| + |
CAMK2A | down-regulates 
phosphorylation
|
OPRM1 |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-79678 |
Ser268 |
LKSVRMLsGSKEKDR |
Homo sapiens |
|
| pmid |
sentence |
| 10908300 |
The decrease in mu-opioid receptor activity after chronic agonist exposure (1 microm [d-ala(2),n-mephe(4),gly-ol(5)]-enkephalin) is largely due to kinase-mediated phosphorylation of intracellular receptor domains. We have recently shown that the substitution of two putative ca(2+)/calmodulin-dependent protein kinase ii (camk ii) phosphorylation sites, s261 and s266, by alanines in the third intracellular loop of the rat mu-opioid receptor (rmor1) confers resistance to camk ii-induced receptor desensitization. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-79682 |
Ser270 |
SVRMLSGsKEKDRNL |
Homo sapiens |
|
| pmid |
sentence |
| 10908300 |
The decrease in mu-opioid receptor activity after chronic agonist exposure (1 microm [d-ala(2),n-mephe(4),gly-ol(5)]-enkephalin) is largely due to kinase-mediated phosphorylation of intracellular receptor domains. We have recently shown that the substitution of two putative ca(2+)/calmodulin-dependent protein kinase ii (camk ii) phosphorylation sites, s261 and s266, by alanines in the third intracellular loop of the rat mu-opioid receptor (rmor1) confers resistance to camk ii-induced receptor desensitization. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-79686 |
Thr372 |
STRIRQNtRDHPSTA |
Homo sapiens |
|
| pmid |
sentence |
| 10908300 |
The decrease in mu-opioid receptor activity after chronic agonist exposure (1 microm [d-ala(2),n-mephe(4),gly-ol(5)]-enkephalin) is largely due to kinase-mediated phosphorylation of intracellular receptor domains. We have recently shown that the substitution of two putative ca(2+)/calmodulin-dependent protein kinase ii (camk ii) phosphorylation sites, s261 and s266, by alanines in the third intracellular loop of the rat mu-opioid receptor (rmor1) confers resistance to camk ii-induced receptor desensitization. |
|
| Publications: |
3 |
Organism: |
Homo Sapiens |
| Tissue: |
Kidney |
| + |
GRK2 | down-regulates activity
phosphorylation
|
OPRM1 |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-251458 |
Ser357 |
REFCIPTsSNIEQQN |
Homo sapiens |
|
| pmid |
sentence |
| 12123746 |
GRK2-mediated phosphorylation is involved in the development of agonist-induced μ-opioid receptor desensitization. two C-terminal amino acids, Ser355 and Thr357, are required for short-term homologous desensitization of μ-opioid receptors expressed in HEK 293 cells. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-249661 |
Ser358 |
EFCIPTSsNIEQQNS |
Homo sapiens |
HEK-293 Cell |
| pmid |
sentence |
| 12123746 |
These results suggest that two C-terminal amino acids, Ser(355) and Thr(357), are required for short-term homologous desensitization and agonist-induced phosphorylation of mu-opioid receptors expressed in HEK 293 cells |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-247782 |
Thr356 |
FREFCIPtSSNIEQQ |
Homo sapiens |
HEK-293 Cell |
| pmid |
sentence |
| 12123746 |
These results suggest that two C-terminal amino acids, Ser(355) and Thr(357), are required for short-term homologous desensitization and agonist-induced phosphorylation of mu-opioid receptors expressed in HEK 293 cells |
|
| Publications: |
3 |
Organism: |
Homo Sapiens |
| + |
GRK3 | down-regulates activity
phosphorylation
|
OPRM1 |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-247915 |
Thr182 |
VKALDFRtPRNAKII |
Xenopus laevis |
|
| pmid |
sentence |
| 11060299 |
These results demonstrate that the T180A mutation probably blocks GRK3- and arr3-mediated desensitization of MOR by preventing a critical agonist-dependent receptor phosphorylation and suggest a novel GRK3 site of regulation not yet described for other G-protein-coupled receptors |
|
| Publications: |
1 |
Organism: |
Xenopus Laevis |
| Tissue: |
Primary Oocyte |
| + |
2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexanol | up-regulates activity 
chemical activation
|
OPRM1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258149 |
|
|
Cricetulus longicaudatus |
CHO Cell |
| pmid |
sentence |
| 19282177 |
A series of novel high affinity opioid receptor ligands have been made whereby the phenolic-OH group of nalbuphine, naltrexone methiodide, 6-desoxonaltrexone, hydromorphone and naltrindole was replaced by a carboxamido group and the furan ring was opened to the corresponding 4-OH derivatives. These furan ring “open” derivatives display very high affinity for μ and κ receptors and much less affinity for δ. |
|
| Publications: |
1 |
Organism: |
Cricetulus Longicaudatus |
| + |
Dynorphin B | up-regulates activity
chemical activation
|
OPRM1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258798 |
|
|
Cricetulus griseus |
CHO Cell |
