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Agonist activity at human CysLT1 receptor
Assay data:3 Active, 1 Activity ≤ 1 nM, 3 Activity ≤ 1 µM, 3 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Antagonist activity against human CysLT1 expressed in CHO cells assessed as inhibition of LTD4 induced cytosolic Calcium ion mobilization measured after 75 mins by Fluo4 dye based fluorimetric microplate reader assay relative to control
Assay data:7 Active, 16 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Antagonist activity against human CysLT1 expressed in CHO cells assessed as inhibition of LTD4 induced cytosolic Calcium ion mobilization at 10 uM measured after 75 mins by Fluo4 dye based fluorimetric microplate reader assay relative to control
Assay data:16 Tested
SummaryPubMed CitationRelated BioAssays by Target
Antagonist activity at human CysLT1 receptor
Assay data:4 Active, 1 Activity ≤ 1 nM, 3 Activity ≤ 1 µM, 4 Tested
CYSLT1_HS Eurofins SafetyScreen44 (BI)
Assay data:1 Tested
SummaryRelated BioAssays by Target
Displacement of [3H]LTD4 from recombinant human CysLT1 receptor at 10 uM after 60 mins by scintillation counting method relative to control
Leukotriene, Cysteinyl CysLT2 Eurofins-Panlabs radioligand binding assay
Assay data:2 Tested
PRESTO-Tango GPCRome screening (CYSLTR1)
LTD4 (h) (CysLT1) CEREP ligand profiling
Human Whole Blood Cys LT a-IgE
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
CYSLT1_HS Eurofins-Panlabs selectivity data (BI)
LTD4/H Cerep selectivity data (BI)
Inhibition of LTD4 (unknown origin) at 0.1 to 1 uM
Binding affinity to Leukotriene D4 receptor (unknown origin) 10 umol/L by radioligand binding assay
Inhibition of human CYSLTR1 expressed in CHO-K1 cells at 10 uM relative to control
Displacement of [3H]-LTD4 from human recombinant CysLT1 Leukotriene receptor at 10 uM incubated for 60 mins by scintillation counting analysis relative to control
Displacement of [3H]LTD4 from full length recombinant human CysLT1 Leukotriene receptor expressed in CHO-K1 cells assessed as residual binding level for radioligand at 10 uM incubated for 30 mins radiometric scintillation analysis relative to control
Displacement of [3H]LTD4 from full length recombinant human CysLT1 Leukotriene receptor expressed in CHO-K1 cells at 30 uM incubated for 30 mins by radiometric scintillation analysis relative to control
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