GPR

GPR製品

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• 新製品

製品コード	製品名称	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S2637	Fasiglifam(TAK-875) Hemihydrate	Fasiglifam(TAK-875) Hemihydrateは、ヒトGPR40発現CHO細胞株においてEC50が14 nMの選択的GPR40アゴニストであり、オレイン酸よりも400倍強力です。	Sci Rep, 2025, 15(1):11403 Endocrinology, 2021, 162(3)bqab002 Psychopharmacology (Berl), 2021, 10.1007/s00213-021-05837-4
S8014	GW9508	GW9508は、FFA1 (GPR40)に対する強力かつ選択的なアゴニストであり、pEC50は7.32です。GPR120に対して100倍選択的で、グルコース感受性方式でインスリン分泌を刺激します。	J Enzyme Inhib Med Chem, 2021, 36(1):1651-1658 Bioorg Chem, 2020, 99:103830 Arch Pharm (Weinheim), 2020, e2000275
S8673	ONC212	ONC212, a fluorinated-ONC201 analogue, is a selective agonist of GPR132. ONC212 is broadly efficacious across most solid tumors and hematological malignancies in the low nanomolar range and has robust anti-leukemic activity.	Mol Oncol, 2025, 10.1002/1878-0261.70081 Oncogenesis, 2025, 14(1):20 Elife, 2024, 12RP91313
S6651	G15	G15 is a cell-permeable high affinity and selective G-protein coupled estrogen receptor 1 (GPER, GPR30) antagonist with an affinity of approximately 20 nM that displays no affinity for ERα and ERβ at concentrations up to 10 μM.	Biol Pharm Bull, 2025, 48(5):657-671 iScience, 2024, 27(3):109125 Nutrients, 2023, 16(1)38
S9477	AH7614	AH7614 (compound 39) is a selective FFA4 (GPR120) antagonist with pIC50s of 7.1 for human FFA4 and 8.1 for mouse FFA4.	Biochem Biophys Res Commun, 2025, 781:152546 Cell Prolif, 2023, e13551. Cell Death Differ, 2021, 10.1038/s41418-021-00887-9
S5400	3-chloro-5-hydroxybenzoic Acid	3-chloro-5-hydroxybenzoic Acid is a selective agonist of the lactate receptor GPR81.	MedComm (2020), 2023, 4(2):e242 Antioxidants (Basel), 2023, 12(12)2087
S0135	JMS-17-2	JMS-17-2 is a potent and selective small-molecule antagonist of CX3C chemokine receptor 1 (CX3CR1/GPR13) with IC50 of 0.32 nM. JMS-17-2 is used in the research of metastatic disease in breast cancer patients.	Int J Oncol, 2022, 60(4)47 Brain Res Bull, 2021, S0361-9230(21)00289-6
S6889	Monomethyl Fumarate	Monomethyl Fumarate (MMF, Monomethylfumarate, Fumaric acid monomethyl ester, Methyl hydrogen fumarate), the active metabolite of the psoriasis drug Fumaderm, is a potent GPR109A agonist. Monomethyl Fumarate prevents major dysfunctions associated with neurodegenerative diseases: oxidative stress, mitochondrial dysfunction, apoptosis and autophagy.	Cell Cycle, 2022, 1-11. Aging (Albany NY), 2021, 13(13):17097-17117
S2149	GSK1292263	GSK1292263は、2型糖尿病治療の可能性を示す新規GPR119アゴニストである。第2相。	PLoS One, 2015, 10(7):e0134051
S7263	AZD1981	AZD1981は、IC50が4 nMの強力で選択的なCRTh2（DP2）受容体拮抗薬であり、DP1を含む340以上の他の酵素や受容体に対して1000倍以上の選択性を示します。第2相。	Mol Cancer Ther, 2019, 18(11):2097-2110
S0080	SNAP94847 hydrochloride	SNAP 94847 hydrochloride is a high affinity and selective antagonist of the MCH1 receptor with an IC50 of 230 nM for rat MCH1 in FLIPR calcium mobility assay.	J Biol Chem, 2025, 301(5):108486
S6759	TC-G-1008 (GPR39-C3)	TC-G-1008 (GPR39-C3) is a potent and orally available G-protein coupled receptor 39 (GPR39)(zinc receptor) agonist with EC50 of 0.4 nM and 0.8 nM for rat and human receptors, respectively.	J Cachexia Sarcopenia Muscle, 2025, 16(2):e13771
S6850	NE 52-QQ57	NE 52-QQ57 is a selective, and orally available antagonist of G-protein coupled receptor 4 (GPR4) with IC50 of 0.07 μM. NE 52-QQ57 effectively blocks GPR4-mediated cAMP accumulation with IC50 of 26.8 nM in HEK293 cells. The antagonism of GPR4 with NE 52-QQ57 significantly inhibits the AGE-induced increased expression of several key inflammatory cytokines and signaling molecules, including tumor necrosis factor-α (TNF-α), interleukin (IL)-1β, IL-6, inducible nitric oxide synthase (iNOS), nitric oxide (NO), cyclooxygenase 2 (COX2), and prostaglandin E2 (PGE2).	Exp Hematol Oncol, 2024, 13(1):13
