CCR

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  1. CCR8 Agonist

    LMD-902 is a potent CCR8 agonist with an EC50 of 15 nM, demonstrating enhanced binding capacity influenced by critical residues such as PheVI:16. This compound is instrumental in researching inflammatory diseases, including bronchial asthma, as well as central nervous system disorders such as multiple sclerosis. Its specificity and efficacy make LMD-902 a valuable tool for advancing understanding in these therapeutic areas.
  2. CCR2 Antagonist

    JNJ-17166864 is a highly selective CCR2 antagonist that demonstrates significant potential in modulating inflammatory responses. This compound has shown efficacy in reducing alveolar bone loss in a mouse model of periodontitis induced by Porphyromonas gingivalis infection. JNJ-17166864 is useful for research applications focused on inflammatory diseases, including allergic rhinitis and periodontal conditions. Its selectivity and biological activity make it a valuable tool for understanding CCR2-mediated pathways in these disease models.
  3. CCR2/CCR5 Antagonist

    LUF8100 is a dual-target antagonist of CCR2 and CCR5, exhibiting pKi values of 5.23 for CCR2 and 4.97 for CCR5. This compound demonstrates significant potential in modulating immune responses and has relevance in cancer research, allowing for the investigation of immune homeostasis and potential therapeutic applications in pathologies driven by these chemokine receptors.
  4. CXCR2/CCR7 Antagonist

    CXCR2/CCR7 antagonist-1 is a potent dual antagonist of the chemokine receptors CXCR2 and CCR7, exhibiting IC50 values of 0.0046 μM and 0.0014 μM, respectively. This compound serves as a valuable tool in the investigation of cancer metastasis and the mechanisms underlying autoimmune diseases, facilitating the study of therapeutic strategies targeting these pathways. Its efficacy in inhibiting both receptors makes it suitable for a range of biochemical and pharmacological research applications.
  5. CCR1 Antagonist

    CP-481715 is a potent and selective antagonist of the CCR1 receptor, exhibiting a Kd of 9.2 nM for human CCR1. This compound demonstrates over 100-fold selectivity for CCR1 compared to a wide array of G-protein-coupled receptors, including related chemokine receptors. CP-481715 is primarily utilized in research related to rheumatoid arthritis and various inflammatory diseases, making it a valuable tool for investigating immune responses and therapeutic interventions in these conditions.
  6. CCR4 Antagonist

    GSK-2239633 is a potent CCR4 antagonist that inhibits the chemokine receptor involved in the regulation of immune responses. This compound demonstrates significant biological activity in modulating T cell trafficking and has potential applications in asthma research and related inflammatory disorders. GSK-2239633 is valuable for studies focusing on immune modulation and therapeutic approaches for allergy and respiratory conditions.
  7. CCR3 Inhibitor

    ALK4290 dihydrochloride is a potent inhibitor of the CCR3 receptor, exhibiting a Ki value of 3.2 nM for human CCR3. This compound demonstrates significant potential for modulating immune responses, making it a valuable tool in the study of neovascular age-related macular degeneration and Parkinson's disease. Researchers can utilize ALK4290 to investigate its effects on CCR3-related signaling pathways and its implications in various pathological conditions.
  8. CCR2 Inhibitor

    ECL1i is an allosteric inhibitor targeting the CCR2 receptor. It selectively disrupts CCL2/CCR2-mediated chemotaxis, thereby impeding the recruitment of CCR2-positive cells. ECL1i has demonstrated efficacy in attenuating disease progression in models of experimental autoimmune encephalomyelitis, making it a valuable tool for studying autoimmune disease mechanisms and potential therapeutic interventions.
  9. CCR2 Antagonists

    CCR2-RA is an allosteric antagonist of the chemokine (C-C motif) receptor 2 (CCR2). This compound selectively inhibits CCR2 signaling, making it a valuable tool in cancer research to explore the role of chemokine receptors in tumor progression and metastasis. Its application extends to investigating the modulation of immune responses in the tumor microenvironment.
  10. CCR1 Antagonist

