CCR

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  1. CCR5 inhibitor

    CB-0821 is a high-affinity CCR5 inhibitor with a Ki value of 0.04 nM. It effectively binds to the hydrophobic pocket of the CCR5 protein, disrupting the interactions between viral proteins and CCR5, which inhibits viral entry into cells. This compound is poised for use in anti-HIV research applications, facilitating studies on viral tropism and potential therapeutic strategies.
  2. CCR5 Antagonist

    E913 is a selective antagonist of the CCR5 receptor, effectively inhibiting the binding of macrophage inflammatory protein-1alpha (MIP-1alpha) to CCR5 with an IC50 of 0.002 μM. This compound also blocks MIP-1alpha-induced cellular Ca2+ mobilization, demonstrating an IC50 of 0.02 μM. E913 significantly suppresses the replication of both laboratory and primary R5 HIV-1 strains, including multidrug-resistant variants, with IC50 values ranging from 0.03 to 0.06 μM. This reagent is valuable for research into HIV-1 infection and related mechanisms of immune response.
  3. CCR5 Antagonist

    GSK-214096 is a selective CCR5 antagonist that inhibits HIV-1 entry through the blockade of the virus's glycoprotein 120 (gp120). By targeting the CCR5 co-receptor, this compound plays a critical role in interrupting HIV-1 infection pathways. It is valuable for research applications focused on HIV-1 biology and therapeutic discovery.
  4. CcrM Inhibitor

    NSC177365 is a potent CcrM inhibitor that acts by competitively disrupting DNA binding. It demonstrates significant antibacterial activity, displaying IC50 values of 2.3 μM and 14.6 μM against C. crescentus and M. lincolnii, respectively. Furthermore, NSC177365 has potential applications in reversing neurodegenerative disorders and shows promise as an anticancer agent, making it a valuable tool for chemical research.
  5. CCR6 Antagonist

    CCR6 antagonist 1 is a selective antagonist of the CCR6 receptor, effectively inhibiting the CCL20/CCR6 signaling pathway. This compound is instrumental in research focusing on autoimmune-mediated inflammatory diseases, particularly inflammatory bowel diseases (IBDs). Its role in modulating the CCR6 axis provides insights into potential therapeutic strategies for managing such conditions.
  6. CCR Antagonist

    Abaucin is a potent CCR2 antagonist, demonstrating an IC50 of 360 nM. It selectively inhibits CCR2 without affecting CCR1, making it a valuable tool for studying immunological responses and inflammatory processes. Abaucin is applicable in research focusing on the role of CCR2 in disease models and therapeutic interventions targeting chemokine receptors.
  7. CCR Inhibitor

    CCR6 Inhibitor 1 is a highly selective inhibitor of the CCR6 receptor, demonstrating IC50 values of 0.45 nM for monkey CCR6 and 6 nM for human CCR6, while exhibiting minimal activity against human CCR1 and CCR7. This inhibitor effectively prevents ERK phosphorylation, making it a valuable tool in the study of signaling pathways. CCR6 Inhibitor 1 is employed in research focused on autoimmune diseases and cancer, facilitating insights into therapeutic strategies targeting CCR6-related pathways.
  8. CCR7 Antagonist

    CCR7 Ligand 1 is a potent allosteric antagonist targeting the human CC chemokine receptor 7 (CCR7), with a dissociation constant (Kd) of 3 nM. This thiadiazole-dioxide compound effectively inhibits arrestin binding upon CCL19 activation, exhibiting an IC50 of 7.3 μM. CCR7 Ligand 1 is valuable for research applications focused on immune response modulation, chemokine signaling pathways, and therapeutic development for related conditions.
  9. CCR4 Inhibitor

    Zelnecirnon is an orally active CCR4 inhibitor that effectively blocks the recruitment of Th2 inflammatory immune cells to inflamed tissues. This compound exhibits potent anti-inflammatory activity, making it valuable in researching allergic inflammation associated with conditions such as atopic dermatitis and asthma. Zelnecirnon serves as a critical tool for understanding and developing therapeutic strategies in inflammatory diseases.
  10. CCR1 Antagonist

