GPCR/Proteína-G

<p>(S)-YNT-3708 is the S-isomer of YNT-3708, demonstrating relatively low activity against OX1R and OX2R receptors, with EC50 values of 3595 nM and 1661 nM, respectively.</p>

<p>DCB-3503, a tylophorine analog, may treat cancer and suppress immunity by blocking protein synthesis and modulating HSC70's ATPase activity.</p>

YGZ-331, a sedative hypnotic, acts by elevating GABA levels as a derivative of the adenosine nucleoside NGBA. It functions through activating A1R and A2aR, and inhibiting the phosphorylation of CaMKII (pCaMKII), thereby exerting its calming effects. Additionally, YGZ-331 reduces spontaneous motor activity in mice.

<p>BAY-899, oral LH-R antagonist, IC50: 185 nM (hLH), 46 nM (rLH), lowers sex hormones in vivo.</p>

<p>U75302 is an antagonist of thymosin beta-4 (TB4) receptor with a Ki value of 159 nM on guinea pig lung membranes.</p>

Danavorexton is an orexin receptor agonist.

<p>Becondogrel (2-Oxoclopidogrel) is a metabolite of Clopidogrel. It irreversibly inhibits the P2Y12 receptor, thereby preventing platelet aggregation and thrombosis.</p>

<p>SB 243213 dihydrochloride is an orally active, selective and high-affinity antagonist of 5-hydroxytryptamine (5-HT)2C receptor(pKi of 9.37 and a pKb of 9.8 for</p>

<p>BI-44370, a CGRP (calcitonin gene-related peptide) receptor antagonist, can be used to treat migraines and other chronic pain.</p>

<p>Delmadinone acetate is an orally active compound used to control estrus and ovulation in both female and male pets. It induces adrenal suppression by inhibiting the pituitary release of ACTH.</p>

<p>GnRH antagonist 2 is a GnRH receptor antagonist, useful for studying endocrine diseases.</p>

<p>CCR7-Cmp2105 is a thiadiazole-dioxide allosteric antagonist for CCR7 with a Kd of 3 nM and IC50 of 7.3 μM against arrestin binding.</p>

Ici D1542: potent TXS inhibitor & TXA2 receptor antagonist, effective thromboxane blocker in vitro.

<p>DMPX (3,7-Dimethyl-1-propargylxanthine) is a caffeine-like compound capable of crossing the blood-brain barrier. It serves as an A2-selective adenosine receptor (AR) antagonist, effectively and selectively blocking the hypothermia and behavioral inhibition induced by A2 adenosine receptor agonists, such as NECA. DMPX is utilized in research on diseases like Parkinson's disease.</p>

<p>BI 703704, a soluble guanylate cyclase (sGC) activator, inhibits the progression of diabetic nephropathy in the ZSF1 rat [1].</p>

<p>5-HT2A and 2C receptor antagonist</p>

<p>Bometolol Hydrochloride is a beta-adrenergic blocking compound used for the treatment of cardiovascular disease.</p>

<p>BRD50837 is a potent and selective inhibitor of Sonic Hedgehog (Shh).</p>

<p>L-365260 hemihydrate: selective oral CCK-B/gastrin blocker, Ki=1.9/2.0 nM, competes with guinea pig receptors.</p>

<p>CP-865569 is a CCR1 antagonist useful in the research of inflammatory and autoimmune diseases, including conditions such as rheumatoid arthritis and multiple sclerosis.</p>

<p>EP3 and EP1 receptor agonist</p>

<p>Compound 1f, a potent MRGPRX1 agonist, has an EC50 of 0.22 μM, useful for neuropathic pain studies.</p>

Anthrotainin is a tetracyclic compound that acts as an inhibitor of the binding of P substance (substance P), with an IC50 of 3 μM.

