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IND 100 Publications
Jul 17,2023
Discovery of a highly selective and H435R-sensitive thyroid hormone receptor β agonist. PK properties of the TRβ agonist were analyzed by Medicilon.
Thyroid hormone receptors (TRs) are ligand-dependent transcription factors that belong to the nuclear receptor superfamily and also participate in important physiological functions. In this study, Compound 16g is a well-characterized selective and mutation-sensitive TRβ agonist for further investigating its function in treating dyslipidemia, nonalcoholic steatohepatitis (NASH), and resistance to thyroid hormone (RTH). Compound 16g showed excellent lipid metabolism, safety, metabolic stability, and pharmacokinetic properties. PK properties of Compound 16g were analyzed by Medicilon.
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Discovery of a highly selective and H435R-sensitive thyroid hormone receptor β agonist. PK properties of the TRβ agonist were analyzed by Medicilon.
Jul 17,2023
Discovery of novel dual RAGE/SERT inhibitors for treatment of Alzheimer's disease and depression. Pharmacokinetic studies were commissioned by Medicilon
Alzheimer's disease (AD) is a progressive and devastating neurodegenerative disorder, characterized by the presence of β-amyloid (Aβ) peptide plaques, neurofibrillary tangles, and neuroinflammation. Receptor for advanced glycation end products (RAGE) belongs to the immunoglobulin superfamily, which functions as a cell surface acceptor for Aβ peptide. RAGE plays an important role in the Aβ-mediated neuronal damage that closely related to the pathogenesis of AD. In this study, Compound 12 showed good dual-target bioactivities against RAGE and SERT in vitro, good liver microsomal stability, and acceptable pharmacokinetic properties. Pharmacokinetic studies were commissioned by Medicilon.
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Discovery of novel dual RAGE/SERT inhibitors for treatment of Alzheimer's disease and depression. Pharmacokinetic studies were commissioned by Medicilon
Jul 17,2023
TRIM24 and BRPF1 are potential therapeutic targets for cancer. Y08624 is a new TRIM24/BRPF1 dual inhibitor with reasonable Caco-2 permeability. Caco-2 permeability assay was performed by Medicilon
TRIM24 (tripartite motif-containing protein 24) and BRPF1 (bromodomain and PHD finger containing protein 1) are epigenetics "readers”and potential therapeutic targets for cancer and other diseases. Y08624 (Compound 20l) is a new TRIM24/BRPF1 dual inhibitor. Y08624 displays reasonable Caco-2 permeability. Caco-2 permeability assay was performed by Medicilon.
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TRIM24 and BRPF1 are potential therapeutic targets for cancer. Y08624 is a new TRIM24/BRPF1 dual inhibitor with reasonable Caco-2 permeability. Caco-2 permeability assay was performed by Medicilon
Jul 17,2023
IAP proteins are attractive cancer therapeutic targets. SM-406 is a potent and orally bioavailable antagonist of the IAPs. PK studies of SM-406 in male SD rats, beagle dogs and NHP were performed by Medicilon
Apoptosis is a cellular process critical to the normal development and homeostasis of multicellular organisms. The inhibitor of apoptosis proteins (IAPs) are a class of key apoptosis regulators. IAP proteins are attractive cancer therapeutic targets. SM-406 (compound 2) is a potent and orally bioavailable antagonist of the IAPs. Pharmacokinetic (PK) studies of SM-406 (compound 2) in male Sprague Dawley rats, beagle dogs and cynomolgus monkeys (non-human primates) were performed by the Division of Pharmacokinetics and Metabolism, Medicilon. SM-406 (compound 2) has an excellent PK profile and good oral bioavailability in each of these four species.
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IAP proteins are attractive cancer therapeutic targets. SM-406 is a potent and orally bioavailable antagonist of the IAPs. PK studies of SM-406 in male SD rats, beagle dogs and NHP were performed by Medicilon
Jul 17,2023
Design, synthesis and biological evaluation of a series of FGFRs-dominant multi-target receptor tyrosine kinase inhibitors for the treatment of gastric cancer. The pharmacokinetic analysis was performed by Medicilon
Gastric cancer is the second most lethal cancer across the world. Compounds 8f, inhibits FGFR1 signaling pathways as well as induces cell apoptosis, is a potential agent for the treatment of gastric cancer. The pharmacokinetical profile (PK) of 8f was tested in SD rats. Compound 8f showed an acceptable half-time of 3 h and displayed moderate maximum concentrations, which is enough to meet the concentration of the compound 8f to exert its efficacy in vivo. The pharmacokinetic analysis was performed by the testing service provided by Medicilon.
