GPCR/Proteína-G

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

<p>Uridine 5'-diphosphate acts as a P2Y6 receptor agonist, exhibiting an EC50 value of 0.013 μM for the human P2Y6 receptor [1].</p>

<p>4-Thiouridine 5′-triphosphate tetralithium (4-Thio-UTP), a potent P2Y2 and P2Y4 receptor agonist, exhibits EC50 values of 35 nM for hP2Y2 and 350 nM for hP2Y4.</p>

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

<p>GP3269 is a selective, potent, orally active human adenosine kinase (AK) inhibitor (IC50: 11 nM) with anticonvulsant effects in rats.</p>

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

<p>(Rac)-Modipafantis a PAFR antagonist that inhibits PAF-induced aggregation of washed platelets in rabbits.</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>APJ receptor agonist 6 is a potent agonist of the APJ (apelin receptor) (Ki: 0.059 μM). (EC50: 6.22 μM).</p>

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

<p>TC-SP 14 (compound 14) is a potent, orally available S1P1 agonist with EC50 of 0.042 μM; minimal S1P3 binding (EC50 3.47 μM); reduces blood lymphocytes.</p>

<p>TA-1887: Selective SGLT2 inhibitor, treats type 2 diabetes, lowers glucose in high-fat diet mice, boosts UGE, has good pharmacokinetics.</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>Pecavaptan is a vasopressin receptor antagonist.</p>

<p>MK3577 is a glucagon receptor antagonist.</p>

<p>S1P5-selective agonist; less so for S1P1/S1P3; useful for CNS disorders.</p>

<p>Encaleret( JIT-305) is an antagonist of oral calcium-sensing receptor (CaSR), it is used for the treatment of osteoporosis.</p>

<p>NCGC00229600: Allosteric inverse TSHR agonist; blocks TSH and antibody TSHR activation; for Graves' disease research.</p>

<p>Hedgehog IN-2 (Compound 20) functions as an inhibitor of the Hedgehog signaling pathway, exhibiting an IC50 of &lt;0.003 μM in C3H10T1/2 cells [1].</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>Compound 39, or Y1R probe-1, is a fluorescent probe for Neuropeptide Y Y1 Receptor used in cancer research.</p>

<p>Velagliflozin proline hydrate, an oral SGLT2 inhibitor, reduces blood sugar by inhibiting renal glucose reabsorption.</p>

<p>Veldoreotide (DG3173) TFA, a somatostatin analogue, effectively binds to and activates somatostatin receptors (SSTR) 2, 4, and 5. This compound demonstrates a higher efficacy in inhibiting growth hormone (GH) secretion in adenomas than Octreotide, showcasing its potential as a pain modulating agent [1].</p>

<p>Cis-J-113863 is a competitive antagonist for the chemokine receptor 1 (CCR1), demonstrating inhibitory concentration 50 (IC50) values of 0.9 nM for human CCR1 receptors and 5.8 nM for mouse CCR1 receptors, respectively [1].</p>

<p>CCR4 Antagonist 4 (Compound 22) is a potent and selective antagonist of the CC chemokine receptor-4 (CCR4), displaying an IC50 value of 0.02 μM. It also inhibits MDC-mediated chemotaxis and Ca2+ mobilization, with IC50 values of 0.007 μM and 0.003 μM, respectively. This compound is utilized in research on allergic inflammation [1].</p>

<p>ABT-702 hydrochloride effectively inhibits adenosine kinase, exhibiting an IC50 value of 1.7 nM [1] [2].</p>

<p>RXFP1 receptor agonist-4 (Example 268) is an agonist for the RXFP1 receptor, demonstrated to suppress cAMP production in HEK293 cells that stably express the</p>

<p>Dothiepin (Dosulepin; Dothep), an antidepressant with sedative/anxiolytic properties, preferentially inhibits noradrenaline over serotonin uptake, enhancing</p>