| pmid |
sentence |
| 9686407 |
Accordingly, for the OTDP, the binding affinity and activity of a large number of opiate compounds have been tested at μ-, δ-, and κ-opiate receptors. Binding studies were originally conducted in guinea pig brain membranes, and subsequent studies have been carried out in CHO cells transfected with human receptors. Table 7 shows a biochemical method for determining activity and potency of opioid compounds, stimulation of [35S]GTPγS binding in membranes from cells transfected with human μ, δ, or κ receptors. |
|
| Publications: |
1 |
Organism: |
Cricetulus Griseus |
| + |
naloxone | down-regulates activity
chemical inhibition
|
OPRM1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258941 |
|
|
Cricetulus griseus |
CHO Cell |
| pmid |
sentence |
| 9686407 |
Accordingly, for the OTDP, the binding affinity and activity of a large number of opiate compounds have been tested at μ-, δ-, and κ-opiate receptors. Binding studies were originally conducted in guinea pig brain membranes, and subsequent studies have been carried out in CHO cells transfected with human receptors. Table 7 shows a biochemical method for determining activity and potency of opioid compounds, stimulation of [35S]GTPγS binding in membranes from cells transfected with human μ, δ, or κ receptors. |
|
| Publications: |
1 |
Organism: |
Cricetulus Griseus |
| + |
OPRM1 | up-regulates activity
binding
|
GNAO1 |
0.63 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-256990 |
|
|
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. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-282440 |
|
|
Homo sapiens |
HEK-293A Cell |
| pmid |
sentence |
| 37742189 |
Here, we quantitatively measure the enzymatic activity of GPCRs in living cells and reveal the G protein selectivity of 124 GPCRs with the exact rank order of their G protein preference. Using this information, we establish a classification of GPCRs by functional selectivity, discover the existence of a G12/13-coupled receptor, G15-coupled receptors, and a variety of subclasses for Gi/o-, Gq-, and Gs-coupled receptors, culminating in development of the predictive algorithm of G protein selectivity. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-282174 |
|
|
Homo sapiens |
HEK-293A Cell |
| pmid |
sentence |
| 35302493 |
This study describes the development and validation of a genetically encoded ebBRET-based biosensor platform allowing live-cell mapping of GPCR-G protein coupling preferences covering 12 heterotrimeric G proteins. Profiling of 100 therapeutically relevant human GPCRs resulted in 1500 pathway-specific concentration-response curves and revealed a great diversity of coupling profiles ranging from exquisite selectivity to broad promiscuity.In our dataset, which is the first using unmodified GPCRs and Gα proteins (except for Gs), 29% of the receptors coupled to only one family, whereas others displayed more promiscuity by coupling to 2, 3, or 4 families (36%, 25%, and 10%, respectively). |
|
| Publications: |
3 |
Organism: |
Homo Sapiens |
| + |
codeine | up-regulates activity
chemical activation
|
OPRM1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258933 |
|
|
Cricetulus griseus |
CHO Cell |
| pmid |
sentence |
| 9686407 |
Accordingly, for the OTDP, the binding affinity and activity of a large number of opiate compounds have been tested at μ-, δ-, and κ-opiate receptors. Binding studies were originally conducted in guinea pig brain membranes, and subsequent studies have been carried out in CHO cells transfected with human receptors. Table 7 shows a biochemical method for determining activity and potency of opioid compounds, stimulation of [35S]GTPγS binding in membranes from cells transfected with human μ, δ, or κ receptors. |
|
| Publications: |
1 |
Organism: |
Cricetulus Griseus |
| + |
Ethylketocyclazocine | up-regulates activity
chemical activation
|
OPRM1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258780 |
|
|
Cricetulus griseus |
CHO Cell |
| pmid |
sentence |
| 9686407 |
Accordingly, for the OTDP, the binding affinity and activity of a large number of opiate compounds have been tested at μ-, δ-, and κ-opiate receptors. Binding studies were originally conducted in guinea pig brain membranes, and subsequent studies have been carried out in CHO cells transfected with human receptors. Table 7 shows a biochemical method for determining activity and potency of opioid compounds, stimulation of [35S]GTPγS binding in membranes from cells transfected with human μ, δ, or κ receptors. |
|
| Publications: |
1 |
Organism: |
Cricetulus Griseus |
| + |
Normorphine | up-regulates activity
chemical activation
|
OPRM1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258823 |
|
|
Cricetulus griseus |
CHO Cell |
| pmid |
sentence |
| 9686407 |