<p>Compound 12a (D1R antagonist 1) is a D1R antagonist that participates in both G-protein-coupled and β-arrestin-mediated signaling pathways [1].</p>

<p>BNS808 is an orally active, selective CB1R antagonist with an IC50 of 0.8 nM, demonstrating significant selectivity for CB2R and minimal brain penetration. It is being studied for the treatment of obesity and related metabolic complications, such as metabolic dysfunction-associated steatotic liver disease (MASLD). BNS808 reduces drug exposure to the central nervous system, enhancing safety, and minimizes drug interactions through high plasma protein binding.</p>

<p>D3/5-HT receptor modulator-1 (compound 5i) is a selective antagonist of the dopamine D3 and 5-HT2A receptors, and a partial agonist at the 5-HT1A receptor. It exhibits Ki values of 4.5 nM, 11.9 nM, and 15.3 nM for the dopamine D3, 5-HT2A, and 5-HT1A receptors respectively. The compound shows lower affinity for the dopamine D2 receptor, 5-HT2C receptor, and hERG channel. D3/5-HT receptor modulator-1 possesses atypical antipsychotic properties.</p>

<p>NK3 receptor antagonist</p>

<p>CI-624 reduces the secretion and output of hydrogen ions, sodium ions, potassium ions, and pepsin. This compound may be utilized in research focusing on cancer and autoimmune diseases.</p>

<p>AFP 07 free acid is a 7,7-difluoroprostacyclin derivative. It also acts as a selective and highly potent agonist for the IP receptor.</p>

<p>5-HT1A modulator 4 (Compound 1) is a ligand for the 5-HT receptor, with Ki values of 2.18 μM for 5-HT1A and 19.7 μM for 5-HT2A.</p>

<p>THRX-194556 is an agonist of the 5-HT4 receptor. It is applicable in the study of gastrointestinal functional disorders and Alzheimer's disease.</p>

<p>LTF4, made in vitro from LTE4 with enzymes, contracts vascular muscle weakly; potency is LTD4 &gt; LTC4 &gt; LTE4 &gt;&gt; LTF4.</p>

<p>MK-0812 is a dual antagonist of the CCR2 and CCR5 receptors that can alleviate adipose inflammation in ob/ob mice.</p>

<p>Nedemelteon is an agonist of the melatonin receptor (melatonin receptor).</p>

<p>Serotonin hydrogen maleate serves as a monoaminergic neurotransmitter and an endogenous 5-HT receptor agonist within the central nervous system (CNS). It also functions as an inhibitor of catechol O-methyltransferase (COMT), exhibiting a Ki value of 44 μM.</p>

<p>Opipramol (Ensidon) is an atypical tricyclic antidepressant (TCA) primarily functioning as a sigma (σ) receptor agonist. It interacts effectively with sigma recognition sites, having a Ki value of 50 nM. Opipramol is applicable in the study of generalized anxiety disorder (GAD).</p>

<p>CRHR1 antagonist 1 (compound 10a) is a non-peptide antagonist of corticotropin-releasing hormone receptor 1 (CRHR1). It serves as a useful tool in the study of psychiatric disorders.</p>

<p>Metrazoline (o-Methyl-tracizoline) acts as a ligand for adrenergic receptors (low affinity) and imidazoline I2 receptors.</p>

<p>Fosrolapitant is an antagonist of the neurokinin 1 (NK1) receptor.</p>

<p>Pentacosafluorotridecanoic Acid (PFTrDA) is a perfluoroalkyl substance (PFAS) that exhibits various biological impacts across different species. In zebrafish embryos, exposure to PFTrDA induces yolk sac edema and increases mRNA expression of thyroid hormone synthesis genes, including tshβ, at concentrations of 0.1 and 0.3 mg/L. At a dosage of 10 mg/kg, PFTrDA reduces serum testosterone and luteinizing hormone levels, as well as palmitic acid, linoleic acid, and oleic acid levels in the testicular interstitial cells of late adolescent rats. In humans, maternal plasma levels of PFTrDA during pregnancy are positively correlated with the development of eczema in female infants (but not male infants), and PFTrDA levels are higher in the livers of cancerous humans compared to non-cancerous ones. Additionally, PFTrDA is found in marine mammals.</p>

<p>Elsovaptan is an antagonist of the vasopressin receptor and is applicable for research in Alzheimer's disease.</p>

<p>Terguride: treats hyperprolactinemia, blocks 5-HT2A/B, activates dopamine receptors, studied for PAH.</p>

