GPCR/G-Protein

<p>Lazuvapagon is a vasopressin V2 receptor agonist that can be used to study enuresis.</p>

<p>TASP0376377 is a potent antagonist of CRTH2.</p>

<p>gonadotropin-releasing hormone (GnRH, LHRH) receptor antagonist,orally active</p>

<p>SKF 81297 hydrobromide, a selective agonist of the dopamine D1-like receptor，exhibits central activity and is widely used to study the neuromodulatory effects.</p>

<p>EX-1314 (BMS-604992) is a growth hormone secretagogue receptor (GHSR) agonist.</p>

<p>AZD2423 is a potent, selective, orally bioavailable, and non-competitive CCR2 chemokine receptor negative allosteric modulator and it has an IC50 of 1.2 nM for</p>

<p>Compound 39, an APJ receptor agonist, has a K i of 0.6 nM, activates Gαi1 (EC50 0.8 nM), recruits β-arrestin2 (EC50 31 nM), and affects heart function.</p>

<p>17-Phenyl trinor Prostaglandin F2αdiethyl amide (17-phenyl trinor PGF2αdiethyl amide) is a Prostaglandin F2α(PGF2α) analog characterized by the substitution of the C-1 carboxyl group with an N-diethyl amide. Prostaglandin (PG) esters and N-ethyl amides have demonstrated ocular hypotensive properties, with N-ethyl amides introduced as alternative options for PG hypotensive prodrugs. Studies indicate that both bovine and human corneal tissues can convert N-ethyl amides of various PGs into their free acid forms at a rate of approximately 2.5 µg/g corneal tissue/hr. However, dialkyl amides like 17-phenyl trinor PGF2αdiethyl amide resist conversion by corneal amidase, showing no detectable transformation into free acids. This characteristic suggests their potential as valuable investigative tools for assessing the intrinsic intraocular hypotensive activities of PG amides.</p>

<p>GSK-554418A, a novel azaindole CB(2) agonists, is used for the treatment of chronic pain. It is efficacious in the acute model and the chronic joint pain model.</p>

<p>ONO-2050297 is the first potent dual CysLT1 and CysLT2 antagonist with IC50 values of 0.017 μM (CysLT1) and 0.00087 μM (CysLT2), respectively.</p>

<p>Aganepag isopropyl can be used to treat Glaucoma.</p>

<p>Abaperidone is an atypical antipsychotic, antagonizes 5-HT2A (IC50=6.2 nM) and D2 receptors (IC50=17 nM), reduces hsp70 mRNA in rat brains.</p>

<p>Velusetrag(TD-5108), a potent 5-HT4 agonist, is in development for gastroparesis, constipation, and IBS.</p>

<p>APJ receptor agonist 6 is a potent agonist of the APJ (apelin receptor) (Ki: 0.059 μM). (EC50: 6.22 μM).</p>

<p>Bufuralol (Ro 3-4787) is a 尾-adrenergic receptor blocker with a certain degree of sympathomimetic effects and can be used to study cardiovascular diseases.</p>

<p>FR-181157, a novel prostaglandin (PG) mimetic, shows high potency and agonist efficacy at the IP receptor and has good bioavailability.</p>

<p>11-Keto Fluprostenol, a potent analog of prostaglandin F2α (PGF2α), primarily interacts with the FP receptor. It is a structurally modified derivative of prostaglandin D2 (PGD2) designed to enhance its potency and extend its half-life. The compound is produced by oxidizing fluprostenol at the C-11 position, which results in 11-keto fluprostenol. This modification allows 11-keto Fluprostenol to exhibit moderate affinity for the CRTH2/DP2 receptor, though it shows negligible activity at the DP1 receptor, distinguishing its action from that of PGD2.</p>

<p>E-6123 is an antagonist of platelet-activating factor (PAF) receptor.</p>

<p>ACT-335827: oral, brain-penetrant OXR1 selective antagonist; IC50: 6 nM (OXR1), 417 nM (OXR2); for neurological research.</p>

<p>PSB-10 hydrochloride is a human adenosine A3 receptor antagonist.</p>

<p>GSA-10 is a potent Smoothened (Smo) receptor agonist with an EC50 of 1.2 μM.</p>

<p>LY320954 is an antagonist of 5-HT2A receptor.</p>

<p>(S)-Renzapride (BRL 24924), 5-HT4 agonist (Ki 115 nM), 5HT2b/5HT3 antagonist, for C-IBS study.</p>

<p>Xanthine amine congener is an Adenosine receptor antagonist.</p>

<p>BMS-763534 is a potent antagonist of corticotropin-releasing factor/hormone receptor 1 (CRHR-1).</p>

<p>YM44778 is a NK1-receptor antagonist for treating restless legs syndrome.</p>

<p>GR-127935 is a potent and selective 5-HT1B/1D receptor antagonist.</p>

<p>Hh-Ag1.5 is a dual Hedgehog/Smo agonist (EC50/Ki: 0.5-2.3 nM), reprograms hepatic stem cells, and differentiates hiPSCs into neural/skin cells.</p>

