| Assay ID | Title | Year | Journal | Article |
|---|
| AID614118 | Antiproliferative activity against CCL5-induced human LNCAP cells at 500 nM | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
| The natural product CCR5 antagonist anibamine and its analogs as anti-prostate cancer agents. |
| AID43231 | Inhibition of chemotactic protein to CCR5 | 2002 | Journal of medicinal chemistry, Apr-11, Volume: 45, Issue:8
| Inhibition of protein-protein association by small molecules: approaches and progress. |
| AID152812 | Inhibitory effects on HIV-1 (Ba-L) replication was evaluated in PBMCs | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Discovery of novel, potent, and selective small-molecule CCR5 antagonists as anti-HIV-1 agents: synthesis and biological evaluation of anilide derivatives with a quaternary ammonium moiety. |
| AID381455 | Antagonist activity at CCR2/CXCR4 expressed in CHOK1 cells assessed as inhibition of MCP1-induced signaling by aequorin-based assay | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Allosteric transinhibition by specific antagonists in CCR2/CXCR4 heterodimers. |
| AID1453075 | Selectivity ratio of IC50 for displacement of [125I]RANTES from human CCR2 to IC50 for displacement of [125I]RANTES from human CCR5 | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Synthesis and biological evaluation of chemokine receptor ligands with 2-benzazepine scaffold. |
| AID43221 | Binding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells | 2003 | Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
| CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach. |
| AID102403 | Inhibitory effects on HIV-1 (Ba-L) replication was evaluated in MAGI-CCR5 cells | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Discovery of novel, potent, and selective small-molecule CCR5 antagonists as anti-HIV-1 agents: synthesis and biological evaluation of anilide derivatives with a quaternary ammonium moiety. |
| AID44760 | Inhibition of chemotaxis by C-C chemokine receptor type 2 antagonist in human monocytes was measured in the presence 1 nM MCP-1 | 2003 | Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
| CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach. |
| AID1453066 | Displacement of [3H]INCB3344 from human CCR2 expressed in human U2OS cells after 120 mins by scintillation spectrometric analysis | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Synthesis and biological evaluation of chemokine receptor ligands with 2-benzazepine scaffold. |
| AID43214 | Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells | 2003 | Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
| CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach. |
| AID1497320 | Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay | 2018 | Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
| Discovery and synthesis of 6,7,8,9-tetrahydro-5H-pyrido[4,3-c]azepin-5-one-based novel chemotype CCR2 antagonists via scaffold hopping strategy. |
| AID381444 | Displacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Allosteric transinhibition by specific antagonists in CCR2/CXCR4 heterodimers. |
| AID381445 | Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Allosteric transinhibition by specific antagonists in CCR2/CXCR4 heterodimers. |
| AID418629 | Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells | 2009 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
| Design, synthesis, and structure-activity relationship of novel CCR2 antagonists. |
| AID44756 | Inhibitory effect on the binding of [125I]- MCP-1 to C-C chemokine receptor type 2-expressing CHO cells | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Discovery of novel, potent, and selective small-molecule CCR5 antagonists as anti-HIV-1 agents: synthesis and biological evaluation of anilide derivatives with a quaternary ammonium moiety. |
| AID44755 | Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity) | 2003 | Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
| CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach. |
| AID1453068 | Positive allosteric modulation of human CCR5 expressed in HEK293T cells co-expressing CAMYEL assessed as increase in CCL4-induced inhibition of forskolin-stimulated cAMP accumulation after 10 mins by BRET assay | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Synthesis and biological evaluation of chemokine receptor ligands with 2-benzazepine scaffold. |