    J-113863 is a potent and selective antagonist of the CCR1 receptor, demonstrating IC50 values of 0.9 nM and 5.8 nM for human and mouse CCR1, respectively. Additionally, it acts as a strong antagonist of the human CCR3 receptor (IC50 of 0.58 nM), while exhibiting weak antagonistic activity against mouse CCR3 (IC50 of 460 nM). J-113863 shows inactivity toward CCR2, CCR4, and CCR5, as well as LTB4 and TNF-α receptors. This compound is primarily utilized in anti-inflammatory research applications.
  11. CCR4 Antagonist

    C-021 dihydrochloride is a highly effective antagonist of the CC chemokine receptor-4 (CCR4). It significantly inhibits chemotaxis in both human and mouse models, exhibiting IC50 values of 140 nM and 39 nM, respectively. Additionally, C-021 dihydrochloride demonstrates capability in preventing the binding of human CCL22-derived [35S]GTPγS to CCR4, with an IC50 of 18 nM. This compound is valuable for research applications focused on immune response modulation and related therapeutic strategies.
  12. CCR6 Antagonist

    PF-07054894 is a potent and orally active antagonist of the C-C Chemokine Receptor 6 (CCR6), effectively blocking CCR6-mediated chemotaxis with an IC50 of 5.7 nM in vitro. As a target of G protein-coupled receptors (GPCRs), PF-07054894 demonstrates significant potential in the study of inflammatory bowel disease and related immunological disorders, providing a valuable tool for understanding CCR6’s role in inflammation.
  13. CCR4 Antagonist

    C-021 is a potent antagonist of the CC chemokine receptor-4 (CCR4). It effectively inhibits functional chemotaxis in both human and mouse models, exhibiting IC50 values of 140 nM and 39 nM, respectively. Additionally, C-021 demonstrates strong efficacy in blocking the binding of human CCL22-derived [35S]GTPγS to CCR4, with an IC50 of 18 nM. This compound is valuable for research applications focused on immune response modulation and cancer biology.
  14. CCR10 Antagonist

    BI-6901 is a potent and selective antagonist of the CCR10 receptor, exhibiting a pIC50 of 9.0. It demonstrates high selectivity among various GPCRs, including multiple chemokine receptors. BI-6901 has shown efficacy in the murine DNFB model of contact hypersensitivity, making it a valuable tool in inflammation research.
  15. CCR Antagonist

    INCB 3284 is a selective and potent antagonist of the human CCR2 receptor, functioning by inhibiting the binding of monocyte chemoattractant protein-1 to hCCR2, with an IC50 value of 3.7 nM. This compound is of particular interest in studies related to acute liver failure, providing insights into the role of CCR2 signaling in inflammatory processes. Its oral bioavailability makes it a valuable tool for in vivo research applications.
  16. CCR4 Antagonist

    Tivumecirnon is a selective CCR4 antagonist that functions by blocking the interaction of CCR4 with its ligands, CCL17 and CCL22. This mechanism reduces the infiltration of regulatory T cells (Tregs) into the tumor microenvironment, thereby enhancing antitumor activity. It is useful for research applications aimed at understanding immune modulation in cancer therapy.
  17. CCR2b Antagonist

    CCR2 antagonist 4 hydrochloride is a selective antagonist targeting the CCR2b receptor, exhibiting a potent inhibitory effect with an IC50 value of 180 nM. This compound effectively reduces MCP-1-induced chemotaxis, with an IC50 of 24 nM, making it a valuable tool for studying inflammatory pathways. Its application in research includes investigations into immune responses and the role of CCR2 in various disease models, particularly those related to monocyte migration and chronic inflammation.
  18. CCR Inhibitor

    Ilacirnon is a potent CCR2 antagonist that specifically targets the C-C chemokine receptor type 2 (CCR2). This compound exhibits significant inhibitory activity, making it valuable in research focused on inflammatory diseases and immune response modulation. Ilacirnon can be utilized in studies exploring the role of CCR2 in various pathophysiological conditions, including atherosclerosis and chronic kidney disease.
  19. CCR1 Antagonist

    AZD-4818 is a potent, orally active antagonist of the chemokine receptor CCR1. This compound selectively inhibits CCR1 signaling, making it a valuable tool for studying the role of this receptor in various inflammatory conditions. Applications include research into chronic obstructive pulmonary disease (COPD) and other related respiratory disorders.
  20. CCR2 Antagonist