    BAY-3153 is a selective antagonist of the C-C motif chemokine receptor 1 (CCR1), with human IC50 values of 3 nM, rat IC50 of 11 nM, and mouse IC50 of 81 nM. This compound serves as a valuable tool for investigating the role of CCR1 in various biological processes, including inflammation and immune response modulation. Its specificity and potency make it suitable for research applications involving chemokine signaling and receptor activity.
  11. CCR8 Antagonist

    SB-649701 is a potent antagonist of the human CCR8 receptor, exhibiting a pIC50 of 7.7. This compound is primarily utilized in research related to asthma, providing insights into inflammatory pathways and the role of CCR8 in immune responses. Its mechanism of action makes it valuable for exploring therapeutic strategies targeting airway hyperreactivity and allergic conditions.
  12. CCR2 Antagonist

    BMS-741672 is a selective orally active antagonist of the CCR2 receptor, exhibiting an IC50 of 1.1 nM. This compound demonstrates over 700-fold selectivity for CCR2 compared to CCR5, making it a valuable tool for investigating the role of CCR2 in inflammatory processes. BMS-741672 has potential applications in studies of immune responses and related pathologies, contributing to the understanding of therapeutic strategies targeting chemokine signaling pathways.
  13. CCR3 Agonist

    CH0076989 is a selective agonist of the CCR3 receptor that activates eosinophils and transfectants expressing both wild-type CCR3 and a CCR1:CCR3 chimeric receptor lacking the CCR3 amino-terminus. This compound exhibits a direct interaction with the transmembrane helices of CCR3; activity is abolished by mutations of key residues Y41, Y113, and E287. CH0076989 is ideal for research into inflammation and allergic diseases, including asthma, making it a valuable tool for understanding these pathological conditions.
  14. CCR2 Antagonist

    RO5234444 is an orally active CCR2 antagonist with an IC50 of 22 nM for human CCR2 and 161 nM for mouse CCR2. This compound demonstrates significant biological activity by alleviating glomerulosclerosis, reducing albuminuria, and improving glomerular filtration rate (GFR) in the uninephrectomized type 2 diabetic db/db mouse model. RO5234444 serves as an essential tool for the investigation of type 2 diabetic nephropathy.
  15. CCR3 Antagonist

    YM-344031 is a potent orally active antagonist targeting the CCR3 chemokine receptor. It effectively inhibits the binding of Eotaxin-1 and RANTES to CCR3 with IC50 values of 3.0 nM and 16.3 nM, respectively. This compound also reduces ligand-induced increases in intracellular calcium levels and chemotactic responses. Additionally, YM-344031 demonstrates the ability to ameliorate eotaxin-1-induced morphological changes in eosinophils from macaque blood and mitigates allergic skin responses in murine models, making it a valuable tool for research in allergic and inflammatory conditions.
  16. CCR1 Antagonist

    CCR1 antagonist 12 is a selective antagonist of the CCR1 receptor, exhibiting an IC50 of 3 nM for human CCR1. This compound effectively inhibits CCL3-induced transwell chemotaxis, with an IC50 of 0.009 µM, making it a valuable tool for studying chemokine-mediated signaling pathways. Additionally, CCR1 antagonist 12 demonstrates favorable pharmacokinetic properties in rat models, supporting its potential use in preclinical research.
  17. CCR3 Antagonist

    Maceneolignan H is a selective CCR3 antagonist, with an EC50 value of 1.4 μM. Isolated from the arils of Myristica fragrans, this neolignane compound demonstrates significant potential in the study of allergic diseases. Its ability to inhibit CCR3 suggests applications in researching therapeutic strategies for conditions mediated by this receptor.
  18. Ligand for CCR2