| AID279329 | Ratio of IC50 for HIV1 KK infected PBMC to IC50 for compound treated HIV1 KK infected PBMC after 67 passages | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Isolation and characterization of human immunodeficiency virus type 1 resistant to the small-molecule CCR5 antagonist TAK-652. |
| AID43228 | Inhibition of chemotactic protein to CCR2b | 2002 | Journal of medicinal chemistry, Apr-11, Volume: 45, Issue:8
| Inhibition of protein-protein association by small molecules: approaches and progress. |
| AID45593 | Inhibition of [125I]RANTES association with CCR5 expressed in CHO cells at 100 nM | 2002 | Journal of medicinal chemistry, Apr-11, Volume: 45, Issue:8
| Inhibition of protein-protein association by small molecules: approaches and progress. |
| AID42497 | Inhibitory effect on Chemokine binding to C-C chemokine receptor type 5 using [125I]RANTES | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Discovery of novel, potent, and selective small-molecule CCR5 antagonists as anti-HIV-1 agents: synthesis and biological evaluation of anilide derivatives with a quaternary ammonium moiety. |
| AID44762 | Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2) | 2003 | Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
| CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach. |
| AID510358 | Selectivity index, CC50 for human CEMx174 5.25M7 cells to IC50 for R5 tropic HIV1 BaL | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
| Tricyclononene carboxamide derivatives as novel anti-HIV-1 agents. |
| AID44753 | Compound was evaluated for the antagonist activity against C-C chemokine receptor type 2 | 2000 | Bioorganic & medicinal chemistry letters, Aug-21, Volume: 10, Issue:16
| CCR2B receptor antagonists: conversion of a weak HTS hit to a potent lead compound. |
| AID381446 | Inhibition of migration of human CD4+ lymphoblasts towards MCP1 by chemotaxis assay | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Allosteric transinhibition by specific antagonists in CCR2/CXCR4 heterodimers. |
| AID381456 | Displacement of [125I]MCP1 from human CCR2/CXCR4 in CD+ T lymphocytes | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Allosteric transinhibition by specific antagonists in CCR2/CXCR4 heterodimers. |
| AID381448 | Induction of [125I]MCP1 dissociation from CCR2 expressed in CHOK1 cells by non-equilibrium binding assay | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Allosteric transinhibition by specific antagonists in CCR2/CXCR4 heterodimers. |
| AID1232303 | Displacement of [125I]-CCL2 from human CCR2 expressed in U2OS cells incubated for 150 mins by scintillation spectrometry | 2015 | Bioorganic & medicinal chemistry, Jul-15, Volume: 23, Issue:14
| Synthesis and biological evaluation of spirocyclic antagonists of CCR2 (chemokine CC receptor subtype 2). |
| AID612004 | Antiviral activity against R5 tropic multidrug-resistant HIV1 MM infected PBMC assessed as inhibition of viral p24 antigen expression | 2011 | Bioorganic & medicinal chemistry, Jul-01, Volume: 19, Issue:13
| Discovery of 4-[4-({(3R)-1-butyl-3-[(R)-cyclohexyl(hydroxy)methyl]-2,5-dioxo-1,4,9-triazaspiro[5.5]undec-9-yl}methyl)phenoxy]benzoic acid hydrochloride: a highly potent orally available CCR5 selective antagonist. |
| AID510356 | Antiviral activity against R5 tropic HIV1 BaL infected in human CEMx174 5.25M7 cells after 3 days by luciferase assay | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
| Tricyclononene carboxamide derivatives as novel anti-HIV-1 agents. |
| AID261802 | Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5 | 2006 | Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
| Highly potent and orally active CCR5 antagonists as anti-HIV-1 agents: synthesis and biological activities of 1-benzazocine derivatives containing a sulfoxide moiety. |
| AID43211 | Binding affinity of compound (10 uM) towards E291Q receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells | 2003 | Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
| CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach. |
| AID43217 | Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells | 2003 | Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
| CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach. |
| AID261801 | Displacement of [125I]RANTES from CCR5 expressed in CHO cells | 2006 | Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
| Highly potent and orally active CCR5 antagonists as anti-HIV-1 agents: synthesis and biological activities of 1-benzazocine derivatives containing a sulfoxide moiety. |
| AID510357 | Cytotoxicity against human CEMx174 5.25M7 cells after 4 days by XTT assay | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
