GPCR/G-Protein

MB-28767 is an agonist of prostaglandin E2 (PGE2) receptor.

SB-649701 is a potent antagonist of the human CCR8 receptor, exhibiting a pIC50 value of 7.7, and is utilized in asthma research [1].

20-Ethyl Prostaglandin E2 (20-ethyl PGE2) is an analog of Prostaglandin E2 (PGE2) characterized by an extended ω-chain due to two additional methylene carbon atoms. Compared to unoprostone, a clinically approved glaucoma medication and the only extensively studied prostaglandin analog sharing this structural modification, 20-ethyl PGE2 maintains the natural 15(S) allylic hydroxyl in its lower side chain, potentially enhancing its effectiveness. Unoprostone, despite being an F-series prostaglandin, exhibits reduced affinity for FP receptors because of its lower side chain modifications (13,14-dihydro-15-keto), which diminishes its medicinal potency. Notably, 20-ethyl PGE2's efficacy relative to unoprostone and its interaction with EP or other prostanoid receptors remains unconfirmed due to the lack of published ligand binding assays. E-type prostaglandins, including 20-ethyl PGE2, are broadly acknowledged for their inflammatory, cytoprotective, and diverse biological activities.

CMPD167 (MRK-1) is a potent, orally active inhibitor of CCR5 with significant in vitro antiviral efficacy [1].

BI-167107 is a high affinity, full agonist that binds to the β2 adrenergic receptor (β2AR, Kd of 84 pM).

Cenerimod (ACT-334441) is an S1P1 agonist used in the study of murine experimental autoimmune encephalomyelitis (EAE) and murine scleroderma.

GS-6201 (CVT-6883) is a selective antagonist of adenosine A2B receptor.

SB 258719 is a selective antagonist of 5-HT7 receptor with pKi of 7.5.

JNJ-19567470 is a selective, non-peptide CRF receptor 1 antagonist.

PF-184563 is an effective and selective non-peptide antagonist of the V1a receptor with oral activity, suitable for studying Raynaud's disease dysmenorrhoea.

Omidenepag isopropyl (DE-117) is a prostaglandin EP2 receptor agonist used in the study of glaucoma and hypertension.

MK 0893 is a potent and selective Glucagon Receptor (GR) antagonist competitive, reversible cAMP activity, which attenuates blood glucose elevation.

4-Amino-PPHT Hydrobromide is a precursor for fluorescent labeled Dopamine D2 receptors agonist.

BMS-639623 is a CCR3 antagonist with a picomolar inhibitory effect on eosinophilic chemotaxis and can be used in the treatment of asthma.

GSK1842799 is a selective S1P1 receptor agonist with good oral bioavailability.

DG-041: EP3 receptor antagonist, high affinity (IC50: 4.6 & 8.1 nM), inhibits PGE2 in platelets, blood-brain barrier permeable.

RBC10 inhibits the binding of Ral to its effector RALBP1, as well as inhibiting Ral-mediated cell spreading of murine embryonic fibroblasts and anchorage-

L 662025 is a PAF receptor antagonist.

Isopropyl dodec-11-enylfluorophosphonate (IDEFP) is an organophosphorus ester functioning as a central cannabinoid receptor (CB1) antagonist and exhibits

Gentisein (NSC-329491), a primary metabolite of Mangiferin, exhibits significant inhibition of serotonin uptake, demonstrating potency with an IC50 value of 4.7

adenosine A2B receptor antagonist

BAY-298: oral LH-R antagonist; IC50: 96nM (hLH), 23nM (rLH), 78nM (cLH); first to lower sex hormones in vivo.

KP496 is a selective, dual antagonist for Thromboxane A2 receptor and Leukotriene D4 receptor.

L-054,522 is potent, selective agonists of somatostatin receptor.

17-Phenyl trinor Prostaglandin E2 (17-phenyl trinor PGE2) is a synthetic analog of PGE2, functioning as an agonist at the EP1 and EP3 receptors. It induces contraction of the guinea pig ileum at a 11 µM concentration and displays slightly less potency than PGE2 in stimulating the gerbil colon and rat uterus. Notably, with an ED50 value of 350 µg/kg, 17-phenyl trinor PGE2 exhibits 4.4 times greater antifertility efficacy in hamsters compared to PGE2.