    CCR2 ligand-1 is a potent ligand for the chemokine receptor CCR2, playing a crucial role in mediating inflammatory responses. This compound is valuable for studying CCR2 signaling pathways and its implications in diseases such as cancer and rheumatoid arthritis. Additionally, CCR2 ligand-1 can be utilized in the synthesis of LUF7996 when conjugated with Linker PIN1 degrader-3 and E3 ligase ligand Thalidomide 4-fluoride, facilitating research in targeted protein degradation.
  19. CCR3 Antagonist

    BMS-639623 is a highly potent and orally bioavailable antagonist of the chemokine receptor CCR3, exhibiting an IC50 value of 0.3 nM. This compound demonstrates exceptional inhibitory activity against eosinophil chemotaxis, with an IC50 of 38 pM. BMS-639623 is primarily utilized in research focused on asthma and related inflammatory conditions.
  20. CCR3 Antagonist

    CCR3 Antagonist 2 is a selective antagonist of the CCR3 receptor, a chemokine receptor involved in mediating inflammatory responses. This compound is particularly useful for research applications related to inflammatory and allergic conditions, including obstructive airways diseases. By interfering with CCR3 signaling, it allows for the exploration of therapeutic strategies aimed at modulating immune responses associated with these pathologies.
  21. CCR Antagonist

    RAP-103 is a potent orally active CCR antagonist that targets the CCR pathway to provide synaptic protection. It effectively inhibits and reverses cytoskeletal alterations induced by PrPC/NOX signaling. RAP-103 is particularly relevant for research applications focused on Alzheimer's disease, offering insights into neuroprotective mechanisms and potential therapeutic strategies.
  22. CCR1 Inhibitor

    BX-513 is a potent and selective antagonist of the CCR1 receptor. It effectively inhibits the binding of radiolabeled MIP-1α and RANTES to CCR1, with inhibition constants (Ki) of 40 nM and 60 nM, respectively. BX-513 demonstrates the ability to suppress MIP-1α-induced extracellular acidification, as well as MIP-1α- and RANTES-induced intracellular calcium mobilization and peripheral blood mononuclear cell migration. This compound is applicable in research focusing on autoimmune diseases such as rheumatoid arthritis and multiple sclerosis.
  23. CCR2/CCR5 Antagonist

    PF-4178903 is a potent dual antagonist of the chemokine receptors CCR2 and CCR5, exhibiting IC50 values of 3 nM and 5.3 nM, respectively. This orally active compound is valuable in the study of chronic inflammatory conditions and autoimmune diseases, providing insights into the modulation of immune responses. Its dual targeting capability makes PF-4178903 a significant tool for exploring therapeutic avenues in related research applications.
  24. CCR8 Agonist

    LMD-584 is a selective agonist of CCR8, a chemokine receptor involved in immune responses and inflammation. This compound demonstrates significant biological activity in modulating CCR8 signaling pathways, making it a valuable tool for research applications focused on immune cell trafficking and related pathologies. LMD-584 may aid in understanding the role of CCR8 in various diseases, including cancer and autoimmune disorders.
  25. CCR5 Modulator

    CCR5 modulator-1 is a selective modulator of the CCR5 chemokine receptor. This compound plays a significant role in the regulation of inflammatory processes and can be applied in research aimed at understanding various inflammatory diseases. Its use may provide insights into therapeutic strategies targeting CCR5-related pathways.
  26. Anti-CCR2 Antibody

    Minokitug is a humanized monoclonal antibody that specifically targets the CCR2 protein. It exhibits significant biological activity by inhibiting CCR2-mediated signaling pathways, making it a valuable tool for studying inflammatory processes. This reagent is particularly relevant in research focused on refractory or relapsed ulcerative colitis, aiding in the understanding of the disease's pathophysiology and potential therapeutic interventions.
  27. CCR2 PROTAC Degrader

