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. |
|
|
A2657 |
Anti-GPR49 / LGR5 (BNC101)
|
Anti-GPR49 / LGR5 (BNC101) is a human specific monoclonal antibody targeting the GPCR-LGR5. It can be used in the treatment of metastatic colorectal cancer (CRC). MW :150 KD. |
|
|
A2473 |
Anti-GPRC5D
|
Anti-GPRC5D is a specific antibody against G protein-coupled receptor C5 family member D (GPRC5D). |
|
|
A2474 |
Petosemtamab (Anti-GPR49 / LGR5)
|
Petosemtamab (Anti-GPR49 / LGR5) is an monoclonal antibody that targets GPR49/LGR5. It blocks the appearance of metastases and slows the growth of primary tumors in experimental cancer models. Petosemtamab can be used in the research of solid tumors, such as head and neck squamous cell carcinoma (HNSCC), metastatic colorectal cancer (CRC). MW: 145.5 KD. |
|
|
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). |
|
|
A2925 |
Anti-GPR64 / ADGRG2
|
Anti-GPR64 / ADGRG2 is a monoclonal antibody (mAb) against G protein-coupled receptor 64 isoform 4 (anti-GPR64) with potential anti-tumour activity. MW: 146.1. |
|
|
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. |
|
|
A2702 |
Anti-GPR20 (DS-6157)
|
Anti-GPR20 (DS-6157) is a monoclonal antibody directed against the G protein-coupled receptor 20 (GPR20) with potential antineoplastic activity. MW : 150 kD. |
|
|
A2709 |
Anti-GPR44 / PTGDR2 / CD294
|
Anti-GPR44 / PTGDR2 / CD294 is a monoclonal antibody against a transmembrane G-protein-coupled receptor (GPR44, also known as CRTH2, PTGDR2,or CD294) with the potential to treat asthma. MW: 147.66 KD. |
|
|
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. |
|
|