| Tricyclononene carboxamide derivatives as novel anti-HIV-1 agents. |
| AID1242366 | Toxicity against human HeLa67 cells | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7
| Pyrazolo-Piperidines Exhibit Dual Inhibition of CCR5/CXCR4 HIV Entry and Reverse Transcriptase. |
| AID509040 | Antiviral activity against HIV1 JRCSF infected in human vaginal epithelium assessed as inhibition of viral genomic integration by titration assay | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| Ex vivo comparison of microbicide efficacies for preventing HIV-1 genomic integration in intraepithelial vaginal cells. |
| AID43218 | Binding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells | 2003 | Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
| CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach. |
| AID509031 | Antiviral activity against HIV1 JRCSF infected in human vaginal intraepithelial cells assessed as decrease in viral genomic integration at 30 uM by singleplex PCR assay | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| Ex vivo comparison of microbicide efficacies for preventing HIV-1 genomic integration in intraepithelial vaginal cells. |
| AID43215 | Binding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells | 2003 | Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
| CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach. |
| AID614112 | Inhibition of CCL5 binding to CCR5 expressed in CHO cells | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
| The natural product CCR5 antagonist anibamine and its analogs as anti-prostate cancer agents. |
| AID1140541 | Antiproliferative activity against human M12 cells after 72 hrs by WST-1 assay | 2014 | Bioorganic & medicinal chemistry letters, May-15, Volume: 24, Issue:10
| Design, syntheses, and characterization of piperazine based chemokine receptor CCR5 antagonists as anti prostate cancer agents. |
| AID279328 | Antiviral activity in long term culture of HIV1 KK infected PBMCs after 67 passages assessed as p24 antigen levels at escalating concentrations | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Isolation and characterization of human immunodeficiency virus type 1 resistant to the small-molecule CCR5 antagonist TAK-652. |
| AID707904 | Binding affinity to CCR5 | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Chemokine receptor antagonists. |
| AID1528117 | Antagonist activity at human TEV cleavage site-linked CCR5 expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL3-induced beta-arrestin recruitment incubated for 30 mins followed by CCL3 stimulation and measure | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Synthesis and Pharmacological Evaluation of Triazolopyrimidinone Derivatives as Noncompetitive, Intracellular Antagonists for CC Chemokine Receptors 2 and 5. |
| AID427793 | Inhibition of HIV1 (isolate YU2) envelope glycoprotein 120-mediated membrane fusion between virus-transfected african green monkey COS cells and human TZM-bl cells by luciferase-based cell-cell fusion assay in absence of IC9564 | 2008 | Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
| Betulinic acid derivatives that target gp120 and inhibit multiple genetic subtypes of human immunodeficiency virus type 1. |
| AID43226 | Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells | 2003 | Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
| CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach. |
| AID509037 | Antiviral activity against HIV1 isolate M1 infected in human vaginal intraepithelial cells assessed as decrease in viral genomic integration at 1 uM after 48 hrs by multiplex PCR assay | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| Ex vivo comparison of microbicide efficacies for preventing HIV-1 genomic integration in intraepithelial vaginal cells. |
| AID43223 | Binding affinity of compound (10 uM) towards Y210A-292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells | 2003 | Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
| CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach. |
| AID1587014 | Antiviral activity against CXCR4 tropic HIV1 3B infected in human MAGI-CCR5/CXCR4 cells measured after 2 to 6 days by beta-galactosidase reporter gene assay | 2019 | ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
| Tetrahydroisoquinoline CXCR4 Antagonists Adopt a Hybrid Binding Mode within the Peptide Subpocket of the CXCR4 Receptor. |
| AID612003 | Antiviral activity against R5 tropic HIV1 Ba-L infected PBMC assessed as inhibition of viral p24 antigen expression | 2011 | Bioorganic & medicinal chemistry, Jul-01, Volume: 19, Issue:13
