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Muscarinic M4 Eurofins Panlabs panel
Assay data:1 Tested
SummaryRelated BioAssays by Target
Binding affinity towards human CHRM4 in an in vitro assay with cellular components measured by membrane filtration
Assay data:13 Active, 2 Activity ≤ 1 nM, 7 Activity ≤ 1 µM, 85 Tested
Agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 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 M4 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:2 Tested
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 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 relative to control
Assay data:8 Tested
Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 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:6 Active, 2 Activity ≤ 1 µM, 8 Tested
Positive allosteric modulator activity at human M4 receptor assessed as equilibrium binding constant at 1 uM
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as leftward shift in concentration response at 10 uM measured after 140 sec by fold shift assay
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in absence of EC20 concentration of acetylcholine by calcium mobilization assay
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as maximal response to ACh by calcium mobilization assay relative to contol
Assay data:14 Tested
Positive allosteric modulator activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 in presence of EC20 concentration of acetylcholine by calcium mobilization assay
Assay data:14 Active, 14 Activity ≤ 1 µM, 14 Tested
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
Assay data:10 Active, 4 Activity ≤ 1 nM, 10 Activity ≤ 1 µM, 10 Tested
Antagonist activity at human muscarinic M4 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assay
Positive allosteric modulator activity at human M4 receptor
Inhibition of muscarinic M4 receptor (unknown origin) at 10 uM
Binding affinity to muscarinic 4 receptor (unknown origin)
Assay data:1 Active, 1 Tested
Antagonist activity at human muscarinic M4 receptor
Assay data:5 Tested
SummaryPubMed CitationRelated BioAssays by Target
Selectivity interaction (NIMH Psychoactive Drug Screening Program Selectivity Panel (radioligand binding assay)) EUB0000214b CHRM4
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a CHRM4
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000316c CHRM4
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