S0851	G-1 (LNS 8801)	G-1 (LNS 8801) is a nonsteroidal and selective agonist of G protein-coupled receptor 30 (GPR30, G protein-coupled estrogen receptor 1, GPER) with Ki of 11 nM.	iScience, 2024, 27(3):109125
S0208	6-OAU	6-OAU (GTPL5846, 6-n-octylaminouracil) is a surrogate agonist of G protein-coupled receptor 84 (GPR84) that activates human GPR84 in the presence of Gqi5 chimera in HEK293 cells with EC50 of 105 nM in the PI assay. 6-OAU (GTPL5846, 6-n-octylaminouracil) increases [35S]GTPγS incorporated in Sf9 cell membranes expressing human GPR84-Gαi fusion protein with EC50 of 512 nM.	J Orthop Surg Res, 2023, 18(1):3
E2660	Pamoic acid disodium	Pamoic acid disodium, a potent GPR35 agonist with an EC50 value of 79 nM, induces GPR35a internalization and activates ERK1/2 with EC50 values of 22 nM and 65 nM, respectively, also potently recruits β-arrestin2 to GPR35 showing an antinociceptive effect.	Poult Sci, 2025, 104(2):104761
S0001	GSK137647A	GSK137647A (GSK 137647) is a selective, non-carboxylic agonist of free fatty acid receptor 4 (FFA4/GPR120) with EC50 of 501 nM.
S6976	TC-O 9311	TC-O 9311 is a potent orphan G protein-coupled receptor 139 (GPR139) agonist with an EC50 of 39 nM.
S6746	APD668	APD668 is a potent GPR119 agonist with EC50s of 2.7 and 33 nM for human and rat forms, respectively.
E1235	NF-56-EJ40	NF-56-EJ40 is a potent, high-affinity, and highly selective human SUCNR1 (GPR91) antagonist with an IC50 of 25 nM and a Ki of 33 nM, has high affinity for humanized rat SUCNR1 with a Ki value of 17.4 nM.
E7448	[Pyr1]-Apelin-13	[Pyr1]-Apelin-13 is one of the endogenous agonists of the APJ receptor with high binding affinity Kd of 4.5 nM for hAPJ, predominantly found in the myocardium and plasma. It exhibits analgesic effects and improves cardiovascular function, making it a promising candidate for neuropathic pain and heart failure research.
E6509New	AR420626	AR420626 is a selective agonist of FFAR3 (GPR41) with an IC50 of 117 nM, that prevents serotonin-induced circular muscle relaxation ex vivo and defecation in vivo.
S0742	DC260126	DC260126, a small organic antagonist for GPR40 (FFAR1), dose-dependently inhibits GPR40-mediated Ca2+ elevations stimulated by linoleic acid, oleic acid, palmitoleic acid and lauric acid (IC50=6.28, 5.96, 7.07, 4.58 μM, respectively), reduces GTP-loading and ERK1/2 phosphorylation stimulated by linoleic acid in GPR40-CHO cells, suppresses palmitic acid potentiated glucose-stimulated insulin secretion, and negatively regulates GPR40 mRNA expression induced by oleic acid in Min6 cells.
E1768	MEDICA16	MEDICA16 is an inhibitor of ATP-citrate lyase and also acts as an agonist of G protein-coupled receptor 40 (GPR40). It functions to blunt the development of insulin resistance in the JCR:LA-cp rat as well as it is a potent triacylglycerol-lowering agent.
E7046	TRAP-6	TRAP-6 (PAR-1 agonist peptide) is a synthetic hexapeptide (SFLLRN) that acts as a agonist of PAR-1 (protease-activated receptor-1). It also activates GPR15 on T-cells, regulating immune responses by suppressing acute GvHD while maintaining GvT activity.
E4875	Lodoxamide	Lodoxamide (U-42585E free acid) is a potent agonist of GPR35 with an EC50 of 1 nM. It also inhibits eosinophil peroxidase release after IgA activation and reduces eosinophil cationic protein and eosinophil-derived neurotoxin, suggesting direct effects on eosinophils. It is a mast cell stabilizer used to treat asthma, allergic conjunctivitis, and superior limbic keratoconjunctivitis.
E2037	Kisspeptin-10 (human)	Kisspeptin-10, human is a potent vasoconstrictor and inhibitor of angiogenesis, acts as a tumor metastasis suppressor via its receptor GPR54, inducing osteoblast differentiation via NFATc4-mediated BMP2 expression.
