S2637 |
Fasiglifam(TAK-875) Hemihydrate
|
Fasiglifam(TAK-875) Hemihydrate is a selective GPR40 agonist with EC50 of 14 nM in human GPR40 expressing CHO cell line, 400-fold more potent than oleic acid. |
-
Endocrinology, 2021, 162(3)bqab002
-
Psychopharmacology (Berl), 2021, 10.1007/s00213-021-05837-4
-
Environ Sci Technol, 2020, 54(6):3428-3436
|
|
S8014 |
GW9508
|
GW9508 is a potent and selective agonist for FFA1 (GPR40) with pEC50 of 7.32, 100-fold selective against GPR120, stimulates insulin secretion in a glucose-sensitive manner. |
-
J Enzyme Inhib Med Chem, 2021, 36(1):1651-1658
-
Bioorg Chem, 2020, 99:103830
-
Arch Pharm (Weinheim), 2020, e2000275
|
|
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. |
-
iScience, 2024, 27(3):109125
-
Nutrients, 2023, 16(1)38
-
Chem Biol Interact, 2023, 10.1016/j.cbi.2023.110728
|
|
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. |
-
OPARU, 2023, 10.18725/OPARU-48122
-
Pharmacol Res Perspect, 2022, 10(4):e00993
-
Front Pharmacol, 2021, 12:737637
|
|
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. |
-
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
|
|
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 is a novel GPR119 agonist, showing potential for the treatment of type 2 diabetes. Phase 2. |
-
PLoS One, 2015, 10(7):e0134051
|
|
S7263 |
AZD1981
|
AZD1981 is a potent, selective CRTh2 (DP2) receptor antagonist with IC50 of 4 nM, showing >1000-fold selectivity over more than 340 other enzymes and receptors, including DP1. Phase 2. |
-
Mol Cancer Ther, 2019, 18(11):2097-2110
|
|
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
-
MedComm (2020), 2023, 4(2):e242
-
Antioxidants (Basel), 2023, 12(12)2087
|
|
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
|
|
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 (JNJ28630368) 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. |
|
|
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. |
|
|
E1768New |
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. |
|
|
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. |
|
|
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. |
|
|
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. |
|
|
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. |
|
|
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). |
|
|
S6759 |
TC-G-1008 (GPR39-C3)
|
TC-G-1008 (GPR39-C3) is a potent and orally bioavailable agonist of GPR39 with EC50 of 0.4nM and 0.8nM for rat and human receptor, respectively. |
|
|
E0113New |
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. |
|
|
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. |
|
|
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
|
|
S2822 |
OC000459
|
OC000459 is a potent and selective D prostanoid receptor 2 (DP2) antagonist with IC50 of 13 nM. Phase 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. |
|
|
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
|
|
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. |
|
|
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. |
|
|
E1922New |
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). |
|
|
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. |
- iScience, 2024, 27(3):109125
- Nutrients, 2023, 16(1)38
- Chem Biol Interact, 2023, 10.1016/j.cbi.2023.110728
|
|
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. |
- 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 is a potent, selective CRTh2 (DP2) receptor antagonist with IC50 of 4 nM, showing >1000-fold selectivity over more than 340 other enzymes and receptors, including DP1. Phase 2. |
- Mol Cancer Ther, 2019, 18(11):2097-2110
|
|
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. |
|
|
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. |
|
|
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. |
|
|
E0113New |
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. |
|
|
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
|
|
S2822 |
OC000459
|
OC000459 is a potent and selective D prostanoid receptor 2 (DP2) antagonist with IC50 of 13 nM. Phase 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. |
|
|
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
|
|
S2637 |
Fasiglifam(TAK-875) Hemihydrate
|
Fasiglifam(TAK-875) Hemihydrate is a selective GPR40 agonist with EC50 of 14 nM in human GPR40 expressing CHO cell line, 400-fold more potent than oleic acid. |
- Endocrinology, 2021, 162(3)bqab002
- Psychopharmacology (Berl), 2021, 10.1007/s00213-021-05837-4
- Environ Sci Technol, 2020, 54(6):3428-3436
|
|
S8014 |
GW9508
|
GW9508 is a potent and selective agonist for FFA1 (GPR40) with pEC50 of 7.32, 100-fold selective against GPR120, stimulates insulin secretion in a glucose-sensitive manner. |
- 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. |
- OPARU, 2023, 10.18725/OPARU-48122
- Pharmacol Res Perspect, 2022, 10(4):e00993
- Front Pharmacol, 2021, 12:737637
|
|
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 is a novel GPR119 agonist, showing potential for the treatment of type 2 diabetes. Phase 2. |
- PLoS One, 2015, 10(7):e0134051
|
|
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
- MedComm (2020), 2023, 4(2):e242
- Antioxidants (Basel), 2023, 12(12)2087
|
|
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
|
|
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 (JNJ28630368) is a potent GPR119 agonist with EC50s of 2.7 and 33 nM for human and rat forms, respectively. |
|
|
E1768New |
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. |
|
|
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). |
|
|
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). |
|
|
S6759 |
TC-G-1008 (GPR39-C3)
|
TC-G-1008 (GPR39-C3) is a potent and orally bioavailable agonist of GPR39 with EC50 of 0.4nM and 0.8nM for rat and human receptor, respectively. |
|
|
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. |
|
|
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. |
|
|
E1922New |
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. |
|
|