Accordingly, for the OTDP, the binding affinity and activity of a large number of opiate compounds have been tested at μ-, δ-, and κ-opiate receptors. Binding studies were originally conducted in guinea pig brain membranes, and subsequent studies have been carried out in CHO cells transfected with human receptors. Table 7 shows a biochemical method for determining activity and potency of opioid compounds, stimulation of [35S]GTPγS binding in membranes from cells transfected with human μ, δ, or κ receptors. |
|
| Publications: |
1 |
Organism: |
Cricetulus Griseus |
| + |
2-[[2-[[2-[[2-[[2-amino-3-(4-hydroxyphenyl)-1-oxopropyl]amino]-1-oxoethyl]amino]-1-oxoethyl]amino]-1-oxo-3-phenylpropyl]amino]-4-methylpentanoic acid | up-regulates activity
chemical activation
|
OPRM1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258805 |
|
|
Cricetulus griseus |
CHO Cell |
| pmid |
sentence |
| 9686407 |
Accordingly, for the OTDP, the binding affinity and activity of a large number of opiate compounds have been tested at μ-, δ-, and κ-opiate receptors. Binding studies were originally conducted in guinea pig brain membranes, and subsequent studies have been carried out in CHO cells transfected with human receptors. Table 7 shows a biochemical method for determining activity and potency of opioid compounds, stimulation of [35S]GTPγS binding in membranes from cells transfected with human μ, δ, or κ receptors. |
|
| Publications: |
1 |
Organism: |
Cricetulus Griseus |
| + |
Nalorphine | down-regulates activity
chemical inhibition
|
OPRM1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258813 |
|
|
Cricetulus griseus |
CHO Cell |
| pmid |
sentence |
| 9686407 |
Accordingly, for the OTDP, the binding affinity and activity of a large number of opiate compounds have been tested at μ-, δ-, and κ-opiate receptors. Binding studies were originally conducted in guinea pig brain membranes, and subsequent studies have been carried out in CHO cells transfected with human receptors. Table 7 shows a biochemical method for determining activity and potency of opioid compounds, stimulation of [35S]GTPγS binding in membranes from cells transfected with human μ, δ, or κ receptors. |
|
| Publications: |
1 |
Organism: |
Cricetulus Griseus |
| + |
levomethadone | up-regulates activity
chemical activation
|
OPRM1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258808 |
|
|
Cricetulus griseus |
CHO Cell |
| pmid |
sentence |
| 9686407 |
Accordingly, for the OTDP, the binding affinity and activity of a large number of opiate compounds have been tested at μ-, δ-, and κ-opiate receptors. Binding studies were originally conducted in guinea pig brain membranes, and subsequent studies have been carried out in CHO cells transfected with human receptors. Table 7 shows a biochemical method for determining activity and potency of opioid compounds, stimulation of [35S]GTPγS binding in membranes from cells transfected with human μ, δ, or κ receptors. |
|
| Publications: |
1 |
Organism: |
Cricetulus Griseus |
| + |
OPRM1 | up-regulates activity
binding
|
GNAI1 |
0.589 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-256711 |
|
|
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. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-281594 |
|
|
Homo sapiens |
HEK-293A Cell |
| pmid |
sentence |
| 31142646 |
Here, we directly assess coupling between 14 representative GPCRs and 16 Gα subunits, including one wild-type Gα subunit from each of the four families and 12 chimeras with exchanged C termini. We use a sensitive bioluminescence resonance energy transfer (BRET) assay that provides control over both ligand and nucleotide binding, and allows direct comparison across G protein families. We find that the Gs- and Gq-coupled receptors we studied are relatively promiscuous and always couple to some extent to Gi1 heterotrimers. In contrast, Gi-coupled receptors are more selective. Our results with Gα subunit chimeras show that the Gα C terminus is important for coupling selectivity, but no more so than the Gα subunit core. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-282050 |
|
|
Homo sapiens |
HEK-293A Cell |
| pmid |
sentence |
| 35302493 |
This study describes the development and validation of a genetically encoded ebBRET-based biosensor platform allowing live-cell mapping of GPCR-G protein coupling preferences covering 12 heterotrimeric G proteins. Profiling of 100 therapeutically relevant human GPCRs resulted in 1500 pathway-specific concentration-response curves and revealed a great diversity of coupling profiles ranging from exquisite selectivity to broad promiscuity.In our dataset, which is the first using unmodified GPCRs and Gα proteins (except for Gs), 29% of the receptors coupled to only one family, whereas others displayed more promiscuity by coupling to 2, 3, or 4 families (36%, 25%, and 10%, respectively). |
