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Results for "

Clinical efficacy

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5 alpha Reductase (1) 5-HT Receptor (1) Acetyl-CoA synthetase (1) Adrenergic Receptor (2) Akt (1) Amyloid-β (2) Androgen Receptor (1) Antibiotic (2) Bacterial (1) Dengue Virus (1) Dopamine Receptor (1) Endogenous Metabolite (1) Flavivirus (1) Histamine Receptor (1) HIV (1) LPL Receptor (1) mGluR (1) Monoamine Transporter (1) nAChR (1) Parasite (3) PPAR (1) Reactive Oxygen Species (ROS) (1) Reverse Transcriptase (1) Ser/Thr Protease (1) TrxR (1) Virus Protease (1) γ-secretase (2)
By Research Areas:	Cancer (2) Endocrinology (2) Infection (7) Inflammation/Immunology (1) Metabolic Disease (3) Neurological Disease (2)

By Targets:

5 alpha Reductase (1)

5-HT Receptor (1)

Acetyl-CoA synthetase (1)

Adrenergic Receptor (2)

Akt (1)

Amyloid-β (2)

Androgen Receptor (1)

Antibiotic (2)

Bacterial (1)

Dengue Virus (1)

Dopamine Receptor (1)

Endogenous Metabolite (1)

Flavivirus (1)

Histamine Receptor (1)

HIV (1)

LPL Receptor (1)

mGluR (1)

Monoamine Transporter (1)

nAChR (1)

Parasite (3)

PPAR (1)

Reactive Oxygen Species (ROS) (1)

Reverse Transcriptase (1)

Ser/Thr Protease (1)

TrxR (1)

Virus Protease (1)

γ-secretase (2)

By Research Areas:

Cancer (2)

Endocrinology (2)

Infection (7)

Inflammation/Immunology (1)

Metabolic Disease (3)

Neurological Disease (2)

Inhibitors & Agonists

Screening Libraries

Peptides

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-14267

Lersivirine UK-453061	HIV Reverse Transcriptase	Infection
Lersivirine (UK-453061) is potent and selective non-nucleoside reverse transcription inhibitor (NNRTI; IC₅₀=119 nM) with excellent efficacy against NNRTI-resistant viruses. Lersivirine exhibits potent antiretroviral activity against wild-type HIV virus and clinically relevant NNRTI-resistant strains .

HY-139602

(+)-JNJ-A07 2 Publications Verification	Flavivirus Dengue Virus Virus Protease	Infection
(+)-JNJ-A07 is a highly potent, orally active pan-serotype dengue virus inhibitor targeting the NS3-NS4B interaction. (+)-JNJ-A07 exerts nanomolar to picomolar activity against a panel of 21 clinical isolates. (+)-JNJ-A07 has a favourable pharmacokinetic profile that results in outstanding efficacy against dengue virus infection in mouse infection models .

HY-B0755

Etimicin sulfate	Antibiotic	Infection
Etimicin (sulfate), a fourth-generation aminoglycoside antibiotic, is now widely clinically used due to its high efficacy and low toxicity.

HY-16632

ELND 006	γ-secretase Amyloid-β	Metabolic Disease
ELND 006 (Compound 30) is a metabolically stable γ-secretase inhibitor designed to selectively inhibit amyloid beta (Aβ) generation while sparing Notch signaling. It was developed through a synthetic strategy emphasizing diversity and chirality. ELND 006, along with its analog ELND007 (Compound 34), progressed into human clinical trials. In preclinical studies, both compounds demonstrated effective reduction of Aβ levels in vitro and in vivo. Comparisons with other γ-secretase inhibitors like Semagacestat, Begacestat, and Avagacestat underscored their potency and specificity in lowering Aβ levels in cerebrospinal fluid (CSF) of healthy human volunteers, suggesting potential therapeutic efficacy in Alzheimer's disease .

HY-106614

Osaterone acetate	Androgen Receptor 5 alpha Reductase	Endocrinology
Osaterone acetate is an orally active steroid anti-androgen agent, mainly used for benign prostatic hyperplasia (BPH) in dogs. Osaterone acetate competitively antagonizes androgen receptor and inhibits 5α-reductase, reducing the concentration of dihydrotestosterone (DHT) while blocking the growth-stimulating effects of testosterone and DHT on prostate cells. Osaterone acetate can rapidly alleviate the symptoms of BPH in dogs without affecting the fertility of breeding dogs .