    BMS CCR2 22 is a potent antagonist of CC-type chemokine receptor 2 (CCR2), exhibiting a high binding affinity with an IC50 value of 5.1 nM. This compound demonstrates strong functional antagonism, as evidenced by its calcium flux IC50 of 18 nM and chemotaxis IC50 of 1 nM. BMS CCR2 22 is valuable for research applications targeting inflammatory responses and immune cell trafficking, providing insights into CCR2-related pathways.
  21. CCR Antagonist

    MK-0812 Succinate is a potent and selective antagonist of the CCR2 receptor. It demonstrates high affinity for CCR2 and effectively inhibits its signaling pathway, making it a valuable tool for research into inflammatory and immune response processes. This compound is particularly relevant for studies focused on chronic pain, cardiovascular diseases, and various inflammatory disorders.
  22. CCR9 Antagonist

    Vercirnon sodium is a potent and selective antagonist of CCR9, acting primarily by inhibiting CCR9-mediated Ca2+ mobilization and chemotaxis. This compound demonstrates significant biological activity, exhibiting IC50 values of 5.4 nM for Ca2+ mobilization and 3.4 nM for chemotaxis in Molt-4 cells. Vercirnon sodium shows high selectivity for CCR9, with IC50 values greater than 10 μM for other CCR and CX3CR subtypes. It effectively inhibits CCL25-directed chemotaxis in both CCR9 splice forms, CCR9A and CCR9B, with IC50 values of 2.8 nM and 2.6 nM, respectively, making it a valuable tool for research in inflammatory responses and related pathways.
  23. CCR4 Antagonist

    CCR4 Antagonist 4 is a selective and potent inhibitor of the CC chemokine receptor-4 (CCR4), exhibiting an IC50 of 0.02 μM. This compound effectively blocks MDC-mediated chemotaxis and Ca2+ mobilization, with IC50 values of 0.007 μM and 0.003 μM, respectively. CCR4 Antagonist 4 is valuable for investigations into allergic inflammation mechanisms and related therapeutic applications.
  24. CCR8 Antagonist

    CCR8 antagonist 1 is a potent antagonist of human CCR8, exhibiting an inhibition constant (Ki) of 1.6 nM. This compound demonstrates high safety and metabolic stability, making it suitable for in vitro and in vivo studies. CCR8 antagonist 1 is valuable for researching conditions such as asthma and multiple sclerosis, where CCR8-mediated pathways play a significant role in disease progression.
  25. CCR2 Negative Allosteric Modulator

    AZD2423 functions as a negative allosteric modulator of the CCR2 chemokine receptor, exhibiting potent selectivity and oral bioavailability. With an IC50 value of 1.2 nM for CCR2-mediated Ca2+ flux, this compound is valuable for investigating the role of CCR2 in various physiological and pathological processes. AZD2423 is useful in research applications related to inflammation, cancer, and immune system modulation.
  26. CCR Antagonist

    CCX354 is a CCR1 antagonist that primarily functions by inhibiting the receptor's signaling pathways, leading to a reduction in inflammatory responses. This compound demonstrates significant anti-inflammatory activity, making it a valuable tool for research into inflammatory diseases and conditions where CCR1-mediated signaling is implicated. Researchers can utilize CCX354 to explore mechanisms of inflammation and potential therapeutic strategies targeting CCR1.
  27. CCR1 Antagonist

    CCR1 antagonist 9 is a potent and selective antagonist of the CCR1 receptor, exhibiting an IC50 of 6.8 nM in calcium flux assays. This compound plays a significant role in research related to inflammatory responses and immune system modulation. CCR1 antagonist 9 is valuable in studying the impact of CCR1 inhibition in various disease models including autoimmune and chronic inflammatory conditions.
  28. CCR1 Antagonist

    BMS-817399 is a selective CCR1 antagonist that demonstrates high potency with a binding affinity IC50 of 1 nM and chemotaxis inhibition at 6 nM. This compound is orally bioavailable, making it suitable for in vivo studies. BMS-817399 is primarily utilized in research related to rheumatoid arthritis, providing insights into the modulation of inflammatory responses mediated by CCR1.
  29. CCR Antagonist

    CCR3 Antagonist 1 is a potent antagonist of the CCR3 receptor, which plays a critical role in the pathogenesis of immunologic and inflammatory diseases. This compound is instrumental in studying the modulation of immune responses and the development of therapeutic strategies targeting CCR3-mediated signaling pathways. Its application is pivotal for researchers investigating conditions such as asthma, allergic responses, and other related disorders.
  30. CCR3 Inhibitor