E1928New	Azelaprag	Azelaprag (AMG 986) is a potent agonist of apelin receptor (APJ) with an EC50 of 0.32 nM. It exhibits potential and can be used in Heart failure (HF) research.
E0347	AS1269574	AS 1269574, a small-molecule G protein-coupled receptor 119 (GPR119) agonist, has an EC50 of 2.5 μM in HEK293 cells transiently expressing human GPR119 and enhances insulin secretion in the mouse pancreatic β-cell line MIN-6 only under high-glucose (16.8 mM) conditions.
E4773New	NOX-6-18（GPR132-B-160）	NOX-6-18 (GPR132-B-160) is a potent and selective antagonist of GPR132 with an IC50 of 17 nM. It regulates macrophage reprogramming within pancreatic islets, reduces weight gain, and improves glucose metabolism in mice on a high-fat diet.
S0083	DJ-V-159	DJ-V-159 is an agonist for G protein-coupled receptor family C group 6 member A (GPRC6A).
E0377	CLP-3094	CLP-3094, a potent inhibitor targeting the binding function 3 (BF3) site of androgen receptor (AR), inhibits AR transcriptional activity with IC50 of 4 μM, also is a selective, potent GPR142 antagonist.
E7663	O-1602	O-1602 is a potent agonist of G-protein coupled receptor 55 (GPR55). It exhibits anxiolytic and antidepressant effects by preventing Methamphetamine (METH)-induced hippocampal neurogenic damage and neuroinflammation, as well as stress from chronic social defeat.
S0110	APD597	APD-597 (JNJ-38431055) is a potent and selective G protein-coupled receptor 119 (GPR119) agonist with EC50 of 46 nM for hGPR119 and an inhibitor of Cytochrome P450 2C9 (CYP2C9) with IC50 of 5.8 μM. APD-597 (JNJ-38431055) is developed for treating Type 2 diabetes (T2D).
E0113	GPR84 antagonist 8	GPR84 antagonist 8 is an antagonist of GPR84,which abrogates the enhanced inflammatory response mediated by 6-OAU. It has the potential to reduce the inflammatory responses associated with the activation of the GPR84 receptor.
E7690	7α,25-Dihydroxycholesterol	7α,25-Dihydroxycholesterol (7α,25-OHC) is a potent and selective endogenous agonist of the orphan G protein-coupled receptor EBI2 (GPR183). It exhibits high potency in activating EBI2, with an EC50 of 140 pM and a Kd of 450 pM.
S6425	JNJ 63533054	JNJ 63533054 is a potent and selective GPR139 agonist. It specifically activated human GPR139 in the calcium mobilization (EC50 = 16 ± 6 nM) and GTPγS binding (EC50 = 17 ± 4 nM) assays.
E0106	ML401	ML401, a potent chemical probe, selectively antagonizes G-protein coupled receptor 183 (GPR183, EBI2) with an IC50 of 1.03 nM, and displays activity in a chemotaxis assay with IC50 of 6.24 nM.
S0156	CID 1375606	CID 1375606 (2,4-Dichloro-N-(phenylcarbamoyl)phenylbenzamide) is an orphan G protein-coupled receptor GPR27 agonist.
S2822	OC000459	OC000459は、Dプロスタノイド受容体2（DP2）の強力かつ選択的なアンタゴニストであり、IC50は13 nMです。現在フェーズ2。
S0183	NIBR189	NIBR189 is a potent antagonist of the Epstein-Barr virus-induced gene 2 (EBI2, GPR183) receptor with IC50 of 16 nM for binding and 11 nM for function, respectively.
S4709	Latanoprost	Latanoprost (Xalatan, PhXA41) is a prostaglandin F2alpha analogue and a prostanoid selective FP receptor agonist with an ocular hypertensive effect. Latanoprost increases uveoscleral outflow and thereby reduces intraocular pressure.
S2954	4-CMTB	4-CMTB is a selective allosteric agonist of free fatty acid receptor 2(FFA2, GPR43) with pEC50 of 6.38.
E1162New	GLPG0974	GLPG0974 is a potent and selective antagonist of the human free fatty acid receptor 2 (FFA2/GPR43) with an IC50 of 9 nM and also inhibits SCFA‐induced neutrophil activation and migration.
E1922	OX04528	OX04528 (compound 68) is a potent and G-protein-biased agonist of G protein-coupled receptor 84 (GPR84). OX04528 inhibits cAMP production with an EC50 value of 0.00598 nM (5.98 pM), respectively.
S4440	2-Phenylacetamide	2-Phenylacetamide, the main compound isolated from the seeds of Lepidium apetalum Willd (LA) with estrogenic activities, increases the expression of Estrogen receptorα (ERα), ERβ and GPR30 in the uterus and MCF-7 cells.
