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Inhibition of human CCR4 at 10 uM relative to control
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Antagonist activity against CCR4 (unknown origin) assessed as inhibition of beta-arrestin 2 recruitment at 10 microM by beta arrestin assay relative to control
Agonist activity against CCR4 (unknown origin) assessed as induction of beta-arrestin 2 recruitment at 10 microM by beta arrestin assay relative to control
FLIPR Assay from US Patent US9090596: "Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds for use in the treatment of chemokine-mediated pathologies"
Assay data:4 Active, 4 Activity ≤ 1 µM, 4 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Cell-Based Assay from Article 10.1111/j.1747-0285.2007.00551.x: "Bipiperidinyl carboxylic acid amides as potent, selective, and functionally active CCR4 antagonists."
Assay data:17 Active, 1 Activity ≤ 1 µM, 30 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Ca Flux assay from US Patent US10246462: "Chemokine receptor modulators and uses thereof"
Assay data:71 Active, 88 Activity ≤ 1 µM, 88 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
In Vitro Affinity Assay from US Patent US9580412: "Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds for use in the treatment of chemokine-mediated diseases"
Assay data:21 Active, 20 Activity ≤ 1 µM, 21 Tested
Chemokine CCR4 Eurofins-Panlabs radioligand binding assay
SummaryRelated BioAssays by Target
PRESTO-Tango GPCRome screening (CCR4)
Antagonist activity at CCR4 (unknown origin) assessed as inhibition of ligand-induced calcium flux measured upto 10 uM
Displacement of [125I]chemokine from CCR4 (unknown origin) by gamma counter method
Antagonist activity at CCR4 in human MDA-MB-231 cells assessed as inhibition of CCL12-mediated chemotaxis at 100 nM after 22 hrs by transwell assay
Assay data:2 Active, 2 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Antagonist activity at human Gi/G0-coupled CCR4 receptor expressed in CHO-K1 cells assessed as inhibition of CCL22-induced beta arrestin2 recruitment at 500 nM preincubated for 30 mins followed by CCL22 stimulation and measured after 90 to 180 mins by pathhunter assay
Assay data:1 Active, 1 Tested
Antagonist activity at CCR4 in human Treg cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL17-mediated chemotaxis preincubated for 30 mins followed by CCL17 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
Assay data:28 Active, 26 Activity ≤ 1 µM, 31 Tested
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
Assay data:22 Active, 21 Activity ≤ 1 µM, 25 Tested
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
Assay data:29 Active, 28 Activity ≤ 1 µM, 30 Tested
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
Assay data:15 Active, 13 Activity ≤ 1 µM, 21 Tested
Activity at human CCR4 up to 10 uM
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