|
| Publications: |
3 |
Organism: |
Homo Sapiens |
| + |
(D-Ala(2)-mephe(4)-gly-ol(5))enkephalin | up-regulates activity
chemical activation
|
OPRM1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258783 |
|
|
Cricetulus griseus |
CHO Cell |
| pmid |
sentence |
| 9686407 |
Accordingly, for the OTDP, the binding affinity and activity of a large number of opiate compounds have been tested at μ-, δ-, and κ-opiate receptors. Binding studies were originally conducted in guinea pig brain membranes, and subsequent studies have been carried out in CHO cells transfected with human receptors. Table 7 shows a biochemical method for determining activity and potency of opioid compounds, stimulation of [35S]GTPγS binding in membranes from cells transfected with human μ, δ, or κ receptors. |
|
| Publications: |
1 |
Organism: |
Cricetulus Griseus |
| + |
Diprenorphine | down-regulates activity
chemical inhibition
|
OPRM1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258789 |
|
|
Cricetulus griseus |
CHO Cell |
| pmid |
sentence |
| 9686407 |
Accordingly, for the OTDP, the binding affinity and activity of a large number of opiate compounds have been tested at μ-, δ-, and κ-opiate receptors. Binding studies were originally conducted in guinea pig brain membranes, and subsequent studies have been carried out in CHO cells transfected with human receptors. Table 7 shows a biochemical method for determining activity and potency of opioid compounds, stimulation of [35S]GTPγS binding in membranes from cells transfected with human μ, δ, or κ receptors. |
|
| Publications: |
1 |
Organism: |
Cricetulus Griseus |
| + |
methylnaltrexone | down-regulates activity
chemical inhibition
|
OPRM1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258148 |
|
|
Cricetulus longicaudatus |
|
| pmid |
sentence |
| 19282177 |
A series of novel high affinity opioid receptor ligands have been made whereby the phenolic-OH group of nalbuphine, naltrexone methiodide, 6-desoxonaltrexone, hydromorphone and naltrindole was replaced by a carboxamido group and the furan ring was opened to the corresponding 4-OH derivatives. These furan ring “open” derivatives display very high affinity for μ and κ receptors and much less affinity for δ. |
|
| Publications: |
1 |
Organism: |
Cricetulus Longicaudatus |
| + |
etorphine | up-regulates activity
chemical activation
|
OPRM1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258804 |
|
|
Cricetulus griseus |
|
| pmid |
sentence |
| 9686407 |
Accordingly, for the OTDP, the binding affinity and activity of a large number of opiate compounds have been tested at μ-, δ-, and κ-opiate receptors. Binding studies were originally conducted in guinea pig brain membranes, and subsequent studies have been carried out in CHO cells transfected with human receptors. Table 7 shows a biochemical method for determining activity and potency of opioid compounds, stimulation of [35S]GTPγS binding in membranes from cells transfected with human μ, δ, or κ receptors. |
|
| Publications: |
1 |
Organism: |
Cricetulus Griseus |
| + |
Naltrindole | down-regulates activity
chemical inhibition
|
OPRM1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258818 |
|
|
Cricetulus griseus |
|
| pmid |
sentence |
| 9686407 |
Accordingly, for the OTDP, the binding affinity and activity of a large number of opiate compounds have been tested at μ-, δ-, and κ-opiate receptors. Binding studies were originally conducted in guinea pig brain membranes, and subsequent studies have been carried out in CHO cells transfected with human receptors. Table 7 shows a biochemical method for determining activity and potency of opioid compounds, stimulation of [35S]GTPγS binding in membranes from cells transfected with human μ, δ, or κ receptors. |
|
| Publications: |
1 |
Organism: |
Cricetulus Griseus |
| + |
Norbinaltorphimine | down-regulates activity
chemical inhibition
|
OPRM1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258821 |
|
|
Cricetulus griseus |
CHO Cell |
| pmid |
sentence |
| 9686407 |
Accordingly, for the OTDP, the binding affinity and activity of a large number of opiate compounds have been tested at μ-, δ-, and κ-opiate receptors. Binding studies were originally conducted in guinea pig brain membranes, and subsequent studies have been carried out in CHO cells transfected with human receptors. Table 7 shows a biochemical method for determining activity and potency of opioid compounds, stimulation of [35S]GTPγS binding in membranes from cells transfected with human μ, δ, or κ receptors. |
|
| Publications: |
1 |
Organism: |
Cricetulus Griseus |
| + |
MET-enkephalin | up-regulates activity
chemical activation
|
OPRM1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-257554 |
|
|
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 |