HY-16525

XEN-2174	Monoamine Transporter Adrenergic Receptor	Neurological Disease
XEN-2174 is a noradrenaline transporter (NET) inhibitor. XEN-2174 inhibits the reuptake of noradrenaline through non-competitive inhibition, increasing the concentration of noradrenaline in the synaptic cleft, thereby activating α2-adrenergic receptor at the spinal level and exerting analgesic effects. XEN-2174 exhibits long-lasting analgesic effects in models of neuropathic pain and postoperative pain in rats. XEN-2174 can be used in pain research .

HY-16622A

GSK 1842799 TFA	LPL Receptor	Others
GSK1842799, an alkyl-substituted biaryl amino alcohol, is a selective S1P1 modulator developed for multiple sclerosis (MS). Upon phosphorylation, GSK1842799-P exhibited subnanomolar S1P1 agonist activity with over 1000-fold selectivity over S1P3. The compound showed good oral bioavailability, rapid in vivo conversion to GSK1842799-P, and significant lymphocyte count reduction at 0.1 mg/kg. It matched FTY720 efficacy at 3 mg/kg in the mouse EAE model and achieved comparable plasma levels to FTY-720 phosphate in cynomolgus monkeys. With favorable ADME, PK/PD properties, and toxicology, GSK1842799 advanced to further clinical development .

HY-12629

PF470 PF-06297470	mGluR	Others
PF470 (PF-06297470) is a negative allosteric modulator of metabotropic glutamate receptor 5 (mGluR5) with significant efficacy in Parkinson's disease models, but clinical development was halted due to potential issues found in toxicology studies.

HY-14915

Bedoradrine	Adrenergic Receptor	Endocrinology
Bedoradrine is a highly selective β2-adrenergic agonist with activity in suppressing asthma and chronic obstructive pulmonary disease (COPD). Bedoradrine is administered by intravenous infusion and is specifically indicated for the suppression of acute asthma attacks. Bedoradrine has shown good safety and preliminary efficacy in clinical trials, especially in patients with stable moderate to severe asthma. The results of Bedoradrine studies have shown that it can provide clinical benefits without increasing clinical risks, especially for patients who are unable to use inhalation or nebulization suppression .

HY-118557A

Iferanserin hydrochloride S-MPEC hydrochloride	5-HT Receptor	Others
Iferanserin hydrochloride (S-MPEC hydrochloride) is a selective serotonin receptor antagonist with the potential to inhibit internal hemorrhoids. Iferanserin hydrochloride demonstrated efficacy and tolerability in ongoing Phase IIb clinical trials, with the ability to significantly reduce patient-reported symptoms of bleeding and pruritus .

HY-163073

Anti-MRSA agent 9	Bacterial	Infection
Anti-MRSA agent 9 (compound 39) shows antibacterial effects against clinically isolated methicillin-resistant Staphylococcus aureus (MRSA) with MIC values of 1 μg/ml. Anti-MRSA agent 9 also shows anti-MRSA efficacy in vivo .

HY-116149

A-424274	nAChR	Others
A-424274 is a positive allosteric modulator of the α4β2 neuronal nicotinic acetylcholine receptor with activity to enhance the efficacy of analgesics. A-424274 selectively enhances the potency of a range of nicotinic acetylcholine receptor agonists at the α4β2 receptor and, in preclinical models, co-administration with an α4β2 PAM significantly enhances the analgesic efficacy of ABT-594 at clinically well-tolerated doses in humans.

HY-B0357B

Diclazuril sodium R-64433 sodium	Parasite Antibiotic	Infection
Diclazuril sodium (R-64433 sodium) is an anticoccidial agent active in preventing parasitic contamination of livestock and poultry feed. Evaluation of the efficacy of Diclazuril sodium in the treatment of Eimeria infection showed poor performance in sustained levels of oocyst excretion compared with controls. Diclazuril sodium has a significant impact on the pathological effects of young animals in clinical applications .

HY-119467

MDK0734	Ser/Thr Protease	Cancer
MDK0734 is a selective inhibitor that inhibits feline hepsin B endopeptidase and exopeptidase activities. MDK0734 demonstrated efficacy in a cell-based in vitro tumor invasion model, significantly attenuating the invasive ability of MCF-10A neoT cells. MDK0734 provides new potential inhibitors for the development of clinically useful compounds targeting the deleterious effects of feline hepsin B in cancer progression .

HY-13736

Quinagolide CV205-502	Dopamine Receptor	Neurological Disease
Quinagolide (CV205-502) is a non-ergot dopamine D(2) receptor agonist that promotes dopamine activity. Quinagolide has shown effectiveness in modulating endocrine function, particularly in inhibiting disorders associated with dopamine deficiency. Quinagolide is used to suppress hyperprolactinemia and corresponding clinical symptoms, showing good efficacy. Quinagolide's biological activity enables its use as an important research compound in drug isolation and analysis .

