also inhibits thrombin-induced platelet activation.

GW 627368X is a selective prostanoid EP4 receptor competitive antagonist with additional affinity at TP receptors (pKi values are 7.0 and 6.8 in competition radioligand bioassays).

GSK-137647 is a potent and selective FFA4 (GPR120) agonist (pEC50 values are 6.3, 6.2 and 6.1 at the human, mouse and rat receptor, respectively). Exhibits ≥100-fold selectivity against a panel of 61 targets including FFA1, FFA2 and FFA3.

Grapiprant is a selective EP4 receptor antagonist whose physiological ligand is prostaglandin E2 (PGE2)

GPR120 compound A is an orally available, high-affinity agonist of GPR120 (EC50 = ~0.35 µm) that demonstrates potent selectivity over another lipid-sensing G-protein, GPR40 (FFAR1).

Glycopyrrolate(Glycopyrronium Br) is a muscarinic competitive antagonist used as an antispasmodic.

Fosaprepitant (MK-0517, L-758,298) is a water-soluble phosphoryl prodrug for Aprepitant which is a NK1 antagonist.

Fexofenadine is a third-generation antihistamine pharmaceutical drug used in the treatment of allergy symptoms, such as hay fever, nasal congestion, and urticaria.

Fevipiprant(QAW039) is a selective, potent, reversible competitive CRTh2 antagonist with an in vitro dissociation constant KD value of 1.1nM at the CRTh2 receptor and an IC50 value of 0.44 nM for inhibition of PGD2-induced eosinophil shape change.

Fesoterodine Fumarate is an antimuscarinic agent and is rapidly de-esterified to its active metabolite 5-hydroxymethyl tolterodine that is a muscarinic receptor antagonist.

Etrasimod (APD334) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1(S1P1) receptor with an IC50 value of 1.88 nM in CHO cells.

Eptapirone (F-11,440) is a very potent and highly selective 5-HT1A receptor full agonist of the azapirone family.

EMPA is a high-affinity, reversible and selective orexin OX2 receptor antagonist. [3H]EMPA binds to human and rat OX2-HEK293 membranes with KD values of 1.1 and 1.4 nM respectively.

EMA401(Olodanrigan) is a highly selective AT2R antagonist, inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons.

Eluxadoline is an orally active mixed μ opioid receptor (μOR) agonist δ opioid receptor (δOR) antagonist.