S3451	PH-064	PH-064 (BIM-46187) is a novel imidazo-pyrazine derivative that inhibits the heterotrimeric G-protein complex effectively. PH-064 (BIM46174) inhibits heterotrimeric G-protein signalling in GPCRsthat mediate cyclic AMP generation (GAs), calcium release (GAq), cancer cell invasion by Wnt-2 frizzled receptors, and high-affinity neurotensin receptors (GAo/i and GAq).
S2637	Fasiglifam(TAK-875) Hemihydrate	Fasiglifam(TAK-875) Hemihydrateは、ヒトGPR40発現CHO細胞株においてEC50が14 nMの選択的GPR40アゴニストであり、オレイン酸よりも400倍強力です。	Sci Rep, 2025, 15(1):11403 Endocrinology, 2021, 162(3)bqab002 Psychopharmacology (Berl), 2021, 10.1007/s00213-021-05837-4
S8014	GW9508	GW9508は、FFA1 (GPR40)に対する強力かつ選択的なアゴニストであり、pEC50は7.32です。GPR120に対して100倍選択的で、グルコース感受性方式でインスリン分泌を刺激します。	J Enzyme Inhib Med Chem, 2021, 36(1):1651-1658 Bioorg Chem, 2020, 99:103830 Arch Pharm (Weinheim), 2020, e2000275
S8673	ONC212	ONC212, a fluorinated-ONC201 analogue, is a selective agonist of GPR132. ONC212 is broadly efficacious across most solid tumors and hematological malignancies in the low nanomolar range and has robust anti-leukemic activity.	Mol Oncol, 2025, 10.1002/1878-0261.70081 Oncogenesis, 2025, 14(1):20 Elife, 2024, 12RP91313
S5400	3-chloro-5-hydroxybenzoic Acid	3-chloro-5-hydroxybenzoic Acid is a selective agonist of the lactate receptor GPR81.	MedComm (2020), 2023, 4(2):e242 Antioxidants (Basel), 2023, 12(12)2087
S6889	Monomethyl Fumarate	Monomethyl Fumarate (MMF, Monomethylfumarate, Fumaric acid monomethyl ester, Methyl hydrogen fumarate), the active metabolite of the psoriasis drug Fumaderm, is a potent GPR109A agonist. Monomethyl Fumarate prevents major dysfunctions associated with neurodegenerative diseases: oxidative stress, mitochondrial dysfunction, apoptosis and autophagy.	Cell Cycle, 2022, 1-11. Aging (Albany NY), 2021, 13(13):17097-17117
S2149	GSK1292263	GSK1292263は、2型糖尿病治療の可能性を示す新規GPR119アゴニストである。第2相。	PLoS One, 2015, 10(7):e0134051
S6759	TC-G-1008 (GPR39-C3)	TC-G-1008 (GPR39-C3) is a potent and orally available G-protein coupled receptor 39 (GPR39)(zinc receptor) agonist with EC50 of 0.4 nM and 0.8 nM for rat and human receptors, respectively.	J Cachexia Sarcopenia Muscle, 2025, 16(2):e13771
S0208	6-OAU	6-OAU (GTPL5846, 6-n-octylaminouracil) is a surrogate agonist of G protein-coupled receptor 84 (GPR84) that activates human GPR84 in the presence of Gqi5 chimera in HEK293 cells with EC50 of 105 nM in the PI assay. 6-OAU (GTPL5846, 6-n-octylaminouracil) increases [35S]GTPγS incorporated in Sf9 cell membranes expressing human GPR84-Gαi fusion protein with EC50 of 512 nM.	J Orthop Surg Res, 2023, 18(1):3
E2660	Pamoic acid disodium	Pamoic acid disodium, a potent GPR35 agonist with an EC50 value of 79 nM, induces GPR35a internalization and activates ERK1/2 with EC50 values of 22 nM and 65 nM, respectively, also potently recruits β-arrestin2 to GPR35 showing an antinociceptive effect.	Poult Sci, 2025, 104(2):104761
S0001	GSK137647A	GSK137647A (GSK 137647) is a selective, non-carboxylic agonist of free fatty acid receptor 4 (FFA4/GPR120) with EC50 of 501 nM.
S6976	TC-O 9311	TC-O 9311 is a potent orphan G protein-coupled receptor 139 (GPR139) agonist with an EC50 of 39 nM.
S6746	APD668	APD668 is a potent GPR119 agonist with EC50s of 2.7 and 33 nM for human and rat forms, respectively.
E6509New	AR420626	AR420626 is a selective agonist of FFAR3 (GPR41) with an IC50 of 117 nM, that prevents serotonin-induced circular muscle relaxation ex vivo and defecation in vivo.
E1768	MEDICA16	MEDICA16 is an inhibitor of ATP-citrate lyase and also acts as an agonist of G protein-coupled receptor 40 (GPR40). It functions to blunt the development of insulin resistance in the JCR:LA-cp rat as well as it is a potent triacylglycerol-lowering agent.
