GPCR/G-Protein

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

MIN-117, a SSRI/5-HT receptor antagonist, is potentially used for the treatment of depression.

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

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.

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

RO5527239 is a potent, orally available GPBAR1 agonist agent.

<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>Dibenamine hydrochloride is a competitive and irreversible blocking agent of the β-adrenergic receptor.</p>

Sonepiprazole (PNU-101387G) is a chemical compound known for its selective antagonistic properties toward D4 dopamine receptors, exhibiting dissociation

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

Phentolamine Analogue 1 is an analogue of phentolamine. Phentolamine is a nonselective antagonist of α-adrenergic.

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].

<p>ATL802 is an adenosine A2B Receptor antagonist.</p>

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

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

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

MK-1421 is a potent and selective sstr3 antagonist.

<p>NH2-UAMC1110 TFA is an aminobutoxy derivative of UAMC1110 used in the synthesis of FAPI-QS. UAMC1110 is a fibroblast activating protein (fap) inhibitor.</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.

Selective, high affinity 5-HT1A receptor antagonist

RP-23618 is a non-peptidic antagonist of RANTES.

<p>FTY720 (S)-Phosphate, an S1P receptor 1 (S1PR1) agonist, is utilized in studying acute inflammatory diseases, including acute lung injury.</p>

Gestonorone Capronate  is a progesterone used in benign prostatic hyperplasia and endometrial cancer studies.

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.

Dersalazine, potential ulcerative colitis drug, inhibits PAF & TNFα, reduces inflammation and MPO activity in rats.

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

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

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

<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>16-phenoxy tetranor PGE2, the free acid form of sulprostone, results from the hydrolysis of the methylsulfonamide bond. It is identified as a minor metabolite in human plasma following the parenteral administration of sulprostone.</p>

CCG-63808 is a reversible inhibitor of regulator of G-protein signaling (RGS) proteins.

<p>CaSR Antagonist-1 is a potent inhibitor of the calcium-sensing receptor (CaSR) with an inhibitory concentration (IC50) of 50 nM, suitable for the investigation</p>

<p>BVFP is a PGRN-SORT1 inhibitor/SORT1 antagonist that binds to key residues 588-593 of PGRN,blocking PGRN-SORT1 binding and having potential for FTLD-TDP.</p>

<p>LAS191859, a CRTH2 antagonist, IC50: 7.6-15.5nM across species, 21h half-life for sustained in vivo effect.</p>

Tafluprost, an analog of prostaglandin F2α (PGF2α) that primarily targets the FP receptor, is employed in glaucoma treatment. Tafluprost (free acid) serves as a potent FP receptor agonist with a Ki value of 0.4 nM. Its derivative, tafluprost ethyl ester, potentially offers enhanced lipid solubility relative to its free acid form, possibly leading to superior tissue absorption and reduced effective concentration requirements.

VCH-286 is a C-C chemokine receptor type 5 (CCR5) receptor antagonist.

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

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

<p>Mocravimod hydrochloride (KRP-203) is an effecitive and orally active agonist of sphingosine 1-phosphate receptor type 1(S1PR1).</p>

Timiperone exhibits a high affinity for cerebral dopamine D2 receptors, demonstrating antipsychotic activity as it mitigates stereotyped behavior.

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

<p>TCS 2510 (CAY10598) 是一种选择性 PGE2 和 EP4 受体激动剂，可增强细胞内 cAMP 浓度和活性 β-caten 的丰度。TCS 2510 抑制TNF-α 产生，可用于研究代谢紊乱带来的疾病。</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).

RU-SKI 43: Potent, selective Hhat inhibitor, IC50 850 nM. Anticancer; potential lung adenocarcinoma treatment. Inhibits Gli-1, Akt, mTOR pathways.

SC-50605 is a second-generation LTB4 receptor antagonist.

SC 51322 is an EP1 prostanoid receptor antagonist.

