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Radioligand Binding Assay from US Patent US12071420: "Pyridine and pyrazine compounds as inhibitors of cannabinoid receptor 2"
Assay data:39 Active, 36 Activity ≤ 1 µM, 39 Tested
SummaryRelated BioAssays by Target
Selectivity interaction (Eurofins CEREP Diversity Profile (receptors and ion channels)) EUB0000279b CNR2
Assay data:1 Tested
Selectivity interaction (Panel of non-epigenetic targets (kinases, GPCRs, ion channels, and transporters, Eurofins) ) EUB0000271b CNR2
Selectivity interaction (Panel of kinases, GPCRs, ion channels and transporters (enzymatic assay)) EUB0000223bCl CNR2
Selectivity interaction (Panel of kinases, GPCRs, ion channels and transporters (enzymatic assay)) EUB0000266bCl CNR2
Inhibition of Cannabinoid CB2 at 10.0 M in the Eurofins Panlabs Safety Screen
Activity against CB2/PERIPH/H in the Eurofins SafetyScreen44 (CEREP) (BI) by Radioactive Assay (Cerep_37)
Assay data:4 Tested
SafetyScreen: CB2 Human Cannabinoid GPCR Binding Agonist Radioligand LeadHunter Assay, catalogue number: 37
Assay data:10 Tested
Potency index, ratio of alpha-santalol Ki to test compound Ki for displacement of [3H]-CP55940 from human CB2 receptor expressed in CHO cell membranes incubated for 1 hr by TopCount liquid scintillation counting analysis
SummaryPubMed CitationRelated BioAssays by Target
Agonist activity at CB2 receptor (unknown origin) expressed in human SH-SY5Y cells assessed as increase in intracellular calcium flux at 0.032 to 0.1 uM incubated for 3 mins in presence of 10 uM raloxifene by Fluo-4AM dye based fluorescence analysis
Agonist activity at CB2 receptor (unknown origin) expressed in human SH-SY5Y cells assessed as increase in intracellular calcium flux at 0.032 to 0.1 uM incubated for 3 mins in presence of 60 nM AM-630 by Fluo-4AM dye based fluorescence analysis
Agonist activity at CB2 receptor (unknown origin) expressed in human SH-SY5Y cells assessed as increase in intracellular calcium flux at 0.032 to 0.1 uM incubated for 3 mins by Fluo-4AM dye based fluorescence analysis
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Agonist activity at CB2 receptor (unknown origin) expressed in human SH-SY5Y cells assessed as increase in intracellular calcium flux at 3.2 to 10 uM incubated for 3 mins in presence of 10 uM raloxifene by Fluo-4AM dye based fluorescence analysis
Assay data:2 Tested
Agonist activity at CB2 receptor (unknown origin) expressed in human SH-SY5Y cells assessed as increase in intracellular calcium flux at 3.2 to 10 uM incubated for 3 mins in presence of 60 nM AM-630 by Fluo-4AM dye based fluorescence analysis
Displacement of [3H]-CP55940 from human CB2 receptor expressed in CHO cell membranes at 10 uM incubated for 1 hr by TopCount liquid scintillation counting analysis relative to control
Assay data:13 Tested
Displacement of [3H]-CP55940 from human CB2 receptor expressed in CHO cell membranes assessed as inhibition constant incubated for 1 hr by TopCount liquid scintillation counting analysis
Assay data:4 Active, 4 Activity ≤ 1 µM, 6 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Agonist activity at CB2 receptor (unknown origin) expressed in human SH-SY5Y cells assessed as increase in intracellular calcium flux at 3.2 to 10 uM incubated for 3 mins by Fluo-4AM dye based fluorescence analysis
Assay data:2 Active, 2 Tested
Agonist activity at CB2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assay
Assay data:1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Agonist activity at CB2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production at 1 uM measured after 45 mins by HTRF-based assay
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