<p>LX-1031 is an effective inhibitor of tryptophan 5-hydroxylase. LX-1031 decreases serotonin (5-HT) synthesis peripherally.</p>

<p>UNC9994 is a β-arrestin-biased dopamine D₂ receptor agonist (β-arrestin EC50 = 50 nM; Emax = 97%) with robust in vivo antipsychotic drug-like activities.</p>

<p>Compound 40, a cyclic Ape13 analogue and potent APJ agonist (Ki 5.7 nM), shows Gα12-bias and longer half-life.</p>

<p>UCB-35440, a 5-lipoxygenase inhibitor and a histamine H1 receptor antagonist, is used potentially for the treatment of dermatitis.</p>

<p>2-Furoyl-LIGRLO-amide TFA is a potent and selective agonist of the proteinase-activated receptor 2 (PAR2), exhibiting a pD2 value of 7.0 [1] [2].</p>

<p>"YM543 is an effective, oral SGLT2 inhibitor that lowers blood glucose, useful for diabetes research."</p>

<p>CCR2 antagonist 4 (Teijin compound 1) is a potent and specific antagonist of CCR2(IC50s of 180 nM), and potently inhibits MCP-1-induced chemotaxis(IC50 of 24 nM</p>

[D-Ala6]-LH-RH, a Luteinizing-hormone-releasing hormone (LHRH) analogue, functions as a gonadotropin-releasing hormone (GnRH) receptor agonist [1].

<p>PD-140548 is a potent, CCKA receptor-selective antagonist.</p>

<p>S1P5 Receptor Agonist-1 (example 6) is a highly potent and selective agonist for the S1P5 receptor, exhibiting an EC50 value of 20 nM.</p>

<p>AGN-191129 (PGF2α-OMe) is a PGF2α analog with C-1 carboxyl replaced by O-methyl; it lowers eye pressure, but its receptors are unclear.</p>

<p>Dihydrexidine is a full efficacy D1-like dopamine receptor (D1/D5) agonist (IC50: 10 nM for D1 receptor). It also shows potent antiparkinsonian activity.</p>

<p>(+)-Dihydrexidine hydrochloride is an agonist of dopamine D1 receptor(EC50 of 72± 21 nM).</p>

<p>γ-Linolenoyl monoethanolamide, a fatty N-acyl ethanolamine, acts as an endocannabinoid [1] [2].</p>

<p>Prostaglandin E1 (PGE1), though not predominantly found in nature, plays a significant role in clinical treatments, addressing conditions such as peripheral occlusive vascular disease, erectile dysfunction, and neonatal cardiology issues. The metabolism of PGE1 primarily begins with the oxidation at C-15, producing 13,14-dihydro-15-keto PGE1 as its major metabolite. Alternatively, inhibiting this pathway or overwhelming it with too much PGE1 could potentially enhance the production of 2,3-dinor metabolites, like 2,3-dinor PGE1, though their biological activities remain unreported. Cayman Chemical stands out as a prominent provider of prostaglandins and their metabolites, uniquely manufacturing 2,3-dinor PGE1.</p>

<p>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].</p>

<p>IPG7236, a selective CCR8 antagonist, demonstrates notable tumor suppression in a mouse xenograft model of human breast cancer and is applicable in cancer</p>

<p>Prostaglandin E2-1-glyceryl ester, a member of the Prostaglandin Glycerol Ester family, serves as an endocannabinoid ligand targeting the CB1 receptor. This compound triggers a swift and transient surge in intracellular free calcium levels [1] [2].</p>

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

<p>Prostaglandin K2 (PGK2), a 9,11-diketone derivative, results from PGE2 or PGD2 oxidation. Its biological presence remains speculative; however, it demonstrates resistance to in vitro metabolism by 15-hydroxy PGDH.</p>

<p>L 691678 is a potent leukotriene biosynthesis inhibitor.</p>

<p>Quinpirole dihydrochloride is an agonist of the D2-like dopamine receptor.</p>

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

<p>PSB-SB1202 (Compound 21a), a phenyl coumarin compound, acts as a CB1/CB2 agonist. It demonstrates EC50 values of 56 and 14 nM and K i values of 32 and 49 nM for CB1 and CB2 receptors, respectively [1].</p>

<p>RO5527239 is a potent, orally available GPBAR1 agonist agent.</p>

Tarazepide is a potent and specific antagonist of CCK-A receptor.

<p>CGS 21680 is a chemical compound that acts as a selective agonist for both adenosine and its A2A receptor, demonstrating a binding affinity (K i) of 27 nM.</p>

<p>Pronethalol ((±)-Pronethalol), a non-selective β-adrenergic antagonist, effectively inhibits Sox2 expression and offers protection against Digitalis-induced ventricular arrhythmias. Additionally, it can reverse such arrhythmias and limit the development of cerebral arteriovenous malformations (AVMs) [1] [2].</p>

<p>DU-125530 is a 5-HT1A receptor antagonist.</p>

CB2R-IN-1 is a potent inverse agonist of the cannabinoid CB2 receptor (Ki: 0.9 nM).