HY-167950

PPARα/γ agonist 5	PPAR	Metabolic Disease
PPARα/γ agonist 5 is a dual PPARα/γ agonist with significant biological activity exhibited at low concentrations. The EC₅₀ of PPARα/γ agonist 5 are 0.358μM and 1.21μM respectively, showing its potential in inhibiting type 2 diabetes and lipid metabolism disorders. PPARα/γ agonist 5 was selected for clinical development due to its high efficacy .

HY-16469

SR 13668	Akt	Cancer
SR13668 is a potent indole analog derived from indole-3-carbinol (I3C), known for its natural anticancer properties but limited by poor metabolic characteristics. Developed to enhance I3C's anticancer efficacy, SR13668 effectively inhibits growth factor-stimulated Akt activation. It demonstrates strong oral anticancer activity across different cancer types in preclinical studies, showing promise in clinical development due to its favorable safety profile and potent therapeutic effects .

HY-16633

ELND 007	γ-secretase Amyloid-β	Metabolic Disease
ELND 007 (Compound 34) is a metabolically stable γ-secretase inhibitor designed to selectively inhibit amyloid beta (Aβ) generation while minimizing Notch inhibition. Developed alongside ELND 006 (Compound 30), it underwent human clinical trials following a synthetic strategy emphasizing diversity and chirality. In preclinical studies, ELND 007 showed promising in vitro and in vivo characteristics, effectively reducing Aβ levels. Comparative studies with other γ-secretase inhibitors like Semagacestat, Begacestat, and Avagacestat highlighted its efficacy in lowering Aβ production, particularly demonstrated by reduced Aβ levels in the cerebrospinal fluid (CSF) of healthy human volunteers, suggesting potential therapeutic benefit for Alzheimer's disease .

HY-12193

A-349821	Histamine Receptor	Others
A-349821 is a histamine H3 receptor antagonist characterized as a radioligand ([3H]-A-349821) for in vivo receptor occupancy assessment. In rats, [3H]-A-349821 penetrated the brain, showing higher levels in the cortex compared to the cerebellum, indicating selective H3 receptor binding. Its cortical occupancy was saturable, correlating with in vitro binding data. Inhibition studies with ABT-239 and other H3 antagonists showed dose-dependent reductions in receptor occupancy, matching blood levels associated with cognitive efficacy in preclinical models. [3H]-A-349821 thus serves as a valid tracer for H3 receptor occupancy, aiding in the development and clinical interpretation of H3 receptor antagonists .

HY-182683

MMV085203	Parasite TrxR Reactive Oxygen Species (ROS)	Infection
MMV085203 is a potent Plasmodium falciparum inhibitor, with a PfTrxR EC₅₀ of 900 nM. MMV085203 exerts potent antimalarial activity against both blood‑stage and sexual‑stage Plasmodium falciparum parasites, with superior efficacy toward clinical isolates of high clonal diversity. MMV085203 modulates parasite redox homeostasis, induces ROS production, and elevates mitochondrial TCA cycle intermediates. MMV085203 can be used for the research of malaria .

HY-116184

PF-05387252	Endogenous Metabolite	Inflammation/Immunology
PF-05387252 is a potent and selective IRAK4 inhibitor with the activity of inhibiting endogenous TLR signaling pathways. PF-05387252 has shown anti-inflammatory activity in experimental models and may have potential clinical application value in inhibiting psoriasis. Although PF-05387252 and its related compounds have shown anti-inflammatory effects in animal models, their efficacy in inhibiting psoriasis has not yet been verified .

HY-182685

MMV693183	Acetyl-CoA synthetase Parasite	Infection
MMV693183 is an orally active inhibitor of Plasmodium falciparum acetyl-CoA synthetase (AcAS), with an IC₅₀ of 300 nM against Plasmodium falciparum. MMV693183 exhibits potent inhibitory activity against clinical isolates of malaria parasites, including Artemisinin (HY-B0094)-resistant strains. MMV693183 is metabolized in vivo into the active antimetabolite CoA-MMV693183, which exerts effects of killing asexual blood-stage parasites and blocking transmission to Anopheles mosquitoes by binding to and inhibiting the function of acetyl-CoA synthetase, thereby reducing the levels of acetyl-CoA and 4'-phosphopantetheine. In humanized mouse models, MMV693183 shows favorable in vivo efficacy, drug-like properties, and no significant cytotoxicity or off-target activity against human cells. MMV693183 is widely used in malaria-related research as a parasiticide and metabolic disruptor .