E4875	Lodoxamide	Lodoxamide (U-42585E free acid) is a potent agonist of GPR35 with an EC50 of 1 nM. It also inhibits eosinophil peroxidase release after IgA activation and reduces eosinophil cationic protein and eosinophil-derived neurotoxin, suggesting direct effects on eosinophils. It is a mast cell stabilizer used to treat asthma, allergic conjunctivitis, and superior limbic keratoconjunctivitis.
E1928New	Azelaprag	Azelaprag (AMG 986) is a potent agonist of apelin receptor (APJ) with an EC50 of 0.32 nM. It exhibits potential and can be used in Heart failure (HF) research.
E0347	AS1269574	AS 1269574, a small-molecule G protein-coupled receptor 119 (GPR119) agonist, has an EC50 of 2.5 μM in HEK293 cells transiently expressing human GPR119 and enhances insulin secretion in the mouse pancreatic β-cell line MIN-6 only under high-glucose (16.8 mM) conditions.
S0083	DJ-V-159	DJ-V-159 is an agonist for G protein-coupled receptor family C group 6 member A (GPRC6A).
E7663	O-1602	O-1602 is a potent agonist of G-protein coupled receptor 55 (GPR55). It exhibits anxiolytic and antidepressant effects by preventing Methamphetamine (METH)-induced hippocampal neurogenic damage and neuroinflammation, as well as stress from chronic social defeat.
S0110	APD597	APD-597 (JNJ-38431055) is a potent and selective G protein-coupled receptor 119 (GPR119) agonist with EC50 of 46 nM for hGPR119 and an inhibitor of Cytochrome P450 2C9 (CYP2C9) with IC50 of 5.8 μM. APD-597 (JNJ-38431055) is developed for treating Type 2 diabetes (T2D).
E7690	7α,25-Dihydroxycholesterol	7α,25-Dihydroxycholesterol (7α,25-OHC) is a potent and selective endogenous agonist of the orphan G protein-coupled receptor EBI2 (GPR183). It exhibits high potency in activating EBI2, with an EC50 of 140 pM and a Kd of 450 pM.
S6425	JNJ 63533054	JNJ 63533054 is a potent and selective GPR139 agonist. It specifically activated human GPR139 in the calcium mobilization (EC50 = 16 ± 6 nM) and GTPγS binding (EC50 = 17 ± 4 nM) assays.
S0156	CID 1375606	CID 1375606 (2,4-Dichloro-N-(phenylcarbamoyl)phenylbenzamide) is an orphan G protein-coupled receptor GPR27 agonist.
S4709	Latanoprost	Latanoprost (Xalatan, PhXA41) is a prostaglandin F2alpha analogue and a prostanoid selective FP receptor agonist with an ocular hypertensive effect. Latanoprost increases uveoscleral outflow and thereby reduces intraocular pressure.
S2954	4-CMTB	4-CMTB is a selective allosteric agonist of free fatty acid receptor 2(FFA2, GPR43) with pEC50 of 6.38.
E1922	OX04528	OX04528 (compound 68) is a potent and G-protein-biased agonist of G protein-coupled receptor 84 (GPR84). OX04528 inhibits cAMP production with an EC50 value of 0.00598 nM (5.98 pM), respectively.
E7448	[Pyr1]-Apelin-13	[Pyr1]-Apelin-13 is one of the endogenous agonists of the APJ receptor with high binding affinity Kd of 4.5 nM for hAPJ, predominantly found in the myocardium and plasma. It exhibits analgesic effects and improves cardiovascular function, making it a promising candidate for neuropathic pain and heart failure research.
S3451	PH-064	PH-064 (BIM-46187) is a novel imidazo-pyrazine derivative that inhibits the heterotrimeric G-protein complex effectively. PH-064 (BIM46174) inhibits heterotrimeric G-protein signalling in GPCRsthat mediate cyclic AMP generation (GAs), calcium release (GAq), cancer cell invasion by Wnt-2 frizzled receptors, and high-affinity neurotensin receptors (GAo/i and GAq).
E7046	TRAP-6	TRAP-6 (PAR-1 agonist peptide) is a synthetic hexapeptide (SFLLRN) that acts as a agonist of PAR-1 (protease-activated receptor-1). It also activates GPR15 on T-cells, regulating immune responses by suppressing acute GvHD while maintaining GvT activity.
S4440	2-Phenylacetamide	2-Phenylacetamide, the main compound isolated from the seeds of Lepidium apetalum Willd (LA) with estrogenic activities, increases the expression of Estrogen receptorα (ERα), ERβ and GPR30 in the uterus and MCF-7 cells.
