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Binding affinity towards human CHRM2 in an in vitro assay with cellular components measured by scintillation counting
Assay data:20 Active, 3 Activity ≤ 1 nM, 11 Activity ≤ 1 µM, 37 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Assay data:58 Active, 2 Activity ≤ 1 nM, 37 Activity ≤ 1 µM, 301 Tested
Agonist activity at human TBXA2R in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
Assay data:13 Active, 8 Activity ≤ 1 µM, 927 Tested
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
Assay data:41 Active, 16 Activity ≤ 1 µM, 1178 Tested
Binding affinity towards human CHRNA4 in an in vitro assay with cellular components measured by scintillation proximity assay
Assay data:16 Active, 3 Activity ≤ 1 µM, 1170 Tested
Assay data:155 Active, 74 Activity ≤ 1 µM, 927 Tested
Agonist activity at human CHRM2 in an in vitro cell-based assay measured by fluorescent imaging plate reader
Assay data:15 Active, 2 Activity ≤ 1 µM, 1195 Tested
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
Assay data:14 Active, 11 Activity ≤ 1 µM, 842 Tested
Vasorelaxant activity in rat endothelium-intact main mesenteric artery assessed as relaxation response at 10 uM
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed Citation
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
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
Agonist activity at C-terminal NanoLuc tagged human muscarinic M3 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
Agonist activity at C-terminal NanoLuc tagged human muscarinic M2 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
Agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M1 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
Antiinflammatory activity in LPS-induced mouse RAW264.7 cells assessed as enhancement of STAT3 phosphorylation at 1 mM pretreated with compound for 2 hrs followed by LPS-stimulation and measured after 30 mins by Western blot analysis
Assay data:2 Active, 2 Tested
Antiinflammatory activity in LPS-induced mouse RAW264.7 cells assessed as enhancement of STAT3 phosphorylation at 20 uM pretreated with compound for 2 hrs followed by LPS-stimulation and measured after 30 mins by Western blot analysis
Antiinflammatory activity in LPS-induced mouse RAW264.7 cells assessed as enhancement of JAK2 phosphorylation at 1 mM pretreated with compound for 2 hrs followed by LPS-stimulation and measured after 30 mins by Western blot analysis
Antiinflammatory activity in LPS-induced mouse RAW264.7 cells assessed as enhancement of JAK2 phosphorylation at 20 uM pretreated with compound for 2 hrs followed by LPS-stimulation and measured after 30 mins by Western blot analysis
functional assay from US Patent US10667515: "(S)-5-ethynyl-anabasine, derivatives thereof, and related compositions and methods of making and using"
Assay data:9 Active, 4 Activity ≤ 1 µM, 17 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µM
Interaction Assay from Article 10.1021/bi1006354: "Interaction kinetic and structural dynamic analysis of ligand binding to acetylcholine-binding protein."
Assay data:8 Active, 1 Activity ≤ 1 nM, 7 Activity ≤ 1 µM, 8 Tested
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