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Restrict the search for
phenyl aminosalicylate
to a specific field?
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Luminespib (NVP-AUY922) is a highly potent isoxazole-based, nongeldanamycin HSP90 inhibitor that inhibits the adenosine triphosphatase activity of
HSP90. Luminespib is a highly potent HSP90 inhibitor for HSP90α/β with IC50 of 13 nM /21 nM in cell-free assays, weaker potency against the HSP90 family members GRP94 and TRAP-1, exhibits the tightest binding of any small-molecule HSP90 ligand. Luminespib potently inhibited in vitro growth in all 41 NSCLC cell lines evaluated with IC50 less than 100 nM. IC100 value less than 40 nM was seen in 36 of 41 lines. Luminespib (NVP-AUY922) has greater potency, reduced hepatotoxicity, and lower dependence on DT-diaphorase than the first-generation HSP90 inhibitors. Luminespib was discovered in a multiparameter lead optimization program based on a high-throughput screening hit methodology developed jointly by The Institute of Cancer Research, UK and the pharmaceutical company Vernalis. It has been licensed to Novartis. Luminespib activity is independent of NQO1/DT-diaphorase, maintained in drug-resistant cells and under hypoxic conditions. The molecular signature of HSP90 inhibition, comprising induced HSP72 and depleted client proteins, was readily demonstrable. Pre-clinical studies proved that Luminespib acts via several processes (cytostasis, apoptosis, invasion, and angiogenesis) to inhibit tumor growth and metastasis. These results helped Luminespib to enter clinical trials for various cancers including breast cancers. From 2011 to 2014 it was in Phase II clinical trials.
Status:
Investigational
Source:
NCT01496495: Phase 1 Interventional Completed Myelodysplastic Syndromes
(2012)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Pexmetinib (ARRY-614) is a potent, orally bioavailable, dual p38 MAPK/Tie-2 inhibitor with potential antineoplastic, anti-inflammatory and antiangiogenic activities. Pexmetinib inhibited leukemic proliferation, prevented activation of downstream effector kinases and abrogated the effects of TNF-alpha on healthy hematopoietic stem cells. In ex vivo stimulated human whole blood, LPS-induced cytokines was inhibited by Pexmetinib with an IC50 value ranging from 50-120 nM. ARRY-614 inhibited the release of IL-6 from SEA- or LPS-challenged mice with an ED50 value less than 10 mg/kg. Combining Pexmetinib with lenalidomide inhibited both pro-inflammatory cytokines and tumor growth in vivo with higher potency, compared with either agent alone. In dose escalation or expansion cohorts, treatment with Pexmetinib either once daily or twice daily was applied to forty-five patients. Pexmetinib reduced the levels of circulating biomarkers and the p38 MAPK activation of bone marrow.
Status:
Investigational
Source:
NCT04663308: Phase 2 Interventional Recruiting Primary Sclerosing Cholangitis
(2020)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Volixibat (SHP626; formerly LUM002) is a potent inhibitor of the apical sodium-dependent bile acid transporter (ASBT) that was developed for the treatment of nonalcoholic steatohepatitis. Volixibat participated in phase II clinical trial to investigate its safety, effectiveness in adults with nonalcoholic steatohepatitis. However, this study was discontinued, without any further explanation for the possible causes. In addition, volixibat was studied in a clinical trial in healthy adults and in patients with type 2 diabetes mellitus, where was shown that the drug was generally well tolerated.
Status:
Investigational
Source:
NCT03872427: Phase 2 Interventional Active, not recruiting Advanced Malignant Solid Neoplasm
(2019)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Class (Stereo):
CHEMICAL (RACEMIC)
Alozafone is an anticonvulsant (CNS depressant).
Status:
Investigational
Source:
NCT03267303: Phase 2 Interventional Completed Narcolepsy
(2017)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Enerisant is a histamine H3 receptor antagonist. In H3 receptor binding assay using (R)-α-methyl[3H]histamine, enerisant showed IC50 of 4.9 nM. Enerisant may be useful for the treatment of Alzheimer's disease, schizophrenia, etc.
Status:
Investigational
Source:
NCT03267303: Phase 2 Interventional Completed Narcolepsy
(2017)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Enerisant is a histamine H3 receptor antagonist. In H3 receptor binding assay using (R)-α-methyl[3H]histamine, enerisant showed IC50 of 4.9 nM. Enerisant may be useful for the treatment of Alzheimer's disease, schizophrenia, etc.
Class (Stereo):
CHEMICAL (UNKNOWN)
Targets:
Conditions:
Acifran (AY-25,712), an uncommercialized Ayerst compound exerting lipid-lowering activity in vivo, has been shown to also elicit similar effects as niacin in preliminary clinical testing and has been shown to bind to both high affinity (HM74A; GPR109A) and low affinity (HM74; GPR109B) niacin receptors. The EC50 values of the separated acifran enantiomers for the GPR109a and 109b receptors showed that, as with acifran itself, the (+)-enantiomers were essentially twice as active as the racemic mixtures, whereas the activity of the (-)-enantiomers was more variable and highly dependent on purity. S-enantiomer of acifran is the active principle. All of the activity of racemic acifran could be attributed to the (S)-enantiomer, and hence, from this precedent, (+)-enantiomers would be assigned to the S-configuration. However, the absolute configuration was not confirmed experimentally.
Status:
Investigational
Source:
NCT02215629: Phase 1 Interventional Withdrawn Relapsed or Refractory Acute Myeloid Leukemia
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
PND-1186, also known as SR-2156 and VS-4718, is a potent FAK inhibitor with a 50% inhibitory concentration (IC50) of 1.5 nM in vitro. PND-1186 has an IC50 of ~100 nM in breast carcinoma cells. PND-1186 is currently being evaluated in a Phase 1 trial in patients with advanced solid tumors. In addition, an ongoing collaboration with Wash U is evaluating PND-1186 in combination with gemcitabine and Abraxane in 1st line pancreatic cancer.
Status:
Investigational
Source:
NCT02983617: Phase 2 Interventional Completed Chronic Lymphocytic Leukemia
(2017)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Entospletinib (GS-9973) is an adenosine triphosphate competitive inhibitor of Syk that disrupts kinase activity, which is currently in clinical trials for multiple B-cell malignancies. The most common treatment-emergent serious adverse events included dyspnea, pneumonia, febrile neutropenia, dehydration, and pyrexia.
