| + |
NYYJKMXNVNFOFQ-MHZLTWQESA-N | up-regulates activity 
chemical activation
|
ADRB3 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-257856 |
|
|
Cricetulus longicaudatus |
CHO-K1 Cell |
| pmid |
sentence |
| 20590599 |
There were several β3-selective compounds (e.g. AZ 40140d, L 755507, L 748337 and TAK 677) |
|
| Publications: |
1 |
Organism: |
Cricetulus Longicaudatus |
| + |
adrenaline | up-regulates activity
chemical activation
|
ADRB3 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-257877 |
|
|
Cricetulus longicaudatus |
CHO-K1 Cell |
| pmid |
sentence |
| 20590599 |
Of the agonists studied here, there was a general trend that those with highest intrinsic efficacy were so across all three receptor subtypes (i.e. at the top of Tables 3–5, e.g. fenoterol, terbutaline, metaproterenol and adrenaline) |
|
| Publications: |
1 |
Organism: |
Cricetulus Longicaudatus |
| + |
terbutaline | up-regulates activity
chemical activation
|
ADRB3 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-257871 |
|
|
Cricetulus longicaudatus |
CHO-K1 Cell |
| pmid |
sentence |
| 20590599 |
Of the agonists studied here, there was a general trend that those with highest intrinsic efficacy were so across all three receptor subtypes (i.e. at the top of Tables 3–5, e.g. fenoterol, terbutaline, metaproterenol and adrenaline) |
|
| Publications: |
1 |
Organism: |
Cricetulus Longicaudatus |
| + |
isoprenaline | up-regulates activity
chemical activation
|
ADRB3 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258577 |
|
|
Chlorocebus aethiops |
COS-7 Cell |
| pmid |
sentence |
| 8982677 |
K i values of the agonists for [~25I]iodocyanopindolol binding to the COS-7 cell membranes are shown in Table 1. In the membranes expressing one of the 13-adrenoceptor subtypes, both isoproterenol and T-0509 caused monophasic dis- placement of [~25I]iodocyanopindolol, suggesting a single binding site of the agonists. |
|
| Publications: |
1 |
Organism: |
Chlorocebus Aethiops |
| + |
fenoterol | up-regulates activity
chemical activation
|
ADRB3 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-257868 |
|
|
Cricetulus longicaudatus |
CHO-K1 Cell |
| pmid |
sentence |
| 20590599 |
Finally, comparisons of the rank order of ligands for the three different receptors provide information about relative intrinsic efficacies. Fenoterol is a full and efficacious agonist at the β1-adrenoceptor, ranking third out of the agonists studied. It was also a full agonist at the β2- and β3-adrenoceptors with the highest intrinsic efficacy (i.e. top of Tables 4 and and5,5, rank 1). |
|
| Publications: |
1 |
Organism: |
Cricetulus Longicaudatus |
| + |
ADRB3 | up-regulates activity
binding
|
GNAL |
0.435 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-256896 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 31160049 |
Here we systematically quantified ligand-induced interactions between 148 GPCRs and all 11 unique G alpha subunit C-termini. For each receptor, we probed chimeric G alpha subunit activation via a transforming growth factor-alpha (TGF alpha) shedding response in HEK293 cells lacking endogenous Gq/11- and G12/13- signaling. | We defined positive coupling if any member of the subfamily scored LogRAi ≥ -1 and negative coupling if all of the members scored LogRAi < -1 (Figure 3A-B). ROC analysis gives AUC = 0.78 (Figure S4A) when considering high-confidence known coupling data and suggested a threshold of LogRAi ≥ -1.0 for defining true couplings. | The score associated to this interaction has a LogRAi ≥ -1.0. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
L-isoprenaline | up-regulates activity
chemical activation
|
ADRB3 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-257458 |
|
|
Homo sapiens |
HEK-293A Cell |
| pmid |
sentence |
| 31160049 |
Here we systematically quantified ligand-induced interactions between 148 GPCRs and all 11 unique G alpha subunit C-termini. For each receptor, we probed chimeric G alpha subunit activation via a transforming growth factor-alpha (TGF alpha) shedding response in HEK293 cells lacking endogenous Gq/11- and G12/13- signaling. | We defined positive coupling if any member of the subfamily scored LogRAi ≥ -1 and negative coupling if all of the members scored LogRAi < -1 (Figure 3A-B). ROC analysis gives AUC = 0.78 (Figure S4A) when considering high-confidence known coupling data and suggested a threshold of LogRAi ≥ -1.0 for defining true couplings. | The score associated to this interaction has a LogRAi ≥ -1.0. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
N-[2-hydroxy-5-(1-hydroxy-2-{[1-(4-methoxyphenyl)propan-2-yl]amino}ethyl)phenyl]formamide | up-regulates activity
chemical activation
|
ADRB3 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-257855 |
|
|
Cricetulus longicaudatus |
|
| pmid |
sentence |
| 20590599 |
Thus, overall, salmeterol is a highly selective β2-adrenoceptor agonist because of its higher β2-affinity and not because of higher β2-intrinsic efficacy. A similar reasoning can be applied to formoterol, although this agonist has higher intrinsic efficacy at all three receptors (rank 6, 8 and 5 at β1, β2 and β3). |
|
| Publications: |
1 |
Organism: |
Cricetulus Longicaudatus |
| + |
ADRB3 | up-regulates activity
binding
|
GNAS |
0.605 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-256753 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 31160049 |
Here we systematically quantified ligand-induced interactions between 148 GPCRs and all 11 unique G alpha subunit C-termini. For each receptor, we probed chimeric G alpha subunit activation via a transforming growth factor-alpha (TGF alpha) shedding response in HEK293 cells lacking endogenous Gq/11- and G12/13- signaling. | We defined positive coupling if any member of the subfamily scored LogRAi ≥ -1 and negative coupling if all of the members scored LogRAi < -1 (Figure 3A-B). ROC analysis gives AUC = 0.78 (Figure S4A) when considering high-confidence known coupling data and suggested a threshold of LogRAi ≥ -1.0 for defining true couplings. | The score associated to this interaction has a LogRAi ≥ -1.0. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
metaproterenol | up-regulates activity
chemical activation
|
ADRB3 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-257874 |
|
|
Cricetulus longicaudatus |
CHO-K1 Cell |
| pmid |
sentence |
| 20590599 |
Of the agonists studied here, there was a general trend that those with highest intrinsic efficacy were so across all three receptor subtypes (i.e. at the top of Tables 3–5, e.g. fenoterol, terbutaline, metaproterenol and adrenaline) |
|
| Publications: |
1 |
Organism: |
Cricetulus Longicaudatus |
3.0
ADRB3
- 
- 