||Azathioprine, an immunosuppressive agent, inhibits purine synthesis and GTP-binding protein Rac1 activation.
||GW9508 is a potent and selective agonist for FFA1 (GPR40), stimulates insulin secretion in a glucose-sensitive manner.
||MBX-2982 is a selective, orally-available GPR119 agonist, used for the treatment of diabetes.
||6-OAU(GTPL5846; 6-n-octylaminouracil) is a surrogate agonist of GPR84; activates human GPR84 in the presence of Gqi5 chimera in HEK293 cells with an EC50 of 105 nM in the PI assay.
||Palosuran (ACT-058362) is a new potent and specific antagonist of the human UT receptor.
||APD668 is a potent GPR119 agonist with EC50 of 2.7 nM and 33 nM for hGPR119 and ratGPR119, respectively.
||TAK875 is a potent, selective and orally bioavailable GPR40 agonist.
||TAK-875 is a selective GPR40 agonist with EC50 of 14 nM, 400-fold more potent than oleic acid.
||Ramatroban (BAY u3405) is a thromboxane A(2) (TxA(2)) antagonist marketed for allergic rhinitis. It has been used in trials studying the treatment of Asthma.
||Latanoprost is a prostaglandin F2alpha analogue and a prostanoid selective FP receptor agonist with an ocular hypertensive effect.
||OC000459 is a potent and selective D prostanoid receptor 2 (DP2) antagonist (IC50: 13 nM).
||GSK1292263 is a GPR119 agonist and has been investigated for the treatment of DIABETES MELLITUS, TYPE 2.
||JNJ-63533054 is a potent and selective agonist of hGPR139 with an EC50 = 16 nM.
||GSK137647A is a selective FFA4 agonist.
||APD597 is a GPR119 agonist, used in the treatment of type 2 diabetes.
||TUG-891 is a G protein-coupled receptor (GPCR) expressed in intestine, adipocytes, and pro-inflammatory macrophages that is activated by long chain free fatty acids.
||Setipiprant is an orally available, selective CRTH2 antagonist (IC50: 6.0 nM). CRTH2 is a G protein-coupled receptor for prostaglandin (PGD2). PGD2 is produced by the mast cells an
||Fevipiprant is a selective, potent, reversible competitive CRTh2 antagonist.
||AZD1981 is an effective and specific CRTh2 (DP2) receptor antagonist (IC50: 4 nM), showing >1000-fold selectivity over more than 340 other enzymes and receptors, including DP1. AZD
||HA15 targets specifically BiP/GRP78/HSPA5. HA15 exhibits anti-cancerous activity on all melanoma cells tested, including cells isolated from patients and cells that developed resis
||VER-155008 is a potent Hsp70 family inhibitor with IC50 of 0.5 μM, 2.6 μM, and 2.6 μM in cell-free assays for HSP70, HSC70, and GRP78, respectively, >100-fold selectivity over H
||GPR120 receptor agonist
||A potent and selective GPR120 receptor agonist.
||Palosuran hydrochloride 540769-28-6(free base）
||Palosuran is a new potent and specific antagonist of the human UT receptor with an IC50 of 3.6±0.2 nM.
||TC-O 9311 is a potent GPR139 agonist.
||MS21570 as a GPR171 antagonist based on its ability to block,with an IC50 of 220 Nm,that reduces anxiety-like behavior and fear conditioning in mice.
||Grp94 Inhibitor-1 is a potent, selective Grp94 inhibitor (IC50 : 2 nM).
||DC260126 is a small-molecule antagonist of FFA1 (GPR40)
||CAY 10471 is a potent, highly selective CRTH2/DP 2 receptor antagonist. CAY10471 binds to the human CRTH2/DP2, DP1, and TP receptors( Ki values of 0.6, 1200, and >10,000 nM,respect
||3-chloro-5-hydroxy Benzoic Acid (3-chloro-5-hydroxy BA) is an agonist of GPR81 (EC50 : 16 M)
||Benzyl Nicotinate is a agonist of GPR109A receptor and GPR109B receptor
||AMG 837 calcium hydrate
||AMG 837 calcium hydrate is a potent GPR40 agonist(EC50: 13 nM) with highly selective over GPR41, GPR43, and GPR120 (EC50 > 10,000 nM).
||MK-7246 is a potent and specific CRTH2 antagonist (Ki: 2.5 nM).
||MK-6892 is a selective and full agonist for the high-affinity nicotinic acid receptor GPR109A (Ki: 4 nM; GTPγS EC50: 16 nM).
||TUG-770 is a highly potent agonist of free fatty acid receptor 1 (FFA1/GPR40, EC50: 6 nM for hFFA1).
