||TAK875 is a potent, selective and orally bioavailable GPR40 agonist.
||GSK1292263 is a GPR119 agonist and has been investigated for the treatment of DIABETES MELLITUS, TYPE 2.
||MBX-2982 is a selective, orally-available GPR119 agonist, used for the treatment of diabetes.
||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 HSP90.
||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.
||GPR120 receptor agonist
||A potent and selective GPR120 receptor agonist.
||Latanoprost is a prostaglandin F2alpha analogue and a prostanoid selective FP receptor agonist with an ocular hypertensive effect.
||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.
||TAK-875 is a selective GPR40 agonist with EC50 of 14 nM, 400-fold more potent than oleic acid.
||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 resistance to BRAF inhibitors.
||JNJ-63533054 is a potent and selective agonist of hGPR139 with an EC50 = 16 nM.
||GSK137647A is a selective FFA4 agonist.
||Azathioprine, an immunosuppressive agent, inhibits purine synthesis and GTP-binding protein Rac1 activation.
||ACT 058362; Palosuran
||Palosuran (ACT-058362) is a new potent and specific antagonist of the human UT receptor.
||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. AZD1981 has been used in trials studying the treatment and basic science of Asthma, Postmenopausal, Pharmakokinetic, Asthma
||APD668 is a potent GPR119 agonist with EC50 of 2.7 nM and 33 nM for hGPR119 and ratGPR119, respectively.
||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.
||OC000459 is a potent and selective D prostanoid receptor 2 (DP2) antagonist (IC50: 13 nM).
||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 and is a key mediator in various inflammatory diseases, including allergy and asthma. Binding of PGD2 to CRTH2, which are
||Fevipiprant is a selective, potent, reversible competitive CRTh2 antagonist.
||GW9508 is a potent and selective agonist for FFA1 (GPR40), stimulates insulin secretion in a glucose-sensitive manner.
||APD597 is a GPR119 agonist, used in the treatment of type 2 diabetes.