attractive target

By Targets:	Cholecystokinin Receptor (1) CRM1 (1) NAMPT (1) Opioid Receptor (1) SARS-CoV (5) Separase (1)
By Research Areas:	Cancer (3) Cardiovascular Disease (1) Infection (5) Metabolic Disease (1) Neurological Disease (1)

Targets Recommended: Target Protein Ligand-Linker Conjugates Ligands for Target Protein for PROTAC

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-144776

NAT	NAMPT	Neurological Disease Cancer
NAT is an initial hit of NAMPT activator. NAMPT is the rate-limiting enzyme in the NAD salvage pathway, which makes it an attractive target for the research of many diseases associated with NAD exhaustion such as neurodegenerative diseases .

HY-138084

SIC5-6	Separase	Cancer
SIC5-6 is a potent Separase inhibitor. Separase, a large cysteine protease, involves in chromosome segregation during mitosis and meiosis, DNA damage repair, centrosome disengagement and duplication, spindle stabilization and elongation. Separase is highly overexpressed in many solid cancers, serves as an attractive chemotherapeutic target .

HY-N144101

SARS-CoV MPro-IN-2	SARS-CoV	Infection
SARS-CoV MPro-IN-2 (compound 15) is a potent inhibitor of SARS-CoV-2 M ^pro with an IC₅₀ value of 72.07 nM. The main protease (M ^pro) of the virus as the major enzyme processing viral polyproteins contributes to the replication and transcription of SARS-CoV-2 in host cells, and has been characterized as an attractive target in agent discovery. SARS-CoV MPro-IN-2 has the potential for the research of COVID-19 .

HY-144260

3CPLro-IN-1	SARS-CoV	Infection
3CPLro-IN-1 (compound A17) is a potent and orally active inhibitor of SARS-CoV-2 3CLpro with an IC₅₀ of 5.65 μM. 3-Chymotrypsin-like cysteine protease (3CLpro) is an indispensable protein in viral replication and represents an attractive agent target for fighting COVID-19 .

HY-146384

CRM1 degrader 1	CRM1	Cancer
CRM1 degrader 1 (1l) is a low toxic chromosome region maintenance 1 (CRM1) degrader. CRM1 is the sole nuclear exporter of several tumor suppressor, a growth regulatory protein as an attractive cancer agent target. CRM1 degrader 1 induces the apoptosis in gastric carcinoma and selectively inhibits proliferation of gastric cancer .

HY-144263

3CPLro-IN-2	SARS-CoV	Infection
3CPLro-IN-2 (compound C1) is a potent and orally active inhibitor of SARS-CoV-2 3CLpro with an IC₅₀ and K_i of 1.55 and 6.09 μM, respectively. 3-Chymotrypsin-like cysteine protease (3CLpro) is an indispensable protein in viral replication and represents an attractive agent target for fighting COVID-19 .

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-111313

JNJ-26070109	Cholecystokinin Receptor	Metabolic Disease
JNJ-26070109 is a high-affinity, competitive, orally bioactive, and selective cholecystokinin 2 (CCK2) receptor antagonist with good pharmacokinetic properties, with pK_is of 8.49, 7.99, and 7.70 for human, rat, and dog CCK2 receptors, respectively. The dual function of CCK2 receptors in regulating gastric acid secretion and growth of the gastrointestinal mucosa make this an attractive and novel target for the research of gastroesophageal reflux disease .

HY-145276

SARS-CoV-2-IN-10	SARS-CoV	Infection
SARS-CoV-2-IN-10 is a potent and nontoxic inhibitor of SARS-CoV-2 3CL protease (3CLpro) with an IC₅₀ and EC₅₀ of 0.13 and 1.03 nM, respectively. SARS-CoV-2 3C-like protease (3CLpro), an enzyme essential for viral replication, is an attractive target for intervention. SARS-CoV-2-IN-11 may lead to the emergence of effective SARS-CoV-2-specific antivirals .

HY-145277

SARS-CoV-2-IN-11	SARS-CoV	Infection
SARS-CoV-2-IN-11 is a potent and nontoxic inhibitor of SARS-CoV-2 3CL protease (3CLpro) with an IC₅₀ and EC₅₀ of 0.17 and 1.45 nM, respectively. SARS-CoV-2 3C-like protease (3CLpro), an enzyme essential for viral replication, is an attractive target for intervention. SARS-CoV-2-IN-11 may lead to the emergence of effective SARS-CoV-2-specific antivirals .

Cat. No.	Product Name

HY-L006

GPCR/G Protein Compound Library	2286 compounds
GPCRs are a large family of cell surface receptors that respond to a variety of external signals. Binding of a signaling molecule to a GPCR results in G protein activation, which in turn triggers the production of any number of second messengers. GPCRs play an important role in the human body, and increased understanding of these receptors has greatly affected modern medicine. In fact, researchers estimate that between one-third to one-half of all approved drugs act by binding to GPCRs. GPCRs are a large group of drug targets in drug discovery. MCE provides a unique collection of 2286 small molecules targeting GPCRs that can be used in the screening for various GPCRs-related research and drug development projects.

GPCR/G Protein Compound Library

2286 compounds

GPCRs are a large family of cell surface receptors that respond to a variety of external signals. Binding of a signaling molecule to a GPCR results in G protein activation, which in turn triggers the production of any number of second messengers. GPCRs play an important role in the human body, and increased understanding of these receptors has greatly affected modern medicine. In fact, researchers estimate that between one-third to one-half of all approved drugs act by binding to GPCRs. GPCRs are a large group of drug targets in drug discovery.

MCE provides a unique collection of 2286 small molecules targeting GPCRs that can be used in the screening for various GPCRs-related research and drug development projects.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N144101

SARS-CoV MPro-IN-2	Infection Quinones Classification of Application Fields Source classification Plants Lithospermum canescens Lehm. Naphthalene Quinones Disease Research Fields Boraginaceae	SARS-CoV
SARS-CoV MPro-IN-2 (compound 15) is a potent inhibitor of SARS-CoV-2 M ^pro with an IC₅₀ value of 72.07 nM. The main protease (M ^pro) of the virus as the major enzyme processing viral polyproteins contributes to the replication and transcription of SARS-CoV-2 in host cells, and has been characterized as an attractive target in agent discovery. SARS-CoV MPro-IN-2 has the potential for the research of COVID-19 .

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