<p>MRS4833 (compound 15) is an orally active, potent, competitive antagonist of P2Y14R, exhibiting IC50 values of 5.92 nM for hP2Y14R and 4.8 nM for mP2Y14R. It reduces airway eosinophilia in protease-mediated asthma models and reverses chronic neuropathic pain in mouse CCI models.</p>

<p>MDA7 is a selective agonist of the cannabinoid receptor 2 (CB2), demonstrating an EC50 of 128 nM in human CB2 receptors and 67.4 nM in rat CB2 receptors. The compound exhibits good affinity for CB2 receptors, with Ki values of 422 nM for humans and 238 nM for rats. In rat models, MDA7 shows analgesic activity.</p>

<p>Cicaprost (ZK 96480) is an IP agonist with artery relaxing effects; EC50 is 5.8 nM.</p>

<p>AM8936: potent CB1 agonist, EC50 rCB1=8.6nM/hCB1=1.4nM, Ki rat CB1=0.55nM; potential for CNS, metabolic, pain, glaucoma research.</p>

<p>Befiradol HCl (NLX-112) is a selective 5-HT1A receptor agonist with anxiolytic effects and prevents ATXN3 aggregation.</p>

<p>Pexacerfont (BMS-562086) is a selective antagonist of the corticotropin-releasing factor receptor (IC50: 6.1±0.6 nM for the human CRF1 receptor).</p>

<p>DM-4111, one of the primary monohydroxy metabolites of Tolvaptan, is an effective vasopressin V2 receptor (vasopressin V2 receptor) inhibitor. By inhibiting water reabsorption in renal tubules, it facilitates the excretion of electrolyte-free water. DM-4111 holds potential for research in cardiovascular diseases.</p>

<p>AL 6598, a prodrug of PGD2 agonist AL 6556, reduces IOP by 53% at 1μg twice daily in monkeys; binds DP receptors with Ki of 3.2μM.</p>

<p>UNC10099984A (Compound 6) is a functionally selective ligand for the dopamine D2 receptor, exhibiting a Ki value of 4.6 nM and an EC50 of 6.2 nM for β-arrestin. This compound is useful for research into central nervous system diseases related to the D2 receptor.</p>

<p>MrgprX2 antagonist-7 is an anti-allergic agent with significant anti-allergic effects and inhibits mast cell degranulation.</p>

<p>Revexepride, a 5-HT4 agonist, may boost CYP3A4, used for treating GERD.</p>

<p>TAAR1 agonist 2 (compound 30), a full agonist at trace amine-associated receptor 1 (TAAR1) (pEC50=7.5), also displays agonistic properties at H1 receptors and activates various muscarinic acetylcholine receptors, including the M2 receptor (pEC50=5). This compound is utilized in researching neuropsychiatric diseases.</p>

<p>YM-49598 iodide is a tachykinin NK-1 receptor antagonist. It inhibits drug-induced bladder contractions in rats with an IC50 of 11 μg/kg.</p>

<p>GLP-1 receptoragonist 16 (Example 53) is a GLP-1 agonist applicable for research in diabetes, obesity, or diseases related to non-alcoholic steatohepatitis.</p>

<p>CS-0777 is a potent, selective, and orally active S1P1 agonist (sphingosine 1-phosphate receptor modulator).</p>

<p>inhibitor of human CCR5 binding to HIV-1 gp120</p>

<p>Compound 6.4, also known as 5-HT7R antagonist 3, is a selective antagonist of the 5-HT7R with a Ki of 8 nM. It exhibits significantly less affinity towards D2R, 5-HT1AR, and 5-HT2AR with Ki values of 511 nM, 8930 nM, and 5786 nM, respectively. In mice, 5-HT7R antagonist 3 demonstrates anti-depressant and anti-anxiety activities.</p>

<p>GLP-1R agonist 8 is a potent agonist of GLP-1R (EC50 &lt; 2 nM).</p>

<p>CB1 antagonist 4 is an inverse agonist of cannabinoid receptor 1 (CB1) with an IC50 of 0.4 nM. It can reduce body weight, improve plasma inflammatory markers, and enhance glucose homeostasis [1].</p>

