Ligand source activities (1 row/activity)
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
| 1324 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 11 | 11.0 | 1 | 8 | Agonist activity against mouse MC1R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assayAgonist activity against mouse MC1R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.3c00432 | ||||
| 16154396 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 11 | 11.0 | 1 | 8 | Agonist activity against mouse MC1R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assayAgonist activity against mouse MC1R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.3c00432 | ||||
| 16197727 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 11 | 11.0 | 1 | 8 | Agonist activity against mouse MC1R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assayAgonist activity against mouse MC1R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.3c00432 | ||||
| 16197727.0 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 11 | 11.0 | 1 | 8 | Agonist activity against mouse MC1R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assayAgonist activity against mouse MC1R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.3c00432 | ||||
| 44285019 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 11 | 11.0 | 1 | 8 | Agonist activity against mouse MC1R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assayAgonist activity against mouse MC1R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.3c00432 | ||||
| 57514683 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 11 | 11.0 | 1 | 8 | Agonist activity against mouse MC1R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assayAgonist activity against mouse MC1R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.3c00432 | ||||
| 91898441 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 11 | 11.0 | 1 | 8 | Agonist activity against mouse MC1R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assayAgonist activity against mouse MC1R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.3c00432 | ||||
| CHEMBL441738 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 11 | 11.0 | 1 | 8 | Agonist activity against mouse MC1R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assayAgonist activity against mouse MC1R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.3c00432 | ||||
| DB04931 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 11 | 11.0 | 1 | 8 | Agonist activity against mouse MC1R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assayAgonist activity against mouse MC1R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.3c00432 | ||||
| 137653739 | 158787 | None | 0 | Human | Functional | pEC50 | = | 11 | 11.0 | 28 | 4 | Agonist activity at human MC1R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation measured after 3 minsAgonist activity at human MC1R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation measured after 3 mins |
ChEMBL | 1632 | 51 | 23 | 21 | -3.6 | CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)CN[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C | 10.1021/acs.jmedchem.7b01295 | ||
| CHEMBL4093140 | 158787 | None | 0 | Human | Functional | pEC50 | = | 11 | 11.0 | 28 | 4 | Agonist activity at human MC1R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation measured after 3 minsAgonist activity at human MC1R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation measured after 3 mins |
ChEMBL | 1632 | 51 | 23 | 21 | -3.6 | CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)CN[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C | 10.1021/acs.jmedchem.7b01295 | ||
| 1324 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 11 | 11.0 | 1 | 8 | Agonist activity at mouse MC1R by alphascreen cAMP assayAgonist activity at mouse MC1R by alphascreen cAMP assay |
ChEMBL | None | None | None | None | 10.1021/acsmedchemlett.9b00641 | ||||
| 16154396 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 11 | 11.0 | 1 | 8 | Agonist activity at mouse MC1R by alphascreen cAMP assayAgonist activity at mouse MC1R by alphascreen cAMP assay |
ChEMBL | None | None | None | None | 10.1021/acsmedchemlett.9b00641 | ||||
| 16197727 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 11 | 11.0 | 1 | 8 | Agonist activity at mouse MC1R by alphascreen cAMP assayAgonist activity at mouse MC1R by alphascreen cAMP assay |
ChEMBL | None | None | None | None | 10.1021/acsmedchemlett.9b00641 | ||||
