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Search Result

Search Results for " gpcr "

Targets

GPCR19 Others

42

Compounds

4

Natural Products

7

Recombinant Proteins

6

Libraries

Cat No. Product Name Synonyms Targets
T40685L Orphan GPCR SP9155 agonist P550 (mouse, rat) acetate Orphan GPCR SP9155 agonist P550 (mouse, rat) acetate (600171-70-8 Free base) Others
Orphan GPCR SP9155 agonist P550 (mouse, rat) acetate (Orphan GPCR SP9155 agonist P550 ) is a member of the RFamide peptide family with orexigenic effects.
T60074 GPCR agonist-2 4-(Cyclopropylamino)-3-nitrobenzoic acid GPR
GPCR agonist-2 (4-(Cyclopropylamino)-3-nitrobenzoic acid) is an agonist of the orphan human GPCR GPR109B.
T40685 Orphan GPCR SP9155 agonist P550 (mouse, rat) 26RFa (mouse, rat),Orphan GPCR SP9155 agonist P550 (mouse, rat)
Orphan GPCR SP9155 agonist P550 (mouse, rat) (26RFa (mouse, rat)) is an orphan GPCR with an orexigenic effect belonging to the RFamide peptide family. It acts as the cognate ligand for the mouse orphan receptor GPR103, w...
T9407 Rasarfin Others , Ras
Rasarfin inhibits Ras and ARF6.
T9357 Ro 5212773 Epptb Others
Ro 5212773 (Epptb) is a selective TAAR1 antagonist.
T21874 CID 2745687 GPR
CID 2745687 is a GPR35 antagonist that inhibited the effects at human GPR35 of cromolyn disodium and zaprinast, two agonists that share an overlapping binding site.
T8329 AR 231453 GPR
AR 231453 is a selective and orally available GPR119 agonist,can stimulate β-cell replication and improve islet graft function.
T15432 GSK256073 GPR , Others
GSK256073 is an orally active GPR109A agonist. GSK256073 also is a long-lasting and non-flushing HCA2 (hydroxy-carboxylic acid receptor 2) full agonist (pEC50: 7.5). GSK256073 acutely improves glucose homeostasis via inh...
T9146 Ms48107 Benzenemethanol, 2-[4-amino-6-[[(4-phenoxyphenyl)methyl]amino]-1,3,5-triazin-2-yl]-3-fluoro- Others
MS48107 is a potent, selective positive allosteric modulator of G protein-coupled receptor 68 (GPR68), demonstrating specificity for GPR68 over closely related proton GPCRs, neurotransmitter transporters, and hERG ion ch...
T2613 Almorexant ACT 078573 OX Receptor
Almorexant (ACT 078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively.
T6155 Almorexant hydrochloride ACT-078573 hydrochloride,Almorexant HCl OX Receptor
Almorexant hydrochloride (ACT-078573 hydrochloride) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively.
T12684 Radioprotectin-1 5-chloro-2-[4-(1,3-dioxobenzo[de]isoquinolin-2-yl)butylsulfamoyl]benzoic acid LPA Receptor
Radioprotectin-1 is a selective agonist of LPA2 with EC50 of 25 nM for murine LPA2 GPCR and exerts radioprotective and radiomitigative action.
T10363 Arazine N-Acetyl-S-farnesyl-L-cysteine Others
Arazine (N-Acetyl-S-farnesyl-L-cysteine) can be a a substrate for isoprenylcysteine methyltransferase by competing with prenylated G protein or its receptors site. Arazine is a cell-permeable modulator of G protein and G...
