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cocrystal structures

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-157553
    FAK-IN-19

    		FAK Cancer
    FAK-IN-19 (ligand3) is an inhibitor in a co-crystal structure with FAK. FAK-IN-19 has anticancer effects .
    FAK-IN-19
  • HY-157032
    Proteasome-IN-5

    		Proteasome Others
    Proteasome-IN-5 (compound 5) is a proteasome inhibitor .
    Proteasome-IN-5
  • HY-125473
    IDX375

    		Others Infection
    IDX375 is a novel non-nucleoside inhibitor with selective inhibitory activity against HCV NS5B. IDX375 has good selectivity for genotypes 1a and 1b. The structure and binding site of IDX375 were confirmed by X-ray cocrystal studies .
    IDX375
  • HY-158335
    DXR-IN-1

    		Parasite Infection
    DXR-IN-1 (Compound 13E) is an inhibitor of 1-deoxy-D-ketose 5-phosphate reductoisomerase (DXR). DXR-IN-1 is highly selective for P. falciparum DXR (IC50=0.030 μM). DXR-IN-1 inhibits the growth of P. falciparum by binding to the active site of DXR and blocking its catalytic activity .
    DXR-IN-1
  • HY-118046
    GSK2163632A

    		G Protein-coupled Receptor Kinase (GRK) Cardiovascular Disease
    GSK2163632A is a selective G protein-coupled receptor kinase (GRK) inhibitor that may serve as a probe for studying heart failure and Parkinson's disease. Screening of known protein kinase inhibitors by differential scanning fluorescence method revealed that the melting points of GRK2 and GRK5 increased. Enzymatic assays of the 14 most stable hits revealed that three exhibited nanomolar inhibitory potency against a single GRK, with some showing significant selectivity. Most of the identified compounds can be divided into two categories: indazole/dihydropyrimidine compounds selectively inhibit GRK2, and pyrrolopyrimidine compounds effectively inhibit GRK1 and GRK5 but with modest selectivity. The two most inhibitory representative compounds, GSK180736A and GSK2163632A, are co-crystals with GRK2 and GRK1, respectively, and their atomic structures were determined to 2.6 and 1.85 ? distances, respectively. GSK180736A, as an inhibitor of Rho-related coiled-coil protein kinase, binds to GRK2 in a manner similar to paroxetine, while GSK2163632A, as an inhibitor of insulin-like growth factor 1 receptor, occupies a novel region of the GRK active site cleft and may be used to achieve more Selectivity. However, both compounds inhibited GRK no more potently than their original targets. These data provide a basis for the rational design of more effective and selective GRK inhibitors in the future .
    GSK2163632A

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