U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 141 - 150 of 1154 results

Status:
Investigational
Source:
NCT02863952: Not Applicable Interventional Unknown status Coronary Artery Disease
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Zinc telluride is a binary chemical compound with the formula ZnTe. Zinc telluride (ZnTe) is a wide-band-gap II–VI semiconductor (E g=2.25 eV at 300 K) crystallizing in the cubic, zinc-blende structure. This material is promising for application as a purely green light-emitting diode. As Zinc telluride can be easily doped, and for this reason it is one of the more common semiconducting materials used in optoelectronics. Zinc telluride finds applications in the following: LEDs and laser diodes Solar cells Tetrahertz imaging Electro-optic detector Holographic interferometry Laser optical phase conjugation devices. Gold–zinc telluride (Au–ZnTe) core–shell nanoparticles were synthesized to support surface modifications for enhanced drug delivery in cancer therapeutics.
Status:
Investigational
Source:
INN:desmetramadol [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

O-Desmethyl tramadol (O-Desmethyltramadol, O-DSMT) is a metabolite of tramadol. O-Desmethyltramadol is an opioid analgesic and the main active metabolite of tramadol. (+)-O-Desmethyltramadol is the most important metabolite of tramadol produced in the liver after tramadol is consumed. This metabolite is considerably more potent as a μ-opioid agonist than the parent compound. O-desmethyl tramadol, inhibits 5-hydroxytryptamine type 2C receptors expressed in xenopus oocytes. O-desmethyl tramadol inhibits functions of M(1) receptors but has little effect on those of M(3) receptors. O-desmethyl tramadol has been widely used clinically and has analgesic activity.
Vorasidenib (also known as AG 881) was developed as an isocitrate dehydrogenase (IDH) type 1 in the cytoplasm and type 2 in the mitochondria, with potential antineoplastic activity. It is known that IDH is an essential enzyme for cellular respiration in the tricarboxylic acid (TCA) cycle. Isocitrate dehydrogenases 1 and 2 (IDH1/2) are homodimeric enzymes that catalyze the conversion of isocitrate to α-ketoglutarate (α-KG) in the tricarboxylic acid cycle. Vorasidenib participated in phase I clinical trials in patients with advanced hematologic malignancies and in gliomas.
Status:
Investigational
Source:
INN:decoglurant [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Decoglurant is a negative allosteric modulator of the mGlu2 and mGlu receptors developed by Roche. Decoglurant was investigated in a phase 2 clinical trials in patients with major depressive disorder. Negative results were reported and the development was discontinued in 2015.
Status:
Investigational
Source:
JAN:NAPABUCASIN [JAN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Napabucasin (BBI608) is an orally administered small molecule that blocks stem cell activity in cancer cells by targeting the signal transducer and activator of transcription 3 pathway, which is over-activated in many types of cancer and has been shown to be an important pathway in cancer stem cell-mediated propagation of cancer. Napabucasin has already shown promising efficacy on different cancer types, both as a monotherapy and in combination with conventional chemotherapeutic agents. Early-phase trials have shown promising anti-tumor efficacy when patients are treated with napabucasin in combination with standard chemotherapy agents, and preclinical results suggest that napabucasin can synergize with chemotherapy agents, such as paclitaxel, to potentially overcome drug resistance. Encouraging phase Ib/II trial results warrant further clinical study with napabucasin and paclitaxel combination therapy, especially in malignancies where there is an urgent and unmet need for effective therapeutics, such as in patients with advanced pancreatic adenocarcinoma.
Status:
Investigational
Source:
INN:ladarixin [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


LADARIXIN is a dual inhibitor of chemokine receptors CXCR1 and CXCR2. It inhibits human polymorphonuclear leukocyte (PMN) migration to chemokine CXCL8 in vitro and prevents PMN infiltration and tissue damage in several models of cerebral ischemia/reperfusion in vivo. It is under development for the treatment of type 1 diabetes.
Status:
Investigational
Source:
INN:edasalonexent [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

CAT-1004 (Edasalonexent)is an orally administered small molecule designed to inhibit NF-κB, which is activated from infancy in Duchenne muscular dystrophy and is central to causing muscle damage and preventing muscle regeneration. Structurally CAT-1004 represents covalently links salicylic acid and docosahexaenoic acid -- two compounds known to inhibit NF-κB. . In a Phase 1 study in adults, NF-κB activity in peripheral mononuclear cells was inhibited following a single dose of edasalonexent but not by equimolar doses of salicylic acid and docosahexaenoic acid. Chronic activation of NF-κB is a key driver of muscle degeneration and suppression of muscle regeneration in Duchenne muscular dystrophy, which occurs early in the disease process and precedes loss of muscle function. Salicylic acid prevents NF-κB mediated muscle atrophy and decreases protein catabolism in muscle. Docosahexaenoic acid has been shown to upregulate anti-inflammatory pathways and suppress pro-inflammatory pathways via modulation of NF-κB activity. Edasalonexent is endocytosed and hydrolyzed by intracellular fatty acid amide hydrolase (FAAH) to release salicylic acid and DHA in the intracellular compartment, thus having a potential advantage of selectively delivering higher doses in target muscle cells where FAAH is abundant.
Status:
Investigational
Source:
NCT01740609: Phase 1 Interventional Completed Healthy
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Parafluorofentanyl is a selective mu-opioid agonist, an analog of fentanyl, developed by Janssen. The drug was not developed for human use but is produced and abused illegally.
Status:
Investigational
Source:
NCT03506945: Not Applicable Interventional Recruiting Depressive Symptoms
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



MPEP (2-methyl-6-(phenylethynyl)pyridine) was one of the first compounds found to act a selective antagonist for the metabotropic glutamate receptor subtype mGluR5. It was under development by Novartis in the late 1990's. MPEP was found to produce neuroprotective effects following acute brain injury in animals. MPEP was also found to have positive effects on animal models of depression, anxiety and morphine withdrawl.