| 16197727.0 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 11 | 11.0 | 1 | 8 | Agonist activity at mouse MC1R by alphascreen cAMP assayAgonist activity at mouse MC1R by alphascreen cAMP assay |
ChEMBL | None | None | None | None | 10.1021/acsmedchemlett.9b00641 | ||||
| 44285019 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 11 | 11.0 | 1 | 8 | Agonist activity at mouse MC1R by alphascreen cAMP assayAgonist activity at mouse MC1R by alphascreen cAMP assay |
ChEMBL | None | None | None | None | 10.1021/acsmedchemlett.9b00641 | ||||
| 57514683 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 11 | 11.0 | 1 | 8 | Agonist activity at mouse MC1R by alphascreen cAMP assayAgonist activity at mouse MC1R by alphascreen cAMP assay |
ChEMBL | None | None | None | None | 10.1021/acsmedchemlett.9b00641 | ||||
| 91898441 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 11 | 11.0 | 1 | 8 | Agonist activity at mouse MC1R by alphascreen cAMP assayAgonist activity at mouse MC1R by alphascreen cAMP assay |
ChEMBL | None | None | None | None | 10.1021/acsmedchemlett.9b00641 | ||||
| CHEMBL441738 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 11 | 11.0 | 1 | 8 | Agonist activity at mouse MC1R by alphascreen cAMP assayAgonist activity at mouse MC1R by alphascreen cAMP assay |
ChEMBL | None | None | None | None | 10.1021/acsmedchemlett.9b00641 | ||||
| DB04931 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 11 | 11.0 | 1 | 8 | Agonist activity at mouse MC1R by alphascreen cAMP assayAgonist activity at mouse MC1R by alphascreen cAMP assay |
ChEMBL | None | None | None | None | 10.1021/acsmedchemlett.9b00641 | ||||
| 1324 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 11 | 11.0 | 1 | 8 | Agonist activity at mouse MC1R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assayAgonist activity at mouse MC1R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.8b00684 | ||||
| 16154396 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 11 | 11.0 | 1 | 8 | Agonist activity at mouse MC1R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assayAgonist activity at mouse MC1R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.8b00684 | ||||
| 16197727 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 11 | 11.0 | 1 | 8 | Agonist activity at mouse MC1R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assayAgonist activity at mouse MC1R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.8b00684 | ||||
| 16197727.0 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 11 | 11.0 | 1 | 8 | Agonist activity at mouse MC1R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assayAgonist activity at mouse MC1R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.8b00684 | ||||
| 44285019 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 11 | 11.0 | 1 | 8 | Agonist activity at mouse MC1R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assayAgonist activity at mouse MC1R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.8b00684 | ||||
| 57514683 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 11 | 11.0 | 1 | 8 | Agonist activity at mouse MC1R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assayAgonist activity at mouse MC1R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.8b00684 | ||||
| 91898441 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 11 | 11.0 | 1 | 8 | Agonist activity at mouse MC1R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assayAgonist activity at mouse MC1R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.8b00684 | ||||
| CHEMBL441738 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 11 | 11.0 | 1 | 8 | Agonist activity at mouse MC1R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assayAgonist activity at mouse MC1R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.8b00684 | ||||
| DB04931 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 11 | 11.0 | 1 | 8 | Agonist activity at mouse MC1R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assayAgonist activity at mouse MC1R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.8b00684 | ||||
| 1324 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 11 | 11.0 | 1 | 8 | Agonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.9b00860 | ||||
| 16154396 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 11 | 11.0 | 1 | 8 | Agonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.9b00860 | ||||
