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Binding affinity towards human CHRM5 in an in vitro assay with cellular components measured by membrane filtration
Assay data:19 Active, 13 Activity ≤ 1 µM, 117 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M5 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M5 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation at 100 uM preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
Assay data:4 Tested
SummaryPubMed CitationRelated BioAssays by Target
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M5 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation by measuring maximum efficacy preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
Assay data:9 Tested
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M5 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
Assay data:2 Active, 1 Activity ≤ 1 µM, 4 Tested
Displacement of [3H]N-methylscopolamine from human muscarinic M5 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
Assay data:10 Active, 10 Activity ≤ 1 µM, 10 Tested
Potency index, ratio of VU6027831 IC50 to test compound IC50 for antagonist activity at human M5 muscarinic receptor
Assay data:1 Tested
Antagonist activity at human muscarinic M5 receptor assessed as minimal acetylcholine response relative to control
Antagonist activity at human muscarinic M5 receptor
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as minimal acetylcholine response by calcium mobilisation assay relative to control
Assay data:15 Tested
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assay
Assay data:11 Active, 10 Activity ≤ 1 µM, 18 Tested
Inhibition of muscarinic M5 receptor (unknown origin) at 10 uM
Inhibition of human muscarinic M5 receptor
Assay data:2 Tested
Assay data:24 Tested
Assay data:20 Active, 17 Activity ≤ 1 µM, 28 Tested
Selectivity interaction (NIMH Psychoactive Drug Screening Program Selectivity Panel (radioligand binding assay)) EUB0000214b CHRM5
Assay data:1 Active, 1 Tested
SummaryCompounds, ActiveRelated BioAssays by Target
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a CHRM5
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Binding affinity to M5 receptor (unknown origin) at 10000 nM by radioligand displacement assay relative to control
Antagonist activity at human muscarinic M5 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:32 Tested
Displacement of [3H]-NMS from human muscarinic M5 receptor expressed in CHO cells by radioligand binding assay
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
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