GPCR/G-Protein

<p>RS 67333 hydrochloride is a selective 5-HT4R partial agonist (pKi=8.7) with neuroprotective properties for Alzheimer's research.</p>

<p>Ex26 (S1P1-IN-Ex26) is an S1P1 antagonist used in experimental autoimmune encephalomyelitis, atherosclerosis, and gastric cancer.</p>

Masilukast(MCC-847) is an oral leukotriene D4 (LTD4) receptor antagonist for the study of diseases associated with inflammation.

Pavinetant (MLE-4901) is an orally available neurokinin-3 receptor (NK3R) antagonist used to improve menopausal symptoms.

<p>Felcisetrag (TD-8954), an oral 5-HT4 agonist with GI prokinetic effects, has a high affinity (pKi 9.4) for h5-HT4(c) receptors.</p>

CP 316311 is a specific CRF1 receptor antagonist with potential antidepressant activity and may be used in the study of depression.

<p>Agomelatine HCl is a MT1/MT2 receptor agonist (Ki: 0.1-0.27 nM) and a 5-HT2C antagonist (pKi: 6.2-6.4).</p>

Antalarmin hydrochloride, a CRF1 antagonist, offers anti-inflammatory benefits and prevents stress ulcers in IBS.

<p>N-[(4-Aminophenyl)methyl]adenosine is an adenosine receptor inhibitor (Ki: 29 nM for Rat ecto-5′-Nucleotidase).</p>

<p>Ordopidine (ACR325) is a dopaminergic stabilizer that suppresses psychostimulant-induced hyperactivity disorder and stimulates behavior during inactivity.</p>

<p>Rafabegron (TAK677) is a potent and selective β3 adrenergic receptor agonist for the study of diabetes and obesity.</p>

2'-MeCCPA is an A1AR agonist that inhibits trichothecene-stimulated adenylate cyclase activity and has analgesic activity for the study of HCV.

GR 46611 is a selective 5-HT1B and 5-HT1D receptor agonist and can be used in studies about the treatment of epilepsy.

<p>Terbogrel is an antiplatelet drug, blocking thromboxane A2 receptor/synthase. Helps prevent clots.</p>

<p>YIL 781 is a selective ghrelin receptor antagonist (GHS-R1a) (Ki = 17 nM), showing a weak affinity for kinesin receptors (K = 6 μM).</p>

<p>CB2R PAM, an oral drug, boosts CB2 receptor response to specific agonists, showing potential in neuropathic pain relief.</p>

<p>PNU-282987 is an α7 nAChR agonist (EC50=154 nM) and a 5-HT3 antagonist (IC50=4541 nM) for nervous system research.</p>

<p>H-9 dihydrochloride: Strong PKA inhibitor, curbs 5-HT response and EGF signaling, affects pharyngeal function.</p>

<p>Sarizotan HCl (EMD 128130 HCl) is a 5-HT1A receptor and dopamine receptor agonist and an hERG channel inhibitor used in Parkinson;s disease research.</p>

<p>BMS-960 is an S1P agonist with potential anti-tumour activity for cancer research.</p>

<p>RS 17053 hydrochloride: selective α1A adrenoceptor antagonist, pKi 9.1, pA2 9.8.</p>

<p>Ebrotidine (FI3542) is a competitive H2-receptor antagonist with Ki of 127.5 nM. Ebrotidine has a potent antisecretory activity and evidenced gastroprotection.</p>

<p>TM-N1324 is a GPR39 agonist; 280 nM potency without Zn2+, 9 nM with; similar effects on murine GPR39 (EC50s: 180 nM/5 nM).</p>

<p>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.</p>

<p>Macimorelin acetate (EP-1572) is an oral GHSR agonist for AGHD and CACS research.</p>

<p>RXFP1 receptor agonist-3 (Example 223) is an agonist of the RXFP1 receptor that inhibits cyclic AMP (cAMP) production in HEK293 cells stably expressing human</p>

<p>Compound 39, or Y1R probe-1, is a fluorescent probe for Neuropeptide Y Y1 Receptor used in cancer research.</p>