| + |
beta-Funaltrexamine | down-regulates activity
chemical inhibition
|
OPRM1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258773 |
|
|
Cricetulus griseus |
CHO Cell |
| pmid |
sentence |
| 9686407 |
Accordingly, for the OTDP, the binding affinity and activity of a large number of opiate compounds have been tested at μ-, δ-, and κ-opiate receptors. Binding studies were originally conducted in guinea pig brain membranes, and subsequent studies have been carried out in CHO cells transfected with human receptors. Table 7 shows a biochemical method for determining activity and potency of opioid compounds, stimulation of [35S]GTPγS binding in membranes from cells transfected with human μ, δ, or κ receptors. |
|
| Publications: |
1 |
Organism: |
Cricetulus Griseus |
| + |
Naloxone benzoylhydrazone | down-regulates activity
chemical inhibition
|
OPRM1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258422 |
|
|
Cricetulus griseus |
CHO Cell |
| pmid |
sentence |
| 9686407 |
Accordingly, for the OTDP, the binding affinity and activity of a large number of opiate compounds have been tested at μ-, δ-, and κ-opiate receptors. Binding studies were originally conducted in guinea pig brain membranes, and subsequent studies have been carried out in CHO cells transfected with human receptors. Table 7 shows a biochemical method for determining activity and potency of opioid compounds, stimulation of [35S]GTPγS binding in membranes from cells transfected with human μ, δ, or κ receptors. |
|
| Publications: |
1 |
Organism: |
Cricetulus Griseus |
| + |
Naltriben | down-regulates activity
chemical inhibition
|
OPRM1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258424 |
|
|
Cricetulus griseus |
CHO Cell |
| pmid |
sentence |
| 9686407 |
Accordingly, for the OTDP, the binding affinity and activity of a large number of opiate compounds have been tested at μ-, δ-, and κ-opiate receptors. Binding studies were originally conducted in guinea pig brain membranes, and subsequent studies have been carried out in CHO cells transfected with human receptors. Table 7 shows a biochemical method for determining activity and potency of opioid compounds, stimulation of [35S]GTPγS binding in membranes from cells transfected with human μ, δ, or κ receptors. |
|
| Publications: |
1 |
Organism: |
Cricetulus Griseus |
| + |
morphine | up-regulates activity
chemical activation
|
OPRM1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258765 |
|
|
Cricetulus griseus |
CHO Cell |
| pmid |
sentence |
| 9686407 |
Accordingly, for the OTDP, the binding affinity and activity of a large number of opiate compounds have been tested at μ-, δ-, and κ-opiate receptors. Binding studies were originally conducted in guinea pig brain membranes, and subsequent studies have been carried out in CHO cells transfected with human receptors. Table 7 shows a biochemical method for determining activity and potency of opioid compounds, stimulation of [35S]GTPγS binding in membranes from cells transfected with human μ, δ, or κ receptors. |
|
| Publications: |
1 |
Organism: |
Cricetulus Griseus |
| + |
Dihydromorphine | up-regulates activity
chemical activation
|
OPRM1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258787 |
|
|
Cricetulus griseus |
CHO Cell |
| pmid |
sentence |
| 9686407 |
Accordingly, for the OTDP, the binding affinity and activity of a large number of opiate compounds have been tested at μ-, δ-, and κ-opiate receptors. Binding studies were originally conducted in guinea pig brain membranes, and subsequent studies have been carried out in CHO cells transfected with human receptors. Table 7 shows a biochemical method for determining activity and potency of opioid compounds, stimulation of [35S]GTPγS binding in membranes from cells transfected with human μ, δ, or κ receptors. |
|
| Publications: |
1 |
Organism: |
Cricetulus Griseus |
| + |
naltrexone | down-regulates activity
chemical inhibition
|
OPRM1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258946 |
|
|
Cricetulus griseus |
CHO Cell |
| pmid |
sentence |
| 9686407 |
Accordingly, for the OTDP, the binding affinity and activity of a large number of opiate compounds have been tested at μ-, δ-, and κ-opiate receptors. Binding studies were originally conducted in guinea pig brain membranes, and subsequent studies have been carried out in CHO cells transfected with human receptors. Table 7 shows a biochemical method for determining activity and potency of opioid compounds, stimulation of [35S]GTPγS binding in membranes from cells transfected with human μ, δ, or κ receptors. |
|
| Publications: |
1 |
Organism: |
Cricetulus Griseus |
| + |
PPBP | down-regulates activity
chemical inhibition
|
OPRM1 |
0.371 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258413 |
|
|
Cricetulus griseus |