T3433 TUG-891 TUG 891,TUG891 GPR
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.
T9162 CID1231538 GPR
CID1231538 is a potent GPR35 antagonist.
T3119 JNJ-63533054 JNJ 63533054 GPR
JNJ-63533054 is a potent and selective agonist of hGPR139 with an EC50 = 16 nM.
T50088 N-phenylthiophene-2-carboximidamide Others
N-phenylthiophene-2-carboximidamide is a thiophene derivative that functions as an inhibitor of protein tyrosine kinases (PTKs) and a ligand for G protein-coupled receptors (GPCRs).
T8423 ML417 Dopamine Receptor , Arrestin
ML417 is a selective and brain penetrant agonist of D3 Dopamine (EC50 : 38 nM).
T10843 CMF019 Apelin receptor
CMF019 is a potent agonist of the Apelin receptor (APJ) with G protein bias. CMF019 binds to APJ (pKis: 8.58, 8.49, and 8.71 for the human, rat, and mouse).
T3360 ZK 756326 ZK756326 2HCl CCR
ZK 756326 is a selective, non-peptide CCR8 chemokine receptor agonist (IC50: 1.8 μM, in human; 2.6 μM, in mouse). Displays no activity at CCR4/5 and CXCR3/4 and shows higher 28-fold selectivity over 26 other GPCRs (less ...
T17243 VU0463271 N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide Potassium Channel
VU0463271 (N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide) is a potent and selective antagonist of the neuronal-specific potassium-chloride cotransporter 2 (KCC2), with an IC50 of 61 nM ...
T24770 SCH-202676 HBr SCH 202676 Hydrobromide,SCH202676 Hydrobromide,SCH-202676 Hydrobromide
SCH-202676 HBr is an allosteric agonist. It also an GPCR antagonist.
T83743 VPM-p15 TFA T1V/F3Phe(4-Me)
VPM-p15, a synthetic peptide agonist targeting the adhesion G protein-coupled receptor (GPCR) G2 (ADGRG2)—an orphan GPCR implicated in male infertility—facilitates cAMP accumulation in HEK293 cells expressing human ADGRG...
T69774 VUF14738
VUF14738 is a robust and fatigue-resistant photoswitchable GPCR antagonist.
T69775 VUF14862
VUF14862 is a robust and fatigue-resistant photoswitchable GPCR antagonist.
T27428 GP-1681 GP 1681,GP1681
GP-1681, a G-protein coupled receptor (GPCR) agonist, is used potentially for the treatment of influenza infection.
T26962 CBP-307 CBP307
CBP-307 is a selective second generation S1P1 (a G-protein coupled receptor -GPCR) modulator.
T73005 PF-07054894
PF-07054894 is a potent antagonist of the CCR6 and a targeted G protein-coupled receptor (GPCR), useful in the research of inflammatory bowel disease.
T63340 CCG-273220
CCG-273220 is a covalent inhibitor of G protein-coupled receptor (GPCR) kinase 5 (GRK5) (IC50: 220 nM).CCG-273220 covalently binds the GRK5 subfamily-specific residue Cys474 and is more selective for GRK5 than GRK2.
T70468 MK-8666
MK-8666 is a partial GPCR agonist that is coordinated with the action of GPR40. MK-8666 has been investigated for treatment of type 2 diabetes mellitus.
T36578 Boc-Lys(Ac)-AMC
