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In Vitro Functional Assay of Muscarinic Acetylcholine Receptor Activity from US Patent US11752149: "Muscarinic acetylcholine M1 receptor antagonists"
Assay data:34 Active, 31 Activity ≤ 1 µM, 34 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Antagonist activity at human muscarinic M1 receptor
Assay data:1 Active, 3 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Antagonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as minimal acetylcholine response by calcium mobilisation assay
Assay data:2 Tested
SummaryPubMed CitationRelated BioAssays by Target
Antagonist activity at human muscarinic M1 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assay
Binding affinity to Muscarinic acetylcholine receptor M1 (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 (NIMH Psychoactive Drug Screening Program Selectivity Panel (radioligand binding assay)) EUB0000214b CHRM1
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a CHRM1
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000320b CHRM1
Selectivity interaction (Receptor panel (Novartis) ) EUB0000164c CHRM1
Assay data:1 Tested
SummaryRelated BioAssays by Target
Affinity On-target Cellular interaction (Fold potentiation assay (addition of EC20 acetylcholine, in human M1 expressing Chinese hamster ovary (CHO) cells, by using calcium mobilization readout on a fluorometric imaging plate reader (FLIPR384))) EUB0000344a CHRM1
Affinity On-target Cellular interaction (Fold potentiation assay (addition of EC20 acetylcholine; in human M1 expressing Chinese hamster ovary (CHO) cells; using calcium mobilization readout on a fluorometric imaging plate reader (FLIPR384))) EUB0000252b CHRM1
Binding affinity to M1 receptor (unknown origin) at 10000 nM by radioligand displacement assay relative to control
Inhibition of muscarinic M1 receptor (unknown origin) at 10 uM relative to control
Antagonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by by Fluo-4AM staining based fluorescence assay relative to control
Assay data:31 Tested
Displacement of [3H]-NMS from human muscarinic M1 receptor expressed in CHO cells by radioligand binding assay
Antagonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by by Fluo-4AM staining based fluorescence assay
Assay data:12 Active, 1 Activity ≤ 1 µM, 33 Tested
Antagonist activity at human M1 receptor at 10 uM relative to control
Agonist activity at human M1 receptor at 10 uM relative to control
Displacement of [3H]-pirenzepine from human recombinant M1 receptor expressed in CHO cells incubated for 60 mins by topcount scintillation counter method
Assay data:1 Active, 1 Tested
Antagonist activity at human M1 mAChR receptor expressed in HEK cells assessed as reduction in total cell response at 100 uM by real-time calcium imaging method relative to control
Assay data:3 Tested
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