| 16197727 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 11 | 11.0 | 1 | 8 | Agonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.9b00860 | ||||
| 16197727.0 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 11 | 11.0 | 1 | 8 | Agonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.9b00860 | ||||
| 44285019 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 11 | 11.0 | 1 | 8 | Agonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.9b00860 | ||||
| 57514683 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 11 | 11.0 | 1 | 8 | Agonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.9b00860 | ||||
| 91898441 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 11 | 11.0 | 1 | 8 | Agonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.9b00860 | ||||
| CHEMBL441738 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 11 | 11.0 | 1 | 8 | Agonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.9b00860 | ||||
| DB04931 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 11 | 11.0 | 1 | 8 | Agonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay |
ChEMBL | None | None | None | None | 10.1021/acs.jmedchem.9b00860 | ||||
| 45487403 | 199891 | None | 0 | Human | Functional | pEC50 | = | 11 | 11.0 | 33 | 4 | Agonistic activity against human MC1RAgonistic activity against human MC1R |
ChEMBL | 788 | 22 | 9 | 7 | 2.4 | N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](CC1=CN=CC1)NC(=O)CCCc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(N)=O | 10.1016/j.bmcl.2009.07.025 | ||
| CHEMBL569693 | 199891 | None | 0 | Human | Functional | pEC50 | = | 11 | 11.0 | 33 | 4 | Agonistic activity against human MC1RAgonistic activity against human MC1R |
ChEMBL | 788 | 22 | 9 | 7 | 2.4 | N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](CC1=CN=CC1)NC(=O)CCCc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(N)=O | 10.1016/j.bmcl.2009.07.025 | ||
| 88944368 | 143589 | None | 0 | Human | Functional | pEC50 | = | 11 | 11.0 | - | 1 | cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in a human melanoma cell line, HBL, that express hMCR-1 (see Kang, L., et al., A selective small molecule agonist of melanocortin-1 receptor inhibits lipopolysaccharide-induced cytokine accumulation and leukocyte infiltration in mice, J. Leuk. Biol. 80:897-904 (2006)) or HEK-293 cells that express hMCR-4. Confluent HBL cells that express hMCR-1 or HEK-293 cells that express recombinant hMCR-4 were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.4ÿ105 cells per well for HBL cells and 0.5x105 cells per well for HEK-293 cells and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a Perkin-Elmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. Maximum efficacy (Emax) values were determined for each test peptide of the present invention, compared to that achieved by the reference melanocortin agonist NDP-α-MSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in a human melanoma cell line, HBL, that express hMCR-1 (see Kang, L., et al., A selective small molecule agonist of melanocortin-1 receptor inhibits lipopolysaccharide-induced cytokine accumulation and leukocyte infiltration in mice, J. Leuk. Biol. 80:897-904 (2006)) or HEK-293 cells that express hMCR-4. Confluent HBL cells that express hMCR-1 or HEK-293 cells that express recombinant hMCR-4 were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.4ÿ105 cells per well for HBL cells and 0.5x105 cells per well for HEK-293 cells and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a Perkin-Elmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. Maximum efficacy (Emax) values were determined for each test peptide of the present invention, compared to that achieved by the reference melanocortin agonist NDP-α-MSH. |
ChEMBL | 1044 | 18 | 14 | 11 | -1.4 | CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O | nan | ||