|
| pmid |
sentence |
| 9686407 |
Accordingly, for the OTDP, the binding affinity and activity of a large number of opiate compounds have been tested at μ-, δ-, and κ-opiate receptors. Binding studies were originally conducted in guinea pig brain membranes, and subsequent studies have been carried out in CHO cells transfected with human receptors. Table 7 shows a biochemical method for determining activity and potency of opioid compounds, stimulation of [35S]GTPγS binding in membranes from cells transfected with human μ, δ, or κ receptors. |
|
| Publications: |
1 |
Organism: |
Cricetulus Griseus |
| + |
nalbuphine | up-regulates activity
chemical activation
|
OPRM1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258041 |
|
|
Cricetulus longicaudatus |
CHO Cell |
| pmid |
sentence |
| 19282177 |
A series of novel high affinity opioid receptor ligands have been made whereby the phenolic-OH group of nalbuphine, naltrexone methiodide, 6-desoxonaltrexone, hydromorphone and naltrindole was replaced by a carboxamido group and the furan ring was opened to the corresponding 4-OH derivatives. These furan ring “open” derivatives display very high affinity for μ and κ receptors and much less affinity for δ. |
|
| Publications: |
1 |
Organism: |
Cricetulus Longicaudatus |
| + |
RPN1 | up-regulates
binding
|
OPRM1 |
0.255 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-184651 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 19289571 |
Ribophorin i (rpni), a component of the oligosaccharide transferase complex, could directly interact with mor. Rpni can be shown to participate in mor export by the intracellular retention of the receptor after small interfering rna knockdown of endogenous rpni. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
3-N-Me-Phe-morphiceptin | up-regulates activity
chemical activation
|
OPRM1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258417 |
|
|
Cricetulus griseus |
CHO Cell |
| pmid |
sentence |
| 9686407 |
Accordingly, for the OTDP, the binding affinity and activity of a large number of opiate compounds have been tested at μ-, δ-, and κ-opiate receptors. Binding studies were originally conducted in guinea pig brain membranes, and subsequent studies have been carried out in CHO cells transfected with human receptors. Table 7 shows a biochemical method for determining activity and potency of opioid compounds, stimulation of [35S]GTPγS binding in membranes from cells transfected with human μ, δ, or κ receptors. |
|
| Publications: |
1 |
Organism: |
Cricetulus Griseus |
| + |
Nalmefene | down-regulates activity
chemical inhibition
|
OPRM1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258810 |
|
|
Cricetulus griseus |
CHO Cell |
| pmid |
sentence |
| 9686407 |
Accordingly, for the OTDP, the binding affinity and activity of a large number of opiate compounds have been tested at μ-, δ-, and κ-opiate receptors. Binding studies were originally conducted in guinea pig brain membranes, and subsequent studies have been carried out in CHO cells transfected with human receptors. Table 7 shows a biochemical method for determining activity and potency of opioid compounds, stimulation of [35S]GTPγS binding in membranes from cells transfected with human μ, δ, or κ receptors. |
|
| Publications: |
1 |
Organism: |
Cricetulus Griseus |
| + |
PDYN | up-regulates activity
chemical activation
|
OPRM1 |
0.678 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258414 |
|
|
Cricetulus griseus |
CHO Cell |
| pmid |
sentence |
| 9686407 |
Accordingly, for the OTDP, the binding affinity and activity of a large number of opiate compounds have been tested at μ-, δ-, and κ-opiate receptors. Binding studies were originally conducted in guinea pig brain membranes, and subsequent studies have been carried out in CHO cells transfected with human receptors. Table 7 shows a biochemical method for determining activity and potency of opioid compounds, stimulation of [35S]GTPγS binding in membranes from cells transfected with human μ, δ, or κ receptors. |
|
| Publications: |
1 |
Organism: |
Cricetulus Griseus |
| + |
OPRM1 | up-regulates activity
binding
|
GNAI2 |
0.547 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-281936 |
|
|
Homo sapiens |
HEK-293A Cell |
| pmid |
sentence |
| 35302493 |
This study describes the development and validation of a genetically encoded ebBRET-based biosensor platform allowing live-cell mapping of GPCR-G protein coupling preferences covering 12 heterotrimeric G proteins. Profiling of 100 therapeutically relevant human GPCRs resulted in 1500 pathway-specific concentration-response curves and revealed a great diversity of coupling profiles ranging from exquisite selectivity to broad promiscuity.In our dataset, which is the first using unmodified GPCRs and Gα proteins (except for Gs), 29% of the receptors coupled to only one family, whereas others displayed more promiscuity by coupling to 2, 3, or 4 families (36%, 25%, and 10%, respectively). |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