Cat. No.	Product Name

HY-L061

Orally Active Compound Library	5,259 compounds
Most of the drugs that are available in the marketplace are administered via the oral route, which is a convenient and cost effective route of administration. Thus, oral bioavailability is one of the key considerations in drug design and development. A high oral bioavailability reduces the amount of an administered drug necessary to achieve a desired pharmacological effect and therefore could reduce the risk of side-effects and toxicity. A poor oral bioavailability can result in low efficacy and higher inter-individual variability and therefore can lead to unpredictable response to a drug. Low oral bioavailability in clinical trials is a major reason for drug candidates failing to reach the market. MCE offers a unique collection of 5,259 compounds with confirmed high oral bioavailability. MCE Orally Active Compound Library is a useful tool for discovering new drugs with oral bioavailability.

Orally Active Compound Library

5,259 compounds

Most of the drugs that are available in the marketplace are administered via the oral route, which is a convenient and cost effective route of administration. Thus, oral bioavailability is one of the key considerations in drug design and development. A high oral bioavailability reduces the amount of an administered drug necessary to achieve a desired pharmacological effect and therefore could reduce the risk of side-effects and toxicity. A poor oral bioavailability can result in low efficacy and higher inter-individual variability and therefore can lead to unpredictable response to a drug. Low oral bioavailability in clinical trials is a major reason for drug candidates failing to reach the market.

MCE offers a unique collection of 5,259 compounds with confirmed high oral bioavailability. MCE Orally Active Compound Library is a useful tool for discovering new drugs with oral bioavailability.

HY-L929

Fragment Library with Good Solubility	2,527 compounds
In drug discovery and development (R&D) area, target binding and druggability optimization are core processes. Among these attributes, high solubility is critical for a compound to achieve druggability, as it directly impacts the progress of drug R&D. Superior solubility ensures the rapid dissolution and uniform distribution of drug molecules in vivo, thereby enhancing bioavailability and effectively mitigating issues such as suboptimal efficacy, increased dosage requirements, or exacerbated toxic and side effects arising from insufficient solubility. From the perspective of medicinal chemistry, high-solubility drug fragments serve as high-quality "molecular building blocks". Based on these fragments, lead compounds with potential druggability can be rapidly screened out, which significantly shortens the drug R&D cycle and reduces R&D costs. Meanwhile, the high-solubility drug fragment library can provide diverse options for drug development in different therapeutic areas, offer solutions for the solubility defects of existing clinical drugs, and facilitate the development of novel, highly effective targeted drugs with higher bioavailability and better safety profiles. MCE has collected and compiled 2,527 experimentally validated small-molecule fragments with high solubility. These fragments can be directly used for drug molecular design, providing high-quality pre-validated solubility fragments that significantly improve the efficiency of lead compound screening and accelerate the progress of drug R&D.

Fragment Library with Good Solubility

2,527 compounds

In drug discovery and development (R&D) area, target binding and druggability optimization are core processes. Among these attributes, high solubility is critical for a compound to achieve druggability, as it directly impacts the progress of drug R&D. Superior solubility ensures the rapid dissolution and uniform distribution of drug molecules in vivo, thereby enhancing bioavailability and effectively mitigating issues such as suboptimal efficacy, increased dosage requirements, or exacerbated toxic and side effects arising from insufficient solubility.

From the perspective of medicinal chemistry, high-solubility drug fragments serve as high-quality "molecular building blocks". Based on these fragments, lead compounds with potential druggability can be rapidly screened out, which significantly shortens the drug R&D cycle and reduces R&D costs. Meanwhile, the high-solubility drug fragment library can provide diverse options for drug development in different therapeutic areas, offer solutions for the solubility defects of existing clinical drugs, and facilitate the development of novel, highly effective targeted drugs with higher bioavailability and better safety profiles.

MCE has collected and compiled 2,527 experimentally validated small-molecule fragments with high solubility. These fragments can be directly used for drug molecular design, providing high-quality pre-validated solubility fragments that significantly improve the efficiency of lead compound screening and accelerate the progress of drug R&D.

Cat. No.	Product Name	Target	Research Area

HY-16525

XEN-2174	Monoamine Transporter Adrenergic Receptor	Neurological Disease
XEN-2174 is a noradrenaline transporter (NET) inhibitor. XEN-2174 inhibits the reuptake of noradrenaline through non-competitive inhibition, increasing the concentration of noradrenaline in the synaptic cleft, thereby activating α2-adrenergic receptor at the spinal level and exerting analgesic effects. XEN-2174 exhibits long-lasting analgesic effects in models of neuropathic pain and postoperative pain in rats. XEN-2174 can be used in pain research .

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