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Assay on Agonistic Effect of Compounds on β1 Receptor by HTRF cAMP Method from US Patent US20230322745: "FUSED TRICYCLIC DERIVATIVE AND PHARMACEUTICAL APPLICATION THEREOF"
Assay data:32 Active, 6 Activity ≤ 1 nM, 32 Activity ≤ 1 µM, 32 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Selectivity interaction (Enzyme panel (receptors, ion channels, other enzymes)) EUB0000679a ADRB2
Assay data:1 Active, 1 Tested
SummaryCompounds, ActiveRelated BioAssays by Target
GPCR beta-arrestin recruitment assay with target: ADRB2 Assay Type: PRESTO-Tango Concentration: 0.0000004
Assay data:211 Tested
SummaryRelated BioAssays by Target
GPCR beta-arrestin recruitment assay with target: ADRB2 Assay Type: PRESTO-Tango Concentration: 0.000002
GPCR beta-arrestin recruitment assay with target: ADRB2 Assay Type: PRESTO-Tango Concentration: 0.00001
Assay data:437 Tested
Binding affinity to beta2 receptor (unknown origin) at 10000 nM by radioligand displacement assay relative to control
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of adrenergic beta-2 receptor (unknown origin) at 10 uM relative to control
Antagonist activity at human beta2 receptor at 10 uM relative to control
Agonist activity at human beta2 receptor at 10 uM relative to control
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
Assay data:29 Active, 1 Activity ≤ 1 nM, 17 Activity ≤ 1 µM, 34 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Binding affinity to immobilized Halo tag-fused beta2 adrenoceptor (unknown origin) expressed in Escherichia coli BL21 (DE3) assessed as association rate constant by receptor chromatography
Assay data:2 Tested
Binding affinity to immobilized Halo tag-fused beta2 adrenoceptor (unknown origin) expressed in Escherichia coli BL21 (DE3) assessed as dissociation rate constant by receptor chromatography
Binding affinity to immobilized Halo tag-fused beta2 adrenoceptor (unknown origin) expressed in Escherichia coli BL21 (DE3) by receptor chromatography
Binding affinity to immobilized Halo tag-fused beta2 adrenoceptor (unknown origin) expressed in Escherichia coli BL21 (DE3) assessed as retention time by chromatography
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
Assay data:4 Active, 4 Activity ≤ 1 nM, 4 Activity ≤ 1 µM, 4 Tested
Inhibition of beta 2 receptor (unknown origin)
Assay data:4 Tested
Invivo agonist beta2 adrenoceptor activity in Dunkin-Hartley guinea pig trachea assessed as histamine induced contraction
Assay data:8 Active, 8 Activity ≤ 1 nM, 8 Activity ≤ 1 µM, 8 Tested
Displacement of 125I-cyanopindolol from human beta2 adrenoceptor expressed in CHO-K1 cell membrane measured after 1 hr by Cheng-prusoff equation analysis
Assay data:10 Active, 9 Activity ≤ 1 nM, 10 Activity ≤ 1 µM, 10 Tested
Binding affinity to immobilized Halo tag-fused beta2 adrenoceptor (unknown origin) expressed in Escherichia coli BL21 (DE3) assessed as reduction in retention time by chromatographic analysis
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Displacement of [3H]-CGP12,177 from immobilized Halo tag-fused beta2 adrenoceptor (unknown origin) expressed in Escherichia coli BL21 (DE3)
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