    LUF7996 is a potent CCR2 PROTAC degrader that selectively targets and degrades CCR2 with a DC50 value of 2.6 μM. This compound effectively engages with the E3 ligase cereblon, promoting sustained and concentration-dependent degradation of CCR2 via the lysosomal pathway. LUF7996 is particularly valuable for research applications involving the inhibition of monocyte migration in vitro, facilitating studies in inflammation and immune response modulation.
  28. CCR1 Antagonist

    cis-J-113863 is a competitive antagonist of chemokine receptor 1 (CCR1) that exhibits potent inhibitory effects, with IC50 values of 0.9 nM for human CCR1 and 5.8 nM for mouse CCR1. This compound is valuable for research in inflammation, immune response, and related therapeutic areas, facilitating the investigation of CCR1's role in various biological processes and disease models.
  29. CCR1 Antagonist

    CCR1 antagonist 13 is a selective antagonist of the CCR1 chemokine receptor. This small molecule inhibitor effectively disrupts CCR1 signaling, making it a valuable tool for investigating the roles of CCR1 in inflammatory responses and immune cell migration. Its applications extend to research on autoimmune diseases, chronic inflammatory conditions, and the modulation of chemokine-mediated pathways.
  30. CCR2 Inhibitor-DOTA Conjugate

    DOTA-ECL1i is a CCR2 inhibitor conjugated with DOTA, designed for use in positron emission tomography (PET) imaging. When radiolabeled with 68Ga, DOTA-ECL1i provides a specific PET tracer that targets CCR2 expression in various pathological conditions. This compound is applicable in research focused on pulmonary fibrosis, cardiac injury, abdominal aortic aneurysm inflammation, atherosclerosis, and cancers of the head, neck, and pancreas.
  31. CCR6/CXCR2 Antagonist

    SQA1 is a squaramide derivative that functions as a CCR6 and CXCR2 antagonist, displaying a dissociation constant (Kd) of 250 nM. It effectively occupies the intracellular pocket, overlapping with the G protein binding site, which helps stabilize the closed conformation of the receptor. This compound is useful in research applications targeting chemokine receptor signaling pathways and their roles in inflammatory responses and immune cell trafficking.
  32. CCR2 Antagonist

    CCR2 Antagonist 6 is a potent CCR2 antagonist with a Ki value of 0.215 μM for CCR2 and 0.174 μM for human CCR2B. This compound exhibits significant biological activity by inhibiting the CCR2 receptor, making it a valuable tool for studying inflammatory processes and autoimmune diseases. Its specificity and efficacy contribute to the understanding of CCR2-related pathways in various pathophysiological conditions.
  33. CCR5 Antagonist

    CCR5 antagonist 5 is an effective CCR5 antagonist that targets the CCR5 receptor, playing a critical role in modulating immune response and inflammation. This compound is particularly valuable for research applications focused on HIV infection and other viral pathogens, offering insights into therapeutic strategies for immunological disorders and viral disease management.
  34. CCR9 Modulator

    CCR9 modulator-1 is a selective modulator of the chemokine receptor CCR9, primarily involved in T-cell trafficking and immune response regulation. This compound demonstrates significant potential in influencing CCR9-mediated immune pathways, making it a valuable tool for the study of inflammatory diseases such as Crohn's disease and other gastrointestinal disorders. Researchers can utilize CCR9 modulator-1 to explore therapeutic strategies targeting CCR9 in various immunological contexts.
  35. CCR1/CCR3 Antagonist

    trans-J-113863 is a potent antagonist of the CCR1 and CCR3 chemokine receptors. It effectively inhibits MIP-1α-induced chemotaxis in CCR1 transfectants and eotaxin-induced chemotaxis in CCR3 transfectants, exhibiting IC50 values of 9.57 nM and 93.8 nM, respectively. This compound serves as a valuable tool for research focused on inflammation and immune responses, offering insights into the roles of these receptors in various biological contexts.
  36. CCR8 Antagonist