<p>Arpromidine (BU-E-50) acts as an agonist for the histamine H2 receptor and an antagonist for the histamine H1 receptor. It demonstrates positive inotropic effects with a lower risk of inducing arrhythmias. Arpromidine can be utilized in studies related to congestive heart failure.</p>

<p>Compound 23: H3R antagonist with 170 nM Ki; inhibits AChE, BChE, hMAO B; IC50s: 180, 880, 775 nM; anti-pain, memory boost; crosses BBB. [1]</p>

<p>RBM10-8 irreversibly inhibits human sphingosine-1- phosphate lyase (hS1PL) while behaving also as an enzyme substrate.</p>

<p>L 668750 is an inhibitor of platelet-activating factor.</p>

<p>LY 292728 is a highly potent antagonist of leukotriene B4 receptor.</p>

<p>AAZ-A 154 mesylate mesylate is a selective, competitive, and non-hallucinogenic antagonist of 5-HT2AR. It enhances neuronal growth in rodents and produces enduring beneficial behavioral effects.</p>

<p>MRS2279 diammonium, a P2Y1 antagonist with K i 2.5 nM, IC 50 51.6 nM, blocks ADP-induced platelet aggregation, pK b 8.05.</p>

<p>Elzasonan hydrochloride is a serotonin 1B and serotonin 1D receptor antagonist. It is utilized in the study of depression.</p>

<p>2,3-dinor-11β-Prostaglandin F2α (2,3-dinor-11β-PGF2α) was recovered from the urine of both normal monkeys and humans when infused with radiolabeled PGD2, where</p>

SAR-150640, a selective β3-adrenergic receptor agonist, prevents an increase in MMP activity and production observed after LPS stimulation or in cases of chorioamnionitis.

<p>MRT-92 is an antagonist of Smoothened (Smo) with anti-cancer activity, featuring a binding affinity (Ki) of 0.7 nM. It inhibits the Hedgehog signaling pathway by obstructing the overlapping binding sites within the transmembrane domain of the Smoothened receptor and suppresses the proliferation of cerebellar granule cells in rodents (IC50=0.4 nM). MRT-92 is utilized for research into cerebellar gliomas.</p>

<p>CM699 is an effective dual inhibitor of the dopamine transporter (DAT) and Sigma receptor (σR), with IC50 values of 311 nM and 14.1 nM, respectively.</p>

LRH-1 modulator-1: potent agonist, boosts IL-10, reduces IL-1b/TNFa, anti-inflammatory in gut.

<p>GLP-1 Receptor Agonist 11 (compound 3) acts as an effective agonist for the GLP Receptor, finding use in research related to conditions like diabetes and non-alc. fatty liver disease [1].</p>

<p>BMS-986104 is an effective selective modulator of the S1P1 receptor. It demonstrates efficacy in the mouse EAE model, comparable to that of FTY720. Furthermore, BMS-986104 shows promising remyelination properties in three-dimensional brain cell cultures subjected to lysophosphatidylcholine (LPC)-induced demyelination.</p>

<p>KF26777 is a potent and selective antagonist of adenosine A3 receptor.</p>

<p>BMS-741672 is a potent, selective CCR2 antagonist for the treatment of neuropathic pain.</p>

<p>CCR4 antagonist 2 (Compound 31) is a novel potent, orally bioavailable small molecule antagonists of CC chemokine receptor 4 (CCR4) that inhibits Treg</p>

<p>Apafant (WEB 2086) is a PAF antagonist that blocks eosinophil activation and can be used to study experimental allergic conjunctivitis in guinea pigs.</p>

<p>AFP-07 is a highly selective and potent agonist. It was used for the prostacyclin receptor.</p>

<p>DA-302168S is an orally active, selective GLP-1R agonist with an EC50 value of 1.32 nM. It promotes insulin secretion and has a hypoglycemic effect. Additionally, DA-302168S reduces food intake. It primarily activates GLP-1R in humans and monkeys, with minimal effect on GLP-1R in rats, mice, and dogs. DA-302168S can be used for research in type 2 diabetes and obesity.</p>

