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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
22 Results for "
Ligand efficiency
" in MedChemExpress (MCE) Product Catalog:
Products (22)
22 Results for "Ligand efficiency" in MCE Product Catalog:
Cat. No.: HY-P5423
CAS No.: 107658-43-5
Cat. No.: HY-P10709
CAS No.: 847058-45-1
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DPyPE is a neutral phosphatidylethanolamine lipid composed of a polyisoprene alkyl chain with two pyridine-containing phosphine ligands. DPyPE is mainly used in liposome formulations and to enhance the efficiency of gene delivery in vitro and in vivo. For example, DPyPE can be mixed with cationic lipids such as VC1052 (HY-156616) (in a 1:1 ratio) to form the vaccine adjuvant Vaxfectin (HY-142998). DPyPE assists VC1052 in binding to negatively charged pDNA to form a uniform liposome complex by regulating the fluidity and stability of the liposome membrane .
Cat. No.: HY-P10489
CAS No.: 374675-19-1
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Cat. No.: HY-172699A
Cat. No.: HY-147376
CAS No.: 192323-14-1
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hACC2-IN-1 is a potent acetyl-CoA carboxylase 2 (ACC2) inhibitor, with an IC50 value of 2.5 μM (hACC2). hACC2-IN-1 could be used for obesity research .
Cat. No.: HY-W023758
CAS No.: 166196-54-9
Synonyms: 4-(4-Bromo-1H-pyrazol-5-yl)pyridine
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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 .
Cat. No.: HY-178282
CAS No.: 2169271-17-2
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JAK1-IN-19 (Compound 18) is a potent JAK1 inhibitor with IC50s of 0.02, 0.5, 91 and 0.2 nM against JAK1, JAK2, JAK3 and TYK2. JAK1-IN-19 exhibits improved rat and human intrinsic clearance. JAK1-IN-19 can be used for the studies of atopic dermatitis and other autoimmune diseases .
Cat. No.: HY-144456
CAS No.: 2276711-87-4
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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 .
Cat. No.: HY-151387
CAS No.: 1784491-64-0
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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 .
Cat. No.: HY-143315
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Protease-Activated Receptor-1 antagonist 3 is a potent protease-activated receptor-1 antagonist with an IC50 value of 7 nM. Protease-Activated Receptor-1 antagonist 3 shows binding affinity for hERG K + channel with an IC50 value of 9 µM .
Cat. No.: HY-14863
CAS No.: 250384-82-8
Synonyms: CTA-018
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Lunacalcipol (CTA-018), as a vitamin D analogue, has a dual role in the pathogenesis of Chronic Kidney Disease (CKD), as an agonist of vitamin D receptor and an antagonist of cytochrome P450 enzyme 24-hydroxylase. Lunacalcipol binds to VDR and regulates transcriptional activity of VDR by influencing ligand binding affinity, ligand-dependent coactivator recruitment or inhibitory factor dissociation, efficiency of ligand entry into target cells, tissue specificity and different metabolism of ligand. Lunacalcipol can be used in the study of CKD, especially Secondary Hyperparathyroidism (sHPT) .
Cat. No.: HY-135711
CAS No.: 1305116-69-1
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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 .
Cat. No.: HY-W003471
CAS No.: 159326-68-8
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 .
Cat. No.: HY-180813
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RORγ-IN-3 (Compound 21) is a potent and highly selective RORγ inhibitor with an EC50 of 84 nM. RORγ-IN-3 can effectively inhibit the production of IL-17, with an IC₅₀ value of 1.0 μM. RORγ-IN-3 can be used for the study of autoimmune diseases .
Cat. No.: HY-W075745
CAS No.: 2049086-35-1
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SK-J003-1n is a nickel catalyst with excellent cross-coupling reaction activity. SK-J003-1n can be used as a ligand in organic synthesis to improve the selectivity and efficiency of the reaction. SK-J003-1n can effectively catalyze the coupling reaction between different substrates, highlighting its important role in compound development and material science.
Cat. No.: HY-L151
527 compounds
PROTACs (Proteolysis-targeting chimeras) is a class of molecules that utilize ubiquitin-proteasome system (UPS) to ubiquitinate and degrade target proteins. The PROTACs molecule consists of two ligands joined by a linker. The one-to-one interaction between PROTACs and target proteins determines the high efficiency of PROTACs, making it a potential molecule for targeted protein degradation (TPD) therapy.
MCE supplies a unique collection of 527 PROTACs that effectively degrade target proteins with more powerful screening capability. MCE PROTAC Library is a useful tool for signal pathway research, protein degradation therapy research, drug discovery and drug repurposing, etc.
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
