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M2 Receptor Affinity Test from US Patent US20230322745: "FUSED TRICYCLIC DERIVATIVE AND PHARMACEUTICAL APPLICATION THEREOF"
Assay data:18 Active, 15 Activity ≤ 1 nM, 18 Activity ≤ 1 µM, 18 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Antagonist activity at human muscarinic M2 receptor
Assay data:2 Tested
SummaryPubMed CitationRelated BioAssays by Target
Binding affinity to Muscarinic acetylcholine receptor M2 (unknown origin) assessed as inhibition constant
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Selectivity interaction (GloSensor assay) EUB0000234b CHRM2
Assay data:1 Tested
SummaryRelated BioAssays by Target
Selectivity interaction (Eurofins Panlabs Discovery Services Panel (enzymes and receptors)) EUB0000234b CHRM2
Selectivity interaction (Eurofins-Panlabs panel) EUB0000295b CHRM2
Selectivity interaction (NIMH Psychoactive Drug Screening Program Selectivity Panel (radioligand binding assay)) EUB0000214b CHRM2
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000333a CHRM2
Selectivity interaction (CEREP panel (nuclear receptors, ion channels, and 32 other enzymes, including 10 kinases, 9 proteases, and 5 phosphodiesterases)) EUB0000195c CHRM2
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a CHRM2
Assay data:1 Active, 1 Tested
SummaryCompounds, ActiveRelated BioAssays by Target
Selectivity interaction (PSP Principial panel 20118+ (panel of GPCRs, transporter, and ion channels)) EUB0000283b CHRM2
Selectivity interaction (Enzymatic assay (PanLabs Profiling)) EUB0000715a CHRM2
Binding affinity to M2 receptor (unknown origin) at 10000 nM by radioligand displacement assay relative to control
Inhibition of muscarinic M2 receptor (unknown origin) at 10 uM relative to control
Displacement of [3H]-NMS from human muscarinic M2 receptor expressed in CHO cells by radioligand binding assay
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 assessed as intracellular calcium mobilization by calcium mobilization assay
Assay data:3 Tested
Agonist activity at human M2 receptor at 10 uM relative to control
Antagonist activity at human M2 receptor at 10 uM relative to control
Agonist activity at muscarinic M2 receptor (unknown origin)
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Antagonist activity at human M2 mAChR receptor expressed in HEK cells at 10 uM by real-time calcium imaging method
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