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Antagonist activity at human muscarinic M5 receptor assessed as inhibition of acetylcholine-induced calcium response
Assay data:4 Active, 3 Activity ≤ 1 µM, 15 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
Assay data:20 Active, 21 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Human M5 receptor (Acetylcholine receptors (muscarinic))
Assay data:54 Active, 54 Tested
Cmax in po dosed Sprague-Dawley rat
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed Citation
Inhibition of CYP2C9 in human liver microsomes using diclofenac as substrate preincubated for 15 mins followed by NADPH addition measured after 8 mins by LC/MS/MS analysis
Negative allosteric modulation of rat muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
Assay data:4 Active, 1 Activity ≤ 1 µM, 4 Tested
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
Assay data:22 Active, 3 Activity ≤ 1 µM, 31 Tested
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cell membranes assessed as decrease in [3H]-NMS dissociation rate at 10 uM after 3.5 hrs by scintillation counting analysis
Discovery of Novel Negative Allosteric Modulators of Muscarinic Receptor M5: Counterscreen against RAT M5
Assay data:5 Active, 1 Activity ≤ 1 µM, 6 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Same ProjectRelated BioAssays by Target
Discovery of Novel Negative Allosteric Modulators (NAM) of Muscarinic Receptor M5: CRC Assay
Assay data:32 Active, 3 Activity ≤ 1 µM, 42 Tested
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