| CHEMBL3898758 | 143589 | None | 0 | Human | Functional | pEC50 | = | 11 | 11.0 | - | 1 | cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in a human melanoma cell line, HBL, that express hMCR-1 (see Kang, L., et al., A selective small molecule agonist of melanocortin-1 receptor inhibits lipopolysaccharide-induced cytokine accumulation and leukocyte infiltration in mice, J. Leuk. Biol. 80:897-904 (2006)) or HEK-293 cells that express hMCR-4. Confluent HBL cells that express hMCR-1 or HEK-293 cells that express recombinant hMCR-4 were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.4ÿ105 cells per well for HBL cells and 0.5x105 cells per well for HEK-293 cells and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a Perkin-Elmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. Maximum efficacy (Emax) values were determined for each test peptide of the present invention, compared to that achieved by the reference melanocortin agonist NDP-α-MSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in a human melanoma cell line, HBL, that express hMCR-1 (see Kang, L., et al., A selective small molecule agonist of melanocortin-1 receptor inhibits lipopolysaccharide-induced cytokine accumulation and leukocyte infiltration in mice, J. Leuk. Biol. 80:897-904 (2006)) or HEK-293 cells that express hMCR-4. Confluent HBL cells that express hMCR-1 or HEK-293 cells that express recombinant hMCR-4 were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.4ÿ105 cells per well for HBL cells and 0.5x105 cells per well for HEK-293 cells and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a Perkin-Elmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. Maximum efficacy (Emax) values were determined for each test peptide of the present invention, compared to that achieved by the reference melanocortin agonist NDP-α-MSH. |
ChEMBL | 1044 | 18 | 14 | 11 | -1.4 | CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O | nan | ||
| 88944179 | 151141 | None | 0 | Human | Functional | pEC50 | = | 10.9 | 10.9 | - | 1 | cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in a human melanoma cell line, HBL, that express hMCR-1 (see Kang, L., et al., A selective small molecule agonist of melanocortin-1 receptor inhibits lipopolysaccharide-induced cytokine accumulation and leukocyte infiltration in mice, J. Leuk. Biol. 80:897-904 (2006)) or HEK-293 cells that express hMCR-4. Confluent HBL cells that express hMCR-1 or HEK-293 cells that express recombinant hMCR-4 were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.4ÿ105 cells per well for HBL cells and 0.5x105 cells per well for HEK-293 cells and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a Perkin-Elmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. Maximum efficacy (Emax) values were determined for each test peptide of the present invention, compared to that achieved by the reference melanocortin agonist NDP-α-MSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in a human melanoma cell line, HBL, that express hMCR-1 (see Kang, L., et al., A selective small molecule agonist of melanocortin-1 receptor inhibits lipopolysaccharide-induced cytokine accumulation and leukocyte infiltration in mice, J. Leuk. Biol. 80:897-904 (2006)) or HEK-293 cells that express hMCR-4. Confluent HBL cells that express hMCR-1 or HEK-293 cells that express recombinant hMCR-4 were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.4ÿ105 cells per well for HBL cells and 0.5x105 cells per well for HEK-293 cells and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a Perkin-Elmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. Maximum efficacy (Emax) values were determined for each test peptide of the present invention, compared to that achieved by the reference melanocortin agonist NDP-α-MSH. |
ChEMBL | 924 | 16 | 13 | 10 | -1.3 | CCCC(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O | nan | ||
| CHEMBL3958741 | 151141 | None | 0 | Human | Functional | pEC50 | = | 10.9 | 10.9 | - | 1 | cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in a human melanoma cell line, HBL, that express hMCR-1 (see Kang, L., et al., A selective small molecule agonist of melanocortin-1 receptor inhibits lipopolysaccharide-induced cytokine accumulation and leukocyte infiltration in mice, J. Leuk. Biol. 80:897-904 (2006)) or HEK-293 cells that express hMCR-4. Confluent HBL cells that express hMCR-1 or HEK-293 cells that express recombinant hMCR-4 were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.4ÿ105 cells per well for HBL cells and 0.5x105 cells per well for HEK-293 cells and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a Perkin-Elmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. Maximum efficacy (Emax) values were determined for each test peptide of the present invention, compared to that achieved by the reference melanocortin agonist NDP-α-MSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in a human melanoma cell line, HBL, that express hMCR-1 (see Kang, L., et