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Results for "

Structure-activity relationship

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16

Inhibitors & Agonists

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Peptides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-124424

    Potassium Channel Others Neurological Disease
    VU0071063 is a potent and specific Kir6.2/SUR1 opener (EC50=7.44 μM) and can be used for investigating Kir6.2/SUR1 expressed in the pancreas and brain. VU0071063 inhibits insulin secretion by inducing hyperpolarization of β-cell membrane potential. VU0071063 chemotype has a very steep structure-activity relationships .
    VU0071063
  • HY-124127

    Others Others
    Allylpyrocatechol is a compound with antimalarial activity isolated from plants. Its antimalarial activity in vitro and in vivo has been verified, and structure-activity relationship analysis of its analogs has also been performed.
    Allylpyrocatechol
  • HY-121623

    Others Others
    VU0359516 is a compound that modulates mGluR4 activity, obtained through structure-activity relationship analysis of mGluR4 positive allosteric modulators, with improved potency and efficacy, as well as selectivity for mGluR4.
    VU0359516
  • HY-124221

    Others Cancer
    Radamide is an inhibitor of Grp94 with anti-migratory activity. Radamide is used to inhibit Grp94-related diseases such as glaucoma, cancer metastasis, and multiple myeloma. Radamide exhibits selective inhibitory activity by acting on the specific structure of Grp94. Radamide derivatives show better potency and selectivity in improved structure-activity relationship studies .
    Radamide
  • HY-126230

    Others Others
    PAT-494 is an ATX inhibitor with significant activity in biochemical and plasma assays. PAT-494 can reduce LPA levels in rat plasma through oral administration. The structure-activity relationship study of PAT-494 shows that its binding mode with ATX is novel and it can effectively occupy the hydrophobic pockets and channels of ATX .
    PAT-494
  • HY-103513

    Others Others
    GABAA receptor agent 2 (compound 13) is a compound used to study the structure and orthosteric ligand binding of GABA(A) receptors. The relevant model of GABAA receptor agent 2 can be used to understand the details of orthosteric ligand binding, and a detailed binding mode hypothesis was created through structure-activity relationships with two homologous series of orthosteric GABA(A)R antagonists.
    GABAA receptor agent 2
  • HY-118198

    Others Others
    NPY Y2 antagonist 1 (compound 36) is a potent, soluble pyridine analog. In summary, highly promising high-throughput screening hits were extensively explored for structure-activity relationships and a range of potency-enhancing modifications were identified. A potent, soluble, and selective NPY Y2 antagonist 36 was discovered that is amenable to in vitro screening studies. In vivo studies on this molecule will be published in due course.
    NPY Y2 antagonist 1
  • HY-157928

    Keap1-Nrf2 Inflammation/Immunology
    Keap1-Nrf2-IN-18 (Compound 22) is an orally active Keap1-Nrf2 protein-protein interaction (PPI) inhibitor with good pharmacokinetics (PK) profiles and more potent in vivo activities in rats. Keap1-Nrf2-IN-18 has the strongest inhibitory activity in structure−activity relationship (SAR) study (KD = 0.0029 μM) .
    Keap1-Nrf2-IN-18
  • HY-120864

    Wnt Cancer
    SEN461 is a potent and orally active Wnt pathway inhibitor. SEN461 shows effective anti-tumor activity and can be used for GBM research .
    SEN461
  • HY-116264

    Others Cancer
    CatB-IN-1 is an enzyme inhibitor with significant inhibitory activity against tumor invasion. CatB-IN-1 may reduce the invasiveness of tumor cells by regulating intracellular protein metabolism. CatB-IN-1 demonstrates effective anti-invasive ability in cell models and can significantly reduce the invasive ability of MCF-10A neoT cells. The structure-activity relationship study of CatB-IN-1 shows that its design can target multiple functions of cat hepsin B .
    CatB-IN-1
  • HY-141649

    Apoptosis Autophagy Ferroptosis Cancer
    Anticancer agent 251 (compound 7j) can induce cell death of bladder cancer cell T24 by inducing apoptosis, autophagy or ferroptosis .
    Anticancer agent 251
  • HY-117948

    Others Cancer
    ML399 is a second-generation probe optimized for inhibitors of menin-mixed lineage leukemia (MLL) protein-protein interactions. Screening through the Molecular Library Probe Production Network (MLPCN) led to the discovery of several chemical classes, including piperidines, which successfully led to the generation of the first-generation probe ML227. However, metabolic instability, potency, and adjuvant pharmacological activity of ML227 were identified as limiting features. To enhance the utility of menin-MLL inhibitor probes for in vivo mechanistic studies, medicinal chemistry efforts were reinvigorated using a structure-based design approach, which ultimately led to the generation of the announced probe ML399. This study describes the structure-activity relationships and properties of this series of compounds.
    ML399
  • HY-159134

    TRP Channel Others
    TRPA1-IN-3 (commound 1) is a TRPA1 inhibitor. TRPA1-IN-3 can be used in skin and respiratory tract related research .
    TRPA1-IN-3
  • HY-117993

    Others Neurological Disease
    MIND4 is a novel thiozoline that was found to inhibit the deacetylase SIRT2 and to have neuroprotective activity in in vitro brain slices and Drosophila models of Huntington's disease (HD). A systems biology approach revealed another SIRT2-independent property of MIND4, namely as an inducer of nuclear factor erythroid 2 p45-derived factor 2 (NRF2) activity. Structure-activity relationship studies further identified a potent NRF2 activator (MIND4-17) that lacks SIRT2 inhibitory activity. MIND compounds induce NRF2 activation responses in both neuronal and non-neuronal cells and reduce the generation of reactive oxygen and nitrogen intermediates. These agent-like thiozolines offer exciting opportunities for the development of multi-target agents with potential synergistic therapeutic benefits for HD and related disorders.
    MIND4
  • HY-145860

    Phosphoglycerate Dehydrogenase (PHGDH) Cancer
    PHGDH-IN-2 is a potent and NAD + competitive PHGDH inhibitor with an IC50 of 5.2 µM. PHGDH-IN-2 inhibits the serine synthetic pathway in MDA-MB-468 cells. PHGDH-IN-2 inhibits the growth of PHGDH-dependent cancer cells .
    PHGDH-IN-2
  • HY-120371
    CPUY192018
    1 Publications Verification

    Others Inflammation/Immunology
    CPUY192018 is a potent Keap1-Nrf2-ARE inhibitor with an IC50 of 0.63 µM. CPUY192018 exhibits induction of Nrf2-dependent gene NQO1 at 100 µM .
    CPUY192018

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