OPRM1 | up-regulates activity
binding
|
GNAZ |
0.5 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-281937 |
|
|
Homo sapiens |
HEK-293A Cell |
| pmid |
sentence |
| 35302493 |
This study describes the development and validation of a genetically encoded ebBRET-based biosensor platform allowing live-cell mapping of GPCR-G protein coupling preferences covering 12 heterotrimeric G proteins. Profiling of 100 therapeutically relevant human GPCRs resulted in 1500 pathway-specific concentration-response curves and revealed a great diversity of coupling profiles ranging from exquisite selectivity to broad promiscuity.In our dataset, which is the first using unmodified GPCRs and Gα proteins (except for Gs), 29% of the receptors coupled to only one family, whereas others displayed more promiscuity by coupling to 2, 3, or 4 families (36%, 25%, and 10%, respectively). |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-257106 |
|
|
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: |
2 |
Organism: |
Homo Sapiens |
| + |
OPRM1 | up-regulates activity
binding
|
GNA15 |
0.455 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-281938 |
|
|
Homo sapiens |
HEK-293A Cell |
| pmid |
sentence |
| 35302493 |
This study describes the development and validation of a genetically encoded ebBRET-based biosensor platform allowing live-cell mapping of GPCR-G protein coupling preferences covering 12 heterotrimeric G proteins. Profiling of 100 therapeutically relevant human GPCRs resulted in 1500 pathway-specific concentration-response curves and revealed a great diversity of coupling profiles ranging from exquisite selectivity to broad promiscuity.In our dataset, which is the first using unmodified GPCRs and Gα proteins (except for Gs), 29% of the receptors coupled to only one family, whereas others displayed more promiscuity by coupling to 2, 3, or 4 families (36%, 25%, and 10%, respectively). |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
Dynorphin A | up-regulates activity
chemical activation
|
OPRM1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258793 |
|
|
Cricetulus griseus |
CHO Cell |
| pmid |
sentence |
| 9686407 |
Accordingly, for the OTDP, the binding affinity and activity of a large number of opiate compounds have been tested at μ-, δ-, and κ-opiate receptors. Binding studies were originally conducted in guinea pig brain membranes, and subsequent studies have been carried out in CHO cells transfected with human receptors. Table 7 shows a biochemical method for determining activity and potency of opioid compounds, stimulation of [35S]GTPγS binding in membranes from cells transfected with human μ, δ, or κ receptors. |
|
| Publications: |
1 |
Organism: |
Cricetulus Griseus |
| + |
Quadazocine | down-regulates activity
chemical inhibition
|
OPRM1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258420 |
|
|
Cricetulus griseus |
CHO Cell |
| pmid |
sentence |
| 9686407 |
Accordingly, for the OTDP, the binding affinity and activity of a large number of opiate compounds have been tested at μ-, δ-, and κ-opiate receptors. Binding studies were originally conducted in guinea pig brain membranes, and subsequent studies have been carried out in CHO cells transfected with human receptors. Table 7 shows a biochemical method for determining activity and potency of opioid compounds, stimulation of [35S]GTPγS binding in membranes from cells transfected with human μ, δ, or κ receptors. |
|
| Publications: |
1 |
Organism: |
Cricetulus Griseus |
| + |
sufentanil | up-regulates activity
chemical activation
|
OPRM1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-257890 |
|
|
Cricetulus longicaudatus |
|
| pmid |
sentence |
| 21215785 |
Experiments were conducted to obtain K(i)'s for 19 approved opioid drugs using a single binding assay in a cell membrane preparation expressing recombinant human MOR. The K(i) values obtained ranged from 0.1380 nM (sufentanil) to 12.486 μM (tramadol). |
|
| Publications: |
1 |
Organism: |
Cricetulus Longicaudatus |
| + |
buprenorphine | up-regulates activity
chemical activation
|
OPRM1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258940 |
|
|
Cricetulus griseus |
CHO Cell |
| pmid |
sentence |
| 9686407 |
Accordingly, for the OTDP, the binding affinity and activity of a large number of opiate compounds have been tested at μ-, δ-, and κ-opiate receptors. Binding studies were originally conducted in guinea pig brain membranes, and subsequent studies have been carried out in CHO cells transfected with human receptors. Table 7 shows a biochemical method for determining activity and potency of opioid compounds, stimulation of [35S]GTPγS binding in membranes from cells transfected with human μ, δ, or κ receptors. |