||AM251 is a effective CB1 receptor antagonist (IC50/Ki: 8 /7.49nM) that displays 306-fold selectivity over CB2 receptors; also effective GPR55 agonist (EC50: 39 nM).
||Pamoic acid is the orphan G protein-coupled receptor GPR35 agonist. Pamoic acid activates ERK and beta-arrestin2 and causes antinociceptive activity.
||Tetrahydromagnolol can activate cannabinoid (CB) receptors.
||AR 231453 is a selective and orally available GPR119 agonist,can stimulate β-cell replication and improve islet graft function.
||NF-56-EJ40 is a high-affinity and highly selective antagonist of human SUCNR1 (GPR91) (IC50 of 25 nM).
||Setogepram sodium salt
||Setogepram sodium salt is an orally active GPR40 agonist and is an antagonist or inverse agonist for GPR84, with anti-fibrotic, anti-inflammatory and anti-proliferative actions.
||CRTh2 antagonist 2
||CRTh2 antagonist selective and potent CRTH2 antagonist, IC50≤10 nM. CRTh2 antagonist 2 can be used to study the direction of androgenic alopecia.
||Dihydromunduletone (DHM) is a carotenoid derivative and selective strong adhesion G protein-coupled receptor (aGPCR) (GPR56 and GPR114/ADGRG5) antagonists, does not inhibit GPR110
||AM-1638 is a full agonist of GPR40/FFA1 (EC50: 0.16 μM).
||AM-4668 is a type 2 diabetes GPR40 agonist. For GPR40, in A9 cells (GPR40 IP3 assay) and CHO cells (GPR40 aequorin assay), the EC50s are 3.6 nM and 36 nM, respectively.
||Firuglipel is an orally available and selective agonist of GPR119.
||FTBMT is a selective GPR52 agonist (EC50: 75 nM) and has antipsychotic and procognitive properties.
||G-1 is a nonsteroidal, high-affinity, and selective GPR30 agonist (Ki: 11 nM).
||GLPG0974 is an antagonist of free fatty acid receptor-2 (IC50: 9 nM).
||Setogepram is an orally active GPR40 agonist and is an antagonist or inverse agonist of GPR84,with anti-inflammatory, anti-fibroticand anti-proliferative actions.
||CAY10595 is a potent antagonist of the CRTH2/DP2 receptor (Ki: 10 nM).
||GPR120 Agonist 1
||GPR120 agonist 1 is an effective and selective GPR120 agonist with good anti-diabetes effect and safety, and is a candidate drug.
||GPR40/FFAR1 modulator 1
||GPR40/FFAR1 modulator 1 is an agonist and an allosteric modulator for Gq-coupled free fatty acid receptor 1 (GPR40/FFAR1).
||GPR4 antagonist 1
||GPR4 antagonist 1 is a GPR4 antagonist, with an IC50 of 189 nM.
||NE 52-QQ57 has anti-inflammatory activity. NE 52-QQ57 is a selective, and orally available GPR4 antagonist with an IC50 of 70 nM.
||GPR84 antagonist 8
||GPR84 antagonist 8 is a selective GPR84 antagonist.
||hGPR91 antagonist 1
||HGPR91 antagonist 1 is a potent and selective small molecule hGPR91 antagonist with an IC50 of 7 μM.
||GSK256073 is a selective and orally active GPR109A (G-protein coupled receptor 109A) agonist. GSK256073 also is a long-lasting and non-flushing HCA2 (hydroxy-carboxylic acid recept
||GW-1100 is a selective antagonist of GPR40 (pIC50: 6.9). GW1100 also plays the role of a GPR40 inverse agonist.
||CRTh2 antagonist 1
||CRTh2 antagonist 1 is a CRTh2 antagonist (IC50: 89 nM).
||GPR40 Agonist 2
||GPR40 Agonist 2 is a GPR40 agonist extracted from patent WO2009054479A1. It can be used in the research of diabetes.
||Lysergol has been used as a hypotensive, psychotropic analgesic, and uterus- and intestine-stimulating drug. Lysergol is a clavinet alkaloid isolated from seeds of Ipomoea muricata
||Urotensin II, mouse acetate
||Urotensin II, mouse acetate is an endogenous ligand for the orphan GPR14 or SENR. It is a potent vasoconstrictor.
||Urotensin II, mouse TFA
||Urotensin II, mouse TFA is an endogenous ligand for the orphan GPR14 or SENR. It is a potent vasoconstrictor.
||RTI-13951-33 is an effective and brain-penetrant GPR88 agonist (EC50: 25 nM, in GPR88 cAMP functional assay).
||Cangrelor tetrasodium is a reversible and selective antagonist of platelet P2Y12, with prompt and potent antiplatelet effects.