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Restrict the search for
m nalidixic acid
to a specific field?
Class (Stereo):
CHEMICAL (RACEMIC)
Lorbamate is a carbamate that has been studied for use as a skeletal muscle relaxer and tranquilizer. It is GABA-A receptors agonist.
Status:
Investigational
Source:
NCT03418714: Phase 1/Phase 2 Interventional Completed Drug Effect
(2017)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Salvinorin A has been reported to be the most potent naturally occurring hallucinogen, with an effective dose in humans in the 200- to the 1,000-μg range when smoked; it has been reported to induce an intense hallucinatory experience in humans, with a typical duration of action being several minutes to an hour or so. Salvinorin A is a highly selective agonist of the kappa-opioid receptor (KOR) with few off-target effects. It is a potent and selective dilator of the cerebral vasculature, exhibits rapid penetration through the blood-brain barrier, has potent anti-inflammatory properties, and has the ability to preserve neurovascular unit integrity. As such, salvinorin A is an ideal compound for the prevention and treatment of cerebral vasospasm following subarachnoid hemorrhage.
Status:
Investigational
Source:
INN:apabetalone [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Apabetalone (RVX-208) is a small molecule BET bromodomain inhibitor selective for BRD4-BD2 undergoing clinical development as a potential therapy to enhance ApoA-I production and treat atherosclerosis and prevent cardiovascular disease events. Apabetalone increases apolipoprotein A-I and high-density lipoprotein cholesterol (HDL-Cholesterol) in vitro and in vivo which is believed to provide a new approach to treating atherosclerosis through the stimulation of reverse cholesterol transport. RVX-208 increased the Tm of all BET bromodomains, indicative of binding. RVX-208 competes for acetylated histone H4 peptide binding to both bromodomains of BRD4, similar to JQ-1, but with a preference for BD2 over BD1. RVX-208 also binds to the bromodomains of BRDs 2 and 3 with a similar preference for BD2 (Kd~5–30 nM) over BD1 (Kd~2–3 uM). Treatment of humans for 1 week with oral RVX-208 increased apoA-I, pre-beta-HDL, and HDL functionality. Resverlogix Corp. has commenced a Phase 3 clinical trial in cardiovascular disease patients with type 2 diabetes mellitus with a primary endpoint of time to first occurrence of Major Adverse Cardiac Events (MACE).
Status:
Investigational
Source:
NCT00712829: Phase 1 Interventional Completed Prostate Cancer
(2008)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
MIP-1095 I-123 is under investigation in clinical trial phase II to evaluate the safety and efficacy in combination with enzalutamide in patients with prostate-specific membrane antigen (PSMA)-avid metastatic castration-resistant prostate cancer who have progressed on abiraterone. It is known that MIP-1095 potently inhibited the glutamate carboxypeptidase activity of PSMA and when radiolabeled with 123I exhibited high affinity for prostate-specific membrane antigen (PSMA) on human prostate cancer LNCaP cells.
Status:
Investigational
Source:
INN:timapiprant [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
OC-459 is a highly potent and selective CRTH2 antagonist which is active on both the recombinant and native human receptor. The Atopix lead compound OC-459 is effective in improving lung function and symptoms in patients with atopic eosinophilic asthma. This group represents 40-50% of all asthmatics and the magnitude of improvement in the responder population is equivalent to high dose inhaled corticosteroids. OC-459 has also been shown to reduce both nasal and eye symptoms in allergic subjects exposed to grass pollen. Of particular interest is the ability of OC-459 to reduce the rate of respiratory infections, an effect related to reduction in Th2 immunity which has a damaging effect on host defence. OC-459 has also demonstrated an excellent safety profile in around 800 subjects exposed drug and no safety issues have been highlighted in long term toxicology. OC-459 is in Phase 2 clinical trial in patients with moderate to severe atopic dermatitis.
Status:
Investigational
Source:
NCT03292822: Early Phase 1 Interventional Unknown status Squamous Cell Carcinoma
(2017)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Licochalcone A (LicA) is a flavonoid isolated from the famous Chinese medicinal herb Glycyrrhiza uralensis Fisch and has a wide spectrum of pharmacological activities such as anti-oxidant, anti-bacterial, anti-viral, and anti-cancer. However, its pharmacological mechanism is not well defined. The anti-Inflammatory effects of LicA on IL-1β-Stimulated human osteoarthritis chondrocytes was reached by activating Nrf2 signaling pathway. LicA showed anti-proliferative and apoptotic effects in breast cancer cells through regulating Sp1 and apoptosis-related proteins in a dose- and a time-dependent manner. In addition, the chemotherapeutic potential of LicA for treatment of human cervical cancer was achieved by inhibition of PI3K/Akt/mTOR signaling.
Status:
Investigational
Source:
JAN:PEFCALCITOL [JAN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Pefcalcitol (previously known as M518101), an analog of vitamin D3 (VD3), is an antipsoriatic drug candidate that is designed to achieve much higher pharmacological effects, such as keratinocyte differentiation. This drug is a phosphodiesterase inhibitor and is being developed as a topical ointment formulation. Pefcalcitol was involved in phase III clinical trials in the USA and in Japan in subjects with plaque psoriasis and with palmoplantar keratoderma. In addition, it participated in phase II clinical trial for the warts treatment.
Status:
Investigational
Source:
NCT03860506: Phase 1 Interventional Completed Healthy
(2008)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
PSI-697 is a quinoline derivative patented by Wyeth, John, and Brother Ltd. as a selectin inhibitor useful for the treatment of acute coronary syndromes. Surface expression of P-selectin on activated platelets induces the formation of platelet-monocyte aggregates and promotes vascular inflammation and thrombosis. In cell-based assays, PSI-697 dose-dependently inhibits the binding of human P-selectin to human P-selectin glycoprotein ligand-1. In preclinical trials, PSI-697, promotes thrombus resolution and decreases inflammation in a baboon model of venous thrombosis. Animals receiving PSI-697 demonstrated significantly increased plasma D-dimer levels versus low-molecular-weight-heparin and control animals six hours post thrombus induction. Unfortunately, in clinical trials, PSI-697 did not inhibit basal or stimulated platelet-monocyte aggregate formation in humans
Status:
Investigational
Source:
INN:sepranolone [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Sepranolone (UC1010) is a GABA-A modulating steroid antagonist (GAMSA) and does not antagonize the effect of GABA itself or other GABAA agonists like benzodiazepines and barbiturates. The interaction of neuroactive steroids (i.e., allopregnanolone and Sepranolone) with GABA-A receptor is particularly important in mood disorders. For example, allopregnanolone administration decreased saccadic eye velocity in healthy female volunteers and induced sedation and these effects were diminished by simultaneous sepranolone administration. Thus, allopregnanolone effects are antagonized by its isomer sepranolone. UC1010 reduces symptom severity and impairment significantly more efficiently than placebo in women with a well-defined, pure premenstrual dysphoric disorder. No severe adverse events were reported during the UC1010 treatment and safety parameters (vital signs and blood chemistry) remained normal during the study. It was revealed also that increases in ring A-reduced progesterone metabolites, particularly Sepranolone, are associated with chronic fatigue syndrome.
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.
