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Ligand+efficiency

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-149204
    SYNTi

    		SDCBP Cancer
    SYNTi is a PDZ domain inhibitor targeting the syndecan/syntenin protein-protein Interaction. SYNTi exhibits an IC50 value of 400 nM and ligand efficiency (LE) value of 0.24. SYNTi can be used for breast cancer research .
    SYNTi
  • HY-W023758
    HDGFRP2/PSIP1-IN-1

    4-(4-Bromo-1H-pyrazol-5-yl)pyridine

    		 DNA/RNA Synthesis Cancer
    HDGFRP2/PSIP1-IN-1 (compound BPP) is a dual inhibitor targeting the PWWP domain of hepatocarcinogenic growth factor-related protein 2 (HDGFRP2) and its homologous protein PSIP1, hinder the development and progression of diffuse intrinsic pontine glioma (DIPG). HDGFRP2/PSIP1-IN-1 binds to HDGFRP2 with a Kd value of 7 μM and a ligand efficiency of 0.47; it binds to the PSIP1 PWWP domain with a Kd value of 27 μM; meanwhile, it has a Kd value of 14 μM for HDGFRP3, indicating its effectiveness as an inhibitor of the HDGFRP2 PWWP subfamily .
    HDGFRP2/PSIP1-IN-1
  • HY-144456
    Xanthine oxidase-IN-5

    		Xanthine Oxidase Metabolic Disease
    Xanthine oxidase-IN-5 is an effective and orally active xanthine oxidase (XO) inhibitor with IC50 value of 0.70 μM. Xanthine oxidase-IN-5 displays favorable agent-like properties with ligand efficiency (LE) and lipophilic ligand efficiency (LLE) values of 0.33 and 3.41, respectively. Xanthine oxidase-IN-5 shows potent hypouricemic effects in hyperuricemic rat model .
    Xanthine oxidase-IN-5
  • HY-151387
    A2AAR antagonist 1

    		Adenosine Receptor Neurological Disease
    A2AAR antagonist 1 (compound 21a) is an A2AAR (adenosine A2A receptor) antagonist with a Ki value of 20 nM. A2AAR antagonist 1 shows high ligand efficiency, and it can be used for the research of neurodegenerative diseases .
    A2AAR antagonist 1
  • HY-135711
    PDE8B-IN-1

    		Phosphodiesterase (PDE) Metabolic Disease
    PDE8B-IN-1 is a selective inhibitor of phosphodiesterase 8B (PDE8B) with the activity of enhancing insulin secretion. PDE8B-IN-1 showed good efficacy in high-throughput screening and optimized its ligand efficiency through rapid deconstruction. PDE8B-IN-1 showed high target selectivity and good bioavailability in preclinical development, providing a basis for exploring its potential inhibitory use .
    PDE8B-IN-1
  • HY-W003471
    Pyrrolo[2,1-f][1,2,4]triazin-4-amine

    		MAP4K Others
    Pyrrolo[2,1-f][1,2,4]triazin-4-amine is a MAP4K4 inhibitor with a surface plasmon resonance (SPR) Kd of 88 μM and a ligand efficiency of 0.56 .
    Pyrrolo[2,1-f][1,2,4]triazin-4-amine
  • HY-10654
    EphB4-IN-2

    		Ephrin Receptor Cancer
    EphB4-IN-2 (compound 66) is a tyrosine kinase inhibitor with an IC50 value of 1.6 nM against human EphB4, and exhibits selectivity toward kinases bearing threonine gatekeeper residues. EphB4-IN-2 also has high ligand efficiency .
    EphB4-IN-2

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