<p>RXFP1 receptor agonist-7 (Example 2) serves as an RXFP1 receptor agonist, effectively inhibiting cAMP production in HEK293 cells that stably express the human</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>Heptadecanoyl ethanolamide, an endogenous cannabinoid, serves as a synthetic analog of PEA, featuring an odd-numbered (17-carbon) fatty acid chain [1].</p>

<p>Orexin antagonist 4: potent, selective for OX2R (IC50=4.27 nM); less for OX1R (IC50=295 nM).</p>

<p>Cenerimod (ACT-334441) is an S1P1 agonist used in the study of murine experimental autoimmune encephalomyelitis (EAE) and murine scleroderma.</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>EP4 antagonist 1: inhibits human/mouse EP4 receptors (IC50: 6.1/16.2 nM), selective over EP1-EP3 (&gt;10 μM). For cancer immunotherapy.</p>

<p>LY3154885 is an orally active dopamine D1 receptor orthosteric modulator (PAM) that reduces the risk of drug-drug interactions (DDI).</p>

<p>SC 34301 (Enisoprost), a strong oral PGE1 analog, decreases bacterial translocation and increases burned mice survival.</p>

<p>(R)-Casopitant ((R)-GW679769), an NK1-receptor antagonist, is used in chemotherapy-induced nausea research.</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>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>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>S1P5-selective agonist; less so for S1P1/S1P3; useful for CNS disorders.</p>

<p>PD 165929 is a selective antagonist of Bombesin BB1.</p>

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

Todralazine hydrochloride, a β2AR blocker with antioxidant properties, is used in hypertension studies.

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

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

<p>Satigrel is a new antiplatelet agent. It also inhibits platelet accumulation in prosthetic arterial grafts.</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>Cipralisant maleate is a potent, selective Histamine H3 receptor antagonist.</p>

<p>Potent oral APJ agonist (EC 50:0.4 nM); improves cardiac function in HF, with good pharmacokinetics and safety.</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>Neladenoson dalanate (BAY-1067197), an oral Adenosine A1 receptor partial agonist, is safe with good pharmacokinetics for chronic heart disease.</p>

<p>Vemtoberant is a β3 adrenergic antagonist used in β3-related disorder research like heart failure.</p>

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

FAUC-312 is a potent and selective agonist of the dopamine D4 receptor.

<p>(Rac)-Modipafantis a PAFR antagonist that inhibits PAF-induced aggregation of washed platelets in rabbits.</p>

<p>NAS-181 is a potent and selective rat 5-hydroxytryptamine 1B (r5-HT1B) antagonist (Ki: 47 nM).NAS-181 enhances the accumulation of 5-HTP in rat brain regions.</p>

<p>IWP-051: potent oral sGC stimulator, &gt;99% protein bound, stable, permeable, no Caco-2 efflux, potential for daily dose.</p>

<p>GLP-1R agonist 9 acts as a GLP-1R agonist, demonstrating efficacy with EC50 values of 1.1 nM and 11 nM against CHO GLP-1R Clone H6 and Clone C6, respectively.</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>

CCG-63802 is a reversible small-molecule inhibitor of regulator of G protein signaling (RGS) proteins.

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

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

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

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

<p>SC 51322 is an EP1 prostanoid receptor antagonist.</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>4-Chloro-L-phenalanine (L-PCPA) is an inhibitor of 5-HT biosynthesis and a non-specific antagonist of tryptophan hydroxylases (TPH1 and TPH2).</p>

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

<p>GLP-1 receptor agonist 3 is a GLP-1 receptor agonist,Example 4A-1, has EC50s of 1.1 nM and 13 nM in Clone H6 and Clone C6 cell lines assay, respectively.</p>

<p>R-96544 is an orally active antagonist of the 5-HT2A receptor that has demonstrated the ability to inhibit platelet aggregation in vitro [1].</p>

<p>Dansyl-NECA is a selective agonist of fluorescent adenosine A1 receptor.</p>

<p>2-Thio-UTP tetrasodium, a potent agonist for P2Y2, P2Y4, and P2Y6 receptors, serves as a crucial compound in cancer research [1].</p>

<p>Quinotolast sodium inhibits histamine, LTC4 and PGD2 release in a concentration-dependent manner in the concentration range of 1-100 μg/mL.</p>

Foropafant (SR27417) is a highly potent and selective platelet-activating factor (PAF) receptor antagonist (Ki: 57 pM).