S6651	G15	G15 is a cell-permeable high affinity and selective G-protein coupled estrogen receptor 1 (GPER, GPR30) antagonist with an affinity of approximately 20 nM that displays no affinity for ERα and ERβ at concentrations up to 10 μM.	Biol Pharm Bull, 2025, 48(5):657-671 iScience, 2024, 27(3):109125 Nutrients, 2023, 16(1)38
S9477	AH7614	AH7614 (compound 39) is a selective FFA4 (GPR120) antagonist with pIC50s of 7.1 for human FFA4 and 8.1 for mouse FFA4.	Biochem Biophys Res Commun, 2025, 781:152546 Cell Prolif, 2023, e13551. Cell Death Differ, 2021, 10.1038/s41418-021-00887-9
S0135	JMS-17-2	JMS-17-2 is a potent and selective small-molecule antagonist of CX3C chemokine receptor 1 (CX3CR1/GPR13) with IC50 of 0.32 nM. JMS-17-2 is used in the research of metastatic disease in breast cancer patients.	Int J Oncol, 2022, 60(4)47 Brain Res Bull, 2021, S0361-9230(21)00289-6
S7263	AZD1981	AZD1981は、IC50が4 nMの強力で選択的なCRTh2（DP2）受容体拮抗薬であり、DP1を含む340以上の他の酵素や受容体に対して1000倍以上の選択性を示します。第2相。	Mol Cancer Ther, 2019, 18(11):2097-2110
S0080	SNAP94847 hydrochloride	SNAP 94847 hydrochloride is a high affinity and selective antagonist of the MCH1 receptor with an IC50 of 230 nM for rat MCH1 in FLIPR calcium mobility assay.	J Biol Chem, 2025, 301(5):108486
S6850	NE 52-QQ57	NE 52-QQ57 is a selective, and orally available antagonist of G-protein coupled receptor 4 (GPR4) with IC50 of 0.07 μM. NE 52-QQ57 effectively blocks GPR4-mediated cAMP accumulation with IC50 of 26.8 nM in HEK293 cells. The antagonism of GPR4 with NE 52-QQ57 significantly inhibits the AGE-induced increased expression of several key inflammatory cytokines and signaling molecules, including tumor necrosis factor-α (TNF-α), interleukin (IL)-1β, IL-6, inducible nitric oxide synthase (iNOS), nitric oxide (NO), cyclooxygenase 2 (COX2), and prostaglandin E2 (PGE2).	Exp Hematol Oncol, 2024, 13(1):13
S0851	G-1 (LNS 8801)	G-1 (LNS 8801) is a nonsteroidal and selective agonist of G protein-coupled receptor 30 (GPR30, G protein-coupled estrogen receptor 1, GPER) with Ki of 11 nM.	iScience, 2024, 27(3):109125
E1235	NF-56-EJ40	NF-56-EJ40 is a potent, high-affinity, and highly selective human SUCNR1 (GPR91) antagonist with an IC50 of 25 nM and a Ki of 33 nM, has high affinity for humanized rat SUCNR1 with a Ki value of 17.4 nM.
S0742	DC260126	DC260126, a small organic antagonist for GPR40 (FFAR1), dose-dependently inhibits GPR40-mediated Ca2+ elevations stimulated by linoleic acid, oleic acid, palmitoleic acid and lauric acid (IC50=6.28, 5.96, 7.07, 4.58 μM, respectively), reduces GTP-loading and ERK1/2 phosphorylation stimulated by linoleic acid in GPR40-CHO cells, suppresses palmitic acid potentiated glucose-stimulated insulin secretion, and negatively regulates GPR40 mRNA expression induced by oleic acid in Min6 cells.
E4773New	NOX-6-18（GPR132-B-160）	NOX-6-18 (GPR132-B-160) is a potent and selective antagonist of GPR132 with an IC50 of 17 nM. It regulates macrophage reprogramming within pancreatic islets, reduces weight gain, and improves glucose metabolism in mice on a high-fat diet.
E0377	CLP-3094	CLP-3094, a potent inhibitor targeting the binding function 3 (BF3) site of androgen receptor (AR), inhibits AR transcriptional activity with IC50 of 4 μM, also is a selective, potent GPR142 antagonist.
E0113	GPR84 antagonist 8	GPR84 antagonist 8 is an antagonist of GPR84,which abrogates the enhanced inflammatory response mediated by 6-OAU. It has the potential to reduce the inflammatory responses associated with the activation of the GPR84 receptor.
E0106	ML401	ML401, a potent chemical probe, selectively antagonizes G-protein coupled receptor 183 (GPR183, EBI2) with an IC50 of 1.03 nM, and displays activity in a chemotaxis assay with IC50 of 6.24 nM.