al., A selective small molecule agonist of melanocortin-1 receptor inhibits lipopolysaccharide-induced cytokine accumulation and leukocyte infiltration in mice, J. Leuk. Biol. 80:897-904 (2006)) or HEK-293 cells that express hMCR-4. Confluent HBL cells that express hMCR-1 or HEK-293 cells that express recombinant hMCR-4 were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.4ÿ105 cells per well for HBL cells and 0.5x105 cells per well for HEK-293 cells and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a Perkin-Elmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. Maximum efficacy (Emax) values were determined for each test peptide of the present invention, compared to that achieved by the reference melanocortin agonist NDP-α-MSH. |
ChEMBL | 924 | 16 | 13 | 10 | -1.3 | CCCC(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O | nan | ||
| 1324 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 10.9 | 10.9 | 1 | 8 | Agonistic activity against mouse MC1RAgonistic activity against mouse MC1R |
ChEMBL | None | None | None | None | 10.1016/j.bmcl.2009.07.025 | ||||
| 16154396 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 10.9 | 10.9 | 1 | 8 | Agonistic activity against mouse MC1RAgonistic activity against mouse MC1R |
ChEMBL | None | None | None | None | 10.1016/j.bmcl.2009.07.025 | ||||
| 16197727 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 10.9 | 10.9 | 1 | 8 | Agonistic activity against mouse MC1RAgonistic activity against mouse MC1R |
ChEMBL | None | None | None | None | 10.1016/j.bmcl.2009.07.025 | ||||
| 16197727.0 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 10.9 | 10.9 | 1 | 8 | Agonistic activity against mouse MC1RAgonistic activity against mouse MC1R |
ChEMBL | None | None | None | None | 10.1016/j.bmcl.2009.07.025 | ||||
| 44285019 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 10.9 | 10.9 | 1 | 8 | Agonistic activity against mouse MC1RAgonistic activity against mouse MC1R |
ChEMBL | None | None | None | None | 10.1016/j.bmcl.2009.07.025 | ||||
| 57514683 | 302 | None | 19 | Mouse | Functional | pEC50 | = | 10.9 | 10.9 | 1 | 8 | Agonistic activity against mouse MC1RAgonistic activity against mouse MC1R |
ChEMBL | None | None | None | None | 10.1016/j.bmcl.2009.07.025 | ||||
Showing 1 to 50 of 2,522 entries
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
| 1324 | 302 | None | 19 | Mouse | Binding | pEC50 | = | 10.7 | 10.7 | - | 4 | Effective concentration for mouse Melanocortin-1 receptorEffective concentration for mouse Melanocortin-1 receptor |
ChEMBL | None | None | None | None | 10.1021/jm049010r | ||||
| 16154396 | 302 | None | 19 | Mouse | Binding | pEC50 | = | 10.7 | 10.7 | - | 4 | Effective concentration for mouse Melanocortin-1 receptorEffective concentration for mouse Melanocortin-1 receptor |
ChEMBL | None | None | None | None | 10.1021/jm049010r | ||||
| 16197727 | 302 | None | 19 | Mouse | Binding | pEC50 | = | 10.7 | 10.7 | - | 4 | Effective concentration for mouse Melanocortin-1 receptorEffective concentration for mouse Melanocortin-1 receptor |
ChEMBL | None | None | None | None | 10.1021/jm049010r | ||||
| 16197727.0 | 302 | None | 19 | Mouse | Binding | pEC50 | = | 10.7 | 10.7 | - | 4 | Effective concentration for mouse Melanocortin-1 receptorEffective concentration for mouse Melanocortin-1 receptor |
ChEMBL | None | None | None | None | 10.1021/jm049010r | ||||
| 44285019 | 302 | None | 19 | Mouse | Binding | pEC50 | = | 10.7 | 10.7 | - | 4 | Effective concentration for mouse Melanocortin-1 receptorEffective concentration for mouse Melanocortin-1 receptor |
ChEMBL | None | None | None | None | 10.1021/jm049010r | ||||
| 57514683 | 302 | None | 19 | Mouse | Binding | pEC50 | = | 10.7 | 10.7 | - | 4 | Effective concentration for mouse Melanocortin-1 receptorEffective concentration for mouse Melanocortin-1 receptor |
ChEMBL | None | None | None | None | 10.1021/jm049010r | ||||
| 91898441 | 302 | None | 19 | Mouse | Binding | pEC50 | = | 10.7 | 10.7 | - | 4 | Effective concentration for mouse Melanocortin-1 receptorEffective concentration for mouse Melanocortin-1 receptor |
ChEMBL | None | None | None | None | 10.1021/jm049010r | ||||
| CHEMBL441738 | 302 | None | 19 | Mouse | Binding | pEC50 | = | 10.7 | 10.7 | - | 4 | Effective concentration for mouse Melanocortin-1 receptorEffective concentration for mouse Melanocortin-1 receptor |
ChEMBL | None | None | None | None | 10.1021/jm049010r | ||||