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Design, synthesis and biological evaluation of a series of FGFRs-dominant multi-target receptor tyrosine kinase inhibitors for the treatment of gastric cancer. The pharmacokinetic analysis was performed by Medicilon
Jul 17,2023
Epigenetic modification plays a major role in the expression of genetic information. The DNA methyltransferase is an attractive target for tumor chemotherapy
Epigenetic modification, like DNA methylation, plays a major role in the expression of genetic information. The DNA methyltransferases (DNMTs), maintain DNA methylation, is an attractive target for tumor chemotherapy. WK-23 displays a good inhibitory effect on human DNMT1 with an IC50 value of 5.0 µM. The PK profile of WK-23 was obtained with quite satisfying oral bioavailability and elimination half-life. In vivo pharmacokinetic properties of WK-22, WK-23, WK-27, and DC_517 were performed by Medicilon.
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Epigenetic modification plays a major role in the expression of genetic information. The DNA methyltransferase is an attractive target for tumor chemotherapy
Jul 17,2023
FBPase is a promising target associated with cancer and type 2 diabetes. Compounds W8 exhibits high selectivity against FBPase. The pharmacokinetic studies of W8 were performed by Medicilon
Fructose-1,6-bisphosphatase (FBPase) is a promising target associated with cancer and type 2 diabetes. Compounds W8 and W8k exhibit high selectivity against FBPase and W8 effectively reduces blood glucose in an Institute of Cancer Research (ICR) mice model and dose-dependent inhibition of glucose production in a primary mouse hepatocyte model. The pharmacokinetic studies of W8 and its leaving group saccharin were performed by Medicilon.
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FBPase is a promising target associated with cancer and type 2 diabetes. Compounds W8 exhibits high selectivity against FBPase. The pharmacokinetic studies of W8 were performed by Medicilon
Jul 17,2023
One of the biggest challenges in drug discovery is to identify high-quality hit and lead compounds
Scaffold hopping refers to computer-aided screening for active compounds with different structures against the same receptor to enrich privileged scaffolds, which is a topic of high interest in organic and medicinal chemistry. One of the biggest challenges in drug discovery is to identify high-quality hit and lead compounds. Lead L12 had an IC50 of 8.7 nM and exhibited a different binding pattern in its crystal structure with PDE5 from the famous starting drug tadalafil, and PK results indicate that L12 could be used as a promising lead for further development. Pharmacokinetic properties of L12 were analyzed by Medicilon.
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One of the biggest challenges in drug discovery is to identify high-quality hit and lead compounds
Jul 17,2023
ANO1 is a potential analgesic target. DFBTA is a potent ANO1 inhibitor with excellent pharmacokinetics properties. In vivo PK were tested by Medicilon
Current pain management is largely limited to opioids and non-steroidal anti-inflammatory drugs. Developing new analgesic drugs remains important to address the unmet medical needs of chronic pain patients. Calcium-activated chloride channel anoctamin-1 (ANO1) is a potential analgesic target. DFBTA is a potent inhibitor with the IC50 of 24 nM. DFBTA shows very weak cytotoxicity, cardiotoxicity, and acute toxicity, as well as excellent pharmacokinetics properties with oral bioavailability >75% and little brain penetration (<1.5% brain/plasma). In vivo PK were tested by Medicilon.
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ANO1 is a potential analgesic target. DFBTA is a potent ANO1 inhibitor with excellent pharmacokinetics properties. In vivo PK were tested by Medicilon
Jul 17,2023
XY153 is a valuable lead compound for the development of potential therapeutics against acute myeloid leukemia. XY153 demonstrated good metabolic stability in vitro. All liver microsome assays were performed by Medicilon
Pan-bromodomain and extra terminal (Pan-BET) inhibitors show profound efficacy but exhibit pharmacology-driven toxicities in clinical trials. The representative Compound 8l (XY153), a novel BD2-selective BET inhibitor, potently binds to BRD4 BD2 with an IC50 value of 0.79 nM. XY153 displayed potent antiproliferative activity against multiple tumor cell lines. XY153 also demonstrated good metabolic stability in vitro. These data indicate that XY153 may serve as a new and valuable lead compound for the development of potential therapeutics against acute myeloid leukemia (AML). All liver microsome assays were performed by Medicilon.
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XY153 is a valuable lead compound for the development of potential therapeutics against acute myeloid leukemia. XY153 demonstrated good metabolic stability in vitro. All liver microsome assays were performed by Medicilon
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688202

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