Search Result

Pathways Recommended:	GPCR/G Protein

Results for "

GPCR kinase

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Free Fatty Acid Receptor (1) G Protein-coupled Receptor Kinase (GRK) (3) Histone Methyltransferase (1) Lipase (1) Opioid Receptor (1) PI3K (1) Potassium Channel (1) PROTACs (1)
By Research Areas:	Cancer (2) Cardiovascular Disease (4) Inflammation/Immunology (2) Metabolic Disease (1)

Inhibitors & Agonists

Screening Libraries

Targets Recommended: G protein-coupled Bile Acid Receptor 1

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-141796

MS67	Histone Methyltransferase PROTACs	Cancer
MS67 is a potent and selective WD40 repeat domain protein 5 (WDR5) degrader with a K_d of 63 nM. MS67 is inactive against other protein methyltransferases, kinases, GPCRs, ion channels, and transporters. MS67 shows potent acticancer effects .

HY-47573

CCG273441	G Protein-coupled Receptor Kinase (GRK)	Cardiovascular Disease Cancer
CCG273441 is a covalent inhibitor of G protein-coupled receptor (GPCR) kinase 5 (GRK5) with an IC₅₀ value of 3.8 nM. CCG273441 is highly selective to GRK5 over GRK2 (IC₅₀=4.8 μM) by binding Cys474, a GRK5 subfamily-specific residue, as a covalent handle .

HY-139690

CCG258747	Opioid Receptor	Cardiovascular Disease
CCG258747 is a selective GRK2 inhibitor (IC₅₀=18 nM) with high selectivity over GRK1, GRK5, PKA, and ROCK1 (518, 83, >5500, and >550–fold, respectively).CCG258747 also blocks the internalization of the µ-opioid receptor. G protein-coupled receptor (GPCR) kinases (GRKs) are attractive targets for the research of heart failure .

HY-15589

GW9508 5 Publications Verification	Free Fatty Acid Receptor Potassium Channel	Cardiovascular Disease Metabolic Disease Inflammation/Immunology
GW9508 is a potent and selective G protein-coupled receptors FFA1 (GPR40) and GPR120 agonist with pEC₅₀s of 7.32 and 5.46, respectively. GW9508 shows ~100-fold selectivity for GPR40 over GPR120. GW9508 is inactive against other GPCRs, kinases, proteases, integrins and PPARs. GW9508 is a glucose-sensitive insulin secretagogue and an ATP-sensitive potassium (K_ATP) channels opener. Anti-inflammatory and anti-atherosclerotic activities .

HY-123862

LAS195319	PI3K Lipase G Protein-coupled Receptor Kinase (GRK)	Inflammation/Immunology
LAS195319 is an orally active and potent inhibitor against PI3Kδ with an IC₅₀ value of 0.5 nM. LAS195319 is also a highly selective inhibitor against an extensive panel of proteins, lipid kinases and *GPCRs*. LAS195319 causes an inhibition of neutrophil and eosinophil infiltration. LAS195319 is promising for research of respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD) .

HY-150022

GRK5-IN-4 CCG-265328	G Protein-coupled Receptor Kinase (GRK)	Cardiovascular Disease
GRK5-IN-4 (Compound 16d, CCG-265328) is a potent and and selective covalent GRK5 (G protein-coupled receptor kinase 5) inhibitor, with an IC₅₀ of 1.1 μM. GRK5-IN-4 shows 90-fold selectivity over GRK2. GRK5-IN-4 can be used for heart failure research . GRK5-IN-4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Cat. No.	Product Name

HY-L158

Highly Selective Inhibitors Library	4,918 compounds
According to reports, most known kinase inhibitors exert their effects through competitive binding in highly conserved ATP pockets. Although genetic techniques such as RNA interference can inactivate specific genes, most kinases are multi domain proteins, each of which has an independent function. Highly selective inhibitors have higher efficiency than non-selective inhibitors, and the selectivity to the target is at least 100 times higher. Therefore, ensuring the validation of targets with the most selective inhibitors is crucial for a more thorough understanding of the pharmacology of the kinase field. The Highly Selective Inhibitors Library contains 4,918 compounds, covering multiple targets and subtypes, such as GPCR protein family, Ion channel, multiple kinases, etc. The Highly Selective Inhibitors Library is an effective tool for screening different phenotypes