| DB04931 | 302 | None | 19 | Mouse | Binding | pEC50 | = | 10.7 | 10.7 | - | 4 | Effective concentration for mouse Melanocortin-1 receptorEffective concentration for mouse Melanocortin-1 receptor |
ChEMBL | None | None | None | None | 10.1021/jm049010r | ||||
| 1323 | 2688 | None | 38 | Mouse | Binding | pEC50 | = | 10.7 | 10.7 | - | 4 | Activity in mouse melanocortin-1 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-1 receptor stably expressed in HEK293 cells |
ChEMBL | None | None | None | None | 10.1021/jm020296e | ||||
| 92432 | 2688 | None | 38 | Mouse | Binding | pEC50 | = | 10.7 | 10.7 | - | 4 | Activity in mouse melanocortin-1 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-1 receptor stably expressed in HEK293 cells |
ChEMBL | None | None | None | None | 10.1021/jm020296e | ||||
| CHEMBL430239 | 2688 | None | 38 | Mouse | Binding | pEC50 | = | 10.7 | 10.7 | - | 4 | Activity in mouse melanocortin-1 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-1 receptor stably expressed in HEK293 cells |
ChEMBL | None | None | None | None | 10.1021/jm020296e | ||||
| 44327392 | 141950 | None | 0 | Mouse | Binding | pEC50 | = | 10.7 | 10.7 | - | 0 | In vitro activation of mouse recombinant Melanocortin-1 receptor.In vitro activation of mouse recombinant Melanocortin-1 receptor. |
ChEMBL | 1025 | 21 | 12 | 12 | -0.6 | CCCC[C@H](NC(C)=O)C(=O)N1C(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H]1CC(=O)O | 10.1021/jm0104872 | ||
| CHEMBL386583 | 141950 | None | 0 | Mouse | Binding | pEC50 | = | 10.7 | 10.7 | - | 0 | In vitro activation of mouse recombinant Melanocortin-1 receptor.In vitro activation of mouse recombinant Melanocortin-1 receptor. |
ChEMBL | 1025 | 21 | 12 | 12 | -0.6 | CCCC[C@H](NC(C)=O)C(=O)N1C(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H]1CC(=O)O | 10.1021/jm0104872 | ||
| 1323 | 2688 | None | 38 | Mouse | Binding | pEC50 | = | 10.7 | 10.7 | - | 4 | Effective concentration for mouse Melanocortin-1 receptorEffective concentration for mouse Melanocortin-1 receptor |
ChEMBL | None | None | None | None | 10.1021/jm049010r | ||||
| 92432 | 2688 | None | 38 | Mouse | Binding | pEC50 | = | 10.7 | 10.7 | - | 4 | Effective concentration for mouse Melanocortin-1 receptorEffective concentration for mouse Melanocortin-1 receptor |
ChEMBL | None | None | None | None | 10.1021/jm049010r | ||||
| CHEMBL430239 | 2688 | None | 38 | Mouse | Binding | pEC50 | = | 10.7 | 10.7 | - | 4 | Effective concentration for mouse Melanocortin-1 receptorEffective concentration for mouse Melanocortin-1 receptor |
ChEMBL | None | None | None | None | 10.1021/jm049010r | ||||
| 1324 | 302 | None | 19 | Human | Binding | pEC50 | = | 10.6 | 10.6 | 2 | 4 | Effective concentration required for the biological activity against human Melanocortin 1 receptorEffective concentration required for the biological activity against human Melanocortin 1 receptor |
ChEMBL | None | None | None | None | 10.1021/jm0303103 | ||||
| 16154396 | 302 | None | 19 | Human | Binding | pEC50 | = | 10.6 | 10.6 | 2 | 4 | Effective concentration required for the biological activity against human Melanocortin 1 receptorEffective concentration required for the biological activity against human Melanocortin 1 receptor |
ChEMBL | None | None | None | None | 10.1021/jm0303103 | ||||
| 16197727 | 302 | None | 19 | Human | Binding | pEC50 | = | 10.6 | 10.6 | 2 | 4 | Effective concentration required for the biological activity against human Melanocortin 1 receptorEffective concentration required for the biological activity against human Melanocortin 1 receptor |
ChEMBL | None | None | None | None | 10.1021/jm0303103 | ||||
| 16197727.0 | 302 | None | 19 | Human | Binding | pEC50 | = | 10.6 | 10.6 | 2 | 4 | Effective concentration required for the biological activity against human Melanocortin 1 receptorEffective concentration required for the biological activity against human Melanocortin 1 receptor |
ChEMBL | None | None | None | None | 10.1021/jm0303103 | ||||
| 44285019 | 302 | None | 19 | Human | Binding | pEC50 | = | 10.6 | 10.6 | 2 | 4 | Effective concentration required for the biological activity against human Melanocortin 1 receptorEffective concentration required for the biological activity against human Melanocortin 1 receptor |
ChEMBL | None | None | None | None | 10.1021/jm0303103 | ||||
