Binding affinity for human beta-2 adrenergic receptor
|
Homo sapiens
|
1.0
nM
|
|
Concentration required to inhibit electrically induced contraction of superfused guinea-pig trachea was determined
|
Cavia porcellus
|
15.0
nM
|
|
Agonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMP
|
Homo sapiens
|
0.07
nM
|
|
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
|
Homo sapiens
|
0.07
nM
|
|
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
|
Homo sapiens
|
794.33
nM
|
|
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
|
Homo sapiens
|
0.2512
nM
|
|
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
|
Cavia porcellus
|
5.012
nM
|
|
Inhibition of prostaglandin F2alpha-induced contraction in human lung bronchus
|
Homo sapiens
|
5.0
nM
|
|
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
|
Homo sapiens
|
0.39
nM
|
|
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
|
Homo sapiens
|
0.32
nM
|
|
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 mins
|
Cavia porcellus
|
3.5
nM
|
|
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
|
Homo sapiens
|
0.2512
nM
|
|
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
|
Homo sapiens
|
794.33
nM
|
|
Inhibition of CETP in rabbit serum at 10 uM after 1 hr by fluorescent cholesteryl esters transfer assay
|
Oryctolagus cuniculus
|
27.4
%
|
|
Displacement of [3H]CGP12177 from human beta2 adrenoceptor
|
Homo sapiens
|
3.2
nM
|
|
Displacement of [3H]CGP12177 from human beta-1 adrenoceptor
|
Homo sapiens
|
801.0
nM
|
|
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
|
Homo sapiens
|
0.07
nM
|
|
Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs
|
Homo sapiens
|
2.4
nM
|
|
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
|
Homo sapiens
|
0.33
nM
|
|
Displacement of [125I]-CYP from human beta2-adrenergic receptor expressed in COS-7 cells by gamma counting
|
Homo sapiens
|
1.5
nM
|
|
Displacement of [125I]-CYP from human beta2-adrenergic receptor Y308A mutant expressed in COS-7 cells by gamma counting
|
Homo sapiens
|
184.0
nM
|
|
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
|
Homo sapiens
|
0.7943
nM
|
|
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
|
Homo sapiens
|
0.7943
nM
|
|
Binding affinity to adrenergic beta1 receptor
|
None
|
501.19
nM
|
|
Agonist activity at adrenergic beta1 receptor
|
None
|
794.33
nM
|
|
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
|
Cavia porcellus
|
5.012
nM
|
|
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulation
|
Homo sapiens
|
794.33
nM
|
|
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
|
Homo sapiens
|
0.2512
nM
|
|
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
|
Homo sapiens
|
0.2512
nM
|
|
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulation
|
Homo sapiens
|
794.33
nM
|
|
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
|
Cavia porcellus
|
5.012
nM
|
|
Displacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation counting
|
None
|
5.012
nM
|
|
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
|
Homo sapiens
|
0.3162
nM
|
|
Agonist activity at recombinant human beta1-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
|
Homo sapiens
|
251.19
nM
|
|
Agonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassay
|
Homo sapiens
|
0.5012
nM
|
|
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
|
Homo sapiens
|
0.7943
nM
|
|
Binding affinity to beta1 adrenoceptor
|
None
|
501.19
nM
|
|
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
|
Homo sapiens
|
794.33
nM
|
|
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
|
Homo sapiens
|
0.2512
nM
|
|
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
|
Homo sapiens
|
0.3162
nM
|
|
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
|
Homo sapiens
|
2.512
nM
|
|
Agonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contraction
|
Cavia porcellus
|
31.62
nM
|
|
Agonist activity at human recombinant beta1 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
|
Homo sapiens
|
251.19
nM
|
|
Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay
|
Homo sapiens
|
0.5012
nM
|
|
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
|
Homo sapiens
|
3.2
nM
|
|
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
|
Homo sapiens
|
784.0
nM
|
|
Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction
|
Cavia porcellus
|
3.5
nM
|
|
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
|
Homo sapiens
|
2.512
nM
|
|
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assay
|
Homo sapiens
|
251.19
nM
|
|
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
|
Homo sapiens
|
0.3162
nM
|
|
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
|
Homo sapiens
|
0.5012
nM
|
|
Activity at beta2 adrenoceptor/muscarinic M3 receptor in guinea pig trachea assessed as inhibition of electric fileld-stimulated contraction
|
Cavia porcellus
|
6.9
nM
|
|
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of histamine-induced contraction
|
Cavia porcellus
|
2.7
nM
|
|
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
|
Homo sapiens
|
0.18
nM
|
|
Antibacterial activity against Staphylococcus aureus MRSA ATCC 43300 (CO-ADD:GP_020); MIC in CAMBH media, using NBS plates, by OD(600)
|
Staphylococcus aureus subsp. aureus
|
15.16
%
|
|
Antibacterial activity against Escherichia coli ATCC 25922 (CO-ADD:GN_001); MIC in CAMBH media using NBS plates, by OD(600)
|
Escherichia coli
|
8.33
%
|
|
Antibacterial activity against Klebsiella pneumoniae MDR ATCC 70063 (CO-ADD:GN_003); MIC in CAMBH media using NBS plates, by OD(600)
|
Klebsiella pneumoniae
|
16.35
%
|
|
Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 (CO-ADD:GN_042); MIC in CAMBH media using NBS plates, by OD(600)
|
Pseudomonas aeruginosa
|
18.07
%
|
|
Antibacterial activity against Acinetobacter baumannii ATCC 19606 (CO-ADD:GN_034); MIC in CAMBH media using NBS plates, by OD600
|
Acinetobacter baumannii
|
31.88
%
|
|
Antifungal activity against Candida albicans ATCC 90028 (CO-ADD:FG_001); MIC in YNB media using NBS plates, by OD630
|
Candida albicans
|
5.42
%
|
|
Antifungal activity against Cryptococcus neoformans H99 ATCC 208821 (CO-ADD:FG_002); MIC in YNB media using NBS plates, by Resazurin OD(600-570)
|
Cryptococcus neoformans
|
-8.37
%
|
|
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
|
Homo sapiens
|
0.07762
nM
|
|
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assay
|
Mus musculus
|
550.0
nM
|
|
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
|
Homo sapiens
|
0.25
nM
|
|
Agonist activity at beta1-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GRK5 and coelenterazine 400a by BRET assay
|
Homo sapiens
|
199.53
nM
|
|
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assay
|
Homo sapiens
|
0.7943
nM
|
|
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK2 and coelenterazine 400a by BRET assay
|
Homo sapiens
|
0.1259
nM
|
|
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assay
|
Homo sapiens
|
0.07943
nM
|
|
Antiviral activity against DENV2 infected in human Huh7 cells by qRT-PCR analysis
|
Dengue virus 2
|
670.0
nM
|
|
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
|
Homo sapiens
|
0.3
nM
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
13.05
%
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
-0.25
%
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
-0.25
%
|
|
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
|
Homo sapiens
|
0.04467
nM
|
|
Agonist activity at human beta1 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
|
Homo sapiens
|
316.23
nM
|
|
Agonist activity at human beta1 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology
|
Homo sapiens
|
67.0
nM
|
|
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology
|
Homo sapiens
|
0.71
nM
|
|
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
|
Homo sapiens
|
371.54
nM
|
|
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
|
Homo sapiens
|
0.1349
nM
|
|