|
| Publications: |
1 |
Organism: |
Cricetulus Griseus |
| + |
alvimopan | down-regulates activity
chemical inhibition
|
OPRM1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-257773 |
|
|
in vitro |
|
| pmid |
sentence |
| 18313920 |
A series of N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines, l opioid receptor antagonists, analogs of alvimopan, were prepared using solid phase methodology. This study led to the identification of a highly selective l opioid receptor antagonist, which interacts selectively with l peripheral receptors. |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
pentazocine | up-regulates activity
chemical activation
|
OPRM1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258935 |
|
|
Cricetulus griseus |
CHO Cell |
| pmid |
sentence |
| 9686407 |
Accordingly, for the OTDP, the binding affinity and activity of a large number of opiate compounds have been tested at μ-, δ-, and κ-opiate receptors. Binding studies were originally conducted in guinea pig brain membranes, and subsequent studies have been carried out in CHO cells transfected with human receptors. Table 7 shows a biochemical method for determining activity and potency of opioid compounds, stimulation of [35S]GTPγS binding in membranes from cells transfected with human μ, δ, or κ receptors. |
|
| Publications: |
1 |
Organism: |
Cricetulus Griseus |
| + |
hydromorphone | up-regulates activity
chemical activation
|
OPRM1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258038 |
|
|
Cricetulus longicaudatus |
CHO Cell |
| pmid |
sentence |
| 19282177 |
A series of novel high affinity opioid receptor ligands have been made whereby the phenolic-OH group of nalbuphine, naltrexone methiodide, 6-desoxonaltrexone, hydromorphone and naltrindole was replaced by a carboxamido group and the furan ring was opened to the corresponding 4-OH derivatives. These furan ring “open” derivatives display very high affinity for μ and κ receptors and much less affinity for δ. |
|
| Publications: |
1 |
Organism: |
Cricetulus Longicaudatus |
| + |
(4R,4aS,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-6-(phenylmethylene)-1,2,4,5,7a,13-hexahydro-4,12-methanobenzofuro[3,2-e]isoquinoline-7-one | down-regulates activity
chemical inhibition
|
OPRM1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258774 |
|
|
Cricetulus griseus |
|
| pmid |
sentence |
| 9686407 |
Accordingly, for the OTDP, the binding affinity and activity of a large number of opiate compounds have been tested at μ-, δ-, and κ-opiate receptors. Binding studies were originally conducted in guinea pig brain membranes, and subsequent studies have been carried out in CHO cells transfected with human receptors. Table 7 shows a biochemical method for determining activity and potency of opioid compounds, stimulation of [35S]GTPγS binding in membranes from cells transfected with human μ, δ, or κ receptors. |
|
| Publications: |
1 |
Organism: |
Cricetulus Griseus |
| + |
OPRM1 | up-regulates activity
binding
|
GNAI3 |
0.498 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-256854 |
|
|
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 |
| + |
fentanyl | up-regulates activity
chemical activation
|
OPRM1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258937 |
|
|
Cricetulus griseus |
CHO Cell |
| pmid |
sentence |
| 9686407 |
Accordingly, for the OTDP, the binding affinity and activity of a large number of opiate compounds have been tested at μ-, δ-, and κ-opiate receptors. Binding studies were originally conducted in guinea pig brain membranes, and subsequent studies have been carried out in CHO cells transfected with human receptors. Table 7 shows a biochemical method for determining activity and potency of opioid compounds, stimulation of [35S]GTPγS binding in membranes from cells transfected with human μ, δ, or κ receptors. |
|
| Publications: |
1 |
Organism: |
Cricetulus Griseus |
| + |
bremazocine | down-regulates activity
chemical inhibition
|
OPRM1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258779 |
|
|
Cricetulus griseus |
CHO Cell |
| pmid |
sentence |
| 9686407 |
Accordingly, for the OTDP, the binding affinity and activity of a large number of opiate compounds have been tested at μ-, δ-, and κ-opiate receptors. Binding studies were originally conducted in guinea pig brain membranes, and subsequent studies have been carried out in CHO cells transfected with human receptors. Table 7 shows a biochemical method for determining activity and potency of opioid compounds, stimulation of [35S]GTPγS binding in membranes from cells transfected with human μ, δ, or κ receptors. |
|
| Publications: |
1 |
Organism: |
Cricetulus Griseus |
4.0
OPRM1
- 
- 