| 57514683 | 302 | None | 19 | Human | Binding | pEC50 | = | 10.6 | 10.6 | 2 | 4 | Effective concentration required for the biological activity against human Melanocortin 1 receptorEffective concentration required for the biological activity against human Melanocortin 1 receptor |
ChEMBL | None | None | None | None | 10.1021/jm0303103 | ||||
| 91898441 | 302 | None | 19 | Human | Binding | pEC50 | = | 10.6 | 10.6 | 2 | 4 | Effective concentration required for the biological activity against human Melanocortin 1 receptorEffective concentration required for the biological activity against human Melanocortin 1 receptor |
ChEMBL | None | None | None | None | 10.1021/jm0303103 | ||||
| CHEMBL441738 | 302 | None | 19 | Human | Binding | pEC50 | = | 10.6 | 10.6 | 2 | 4 | Effective concentration required for the biological activity against human Melanocortin 1 receptorEffective concentration required for the biological activity against human Melanocortin 1 receptor |
ChEMBL | None | None | None | None | 10.1021/jm0303103 | ||||
| DB04931 | 302 | None | 19 | Human | Binding | pEC50 | = | 10.6 | 10.6 | 2 | 4 | Effective concentration required for the biological activity against human Melanocortin 1 receptorEffective concentration required for the biological activity against human Melanocortin 1 receptor |
ChEMBL | None | None | None | None | 10.1021/jm0303103 | ||||
| CHEMBL2096742 | 211665 | None | 0 | Human | Binding | pEC50 | = | 10.4 | 10.4 | - | 2 | Effective concentration required for the biological activity against human Melanocortin 1 receptorEffective concentration required for the biological activity against human Melanocortin 1 receptor |
ChEMBL | None | None | None | CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O | 10.1021/jm0303103 | ||||
| 1324 | 302 | None | 19 | Mouse | Binding | pEC50 | = | 10.4 | 10.4 | - | 4 | Activity in mouse melanocortin-1 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-1 receptor stably expressed in HEK293 cells |
ChEMBL | None | None | None | None | 10.1021/jm020296e | ||||
| 16154396 | 302 | None | 19 | Mouse | Binding | pEC50 | = | 10.4 | 10.4 | - | 4 | Activity in mouse melanocortin-1 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-1 receptor stably expressed in HEK293 cells |
ChEMBL | None | None | None | None | 10.1021/jm020296e | ||||
| 16197727 | 302 | None | 19 | Mouse | Binding | pEC50 | = | 10.4 | 10.4 | - | 4 | Activity in mouse melanocortin-1 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-1 receptor stably expressed in HEK293 cells |
ChEMBL | None | None | None | None | 10.1021/jm020296e | ||||
| 16197727.0 | 302 | None | 19 | Mouse | Binding | pEC50 | = | 10.4 | 10.4 | - | 4 | Activity in mouse melanocortin-1 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-1 receptor stably expressed in HEK293 cells |
ChEMBL | None | None | None | None | 10.1021/jm020296e | ||||
| 44285019 | 302 | None | 19 | Mouse | Binding | pEC50 | = | 10.4 | 10.4 | - | 4 | Activity in mouse melanocortin-1 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-1 receptor stably expressed in HEK293 cells |
ChEMBL | None | None | None | None | 10.1021/jm020296e | ||||
| 57514683 | 302 | None | 19 | Mouse | Binding | pEC50 | = | 10.4 | 10.4 | - | 4 | Activity in mouse melanocortin-1 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-1 receptor stably expressed in HEK293 cells |
ChEMBL | None | None | None | None | 10.1021/jm020296e | ||||
| 91898441 | 302 | None | 19 | Mouse | Binding | pEC50 | = | 10.4 | 10.4 | - | 4 | Activity in mouse melanocortin-1 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-1 receptor stably expressed in HEK293 cells |
ChEMBL | None | None | None | None | 10.1021/jm020296e | ||||
| CHEMBL441738 | 302 | None | 19 | Mouse | Binding | pEC50 | = | 10.4 | 10.4 | - | 4 | Activity in mouse melanocortin-1 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-1 receptor stably expressed in HEK293 cells |
ChEMBL | None | None | None | None | 10.1021/jm020296e | ||||
| DB04931 | 302 | None | 19 | Mouse | Binding | pEC50 | = | 10.4 | 10.4 | - | 4 | Activity in mouse melanocortin-1 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-1 receptor stably expressed in HEK293 cells |
ChEMBL | None | None | None | None | 10.1021/jm020296e | ||||
| 1324 | 302 | None | 19 | Mouse | Binding | pEC50 | = | 10.4 | 10.4 | - | 4 | In vitro activation of mouse recombinant Melanocortin-1 receptor.In vitro activation of mouse recombinant Melanocortin-1 receptor. |
