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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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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.