<p>DG-041: EP3 receptor antagonist, high affinity (IC50: 4.6 &amp; 8.1 nM), inhibits PGE2 in platelets, blood-brain barrier permeable.</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>PSNCBAM-1 (PSNCBAM 1) is a CB1 receptor negative allosteric modulator (EC50 = 0.1 μM) with hypophagic effects in vivo.</p>

<p>YM348 is an effective and orally active 5-HT2C receptor agonist. YM348 also shows a high affinity for the cloned human 5-HT2C receptor (Ki: 0.89 nM).</p>

<p>Orvepitant maleate, a selective NK-1 receptor antagonist (pKi 10.2), may treat depression and CRC; crosses the blood-brain barrier.</p>

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

<p>JNJ-19567470 is a selective, non-peptide CRF receptor 1 antagonist.</p>

<p>AH13205 is an agonist of EP2 prostanoid receptor.</p>

<p>FR-181877: nonprostanoid PGI2 agonist, ADP-induced platelet aggregation inhibitor (IC50=0.081μM), orally bioavailable (56%), long half-life (4.3h) in rats.</p>

<p>Domesticine, (-)- is an antagonist of alpha-1D-adrenoceptor.</p>

<p>CP-122288: potent, selective 5-HT1B/D/F agonist; inhibits plasma protein extravasation, neurogenic inflammation.</p>

<p>NGD9002 is a novel generation, topology 2 selective corticotropin releasing factor-1 (CRF-1) receptor antagonist agent.</p>

<p>L 662025 is a PAF receptor antagonist.</p>

<p>ASP6432 is an antagonist of type 1 lysophosphatidic acid receptor (LPA1). For human LPA1 and rat LPA1, the IC50s are 11 nM and 30 nM , respectively.</p>

<p>Tedalinab is an effective and selective cannabinoid receptor 2 agonist.</p>

<p>Droxicam (Droxicamum) is a non-steroidal anti-inflammatory compound and can be used for research on the relief of inflammation and pain in musculoskeletal</p>

<p>L 659837 is an antagonist of ANC-2, lactam, and tackykinin.</p>

<p>neuropeptide Y1 receptor antagonist</p>

<p>NTNCB hydrochloride is an antagonist of neuropeptide Y (NPY) Y5 receptor.</p>

<p>CYM50260 is a potent and exquisitely selective agonist of sphingosine-1-phosphate 4 receptor (S1P4-R, EC50= nM) with no activity against S1P1-R, S1P2-R, S1P3-R</p>

<p>Ubrogepant (MK-1602) is an antagonist of calcitonin gene-related peptide receptor that can be used in the acute treatment of migraine studies.</p>

<p>SC-50605 is a second-generation LTB4 receptor antagonist.</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>adenosine A2B receptor antagonist</p>

<p>WLB-89462 (Compound 20c) is a selective σ2 receptor ligand with a K i of 13 nM, exhibiting neuroprotective properties and the ability to ameliorate Aβ peptide-</p>

<p>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.</p>

<p>SB-414796 is a selective antagonist of the dopamine D3 receptor.</p>

<p>Emicerfont is an antagonist of the corticotropin-releasing factor type 1 receptor (IC50: 66 nM).</p>

<p>S1PR-MO-1 is a modulator of sphingosine-1-phosphate receptor and is used to study hyperproliferative inflammatory diseases.</p>

<p>L-749329 is a ligand of ET(A) and ET(B) endothelin receptor.</p>

<p>Mesembrine is an alkaloid, a 5-HT transporter inhibitor (K i 1.4 nM), and inhibits PDE4B (IC50 7.8 μM).</p>

<p>Tianagliflozin, a sodium/glucose cotransporter 2 (SGLT-2) inhibitor, is used potentially for the treatment of type 2 diabetes.</p>

<p>Cipralisant: H3 receptor antagonist (in vivo), agonist (in vitro, pKi 9.9), Ki 0.47 nM in rats, may treat ADHD.</p>