<p>Substituted piperidines-1 can promote the release of growth hormone in humans and animals.</p>

<p>SGLT1/2-IN-1 is a dual SGLT1/SGLT2 inhibitor.</p>

<p>UR-AK49 (compound 11) is an agonist for the human histamine H1 and H2 receptors. It exhibits an EC50 of 23 nM in the GTPase assay involving hH2R-Gsalpha fusion protein expressed in Sf9 insect cells. UR-AK49 is applicable in neurologically related research.</p>

<p>(E/Z)-Ozagrel (sodium) [(E/Z)-OKY-046 (sodium)] is a mixture of the EZ isomers of Ozagrel (sodium). It acts as a thromboxane A2 (TXA2) synthase inhibitor. As an antiplatelet agent, Ozagrel (sodium) selectively inhibits human platelet aggregation, with an IC50 of 53.12 μM.</p>

<p>SphK2-IN-1 is an SphK2 inhibitor with an IC50 value of 0.359 μM. SphK2-IN-1 can be used to study cancer, inflammation, neurological and cardiovascular diseases.</p>

<p>Ersentilide, a benzamide derivative, functions as both a β1-adrenergic receptor antagonist and an Ikr blocker. It has demonstrated efficacy in animal models of cardiac arrhythmias.</p>

<p>Tipelukast (KCA 757), an oral drug for asthma research, blocks leukotrienes and fights inflammation and fibrosis.</p>

<p>NBI 35965 hydrochloride is a selective CRF1 (corticotropin-releasing factor receptor 1) antagonist that is both orally active and capable of penetrating the brain. It possesses a K i value of 4 nM and a pK i of 8.5, and does not affect CRF2. This compound effectively diminishes CRF or stress-triggered ACTH (adrenocorticotropic hormone) production in vivo, demonstrating pIC 50 values of 7.1 and 6.9. Additionally, NBI 35965 hydrochloride exhibits anxiolytic properties [1] [2].</p>

<p>MRS2179 blocks turkey P2Y1 receptor (Kb 102 nM, pA2 6.99), affects platelet aggregation, and has varying IC50s on P2 receptors.</p>

<p>GRK6-IN-4 is an inhibitor of G protein-coupled receptor kinase 6 (GRK6) with an IC50 value of 1.56 μM. GRK6-IN-4 is applicable for research related to hematological malignancies, inflammatory diseases, and autoimmune disorders.</p>

<p>Selective oral S1P1 agonist 5 inhibits lymphocyte drainage, potential for MS research.</p>

<p>FR-145715 is a histamine H2 receptor antagonist characterized by its specific anti-Helicobacter pylori activity. This compound is utilized in the study of gastric lesions.</p>

<p>Ro 24-4736 is an effective and selective platelet-activating factor antagonist.</p>

<p>Selective, orally active PAR-1 antagonist with an IC50 of 7 nM, potential for cardiovascular disease studies.</p>

<p>SSTR5 antagonist 6, an orally active antagonist specific to the somatostatin receptor subtype 5 (SSTR5), exhibits an IC50 value of 24 nM. This compound is utilized in researching type 2 diabetes [1].</p>

<p>Dinoxyline is a potent dopamine receptor agonist, with dissociation constants (Ki values) for D1, D2, D3, and D4 receptors being 7 nM, 6 nM, 5 nM, and 43 nM, respectively. It is utilized in neuroscience research.</p>

<p>MF-592: EP4 receptor antagonist, hEP4 IC50 3 nM, hWB IC50 78 nM, great oral PK, rat arthritis ED50 0.1 mg/kg/day, promising for development.</p>

<p>TAK-637 is a tachykinin 1 (NK1) receptor antagonist.</p>

<p>SORT1-IN-5 (compound 3) is a SORT1 inhibitor capable of crossing the blood-brain barrier. The MSOH salt form of SORT1-IN-5 exhibits a certain degree of oral bioavailability.</p>

BW A868C is a potent, selective PGD2 antagonist and a BW245C analogue, inert to other prostaglandin receptors.