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...
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 a...
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 ...
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...
HA15 targets specifically BiP/GRP78/HSPA5. HA15 exhibits anti-cancerous activity on all melanoma cells tested, including cells isolated from patients and cells ...
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-fol...
||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, an...
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 ...
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-proli...
||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...
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, respe...
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 action...
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-ca...
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...
||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. |