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. |
|
|
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
|
|
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
|
G-1 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. |
|
|
S2822 |
OC000459
|
OC000459 is a potent and selective D prostanoid receptor 2 (DP2) antagonist with IC50 of 13 nM. Phase 2. |
|
|
S6651 |
G15 (GRB-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. |
-
Steroids, 2021, 177:108935
-
Cell Biochem Funct, 2020, 38(1):38-46
|
|
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). |
|
|
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
|
|
S9477New |
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 Death Differ, 2021, 10.1038/s41418-021-00887-9
|
|
S0001 |
GSK137647A
|
GSK137647A (GSK 137647) is a selective, non-carboxylic agonist of free fatty acid receptor 4 (FFA4/GPR120) with EC50 of 501 nM. |
|
|
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). |
|
|
S0156 |
CID 1375606
|
CID 1375606 (2,4-Dichloro-N-(phenylcarbamoyl)phenylbenzamide) is an orphan G protein-coupled receptor GPR27 agonist. |
|
|
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. |
|
|
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
|
|
S2637 |
Fasiglifam (TAK-875)
|
Fasiglifam (TAK-875) 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
|
|
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. |
|
|
S5400 |
3-chloro-5-hydroxybenzoic Acid
|
3-chloro-5-hydroxybenzoic Acid is a selective agonist of the lactate receptor GPR81. |
|
|
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. |
|
|
S6746 |
APD668
|
APD668 (JNJ28630368) is a potent GPR119 agonist with EC50s of 2.7 and 33 nM for human and rat forms, respectively. |
|
|
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. |
|
|
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. |
-
Aging (Albany NY), 2021, 13(13):17097-17117
|
|
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. |
-
Front Pharmacol, 2021, 12:737637
-
Biomolecules, 2020, 10(10)E1395
|
|
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
|
|
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
|
G-1 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. |
|
|
S2822 |
OC000459
|
OC000459 is a potent and selective D prostanoid receptor 2 (DP2) antagonist with IC50 of 13 nM. Phase 2. |
|
|
S6651 |
G15 (GRB-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. |
- Steroids, 2021, 177:108935
- Cell Biochem Funct, 2020, 38(1):38-46
|
|
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). |
|
|
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
|
|
S9477New |
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 Death Differ, 2021, 10.1038/s41418-021-00887-9
|
|
S0001 |
GSK137647A
|
GSK137647A (GSK 137647) is a selective, non-carboxylic agonist of free fatty acid receptor 4 (FFA4/GPR120) with EC50 of 501 nM. |
|
|
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). |
|
|
S0156 |
CID 1375606
|
CID 1375606 (2,4-Dichloro-N-(phenylcarbamoyl)phenylbenzamide) is an orphan G protein-coupled receptor GPR27 agonist. |
|
|
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. |
|
|
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
|
|
S2637 |
Fasiglifam (TAK-875)
|
Fasiglifam (TAK-875) 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
|
|
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. |
|
|
S5400 |
3-chloro-5-hydroxybenzoic Acid
|
3-chloro-5-hydroxybenzoic Acid is a selective agonist of the lactate receptor GPR81. |
|
|
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. |
|
|
S6746 |
APD668
|
APD668 (JNJ28630368) is a potent GPR119 agonist with EC50s of 2.7 and 33 nM for human and rat forms, respectively. |
|
|
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. |
|
|
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. |
- Aging (Albany NY), 2021, 13(13):17097-17117
|
|
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. |
- Front Pharmacol, 2021, 12:737637
- Biomolecules, 2020, 10(10)E1395
|
|