| Discovery of 4-[4-({(3R)-1-butyl-3-[(R)-cyclohexyl(hydroxy)methyl]-2,5-dioxo-1,4,9-triazaspiro[5.5]undec-9-yl}methyl)phenoxy]benzoic acid hydrochloride: a highly potent orally available CCR5 selective antagonist. |
| AID1546905 | Inhibition of CCR2 (unknown origin) | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| The Race to Bash NASH: Emerging Targets and Drug Development in a Complex Liver Disease. |
| AID675620 | Antiproliferative activity against human LNCAP cells assessed as inhibition of 10 ng/mL CCL5-induced cell proliferation at 500 nM | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | Structure activity relationship studies of natural product chemokine receptor CCR5 antagonist anibamine toward the development of novel anti prostate cancer agents. |
| AID509034 | Antiviral activity against HIV1 JRCSF infected in human vaginal intraepithelial cells assessed as decrease in viral genomic integration at 30 uM by multiplex PCR assay | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| Ex vivo comparison of microbicide efficacies for preventing HIV-1 genomic integration in intraepithelial vaginal cells. |
| AID427794 | Inhibition of HIV1 (isolate YU2) envelope glycoprotein 120-mediated membrane fusion between virus-transfected african green monkey COS cells and human TZM-bl cells by luciferase-based cell-cell fusion assay in presence of IC9564 | 2008 | Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
| Betulinic acid derivatives that target gp120 and inhibit multiple genetic subtypes of human immunodeficiency virus type 1. |
| AID44612 | Inhibitory effect on the binding of [125I]RANTES to C-C chemokine receptor type 1-expressing CHO cells | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Discovery of novel, potent, and selective small-molecule CCR5 antagonists as anti-HIV-1 agents: synthesis and biological evaluation of anilide derivatives with a quaternary ammonium moiety. |
| AID43220 | Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells | 2003 | Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
| CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach. |
| AID381451 | Induction of [125I]SDF1alpha dissociation from CCR2/CXCR4 expressed in CHOK1 cells by non-equilibrium binding assay | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Allosteric transinhibition by specific antagonists in CCR2/CXCR4 heterodimers. |
| AID1453073 | Displacement of [125I]RANTES from human CCR2 expressed in CHO cells after 40 mins by scintillation counting analysis | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Synthesis and biological evaluation of chemokine receptor ligands with 2-benzazepine scaffold. |
| AID1140540 | Antiproliferative activity against human PC3 cells after 72 hrs by WST-1 assay | 2014 | Bioorganic & medicinal chemistry letters, May-15, Volume: 24, Issue:10
| Design, syntheses, and characterization of piperazine based chemokine receptor CCR5 antagonists as anti prostate cancer agents. |
| AID44761 | Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells | 2003 | Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
| CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach. |
| AID568183 | Antiviral activity against multidrug-resistant R5 tropic HIV1 MM infected in human PBMC assessed as inhibition of HIN p24 antigen expression | 2011 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 21, Issue:4
| Spirodiketopiperazine-based CCR5 antagonist: discovery of an antiretroviral drug candidate. |
| AID43216 | Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells | 2003 | Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
| CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach. |
| AID42510 | Compound was evaluated for the antagonist activity against C-C chemokine receptor type 5 | 2000 | Bioorganic & medicinal chemistry letters, Aug-21, Volume: 10, Issue:16
| CCR2B receptor antagonists: conversion of a weak HTS hit to a potent lead compound. |
| AID1546906 | Inhibition of CCR7 (unknown origin) | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| The Race to Bash NASH: Emerging Targets and Drug Development in a Complex Liver Disease. |
| AID42348 | Inhibitory effect on the binding of [125I]- eotaxin to C-C chemokine receptor type 3- expressing CHO cells | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Discovery of novel, potent, and selective small-molecule CCR5 antagonists as anti-HIV-1 agents: synthesis and biological evaluation of anilide derivatives with a quaternary ammonium moiety. |