<p>MRS5698, an A3 adenosine receptor agonist with Ki ~3 nM, blocks chronic pain, highly selective (&gt;1000-fold over A1/A2A).</p>

<p>Ebopiprant (OBE022) is a prostaglandin F2α (PGF2α) receptor antagonist that can be used to study obesity.</p>

<p>NBI-34041: High-affinity CRF1 antagonist; reduces endocrine responses to CRF challenges.</p>

<p>L-796568: potent β3 agonist (EC50 = 3.6 nM), &gt;600-fold selectivity vs β1/β2, good oral bioavailability, long action.</p>

<p>Bimatoprost Serinol Amide (Bima SA), a prostaglandin analog, shows research potential for glaucoma [1].</p>

<p>rat 5-HT1B receptor antagonist</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>

<p>Sulmazole (AR-L 115-BS) is a small molecule Sulmazole is a small molecule cGMP-PDE inhibitor.Sulmazole is a competitive inhibitor of A1 adenosine receptors.</p>

<p>Befiradol (NLX-112) is an agonist of 5-HT1A receptor.</p>

<p>SRX246: potent CNS-penetrant V1a antagonist (Ki=0.3 nM), inactive at V1b/V2, negligible binding at 64 other receptor classes.</p>

<p>A-349821 is an H3 receptor agonist radioligand.</p>

NBI 35965 hydrochloride is a CRF1 antagonist.

<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>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>Selective, high affinity 5-HT1A receptor antagonist</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>

<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>MSX-2 is an A2A adenosine receptor antagonist.</p>

<p>MLN-3897 is an oral CCR1 antagonist, Ki 2.3 nM, blocks 125I-MIP-1α binding, and inhibits Akt signaling in MM cells.</p>

<p>E1R is a positive sigma-1 receptor (Sig1R PAM) allosteric modulator. It has a cognition-enhancing activity.</p>

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

<p>Fiboflapon (GSK2190915), an oral 5-lipoxygenase inhibitor, binds FLAP at 2.9 nM, inhibits LTB4 with 76 nM IC50.</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>CAY10508 is a potent and selective inverse agonist for the central cannabinoid (CB1) receptor with therapeutic potential for treating obesity and drug dependence, lacking psychotropic effects. It exhibits a Ki value of 243 nM and an EC50 of 195 nM. At a concentration of 10 µM, CAY10508 displaces [3H]-CP-55,940 with 100% efficacy at the CB1 receptor and 35% at the peripheral cannabinoid (CB2) receptor. Its inverse agonist activity at the CB1 receptor was confirmed through a [35S]-GTPγS binding assay.</p>

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

<p>RP-001 is a selective agonist of picomolar short-acting S1P1 (EDG1)(EC50 of 9 pM), has little activity on S1P2-S1P4 and only moderate affinity for S1P5.</p>

<p>Amtolmetin guacil (ST-679) 抑制前列腺素合成和环氧合酶。 Amtolmetin guacil 具有与托美汀类似的 NSAID 特性，具有额外的镇痛、解热和胃保护特性。</p>

<p>Glucagon receptor antagonist -3 is a highly effective glucagon receptor antagonist.</p>

<p>Compound 8, a cholic acid derivative, functions as a selective TGR5 agonist and exhibits an EC50 value of 5 μM [1].</p>

<p>SCH 206272 is a potent, orally active antagonist of tachykinin NK(1), NK(2), and NK(3) receptor.</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>15(S)-Fluprostenol, an isomer of the FP receptor agonist fluprostenol, serves as a potential active metabolite of 15(S)-fluprostenol isopropyl ester. It can function as an agonist at FP receptors, though with lower potency compared to its 15(R) epimer, fluprostenol.</p>

<p>Robotnikinin is an Shh signaling inhibitor in a concentration-dependent manner. It acts by exhibiting significant repression of Shh-induced Gli1/Gli2.</p>

<p>Carbidine, a gamma-carboline derivative, is an atypical antipsychotic that modulates dopamine release and tyrosine hydroxylase activity.</p>