ChEMBL | None | None | None | None | 10.1021/jm0104872 | ||||
| 16154396 | 302 | None | 19 | Mouse | Binding | pEC50 | = | 10.4 | 10.4 | - | 4 | In vitro activation of mouse recombinant Melanocortin-1 receptor.In vitro activation of mouse recombinant Melanocortin-1 receptor. |
ChEMBL | None | None | None | None | 10.1021/jm0104872 | ||||
| 16197727 | 302 | None | 19 | Mouse | Binding | pEC50 | = | 10.4 | 10.4 | - | 4 | In vitro activation of mouse recombinant Melanocortin-1 receptor.In vitro activation of mouse recombinant Melanocortin-1 receptor. |
ChEMBL | None | None | None | None | 10.1021/jm0104872 | ||||
| 16197727.0 | 302 | None | 19 | Mouse | Binding | pEC50 | = | 10.4 | 10.4 | - | 4 | In vitro activation of mouse recombinant Melanocortin-1 receptor.In vitro activation of mouse recombinant Melanocortin-1 receptor. |
ChEMBL | None | None | None | None | 10.1021/jm0104872 | ||||
| 44285019 | 302 | None | 19 | Mouse | Binding | pEC50 | = | 10.4 | 10.4 | - | 4 | In vitro activation of mouse recombinant Melanocortin-1 receptor.In vitro activation of mouse recombinant Melanocortin-1 receptor. |
ChEMBL | None | None | None | None | 10.1021/jm0104872 | ||||
| 57514683 | 302 | None | 19 | Mouse | Binding | pEC50 | = | 10.4 | 10.4 | - | 4 | In vitro activation of mouse recombinant Melanocortin-1 receptor.In vitro activation of mouse recombinant Melanocortin-1 receptor. |
ChEMBL | None | None | None | None | 10.1021/jm0104872 | ||||
| 91898441 | 302 | None | 19 | Mouse | Binding | pEC50 | = | 10.4 | 10.4 | - | 4 | In vitro activation of mouse recombinant Melanocortin-1 receptor.In vitro activation of mouse recombinant Melanocortin-1 receptor. |
ChEMBL | None | None | None | None | 10.1021/jm0104872 | ||||
| CHEMBL441738 | 302 | None | 19 | Mouse | Binding | pEC50 | = | 10.4 | 10.4 | - | 4 | In vitro activation of mouse recombinant Melanocortin-1 receptor.In vitro activation of mouse recombinant Melanocortin-1 receptor. |
ChEMBL | None | None | None | None | 10.1021/jm0104872 | ||||
| DB04931 | 302 | None | 19 | Mouse | Binding | pEC50 | = | 10.4 | 10.4 | - | 4 | In vitro activation of mouse recombinant Melanocortin-1 receptor.In vitro activation of mouse recombinant Melanocortin-1 receptor. |
ChEMBL | None | None | None | None | 10.1021/jm0104872 | ||||
| CHEMBL440801 | 216330 | None | 0 | Human | Binding | pEC50 | = | 10.3 | 10.3 | - | 2 | Effective concentration required for the biological activity against human Melanocortin 1 receptorEffective concentration required for the biological activity against human Melanocortin 1 receptor |
ChEMBL | None | None | None | CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(I)cc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC1=O | 10.1021/jm0303103 | ||||
| CHEMBL3350330 | 213931 | None | 0 | Human | Binding | pEC50 | = | 10.2 | 10.2 | - | 0 | Effective concentration for the effect of Melanocortin 1 receptor in the frog skin.Effective concentration for the effect of Melanocortin 1 receptor in the frog skin. |
ChEMBL | None | None | None | CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@@H]([C@@H](C)c2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O | 10.1021/jm00023a012 | ||||
| 16132144 | 211738 | None | 29 | Human | Binding | pEC50 | = | 10.0 | 10.0 | 30 | 4 | Effective concentration required for the biological activity against human Melanocortin 1 receptorEffective concentration required for the biological activity against human Melanocortin 1 receptor |
ChEMBL | None | None | None | CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C | 10.1021/jm0303103 | ||||
| 16133793 | 211738 | None | 29 | Human | Binding | pEC50 | = | 10.0 | 10.0 | 30 | 4 | Effective concentration required for the biological activity against human Melanocortin 1 receptorEffective concentration required for the biological activity against human Melanocortin 1 receptor |
ChEMBL | None | None | None | CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C | 10.1021/jm0303103 | ||||
| 44273719 | 211738 | None | 29 | Human | Binding | pEC50 | = | 10.0 | 10.0 | 30 | 4 | Effective concentration required for the biological activity against human Melanocortin 1 receptorEffective concentration required for the biological activity against human Melanocortin 1 receptor |
ChEMBL | None | None | None | CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C | 10.1021/jm0303103 | ||||
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