Highly Selective Inhibitors Library

4,918 compounds

According to reports, most known kinase inhibitors exert their effects through competitive binding in highly conserved ATP pockets. Although genetic techniques such as RNA interference can inactivate specific genes, most kinases are multi domain proteins, each of which has an independent function. Highly selective inhibitors have higher efficiency than non-selective inhibitors, and the selectivity to the target is at least 100 times higher. Therefore, ensuring the validation of targets with the most selective inhibitors is crucial for a more thorough understanding of the pharmacology of the kinase field. The Highly Selective Inhibitors Library contains 4,918 compounds, covering multiple targets and subtypes, such as GPCR protein family, Ion channel, multiple kinases, etc. The Highly Selective Inhibitors Library is an effective tool for screening different phenotypes

HY-L099

Targeted Diversity Library	2,312 compounds
MCE Targeted Diversity Library contains 2,312 compounds, covering more than 1000 targets and isoforms, such as GPCRs, Ion channel, variety of kinases, etc. 1-3 compounds with high potency and selectivity were carefully selected for each target and isoform. The bioactivity information of each compound has been clearly reported in the literatures. This library is a concise collection of small molecule compounds with comprehensive target coverage, which can be used for phenotypic screening at low cost.

Targeted Diversity Library

2,312 compounds

MCE Targeted Diversity Library contains 2,312 compounds, covering more than 1000 targets and isoforms, such as GPCRs, Ion channel, variety of kinases, etc. 1-3 compounds with high potency and selectivity were carefully selected for each target and isoform. The bioactivity information of each compound has been clearly reported in the literatures. This library is a concise collection of small molecule compounds with comprehensive target coverage, which can be used for phenotypic screening at low cost.

HY-L159

Highly Selective Activators Library	1,550 compounds
Agonistic drugs activate or stimulate their receptors, triggering responses that increase or decrease cell activity. The highly selective activators can act on specific biological or molecular targets, while non-selective activators may interfere with multiple targets or targets simultaneously. The highly selective activators reduce the likelihood of these non-specific effects by targeting specific targets, making research more precise and reliable. The Highly Selective Activators Library contains 1,550 compounds, covering multiple targets and subtypes, such as GPCR protein family, Ion channel, multiple kinases, etc. The Highly Selective Activators Library is an effective tool for screening different phenotypes.

Highly Selective Activators Library

1,550 compounds

Agonistic drugs activate or stimulate their receptors, triggering responses that increase or decrease cell activity. The highly selective activators can act on specific biological or molecular targets, while non-selective activators may interfere with multiple targets or targets simultaneously. The highly selective activators reduce the likelihood of these non-specific effects by targeting specific targets, making research more precise and reliable. The Highly Selective Activators Library contains 1,550 compounds, covering multiple targets and subtypes, such as GPCR protein family, Ion channel, multiple kinases, etc. The Highly Selective Activators Library is an effective tool for screening different phenotypes.

HY-L028

CNS-Penetrant Compound Library	901 compounds
The blood-brain barrier (BBB) is the complex network of brain microvessels. It protects the brain from the external bloodstream environment and supplies the brain with the required nutrients for normal function. However, blood-brain barrier is also the obstacle to deliver beneﬁcial drugs to treat CNS (central nervous system) diseases or brain tumors, as it has the least permeable capillaries in the entire body due to physical barriers (tight junctions). Therefore, it is crucial to discover drugs which can cross this barrier for the treatment of brain-based diseases, such as Alzheimer’s disease (AD), Parkinson’s disease (PD) and epilepsy. MCE offers a unique collection of 901 compounds with confirmed CNS-Penetrant property. It’s a useful tool for the discovery of drugs used for brain diseases, such as brain tumors, mental disorders, and neurodegenerative diseases.

CNS-Penetrant Compound Library

901 compounds

The blood-brain barrier (BBB) is the complex network of brain microvessels. It protects the brain from the external bloodstream environment and supplies the brain with the required nutrients for normal function. However, blood-brain barrier is also the obstacle to deliver beneﬁcial drugs to treat CNS (central nervous system) diseases or brain tumors, as it has the least permeable capillaries in the entire body due to physical barriers (tight junctions). Therefore, it is crucial to discover drugs which can cross this barrier for the treatment of brain-based diseases, such as Alzheimer’s disease (AD), Parkinson’s disease (PD) and epilepsy.

MCE offers a unique collection of 901 compounds with confirmed CNS-Penetrant property. It’s a useful tool for the discovery of drugs used for brain diseases, such as brain tumors, mental disorders, and neurodegenerative diseases.

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