Flesinoxan is a hypotensive agent and is an effective, high affinity, and selective 5-hydroxytryptamine1A receptor agonist (EC50: 24 nM).

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].

L 743310 is an antagonist of the neurokinin-1 receptor.

<p>Prostaglandin D2 serinol amide serves as a mild inhibitor against the hydrolysis of [3H]2-oleoylglycerol [1].</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>

LY-426965 is a selective, potent, orally bioavailable 5-HT1A antagonist.

<p>5-HT2A&amp;5-HT2C agonist-1 (Example 2) is a dual-acting agent targeting the 5-HT2A and 5-HT2C receptors with respective IC50 values of 196 nM and 0.9 nM.</p>

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

Neladenoson dalanate (BAY-1067197), an oral Adenosine A1 receptor partial agonist, is safe with good pharmacokinetics for chronic heart disease.

NBI 35965 hydrochloride is a CRF1 antagonist.

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

BMS-194449 is a full beta 3 agonist.

CP-96021 hydrochloride is a potent and orally active antagonist of leukotriene D4 (LTD4)/platelet activating factor receptor (Kis: 34 nM and 37 nM).

<p>SKF 81297 is a selective and potent agonist for the dopamine D1 receptor [1].</p>

mPGES1-IN-3 is a potent and selective inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1) .

EP2 receptor agonist 4 selectively activates the EP2 receptor with an efficacy concentration (EC50) of 43 nM [1].

L-772,405 is a highly selective agonists of h5-HT(1D) receptor.

Leukotriene B4 (LTB4)-3-aminopropylamide is an analog of LTB4 that exhibits potent and selective binding to the BLT1 receptor with Ki values of 5.1 nM at BLT1 and 1,227 nM at BLT2, indicating its high affinity for BLT1 over BLT2. This compound's effects are mediated through interactions with two receptors, BLT1 and BLT2.

<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>

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

<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>

(2R,3S)-E1R, an enantiomer of E1R, is a sigma-1 receptor modulator for treating cognitive disorders.

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.

CP-293019 is a potent, selective antagonist of dopamine D4 receptor.

Ro-70-0004 is a selective antagonist of alpha1A-adrenoceptor.

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

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>LY-368975 is a potent and selective inhibitor of the norepinephrine (NE) reuptake site. LY-368975 reduces food consumption in rodents.</p>

Sigma-2 receptor antagonist 1 is an antagonist of the sigma-2 (σ-2) receptor.

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

<p>(+)-Fluprostenol (AL-5848), an analogue of prostaglandin F2 alpha, is a prostaglandin F2α receptor PTGFR agonist and decreases the expression of Oviductal</p>

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

<p>5-HT2C agonist-3 ((+)-19), a selective 5-HT2C agonist (EC 50: 24 nM, Ki: 78 nM), exhibits antipsychotic-like activity by blocking amphetamine-induced</p>

<p>(S)-Bexcaserin (compound 2) serves as a 5-HT2C receptor agonist, presenting research possibilities in obesity and psychiatric disorders [1].</p>

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

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

YM44778 is a NK1-receptor antagonist for treating restless legs syndrome.

GSK494581A is a GPR55 agonist and glycine transporter subtype 1 inhibitor.

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

PF 514273 is a CB1 receptor antagonist.

Thromboxane A2: unstable, leads to thromboxane B2, induces platelet aggregation, causes vasoconstriction.

Domesticine, (-)- is an antagonist of alpha-1D-adrenoceptor.

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

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

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

PSB-10 hydrochloride is a human adenosine A3 receptor antagonist.

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

Casopitant mesylate (GW679769B): Selective, brain-permeable NK1 receptor blocker, oral antiemetic.

<p>SCH 206272 is a potent, orally active antagonist of tachykinin NK(1), NK(2), and NK(3) receptor.</p>

<p>MNI-444 is a PET radiotracer for adenosine 2A receptors.</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.