S2822	OC000459	OC000459は、Dプロスタノイド受容体2（DP2）の強力かつ選択的なアンタゴニストであり、IC50は13 nMです。現在フェーズ2。
S0183	NIBR189	NIBR189 is a potent antagonist of the Epstein-Barr virus-induced gene 2 (EBI2, GPR183) receptor with IC50 of 16 nM for binding and 11 nM for function, respectively.
E1162New	GLPG0974	GLPG0974 is a potent and selective antagonist of the human free fatty acid receptor 2 (FFA2/GPR43) with an IC50 of 9 nM and also inhibits SCFA‐induced neutrophil activation and migration.
S2637	Fasiglifam(TAK-875) Hemihydrate	Fasiglifam(TAK-875) Hemihydrateは、ヒトGPR40発現CHO細胞株においてEC50が14 nMの選択的GPR40アゴニストであり、オレイン酸よりも400倍強力です。	Sci Rep, 2025, 15(1):11403 Endocrinology, 2021, 162(3)bqab002 Psychopharmacology (Berl), 2021, 10.1007/s00213-021-05837-4
S8014	GW9508	GW9508は、FFA1 (GPR40)に対する強力かつ選択的なアゴニストであり、pEC50は7.32です。GPR120に対して100倍選択的で、グルコース感受性方式でインスリン分泌を刺激します。	J Enzyme Inhib Med Chem, 2021, 36(1):1651-1658 Bioorg Chem, 2020, 99:103830 Arch Pharm (Weinheim), 2020, e2000275
S8673	ONC212	ONC212, a fluorinated-ONC201 analogue, is a selective agonist of GPR132. ONC212 is broadly efficacious across most solid tumors and hematological malignancies in the low nanomolar range and has robust anti-leukemic activity.	Mol Oncol, 2025, 10.1002/1878-0261.70081 Oncogenesis, 2025, 14(1):20 Elife, 2024, 12RP91313
S5400	3-chloro-5-hydroxybenzoic Acid	3-chloro-5-hydroxybenzoic Acid is a selective agonist of the lactate receptor GPR81.	MedComm (2020), 2023, 4(2):e242 Antioxidants (Basel), 2023, 12(12)2087
S6889	Monomethyl Fumarate	Monomethyl Fumarate (MMF, Monomethylfumarate, Fumaric acid monomethyl ester, Methyl hydrogen fumarate), the active metabolite of the psoriasis drug Fumaderm, is a potent GPR109A agonist. Monomethyl Fumarate prevents major dysfunctions associated with neurodegenerative diseases: oxidative stress, mitochondrial dysfunction, apoptosis and autophagy.	Cell Cycle, 2022, 1-11. Aging (Albany NY), 2021, 13(13):17097-17117
S2149	GSK1292263	GSK1292263は、2型糖尿病治療の可能性を示す新規GPR119アゴニストである。第2相。	PLoS One, 2015, 10(7):e0134051
S6759	TC-G-1008 (GPR39-C3)	TC-G-1008 (GPR39-C3) is a potent and orally available G-protein coupled receptor 39 (GPR39)(zinc receptor) agonist with EC50 of 0.4 nM and 0.8 nM for rat and human receptors, respectively.	J Cachexia Sarcopenia Muscle, 2025, 16(2):e13771
S0208	6-OAU	6-OAU (GTPL5846, 6-n-octylaminouracil) is a surrogate agonist of G protein-coupled receptor 84 (GPR84) that activates human GPR84 in the presence of Gqi5 chimera in HEK293 cells with EC50 of 105 nM in the PI assay. 6-OAU (GTPL5846, 6-n-octylaminouracil) increases [35S]GTPγS incorporated in Sf9 cell membranes expressing human GPR84-Gαi fusion protein with EC50 of 512 nM.	J Orthop Surg Res, 2023, 18(1):3
E2660	Pamoic acid disodium	Pamoic acid disodium, a potent GPR35 agonist with an EC50 value of 79 nM, induces GPR35a internalization and activates ERK1/2 with EC50 values of 22 nM and 65 nM, respectively, also potently recruits β-arrestin2 to GPR35 showing an antinociceptive effect.	Poult Sci, 2025, 104(2):104761
S0001	GSK137647A	GSK137647A (GSK 137647) is a selective, non-carboxylic agonist of free fatty acid receptor 4 (FFA4/GPR120) with EC50 of 501 nM.
S6976	TC-O 9311	TC-O 9311 is a potent orphan G protein-coupled receptor 139 (GPR139) agonist with an EC50 of 39 nM.
S6746	APD668	APD668 is a potent GPR119 agonist with EC50s of 2.7 and 33 nM for human and rat forms, respectively.
E6509New	AR420626	AR420626 is a selective agonist of FFAR3 (GPR41) with an IC50 of 117 nM, that prevents serotonin-induced circular muscle relaxation ex vivo and defecation in vivo.