    CCR8 antagonist 3 is a selective antagonist of the CCR8 receptor, exhibiting an IC50 value of 0.062 µM. This compound demonstrates stability in human microsomes, making it suitable for various in vitro studies. Its potential applications include exploring mechanisms of immune response modulation and investigating therapeutic strategies for inflammatory diseases and cancer.
  37. CCR5/CXCR3 Inhibitor

    CCR5/CXCR3-IN-1 is a potent inhibitor of the chemokine receptors CXCR3 and CCR5. This compound effectively suppresses the chemotaxis of transformed cells expressing CCR5 and CXCR3, while exhibiting no inhibitory effect on CXCR4-expressing transfected cells. CCR5/CXCR3-IN-1 is valuable for research into chronic arthritic rheumatism and other conditions where modulation of these receptors is crucial.
  38. CCR1 Antagonist

    CP-865569 is a potent CCR1 antagonist, specifically designed to inhibit the activity of the CCR1 chemokine receptor. This compound demonstrates potential therapeutic effects in the modulation of inflammatory responses, making it valuable for research into inflammatory and autoimmune diseases, including rheumatoid arthritis and multiple sclerosis. Its ability to selectively target CCR1 makes CP-865569 an important tool for investigating the roles of chemokines in disease pathology and therapeutic intervention.
  39. CCR1 Antagonist

    BMS-457 is a potent and selective antagonist of the chemokine receptor CCR1. This compound demonstrates significant biological activity in modulating inflammatory pathways and is primarily utilized in research applications related to rheumatoid arthritis. Its ability to inhibit CCR1 makes it a valuable tool for studying the role of chemokines in autoimmune disorders.
  40. CCR5 Antagonist

    SCH 350581 is a CCR5 antagonist that effectively inhibits HIV-1 replication. By obstructing viral entry into host cells and preventing the binding of the gp120 protein to primary lymphocytes, SCH 350581 plays a critical role in studying HIV-1 pathogenesis and potential therapeutic interventions. This compound is valuable for research applications focused on antiviral drug development and the mechanisms of HIV entry.
  41. CCR8 Antagonist

    AZ760 is a potent antagonist of the CCR8 receptor, which plays a significant role in immune response modulation. This compound demonstrates excellent potency and favorable lipophilicity, resulting in a high free fraction in blood. However, it is important to note that AZ760 exhibits unacceptable inhibition of the hERG potassium channel, which may have implications for cardiovascular safety in therapeutic applications.
  42. CXCR2/CCR7 Antagonist

    CCR7 antagonist 1 is a potent dual antagonist of CXCR2 and CCR7, exhibiting an IC50 of 11.02 μM for CXCR2 and 0.43 μM for CCR7. This compound demonstrates significant inhibition of chemokine receptor signaling, making it valuable for studying inflammatory responses and immune system modulation. Its application spans various fields, including cancer research and autoimmune disease studies, where targeting these receptors can provide insights into disease mechanisms and potential therapeutic strategies.
  43. CCR7 Antagonist

    SLW131 is a potent CCR7 antagonist, demonstrating a high affinity with a Ki value of 9.85 nM. This compound effectively inhibits CCL19-induced Go protein activation with an IC50 of 29.4 μM, as well as β-arrestin2 recruitment with an IC50 of 6.0 μM. SLW131 also disrupts CCL19-induced morphological alterations in primary bone marrow-derived dendritic cells and impedes CCR7-mediated migration in mouse CD4+ T cells, making it a valuable tool for research in immune response and cell signaling pathways.
  44. CCR6 Antagonist

    IDOR-1117-2520 is a potent and selective reversible antagonist targeting CCR6. It effectively inhibits CCL20-mediated calcium influx with an IC50 of 63 nM and blocks β-arrestin recruitment to human CCR6, showing an IC50 of 30 nM in recombinant cell models. As a substrate of P-glycoprotein/MDR1, IDOR-1117-2520 is a valuable tool for investigating autoimmune diseases and skin inflammation in research settings.

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