<p>(2R,3R)-E1R is a sigma-1 receptor modulator for cognitive/memory disorder treatment.</p>

<p>JTE-952: oral, selective Type II CSF-1R inhibitor, IC50 = 13 nM for CSF1R, 261 nM for TrkA, effective in mouse arthritis model.</p>

<p>TASP0412098 is a potent, selective CRTH2 antagonist with oral activity.</p>

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

<p>PAC1R antagonist 1 is a PAC1 receptor antagonist that inhibits the activation of peptides by pituitary adenylate cyclase and can be used to study tumours.</p>

<p>Example 2 (RXFP1 receptor agonist-8) is a potent RXFP1 receptor agonist that suppresses cAMP production in HEK293 cells expressing human RXFP1, exhibiting an</p>

Lidamidine (Lidamidinum) is an effective antidiarrheal agent that inhibits intestinal secretion, reduces intestinal transit, and inhibits smooth muscle

<p>SLIGRL-NH2 TFA, also known as Protease-Activated Receptor-2 Activating Peptide TFA, is a Protease-Activated Receptor-2 (PAR-2) agonist [1].</p>

<p>Thromboxane A2: unstable, leads to thromboxane B2, induces platelet aggregation, causes vasoconstriction.</p>

<p>CI-949 inhibits LTC4/D4, histamine, TXB2 release (IC50: 0.5, 11.4, 0.1 μM).</p>

<p>Ro-70-0004 is a selective antagonist of alpha1A-adrenoceptor.</p>

<p>LMD-009 is a non-peptide, selective CCR8 agonist that mediates chemotaxis, inositol phosphate accumulation, and calcium release, with an EC50 of 11–87 nM.</p>

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

<p>CB-52 acts as a neutral antagonist and ligand for the CB2 cannabinoid receptor [1].</p>

SSTR5 antagonist 1: selective, oral SSTR5 blocker; IC50: 9.6 nM (human), 57 nM (mouse).

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

<p>Siramesine Fumarate, a sigma receptor agonist, is used potentially for the treatment of generalized anxiety disorder.</p>

<p>9-Keto Fluprostenol, a potent analog of prostaglandin E2 (PGE2), features structural modifications aimed at enhancing its half-life and potency. It derives from Fluprostenol, a thoroughly researched, potent analog of PGF2α, primarily interacting with the FP receptor. The creation of 9-Keto Fluprostenol through the oxidation at C-9 of Fluprostenol suggests a high affinity for EP receptors, potentially functioning as a PGE2 agonist.</p>

<p>TRAP-6-IN-1 inhibits collagen/TRAP-6, IC50: 17.12/11.88 μM, blocks platelet aggregation.</p>

<p>ZINC49534341 is a potent MRGPRX2 antagonist, exhibiting a K_i (inhibition constant) of 32 nM [1].</p>

<p>FTY720 (S)-Phosphate is an active FTY720 derivative modulating S1P receptors, preventing lymphocyte egress, enhancing barrier integrity, aiding immune research.</p>

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

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

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

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

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

<p>MC-4R Agonist 2 hydrochloride (Example 1) serves as an MC4R agonist, with applications in researching obesity, diabetes, inflammation, and erectile dysfunction.</p>

5-HT3 antagonist 1 is a potent and selective antagonist of 5-HT3 receptor.

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

<p>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</p>

<p>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</p>

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

Fiboflapon sodium, an oral 5-LOX-activating protein inhibitor, binds FLAP at 2.9 nM, inhibits LTB4 at 76 nM.

<p>AJ-76 hydrochloride ((+)-AJ 76 hydrochloride) serves as a dopamine autoreceptor antagonist, exhibiting pK i values of 6.95 for hD3, 6.67 for hD4, 6.37 for hD2S, 6.21 for hD2L, and 6.07 for rD2 receptors, indicating its binding affinity strength across these receptor types.</p>

<p>GT-2331 is a histamine H3 receptor antagonist.</p>

<p>PSB-1901: potent A2B Adenosine Receptor Antagonist; Ki=0.0835 nM; &gt;10,000x selective; effective in mice for preclinical studies.</p>

<p>AZD9898 inhibits leukotriene-C4 synthetase (IC50: 0.28 nM), aids asthma research, and reduces GABA binding, liver toxicity.</p>

ACT-209905 is an agonist of S1P1 receptor.

Sigma-1 receptor antagonist 1 is an effective and selective antagonist of sigma-1 receptor.

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

RS 100329 hydrochloride is an antagonist of α1A-adrenergic receptor.

<p>Prostaglandin F2α serinol amide, a serinolamide G protein-coupled receptor, elevates calcium levels in human non-small cell lung cancer cells. Additionally, Prostaglandin F2α functions as a luteinizing hormone in sheep and potentially serves as a nociceptive mediator in the spinal cord [1] [2] [3].</p>

<p>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).</p>