    ALK4290 is a potent, orally active inhibitor of CCR3, exhibiting a Ki of 3.2 nM for human CCR3. Its biological activity positions ALK4290 as a valuable tool for research into neovascular age-related macular degeneration and Parkinsonism. This compound may help elucidate the role of CCR3 in these diseases, facilitating the development of targeted therapeutic strategies.
  31. CCR9 Antagonist

    MLN3126 is a potent CCR9 antagonist that exhibits significant oral bioavailability. It effectively inhibits CCL25-induced calcium mobilization and the chemotaxis of mouse primary thymocytes, demonstrating an IC50 value of 6.3 nM for calcium influx. This compound is valuable for research applications investigating immune cell trafficking and related pathways in inflammatory conditions.
  32. CCR4 Receptor Antagonist

    AZD-1678 is a potent antagonist of the CCR4 receptor, exhibiting a pIC50 of 8.6. This compound demonstrates significant biological activity in inhibiting CCR4-mediated signaling pathways, making it useful for research focused on immune response modulation and cancer immunotherapy. Its specificity for the CCR4 receptor allows for detailed studies in related disease models, enhancing our understanding of targeted therapeutic strategies.
  33. CCR4 Antagonist

    CCR4-351 is a potent and selective antagonist of the CCR4 receptor. With IC50 values of 22 nM and 50 nM in the calcium flux and CTX assays, respectively, this compound demonstrates significant biological activity. CCR4-351 is primarily utilized in research applications exploring its antitumor effects and potential therapeutic benefits in modulating immune responses.
  34. CCR8 Antibody

    Tagmokitug (CHS-114) is a fully human IgG1 antibody that specifically targets the CCR8 receptor. This antibody is valuable for researching head and neck squamous cell carcinoma (HNSCC) and understanding the role of CCR8 in tumor microenvironments. Researchers can utilize Tagmokitug to investigate CCR8-mediated signaling pathways and their implications in cancer progression.
  35. CCR2/5 Antagonist

    PF-04634817 succinate is a potent dual antagonist of the CCR2 and CCR5 receptors, demonstrating comparable efficacy in human and rodent CCR2 with an IC50 of 20.8 nM in rats, while exhibiting a reduced potency for CCR5 (IC50 of 470 nM). This compound is suitable for investigating the role of these receptors in various biological pathways, particularly in the context of diabetic nephropathy. PF-04634817 succinate is an important tool for researchers exploring inflammatory and fibrotic processes associated with chronic kidney disease.
  36. hCCR2 Inhibitor

    JNJ-41443532 is a selective antagonist of the human CCR2 receptor, exhibiting an IC50 of 37 nM for binding and demonstrating potent functional antagonism with an IC50 of 30 nM in chemotaxis assays. This compound shows a Ki value of 9.6 µM for murine CCR2 binding. JNJ-41443532 is suitable for research into inflammatory diseases and related inflammatory pathways.
  37. CCR4 Antagonist

    CCR4-351 hydrochloride is a selective antagonist of the CCR4 receptor. This compound exhibits potent biological activity with IC50 values of 22 nM in the calcium flux assay and 50 nM in the CTX assay. Its antagonistic properties make CCR4-351 hydrochloride a valuable tool for research in cancer biology and therapeutic development, particularly in exploring its antitumor effects.
  38. CCR2 Antagonist

    JNJ-27141491 is a selective noncompetitive antagonist of the human chemokine receptor CCR2. It inhibits CCR2-mediated signaling, making it a valuable tool for studying immune responses and inflammation. This compound is useful in research applications focused on cardiovascular diseases and cancer, where CCR2 plays a significant role in immune cell recruitment and tissue remodeling.
  39. CCR5 Antagonist

    AZD-5672 is a potent and selective antagonist of the CCR5 receptor, exhibiting an IC50 of 0.32 nM. This compound demonstrates moderate activity against the hERG ion channel with a binding IC50 of 7.3 μM and acts as a substrate for human P-glycoprotein, inhibiting P-gp-mediated digoxin transport with an IC50 of 32 μM. AZD-5672 is an effective tool for investigating the role of CCR5 in inflammatory diseases, including rheumatoid arthritis.
  40. CCR5 Antagonist