NK3R-IN-1 (compound 16x), an orally active imidazolepiperazine derivative, acts as a Neurokinin Receptor NK3R inhibitor and has been shown to reduce blood

BLT2 Probe 1, based on CAY10583, is a fluorescent tool for studying BLT2 pharmacology, aiding research in diabetes and GI lesion treatment.

Prostaglandin D3 (PGD3) functions as an inhibitor of platelet aggregation and modulates autonomic neurotransmission in humans [1].

Compound 24e, a leukotriene B4 (LTB4) antagonist, exhibits an inhibitory concentration 50 (IC50) of 477 nM and demonstrates anti-inflammatory activity [1].

AM841, a high-affinity electrophilic ligand, covalently interacts with a cysteine residue in helix six, thus activating the CB1 cannabinoid receptor.

Bivamelagon hydrochloride is a selective MC4R agonist (EC50=36.5 nM, Ki=65 nM), oral and blood-brain barrier penetration, suitable for obesity and diabetes.

LTB4 antagonist 2, a carboxamide-acid compound, serves as an antagonist to leukotriene B4 (LTB4), possessing potential anti-inflammatory properties.

MC-4R Agonist 2 (Example 1), a melanocortin 4 receptor (MC4R) agonist, is employed in the research of conditions such as obesity, diabetes, inflammation, and

PNU109291, a potent and selective agonist of the 5-HT1D receptor, effectively mitigates dural plasma extravasation induced by trigeminal ganglion stimulation.

BLT2 antagonist-1 (compound 15b) is a selective inhibitor of the BLT2 receptor, impeding the chemotaxis of CHO-BLT2 cells at an IC50 of 224 nM, while not

OMDM-5 is a potent vanilloid receptor type 1 (TRPV1, EC50 = 75 nM) agonist, showing weak ligand activity at cannabinoid type 1 receptor (CB1, Ki=4.9 μM).

LTB4 Antagonist 1, a carboxamide-acid derivative, potently inhibits Leukotriene B4 (LTB4) activity with an IC50 value of 288 nM and exhibits notable anti-

O-Arachidonoyl glycidol (compound 1), a 2-arachidonoylglycerol (2-AG) analog, effectively inhibits the hydrolysis of cytosolic 2-oleoylglycerol (2-OG) with an IC50 value of 4.5 µM, and also blocks 2-OG and anandamide hydrolysis in membrane fractions with IC50 values of 19 µM and 12 µM, respectively [1].

Osemozotan Free Base is a 5-HT(1A) receptor agonist.

Epinephrine HCl is a hormone and neurotransmitter secreted by the adrenal medulla, agonist of α-adrenergic and β-adrenergic receptor.

Velagliflozin is an orally available inhibitor of sodium-glucose cotransporter 2.

EP4 receptor agonist 2 (compound 31) is a potent EP4 receptor agonist, demonstrating an EC50 value of 0.8 nM and K_i values of >100,000, 38,000, and 3.1 nM for the EP2, EP3, and EP4 receptors, respectively [1].

Carmoxirole hydrochloride (EMD 45609 hydrochloride) is a selective dopamine D2 receptor agonist with antihypertensive activity in vivo.

AL 8810 methyl ester, a prostaglandin F(2α) analog and receptor agonist, competitively antagonizes FP receptor agonist Fluprostenol effects. It lacks significant potency against TP, DP, EP(2), EP(4) receptor subtypes in cell lines [1].

Fiboflapon (GSK2190915), an oral 5-lipoxygenase inhibitor, binds FLAP at 2.9 nM, inhibits LTB4 with 76 nM IC50.

MRL-650 is an oral, selective CB1 agonist; IC50: CB1=7.5 nM, CB2=4100 nM; anorexigenic effects noted.

O-2050: strong CB1 antagonist (Ki 2.5 nM), CB2 inhibitor (Ki 0.2 nM); reduces mouse food intake, increases activity.

Facinicline hydrochloride (RG3487) is both a novel nicotinic alpha-7 receptor (alpha7nAChR) partial agonist (Ki = 6 nM) and an antagonist of 5-HT3(Ki = 1.2 nM).