E1768	MEDICA16	MEDICA16 is an inhibitor of ATP-citrate lyase and also acts as an agonist of G protein-coupled receptor 40 (GPR40). It functions to blunt the development of insulin resistance in the JCR:LA-cp rat as well as it is a potent triacylglycerol-lowering agent.
E4875	Lodoxamide	Lodoxamide (U-42585E free acid) is a potent agonist of GPR35 with an EC50 of 1 nM. It also inhibits eosinophil peroxidase release after IgA activation and reduces eosinophil cationic protein and eosinophil-derived neurotoxin, suggesting direct effects on eosinophils. It is a mast cell stabilizer used to treat asthma, allergic conjunctivitis, and superior limbic keratoconjunctivitis.
E1928New	Azelaprag	Azelaprag (AMG 986) is a potent agonist of apelin receptor (APJ) with an EC50 of 0.32 nM. It exhibits potential and can be used in Heart failure (HF) research.
E0347	AS1269574	AS 1269574, a small-molecule G protein-coupled receptor 119 (GPR119) agonist, has an EC50 of 2.5 μM in HEK293 cells transiently expressing human GPR119 and enhances insulin secretion in the mouse pancreatic β-cell line MIN-6 only under high-glucose (16.8 mM) conditions.
S0083	DJ-V-159	DJ-V-159 is an agonist for G protein-coupled receptor family C group 6 member A (GPRC6A).
E7663	O-1602	O-1602 is a potent agonist of G-protein coupled receptor 55 (GPR55). It exhibits anxiolytic and antidepressant effects by preventing Methamphetamine (METH)-induced hippocampal neurogenic damage and neuroinflammation, as well as stress from chronic social defeat.
S0110	APD597	APD-597 (JNJ-38431055) is a potent and selective G protein-coupled receptor 119 (GPR119) agonist with EC50 of 46 nM for hGPR119 and an inhibitor of Cytochrome P450 2C9 (CYP2C9) with IC50 of 5.8 μM. APD-597 (JNJ-38431055) is developed for treating Type 2 diabetes (T2D).
E7690	7α,25-Dihydroxycholesterol	7α,25-Dihydroxycholesterol (7α,25-OHC) is a potent and selective endogenous agonist of the orphan G protein-coupled receptor EBI2 (GPR183). It exhibits high potency in activating EBI2, with an EC50 of 140 pM and a Kd of 450 pM.
S6425	JNJ 63533054	JNJ 63533054 is a potent and selective GPR139 agonist. It specifically activated human GPR139 in the calcium mobilization (EC50 = 16 ± 6 nM) and GTPγS binding (EC50 = 17 ± 4 nM) assays.
S0156	CID 1375606	CID 1375606 (2,4-Dichloro-N-(phenylcarbamoyl)phenylbenzamide) is an orphan G protein-coupled receptor GPR27 agonist.
S4709	Latanoprost	Latanoprost (Xalatan, PhXA41) is a prostaglandin F2alpha analogue and a prostanoid selective FP receptor agonist with an ocular hypertensive effect. Latanoprost increases uveoscleral outflow and thereby reduces intraocular pressure.
S2954	4-CMTB	4-CMTB is a selective allosteric agonist of free fatty acid receptor 2(FFA2, GPR43) with pEC50 of 6.38.
E1922	OX04528	OX04528 (compound 68) is a potent and G-protein-biased agonist of G protein-coupled receptor 84 (GPR84). OX04528 inhibits cAMP production with an EC50 value of 0.00598 nM (5.98 pM), respectively.
E6509New	AR420626	AR420626 is a selective agonist of FFAR3 (GPR41) with an IC50 of 117 nM, that prevents serotonin-induced circular muscle relaxation ex vivo and defecation in vivo.
E1928New	Azelaprag	Azelaprag (AMG 986) is a potent agonist of apelin receptor (APJ) with an EC50 of 0.32 nM. It exhibits potential and can be used in Heart failure (HF) research.
E4773New	NOX-6-18（GPR132-B-160）	NOX-6-18 (GPR132-B-160) is a potent and selective antagonist of GPR132 with an IC50 of 17 nM. It regulates macrophage reprogramming within pancreatic islets, reduces weight gain, and improves glucose metabolism in mice on a high-fat diet.
E1162New	GLPG0974	GLPG0974 is a potent and selective antagonist of the human free fatty acid receptor 2 (FFA2/GPR43) with an IC50 of 9 nM and also inhibits SCFA‐induced neutrophil activation and migration.
E6509New	AR420626	AR420626 is a selective agonist of FFAR3 (GPR41) with an IC50 of 117 nM, that prevents serotonin-induced circular muscle relaxation ex vivo and defecation in vivo.
E1928New	Azelaprag	Azelaprag (AMG 986) is a potent agonist of apelin receptor (APJ) with an EC50 of 0.32 nM. It exhibits potential and can be used in Heart failure (HF) research.