<p>11(Z),14(Z)-Eicosadienoic acid is an unsaturated fatty acid and metabolite that inhibits the binding of [3H]LTB4 to neutrophil modules (Ki=3 μm).</p>

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

<p>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].</p>

Fiduxosin is a selective and potent α1-adrenoceptor antagonist with inhibitory effects on α1a-adrenoceptor, α1b-adrenoceptor and α1d-adrenoceptor, with Ki

<p>Wf-516 is a 5-HT reuptake inhibitor (Kis: 5 nM and 40 nM for 5-HT1A receptor and 5-HT2A receptor in humans, respectively), and with potent antidepressant</p>

<p>Pentiapine (CGS 10746) is a novel inhibitor of dopamine release.</p>

<p>(-)-Isoproterenol hydrochloride is used as a β-adrenergic receptor agonist in the treatment of bradycardia and as a bronchodilator.</p>

<p>15(R)-Prostaglandin D2 functions as a DP(2) receptor (Prostaglandin Receptor) agonist with potential roles in prostatic hormone signaling and exhibits anti-inflammatory properties. It enhances actin polymerization in human eosinophils and elevates cAMP levels in platelets [1].</p>

<p>PSB-1114 tetrasodium, a stable P2Y2 agonist (EC50: 134 nM), is &gt;50x more selective over P2Y4 and P2Y6.</p>

<p>AGN 192836 is a potent and selective α2 adrenergic agonist (EC50s: 8.7, 41 and 6.6 nM for α2A, α2B and α2C receptor).</p>

<p>Trans-J-113863 serves as a potent antagonist of chemokine receptors CCR1 and CCR3, effectively inhibiting MIP-1α-induced chemotaxis in CCR1 transfectants and eotaxin-induced chemotaxis in CCR3 transfectants, with respective half-maximal inhibitory concentrations (IC50) of 9.57 nM and 93.8 nM [1] [2].</p>

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

<p>RXFP1 receptor agonist-5 (Example 98) is an agonist that targets the RXFP1 receptor and demonstrates its bioactivity by inhibiting cAMP production in HEK293</p>

NKP608 is a NK-1 receptor antagonist with anticancer and anxiolytic activities.

<p>Bufuralol hydrochloride is a potent, non-selective, orally active β-blocker with partial agonist effects and a CYP2D6 probe.</p>

<p>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 &gt;100,000, 38,000, and 3.1 nM for the EP2, EP3, and EP4 receptors, respectively [1].</p>

<p>Firazorexton hydrate (TAK-994) is a brain-penetrant and orally active agonist of the orexin type 2 receptor (OX2R) with a potent EC50 of 19 nM.</p>

Selective, high affinity 5-HT1A receptor antagonist

<p>CP-96486 is a potent and orally active antagonist of leukotriene D4 (LTD4)/platelet activating factor (PAF) receptor (Kis: 20 and 24 nM).</p>

<p>UWA-101 hydrochloride is a selective, non-cytotoxic inhibitor of DAT/SERT, demonstrating EC50 values of 3.6 µM for DAT and 2.3 µM for SERT inhibition. It mitigates motor disorders and other side effects associated with dopaminergic agent use (e.g., L-DOPA) without exhibiting psychotropic effects. This compound is utilized in research focused on neurodegenerative conditions like Parkinson's disease [1] [2].</p>

<p>Obestatin(rat) TFA, a 23-amino-acid peptide, modulates appetite, gut motility, and body weight; binds GPR39; has anti-inflammatory and antioxidant effects.</p>

<p>RXFP1 receptor agonist-1 (Example 2), an agonist of the RXFP1 receptor, suppresses cAMP production in HEK293 cells that constitutively express the human RXFP1,</p>