Commendamide (N-acyl-3-hydroxypalmitoyl-glycine) is a newly discovered GPCR G2A/GPR132 agonist (EC50=11.8 μM) that isolated from Bacteroides vulgatus. [1] G2A/GPR132 belongs to the guanine nucleotide-binding protein (G p...
TP1279 Neurokinin B (TFA) Neurokinin B TFA
Neurokinin B TFA belongs to the tachykinin family.Neurokinin B binds to a series of GPCR, including neurokinin receptors 1 (NK1R), NK2R, and nk3r, to modulate their biological effects
TP1946 QWF
Tripeptide substance P (SP) antagonist (IC50 = 90 μM). Also inhibits binding of SP to Mas-related GPCR (MRGPR) X2. Inhibits SP-induced IgE-independent degranulation of mast cells in vitro. Inhibits compound 48/80-induced...
T69953 MK-8666 Tris
MK-8666 Tris is a partial GPCR agonist that is coordinated with the action of GPR40. MK-8666 has been investigated for treatment of type 2 diabetes mellitus.
T81683 Neuromedin S (human)
Neuromedin S (human) is a 33-amino acid neuropeptide identified as an endogenous ligand for the orphan G-protein coupled receptor (GPCR) FM-4/TGR-1, acting on the neuromedin U (NMU) receptor 2 (NMUR2) to regulate body we...
T4186 AC-264613 AC264613 Protease-activated Receptor
AC-264613 is an agonist of the GPCR protease-activated receptor 2 (PAR2). AC-264613(AC264613) suppresses interferon regulatory factor 5 and decreases interleukin-12p40 production by lipopolysaccharide-stimulated macropha...
T36550 CAY10535
TPα and TPβ are two isoforms of the human TP receptor, the G protein-coupled receptor (GPCR) that mediates the actions of thromboxane A2 (TXA2). Although their distinct physiological functions have not been fully elucida...
T83926 S-Geranylgeranyl-L-glutathione GGG
S-Geranylgeranyl-L-glutathione acts as a ligand for the orphan G protein-coupled receptor (GPCR) P2RY8, displaying selective affinity by inducing internalization of P2RY8 in preference to the sphingosine-1-phosphate rece...
T83959 CELT-426
CELT-426 is a potent, partially selective fluorescent antagonist of the human D2 dopamine receptor, exhibiting Ki values of 89.3 nM, 194.8 nM, and 263.6 nM for D2, D3, and D4 dopamine receptors, respectively, in radiolig...
T35562 Nat-20(S)-yne
Smoothened (SMO) is a GPCR-like receptor which, with Patched, mediates hedgehog signaling to regulate gene expression through the Gli transcription factors. 20(S)-hydroxy Cholesterol (20(S)-OHC) is an oxysterol which bin...
T83958 CELT-327
CELT-327 is a potent, selective fluorescent hA2B/A3 adenosine receptor antagonist, exhibiting K_i values of 35.6 nM at A2B and 45.7 nM at A3 receptors. It efficiently labels HCT116 cells expressing A2B adenosine receptor...
T77789 Oleoyl-L-alpha-lysophosphatidic acid sodium salt LPA sodium salt
Oleoyl-L-alpha-lysophosphatidic acid sodium salt is an essential cell membrane biosynthetic metabolite that mediates signal transduction by interacting with G protein-coupled receptors (GPCRs) (ie, LPA receptors). It is ...

