CHO
|
EC50 |
0.0027 μM
Compound: alpha-MSH
|
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
|
[PMID: 20329799]
|
CHO
|
EC50 |
1.1 nM
Compound: Alpha-MSH
|
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 3 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 3 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
|
[PMID: 15982875]
|
CHO
|
EC50 |
1.9 nM
Compound: Alpha-MSH
|
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
|
[PMID: 15982875]
|
CHO
|
IC50 |
118 nM
Compound: Alpha-MSH
|
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
|
[PMID: 15982875]
|
CHO
|
EC50 |
17 nM
Compound: Alpha-MSH
|
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
|
[PMID: 15982875]
|
CHO
|
IC50 |
19 nM
Compound: alpha-MSH
|
Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
|
[PMID: 15582434]
|
CHO
|
IC50 |
19 nM
Compound: Alpha-MSH
|
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
|
[PMID: 15982875]
|
CHO
|
IC50 |
19 nM
Compound: Alpha-MSH
|
Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
|
[PMID: 15982875]
|
CHO
|
EC50 |
2.2 nM
Compound: alpha-MSH
|
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
|
[PMID: 20329799]
|
HEK293
|
EC50 |
0.0009 μM
Compound: alpha-MSH
|
Agonist activity at human recombinant MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by enzyme fragment complementation assay
Agonist activity at human recombinant MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by enzyme fragment complementation assay
|
[PMID: 20329799]
|
HEK293
|
EC50 |
0.04 nM
Compound: alpha-MSH
|
Agonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP AlphaScreen assay
Agonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP AlphaScreen assay
|
[PMID: 32184956]
|
HEK293
|
EC50 |
0.14 nM
Compound: alpha-MSH
|
Agonist activity at mouse melanocortin 1 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
Agonist activity at mouse melanocortin 1 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
|
[PMID: 26433448]
|
HEK293
|
EC50 |
0.15 nM
Compound: alpha-MSH
|
Agonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
Agonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
|
[PMID: 26959173]
|
HEK293
|
EC50 |
0.22 nM
Compound: alpha-MSH
|
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
|
[PMID: 32184956]
|
HEK293
|
EC50 |
0.22 nM
Compound: alpha-MSH
|
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
|
[PMID: 32184956]
|
HEK293
|
EC50 |
0.22 nM
Compound: alpha-MSH
|
Agonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
Agonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
|
[PMID: 26005535]
|
HEK293
|
EC50 |
0.28 nM
Compound: alpha-MSH
|
Agonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase assay
Agonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase assay
|
[PMID: 15615519]
|
HEK293
|
EC50 |
0.3 nM
Compound: alpha-MSH
|
Agonist activity at mouse MC1 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
Agonist activity at mouse MC1 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
|
[PMID: 26005535]
|
HEK293
|
EC50 |
0.36 μM
Compound: alpha-MSH
|
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
|
[PMID: 20329799]
|
HEK293
|
EC50 |
0.4 nM
Compound: alpha-MSH
|
Agonist activity at mouse MC3 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
Agonist activity at mouse MC3 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
|
[PMID: 26005535]
|
HEK293
|
EC50 |
0.5 nM
Compound: alpha-MSH
|
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
|
[PMID: 26433448]
|
HEK293
|
EC50 |
0.51 nM
Compound: alpha-MSH
|
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
|
[PMID: 26433448]
|
HEK293
|
EC50 |
0.52 nM
Compound: alpha-MSH
|
Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assay
Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assay
|
[PMID: 15615519]
|
HEK293
|
EC50 |
0.59 nM
Compound: alpha-MSH
|
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
|
[PMID: 26959173]
|
HEK293
|
EC50 |
0.65 nM
Compound: alpha-MSH
|
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
|
[PMID: 24517312]
|
HEK293
|
EC50 |
0.7 nM
Compound: alpha-MSH
|
Agonist activity at mouse MC1R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
Agonist activity at mouse MC1R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
|
[PMID: 18271518]
|
HEK293
|
EC50 |
0.76 nM
Compound: alpha-MSH
|
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
|
[PMID: 26959173]
|
HEK293
|
EC50 |
1.12 nM
Compound: alpha-MSH
|
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
|
[PMID: 15615519]
|
HEK293
|
EC50 |
1.7 nM
Compound: alpha-MSH
|
Agonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
Agonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
|
[PMID: 26005535]
|
HEK293
|
EC50 |
1.8 nM
Compound: alpha-MSH
|
Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation
Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation
|
[PMID: 16451057]
|
HEK293
|
EC50 |
1.89 nM
Compound: alpha-MSH
|
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay
|
[PMID: 15615519]
|
HEK293
|
EC50 |
156 nM
Compound: alpha-MSH
|
Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation
Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation
|
[PMID: 16451057]
|
HEK293
|
EC50 |
16.7 nM
Compound: alpha-MSH
|
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
|
[PMID: 28972753]
|
HEK293
|
EC50 |
18 nM
Compound: alpha-MSH
|
Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation
Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation
|
[PMID: 16451057]
|
HEK293
|
EC50 |
|
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
|
[PMID: 18271518]
|
HEK293
|
EC50 |
2.14 nM
Compound: alpha-MSH
|
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
|
[PMID: 18271518]
|
HEK293
|
EC50 |
2.56 nM
Compound: alpha-MSH
|
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
|
[PMID: 18271518]
|
HEK293
|
EC50 |
2.6 nM
Compound: alpha-MSH
|
Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation
Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation
|
[PMID: 16451057]
|
HEK293
|
EC50 |
2.9 nM
Compound: alpha-MSH
|
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
|
[PMID: 26433448]
|
HEK293
|
EC50 |
2.9 nM
Compound: alpha-MSH
|
Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation
Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation
|
[PMID: 16451057]
|
HEK293
|
EC50 |
21 nM
Compound: alpha-MSH
|
Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation
Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation
|
[PMID: 16451057]
|
HEK293
|
EC50 |
21 nM
Compound: alpha-MSH
|
Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation
Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation
|
[PMID: 16451057]
|
HEK293
|
EC50 |
24.4 nM
Compound: alpha-MSH
|
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay
|
[PMID: 28972753]
|
HEK293
|
EC50 |
27 nM
Compound: alpha-MSH
|
Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation
Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation
|
[PMID: 16451057]
|
HEK293
|
EC50 |
3.7 nM
Compound: alpha-MSH
|
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
|
[PMID: 32184956]
|
HEK293
|
EC50 |
35.3 nM
Compound: alpha-MSH
|
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
|
[PMID: 28972753]
|
HEK293
|
EC50 |
|
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
|
[PMID: 26959173]
|
HEK293
|
EC50 |
7.1 nM
Compound: alpha-MSH
|
Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation
Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation
|
[PMID: 16451057]
|
HEK293
|
EC50 |
89 nM
Compound: alpha-MSH
|
Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation
Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation
|
[PMID: 16451057]
|
HEK293
|
EC50 |
9.2 nM
Compound: alpha-MSH
|
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
|
[PMID: 28972753]
|
SAOS-2
|
EC50 |
1.8 nM
Compound: alpha-MSH
|
Activity at human MC1R by cAMP accumulation in SaoS2 cells
Activity at human MC1R by cAMP accumulation in SaoS2 cells
|
[PMID: 16678415]
|
SAOS-2
|
EC50 |
72.9 nM
Compound: alpha-MSH
|
Activity at human MC4R by cAMP accumulation in SaoS2 cells
Activity at human MC4R by cAMP accumulation in SaoS2 cells
|
[PMID: 16678415]
|