    Met-RANTES (human) is a potent antagonist of the CCR5 chemokine receptor, demonstrating significant inhibitory activity against human MIP-1α and MIP-1β with IC50 values of 5 nM and 2 nM, respectively. This compound has been shown to effectively reduce bone destruction and improve symptoms in models of adjuvant-induced arthritis in rats. Its application in research may provide valuable insights into inflammatory pathways and therapeutic strategies for diseases involving CCR5 signaling.
  41. CCR2 Antagonist

    (1S)-CCR2 antagonist 1 is a selective antagonist targeting the CCR2 receptor. It demonstrates high-affinity binding with a Ki value of 2.4 nM, indicating its potential effectiveness in modulating CCR2-mediated biological processes. This compound is primarily utilized in research applications focused on inflammation, neurodegenerative diseases, and cancer, where CCR2 signaling plays a significant role. Its long residence time enhances its suitability for in vivo studies and therapeutic developments.
  42. CCR4 Antagonist

    CCR4 antagonist 3 is a selective antagonist of chemokine receptor 4 (CCR4) with an IC50 value of 1.7 μM for radiolabeled thymus and activation-regulated chemokine (TARC). This compound effectively inhibits the binding of TARC and macrophage-derived chemokine (MDC) to CCR4 receptors on CEM cell surfaces. Additionally, CCR4 antagonist 3 reduces the in vitro migration of CEM cells induced by TARC, with an IC50 of 6.4 μM. This reagent is valuable for studies investigating CCR4-related immune responses and potential therapeutic interventions in diseases involving CCR4 signaling.
  43. CCR2 Antagonist

    BMS-681 is an orthosteric antagonist of the CC chemokine receptor 2 (CCR2). It effectively inhibits receptor activity by stabilizing transmembrane helix 7, thereby influencing the conformation of transmembrane helix 6, which is pivotal to the orthosteric binding site. This compound is valuable for research into inflammatory neurodegenerative diseases and cancer, allowing for investigations into CCR2-mediated signaling pathways and potential therapeutic interventions.
  44. CCR Antagonist

    CCR1 antagonist 6 is a selective antagonist of chemokine receptor 1 (CCR1), exhibiting an impressive IC50 of 3 nM. This compound is instrumental in research applications focused on inflammatory responses and immune modulation. Its ability to inhibit CCR1 makes it a valuable tool for investigating the role of this receptor in various disease models, including autoimmune and chronic inflammatory disorders.
  45. CCR Antagonist

    CCR1 antagonist 7 (compound 16r) is a selective antagonist of chemokine receptor 1 (CCR1), exhibiting an IC50 of 4 nM. This compound effectively inhibits CCR1 signaling, making it valuable for studies exploring chemokine-related inflammatory processes and immune responses. Its application extends to research in various disease models, including autoimmune disorders and cancer.
  46. CCR Antagonist

    BMS-753426 is a potent antagonist of the chemokine receptor CCR2. It effectively inhibits CCR2-mediated signaling, making it a valuable tool for research into inflammatory and autoimmune diseases. This compound is particularly relevant for studies investigating the role of chemokines in immune cell migration and related pathophysiological processes.
  47. CCR3 Antagonist

    DPC-168 is a potent CCR3 antagonist with an IC50 of 41 nM. It demonstrates significant inhibition of eosinophil chemotaxis and is effective in reducing pulmonary inflammation. This compound is suitable for research applications targeting airway inflammation and related respiratory conditions.
  48. CCR-2 Antagonist

    YJC-10592 is a potent orally active antagonist of the CCR-2 chemokine receptor. It selectively inhibits CCR-2 signaling, making it a valuable tool for investigating the role of this receptor in inflammatory processes. YJC-10592 is suitable for research applications related to asthma and idiopathic dermatitis, contributing to the understanding of disease mechanisms and potential therapeutic strategies.
  49. CCR5 Antagonist

    CCR5 antagonist 4 is a potent oral antagonist of the CCR5 receptor. This compound exhibits significant biological activity by blocking CCR5-mediated signaling pathways, making it an important tool in the study of inflammatory diseases such as rheumatoid arthritis. Its application in research could provide insights into the modulation of immune responses and potential therapeutic strategies.
  50. CCR1 Antagonist

    CCR1 antagonist 10 is a potent and orally bioavailable antagonist of the CCR1 receptor. It effectively inhibits the binding of 125I-MIP-1α to THP-1 cell membranes, demonstrating a Ki value of 2.3 nM. This compound is valuable for research applications involving inflammation, immune response modulation, and related signaling pathways.

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