Compounds

Orphan GPCR SP9155 agonist P550 (mouse, rat) acetate
T40685L
Synonym: Orphan GPCR SP9155 agonist P550 (mouse, rat) acetate (600171-70-8 Free base)
Target: Others
GPCR agonist-2
T60074
Synonym: 4-(Cyclopropylamino)-3-nitrobenzoic acid
Target: GPR
Orphan GPCR SP9155 agonist P550 (mouse, rat)
T40685
Synonym: 26RFa (mouse, rat),Orphan GPCR SP9155 agonist P550 (mouse, rat)
Target:
Rasarfin
T9407
Synonym:
Target: Others, Ras
Ro 5212773
T9357
Synonym: Epptb
Target: Others
CID 2745687
T21874
Synonym:
Target: GPR
AR 231453
T8329
Synonym:
Target: GPR
GSK256073
T15432
Synonym:
Target: GPR, Others
ms48107
T9146
Synonym: Benzenemethanol, 2-[4-amino-6-[[(4-phenoxyphenyl)methyl]amino]-1,3,5-triazin-2-yl]-3-fluoro-
Target: Others
Almorexant
T2613
Synonym: ACT 078573
Target: OX Receptor
Almorexant hydrochloride
T6155
Synonym: ACT-078573 hydrochloride,Almorexant HCl
Target: OX Receptor
Radioprotectin-1
T12684
Synonym: 5-chloro-2-[4-(1,3-dioxobenzo[de]isoquinolin-2-yl)butylsulfamoyl]benzoic acid
Target: LPA Receptor
Arazine
T10363
Synonym: N-Acetyl-S-farnesyl-L-cysteine
Target: Others
TUG-891
T3433
Synonym: TUG 891,TUG891
Target: GPR
CID1231538
T9162
Synonym:
Target: GPR
JNJ-63533054
T3119
Synonym: JNJ 63533054
Target: GPR
N-phenylthiophene-2-carboximidamide
T50088
Synonym:
Target: Others
ML417
T8423
Synonym:
Target: Dopamine Receptor, Arrestin
CMF019
T10843
Synonym:
Target: Apelin receptor
ZK 756326
T3360
Synonym: ZK756326 2HCl
Target: CCR
VU0463271
T17243
Synonym: N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide
Target: Potassium Channel
SCH-202676 HBr
T24770
Synonym: SCH 202676 Hydrobromide,SCH202676 Hydrobromide,SCH-202676 Hydrobromide
Target:
VPM-p15 TFA
T83743
Synonym: T1V/F3Phe(4-Me)
Target:
VUF14738
T69774
Synonym:
Target:
VUF14862
T69775
Synonym:
Target:
GP-1681
T27428
Synonym: GP 1681,GP1681
Target:
CBP-307
T26962
Synonym: CBP307
Target:
PF-07054894
T73005
Synonym:
Target:
CCG-273220
T63340
Synonym:
Target:
MK-8666
T70468
Synonym:
Target:
Boc-Lys(Ac)-AMC
T36578
Synonym:
Target:
Neurokinin B (TFA)
TP1279
Synonym: Neurokinin B TFA
Target:
QWF
TP1946
Synonym:
Target:
MK-8666 Tris
T69953
Synonym:
Target:
Neuromedin S (human)
T81683
Synonym:
Target:
AC-264613
T4186
Synonym: AC264613
Target: Protease-activated Receptor
CAY10535
T36550
Synonym:
Target:
S-Geranylgeranyl-L-glutathione
T83926
Synonym: GGG
Target:
CELT-426
T83959
Synonym:
Target:
Nat-20(S)-yne
T35562
Synonym:
Target:
CELT-327
T83958
Synonym:
Target:
Oleoyl-L-alpha-lysophosphatidic acid sodium salt
T77789
Synonym: LPA sodium salt
Target:
Cat No. Product Name Synonyms Targets
T0853 Adenosine D-Adenosine,Adenine riboside Apoptosis , Nucleoside Antimetabolite/Analog , Endogenous Metabolite , Autophagy
Adenosine (D-Adenosine) is a ribonucleoside comprised of adenine bound to ribose, with vasodilatory, antiarrhythmic and analgesic activities.
T14063 7α,25-Dihydroxycholesterol 7α,25-OHC EBI2/GPR183 , Endogenous Metabolite
7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenous ligand of the orphan GPCR receptor EBI2 (GPR183). 7α, 25-dihydroxycholesterol can serve as a chemokine directing migration of B cel...
TQ0194 Trans-Vaccenic acid TVA,（11E)-octadec-11-enoic acid,11E)-octadec-11-enoic acid Endogenous Metabolite
Trans-Vaccenic acid (TVA) is a naturally occurring trans-fatty acid found in ruminant fats and dairy products that has antitumor activity by regulating CD8+ T cell proliferation through the GPCR-CREB pathway.Trans-Vaccen...
TN5580 Rediocide A
Rediocide A, an insecticide, can inhibit calcium mobilization in Drosophila G-protein- coupled receptors (GPCR)s other than methuselah, it can induce GPCR desensitization and internalization, and such effects are mediate...

Natural Products

Adenosine
T0853
Synonym: D-Adenosine,Adenine riboside
Target: Apoptosis, Nucleoside Antimetabolite/Analog, Endogenous Metabolite, Autophagy
7α,25-Dihydroxycholesterol
T14063
Synonym: 7α,25-OHC
Target: EBI2/GPR183, Endogenous Metabolite
trans-Vaccenic acid
TQ0194
Synonym: TVA,（11E)-octadec-11-enoic acid,11E)-octadec-11-enoic acid
Target: Endogenous Metabolite
Rediocide A
TN5580
Synonym:
Target:

Recombinant Proteins

Species：
Human (7)
Expression System：
HEK293 (4)
Baculovirus-Insect Cells (1)
E. coli (1)
in vitro E. coli expression system (1)
Tag：
His (2)
hFc (2)
C-6His (1)
His,GST (1)
N-terminal 10xHis-tagged (1)
Cat No. Product Name Species Expression System
TMPY-04302 Frizzled 4 Protein, Human, Recombinant (His) Human HEK293
Familial exudative vitreoretinopathy (FEVR) is a hereditary blinding disorder that features defects in retinal vascular development. Mutations in FZD4 are known to cause autosomal dominant exudative vitreoretinopathy (EV...
TMPY-00197 Frizzled 4 Protein, Human, Recombinant (hFc) Human HEK293
Familial exudative vitreoretinopathy (FEVR) is a hereditary blinding disorder that features defects in retinal vascular development. Mutations in FZD4 are known to cause autosomal dominant exudative vitreoretinopathy (EV...
TMPY-04562 GRK2 Protein, Human, Recombinant (His & GST) Human Baculovirus-Insect Cells
G-protein coupled receptor kinase 2 (GRK2), also referred as Adrenergic, beta, receptor kinase 1 (ADRBK1), is a ubiquitous member of the G protein-coupled receptor kinase (GRK) family that appears to play a central, inte...
TMPJ-00983 ARRB1 Protein, Human, Recombinant (His) Human E. coli
β-Arrestin-1 (ARRB1) is a cytoplasmic protein that belongs to the arrestin family. ARRB1 is expressed at high levels in peripheral blood leukocytes and the central nervous system. ARRB1 regulates agonist-mediated G-prote...
TMPY-04207 Motilin Protein, Human, Recombinant (His) Human HEK293
MLN (Motilin) is a Protein Coding gene. 3 alternatively spliced human isoforms have been reported. This gene encodes a small peptide hormone that is secreted by cells of the small intestine to regulate gastrointestinal c...
TMPY-02837 GPR114 Protein, Human, Recombinant (hFc) Human HEK293
GPR114 belongs to the G-protein coupled receptor 2 family. Members of this family share a common molecular architecture which consists of seven transmembrane domains, three extracellular loops, three intracellular loops,...
TMPH-01719 OPRM1 Protein, Human, Recombinant (His) Human in vitro E. coli expression system
Receptor for endogenous opioids such as beta-endorphin and endomorphin. Receptor for natural and synthetic opioids including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphin and methadone. Agonist binding to th...
Cat No. Product Name
L1500 GPCR Compound Library

1940 compounds
A unique collection of 1940 GPCR-active agents for high throughput screening and high content screening for GPCR drug discovery, and new GPCR target identification and research;
L1580 GPCR Compound Library Plus

338 compounds
Well-chosen 338 GPCR targeting compounds with unique structures;
L2600 Neuronal Signaling Compound Library

2540 compounds
A unique collection of 2540 compounds targeting CNS signaling for high throughput screening (HTS) and high content screening (HCS) for new drugs;
L4660 Anti-Nervous System Disease Library

1246 compounds
Well-chosen 1246 compounds with unique structures targeting nervous system;
L2800 Serotonin Receptor-Targeted Compound Library

275 compounds
A unique collection of 275 compounds targeting serotonin receptors for high throughput screening and high content screening;
L7600 Chemokine Inhibitor Library

59 compounds
A unique collection of 59 chemokines or chemokine receptors targeted compounds for high throughput and high content screening;

Libraries

GPCR Compound Library
L1500
Compounds: 1940
GPCR Compound Library Plus
L1580
Compounds: 338
Neuronal Signaling Compound Library
L2600
Compounds: 2540
Anti-Nervous System Disease Library
L4660
Compounds: 1246
Serotonin Receptor-Targeted Compound Library
L2800
Compounds: 275
Chemokine Inhibitor Library
L7600
Compounds: 59
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