gpcrs — TargetMol Chemicals

Cat No.	Product Name	Synonyms	Targets
T8642	4-CMTB		GPR
	4-CMTB is a selective agonist of FFA2 and GPR43.It also is a positive allosteric modulator (pEC50=6.38).		GPR
T24850	Takeda103A	CMPD103A,Takeda-103A,Takeda-103-A,CMPD-103A,Takeda 103 A	GRK
	Takeda103A (CMPD103A) is the GRK2-dependent bovine tubulin oxidation effective inhibitor.		GRK
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).		Others
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...		Others
T3306	PF-04418948	PF 04418948,PF04418948	Prostaglandin Receptor
	PF-04418948 is a potent EP2 receptor antagonist (IC50 = 16 nM for human EP2 receptors). Displays over 2000-fold selectivity for EP2 receptors over EP1, EP3, EP4, DP1 amd CRTH2 receptors; exhibits <30% binding at a divers...		Prostaglandin Receptor
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 ...		Potassium Channel
T8720	PRX-07034 hydrochloride	PRX-07034	5-HT Receptor
	PRX-07034 hydrochloride is a selective antagonist of 5-HT6 receptor. It has cognition and memory-enhancing properties and potently decreases food intake and body weight in rodents. PRX-07034 hydrochloride is both a poten...		5-HT Receptor
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 ...		CCR
T29120	VU0029767	VU 0029767,VU-0029767
	VU0029767 is a selective positive allosteric modulator of M1, a member of the muscarinic acetylcholine family of GPCRs (mAChRs). VU0029767 increases potency and efficacy of acetylcholine (ACh) at M1.
T41159	NCT 501 hydrochloride
	NCT 501 hydrochloride is a potent and selective ALDH1A1 inhibitor (IC50 = 40 nM). Exhibits >1000-fold selectivity for ALDH1A1 over ALDH3A1, ALDH1B1, ALDH2, HPGD and HSD17β4. Also selective over a panel of 168 GPCRs. Bloo...
T10281	Alimemazine	Trimeprazine	Others
	Alimemazine (Trimeprazine) is generally used as an antipruritic agent and also a hemagglutinin (HA)-receptor antagonist. Alimemazine also acts as a partial agonist against the histamine H1 receptor (H1R) and other GPCRs.		Others
T39976	MS67
	MS67 is a potent and selective degrader of the WD40 repeat domain protein 5 (WDR5) with a dissociation constant (Kd) of 63 nM. It exhibits no activity against protein methyltransferases, kinases, G-protein-coupled recept...
TP2086	AdTx1
	Selective, high affinity, non-competitive α1A adrenoceptor antagonist (Ki = 0.35 nM). Exhibits no significant activity against a range of other GPCRs, including α2A, β1 and β2 adrenoceptors. Antagonizes effects of phenyl...
T35804	C16 Lactosylceramide (d18:1/16:0)
	C16 Lactosylceramide is an endogenous bioactive sphingolipid. It forms membrane microdomains with Lyn kinase and the αi subunits of inhibitory G protein-coupled receptors (GPCRs), suggesting a role in cell signaling. Pla...
T75708	Argipressin diacetate
	Argipressin (diacetate) (AVP (diacetate), also known as antidiuretic hormone (ADH)), is a nine-amino acid neuropeptide produced by the posterior pituitary gland. It plays a crucial role in maintaining fluid balance, osmo...
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 ...
T37907	DL 175
	Potent and selective GPR84 biased agonist (EC50 = 33 nM). Exhibits no significant activity in a panel of 168 other GPCRs. Exhibits bias for G protein signaling pathways. Induces morphological changes in primary murine bo...
T37131	MS 15203
	Potent and selective GPR171 partial agonist (EC50 = 90 nM; 28% inhibition of forskolin activated adenylyl cyclase activity in rat hypothalamic memebranes). Exhibits minimal binding to a panel of ~70 GPCRs and 10 other re...
T31995	GRC-17536	GRC17536,GRC 17536
	GRC-17536 is an orally available, potent, and selective transient receptor potential anchor protein 1 (TRPA1) inhibitor that has been shown to be highly effective in the treatment of inflammation and neuropathic pain in ...
T68356	AM-3189
	AM-3189 is a potent and selective GPR40 Agonist with minimal CNS penetration, superior pharmacokinetic properties and in vivo efficacy comparable to AMG 837. AM-3189 maintains the in vivo efficacy of AMG 837 while displa...