| AID675619 | Antiproliferative activity against human DU145 cells assessed as inhibition of 10 ng/mL CCL5-induced cell proliferation at 500 nM | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | Structure activity relationship studies of natural product chemokine receptor CCR5 antagonist anibamine toward the development of novel anti prostate cancer agents. |
| AID1453072 | Antagonist activity at human CCR2b expressed in human Chem1 cells assessed as inhibition of human recombinant CCL2 induced Ca2+ mobilization preincubated for 10 mins followed by CCL2 induction measured every sec for 120 secs by Fluo-4-AM dye-based fluores | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Synthesis and biological evaluation of chemokine receptor ligands with 2-benzazepine scaffold. |
| AID381442 | Displacement of [125I]MCP1 from CCR2 expressed in CHOK1 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Allosteric transinhibition by specific antagonists in CCR2/CXCR4 heterodimers. |
| AID381454 | Antagonist activity at CCR2 expressed in CHOK1 cells assessed as inhibition of MCP1-induced signaling by aequorin-based assay | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Allosteric transinhibition by specific antagonists in CCR2/CXCR4 heterodimers. |
| AID614111 | Antagonist activity at human CCR5 receptor expressed in MOLT4/CCR5 cells assessed as inhibition of CCL5-induced intracellular calcium mobilization by spectrophotometry | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
| The natural product CCR5 antagonist anibamine and its analogs as anti-prostate cancer agents. |
| AID1232305 | Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence ba | 2015 | Bioorganic & medicinal chemistry, Jul-15, Volume: 23, Issue:14
| Synthesis and biological evaluation of spirocyclic antagonists of CCR2 (chemokine CC receptor subtype 2). |
| AID707907 | Binding affinity to CCR2 | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Chemokine receptor antagonists. |
| AID43210 | Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells | 2003 | Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19
| CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach. |
| AID568182 | Antiviral activity against R5 tropic HIV1 Ba-L infected in human PBMC assessed as inhibition of HIN p24 antigen expression | 2011 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 21, Issue:4
| Spirodiketopiperazine-based CCR5 antagonist: discovery of an antiretroviral drug candidate. |
| AID418641 | Inhibition of CCR5 | 2009 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
| Design, synthesis, and structure-activity relationship of novel CCR2 antagonists. |
| AID1232304 | Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay | 2015 | Bioorganic & medicinal chemistry, Jul-15, Volume: 23, Issue:14
| Synthesis and biological evaluation of spirocyclic antagonists of CCR2 (chemokine CC receptor subtype 2). |
| AID42362 | Inhibitory effect on the binding of [125I]TARC to C-C chemokine receptor type 4-expressing CHO cells | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Discovery of novel, potent, and selective small-molecule CCR5 antagonists as anti-HIV-1 agents: synthesis and biological evaluation of anilide derivatives with a quaternary ammonium moiety. |
| AID614117 | Antiproliferative activity against CCL5-induced human DU145 cells at 500 nM | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
| The natural product CCR5 antagonist anibamine and its analogs as anti-prostate cancer agents. |
| AID1453074 | Displacement of [125I]RANTES from human CCR5 expressed in CHO cells after 40 mins by scintillation counting analysis | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Synthesis and biological evaluation of chemokine receptor ligands with 2-benzazepine scaffold. |
| AID1528116 | Antagonist activity at human TEV cleavage site-linked CCR5 expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL3-induced beta-arrestin recruitment at 1 uM incubated for 30 mins followed by CCL3 stimulation and | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Synthesis and Pharmacological Evaluation of Triazolopyrimidinone Derivatives as Noncompetitive, Intracellular Antagonists for CC Chemokine Receptors 2 and 5. |
| AID1453067 | Displacement of [3H]TAK-779 from CCR5 (unknown origin) after 120 mins by scintillation counting method | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Synthesis and biological evaluation of chemokine receptor ligands with 2-benzazepine scaffold. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |